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Sample records for strongest inhibitory effect

  1. Transient negative biochar effects on plant growth are strongest after microbial species loss

    NARCIS (Netherlands)

    Hol, (Gera) W.H.G.; Vestergård, M.; Ten Hooven, F.C.; Duyts, H.; Van de Voorde, T.F.J.; Bezemer, T. Martijn

    2017-01-01

    Biochar has been explored as an organic amendment to improve soil quality and benefit plant growth. The overall positive effects of biochar on crop yields are generally attributed to abiotic changes, while the alternative causal pathway via changes in soil biota is unexplored. We compared plant

  2. Seismic effects of the strongest historical earthquak in the Syracuse area

    Directory of Open Access Journals (Sweden)

    D. Mariotti

    1995-06-01

    Full Text Available The effects of earthquakes that occurred in a given area contribute significantly to the evaluation of to local seismic hazard. The information concerning historical earthquakes of the Mediterranean area covers many centuries, but the wealth of information made available by historical seismology does not appear to ha taken into account by engineering seismologists. By adopting "attenuation laws" based on data contained in the seismic catalogues, not only do we sometimes come up against the gross errors normally found jn logues, but we also lose sight of important details relating to the characteristics of urban seismic scenarios this paper we describe the results obtained from the analysis of seismic scenarios in Ortigia (old Syracuse this analysis we emphasized the qualitative and descriptive data to outline the "largest historical eve reassessed the data concerning five earthquakes that occuned in 1169,1542,1693,1757 and 1846, w reported by the Catalogue of Italian Earthquakes with an intensity greater than or equal to IX MCS epicentre of which was located within 50 km of the city. The last two of these earthquakes turned out t result of mistakes in the transmission of the news and have therefore been removed trom the list of de events. In addjtjon, we reconstructed the damage caused by the 1542 and 1693 earthquakes on a ma ancient town of Ortigia, taking into account the economic, demographic, and urbanistic conditions of t The empirical elements supplied to evaluate the local seismic response can also be of use in the preservation of historical buildings.

  3. Inhibitory effects of Ledebouria ovaltifolia (hyacithaceae) aqueous ...

    African Journals Online (AJOL)

    Inhibitory effects of Ledebouria ovaltifolia (hyacithaceae) aqueous root extract on contractile responses of Rat Vas deferens to K and adrenaline, pendular movement of isolated rabbit jejunum and acetic acid induced pain in Mice.

  4. Correlation between enzymes inhibitory effects and antioxidant ...

    African Journals Online (AJOL)

    ... and phytochemical content of fractions was investigated. The n-butanol fraction showed significant α-glucosidase and α-amylase inhibitory effects (IC50 values 15.1 and 39.42 μg/ml, respectively) along with the remarkable antioxidant activity when compared to the other fractions. High performance liquid chromatography ...

  5. Inhibitory Effect of Gamma-Irradiated Chitosan on the Growth of Denitrifiers

    Directory of Open Access Journals (Sweden)

    Javier Vilcáez

    2009-01-01

    Full Text Available In order to find an environmentally benign substitute to hazardous inhibitory agents, the inhibitory effect of -irradiated chitosans against a mixed culture of denitrifying bacteria was experimentally evaluated. Unlike other studies using pure aerobic cultures, the observed effect was not a complete inhibition but a transient inhibition reflected by prolonged lag phases and reduced growth rates. Raw chitosan under acid conditions (pH 6.3 exerted the strongest inhibition followed by the 100 kGy and 500 kGy irradiated chitosans, respectively. Therefore, because the molecular weight of chitosan decreases with the degree of -irradiation, the inhibitory properties of chitosan due to its high molecular weight were more relevant than the inhibitory properties gained due to the modification of the surface charge and/or chemical structure by -irradiation. High dosage of -irradiated appeared to increase the growth of mixed denitrifying bacteria in acid pH media. However, in neutral pH media, high dosage of -irradiation appeared to enhance the inhibitory effect of chitosan.

  6. The Inhibitory Effects of Neem Oil against the Development of ...

    African Journals Online (AJOL)

    Although neem oil extract is widely used in Africa and Asia for the treatment and prevention of malaria, its inhibitory effect on the growth of malaria parasites in vivo has not been fully tested. In the present study, the inhibitory effects of neem oil extract against the growth of rodent malaria parasite in the mice were investigated ...

  7. In vitro evaluation of inhibitory effect of Phoenix dactylifera bark ...

    African Journals Online (AJOL)

    dactylifera bark extract on rat lipid peroxidation and blood hemolysis ... investigate its in vitro inhibitory effects on lipid peroxidation in the brain, liver, and kidney tissues of rat, as well as on blood ... dactylifera L. were 50.7 mg tannic acid, 10.38 mg rutin, and 5.45 mg cyanidin, respectively, while half- maximal inhibitory ...

  8. Inhibitory effects of antimicrobial agents against Fusarium species.

    Science.gov (United States)

    Kawakami, Hideaki; Inuzuka, Hiroko; Hori, Nobuhide; Takahashi, Nobumichi; Ishida, Kyoko; Mochizuki, Kiyofumi; Ohkusu, Kiyofumi; Muraosa, Yasunori; Watanabe, Akira; Kamei, Katsuhiko

    2015-08-01

    We investigated the inhibitory effects of antibacterial, biocidal, and antifungal agents against Fusarium spp. Seven Fusarium spp: four F. falciforme (Fusarium solani species complex), one Fusarium spp, one Fusarium spp. (Fusarium incarnatum-equiseti species complex), and one F. napiforme (Gibberella fujikuroi species complex), isolated from eyes with fungal keratitis were used in this study. Their susceptibility to antibacterial agents: flomoxef, imipenem, gatifloxacin, levofloxacin, moxifloxacin, gentamicin, tobramycin, and Tobracin® (contained 3,000 μg/ml of tobramycin and 25 μg/ml of benzalkonium chloride (BAK), a biocidal agent: BAK, and antifungal agents: amphotericin B, pimaricin (natamycin), fluconazole, itraconazole, miconazole, voriconazole, and micafungin, was determined by broth microdilution tests. The half-maximal inhibitory concentration (IC50), 100% inhibitory concentration (IC100), and minimum inhibitory concentration (MIC) against the Fusarium isolates were determined. BAK had the highest activity against the Fusarium spp. except for the antifungal agents. Three fluoroquinolones and two aminoglycosides had inhibitory effects against the Fusarium spp. at relatively high concentrations. Tobracin® had a higher inhibitory effect against Fusarium spp. than tobramycin alone. Amphotericin B had the highest inhibitory effect against the Fusarium spp, although it had different degrees of activity against each isolate. Our findings showed that fluoroquinolones, aminoglycosides, and BAK had some degree of inhibitory effect against the seven Fusarium isolates, although these agents had considerably lower effect than amphotericin B. However, the inhibitory effects of amphotericin B against the Fusarium spp. varied for the different isolates. Further studies for more effective medications against Fusarium, such as different combinations of antibacterial, biocidal, and antifungal agents are needed. © The Author 2015. Published by Oxford University Press on

  9. Inhibitory effect of 5-iodotubercidin on pigmentation.

    Science.gov (United States)

    Kim, Kyung-Il; Jeong, Hae Bong; Ro, Hyunju; Lee, Jeung-Hoon; Kim, Chang Deok; Yoon, Tae-Jin

    2017-09-02

    Melanin pigments are the primary contributors for the skin color. They are produced in melanocytes and then transferred to keratinocytes, eventually giving various colors on skin surface. Although many depigmenting and/or skin-lightening agents have been developed, there is still a growing demand on materials for reducing pigmentation. We attempted to find materials for depigmentation and/or skin-lightening using the small molecule compounds commercially available, and found that 5-iodotubercidin had inhibitory potential on pigmentation. When HM3KO melanoma cells were treated with 5-iodotubercidin, pigmentation was dramatically reduced. The 5-iodotubercidin decreased the protein level for pigmentation-related molecules such as MITF, tyrosinase, and TRP1. In addition, 5-iodotubercidin decreased the phosphorylation of CREB, while increased the phosphorylation of AKT and ERK. These data suggest that 5-iodotubercidin inhibits melanogenesis via the regulation of intracellular signaling related with pigmentation. Finally, 5-iodotubercidin markedly inhibited the melanogenesis of zebrafish embryos, an in vivo evaluation model for pigmentation. Together, these data suggest that 5-iodotubercidin can be developed as a depigmenting and/or skin-lightening agent. Copyright © 2017 Elsevier Inc. All rights reserved.

  10. A study on the inhibitory effect of polysaccharides from Radix ...

    African Journals Online (AJOL)

    Different concentrations of polysaccharide extracts were selected, and MTT assay and flow cytometry (FCM) were used to investigate their growth-inhibitory and apoptosis-inducing effects on human breast cancer MCF-7 cell lines. Radix ranunculus ternati polysaccharides had varying degrees of effects on the growth of ...

  11. The Acute Effects of Exercise Intensity on Inhibitory Cognitive Control in Adolescents

    Directory of Open Access Journals (Sweden)

    Fernando Peruyero

    2017-05-01

    Full Text Available Adolescence is an important stage for brain maturation. There are many studies of exercise-cognition relations, but there is still a lack of knowledge about the impact of combining different intensities of exercise on adolescents’ cognitive responses. The main objective of this study was to analyze the effect of three physical education sessions (based on Zumba dance of different intensities (no exercise, predominantly light intensity, and predominantly vigorous intensity on the inhibition response (measured with the Stroop test in adolescents. Forty-four adolescent students (age 16.39 ± 0.68 completed a Stroop test before and after the three different physical education sessions. The results show than the predominantly vigorous session represented the strongest stimulus to increase cognitive inhibitory control. This means that the cognitive effect of exercise can be conditioned by exercise intensity and implies the need to control exercise intensity in physical educational programs for adolescents.

  12. The strongest magnetic fields in the universe

    CERN Document Server

    Balogh, A; Falanga, M; Lyutikov, M; Mereghetti, S; Piran, T; Treumann, RA

    2016-01-01

    This volume extends the ISSI series on magnetic fields in the Universe into the domain of what are by far the strongest fields in the Universe, and stronger than any field that could be produced on Earth. The chapters describe the magnetic fields in non-degenerate strongly magnetized stars, degenerate stars (such as white dwarfs and neutron stars), exotic members called magnetars, and in their environments, as well as magnetic fields in the environments of black holes. These strong fields have a profound effect on the behavior of matter, visible in particular in highly variable processes like radiation in all known wavelengths, including Gamma-Ray bursts. The generation and structure of such strong magnetic fields and effects on the environment are also described.

  13. Inhibitory effects of copper on marine dinoflagellates

    Energy Technology Data Exchange (ETDEWEB)

    Saifullah, S.M.

    1978-01-01

    The effect of copper on three species of marine dinoflagellates (Scrippsiella faeroense (Paulsen) Balech et Soares, Prorocentrum micans Ehrenberg, Gymnodinium splendens Lebour) was studied. It inhibited the growth of all species and was lethal to one species in batch cultures. The effect was more pronounced in semicontinuous culture than in batch cultures. Chlorophyll concentrations and rate of uptake of radioactive carbon by cells of S. faeroense were affected in a manner similar to cell numbers. Copper inhibited growth of cells, most probably either by arresting cell division or by penetrating inside the cell and affecting metabolism.

  14. Effect of partially purified angiotensin converting enzyme inhibitory ...

    African Journals Online (AJOL)

    This study evaluated the effect of partially-purified angiotensin converting enzyme (ACE) inhibitory proteins obtained from the leaves of Moringa oleifera on blood glucose, serum ACE activity and lipid profile of alloxaninduced diabetic rats. Twenty-five apparently healthy male albino rats were divided into five groups of five ...

  15. Experimental study on the inhibitory effect of sodium cantharidinate ...

    African Journals Online (AJOL)

    Backgroud: Cantharidin, and its derivatives can not only inhibit the proliferation of tumor cells, but can also induce tumor cell apoptosis. It shows cantharidin exhibits a wide range of reactivity in anticancer. The objective of this paper was to study the inhibitory effect of sodium cantharidinate on human hepatoma HepG2 cells.

  16. Inhibitory Effects of Various Ratios of Polysaccharides/Alkaloids from ...

    African Journals Online (AJOL)

    Purpose: To investigate the inhibitory effects of various ratios of polysaccharides/ alkaloids from the rhizome of Coptis chinensis Franch (RCC) on α-glucosidase. Methods: The polysaccharides (PSD) and alkaloids (ALK) from RCC were prepared using the water extraction and alcohol precipitation method and Reinecke's ...

  17. Inhibitory effects of (-)-epigallocatechin-3-gallate on melanogenesis ...

    African Journals Online (AJOL)

    Inhibitory effects of (-)-epigallocatechin-3-gallate on melanogenesis in ultraviolet A-induced B16 murine melanoma cell. ... of TRY activity and melanosome maturation and is thus a potential alternative to melanogenesis inhibitor. Keywords: Green tea, Catechins, Melanin, Melanosome, Tyrosinase, Cell proliferation ...

  18. Inhibitory effect of chitosan oligosaccharide on human hepatoma ...

    African Journals Online (AJOL)

    Background: Chitosan oligosaccharide, the degradation products of chitin, was reported to have a wide range of physiological functions and biological activities. In this study, we explored the inhibitory effect of Chitosan oligosaccharide on human hepatoma cells. Materials and Methods: MTT assay was applied to detect cell ...

  19. In Vitro Anticholinesterase and Inhibitory Effects of the Aqueous ...

    African Journals Online (AJOL)

    Methods: The aqueous extract of Combretum molle and an anti-asthmatic, salbutamol (reference), were tested at varying concentrations for their inhibitory effects on breathing. Acetylcholinesterase (AChE) was extracted from rabbit duodenum and its activity determined by Ellman's assay using acethylthiocholine iodide ...

  20. Inhibitory Effect of Polysaccharides from Scutellaria barbata D. Don ...

    African Journals Online (AJOL)

    Purpose: To investigate the inhibitory effect of polysaccharides from Scutellaria barbata (PSB) on invasion and metastasis of lung cancer, and study the possible mechanism. Methods: PSB was extracted with water and by alcohol precipitation, and purified by DEAE-52 column chromatography. A highly invasive and ...

  1. Facilitatory and inhibitory effects of Kinesio tape: Fact or fad?

    Science.gov (United States)

    Cai, C; Au, I P H; An, W; Cheung, R T H

    2016-02-01

    Kinesio tape (KT) is a commonly used intervention in sports. It claims to be able to alter the muscle activity, in terms of both facilitation and inhibition, by certain application methods. This study compared the neuromuscular activity of the wrist extensor muscles and maximal grip strength with facilitatory, inhibitory KT, and tapeless condition in healthy adults who were ignorant about KT. Potential placebo effects were eliminated by deception. Randomized deceptive trial. 33 participants performed maximal grip assessment in a randomly assigned order of three taping conditions: true facilitatory KT, inhibitory KT, and no tape. The participants were blindfolded during the evaluation. Under the pretense of applying a series of adhesive muscle sensors, KT was applied to their wrist extensor muscles of the dominant forearm in the first two conditions. Within-subject comparisons of normalized root mean square of the wrist extensors electromyographic activity and maximal grip strength were conducted across three taping conditions. 31 out of 33 enlisted participants were confirmed to be ignorant about KT. No significant differences were found in the maximum grip strength (p=0.394), electromyographic activity (p=0.276), and self-perceived performance (p=0.825) between facilitatory KT, inhibitory KT, and tapeless conditions. Neither facilitatory nor inhibitory effects were observed between different application techniques of KT in healthy participants. Clinically, alternative method should be used for muscle activity modulation. Copyright © 2015 Sports Medicine Australia. Published by Elsevier Ltd. All rights reserved.

  2. The α-amylase and α-glucosidase inhibitory effects of Irish seaweed extracts.

    Science.gov (United States)

    Lordan, Sinéad; Smyth, Thomas J; Soler-Vila, Anna; Stanton, Catherine; Ross, R Paul

    2013-12-01

    To date, numerous studies have reported on the antidiabetic properties of various plant extracts through inhibition of carbohydrate-hydrolysing enzymes. The objective of this research was to evaluate extracts of seaweeds for α-amylase and α-glucosidase inhibitory effects. Cold water and ethanol extracts of 15 seaweeds were initially screened and from this, five brown seaweed species were chosen. The cold water and ethanol extracts of Ascophyllum nodosum had the strongest α-amylase inhibitory effect with IC50 values of 53.6 and 44.7 μg/ml, respectively. Moreover, the extracts of Fucus vesiculosus Linnaeus were found to be potent inhibitors of α-glucosidase with IC50 values of 0.32 and 0.49 μg/ml. The observed effects were associated with the phenolic content and antioxidant activity of the extracts, and the concentrations used were below cytotoxic levels. Overall, our findings suggest that brown seaweed extracts may limit the release of simple sugars from the gut and thereby alleviate postprandial hyperglycaemia. Copyright © 2013. Published by Elsevier Ltd.

  3. Inhibitory effects of triterpenes and flavonoids on the enzymatic activity of hyaluronic acid-splitting enzymes.

    Science.gov (United States)

    Hertel, Waltraud; Peschel, Gundela; Ozegowski, Jörg-Hermann; Müller, Peter-Jürgen

    2006-06-01

    The effect of triterpenes and flavonoids on the activity of several hyaluronic acid-splitting enzymes was investigated. Studies showed that the inhibitory effect of the triterpenes glycyrrhizin and glycyrrhetinic acid is dependent on the source of hyaluronate lyase. Hyaluronate lyase from Streptococcus agalactiae (Hyal B) and recombinant hyaluronate lyase from Streptococcus agalactiae (rHyal B) demonstrated strongest inhibition. In contrast, hyaluronate lyases from Streptomyces hyalurolyticus (Hyal S), Streptococcus equisimilis (Hyal C) and hyaluronidase from bovine testis (Dase) showed only reduced inhibition action. A non-competitive dead end inhibition with Ki=3.1+/-1.8x10(-6) mol/mL and Kii=6.7+/-2.4x10(-6) mol/mL was found for glycyrrhizin on recombinant hyaluronate lyase from Streptococcus agalactiae. The inhibitory effect of flavonoids on Hyal B, rHyal B and Dase was determined depending on the number of hydroxyl groups and side chain substituents in the molecule. Flavonoids with many hydroxyl groups inhibited hyaluronate lyase stronger than those with only a few. Native hyaluronate lyase (Hyal B) showed a more extensive inhibition than the recombinant protein (rHyal B). Accordingly, the inhibition by triterpenes and flavonoids is presumably specific for each hyaluronic acid (HA)-splitting enzyme.

  4. Inhibitory effects of acetylsalicylic acid on exocrine pancreatic carcinogenesis.

    Science.gov (United States)

    Yıldız, H; Oztas, H; Yıldız, D; Koc, A; Kalipci, E

    2013-05-01

    We investigated short (6 months) and long (12 months) term inhibitory effects of low (200 ppm) and high (400 ppm) dosages of acetylsalicylic acid (aspirin) on exocrine pancreatic carcinogenesis. It is known that exocrine pancreatic carcinogenesis can be detected by the presence of atypical acinar cell foci (AACF) in pancreas. We investigated possible inhibitory effects of acetylsalicylic acid in an azaserine-treated rat model. AACF were produced in rats by injection with azaserine according to previous studies. Our findings showed that the number, volume and diameter of pancreatic AACF were reduced after acetylsalicylic acid application. These observations suggest that acetylsalicylic acid may exert a protective effect against neoplastic development of pancreatic acinar cells in azaserine injected rats. Our findings corroborate reports in the literature concerning the effects of aspirin in reducing neoplastic development.

  5. Inhibitory Effects of Glycyrrhetinic Acid on DNA Polymerase and Inflammatory Activities

    Directory of Open Access Journals (Sweden)

    Tsukasa Ishida

    2012-01-01

    Full Text Available We investigated the inhibitory effect of three glycyrrhizin derivatives, such as Glycyrrhizin (compound 1, dipotassium glycyrrhizate (compound 2 and glycyrrhetinic acid (compound 3, on the activity of mammalian pols. Among these derivatives, compound 3 was the strongest inhibitor of mammalian pols α, β, κ, and λ, which belong to the B, A, Y, and X families of pols, respectively, whereas compounds 1 and 2 showed moderate inhibition. Among the these derivatives tested, compound 3 displayed strongest suppression of the production of tumor necrosis factor-α (TNF-α induced by lipopolysaccharide (LPS in a cell-culture system using mouse macrophages RAW264.7 and peritoneal macrophages derived from mice. Moreover, compound 3 was found to inhibit the action of nuclear factor-κB (NF-κB in engineered human embryonic kidney (HEK 293 cells. In addition, compound 3 caused greater reduction of 12-O-tetradecanoylphorbol-13-acetate-(TPA- induced acute inflammation in mouse ear than compounds 1 and 2. In conclusion, this study has identified compound 3, which is the aglycone of compounds 1 and 2, as a promising anti-inflammatory candidate based on mammalian pol inhibition.

  6. Inhibitory Effects of 5,6,7-Trihydroxyflavones on Tyrosinase

    Directory of Open Access Journals (Sweden)

    Jun Kawabata

    2007-01-01

    Full Text Available Baicalein (1, 6-hydroxyapigenin (6, 6-hydroxygalangin (13 and 6-hydroxy-kaempferol (14, which are naturally occurring flavonoids from a set of 14 hydroxy-flavones tested, exhibited high inhibitory effects on tyrosinase with respect to L-DOPA,while each of the 5,6,7-trihydroxyflavones 1, 6, 13 or 14 acted as a cofactor tomonophenolase. Moreover, 6-hydroxykaempferol (14 showed the highest activity andwas a competitive inhibitor of tyrosinase compared to L-DOPA. 5,6,7-Trihydroxyflavones 1, 6, 13 or 14 showed also high antioxidant activities. Hence, weconclude that the 5,6,7-trihydroxy-flavones are useful as good depigmentation agentswith inhibitory effects in addition to their antioxidant properties.

  7. Inhibitory Effects of Megakaryocytes in Prostate Cancer Bone Metastasis

    Science.gov (United States)

    2010-04-01

    subcutaneous implants and bone lesions. 6 3) The expression of caspase-3 was not significant increased in PC-3 cells after co- culture with K562 cel...Investigator Award, IX International Meeting on Cancer Induced Bone Disease , Nov. 2009, Arlington, VA) 4. Inhibitory effects of megakaryocytes in prostate...Corresponding author: Laurie K. McCauley, DDS, PhD William K. and Mary Anne Najjar Professor Professor and Chair Department of Periodontics and Oral

  8. Inhibitory Effect of Polysaccharides from Scutellaria barbata D. Don ...

    African Journals Online (AJOL)

    Available online at http://www.tjpr.org http://dx.doi.org/10.4314/tjpr.v12i4.11. Original Research Article. Inhibitory Effect of Polysaccharides from Scutellaria barbata D. Don on Invasion and Metastasis of 95-D Cells. Lines via Regulation of C-MET and E-CAD Expressions. Xiao-Kun Yang1,2, Ya-Dong Yang1, Shu-Qian Tang1, ...

  9. C-Methylated Flavonoids from Cleistocalyx operculatus and Their Inhibitory Effects on Novel Influenza A (H1N1) Neuraminidase

    DEFF Research Database (Denmark)

    Dao, Trong-Tuan; Tung, Bui-Thanh; Nguyen, Phi-Hung

    2010-01-01

    As part of an ongoing study focused on the discovery of anti-influenza agents from plants, four new (1-4) and 10 known (5-14) C-methylated flavonoids were isolated from a methanol extract of Cleistocalyx operculatus buds using an influenza H1N1 neuraminidase inhibition assay. Compounds 4, 7, 8......, and 14, with a chalcone skeleton, showed significant inhibitory effects on the viral neuraminidases from two influenza viral strains, H1N1 and H9N2. Compound 4 showed the strongest inhibitory activity against the neuraminidases from novel influenza H1N1 (WT) and oseltamivir-resistant novel H1N1 (H274Y...

  10. Catalytic and inhibitory effects of thechnetium on reduction processes

    International Nuclear Information System (INIS)

    Grases, F.; Genestar, C.; March, J.G.; March, P.

    1986-01-01

    Interactions between technetium and some anthraquinones and tartrazin in the presence of tin(II) are described. It was found that whereas the reductive process between Sn(II) and 1-amino-4-hydroxyanthraquinone is catalyzed by technetium, the reduction of tartrazin is inhibited by this element. Study of such process seems to indicate that the catalytic effect of technetium on the reduction processes is due to Tc(V) action whereas the inhibitory effect is due to the Tc(IV) species. (author)

  11. Syllable Frequency and Spoken Word Recognition: An Inhibitory Effect.

    Science.gov (United States)

    González-Alvarez, Julio; Palomar-García, María-Angeles

    2016-08-01

    Research has shown that syllables play a relevant role in lexical access in Spanish, a shallow language with a transparent syllabic structure. Syllable frequency has been shown to have an inhibitory effect on visual word recognition in Spanish. However, no study has examined the syllable frequency effect on spoken word recognition. The present study tested the effect of the frequency of the first syllable on recognition of spoken Spanish words. A sample of 45 young adults (33 women, 12 men; M = 20.4, SD = 2.8; college students) performed an auditory lexical decision on 128 Spanish disyllabic words and 128 disyllabic nonwords. Words were selected so that lexical and first syllable frequency were manipulated in a within-subject 2 × 2 design, and six additional independent variables were controlled: token positional frequency of the second syllable, number of phonemes, position of lexical stress, number of phonological neighbors, number of phonological neighbors that have higher frequencies than the word, and acoustical durations measured in milliseconds. Decision latencies and error rates were submitted to linear mixed models analysis. Results showed a typical facilitatory effect of the lexical frequency and, importantly, an inhibitory effect of the first syllable frequency on reaction times and error rates. © The Author(s) 2016.

  12. Assessment of the inhibitory effects of pyrethroids against human carboxylesterases.

    Science.gov (United States)

    Lei, Wei; Wang, Dan-Dan; Dou, Tong-Yi; Hou, Jie; Feng, Liang; Yin, Heng; Luo, Qun; Sun, Jie; Ge, Guang-Bo; Yang, Ling

    2017-04-15

    Pyrethroids are broad-spectrum insecticides that widely used in many countries, while humans may be exposed to these toxins by drinking or eating pesticide-contaminated foods. This study aimed to investigate the inhibitory effects of six commonly used pyrethroids against two major human carboxylesterases (CES) including CES1 and CES2. Three optical probe substrates for CES1 (DME, BMBT and DMCB) and a fluorescent probe substrate for CES2 (DDAB) were used to characterize the inhibitory effects of these pyrethroids. The results demonstrated that most of the tested pyrethroids showed moderate to weak inhibitory effects against both CES1 and CES2, but deltamethrin displayed strong inhibition towards CES1. The IC 50 values of deltamethrin against CES1-mediated BMBT, DME, and DMCB hydrolysis were determined as 1.58μM, 2.39μM, and 3.3μM, respectively. Moreover, deltamethrin was cell membrane permeable and capable of inhibition endogenous CES1 in living cells. Further investigation revealed that deltamethrin inhibited CES1-mediated BMBT hydrolysis via competitive manner but noncompetitively inhibited DME or DMCB hydrolysis. The inhibition behaviors of deltamethrin against CES1 were also studied by molecular docking simulation. The results demonstrated that CES1 had at least two different ligand-binding sites, one was the DME site and another was the BMBT site which was identical to the binding site of deltamethrin. In summary, deltamethrin was a strong reversible inhibitor against CES1 and it could tightly bind on CES1 at the same ligand-binding site as BMBT. These findings are helpful for the deep understanding of the interactions between xenobiotics and CES1. Copyright © 2017 Elsevier Inc. All rights reserved.

  13. Inhibitory effects of monoterpenes on seed germination and seedling growth.

    Science.gov (United States)

    Kordali, Saban; Cakir, Ahmet; Sutay, Sunay

    2007-01-01

    Monoterpenes, the chemical constituents of essential oils found in plants, are known biologically active compounds. The present study was conducted to investigate the inhibitory effects of 30 monoterpenes including monoterpene hydrocarbons and oxygenated monoterpenes on seed germination and seedling growth of Amaranthus retroflexus, Chenopodium album and Rumex crispus under laboratory conditions. The monoterpenes were applied at contents of 10 and 20 microl for liquid compounds and 10 and 20 microg for solid compounds. The results show that most of the monoterpenes significantly inhibited seed germination and seedling growth of the tested plants. Oxygenated monoterpenes including beta-citronellol, nerol and terpinen-4-ol completely inhibited seed germination and seedling growth of all tested plants. Their inhibitory effects were also stronger than that of the herbicide 2,4-D. In general, monoterpenes were less effective against seed germination and seedling growth of C. album as compared with R. crispus and A. retroflexus. Phytotoxic effects of monoterpene hydrocarbons were found to be lower than those of oxygenated monoterpenes. The alcohol derivatives of oxygenated monoterpenes were also found to be more phytotoxic as compared with their acetate derivatives. Based on the present results, it can be concluded that the oxygenated monoterpenes can be used as potential bio-herbicides.

  14. Inhibitory Effect of Lactococcus lactis HY 449 on Cariogenic Biofilm.

    Science.gov (United States)

    Kim, Young-Jae; Lee, Sung-Hoon

    2016-11-28

    Dental caries is caused by cariogenic biofilm, an oral biofilm including Streptococcus mutans . Recently, the prevention of dental caries using various probiotics has been attempted. Lactococcus lactis HY 449 is a probiotic bacterium. The aim of this study was to investigate the effect of L. lactis HY 449 on cariogenic biofilm and to analyze its inhibitory mechanisms. Cariogenic biofilm was formed in the presence or absence of L. lactis HY 449 and L. lactis ATCC 19435, and analyzed with a confocal laser microscope. The formation of cariogenic biofilm was reduced in cultures spiked with both L. lactis strains, and L. lactis HY 449 exhibited more inhibitory effects than L. lactis ATCC 19435. In order to analyze and to compare the inhibitory mechanisms, the antibacterial activity of the spent culture medium from both L. lactis strains against S. mutans was investigated, and the expression of glucosyltransferases ( gtfs ) of S. mutans was then analyzed by real-time RT-PCR. In addition, the sucrose fermentation ability of both L. lactis strains was examined. Both L. lactis strains showed antibacterial activity and inhibited the expression of gtfs , and the difference between both strains did not show. In the case of sucrose-fermenting ability, L. lactis HY 449 fermented sucrose but L. lactis ATCC 19435 did not. L. lactis HY 449 inhibited the uptake of sucrose and the gtfs expression of S. mutans , whereby the development of cariogenic biofilm may be inhibited. In conclusion, L. lactis HY 449 may be a useful probiotic for the prevention of dental caries.

  15. Inhibitory Effect of Flavonolignans on the P2Y12 Pathway in Blood Platelets.

    Science.gov (United States)

    Bijak, Michal; Szelenberger, Rafal; Dziedzic, Angela; Saluk-Bijak, Joanna

    2018-02-10

    Adenosine diphosphate (ADP) is the major platelet agonist, which is important in the shape changes, stability, and growth of the thrombus. Platelet activation by ADP is associated with the G protein-coupled receptors P2Y1 and P2Y12. The pharmacologic blockade of the P2Y12 receptor significantly reduces the risk of peripheral artery disease, myocardial infarction, ischemic stroke, and vascular death. Recent studies demonstrated the inhibition of ADP-induced blood platelet activation by three major compounds of the flavonolignans group: silybin, silychristin, and silydianin. For this reason, the aim of the current work was to verify the effects of silybin, silychristin, and silydianin on ADP-induced physiological platelets responses, as well as mechanisms of P2Y12-dependent intracellular signal transduction. We evaluated the effect of tested flavonolignans on ADP-induced blood platelets' aggregation in platelet-rich plasma (PRP) (using light transmission aggregometry), adhesion to fibrinogen (using the static method), and the secretion of PF-4 (using the ELISA method). Additionally, using the double labeled flow cytometry method, we estimated platelet vasodilator-stimulated phosphoprotein (VASP) phosphorylation. We demonstrated a dose-dependent reduction of blood platelets' ability to perform ADP-induced aggregation, adhere to fibrinogen, and secrete PF-4 in samples treated with flavonolignans. Additionally, we observed that all of the tested flavonolignans were able to increase VASP phosphorylation in blood platelets samples, which is correlated with P2Y12 receptor inhibition. All of these analyses show that silychristin and silybin have the strongest inhibitory effect on blood platelet activation by ADP, while silydianin also inhibits the ADP pathway, but to a lesser extent. The results obtained in this study clearly demonstrate that silybin, silychristin, and silydianin have inhibitory properties against the P2Y12 receptor and block ADP-induced blood platelet

  16. Inhibitory effect of Lactobacillus reuteri on periodontopathic and cariogenic bacteria.

    Science.gov (United States)

    Kang, Mi-Sun; Oh, Jong-Suk; Lee, Hyun-Chul; Lim, Hoi-Soon; Lee, Seok-Woo; Yang, Kyu-Ho; Choi, Nam-Ki; Kim, Seon-Mi

    2011-04-01

    The interaction between Lactobacillus reuteri, a probiotic bacterium, and oral pathogenic bacteria have not been studied adequately. This study examined the effects of L. reuteri on the proliferation of periodontopathic bacteria including Aggregatibacter actinomycetemcomitans, Fusobacterium nucleatum, Porphyromonas gingivalis, and Tannerella forsythia, and on the formation of Streptococcus mutans biofilms. Human-derived L. reuteri strains (KCTC 3594 and KCTC 3678) and rat-derived L. reuteri KCTC 3679 were used. All strains exhibited significant inhibitory effects on the growth of periodontopathic bacteria and the formation of S. mutans biofilms. These antibacterial activities of L. reuteri were attributed to the production of organic acids, hydrogen peroxide, and a bacteriocin-like compound. Reuterin, an antimicrobial factor, was produced only by L. reuteri KCTC 3594. In addition, L. reuteri inhibited the production of methyl mercaptan by F. nucleatum and P. gingivalis. Overall, these results suggest that L. reuteri may be useful as a probiotic agent for improving oral health.

  17. Inhibitory effect of alpha-mangostin on Candida biofilms.

    Science.gov (United States)

    Kaomongkolgit, Ruchadaporn; Jamdee, Kusuma

    2017-04-01

    The objective of this study was to determine the inhibitory effect of alpha-mangostin on Candida biofilms. Candida species including Candida albicans, Candida krusei, Candida tropicalis, and Candida glabrata were tested. Candida biofilms were formed in flat-bottomed 96-well microtiter plates. The metabolic activity of cells within biofilms was quantified using the XTT assay. The results demonstrated that alpha-mangostin showed a significant anti-biofilm effect on both developing biofilms and preformed biofilms of Candida species. It may be concluded that alpha-mangostin could be an anti-biofilm agent against Candida species. Further in vivo investigations are needed to uncover the therapeutic values of this medicinal plant.

  18. Inhibitory effects of β-caryophyllene on Streptococcus mutans biofilm.

    Science.gov (United States)

    Yoo, Hyun-Jun; Jwa, Su-Kyung

    2018-04-01

    The biofilm of Streptococcus mutans is associated with induction of dental caries. Also, they produce glucan as an extracellular polysaccharide through glucosyltransferases and help the formation of cariogenic biofilm. β-caryophyllene has been used for therapeutic agent in traditional medicine and has antimicrobial activity. The purpose of this study was to investigate the effect of β-caryophyllene on S. mutans biofilm and the expression of biofilm-related factor. The susceptibility assay of S. mutans for β-caryophyllene was performed to investigate inhibitory concentration for S. mutans growth. To evaluated the effect of β-caryophyllene on S. mutans biofilm, β-caryophyllene was treated on S. mutans in the various concentrations before or after the biofilm formation. Live S. mutans in the biofilm was counted by inoculating on Mitis-salivarius agar plate, and S. mutans biofilm was analyzed by confocal laser scanning microscope after staining bacterial live/dead staining kit. Finally, the expression of glucosyltransferases of S. mutans was investigated by real-time RT-PCR after treating with β-caryophyllene at the non-killing concentration of S. mutans. The growth of S. mutans was inhibited by β-caryophyllene in above concentration of 0.078%, S. mutans biofilm was inhibited by β-caryophyllene in above 0.32%. Also, 2.5% of β-caryophyllene showed anti-biofilm activity for S. mutans biofilm. β-caryophyllene reduced the expression of gtf genes at a non-killing concentration for S. mutans. On the basis on these results, β-caryophyllene may have anti-biofilm activity and the inhibitory effect on biofilm related factor. β-caryophyllene may inhibit cariogenic biofilm and may be a candidate agent for prevention of dental caries. Copyright © 2018. Published by Elsevier Ltd.

  19. Inhibitory effect of verbascoside on xanthine oxidase activity.

    Science.gov (United States)

    Wan, Yin; Zou, Bin; Zeng, Hailong; Zhang, Lunning; Chen, Ming; Fu, Guiming

    2016-12-01

    In this study, we analyzed the inhibitory effect of verbascoside against xanthine oxidase (XOD) in vitro by using animal model and in vivo by direct inhibition assay. Results showed that verbascoside could reduce uric acid in rat serum and inhibit XOD activity in rat liver. The IC 50 value of restraining XOD activity was 81.11mgmL -1 . Fluorescence chromatographic analysis and circular dichroism spectroscopy indicated that the secondary structures of XOD were changed after incubation with verbascoside. The docking simulation showed that verbascoside could enter into the active site of XOD and form hydrogen bonding with amino acid residues (such as Lys-1045, Arg-880, Arg-912, Glu-1261 and Gln-1194). The results suggested that verbascoside, which is a naturally occurring water-soluble antioxidant, could be a potential low-toxicity XOD inhibitor for hyperuricemia treatment. Copyright © 2016 Elsevier B.V. All rights reserved.

  20. Inhibitory effects of seaweed extracts on the growth of the vaginal bacterium Gardnerella vaginalis.

    Science.gov (United States)

    Ha, Yu-Mi; Choi, Jae-Suk; Lee, Bo-Bae; Moon, Hye Eun; Cho, Kwang Keun; Choi, In Soon

    2014-05-01

    Of 44 species of seaweed screened for potential anti-Gardnerella vaginalis activity, 27 (61.4%) showed antimicrobial activity by the agar disk-diffusion method. Among them, the strongest activities against the pathogen were exhibited by Chlorophyta, with Ulva pertusa producing an 11.3-mm zone of inhibition at 5 mg disk⁻¹. The MIC values of U. pertusa extracts against both G. vaginalis KCTC 5096 and KCTC 5097, the main cause of vaginosis, were 312 μg ml⁻¹, while the MIC values against both Candida albicans KCTC 7270 and KCTC 7965, the main cause of candidiasis, were 2.5 mg ml⁻¹. Against Lactobacillus gasseri KCTC 3173 and Lactobacillus jensenii KCTC 5194, members of the normal vaginal microflora, no inhibitory effect was seen even at 10 mg ml⁻¹. To identify the primary active compounds, a U. pertusa powder was successively fractionated according to polarity, and the main active agents against G. vaginalis KCTC 5096 were determined to be nitrogenous compounds (156 μg ml⁻¹ of the MIC value). According to these results, it was suggested that extracts of the seaweed U. pertusa are valuable for the development of natural therapeutic agents for treating women with bacterial vaginosis.

  1. Inhibitory effect of common microfluidic materials on PCR outcome

    KAUST Repository

    Kodzius, Rimantas

    2013-10-10

    In this study, we established a simple method for evaluating the PCR compatibility of various common materials employed when fabricating microfluidic chips, including silicon, several kinds of silicon oxide, glasses, plastics, wax, and adhesives. Two-temperature PCR was performed with these materials to determine their PCR-inhibitory effect. In most cases, adding bovine serum albumin effectively improved the reaction yield. We also studied the individual PCR components from the standpoint of adsorption. Most of the materials did not inhibit the DNA, although they noticeably interacted with the polymerase. We provide a simple method of performing PCR-compatibility testing of materials using inexpensive instrumentation that is common in molecular biology laboratories. Furthermore, our method is direct, being performed under actual PCR conditions with high temperature. Our results provide an overview of materials that are PCR-friendly for fabricating microfluidic devices. The PCR reaction, without any additives, performed best with pyrex glass, and it performed worst with PMMA or acrylic glue materials.

  2. Inhibitory Effect of Natural Phenolic Compounds on Aspergillus parasiticus Growth

    Directory of Open Access Journals (Sweden)

    Romina P. Pizzolitto

    2015-01-01

    Full Text Available Considering the impact of Aspergillus species on crops, it appears to be highly desirable to apply strategies to prevent their growth, as well as to eliminate or reduce their presence in food products. For this reason, the aims of this investigation were to evaluate the effects of ten natural phenolic compounds on the Aspergillus parasiticus growth and to determine which physicochemical properties are involved in the antifungal activity. According to the results of minimum inhibitory concentration (MIC values of the individual compounds, isoeugenol, carvacrol, and thymol were the most active phenolic components (1.26 mM, 1.47 mM, and 1.50 mM, resp., followed by eugenol (2.23 mM. On the other hand, creosol, p-cresol, o-cresol, m-cresol, vanillin, and phenol had no effects on fungal development. Logarithm of the octanol/water partition coefficient (log P, refractivity index (RI, and molar volume (MV were demonstrated to be the descriptors that best explained the antifungal activity correlated to lipophilicity, reactivity of the components, and steric aspect. These findings make an important contribution to the search for new compounds with antifungal activity.

  3. The Strongest Magnetic Field in Sunspots

    Science.gov (United States)

    Okamoto, J.; Sakurai, T.

    2017-12-01

    Sunspots are concentrations of magnetic fields on the solar surface. Generally, the strongest magnetic field in each sunspot is located in the dark umbra in most cases. A typical field strength in sunspots is around 3,000 G. On the other hand, some exceptions also have been found in complex sunspots with bright regions such as light bridges that separate opposite polarity umbrae, for instance with a strength of 4,300 G. However, the formation mechanism of such strong fields outside umbrae is still puzzling. Here we report an extremely strong magnetic field in a sunspot, which was located in a bright region sandwiched by two opposite-polarity umbrae. The strength is 6,250 G, which is the largest ever observed since the discovery of magnetic field on the Sun in 1908 by Hale. We obtained 31 scanned maps of the active region observed by Hinode/SOT/SP with a cadence of 3 hours over 5 days (February 1-6, 2014). Considering the spatial and temporal evolution of the vector magnetic field and the Doppler velocity in the bright region, we suggested that this strong field region was generated as a result of compression of one umbra pushed by the outward flow from the other umbra (Evershed flow), like the subduction of the Earth's crust in plate tectonics.

  4. Inhibitory effect of anethole in nonimmune acute inflammation.

    Science.gov (United States)

    Domiciano, Talita Perdigão; Dalalio, Márcia Machado de Oliveira; Silva, Expedito Leite; Ritter, Alessandra Mileni Versuti; Estevão-Silva, Camila Fernanda; Ramos, Fernando Seara; Caparroz-Assef, Silvana Martins; Cuman, Roberto Kenji Nakamura; Bersani-Amado, Ciomar Aparecida

    2013-04-01

    Anethole [1-methoxy-4-(1-propenyl)benzene] occurs naturally as a major component of the essential oil of star anise (Illicium verum Hook.f., family Illiciaceae), comprising more than 90 % of its volatile components. Studies showed that this substance has antioxidant, antibacterial, antifungal, and anesthetic properties. In this study, the anti-inflammatory properties of anethole in animal models of nonimmune acute inflammation such as croton oil-induced ear edema and carrageenan-induced pleurisy were investigated. The investigated parameters were edema formation, leukocyte migration, and inflammatory mediators involved. Oral administration of anethole at a dose of 250 and 500 mg/kg reduced both the volume of pleural exudates and the number of migrated leukocytes. Levels of nitric oxide (NO) and prostaglandins (PGE2) in the inflammatory exudate were reduced by treatment with anethole, but levels of tumor necrosis factor-α and interleukin-1β were not significantly altered. In ear edema, the oral treatment with anethole inhibited the formation of exudate and the activity of myeloperoxidase, but not after topical administration. These results suggest that the anethole may be effective in controlling some nonimmune acute inflammation-related disease, probably by an inhibitory action on production and/or release of PGE2 and NO.

  5. Galectin-1 exerts inhibitory effects during DENV-1 infection.

    Directory of Open Access Journals (Sweden)

    Karina Alves Toledo

    Full Text Available Dengue virus (DENV is an enveloped RNA virus that is mosquito-transmitted and can infect a variety of immune and non-immune cells. Response to infection ranges from asymptomatic disease to a severe disorder known as dengue hemorrhagic fever. Despite efforts to control the disease, there are no effective treatments or vaccines. In our search for new antiviral compounds to combat infection by dengue virus type 1 (DENV-1, we investigated the role of galectin-1, a widely-expressed mammalian lectin with functions in cell-pathogen interactions and immunoregulatory properties. We found that DENV-1 infection of cells in vitro exhibited caused decreased expression of Gal-1 in several different human cell lines, suggesting that loss of Gal-1 is associated with virus production. In test of this hypothesis we found that exogenous addition of human recombinant Gal-1 (hrGal-1 inhibits the virus production in the three different cell types. This inhibitory effect was dependent on hrGal-1 dimerization and required its carbohydrate recognition domain. Importantly, the inhibition was specific for hrGal-1, since no effect was observed using recombinant human galectin-3. Interestingly, we found that hrGal-1 directly binds to dengue virus and acts, at least in part, during the early stages of DENV-1 infection, by inhibiting viral adsorption and its internalization to target cells. To test the in vivo role of Gal-1 in DENV infection, Gal-1-deficient-mice were used to demonstrate that the expression of endogenous Galectin-1 contributes to resistance of macrophages to in vitro-infection with DENV-1 and it is also important to physiological susceptibility of mice to in vivo infection with DENV-1. These results provide novel insights into the functions of Gal-1 in resistance to DENV infection and suggest that Gal-1 should be explored as a potential antiviral compound.

  6. Inhibitory Effects of Respiration Inhibitors on Aflatoxin Production

    Directory of Open Access Journals (Sweden)

    Shohei Sakuda

    2014-03-01

    Full Text Available Aflatoxin production inhibitors, which do not inhibit the growth of aflatoxigenic fungi, may be used to control aflatoxin without incurring a rapid spread of resistant strains. A respiration inhibitor that inhibits aflatoxin production was identified during a screening process for natural, aflatoxin-production inhibitors. This prompted us to evaluate respiration inhibitors as potential aflatoxin control agents. The inhibitory activities of four natural inhibitors, seven synthetic miticides, and nine synthetic fungicides were evaluated on aflatoxin production in Aspergillus parasiticus. All of the natural inhibitors (rotenone, siccanin, aptenin A5, and antimycin A inhibited fungal aflatoxin production with IC50 values around 10 µM. Among the synthetic miticides, pyridaben, fluacrypyrim, and tolfenpyrad exhibited strong inhibitory activities with IC50 values less than 0.2 µM, whereas cyflumetofen did not show significant inhibitory activity. Of the synthetic fungicides, boscalid, pyribencarb, azoxystrobin, pyraclostrobin, and kresoxim-methyl demonstrated strong inhibitory activities, with IC50 values less than 0.5 µM. Fungal growth was not significantly affected by any of the inhibitors tested at concentrations used. There was no correlation observed between the targets of respiration inhibitors (complexes I, II, and III and their IC50 values for aflatoxin-production inhibitory activity. This study suggests that respiration inhibitors, including commonly used pesticides, are useful for aflatoxin control.

  7. Inhibitory Effects of Standardized Extracts of Phyllanthus amarus and Phyllanthus urinaria and Their Marker Compounds on Phagocytic Activity of Human Neutrophils

    Directory of Open Access Journals (Sweden)

    Yuandani

    2013-01-01

    Full Text Available The standardized methanol extracts of Phyllanthus amarus and P. urinaria, collected from Malaysia and Indonesia, and their isolated chemical markers, phyllanthin and hypophyllanthin, were evaluated for their effects on the chemotaxis, phagocytosis and chemiluminescence of human phagocytes. All the plant extracts strongly inhibited the migration of polymorphonuclear leukocytes (PMNs with the Malaysian P. amarus showing the strongest inhibitory activity (IC50 value, 1.1 µg/mL. There was moderate inhibition by the extracts of the bacteria engulfment by the phagocytes with the Malaysian P. amarus exhibiting the highest inhibition (50.8% of phagocytizing cells. The Malaysian P. amarus and P. urinaria showed strong reactive oxygen species (ROS inhibitory activity, with both extracts exhibiting IC50 value of 0.7 µg/mL. Phyllanthin and hypophyllanthin exhibited relatively strong activity against PMNs chemotaxis, with IC50 values slightly lower than that of ibuprofen (1.4 µg/mL. Phyllanthin exhibited strong inhibitory activity on the oxidative burst with an IC50 value comparable to that of aspirin (1.9 µg/mL. Phyllanthin exhibited strong engulfment inhibitory activity with percentage of phagocytizing cells of 14.2 and 27.1% for neutrophils and monocytes, respectively. The strong inhibitory activity of the extracts was due to the presence of high amounts of phyllanthin and hypophyllanthin although other constituents may also contribute.

  8. An evaluation of the inhibitory effects against rotavirus infection of edible plant extracts

    Directory of Open Access Journals (Sweden)

    Knipping Karen

    2012-07-01

    Full Text Available Abstract Background Rotaviruses are the single most important cause of severe diarrhea in young children worldwide. The developments of specific, potent and accessible antiviral treatments that restrain rotavirus infection remain important to control rotavirus disease. Methods 150 plant extracts with nutritional applications were screened in vitro on MA-104 cells for their antiviral activity against rhesus rotavirus (RRV. One extract (Aspalathus linearis (Burm.f. R.Dahlgren was also tested for its effect on the loss of transepithelial resistance (TER of Caco-2 cells caused by simian rotavirus (SA-11 infection. Results Aqueous extracts of Nelumbo nucifera Gaertn. fruit, Urtica dioica L. root, Aspalathus linearis (Burm.f. R.Dahlgren leaves, Glycyrrhiza glabra L. root and Olea europaea L. leaves were found to have strong significant antiviral activity with a 50% inhibitory concentration (IC50 Glycyrrhiza glabra was found to have the strongest antiviral activity (IC50 46 μM, followed by luteolin and vitexin from Aspalathus linearis (IC50 respectively 116 μM and 129 μM and apigenin-7-O-glucoside from Melissa officinalis (IC50 150 μM. A combination of Glycyrrhiza glabra L. + Nelumbo nucifera Gaertn. and Urtica dioica L. + Nelumbo nucifera Gaertn. showed synergy in their anti-viral activities. Aspalathus linearis (Burm.f. R.Dahlgren showed no positive effect on the maintenance of the TER. Conclusions These results indicate that nutritional intervention with extracts of Nelumbo nucifera Gaertn., Aspalathus linearis (Burm.f. R.Dahlgren, Urtica dioica L., Glycyrrhiza glabra L. and Olea europaea L. might be useful in the treatment of diarrhea caused by rotavirus infection.

  9. Inhibitory effect of common microfluidic materials on PCR outcome

    KAUST Repository

    Kodzius, Rimantas

    2012-02-20

    compatibility of various materials commonly used while producing microfluidic devices is also pertinent and beneficial to other enzymatic reactions in microfluidic devices. Most PCR-friendly materials exhibit similar signals regardless of the inclusion or not of BSA in the PCR mixture; these materials are PP, PTFE, PDMS, wax (Tm 80°C), SiO2 quartz, pyrex and soda-lime glasses, NOA68, and mineral oil. Our results showed that there was near total adsorption of template DNA when the wax (Tm 60°C) was used (RBI = 9.2×101). In contrast, when NOA61, mineral oil and acrylic glue materials were employed, significant adsorption occurred (RBI < 1.5×103). The polymerase-inhibition experiments indicate that following materials do not have strong effects (RBI > 1.1×103) on polymerase: PC, PP, PTFE, PDMS, silicon with a layer of 560 nm SiO2, SiO2 quartz, pyrex, and soda-lime glass. Slight polymerase inhibition (RBI < 9.2×102) was observed with PMMA, PVC, waxes (Tm 56°C and 80°C), silicon, and NOA68. A very strong or near total inhibition (RBI < 1.8×102) was observed with wax (Tm 60°C), ITO glass, SU-8, NOA61, metal tubes, mineral oil, epoxy, and the acrylic glues. \\tOur results show that material selection for microfluidic PCR chips, which are characterized by large SAVR, is a vital part of optimizing PCR outcome. This study of the inhibitory effect of various common microfluidics materials has provided a new rapid testing method using only a PCR cycler, and it has confirmed and expanded the list of tested materials. The type of PCR compatibility test enables the most effectual choice of materials for use in biology-related experiments.

  10. COX-1 inhibitory effect of medicinal plants of Ghana

    DEFF Research Database (Denmark)

    Larsen, Birgitte HV; Soelberg, Jens; Jäger, Anna

    2015-01-01

    Plants used to treat inflammatory ailments, pain, fever and infections in Ghana, were tested for COX-1 inhibitory activity. Ethanolic extracts of 17 species were tested in a COX-1 assay. The extracts of Gardenia ternifolia, Thonningia sanguinea, Triumfetta rhomboidea, and the root of Zanthoxylum ...

  11. Effect of Bacteriocin-like Inhibitory Substances Produced by Vaginal ...

    African Journals Online (AJOL)

    Reduction of vaginal Lactobacillus population leads to overgrowth of opportunistic organisms such as Streptococcus agalactiae (Group B Streptococcus, GBS), which causes life threatening neonatal infections. The activities of bacteriocin-like inhibitory substances (BLIS) produced by Lactobacillus species isolated from the ...

  12. Inhibitory effect of burdock leaves on elastase and tyrosinase activity

    Science.gov (United States)

    Horng, Chi-Ting; Wu, Hsing-Chen; Chiang, Ni-Na; Lee, Chiu-Fang; Huang, Yu-Syuan; Wang, Hui-Yun; Yang, Jai-Sing; Chen, Fu-An

    2017-01-01

    Burdock (Arctium lappa L.) leaves generate a considerable amount of waste following burdock root harvest in Taiwan. To increase the use of burdock leaves, the present study investigated the optimal methods for producing burdock leaf extract (BLE) with high antioxidant polyphenolic content, including drying methods and solvent extraction concentration. In addition, the elastase and tyrosinase inhibitory activity of BLE was examined. Burdock leaves were dried by four methods: Shadow drying, oven drying, sun drying and freeze-drying. The extract solution was then subjected to total polyphenol content analysis and the method that produced BLE with the highest amount of total antioxidant components was taken forward for further analysis. The 1,1-diphenyl-2-pycrylhydrazyl scavenging, antielastase and antityrosinase activity of the BLE were measured to enable the evaluation of the antioxidant and skin aging-associated enzyme inhibitory activities of BLE. The results indicated that the total polyphenolic content following extraction with ethanol (EtOH) was highest using the freeze-drying method, followed by the oven drying, shadow drying and sun drying methods. BLE yielded a higher polyphenol content and stronger antioxidant activity as the ratio of the aqueous content of the extraction solvent used increased. BLE possesses marked tyrosinase and elastase inhibitory activities, with its antielastase activity notably stronger compared with its antityrosinase activity. These results indicate that the concentration of the extraction solvent was associated with the antioxidant and skin aging-associated enzyme inhibitory activity of BLE. The reactive oxygen species scavenging theory of skin aging may explain the tyrosinase and elastase inhibitory activity of BLE. In conclusion, the optimal method for obtaining BLE with a high antioxidant polyphenolic content was freeze-drying followed by 30–50% EtOH extraction. In addition, the antielastase and antityrosinase activities of the

  13. Inhibitory control effects in adolescent binge eating and consumption of sugar-sweetened beverages and snacks.

    Science.gov (United States)

    Ames, Susan L; Kisbu-Sakarya, Yasemin; Reynolds, Kim D; Boyle, Sarah; Cappelli, Christopher; Cox, Matthew G; Dust, Mark; Grenard, Jerry L; Mackinnon, David P; Stacy, Alan W

    2014-10-01

    Inhibitory control and sensitivity to reward are relevant to the food choices individuals make frequently. An imbalance of these systems can lead to deficits in decision-making that are relevant to food ingestion. This study evaluated the relationship between dietary behaviors - binge eating and consumption of sweetened beverages and snacks - and behavioral control processes among 198 adolescents, ages 14 to 17. Neurocognitive control processes were assessed with the Iowa Gambling Task (IGT), a generic Go/No-Go task, and a food-specific Go/No-Go task. The food-specific version directly ties the task to food cues that trigger responses, addressing an integral link between cue-habit processes. Diet was assessed with self-administered food frequency and binge eating questionnaires. Latent variable models revealed marked gender differences. Inhibitory problems on the food-specific and generic Go/No-Go tasks were significantly correlated with binge eating only in females, whereas inhibitory problems measured with these tasks were the strongest correlates of sweet snack consumption in males. Higher BMI percentile and sedentary behavior also predicted binge eating in females and sweet snack consumption in males. Inhibitory problems on the generic Go/No-Go, poorer affective decision-making on the IGT, and sedentary behavior were associated with sweetened beverage consumption in males, but not females. The food-specific Go/No-Go was not predictive in models evaluating sweetened beverage consumption, providing some initial discriminant validity for the task, which consisted of sweet/fatty snacks as no-go signals and no sugar-sweetened beverage signals. This work extends research findings, revealing gender differences in inhibitory function relevant to behavioral control. Further, the findings contribute to research implicating the relevance of cues in habitual behaviors and their relationship to snack food consumption in an understudied population of diverse adolescents not

  14. Inhibitory effect of Zanthoxylum bungeanum essential oil (ZBEO) on Escherichia coli and intestinal dysfunction.

    Science.gov (United States)

    Hong, Lei; Jing, Wu; Qing, Wang; Anxiang, Su; Mei, Xue; Qin, Liu; Qiuhui, Hu

    2017-04-19

    The inhibitory effects of Zanthoxylum bungeanum essential oil (ZBEO) on Escherichia coli (E. coli) in vitro and in vivo were investigated, as well as its function of improvement of intestinal health. The results of in vitro studies, such as minimal inhibitory concentration (MIC) analysis, agar disc diffusion test and growth curve analysis of E. coli, showed that ZBEO had an excellent inhibitory effect on the growth of E. coli, which may be related to the loss of the normal shape of the cell membranes and the leakage of intracellular constituents, on the basis of SEM observation and cell constituents' release assay. ZBEO also had an inhibitory effect on enteritis and intestinal dysfunction induced by infection of E. coli in vivo, and histopathological observation indicated that ZBEO could markedly ameliorate the structural destruction of intestinal tissues, which might be related to its inhibitory effect on the gene expression of inflammatory cytokines (TLR2, TLR4, TNF α and IL-8). In conclusion, ZBEO showed an excellent inhibitory effect on E. coli both in vitro and in vivo, suggesting the potential application of ZBEO as a kind of functional component having the effects of improving intestinal function and health.

  15. Inhibitory Effects of Resveratrol Analogs on Mushroom Tyrosinase Activity

    Directory of Open Access Journals (Sweden)

    Nádia Rezende Barbosa Raposo

    2012-10-01

    Full Text Available Skin pigmentation disorders typically involve an overproduction or uneven distribution of melanin, which results in skin spots. Resveratrol can inhibit tyrosinase, the active enzyme in the synthesis of melanin, but it does not inhibit the synthesis of melanin to an extent that enables its use alone as a skin whitening agent in pharmaceutical formulations, so its use as a coadjuvant in treatment of hyperpigmentation is suggested. Six resveratrol analogs were tested for tyrosinase inhibitory activity in vitro. Among the analogs tested, compound D was the most powerful tyrosinase inhibitor (IC50 = 28.66 µg/mL, two times more active than resveratrol (IC50 = 57.05 µg/mL, followed by the analogs A, E, B, F and C, respectively. This demonstrated that the hydroxylation at C4' on the phenolic ring was the molecular modification with most importance for the observed activity.

  16. Inhibitory effects of Vietnamese medicinal plants on tube-like formation of human umbilical venous cells.

    Science.gov (United States)

    Nam, Nguyen-Hai; Kim, Hwan-Mook; Bae, Ki-Hwan; Ahn, Byung-Zun

    2003-02-01

    Seven of 58 plant materials from Vietnamese medicinal plants showed strong to moderate inhibitory activity on the tube-like formation induced by human umbilical venous endothelial cells in the in vitro angiogenesis assay. These plant materials include the herb of Ephedra sinica, leaves and stem of Ceiba pentandra, seed of Coix lachryma-jobi, rhizome of Drynaria fortunei, fruits and stem of Illicium verum and stem of Bombax ceiba. Of these, the methanol extracts of the herb of Ephedra sinica and stem of -Ceiba pentandra exhibited the strongest activities with inhibition percentages of 89.3% and 87.5% at 30 and 100 microgram/mL, respectively. Copyright 2003 John Wiley & Sons, Ltd.

  17. Multilingual Stroop performance: Effects of trilingualism and proficiency on inhibitory control

    OpenAIRE

    Marian, Viorica; Blumenfeld, Henrike K.; Mizrahi, Elena; Kania, Ursula; Cordes, Anne-Kristin

    2012-01-01

    Previous research suggests that multilinguals’ languages are constantly co-activated and that experience managing this co-activation changes inhibitory control function. The present study examined language interaction and inhibitory control using a colour-word Stroop task. Multilingual participants were tested in their three most proficient languages. The classic Stroop effect was detected in all three languages, with participants performing more accurately on congruent than on incongruent tr...

  18. Effect of inhibitory firing pattern on coherence resonance in random neural networks

    Science.gov (United States)

    Yu, Haitao; Zhang, Lianghao; Guo, Xinmeng; Wang, Jiang; Cao, Yibin; Liu, Jing

    2018-01-01

    The effect of inhibitory firing patterns on coherence resonance (CR) in random neuronal network is systematically studied. Spiking and bursting are two main types of firing pattern considered in this work. Numerical results show that, irrespective of the inhibitory firing patterns, the regularity of network is maximized by an optimal intensity of external noise, indicating the occurrence of coherence resonance. Moreover, the firing pattern of inhibitory neuron indeed has a significant influence on coherence resonance, but the efficacy is determined by network property. In the network with strong coupling strength but weak inhibition, bursting neurons largely increase the amplitude of resonance, while they can decrease the noise intensity that induced coherence resonance within the neural system of strong inhibition. Different temporal windows of inhibition induced by different inhibitory neurons may account for the above observations. The network structure also plays a constructive role in the coherence resonance. There exists an optimal network topology to maximize the regularity of the neural systems.

  19. Inhibitory effects of soluble algae products (SAP) released by Scenedesmus sp. LX1 on its growth and lipid production.

    Science.gov (United States)

    Zhang, Tian-Yuan; Yu, Yin; Wu, Yin-Hu; Hu, Hong-Ying

    2013-10-01

    Soluble algal products (SAP) accumulated in culture medium via water reuse may affect the growth of microalga during the cultivation. Scenedesmus sp. LX1, a freshwater microalga, was used in this study to investigate the effect of SAP on growth and lipid production of microalga. Under the SAP concentrations of 6.4-25.8 mg L(-1), maximum algal density (K) and maximum growth rate (Rmax) of Scenedesmus sp. LX1 were decreased by 50-80% and 35-70% compared with the control group, respectively. The effect of SAP on lipid accumulation of Scenedesmus sp. LX1 was non-significant. According to hydrophilic-hydrophobic and acid-base properties, SAP was fractionized into six fractions. All of the fractions could inhibit the growth of Scenedesmus sp. LX1. Organic bases (HIB, HOB) and hydrophilic acids (HIA) showed the strongest inhibition. HIA could also decrease the lipid content of Scenedesmus sp. LX1 by 59.2%. As the inhibitory effect, SAP should be seriously treated before water reuse. Copyright © 2013 Elsevier Ltd. All rights reserved.

  20. Isolation of proanthocyanidins from red wine, and their inhibitory effects on melanin synthesis in vitro.

    Science.gov (United States)

    Fujimaki, Takahiro; Mori, Shoko; Horikawa, Manabu; Fukui, Yuko

    2018-05-15

    The red wines made from Vitis vinifera were identified as skin-whitening effectors by using in vitro assays. OPCs in the wine were evaluated for tyrosinase activity and melanogenesis. Strong tyrosinase inhibitory activity was observed in fractions with high oligomeric proanthocyanidin (OPC) content. Among OPC dimers, a strong inhibitory effect on tyrosinase was observed with OPCs which contain (+)-catechin as an upper unit. Melanogenesis inhibitory effect was observed with OPCs which have (-)-epicatechin as upper units. Also, OPC trimers, upper and middle units joined with 4 → 8 bonds, showed stronger effects compared to trimers with 4 → 6 linkages. Interestingly, (-)-epicatechin-(4β → 8)-(-)-epicatechin 3-O-gallate, which is a unique component of grapes has potent inhibitory effects on both tyrosinase and melanogenesis. Our data provide structural information about such active compounds. These results suggest that red wines containing OPC, have high melanogenesis inhibitory effect and are supposed to have skin-whitening effect. Copyright © 2017 Elsevier Ltd. All rights reserved.

  1. Studying the Inhibitory Effect of Quercetin and Thymoquinone on Human Cytochrome P450 Enzyme Activities.

    Science.gov (United States)

    Elbarbry, Fawzy; Ung, Aimy; Abdelkawy, Khaled

    2018-01-01

    Quercetin (QR) and thymoquinone (TQ) are herbal remedies that are currently extensively used by the general population to prevent and treat various chronic conditions. Therefore, investigating the potential of pharmacokinetic interactions caused by the concomitant use of these herbal remedies and conventional medicine is warranted to ensure patient safety. This study was conducted to determine the inhibitory effect of QR and TQ, two commonly used remedies, on the activities of selected cytochrome P450 (CYP) enzymes that play an important role in drug metabolism and/or toxicology. The in vitro studies were conducted using fluorescence-based high throughput assays using human c-DNA baculovirus expressed CYP enzymes. For measuring CYP2E1 activity, a validated High-performance liquid chromatography (HPLC) assay was utilized to measure the formation of 6-hydroxychlorzoxazone. The obtained half-maximum inhibitory concentration values with known positive control inhibitors of this study were comparable to the published values indicating accurate experimental techniques. Although QR did not show any significant effect on CYP1A2 and CYP2E1, it exhibited a strong inhibitory effect against CYP2D6 and a moderate effect against CYP2C19 and CYP3A4. On the other hand, TQ demonstrated a strong and a moderate inhibitory effect against CYP3A4 and CYP2C19, respectively. The findings of this study may indicate that consumption of QR or TQ, in the form of food or dietary supplements, with drugs that are metabolized by CYP2C19, CYP2D6, or CYP3A4 may cause significant herb-drug interactions. Neither QR nor TQ has any significant inhibitory effect on the activity of CYP1A2 or CYP2E1 enzymesBoth QR and TQ have a moderate to strong inhibitory effect on CYP3A4 activityQR has a moderate inhibitory effect on CYP2C19 and a strong inhibitory effect on CYP2D6Both QR and TQ are moderate inhibitors of the CYP2C9 activity. Abbreviations used: ABT: Aminobenztriazole, BZF: 7,8 Benzoflavone, CYP

  2. Effects of Hebbian learning on the dynamics and structure of random networks with inhibitory and excitatory neurons.

    Science.gov (United States)

    Siri, Benoît; Quoy, Mathias; Delord, Bruno; Cessac, Bruno; Berry, Hugues

    2007-01-01

    The aim of the present paper is to study the effects of Hebbian learning in random recurrent neural networks with biological connectivity, i.e. sparse connections and separate populations of excitatory and inhibitory neurons. We furthermore consider that the neuron dynamics may occur at a (shorter) time scale than synaptic plasticity and consider the possibility of learning rules with passive forgetting. We show that the application of such Hebbian learning leads to drastic changes in the network dynamics and structure. In particular, the learning rule contracts the norm of the weight matrix and yields a rapid decay of the dynamics complexity and entropy. In other words, the network is rewired by Hebbian learning into a new synaptic structure that emerges with learning on the basis of the correlations that progressively build up between neurons. We also observe that, within this emerging structure, the strongest synapses organize as a small-world network. The second effect of the decay of the weight matrix spectral radius consists in a rapid contraction of the spectral radius of the Jacobian matrix. This drives the system through the "edge of chaos" where sensitivity to the input pattern is maximal. Taken together, this scenario is remarkably predicted by theoretical arguments derived from dynamical systems and graph theory.

  3. Inhibitory control effects in adolescent binge eating and consumption of sugar-sweetened beverages and snacks

    Science.gov (United States)

    Ames, Susan L.; Kisbu-Sakarya, Yasemin; Reynolds, Kim D.; Boyle, Sarah; Cappelli, Christopher; Cox, Matthew G.; Dust, Mark; Grenard, Jerry L.; Mackinnon, David P.; Stacy, Alan W.

    2014-01-01

    Inhibitory control and sensitivity to reward are relevant to the food choices individuals make frequently. An imbalance of these systems can lead to deficits in decision-making that are relevant to food ingestion. This study evaluated the relationship between dietary behaviors – binge eating and consumption of sweetened beverages and snacks - and behavioral control processes, among 198 ethnically diverse adolescents, ranging in age from 14 to 17, in Southern California. Neurocognitive control processes were assessed with the Iowa Gambling Task, a generic Go/No-Go task, and a food-specific Go/No-Go task. The food-specific Go/No-Go task directly ties the task to food cues that trigger responses, addressing an integral link between cue-habit processes. Dietary measures were assessed with self-administered food frequency and binge eating questionnaires. Results of latent variable models revealed marked gender differences. Inhibitory problems on the food-specific and generic Go/No-Go tasks were significantly correlated with binge eating only in females, whereas inhibitory problems measured with these tasks were the strongest correlates of sweet snack consumption in males. Higher BMI percentile and sedentary behavior also predicted binge eating in females and sweet snack consumption in males. Inhibitory problems on the generic Go/No-Go, poorer affective decision-making, assessed with the Iowa Gambling Task, and sedentary behavior were associated with sweetened beverage consumption in males, but not females. The food-specific Go/No-Go was not predictive in models evaluating sweetened beverage consumption, providing some initial discriminant validity for the task, which consisted of sweet/fatty snacks as no-go signals and no sugar-sweetened beverage signals. This research extends other study findings, revealing gender differences in inhibitory function relevant to behavioral control. Further, the findings contribute to research implicating the relevance of cues in

  4. Anterograde effects of a single electroconvulsive shock on inhibitory avoidance and on cued fear conditioning

    Directory of Open Access Journals (Sweden)

    Oliveira M.G.M.

    1998-01-01

    Full Text Available A single electroconvulsive shock (ECS or a sham ECS was administered to male 3-4-month-old Wistar rats 1, 2, and 4 h before training in an inhibitory avoidance test and in cued classical fear conditioning (measured by means of freezing time in a new environment. ECS impaired inhibitory avoidance at all times and, at 1 or 2 h before training, reduced freezing time before and after re-presentation of the ECS. These results are interpreted as a transient conditioned stimulus (CS-induced anxiolytic or analgesic effect lasting about 2 h after a single treatment, in addition to the known amnesic effect of the stimulus. This suggests that the effect of anterograde learning impairment is demonstrated unequivocally only when the analgesic/anxiolytic effect is over (about 4 h after ECS administration and that this impairment of learning is selective, affecting inhibitory avoidance but not classical fear conditioning to a discrete stimulus.

  5. Inhibitory self-control moderates the effect of changed implicit food evaluations on snack food consumption.

    Science.gov (United States)

    Haynes, Ashleigh; Kemps, Eva; Moffitt, Robyn

    2015-07-01

    The current study used a modified implicit association test (IAT) to change implicit evaluations of unhealthy snack food and tested its effects on subsequent consumption. Furthermore, we investigated whether these effects were moderated by inhibitory self-control. A sample of 148 women (17-25 years) motivated to manage weight through healthy eating completed an IAT intervention, and pre- and post-intervention IATs assessing implicit evaluations of unhealthy food. The intervention IAT trained participants to pair unhealthy food stimuli with either positive or negative stimuli. A task disguised as a taste-test was used to assess consumption of unhealthy snack foods. Inhibitory self-control was measured using a self-report scale. As predicted, the implicit evaluation of unhealthy food became more negative from pre- to post-training among participants in the food negative pairing condition; however, there was no corresponding change in the food positive pairing condition. The effect of the training on snack consumption was moderated by inhibitory self-control with only participants low in inhibitory self-control having lower snack intake following the food negative training. This finding is consistent with dual-process models of behaviour which predict that self-control capacity renders impulses less influential on behaviour. Furthermore, it suggests that an intervention that retrains implicit food evaluations could be effective at reducing unhealthy eating, particularly among those with low inhibitory self-control. Copyright © 2015 Elsevier Ltd. All rights reserved.

  6. Inhibitory effect of ethanol, acetic acid, propionic acid and butyric acid on fermentative hydrogen production

    Energy Technology Data Exchange (ETDEWEB)

    Wang, Bo; Wan, Wei; Wang, Jianlong [Laboratory of Environmental Technology, INET, Tsinghua University, Beijing 100084 (China)

    2008-12-15

    The inhibitory effect of added ethanol, acetic acid, propionic acid and butyric acid on fermentative hydrogen production by mixed cultures was investigated in batch tests using glucose as substrate. The experimental results showed that, at 35 C and initial pH 7.0, during the fermentative hydrogen production, the substrate degradation efficiency, hydrogen production potential, hydrogen yield and hydrogen production rate all trended to decrease with increasing added ethanol, acetic acid, propionic acid and butyric acid concentration from 0 to 300 mmol/L. The inhibitory effect of added ethanol on fermentative hydrogen production was smaller than those of added acetic acid, propionic acid and butyric acid. The modified Han-Levenspiel model could describe the inhibitory effects of added ethanol, acetic acid, propionic acid and butyric acid on fermentative hydrogen production rate in this study successfully. The modified Logistic model could describe the progress of cumulative hydrogen production. (author)

  7. Involvement of the insular cortex in regulating glucocorticoid effects on memory consolidation of inhibitory avoidance training.

    Science.gov (United States)

    Fornari, Raquel V; Wichmann, Romy; Atucha, Erika; Desprez, Tifany; Eggens-Meijer, Ellie; Roozendaal, Benno

    2012-01-01

    Glucocorticoids are known to enhance the consolidation of memory of emotionally arousing experiences by acting upon a network of interconnected brain regions. Although animal studies typically do not consider the insular cortex (IC) to be part of this network, the present findings indicate that the IC is importantly involved in regulating glucocorticoid effects on memory consolidation of emotionally arousing inhibitory avoidance training. The specific glucocorticoid receptor (GR) agonist RU 28362 (3 or 10 ng in 0.5 μl) infused bilaterally into the IC of male Sprague-Dawley rats immediately after one-trial inhibitory avoidance training dose-dependently enhanced 48 h retention performance. Moreover, training on the inhibitory avoidance task increased neuronal activity of the IC, as assessed by an increased number of cells expressing immunoreactivity for phosphorylated extracellular signal-regulated kinase 1/2 (pERK1/2). However, systemic administration of a memory-enhancing dose of corticosterone (1 mg/kg) after inhibitory avoidance training rapidly reduced the number of pERK1/2-positive cells in the IC, suggesting that glucocorticoid administration reduces overall neuronal activity of the IC. To investigate which components of the inhibitory avoidance training experience were influenced by the intra-IC glucocorticoid administration, in the last experiment rats were trained on a modified inhibitory avoidance task in which context exposure and footshock training occur on two sequential days. RU 28362 administration into the IC enhanced later retention when infused immediately after either the context or footshock training. Thus, these findings indicate that the IC mediates glucocorticoid effects on the consolidation of memory of different components of inhibitory avoidance training and suggest that the IC might be an important element of the rodent brain network involved in emotional regulation of learning and memory.

  8. Involvement of the insular cortex in regulating glucocorticoid effects on memory consolidation of inhibitory avoidance training

    Directory of Open Access Journals (Sweden)

    Raquel eFornari

    2012-03-01

    Full Text Available Glucocorticoids are known to enhance the consolidation of memory of emotionally arousing experiences by acting upon a network of interconnected brain regions. Although animal studies typically do not consider the insular cortex (IC to be part of this network, the present findings indicate that the IC is importantly involved in regulating glucocorticoid effects on memory consolidation of emotionally arousing inhibitory avoidance training. The specific glucocorticoid receptor agonist RU 28362 (3 or 10 ng in 0.5 l infused bilaterally into the IC of male Sprague-Dawley rats immediately after one-trial inhibitory avoidance training dose-dependently enhanced 48-h retention performance. Moreover, training on the inhibitory avoidance task increased neuronal activity of the IC, as assessed by an increased number of cells expressing immunoreactivity for phosphorylated extracellular signal-regulated kinase 1/2 (pERK1/2. However, systemic administration of a memory-enhancing dose of corticosterone (1 mg/kg after inhibitory avoidance training rapidly reduced the number of pERK1/2-positive cells in the IC, suggesting that glucocorticoid administration reduces overall neuronal activity of the IC. To investigate which components of the inhibitory avoidance training experience were influenced by the intra-IC glucocorticoid administration, in the last experiment rats were trained on a modified inhibitory avoidance task in which context exposure and footshock training occur on two sequential days. RU 28362 administration into the IC enhanced later retention when infused immediately after either the context or footshock training. Thus, these findings indicate that the IC mediates glucocorticoid effects on the consolidation of memory of different components of inhibitory avoidance training and suggest that the IC might be an important element of the rodent brain network involved in emotional regulation of learning and memory.

  9. Inhibitory effects and mechanisms of Hydrilla verticillata (Linn.f.) Royle extracts on freshwater algae.

    Science.gov (United States)

    Zhang, T-T; He, M; Wu, A-P; Nie, L-W

    2012-03-01

    To pursue an effective way to control freshwater algae, four extracts from a submerged macrophyte Hydrilla verticillata (Linn.f.) Royle were tested to study its inhibitory effects on Anabaena flos-aquae FACHB-245 and Chlorella pyrenoidosa Chick FACHB-9. Extract with the highest inhibiting ability was further studied in order to reveal the inhibitory mechanism. The results demonstrated that H. verticillata extracts inhibited the growth of A. flos-aquae and C. pyrenoidosa, and methanol extract had the highest inhibiting ability. The mechanism underlying the algal growth inhibition involves the superoxide anion radical generation that induces the damage of cell wall and release of intracellular components.

  10. Acute alcohol effects on inhibitory control and implicit cognition: implications for loss of control over drinking

    NARCIS (Netherlands)

    Field, M.; Wiers, R.W.; Christiansen, P.; Fillmore, M.T.; Verster, J.C.

    2010-01-01

    Alcohol impairs inhibitory control, and it alters implicit alcohol cognitions including attentional bias and implicit associations. These effects are seen after doses of alcohol which do not lead to global impairments in cognitive performance. We review studies which demonstrate that the effects of

  11. Inhibitory Effect of Lactobacillus reuteri on Some Pathogenic Bacteria Isolated From Women With Bacterial Vaginosis

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    Eslami

    2014-08-01

    Full Text Available Background Considering the high prevalence of bacterial vaginosis and its association with urinary tract infection in women and treatment of gynecologic problems occur when a high recurrence of bacterial vaginosis is often treated with antibiotics. Objectives The purpose of this study was to investigate the inhibitory effect of Lactobacillus reuteri on pathogenic bacteria isolated from women with bacterial vaginosis. Materials and Methods Ninety-six samples were obtained from vaginal discharge of women with bacterial vaginosis by a gynecologist with a Dacron swab and put in sterile tubes containing TSB broth and Thioglycollate broth. Then were immediately sent to the laboratory in cold chain for further assessment. Afterward, culture was transferred on blood agar, EMB, Palcam and differential diagnosis environments. Then cultures were incubated for 24 hours at 37 °C. Lactobacillus reuteri strains were cultured in MRS environment and transferred to laboratory. After purification of pathogenic bacteria, Lactobacillus reuteri inhibitory effect on pathogenic bacteria was evaluated by minimum inhibitory concentration (MIC and antibiogram. Statistical analysis was performed using SPSS software v.16. Results The results of this study demonstrated the inhibitory effect of Lactobacillus reuteri on some pathogenic bacteria that cause bacterial, including Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus saprophyticus, Streptococcus agalactiae, Enterococcus, Listeria monocytogenes and E. coli. Microscopic examination of stained smears of most Lactobacillus and pathogenic bacteria showed reduced. The prevalence of abnormal vaginal discharge, history of drug use, contraceptive methods and douching were 61%, 55%, 42% and 13%, respectively. Significant difference was observed between the use and non-use of IUD in women with bacterial. Conclusions Our findings indicated the inhibitory effect of Lactobacillus reuteri on pathogenic bacteria that

  12. Inhibitory effects of sudanese medicinal plant extracts on hepatitis C virus (HCV) protease.

    Science.gov (United States)

    Hussein, G; Miyashiro, H; Nakamura, N; Hattori, M; Kakiuchi, N; Shimotohno, K

    2000-11-01

    One hundred fifty-two methanol and water extracts of different parts of 71 plants commonly used in Sudanese traditional medicine were screened for their inhibitory effects on hepatitis C virus (HCV) protease (PR) using in vitro assay methods. Thirty-four extracts showed significant inhibitory activity (>/=60% inhibition at 100 microg/mL). Of these, eight extracts, methanol extracts of Acacia nilotica, Boswellia carterii, Embelia schimperi, Quercus infectoria, Trachyspermum ammi and water extracts of Piper cubeba, Q. infectoria and Syzygium aromaticum, were the most active (>/=90% inhibition at 100 microg/mL). From the E. schimperi extract, two benzoquinones, embelin (I) and 5-O-methylembelin (II), were isolated and found as potent HCV-PR inhibitors with IC(50) values of 21 and 46 microM, respectively. Inhibitory activities of derivatives of I against HCV-PR as well as their effects on other serine proteases were also investigated. Copyright 2000 John Wiley & Sons, Ltd.

  13. Inhibitory effects of silver zeolite on in vitro growth of fish egg pathogen, Saprolegnia sp.

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    Seyed Ali Johari

    2014-05-01

    Full Text Available Objective: To investigate the effects of powdered silver zeolite (SZ on the in vitro growth of the fish pathogen Saprolegnia sp. Methods: The antifungal activity of SZ was evaluated by determining the minimum inhibitory concentrations using two-fold serial dilutions of powdered SZ in a glucose yeast extract agar at 22 °C. The growth of Saprolegnia sp. on the SZ agar treatments was compared to that on SZ-free agar controls. Results: The results showed that SZ had an inhibitory effect on the in vitro growth of the tested fungi. The minimum inhibitory concentration of SZ for Saprolegnia sp. was also calculated at 600 mg/L, which is equal to 0.06 percent. Conclusions: SZ is a potential good candidate to replace teratogenic and toxic agents, such as malachite green in aquaculture systems.

  14. Provocative and inhibitory effects of a video-EEG neuropsychologic protocol in juvenile myoclonic epilepsy.

    Science.gov (United States)

    Guaranha, Mirian Salvadori Bittar; da Silva Sousa, Patrícia; de Araújo-Filho, Gerardo Maria; Lin, Katia; Guilhoto, Laura Maria Figueiredo Ferreira; Caboclo, Luís Otávio Sales Ferreira; Yacubian, Elza Márcia Targas

    2009-11-01

    Studies suggest that higher cognitive functions could precipitate seizures in juvenile myoclonic epilepsy (JME). The present study aimed to analyze the effects of higher mental activity on epileptiform discharges and seizures in patients with JME and compare them to those of habitual methods of activation. Seventy-six patients with JME (41 female) underwent a video-EEG (electroencephalography) neuropsychologic protocol (VNPP) and habitual methods of activation for 4-6 h. Twenty-nine of the 76 (38.2%) presented provocative effect, and inhibition was seen in 28 of 31 (90.3%). A mixed effect was observed in 11 (35.5%), and 30 patients (39.5%) suffered no effect of VNPP. Action-programming tasks were more effective than thinking in provoking epileptiform discharges (23.7% and 11.0% of patients, respectively, p = 0.03). Inhibitory effect was observed equally in the various categories of tasks, except in mental calculation, which had a higher inhibitory rate. Habitual methods of activation were more effective than VNPP in provoking discharges. Anxiety disorders were diagnosed in 24 of 58 patients (41.4%); anxious patients had greater discharge indexes and no significant inhibitory effect on VNPP. Praxis exerted the most remarkable provocative effect, in accordance with the motor circuitry hyperexcitability hypothesis in JME. Inhibitory effect, which had no such task specificity, might be mediated by a widespread cortical-thalamic pathway, possibly involving the parietal cortex. The frequent inhibitory effect found under cortical activation conditions, influenced by the presence of anxiety, supports nonpharmacologic therapeutic interventions in JME.

  15. Inhibitory Effects of Siegesbeckia orientalis Extracts on Advanced Glycation End Product Formation and Key Enzymes Related to Metabolic Syndrome

    Directory of Open Access Journals (Sweden)

    Wei-Chin Hung

    2017-10-01

    Full Text Available Metabolic syndrome typically includes Type 2 diabetes associated with hyperglycemia, central obesity, dyslipidemia and hypertension. It is highly related to oxidative stress, formation of advanced glycated end products (AGEs and key enzymes, such as carbohydrate digesting enzymes like pancreatic α-amylase and intestinal α-glucosidase, pancreatic lipase and angiotensin I-converting enzyme (ACE. This study used an in vitro approach to assess the potential of four extracts of Siegesbeckia orientalis linne on key enzymes relevant to metabolic syndrome. In this research, S. orientailis was firstly extracted by ethanol. The ethanol extract (SE was then partitioned sequentially with hexane, ethyl acetate and methanol, and these extracts were named SE-Hex, SE-EA and SE-MeOH, respectively. The experimental results showed that SE-EA had the highest total phenolic content (TPC, 76.9 ± 1.8 mg/g and the total flavonoids content (TFC, 5.3 ± 0.3 mg/g. This extract exhibited the most significant antioxidant activities, including DPPH radical-scavenging capacity (IC50 = 161.8 ± 2.4 μg/mL, ABTS radical-scavenging capacity (IC50 = 13.9 ± 1.5 μg/mL and reducing power. For anti-glycation activities, SE-EA showed the best results in the inhibition of AGEs, as well as inhibitory activities against α-glucosidase (IC50 = 362.3 ± 9.2 μg/mL and α-amylase (IC50 = 119.0 ± 17.7 μg/mL. For anti-obesity activities, SE-EA indicated the highest suppression effect on pancreatic lipase (IC50 = 3.67 ± 0.52 mg/mL. Finally, for anti-hypertension activity, SE-EA also demonstrated the strongest inhibitory activity on ACE (IC50 = 626.6 ± 15.0 μg/mL. Close relationships were observed among the parameters of TPC, antioxidant activities, inhibitory activities on α-amylase, α-glucosidase, lipase and ACE (R > 0.9. Moderate correlations were found among the parameters of TFC, antioxidant activities, and suppression of dicarbonyl compounds formation (R = 0.5–0.9. Taken

  16. INHIBITORY EFFECTS OF PERCHLOROETHYLENE ON HUMAN NEURONAL NICOTINIC ACETYLCHOLINE RECEPTORS.

    Science.gov (United States)

    Perchloroethylene (PERC) is a volatile organic solvent with a variety of industrial uses. PERC exposure has been shown to cause adverse neurological effects including deficits in vision and memory in exposed individuals. Despite knowledge of these effects, the mechanisms by whi...

  17. Inhibitory effect of saponins and polysaccharides from Radix ...

    African Journals Online (AJOL)

    The effects of different Radix ranunculi ternati extracts on human gastric cancer BGC823 cells were investigated, different methods were used to extract the saponins and polysaccharides from Radix ranunculi ternati, and MTT assay and colony formation assay were used to observe the effects of saponins and ...

  18. Bacterial mechanisms to overcome inhibitory effects of dietary tannins

    NARCIS (Netherlands)

    Smith, A.H.; Zoetendal, E.G.; Mackie, R.I.

    2005-01-01

    High concentrations of tannins in fodder plants inhibit gastrointestinal bacteria and reduce ruminant performance. Increasing the proportion of tannin-resistant bacteria in the rumen protects ruminants from antinutritional effects. The reason for the protective effect is unclear, but could be

  19. Inhibitory Effects of Daiokanzoto (Da-Huang-Gan-Cao-Tang on P-Glycoprotein

    Directory of Open Access Journals (Sweden)

    Yuka Watanabe

    2012-01-01

    Full Text Available We have studied the effects of various Kampo medicines on P-glycoprotein (P-gp, a drug transporter, in vitro. The present study focused on Daiokanzoto (Da-Huang-Gan-Cao-Tang, which shows the most potent inhibitory effects on P-gp among the 50 Kampo medicines studied, and investigated the P-gp inhibitory effects of Daiokanzoto herbal ingredients (rhubarb and licorice root and their components by an ATPase assay using human P-gp membrane. Both rhubarb and licorice root significantly inhibited ATPase activity, and the effects of rhubarb were more potent than those of licorice root. The content of rhubarb in Daiokanzoto is double that in licorice root, and the inhibition patterns of Daiokanzoto and rhubarb involve both competitive and noncompetitive inhibition, suggesting that the inhibitory effects of Daiokanzoto are mainly due to rhubarb. Concerning the components of rhubarb, concentration-dependent inhibitory effects were observed for (−-catechin gallate, (−-epicatechin gallate, and (−-epigallocatechin gallate. In conclusion, rhubarb may cause changes in the drug dispositions of P-gp substrates through the inhibition of P-gp. It appears that attention should be given to the interactions between these drugs and Kampo medicines containing rhubarb as an herbal ingredient.

  20. Effect of Jatropha curcas Peptide Fractions on the Angiotensin I-Converting Enzyme Inhibitory Activity

    Directory of Open Access Journals (Sweden)

    Maira R. Segura-Campos

    2013-01-01

    Full Text Available Hypertension is one of the most common worldwide diseases in humans. Angiotensin I-converting enzyme (ACE plays an important role in regulating blood pressure and hypertension. An evaluation was done on the effect of Alcalase hydrolysis of defatted Jatropha curcas kernel meal on ACE inhibitory activity in the resulting hydrolysate and its purified fractions. Alcalase exhibited broad specificity and produced a protein hydrolysate with a 21.35% degree of hydrolysis and 34.87% ACE inhibition. Ultrafiltration of the hydrolysate produced peptide fractions with increased biological activity (24.46–61.41%. Hydrophobic residues contributed substantially to the peptides’ inhibitory potency. The 5–10 and <1 kDa fractions were selected for further fractionation by gel filtration chromatography. ACE inhibitory activity (% ranged from 22.66 to 45.96% with the 5–10 kDa ultrafiltered fraction and from 36.91 to 55.83% with the <1 kDa ultrafiltered fraction. The highest ACE inhibitory activity was observed in F2 ( μg/mL from the 5–10 kDa fraction and F1 ( μg/mL from the <1 kDa fraction. ACE inhibitory fractions from Jatropha kernel have potential applications in alternative hypertension therapies, adding a new application for the Jatropha plant protein fraction and improving the financial viability and sustainability of a Jatropha-based biodiesel industry.

  1. Potent Inhibitory Effect of Chinese Dietary Spices on Fatty Acid Synthase.

    Science.gov (United States)

    Jiang, Bing; Liang, Yan; Sun, Xuebing; Liu, Xiaoxin; Tian, Weixi; Ma, Xiaofeng

    2015-09-01

    Dietary spices have been adopted in cooking since ancient times to enhance flavor and also as food preservatives and disease remedies. In China, the use of spices and other aromatic plants as food flavoring is an integral part of dietary behavior, but relatively little is known about their functions. Fatty acid synthase (FAS) has been recognized as a remedy target, and its inhibitors might be applied in disease treatment. The present work was designed to assess the inhibitory activities on FAS of spices extracts in Chinese menu. The in vitro inhibitory activities on FAS of 22 extracts of spices were assessed by spectrophotometrically monitoring oxidation of NADPH at 340 nm. Results showed that 20 spices extracts (90.9 %) exhibited inhibitory activities on FAS, with half inhibition concentration (IC(50)) values ranging from 1.72 to 810.7 μg/ml. Among them, seven spices showed strong inhibitory effect with IC(50) values lower than 10 μg/ml. These findings suggest that a large proportion of the dietary spices studied possess promising inhibitory activities on FAS, and subsequently might be applied in the treatment of obesity and obesity-related human diseases.

  2. Determinants of aggressive behavior: Interactive effects of emotional regulation and inhibitory control.

    Directory of Open Access Journals (Sweden)

    I-Ju Hsieh

    Full Text Available Aggressive behavior can be defined as any behavior intended to hurt another person, and it is associated with many individual and social factors. This study examined the relationship between emotional regulation and inhibitory control in predicting aggressive behavior. Seventy-eight participants (40 males completed self-report measures (Negative Mood Regulation Scale and Buss-Perry Aggression Questionnaire, a stop signal task, and engaged in a modified version of Taylor Aggression Paradigm (TAP exercise, in which the outcome was used as a measure of direct physical aggression. We used a hierarchical, mixed-model multiple regression analysis test to examine the effects of emotion regulation and inhibitory control on physical reactive aggression. Results indicated an interaction between emotion regulation and inhibitory control on aggression. For participants with low inhibitory control only, there was a significant difference between high and low emotion regulation on aggression, such that low emotion regulation participants registered higher aggression than high emotion regulation participants. This difference was not found among participants with high inhibitory control. These results have implications for refining and targeting training and rehabilitation programs aimed at reducing aggressive behavior.

  3. Inhibitory effect of eugenol on rat ileal motility in vitro

    OpenAIRE

    Trailović Saša M.; Robertson P.A.; Nedeljković-Trailović Jelena

    2009-01-01

    Eugenol, an essential oil of clove oil possesses several different pharmacological properties, including antimicrobial, antifungal, insecticidal and antihelmintic. With regard to the digestive tract, eugenol has shown spasmolitic and relaxant effects. To elucidate some of the mechanisms involved, the effects of eugenol on contractions of isolated rat ileum induced by electrical field stimulation (EFS) were investigated. Eugenol (100 mM) significantly and reversibly reduced EFS induced contrac...

  4. Multilingual Stroop performance: Effects of trilingualism and proficiency on inhibitory control

    Science.gov (United States)

    Marian, Viorica; Blumenfeld, Henrike K.; Mizrahi, Elena; Kania, Ursula; Cordes, Anne-Kristin

    2013-01-01

    Previous research suggests that multilinguals’ languages are constantly co-activated and that experience managing this co-activation changes inhibitory control function. The present study examined language interaction and inhibitory control using a colour-word Stroop task. Multilingual participants were tested in their three most proficient languages. The classic Stroop effect was detected in all three languages, with participants performing more accurately on congruent than on incongruent trials. Multilinguals were faster and more accurate in the within-language-competition condition than in the between-language-competition condition, indicating that additional processing costs are required when stimulus and response languages differ. Language proficiency influenced speed, accuracy and error patterns in multilingual Stroop task performance. These findings augment our understanding of language processing and inhibitory control in multilingual populations and suggest that experience using multiple languages changes demands on cognitive function. PMID:24039546

  5. Inhibitory effects of lapachol derivatives on epstein-barr virus activation.

    Science.gov (United States)

    Sacau, Elisa Pérez; Estévez-Braun, Ana; Ravelo, Angel G; Ferro, Esteban A; Tokuda, Harunkuni; Mukainaka, Teruo; Nishino, Hoyoku

    2003-02-20

    Sixteen derivatives (2-17) synthesized from the naphthoquinone lapachol (1), were tested for their inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol-13-acetate (TPA), as a test for potential cancer chemopreventive agents. They exhibited a variety of inhibitory activities from very high to moderate, which allow us to suggest structure-activity relationships. Ten of these derivatives are reported for the first time, their structures being thoroughly determined by spectroscopic methods.

  6. Cellular target recognition of perfluoroalkyl acids: In vitro evaluation of inhibitory effects on lysine decarboxylase

    Energy Technology Data Exchange (ETDEWEB)

    Wang, Sufang; Lv, Qiyan; Yang, Yu, E-mail: yuyang@rcees.ac.cn; Guo, Liang-Hong, E-mail: LHGuo@rcees.ac.cn; Wan, Bin; Zhao, Lixia

    2014-10-15

    Perfluoroalkyl acids (PFAAs) have been shown to bind with hepatic peroxisome proliferator receptor α, estrogen receptors and human serum albumin and subsequently cause some toxic effects. Lysine decarboxylase (LDC) plays an important role in cell growth and developmental processes. In this study, the inhibitory effect of 16 PFAAs, including 13 perfluorinated carboxylic acids (PFCAs) and 3 perfluorinated sulfonic acids (PFSAs), on lysine decarboxylase (LDC) activity was investigated. The inhibition constants obtained in fluorescence enzyme assays fall in the range of 2.960 μM to 290.8 μM for targeted PFCAs, and 41.22 μM to 67.44 μM for targeted PFSAs. The inhibitory effect of PFCAs increased significantly with carbon chain (7–18 carbons), whereas the short chain PFCAs (less than 7 carbons) did not show any effect. Circular dichroism results showed that PFAA binding induced significant protein secondary structural changes. Molecular docking revealed that the inhibitory effect could be rationalized well by the cleft binding mode as well as the size, substituent group and hydrophobic characteristics of the PFAAs. At non-cytotoxic concentrations, three selected PFAAs inhibited LDC activity in HepG2 cells, and subsequently resulted in the decreased cadaverine level in the exposed cells, suggesting that LDC may be a possible target of PFAAs for their in vivo toxic effects. - Highlights: • Inhibitory effects of PFAAs on lysine decarboxylase activity were evaluated. • Four different methods were employed to investigate the mechanisms. • The long chain PFAAs showed inhibitory effect compare with 4–6 carbon chain. • The long chain PFAAs bound with LDC differently from the short ones. • The results in cells correlate with those obtained from fluorescence assay.

  7. Acetyl-cholinesterase Enzyme Inhibitory Effect of Calophyllum species

    African Journals Online (AJOL)

    have shown them to possess potential pharmaceutical usage such as they indicated cytotoxicity [3], anti-HIV [4], anti-leishmanial [5], antioxidant [6], antibacterial [7], anti-fungal [8] and anti-malarial [9] properties. These promising biological effects of Calophyllum species have attracted attention from our research group.

  8. Simulated inhibitory effects of typical byproducts of biomass ...

    African Journals Online (AJOL)

    Aghomotsegin

    2015-07-29

    Jul 29, 2015 ... the effect of inhibitors on the viability of S. cerevisiae and ethanol productivity does not last and can be overcome by the ... process of the conversion of lignocellulosic materials into bioethanol is not ..... Glucose consumption and ethanol production in the presence of 4 g acetic acid: Large symbols. (glucose) ...

  9. Inhibitory effect of puerarin on proliferation of retinoblastoma cells ...

    African Journals Online (AJOL)

    ... 71.4 ± 4.5 % for control and Bmi-1 siRNA-treated groups, respectively. Conclusions: The results show that puerarin exert suppressive effects on human retinoblastoma Y79 cells and therefore may find application in the treatment of intraocular tumor. Keywords: Cancer, Puerarin, Retinoblastoma Y79 cells, mTOR inhibition, ...

  10. Inhibitory effects of total saponins from Ilex pubescens Hook against ...

    African Journals Online (AJOL)

    Purpose: To study the protective effects of total saponins from Ilex pubescens Hook (IPTS) against cardiomyocyte apoptosis. Methods: Response surface methodology (RSM) based on Box-Benhnken Design (BBD) was carried out to optimize the extraction of IPTS. Thereafter, H9c2 cell model prepared by hydrogen ...

  11. Synergistic Cancer Growth-Inhibitory Effect of Emodin and Low ...

    African Journals Online (AJOL)

    novel agents that can be combined with cisplatin to increase the therapeutic efficacy and decrease side effects. ... natural compound extracted from various Rheum medicinal plant species, with cisplatin on human ... Biological Products Co, Ltd, China), Minimum. Essential Medium (MEM, Invitrogen Corp.,. Carlsbad, CA ...

  12. The inhibitory effect of Curcuma longa extract on telomerase activity ...

    African Journals Online (AJOL)

    Telomerase is reactivated in lung cancer cells, the most prevalent cancer worldwide, but not normal cells. Therefore, targeting it, preferably with natural compounds derive from medicinal plant such as curcumin, could have important effect on treatment of lung cancer. Curcumin, derived from Curcuma longa rhizome, has ...

  13. In vitro evaluation of inhibitory effect of Phoenix dactylifera bark ...

    African Journals Online (AJOL)

    Conclusion: The findings of this study indicate significant anti-lipid peroxidation and anti-hemolytic effects of the bark extract. Therefore, the extract can potentially be used for the in vivo treatment of diseases associated with lipid peroxidation such as cancers and Alzheimer's disease, but further studies are required.

  14. Inhibitory effect of Lycopene against the growth of human gastric ...

    African Journals Online (AJOL)

    Background The aim of this study was to investigate the anti-proliferative effect of Lycopene on HGC-27 cells. Materials and methods HGC-27 cells were treated with varying concentration lycopene for 24, 48, 72 h. The cell growth inhibition was analyzed by MTT. Western blotting was used to indicate changes in the levels of ...

  15. A Comparison of the Inhibitory Effect of Omeprazole And Nifedipine ...

    African Journals Online (AJOL)

    The present study was carried out to determine the effect of the gastric acid inhibitors, nifedipine (a calcium channel blocker) and omeprazole, (a proton pump inhibitor), on histamine-stimulated and carbachol stimulated gastric acid secretion in rats. Thirty intact male Sprague-Dawley rats were used for the study. The rats ...

  16. Comparative in vitro inhibitory effects of cold extracts of some ...

    African Journals Online (AJOL)

    STORAGESEVER

    2008-09-17

    Sep 17, 2008 ... Antifungal effects of some common wild plants species on certain plant pathogenic fungi. Dirasat. Pure Appl. Sci. 20: 149-158. Amadioha AC (1998). Control of Powdery mildew of pepper (Capsicum annum L) by leaf extracts Carica papaya. J. Herbs, spices and med. plants, 6: 41-47. Amadioha AC (2000).

  17. Inhibitory effect of puerarin on proliferation of retinoblastoma cells ...

    African Journals Online (AJOL)

    need to develop new therapeutic options to improve the outcomes of ... them promising targets for future drug discovery. [8]. Out of the millions ... derivatives, topothecan, irinothecan [13], and anthracycline [14]. Therefore, we aimed to elucidate the anti- proliferative effects of Puerarin on retinoblastoma cells [15]. Puerarin is a ...

  18. Effects of Neuromodulation on Excitatory-Inhibitory Neural Network Dynamics Depend on Network Connectivity Structure

    Science.gov (United States)

    Rich, Scott; Zochowski, Michal; Booth, Victoria

    2018-01-01

    Acetylcholine (ACh), one of the brain's most potent neuromodulators, can affect intrinsic neuron properties through blockade of an M-type potassium current. The effect of ACh on excitatory and inhibitory cells with this potassium channel modulates their membrane excitability, which in turn affects their tendency to synchronize in networks. Here, we study the resulting changes in dynamics in networks with inter-connected excitatory and inhibitory populations (E-I networks), which are ubiquitous in the brain. Utilizing biophysical models of E-I networks, we analyze how the network connectivity structure in terms of synaptic connectivity alters the influence of ACh on the generation of synchronous excitatory bursting. We investigate networks containing all combinations of excitatory and inhibitory cells with high (Type I properties) or low (Type II properties) modulatory tone. To vary network connectivity structure, we focus on the effects of the strengths of inter-connections between excitatory and inhibitory cells (E-I synapses and I-E synapses), and the strengths of intra-connections among excitatory cells (E-E synapses) and among inhibitory cells (I-I synapses). We show that the presence of ACh may or may not affect the generation of network synchrony depending on the network connectivity. Specifically, strong network inter-connectivity induces synchronous excitatory bursting regardless of the cellular propensity for synchronization, which aligns with predictions of the PING model. However, when a network's intra-connectivity dominates its inter-connectivity, the propensity for synchrony of either inhibitory or excitatory cells can determine the generation of network-wide bursting.

  19. In vivo hypotensive effect and in vitro inhibitory activity of some Cyperaceae species

    Directory of Open Access Journals (Sweden)

    Monica Lacerda Lopes Martins

    2013-12-01

    Full Text Available In 1820, French naturalist August Saint Hillaire, during a visit in Espírito Santo (ES, a state in southeastern Brazil, reported a popular use of Cyperaceae species as antidote to snake bites. The plant may even have a hypotensive effect, though it was never properly researched. The in vitro inhibitory of the angiotensin converting enzyme (ACE activity of eigth ethanolic extracts of Cyperaceae was evaluated by colorimetric assay. Total phenolic and flavonoids were determined using colorimetric assay. The hypotensive effect of the active specie (Rhychonospora exaltata, ERE and the in vivo ACE assay was measured in vivo using male Wistar Kyoto (ERE, 0.01-100mg/kg, with acetylcholine (ACh as positive control (5 µg/kg, i.v.. The evaluation of ACE in vivo inhibitory effect was performed comparing the mean arterial pressure before and after ERE (10 mg/kg in animals which received injection of angiotensin I (ANG I; 0,03, 03 and 300 µg/kg, i.v.. Captopril (30 mg/kg was used as positive control. Bulbostylis capillaris (86.89 ± 15.20% and ERE (74.89 ± 11.95%, ERE were considered active in the in vitro ACE inhibition assay, at 100 µg/mL concentration. ACh lead to a hypotensive effect before and after ERE's curve (-40±5% and -41±3%. ERE showed a dose-dependent hypotensive effect and a in vivo ACE inhibitory effect. Cyperaceae species showed an inhibitory activity of ACE, in vitro, as well as high content of total phenolic and flavonoids. ERE exhibited an inhibitory effect on both in vitro and in vivo ACE. The selection of species used in popular medicine as antidotes, along with the in vitro assay of ACE inhibition, might be a biomonitoring method for the screening of new medicinal plants with hypotensive properties.

  20. Enzyme inhibitory and radical scavenging effects of some antidiabetic plants of Turkey

    Directory of Open Access Journals (Sweden)

    Nilüfer Orhan

    2014-06-01

    Full Text Available Objective(s:Ethnopharmacological field surveys demonstrated that many plants, such as Gentiana olivieri, Helichrysum graveolens, Helichrysum plicatum ssp. plicatum, Juniperus oxycedrus ssp. oxycedrus, Juniperus  communis var. saxatilis, Viscum album (ssp. album, ssp. austriacum, are used as traditional medicine for diabetes in different regions of Anatolia. The present study was designed to evaluate the in vitro antidiabetic effects of some selected plants, tested in animal models recently. Materials and Methods: α-glucosidase and α-amylase enzyme inhibitory effects of the plant extracts were investigated and Acarbose was used as a reference drug. Additionally, radical scavenging capacities were determined using 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid ABTS radical cation scavenging assay and total phenolic content of the extracts were evaluated using Folin Ciocalteu method. Results: H. graveolens ethanol extract exhibited the highest inhibitory activity (55.7 % ± 2.2 on α-amylase enzyme. Additionally, J. oxycedrus hydro-alcoholic leaf extract had potent α-amylase inhibitory effect, while the hydro-alcoholic extract of J. communis fruit showed the highest α-glucosidase inhibitory activity (IC50: 4.4 μg/ml. Conclusion:Results indicated that, antidiabetic effect of hydro-alcoholic extracts of H. graveolens capitulums, J. communis fruit and J. oxycedrus leaf might arise from inhibition of digestive enzymes.

  1. Study on inhibitory effect of Spica Prunellae extract on T Lymphoma ...

    African Journals Online (AJOL)

    Tumour inhibition rate and tumour apoptosis-related protein status were determined using the mice model of transplanted T lymphoma cell EL-4 tumour, and by immunohistochemical method. The results revealed that Spica prunellae extract showed certain tumour inhibitory effect, and compared with the model group.

  2. Imagined Positive Emotions and Inhibitory Control: The Differentiated Effect of Pride versus Happiness

    Science.gov (United States)

    Katzir, Maayan; Eyal, Tal; Meiran, Nachshon; Kessler, Yoav

    2010-01-01

    "Inhibitory control" is a cognitive mechanism that contributes to successful self-control (i.e., adherence to a long-term goal in the face of an interfering short-term goal). This research explored the effect of imagined positive emotional events on inhibition. The authors proposed that the influence of imagined emotions on inhibition…

  3. INHIBITORY EFFECTS OF VOLATILE ORGANIC COMPOUNDS ON NEURONAL NICOTINIC ACETYLCHOLINE RECEPTORS.

    Science.gov (United States)

    INHIBITORY EFFECTS OF VOLATILE ORGANIC COMPOUNDS ON NEURONAL NICOTINIC ACETYLCHOLINE RECEPTORS. A.S. Bale*; P.J. Bushnell; C.A. Meacham; T.J. Shafer Neurotoxicology Division, NHEERL, ORD, US Environmental Protection Agency, Research Triangle Park, NC, USA Toluene (TOL...

  4. Inhibitory effect of rhubarb on intestinal α-glucosidase activity in type ...

    African Journals Online (AJOL)

    Purpose: To investigate the inhibitory effect of rhubarb on α-glucosidase activity in the small intestine of rats with type 1 diabetes. Methods: Type 1 diabetic rat model was established by intraperitoneally injecting 30 male SD rats with 1 % streptozocin (STZ). Rats with fasting blood glucose > 11 mmol/L (24) were used for the ...

  5. α-Amylase and α-glucosidase inhibitory effects of Sclerocarya birrea ...

    African Journals Online (AJOL)

    Inhibition of intestinal α-amylase and α-glucosidase is an important strategy to control post-prandial hyperglycemia associated with type 2 diabetes mellitus. In vitro inhibitory effects of crude Sclerocarya birrea stem bark (SBSB) extracts against human urinary α-amylase and Bacillus steatothermophilus α-glucosidase were ...

  6. Inhibitory effect of emodin on raw 264.7 activated with double ...

    African Journals Online (AJOL)

    Inhibitory effect of emodin on raw 264.7 activated with double stranded RNA analogue poly I:C. Young-Jin Kim, Ji Young Lee, Hyun-Ju Kim, Do-Hoon Kim, Tae Hee Lee, Mi Suk Kang, You-Kyung Choi, Hye Lim Lee, Jaieun Kim, Hyo-Jin An, Wansu Park ...

  7. Selective Attention and Inhibitory Deficits in ADHD: Does Subtype or Comorbidity Modulate Negative Priming Effects?

    Science.gov (United States)

    Pritchard, Verena E.; Neumann, Ewald; Rucklidge, Julia J.

    2008-01-01

    Selective attention has durable consequences for behavior and neural activation. Negative priming (NP) effects are assumed to reflect a critical inhibitory component of selective attention. The performance of adolescents with Attention Deficit/Hyperactivity Disorder (ADHD) was assessed across two conceptually based NP tasks within a selective…

  8. The effect of aging on fronto-striatal reactive and proactive inhibitory control

    NARCIS (Netherlands)

    Kleerekooper, I.; van Rooij, S.J.H; van den Wildenberg, W.P.M.; de Leeuw, M.; Kahn, R.S.; Vink, M.

    2016-01-01

    Inhibitory control, like most cognitive processes, is subject to an age-related decline. The effect of age on neurofunctional inhibition processing remains uncertain, with age-related increases as well as decreases in activation being reported. This is possibly because reactive (i.e., outright

  9. Increased sink strength offsets the inhibitory effect of sucrose on sugarcane photosynthesis

    NARCIS (Netherlands)

    Ribeiro, Rafael V.; Machado, Eduardo C.; Magalhães Filho, José R.; Lobo, Ana K.M.; Martins, Márcio O.; Silveira, Joaquim A.G.; Yin, Xinyou; Struik, Paul C.

    2017-01-01

    Spraying sucrose inhibits photosynthesis by impairing Rubisco activity and stomatal conductance (gs), whereas increasing sink demand by partially darkening the plant stimulates sugarcane photosynthesis. We hypothesized that the stimulatory effect of darkness can offset the inhibitory

  10. Inhibitory Effect of Autoclaving Whey-Based Medium on Propionic Acid Production by Propionibacterium shermanii

    Science.gov (United States)

    Anderson, Thomas M.; Bodie, Elizabeth A.; Goodman, Nelson; Schwartz, Robert D.

    1986-01-01

    Propionic acid production by Propionibacterium shermanii was compared in pasteurized and autoclaved whey-based media. Propionic acid production decreased with increasing whey concentration in autoclaved media but not in pasteurized media. Increasing the yeast extract concentration from 5 to 10 g/liter greatly reduced the inhibitory effect of autoclaving. PMID:16346998

  11. Inhibitory Effect of Autoclaving Whey-Based Medium on Propionic Acid Production by Propionibacterium shermanii

    OpenAIRE

    Anderson, Thomas M.; Bodie, Elizabeth A.; Goodman, Nelson; Schwartz, Robert D.

    1986-01-01

    Propionic acid production by Propionibacterium shermanii was compared in pasteurized and autoclaved whey-based media. Propionic acid production decreased with increasing whey concentration in autoclaved media but not in pasteurized media. Increasing the yeast extract concentration from 5 to 10 g/liter greatly reduced the inhibitory effect of autoclaving.

  12. Inhibitory effects of the macrolide antimicrobial tylosin on anaerobic treatment.

    Science.gov (United States)

    Shimada, Toshio; Zilles, Julie L; Morgenroth, Eberhard; Raskin, Lutgarde

    2008-09-01

    A laboratory-scale anaerobic sequencing batch reactor (ASBR) was operated using a glucose-based synthetic wastewater to study the effects of tylosin, a macrolide antimicrobial commonly used in swine production, on treatment performance. The experimental period was divided into three consecutive phases with different influent tylosin concentrations (0, 1.67, and 167 mg/L). The addition of 1.67 mg/L tylosin to the reactor had negligible effects on the overall treatment performance, that is, total methane production and effluent chemical oxygen demand did not change significantly (P tylosin was added. The addition of 167 mg/L tylosin to the reactor resulted in a gradual decrease in methane production and the accumulation of propionate and acetate. Subsequent inhibition of methanogenesis was attributed to a decrease in the pH of the reactor. After the addition of 167 mg/L tylosin to the reactor, an initial decrease in the rate of glucose uptake during the ASBR cycle followed by a gradual recovery was observed. In batch tests, the specific biogas production with the substrate butyrate was completely inhibited in the presence of tylosin. This study indicated that tylosin inhibited propionate- and butyrate-oxidizing syntrophic bacteria and fermenting bacteria resulting in unfavorable effects on methanogenesis.

  13. Evaluation of inhibitory effects of iranian propolis against filamentous bacteria

    International Nuclear Information System (INIS)

    Eshraghi, S.; Valafar, S.

    2008-01-01

    To investigate the antibacterial activities of propolis in samples collected from Zanjan province Iran, against 25 pathogenic strains of bacteria. In order to evaluate the biological properties of methanol extract of propolis using agar distribution methods (disk and drop plate). Seven concentrations of methanolic extract of propolis were prepared and added drop wise to the bacterial seed layer cultured agar media individually. The diameter of the clear zone formed in each concentration was measured and correlated to the ability of the extracts to inhibit the growth of bacteria. Nocardia asteroides and N. brasiliensis has nearly shown the same susceptibility to various concentrations of propolis extract, and the complete clear zones revealed that this effect was quite remarkable. For other bacteria, different degrees of susceptibility to propolis were observed. We came to this conclusion that zones formed by 50mg/ml Amikacin in agar was similar to that of 5% concentration of propolis, and that the potency of propolis is 80% of Amikacin potency, which is the most effective antibiotic against Nocardia. (author)

  14. Carbonic anhydrase and acetylcholinesterase inhibitory effects of carbamates and sulfamoylcarbamates.

    Science.gov (United States)

    Göçer, Hülya; Akincioğlu, Akın; Göksu, Süleyman; Gülçin, İlhami; Supuran, Claudiu T

    2015-04-01

    Carbonic anhydrases (CA), as a family of metalloenzymes, are found in almost every type of tissue and play an important role in catalyzing the equilibration of carbon dioxide and carbonic acid. In this study, a series of carbamate derivative was synthesized, and their inhibition effects on hCA I, hCA II and acetylcholinesterase (AChE) enzymes were investigated. They were determined to be very good inhibitor against for both isoenzymes (hCA I and hCA II) and AChE. The hCA I and hCA II were effectively inhibited by the carbamate derivatives, with inhibition constants (Ki) in the range of 194.4-893.5 nM (for hCA I) and 103.9-835.7 nM (for hCA II). On the other hand, Ki parameters of these compounds for AChE enzyme inhibition were determined in the range of 12.0-61.3 nM. The results clearly showed that both CA isoenzymes and AChE were inhibited by carbamate derivatives at the nM levels.

  15. Inhibitory effects of xylitol on gastric emptying and food intake

    International Nuclear Information System (INIS)

    Shafer, R.B.; Levine, A.S.; Marlette, J.M.; Morley, J.E.

    1985-01-01

    The authors have previously shown, using a 99m-Tc scrambled egg meal, that pentose sugars (i.e. xylose and arabinose) markedly prolong gastric emptying. Others have reported that slowing of gastric emptying may decrease appetite and thus decrease food intake. In the present study, the authors utilized the effects of xylitol (an FDA-approved pentose sugar) on gastric emptying to study the correlation between gastric emptying and food intake. Initially, gastric emptying was measured in human volunteers utilizing a standardized 99m-Tc-scrambled egg meal washed with 50 cc tap water. Results demonstrated a significant reduction in food intake (892 +- 65 kcal with water vs 654 +- 26 kcal following the ingestion of 25 gm xylitol (p<0.05). We conclude that the effect of pentose sugars in prolonging gastric emptying directly influences food intake and contributes to early satiety. The data suggest a role of xylitol as an essentially non-caloric food additive potentially important in diet control

  16. Alpha-glucosidase inhibitory effect and inorganic constituents of Phyllanthus amarus Schum. & Thonn. ash

    Directory of Open Access Journals (Sweden)

    Malinee Wongnawa

    2014-10-01

    Full Text Available This study investigated the -glucosidase inhibitory effect and determined the concentration of some inorganic constituents in P. amarus ash. Oral glucose and sucrose tolerance test were performed on normal mice. In vitro -glucosidase inhibitory activity was evaluated by using yeast a-glucosidase. The element concentrations were measured by inductively coupled plasma (ICP spectroscopy. Single oral administration of P. amarus ash did not show antihyperglycemic effect after glucose administration, but decreased blood glucose level after sucrose administration. The ash showed -glucosidase inhibitory activity in vitro with IC50 of 982 mg/mL. The concentrations of K, Ca, Mg, Mn, Fe, Zn, Cu, Pb, Cr, Ni and Co in P. amarus ash were 35049.80±340.64, 3337.24±52.10, 1368.52±13.29, 90.81±1.34, 87.68±1.15, 18.28±0.22, 4.69±0.07, 1.07±0.15, 0.29±0.03, 0.20±0.04 and 0.10±0.02 mg/g, respectively. These results indicate that the antihyperglycemic effect of P. amarus ash might be partly due to the -glucosidase inhibitory activity of the inorganic constituents.

  17. ATF3 mediates inhibitory effects of ethanol on hepatic gluconeogenesis.

    Science.gov (United States)

    Tsai, Wen-Wei; Matsumura, Shigenobu; Liu, Weiyi; Phillips, Naomi G; Sonntag, Tim; Hao, Ergeng; Lee, Soon; Hai, Tsonwin; Montminy, Marc

    2015-03-03

    Increases in circulating glucagon during fasting maintain glucose balance by stimulating hepatic gluconeogenesis. Acute ethanol intoxication promotes fasting hypoglycemia through an increase in hepatic NADH, which inhibits hepatic gluconeogenesis by reducing the conversion of lactate to pyruvate. Here we show that acute ethanol exposure also lowers fasting blood glucose concentrations by inhibiting the CREB-mediated activation of the gluconeogenic program in response to glucagon. Ethanol exposure blocked the recruitment of CREB and its coactivator CRTC2 to gluconeogenic promoters by up-regulating ATF3, a transcriptional repressor that also binds to cAMP-responsive elements and thereby down-regulates gluconeogenic genes. Targeted disruption of ATF3 decreased the effects of ethanol in fasted mice and in cultured hepatocytes. These results illustrate how the induction of transcription factors with overlapping specificity can lead to cross-coupling between stress and hormone-sensitive pathways.

  18. Inhibitory effects of cefotaxime on the activity of mushroom tyrosinase.

    Science.gov (United States)

    Hu, Yong-Hua; Zhuang, Jiang-Xing; Yu, Feng; Cui, Yi; Yu, Wen-Wen; Yan, Chong-Ling; Chen, Qing-Xi

    2016-04-01

    Tyrosinase (EC 1.14.18.1) catalyzes both the hydroxylation of tyrosine into o-diphenols and the oxidation of o-diphenols into o-quinones that form brown or black pigments. In the present paper, cefotaxime, a cephalosporin antibacterial drug, was tested as an inhibitor of tyrosinase. The results show that cefotaxime inhibits both the monophenolase and diphenolase activities of tyrosinase. For the monophenolase activity, cefotaxime increased the lag time and decreased the steady-state activity with an IC50 of 3.2 mM. For the diphenolase activity, the inhibition by cefotaxime is reversible and mix-I type with an IC50 of 0.14 mM. The inhibition constants (K(I) and K(IS)) were determined to be 0.14 and 0.36 mM, respectively. The molecular mechanism of inhibition of tyrosinase by cefotaxime was determined by fluorescence quenching and molecular docking. The results demonstrated that cefotaxime was a static quencher of tyrosinase and that cefotaxime could dock favorably in the active site of tyrosinase. This research may offer a lead for designing and synthesizing novel and effective tyrosinase inhibitors in the future. Copyright © 2015 The Society for Biotechnology, Japan. Published by Elsevier B.V. All rights reserved.

  19. Sorafenib Has sEH Inhibitory Activity Which Contributes to Its Effect Profile in vivo

    OpenAIRE

    Liu, Jun-Yan; Park, See-Hyoung; Morisseau, Christophe; Hwang, Sung Hee; Hammock, Bruce D.; Weiss, Robert H.

    2009-01-01

    The advent of multi-kinase inhibitors targeting the VEGF-receptor has revolutionized the treatment of highly angiogenic malignances such as renal cell carcinoma. Interestingly, several such inhibitors are commercially available, and they each possess diverse specific beneficial and adverse effect profiles. In examining the structure of sorafenib, it was hypothesized that this compound would possess inhibitory effects on the soluble epoxide hydrolase (sEH), an enzyme with pleiotropic effects o...

  20. [Inhibitory effects and chemical basis of Eucalyptus orelliana wood meals on the growth of Alexandrium tamarense].

    Science.gov (United States)

    Yang, Wei-dong; Liu, Yu-rong; Liu, Jie-sheng; Liu, Zheng

    2008-08-01

    To provide information on the screen of newly and efficient algaecides in controlling harmful algal blooms (HABs), the effects of wood meals from Eucalyptus torelliana, Eucalyptus urophylla, Eucalyptus exserta on the growth of Alexandrium tamarense were observed and the chemical basis of the antialgal effect was discussed. The results show that the inhibitory activities of the three wood meals are different, and E. torelliana wood meals have the highest inhibitory activity. There are little differences in antialgal action between asepsis and rude wood meals, suggesting that some antialgal compounds from wood meals may be responsible for the inhibition and that microorganisms from wood meals have little effect on the inhibition. The acetone-water extract from E. torelliana wood meals is shown to have stronger inhibition on A. tamarense than that from ethyl acetate, water and methanol extracts. The acetone-water extract from E. torelliana wood meals was further divided into extract A, B, C and D and the inhibitory activities were compared. The extract D is shown to have highest inhibitory activity. 3 mg/L of the extract appears 81% inhibition rate to A. tamarense in the 3rd day. GC-MS show that extract D contains mostly ketones such as 4-hydroxy-3,5,6-trimethyl-4-(3-oxo-1-butenyl)-2-cyclohexen-1-one and 5,6,7,7a-tetrahydro-4,4,7a-trimethyl-2(4H)-benzofuranone. These results suggest that wood meals from E. torelliana had certain inhibitory effect on A. tamarense, and that ketones may be responsible for the inhibition.

  1. [Inhibitory effects of ursolic acid on diabetic retinopathy in mice].

    Science.gov (United States)

    Sun, Yan; Sun, Xiaonan; Wang, Fang; Liu, Shanshan

    2015-08-25

    To explore the protective effect and its mechanisms of intravitreal injection of ursolic acid (UA) on retinal injury in diabetic retinopathy (DR) mice. DR model was set up by using alloxan. 60 C57BL/6 male mice (clean animal, aged 12 weeks) were randomly and evenly divided into 6 groups: blank control group, DR model group, positive control group (triamcinolone acetonide), UA intervention groups (low, moderate and high dose). Mice were killed one week after drug intervention and the eyeballs were removed to prepare paraffin section. Retinal new blood vessel was examined by histopathological methods. The mRNA and protein expressions of vascular endothelial growth factor (VEGF), cyclooxygenase 2 (COX-2), and Matrix Metalloproteinase 2 (MMP-2) in retinal tissues were detected by real-time PCR and Western blotting, respectively. The superoxide dismutase (SOD) activity and malondialdehyde (MDA) content were detected by related kits. The HE and PAS staining showed uniform inner limiting membrane structure and orderly vascular endothelial cells in blank control group, and neovascularization was seldom detected. In DR model group, numerous new blood vessels were formed beyond inner limiting membrane. UA intervention group with low dose had almost the same results with DR group, while the results of UA intervention group with high dose were similar with positive control group, in which the inner limiting membrane structure was uniform and new blood vessels were seldom seen. The mRNA expressions of VEGF, COX-2, and MMP-2 in DR model group were significantly higher than those of blank control group (Pcontent of retinal tissue in DR model group was significantly higher than those of blank control group (P=0.001) and UA intervention groups with moderate and high dose (P=0.026, 0.007). The activity of SOD was significantly lower in DR model group than those of blank control group (P<0.001) and UA intervention groups with low, moderate and high dose (P=0.040, 0.021, 0.003). UA

  2. Acute effect of vigorous aerobic exercise on the inhibitory control in adolescents

    Directory of Open Access Journals (Sweden)

    Rodrigo Alberto Vieira Browne

    2016-06-01

    Full Text Available Abstract Objective: To assess the acute effect of vigorous aerobic exercise on the inhibitory control in adolescents. Methods: Controlled, randomized study with crossover design. Twenty pubertal individuals underwent two 30-minute sessions: (1 aerobic exercise session performed between 65% and 75% of heart rate reserve, divided into 5 min of warm-up, 20 min at the target intensity and 5 min of cool down; and (2 control session watching a cartoon. Before and after the sessions, the computerized Stroop test-Testinpacs™ was applied to evaluate the inhibitory control. Reaction time (ms and errors (n were recorded. Results: The control session reaction time showed no significant difference. On the other hand, the reaction time of the exercise session decreased after the intervention (p<0.001. The number of errors made at the exercise session were lower than in the control session (p=0.011. Additionally, there was a positive association between reaction time (Δ of the exercise session and age (r2=0.404, p=0.003. Conclusions: Vigorous aerobic exercise seems to promote acute improvement in the inhibitory control in adolescents. The effect of exercise on the inhibitory control performance was associated with age, showing that it was reduced at older age ranges.

  3. Diffused and sustained inhibitory effects of intestinal electrical stimulation on intestinal motility mediated via sympathetic pathway.

    Science.gov (United States)

    Zhao, Xiaotuan; Yin, Jieyun; Wang, Lijie; Chen, Jiande D Z

    2014-06-01

    The aims were to investigate the energy-dose response effect of intestinal electrical stimulation (IES) on small bowel motility, to compare the effect of forward and backward IES, and to explore the possibility of using intermittent IES and mechanism of IES on intestinal motility. Five dogs implanted with a duodenal cannula and one pair of intestinal serosal electrodes were studied in five sessions: 1) energy-dose response study; 2) forward IES; 3) backward IES; 4) intermittent IES vs. continuous IES; 5) administration of guanethidine. The contractile activity and tonic pressure of the small intestine were recorded. The duration of sustained effect after turning off IES was manually calculated. 1) IES with long pulse energy dose dependently inhibited contractile activity and tonic pressure of the small intestine (p intestine depended on the energy of IES delivered (p intestine. 5) Guanethidine blocked the inhibitory effect of IES on intestinal motility. IES with long pulses inhibits small intestinal motility; the effect is energy-dose dependent, diffused, and sustained. Intermittent IES has the same efficacy as the continuous IES in inhibiting small intestinal motility. Forward and backward IES have similar inhibitory effects on small bowel motility. This IES-induced inhibitory effect is mediated via the sympathetic pathway. © 2013 International Neuromodulation Society.

  4. Antihypertensive effects of silk fibroin hydrolysate by alcalase and purification of an ACE inhibitory dipeptide.

    Science.gov (United States)

    Zhou, Fengjuan; Xue, Zhaohui; Wang, Jiehua

    2010-06-09

    Silk fibroin, which is normally discarded as an industrial byproduct in clothing plants, was hydrolyzed with alcalase. Angiotensin I converting enzyme (ACE) inhibitory activities of the silk fibroin hydrolysates (SFH) were investigated, and the hydrolysate with hydrolysis degree of 17% exhibited the highest ACE inhibitory activity. At the tested 600 mg/kg.d and 1200 mg/kg x d doses, SFH significantly lowered blood pressure of spontaneously hypertensive rats (SHR) after chronic oral administration. SFH was further purified using consecutive chromatographic methods on Sephadex G-15 column and reverse phase high-performance liquid chromatography (RP-HPLC) on an octadecylsilane column. After its purity was confirmed by analytical RP-HPLC and capillary electrophoresis, one ACE inhibitory dipeptide was isolated, and its molecular mass and amino acid sequence were determined as 238.2 Da and Gly-Tyr, respectively, by LC-ESI/MS. The results of this study suggest that silk fibroin byproducts have the possibility to become an effective source for ACE inhibitory peptides.

  5. Impairment of inhibitory control processing related to acute psychotomimetic effects of cannabis.

    Science.gov (United States)

    Bhattacharyya, Sagnik; Atakan, Z; Martin-Santos, R; Crippa, J A; Kambeitz, J; Malhi, S; Giampietro, V; Williams, S; Brammer, M; Rubia, K; Collier, D A; McGuire, P K

    2015-01-01

    Cannabis use can induce acute psychotic symptoms and increase the risk of schizophrenia. Impairments in inhibitory control and processing are known to occur both under the influence of cannabis and in schizophrenia. Whether cannabis-induced impairment in inhibitory processing is related to the acute induction of psychotic symptoms under its influence is unclear. We investigated the effects of acute oral administration of 10mg of delta-9-tetrahydrocannabinol (delta-9-THC), the main psychoactive ingredient of cannabis, on inhibitory control and regional brain activation during inhibitory processing in humans and examined whether these effects are related to the induction of psychotic symptoms under its influence using a repeated-measures, placebo-controlled, double-blind, within-subject design. We studied thirty-six healthy, English-speaking, right-handed men with minimal previous exposure to cannabis and other illicit drugs twice using functional magnetic resonance imaging (fMRI) while they performed a response inhibition (Go/No-Go) task. Relative to placebo, delta-9-THC caused transient psychotic symptoms, anxiety, intoxication and sedation, inhibition errors and impaired inhibition efficiency. Severity of psychotic symptoms was directly correlated with inhibition error frequency and inversely with inhibition efficiency under the influence of delta-9-THC. Delta-9-THC attenuated left inferior frontal activation which was inversely correlated with the frequency of inhibition errors and severity of psychotic symptoms and positively with inhibition efficiency under its influence. These results provide experimental evidence that impairments in cognitive processes involved in the inhibitory control of thoughts and actions and inferior frontal function under the influence of cannabis may have a role in the emergence of transient psychotic symptoms under its influence. Copyright © 2014 Elsevier B.V. and ECNP. All rights reserved.

  6. Essential Oils from Ugandan Aromatic Medicinal Plants: Chemical Composition and Growth Inhibitory Effects on Oral Pathogens.

    Science.gov (United States)

    Ocheng, Francis; Bwanga, Freddie; Joloba, Moses; Softrata, Abier; Azeem, Muhammad; Pütsep, Katrin; Borg-Karlson, Anna-Karin; Obua, Celestino; Gustafsson, Anders

    2015-01-01

    The study assessed the growth inhibitory effects of essential oils extracted from ten Ugandan medicinal plants (Bidens pilosa, Helichrysum odoratissimum, Vernonia amygdalina, Hoslundia opposita, Ocimum gratissimum, Cymbopogon citratus, Cymbopogon nardus, Teclea nobilis, Zanthoxylum chalybeum, and Lantana trifolia) used traditionally in the management of oral diseases against oral pathogens. Chemical compositions of the oils were explored by GC-MS. Inhibitory effects of the oils were assessed on periodontopathic Porphyromonas gingivalis and Aggregatibacter actinomycetemcomitans and cariogenic Streptococcus mutans and Lactobacillus acidophilus using broth dilution methods at concentrations of 1%, 0.1%, and 0.01%. The most sensitive organism was A. actinomycetemcomitans. Its growth was markedly inhibited by six of the oils at all the concentrations tested. Essential oil from C. nardus exhibited the highest activity with complete growth inhibition of A. actinomycetemcomitans and P. gingivalis at all the three concentrations tested, the major constituents in the oil being mainly oxygenated sesquiterpenes. Most of the oils exhibited limited effects on L. acidophilus. We conclude that essential oils from the studied plants show marked growth inhibitory effects on periodontopathic A. actinomycetemcomitans and P. gingivalis, moderate effects on cariogenic S. mutans, and the least effect on L. acidophilus. The present study constitutes a basis for further investigations and development of certain oils into alternative antiplaque agents.

  7. Inhibitory effects of pepstatin A and mefloquine on the growth of Babesia parasites.

    Science.gov (United States)

    Munkhjargal, Tserendorj; AbouLaila, Mahmoud; Terkawi, Mohamad Alaa; Sivakumar, Thillaiampalam; Ichikawa, Madoka; Davaasuren, Batdorj; Nyamjargal, Tserendorj; Yokoyama, Naoaki; Igarashi, Ikuo

    2012-10-01

    We evaluated the inhibitory effects of pepstatin A and mefloquine on the in vitro and in vivo growths of Babesia parasites. The in vitro growth of Babesia bovis, B. bigemina, B. caballi, and B. equi was significantly inhibited (P mefloquine (50% inhibitory concentrations = 59.7, 56.7, 20.7, and 4 μM, respectively). Furthermore, both reagents either alone at a concentration of 5 mg/kg or in combinations (2.5/2.5 and 5/5 mg/kg) for 10 days significantly inhibited the in vivo growth of B. microti in mice. Mefloquine treatment was highly effective and the combination treatments were less effective than other treatments. Therefore, mefloquine may antagonize the actions of pepstatin A against babesiosis and aspartic proteases may play an important role in the asexual growth cycle of Babesia parasites.

  8. Inhibitory effects of Ge-132 (carboxyethyl germanium sesquioxide) derivatives on enkephalin-degrading enzymes.

    Science.gov (United States)

    Komuro, T; Kakimoto, N; Katayama, T; Hazato, T

    1986-10-01

    Twenty-eight species of carboxyethyl germanium sesquioxide (Ge-132) derivatives were examined for their inhibitory effects on enkephalin-degrading enzymes that were purified from monkey brain, the longitudinal muscle layer of bovine small intestine, and human cerebrospinal fluid (CSF). A series of the sulfurized Ge-132 derivatives showed strong inhibition of these purified enzymes. The most effective ones were Ge-014 and Ge-107, which showed IC50 values of 60 and 100 micrograms/ml, respectively, for dipeptidylcarboxypeptidase from the longitudinal muscle layer. They also exhibited inhibitory activity against aminopeptidase from human CSF, the IC50 values being 450 and 440 micrograms/ml, respectively. Furthermore, these compounds showed inhibition of dipeptidylaminopeptidase from monkey brain and the longitudinal muscle layer of bovine small intestine. These compounds are expected to have analgesic effects due to their inhibition of the degradation of endogenous opioid peptides.

  9. Inhibitory effects of xanthohumol from hops (Humulus lupulus L.) on human hepatocellular carcinoma cell lines.

    Science.gov (United States)

    Ho, Yi-Chien; Liu, Chi-Hsien; Chen, Chien-Nan; Duan, Kow-Jen; Lin, Ming-Tse

    2008-11-01

    Xanthohumol is one of the main flavonoids in hop extracts and in beer. Very few investigations of xanthohumol have studied hepatocellular carcinoma. In this study, the inhibitory effects of xanthohumol on human hepatocellular carcinoma cell lines were investigated. The IC(50) values of xanthohumol for two hepatocellular carcinoma cell lines and one normal hepatocyte cell line were 108, 166 and 211 microm, respectively. Normal murine hepatocyte cell line had more resistance to xanthohumol than hepatocellular carcinoma cell lines. Besides, the inhibitory effects of xanthohumol on human hepatocellular carcinoma cell lines were attributed to apoptosis as indicated in the results of flow cytometry, fluorescent nuclear staining and electrophoresis of oligonucleosomal DNA fragments. Hop xanthohumol was more efficient in the growth inhibition of hepatocellular carcinoma cell lines than the flavonoids silibinin and naringin from thistle and citrus. It was shown for the first time that xanthohumol from hops effectively inhibits proliferation of human hepatocellular carcinoma cells in vitro.

  10. Age Effect on Automatic Inhibitory Function of the Somatosensory and Motor Cortex: An MEG Study

    Directory of Open Access Journals (Sweden)

    Chia-Hsiung Cheng

    2018-03-01

    Full Text Available Age-related deficiency in the top-down modulation of cognitive inhibition has been extensively documented, whereas the effects of age on a bottom-up or automatic operation of inhibitory function were less investigated. It is unknown that whether the older adults (OA’ reduced behavioral performance and neural responses are due to the insufficient bottom-up processes. Compared to behavioral assessments which have been widely used to examine the top-down control of response inhibition, electrophysiological recordings are more suitable to probe the early-stage processes of automatic inhibitory function. Sensory gating (SG, a phenomenon of attenuated neural response to the second identical stimulus in a paired-pulse paradigm, is an indicator to assess automatic inhibitory function of the sensory cortex. On the other hand, electricity-induced beta rebound oscillation in a single-pulse paradigm reflects cortical inhibition of the motor cortex. From the neurophysiological perspective, SG and beta rebound oscillation are replicable indicators to examine the automatic inhibitory function of human sensorimotor cortices. Thus, the present study aimed to use a whole-head magnetoencephalography (MEG to investigate the age-related alterations of SG function in the primary somatosensory cortex (SI and of beta rebound oscillation in the primary motor cortex (MI in 17 healthy younger and 15 older adults. The Stimulus 2/Stimulus 1 (S2/S1 amplitude ratio in response to the paired-pulse electrical stimulation to the left median nerve was used to evaluate the automatic inhibitory function of SI, and the beta rebound response in the single-pulse paradigm was used to evaluate the automatic inhibitory function of MI. Although there were no significant age-related differences found in the SI SG ratios, the MI beta rebound power was reduced and peak latency was prolonged in the OA. Furthermore, significant association between the SI SG ratio and the MI beta rebound

  11. Age Effect on Automatic Inhibitory Function of the Somatosensory and Motor Cortex: An MEG Study

    Science.gov (United States)

    Cheng, Chia-Hsiung; Lin, Mei-Yin; Yang, Shiou-Han

    2018-01-01

    Age-related deficiency in the top-down modulation of cognitive inhibition has been extensively documented, whereas the effects of age on a bottom-up or automatic operation of inhibitory function were less investigated. It is unknown that whether the older adults (OA)’ reduced behavioral performance and neural responses are due to the insufficient bottom-up processes. Compared to behavioral assessments which have been widely used to examine the top-down control of response inhibition, electrophysiological recordings are more suitable to probe the early-stage processes of automatic inhibitory function. Sensory gating (SG), a phenomenon of attenuated neural response to the second identical stimulus in a paired-pulse paradigm, is an indicator to assess automatic inhibitory function of the sensory cortex. On the other hand, electricity-induced beta rebound oscillation in a single-pulse paradigm reflects cortical inhibition of the motor cortex. From the neurophysiological perspective, SG and beta rebound oscillation are replicable indicators to examine the automatic inhibitory function of human sensorimotor cortices. Thus, the present study aimed to use a whole-head magnetoencephalography (MEG) to investigate the age-related alterations of SG function in the primary somatosensory cortex (SI) and of beta rebound oscillation in the primary motor cortex (MI) in 17 healthy younger and 15 older adults. The Stimulus 2/Stimulus 1 (S2/S1) amplitude ratio in response to the paired-pulse electrical stimulation to the left median nerve was used to evaluate the automatic inhibitory function of SI, and the beta rebound response in the single-pulse paradigm was used to evaluate the automatic inhibitory function of MI. Although there were no significant age-related differences found in the SI SG ratios, the MI beta rebound power was reduced and peak latency was prolonged in the OA. Furthermore, significant association between the SI SG ratio and the MI beta rebound power, which was

  12. Inhibitory effects of pectenotoxins from marine algae on the polymerization of various actin isoforms.

    Science.gov (United States)

    Butler, Suzanne C; Miles, Christopher O; Karim, Amna; Twiner, Michael J

    2012-04-01

    Pectenotoxins (PTXs) are marine toxins produced by dinoflagellates and which accumulate in shellfish. There are at least 14 different analogs of PTX with slight variations in structure leading to different chemical properties and consequently different toxicities. Since preliminary studies have shown that the parent compound PTX1 targets actin, we investigated the effects of two analogs, PTX2 and PTX2 seco acid, on the polymerization and depolymerization of skeletal muscle actin, smooth muscle actin, cardiac muscle actin, and non-muscle actin. Optimized actin assays using fluorescently labeled skeletal muscle actin and SDS-PAGE were jointly used to determine the relative amounts of filamentous and globular actin formed during polymerization and depolymerization experiments. Our findings suggest that PTX2 causes a dose-dependent decrease in both the rate and yield of skeletal muscle actin polymerization (IC50 values of 44 and 177 nM; respectively), with no significant effects on depolymerization. Moreover, the inhibitory effects of PTX2 are conserved towards other actin isoforms (i.e., smooth muscle, cardiac muscle, and non-muscle), as the inhibitory effects on actin polymerization were also observed with similar IC50 values (range: 19-94 nM). No inhibitory effects on polymerization were observed for PTX2 seco acid, suggesting an intact lactone ring is necessary for bioactivity. Copyright © 2011 Elsevier Ltd. All rights reserved.

  13. Mannose-binding lectin impairs Leptospira activity through the inhibitory effect on the motility of cell.

    Science.gov (United States)

    Xu, Jun; Guo, Yijie; Nakamura, Shuichi; Islam, Md Shafiqul; Tomioka, Rintaro; Yoneyama, Hiroshi; Isogai, Emiko

    2015-02-01

    Mannose-binding lectin (MBL) plays key role in lectin pathway of innate immunity, and shows the ability of triggering opsonization intermediately. Substantial increase in the serum level of MBL has been confirmed during leptospirosis, which caused by a pathogenic spirochete, Leptospira. Leptospira has a fascinating locomotion pattern, which simultaneously gyrating and swimming forward, such motility enables that Leptospira is difficult to be captured by immune cells if without any assistance. In this study, the effect of mannose-binding lectin to Leptospira was quantitatively investigated by measuring some kinematic parameters, to discover the mechanism behind MBL-mediated immune responses during leptospiral infection. The results showed that mannose-binding lectin is capable of inhibiting the motility of Leptospira by transforming free swimming cells to tumbled rotating cells, resulted in the increase number of rotating cells. Otherwise, decrease in rotation rate of rotating cell has been observed. However, the swimming speed of swimming Leptospira cells showed no observable change under the effect of MBL. The inhibitory effect were only valid in a relatively short period, Leptospira cells regained their original motility after 2 h. This raises an interesting topic that Leptospira is somehow able to escape from the inhibitory effect of MBL by dragging such unfavorable molecules toward to the cell end and eventually throwing it out. The inhibitory effect of MBL on the motility of Leptospira is expected to provide a new insight into lectin pathway. Copyright © 2015 Elsevier GmbH. All rights reserved.

  14. [Inhibitory effect of diclofenac sodium on the proliferation of rabbit corneal epithelial cells in vitro].

    Science.gov (United States)

    Wu, Ningling; Du, Zhiyu

    2010-11-01

    To investigate the inhibitory effect of diclofenac sodium on rabbit corneal epithelial cells (RCECs) in vitro and explore its pharmacological mechanism. The fresh rabbit cornea was cultured to obtain the primary RCECs, and RCECs of passage 2 were used in this research. The cells were divided into experimental groups, the cells in which were incubated with different concentrations (18.18, 27.27, 36.36, 45.45, 54.55 μg/ml) of diclofenac sodium, and control group. The effect of diclofenac sodium on the proliferation of cells was measured by methyl thiazolyl thiazolium (MTT) assay 24, 48 and 72 h after incubation. While the RCECs were divided into experimental groups, the cells in which were incubated with 9 and 12.5 μg/ml diclofenac sodium, and control group. The cell cycle and apoptotic rate were observed by flow cytometer. MTT assay showed that diclofenac sodium had obvious inhibitory effect on RCECs, and the inhibition rate was increasing along with the increasing concentration of diclofenac sodium and the incubation time(Pdiclofenac sodium, the cells in G0/G1 phase were obviously increased, and the apoptosis cusp and apoptotic rate were increased. Diclofenac sodium exerts significant inhibitory effect on RCECs in a dosage-dependent manner, and it may function by inducing cell apoptosis and ceasing cell cycles.

  15. Inhibitory effect of vanillin on cellulase activity in hydrolysis of cellulosic biomass.

    Science.gov (United States)

    Li, Yun; Qi, Benkun; Wan, Yinhua

    2014-09-01

    Pretreatment of lignocellulosic material produces a wide variety of inhibitory compounds, which strongly inhibit the following enzymatic hydrolysis of cellulosic biomass. Vanillin is a kind of phenolics derived from degradation of lignin. The effect of vanillin on cellulase activity for the hydrolysis of cellulose was investigated in detail. The results clearly showed that vanillin can reversibly and non-competitively inhibit the cellulase activity at appropriate concentrations and the value of IC50 was estimated to be 30 g/L. The inhibition kinetics of cellulase by vanillin was studied using HCH-1 model and inhibition constants were determined. Moreover, investigation of three compounds with similar structure of vanillin on cellulase activity demonstrated that aldehyde group and phenolic hydroxyl groups of vanillin had inhibitory effect on cellulase. These results provide valuable and detailed information for understanding the inhibition of lignin derived phenolics on cellulase. Copyright © 2014 Elsevier Ltd. All rights reserved.

  16. Inhibitory effect of Sphagnum palustre extract and its bioactive compounds on aromatase activity

    Directory of Open Access Journals (Sweden)

    Hee Jeong Eom

    2016-09-01

    Full Text Available Sphagnum palustre (a moss has been traditionally used in Korea for the cure of several diseases such as cardiac pain and stroke. In this research, the inhibitory effect of S. palustre on aromatase (cytochrome P450 19, CYP19 activity was studied. [1β-3H] androstenedione was used as a substrate and incubated with S. palustre extract and recombinant human CYP19 in the presence of NADPH. S. palustre extract inhibited aromatase in a concentration-dependent manner (IC50 value: 36.4 ± 8.1 µg/mL. To elucidate the major compounds responsible for the aromatase inhibitory effects of S. palustre extract, nine compounds were isolated from the extract and tested for their inhibition of aromatase activity. Compounds 1, 6, and 7 displayed aromatase inhibition, while the inhibition by the other compounds was negligible.

  17. Novel Inhibitory Effect of N-(2-Hydroxycyclohexylvaliolamine on Melanin Production in a Human Skin Model

    Directory of Open Access Journals (Sweden)

    Bum-Ho Bin

    2014-07-01

    Full Text Available Hyper-pigmentation causes skin darkness and medical disorders, such as post-inflammatory melanoderma and melasma. Therefore, the development of anti-melanogenic agents is important for treating these conditions and for cosmetic production. In our previous paper, we demonstrated that the anti-diabetic drug voglibose, a valiolamine derivative, is a potent anti-melanogenic agent. In addition, we proposed an alternative screening strategy to identify valiolamine derivatives with high skin permeability that act as anti-melanogenic agents when applied topically. In this study, we synthesized several valiolamine derivatives with enhanced lipophilicity and examined their inhibitory effects in a human skin model. N-(2-hydroxycyclohexylvaliolamine (HV possesses a stronger inhibitory effect on melanin production than voglibose in a human skin model, suggesting that HV is a more potent anti-melanogenic agent for the skin.

  18. Inhibitory effects of Ajowan (Trachyspermum ammi) ethanolic extract on A. ochraceus growth and ochratoxin production

    OpenAIRE

    MURTHY, Pushpa Srinivas; BORSE, Babasaheb Bhaskarrao; KHANUM, Hafeeza; SRINIVAS, Pullabhatla

    2009-01-01

    Ajowan is an aromatic seed spice that has a medicinal value. In this paper Ajowan Ethanolic Extract (AEE), which was prepared from Ajowan seeds, was assessed for antibacterial and antifungal activity against selected pathogenic bacteria and fungi by agar well diffusion assay. AEE exhibited considerable inhibitory effects against all the organisms tested. Emphasis of the study was on the affect of AEE on the mycelial growth and spore germination of toxigenic fungi A. ochraceus. Cultures were i...

  19. Inhibitory effect of azo dyes on ammoni-n oxidation by nitrtosomonas ...

    African Journals Online (AJOL)

    The potential inhibitory effect of five azo dyes on ammonia-N oxidation was investigated. Ammonia-N oxidation was inhibited by the dyes: Mordant Black 17, Direct Red 2, Reactive Red 4, Reactive Yellow 2 and Direct Blue 14 at the concentrations (0.01mgL-1 to 100mgL-1) tested. Inhibition of ammonia-N oxidation ...

  20. A comparison about the inhibitory effect of curcunmin and Avastin on the rat corneal neovascularization

    Directory of Open Access Journals (Sweden)

    Yi Wu

    2013-06-01

    Full Text Available AIM: To compare the inhibitory effect of curcunmin and Avastin on the rat corneal neovascularization(CNV, and approach the mechanism of the curcunmin's inhibition. METHODS: CNV was established in thirty SD rats by alkaline burning. Rats were divided equally to group A and group B at random. In group A, right eyes were experimental group A1, treated by 40μmol/L curcunmin solution, and left eyes were control group A2, treated by 0.09% sodium chloride. In group B, right eyes were experimental group group B1, treated by 5g/L avastin, and left eyes were control group B2, treated by 0.09% sodium chloride. Cornea and aqueous humor were collected by time spot. The capillary vessels were study, and the expressions of VEGF were detected by Enzyme-Linked immunosorbnent Assay(ELISA. RESULTS: No toxic effects of the drugs were found. The capillary vessels in experimental group were less than those of control group(P<0.01. No statistical different of the capillary vessels between two drugs were found. The expressions of VEGF in experimental group were less than those in control group(P<0.01. The expressions of VEGF in B1 group were less than in group A1. CONCLUSION: The inhibitory effect to CNV of curcunmin and avastin have no statistical different in the experiment, but curcunmin has the less inhibitory effect to the expressions of VEGF than avastin. Curcunmin may have other mechanism in the inhibitory action on CNV.

  1. Effects of hypertonic saline on macrophage migration inhibitory factor in traumatic conditions

    OpenAIRE

    KIM, JUNG-YOUN; CHOI, SUNG-HYUK; YOON, YOUNG-HOON; MOON, SUNG-WOO; CHO, YOUNG-DUCK

    2012-01-01

    Trauma-induced suppression of cellular immune function contributes to sepsis, multiple organ dysfunction syndrome (MODS) and mortality. Macrophage migration inhibitory factor (MIF) has been revealed to be central to several immune responses. However, the role of MIF in trauma-like conditions is unknown. Therefore, the present study evaluated MIF in macrophages and polymorphonuclear neutrophils (PMNs). The effects of hypertonic saline (HTS) on lipopolysaccharide (LPS)-induced MIF levels were e...

  2. Inhibitory Effect of Waste Glass Powder on ASR Expansion Induced by Waste Glass Aggregate

    Directory of Open Access Journals (Sweden)

    Shuhua Liu

    2015-10-01

    Full Text Available Detailed research is carried out to ascertain the inhibitory effect of waste glass powder (WGP on alkali-silica reaction (ASR expansion induced by waste glass aggregate in this paper. The alkali reactivity of waste glass aggregate is examined by two methods in accordance with the China Test Code SL352-2006. The potential of WGP to control the ASR expansion is determined in terms of mean diameter, specific surface area, content of WGP and curing temperature. Two mathematical models are developed to estimate the inhibitory efficiency of WGP. These studies show that there is ASR risk with an ASR expansion rate over 0.2% when the sand contains more than 30% glass aggregate. However, WGP can effectively control the ASR expansion and inhibit the expansion rate induced by the glass aggregate to be under 0.1%. The two mathematical models have good simulation results, which can be used to evaluate the inhibitory effect of WGP on ASR risk.

  3. Acute neuropharmacological effects of atomoxetine on inhibitory control in ADHD children: A fNIRS study

    Directory of Open Access Journals (Sweden)

    Masako Nagashima

    2014-01-01

    Full Text Available The object of the current study is to explore the neural substrate for effects of atomoxetine (ATX on inhibitory control in school-aged children with attention deficit hyperactivity disorder (ADHD using functional near-infrared spectroscopy (fNIRS. We monitored the oxy-hemoglobin signal changes of sixteen ADHD children (6–14 years old performing a go/no-go task before and 1.5 h after ATX or placebo administration, in a randomized, double-blind, placebo-controlled, crossover design. Sixteen age- and gender-matched normal controls without ATX administration were also monitored. In the control subjects, the go/no-go task recruited the right inferior and middle prefrontal gyri (IFG/MFG, and this activation was absent in pre-medicated ADHD children. The reduction of right IFG/MFG activation was acutely normalized after ATX administration but not placebo administration in ADHD children. These results are reminiscent of the neuropharmacological effects of methylphenidate to up-regulate reduced right IFG/MFG function in ADHD children during inhibitory tasks. As with methylphenidate, activation in the IFG/MFG could serve as an objective neuro-functional biomarker to indicate the effects of ATX on inhibitory control in ADHD children. This promising technique will enhance early clinical diagnosis and treatment of ADHD in children, especially in those with a hyperactivity/impulsivity phenotype.

  4. Synergistic inhibitory effect of citral with selected phenolics against Zygosaccharomyces bailii.

    Science.gov (United States)

    Rivera-Carriles, Karla; Argaiz, Alvaro; Palou, Enrique; López-Malo, Aurelio

    2005-03-01

    Antifungal susceptibilities of Zygosaccharomyces bailii to individual and binary mixtures of citral with selected phenolics were evaluated to identify synergistic combinations. Individual effects of citral, vanillin, thymol, carvacrol, and eugenol concentrations and combined effects of citral with the other phenolic compounds on the growth of Z. bailii were evaluated in potato dextrose agar, adjusted with sucrose to a water activity of 0.99 or 0.95, and hydrochloric acid to pH 4.5 or 3.5. MICs for individual and binary antimicrobial mixtures were identified and then transformed to fractional inhibitory concentrations. Inhibitory concentrations of citral and vanillin were higher than 650 ppm, whereas for thymol, eugenol, and carvacrol, concentrations were lower than 250 ppm for several of the studied water activity-pH conditions. Combining citral with the other phenolic compounds, fractional inhibitory concentration (FIC) and FIC(Index) varied from 0.216 to 0.582. FIC(Index) demonstrated synergistic effects on Z. bailii inhibition when citral was used in combination with vanillin, thymol, carvacrol, or eugenol. Therefore, the relative amount of antimicrobials could be greatly reduced.

  5. Effect of Jatropha curcas Peptide Fractions on the Angiotensin I-Converting Enzyme Inhibitory Activity

    Science.gov (United States)

    Segura-Campos, Maira R.; Peralta-González, Fanny; Castellanos-Ruelas, Arturo; Chel-Guerrero, Luis A.; Betancur-Ancona, David A.

    2013-01-01

    Hypertension is one of the most common worldwide diseases in humans. Angiotensin I-converting enzyme (ACE) plays an important role in regulating blood pressure and hypertension. An evaluation was done on the effect of Alcalase hydrolysis of defatted Jatropha curcas kernel meal on ACE inhibitory activity in the resulting hydrolysate and its purified fractions. Alcalase exhibited broad specificity and produced a protein hydrolysate with a 21.35% degree of hydrolysis and 34.87% ACE inhibition. Ultrafiltration of the hydrolysate produced peptide fractions with increased biological activity (24.46–61.41%). Hydrophobic residues contributed substantially to the peptides' inhibitory potency. The 5–10 and Jatropha kernel have potential applications in alternative hypertension therapies, adding a new application for the Jatropha plant protein fraction and improving the financial viability and sustainability of a Jatropha-based biodiesel industry. PMID:24224169

  6. Inhibitory effects of flavonoids on biofilm formation by Staphylococcus aureus that overexpresses efflux protein genes.

    Science.gov (United States)

    Lopes, Laênia Angélica Andrade; Dos Santos Rodrigues, Jéssica Bezerra; Magnani, Marciane; de Souza, Evandro Leite; de Siqueira-Júnior, José P

    2017-06-01

    This study evaluated the efficacy of glycone (myricitrin, hesperidin and phloridzin) and aglycone flavonoids (myricetin, hesperetin and phloretin) in inhibiting biofilm formation by Staphylococcus aureus RN4220 and S. aureus SA1199B that overexpress the msrA and norA efflux protein genes, respectively. The minimum inhibitory concentration (MIC) and minimum biofilm inhibitory concentration (MBIC 50 - defined as the lowest concentration that resulted in ≥50% inhibition of biofilm formation) of flavonoids were determined using microdilution in broth procedures. The flavonoids showed MIC >1024 μg/mL against S. aureus RN4220 and S. aureus SA1199B; however, these compounds at lower concentrations (1-256 μg/mL) showed inhibitory effects on biofilm formation by these strains. Aglycone flavonoids showed lower MBIC 50 values than their respective glycone forms. The lowest MBIC 50 values (1 and 4 μg/mL) were observed against S. aureus RN4220. Myricetin, hesperetin and phloretin exhibited biofilm formation inhibition >70% for S. aureus RN4220, and lower biofilm formation inhibition against S. aureus SA1199B. These results indicate that sub-MICs of the tested flavonoids inhibit biofilm formation by S. aureus strains that overexpress efflux protein genes. These effects are more strongly established by aglycone flavonoids. Copyright © 2017 Elsevier Ltd. All rights reserved.

  7. The Inhibitory Effect of Prunella vulgaris L. on Aldose Reductase and Protein Glycation

    Directory of Open Access Journals (Sweden)

    Hong Mei Li

    2012-01-01

    Full Text Available To evaluate the aldose reductase (AR enzyme inhibitory ability of Prunella vulgaris L. extract, six compounds were isolated and tested for their effects. The components were subjected to in vitro bioassays to investigate their inhibitory assays using rat lens aldose reductase (rAR and human recombinant AR (rhAR. Among them, caffeic acid ethylene ester showed the potent inhibition, with the IC50 values of rAR and rhAR at 3.2±0.55 μM and 12.58±0.32 μM, respectively. In the kinetic analyses using Lineweaver-Burk plots of 1/velocity and 1/concentration of substrate, this compound showed noncompetitive inhibition against rhAR. Furthermore, it inhibited galactitol formation in a rat lens incubated with a high concentration of galactose. Also it has antioxidative as well as advanced glycation end products (AGEs inhibitory effects. As a result, this compound could be offered as a leading compound for further study as a new natural products drug for diabetic complications.

  8. Salomon: '97 E and P looking strongest in 9 years

    International Nuclear Information System (INIS)

    Anon.

    1997-01-01

    Based on companies' disclosed spending plans, 1997 is shaping up to be the strongest year-ahead outlook in 9 years, according to Salomon Bros. Inc. Salomon Bros.' conclusion stems from its 15th annual survey of worldwide oil and gas exploration and production spending. The survey, released last month, included 125 US independents, 97 Canadian companies, 103 companies outside the US and Canada, and 15 majors. Significantly, when the 15% growth experienced in 1996 is combined with the 1997 outlook, it represents the strongest indicator of 2-year activity in the past 15 years, said Salomon Bros. Double-digit spending growth is projected in all regions for 1997, the analyst said. Salomon Bros. said a higher percentage of companies' E and P budgets are being allocated to offshore projects, driven in part by attractive prospects, 3D seismic technology, and increased operational efficiencies

  9. Potent inhibitory effect of alcoholic beverages upon gastrointestinal passage of food and gallbladder emptying.

    Science.gov (United States)

    Kasicka-Jonderko, Anna; Jonderko, Krzysztof; Bożek, Małgorzata; Kamińska, Magdalena; Mgłosiek, Patrycja

    2013-12-01

    Current knowledge about the effect of alcoholic beverages on postprandial functioning of the digestive system is scarce and inconsistent. This study addresses their influence upon meal movement along the gut and meal-induced gallbladder emptying. Three examination blocks involved each 12 healthy volunteers. Ingestion of a solid 1485 kJ meal was followed by intake of 400 ml beer (4.7%vol), 200 ml red wine (13.7%vol) or 100 ml whisky (43.5%vol) or matching volumes of control fluids. Gastric myoelectrical activity and emptying, orocecal transit and gallbladder emptying was monitored noninvasively. Alcoholic beverages (beer, red wine, whisky) caused a significant slowdown of the gastric evacuation of the solid meal, the delay being the more potent, the greater was the concentration of ethanol. This inhibitory effect was not caused by interference with the gastric myoelectric activity. Alcoholic beverages produced only by fermentation (beer, red wine), at odds with the effect of their counterpartying aqueous ethanol solutions, did not elongate the orocecal transit of the solid food. Products of distillation-whisky and high proof ethanol solution--elicited a profound delay of the orocecal transit. Alcoholic beverages exerted an inhibitory effect upon the meal-stimulated gallbladder emptying, the magnitude of which increased in the order: beer → red wine → whisky. Alcoholic beverages exert an inhibitory effect upon the gastric emptying of a solid food and the meal-induced gallbladder emptying, whereas the effect upon the orocecal transit depends on the type of a beverage-whisky elicits a delay but beer or red wine are devoid of this effect.

  10. Inhibitory site of α-hairpinin peptide from tartary buckwheat has no effect on its antimicrobial activities.

    Science.gov (United States)

    Cui, Xiaodong; Du, Jingjing; Li, Jiao; Wang, Zhuanhua

    2018-03-02

    Antimicrobial peptides (AMPs) are known to play important roles in the innate host defense mechanisms of most living organisms. Protease inhibitors from plants potently inhibit the growth of a variety of pathogenic bacteria and fungi. Therefore, there are excellent candidates for the development of novel antimicrobial agents. In this study, an antimicrobial peptide derived from tartary buckwheat seeds (FtAMP) was obtained by gene cloning, expression and purification, which exhibited inhibitory activity toward trypsin. Furthermore, the relationship between the antimicrobial and inhibitory activities of FtAMP was investigated. Two mutants (FtAMP-R21A and FtAMP-R21F) were generated through site-directed mutagenesis. Inhibitory activity analysis showed that both FtAMP-R21A and FtAMP-R21F lost trypsin-inhibitory activity. However, FtAMP-R21A and FtAMP-R21F showed novel inhibitory activities against elastase and α-chymotrypsin, respectively, suggesting that Arg-21 in the inhibitory site loop is specific for the inhibitory activity of FtAMP against trypsin. Antimicrobial assays showed that all three peptides exhibited strong antifungal activity against Trichoderma koningii, Rhizopus sp., and Fusarium oxysporum. These results showed that the changes in FtAMP inhibitory site have no effect on their antifungal properties.

  11. Inhibitory effects of polyphenols from grape pomace extract on collagenase and elastase activity.

    Science.gov (United States)

    Wittenauer, Judith; Mäckle, Sonja; Sußmann, Daniela; Schweiggert-Weisz, Ute; Carle, Reinhold

    2015-03-01

    Breakdown and disorganization of extracellular matrix proteins like collagen, fibronectin and elastin are main characteristics of skin aging due to the enhanced activation of proteolytic enzymes such as collagenases and elastases. Inhibition of their enzymatic activities by natural plant compounds might be a promising approach to prevent extrinsic skin aging. Especially polyphenols are supposed to interact with those enzymes due to their molecular nature. In our investigation, extracts of pomace from Riesling grapes were analyzed for their inhibitory properties on collagenase as well as elastase. Crude grape pomace extract showed a dose-dependent inhibitory activity against both enzymes with IC50-values of 20.3μg/ml and 14.7μg/ml for collagenase and elastase activity, respectively. The extracts were fractionated into four fractions containing phenolic compounds differing in chemical structure and polarity. Except for the stilbene containing fraction, all other fractions showed inhibitory effects on both enzyme activities. The most pronounced impact was found for the hydrophilic low molecular weight polyphenols containing the free phenolic acids. In particular, gallic acid showed considerable inhibition values. EGCG was used as a positive control and showed a dose-dependent inhibition of collagenase activity (IC50=0.9mM). Copyright © 2015 Elsevier B.V. All rights reserved.

  12. Inhibitory effects of Colocasia esculenta (L.) Schott constituents on aldose reductase.

    Science.gov (United States)

    Li, Hong Mei; Hwang, Seung Hwan; Kang, Beom Goo; Hong, Jae Seung; Lim, Soon Sung

    2014-08-27

    The goal of this study was to determine the rat lens aldose reductase-inhibitory effects of 95% ethanol extracts from the leaves of C. esculenta and, its organic solvent soluble fractions, including the dichloromethane (CH2Cl2), ethyl acetate (EtOAc), n-butanol (BuOH) and water (H2O) layers, using dl-glyceraldehyde as a substrate. Ten compounds, namely tryptophan (1), orientin (2), isoorientin (3), vitexin (4), isovitexin (5), luteolin-7-O-glucoside (6), luteolin-7-O-rutinoside (7), rosmarinic acid (8), 1-O-feruloyl-d-glucoside (9) and 1-O-caffeoyl-d-glucoside (10) were isolated from the EtOAc and BuOH fractions of C. esculenta. The structures of compounds 1-10 were elucidated by spectroscopic methods and comparison with previous reports. All the isolates were subjected to an in vitro bioassay to evaluate their inhibitory activity against rat lens aldose reductase. Among tested compounds, compounds 2 and 3 significantly inhibited rat lens aldose reductase, with IC50 values of 1.65 and 1.92 μM, respectively. Notably, the inhibitory activity of orientin was 3.9 times greater than that of the positive control, quercetin (4.12 μM). However, the isolated compounds showed only moderate ABTS+ [2,29-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid)] activity. These results suggest that flavonoid derivatives from Colocasia esculenta (L.) Schott represent potential compounds for the prevention and/or treatment of diabetic complications.

  13. Inhibitory effects of Angelica pubescens f. biserrata on 5-lipoxygenase and cyclooxygenase.

    Science.gov (United States)

    Liu, J H; Zschocke, S; Reininger, E; Bauer, R

    1998-08-01

    Linoleic acid, osthol, osthenol and two polyacetylenes, falcarindiol and 11(S),16(R)-dihydroxyoctadeca-9Z,17-diene-12,14-diyn-1 -yl acetate were found to be the most active compounds responsible for the inhibitory activity of the dichloromethane extract of the roots of Angelica pubescens f. biserrata on 5-lipoxygenase (5-LO) and cyclooxygenase (COX-1) in vitro. They showed prominent inhibitory effect on 5-LO with IC50 values of 27.9 microM, 36.2 microM, 43.1 microM, 9.4 microM and 24.0 microM, respectively. Linoleic acid, osthenol, falcarindiol and 11(S), 16(R)-dihydroxyoctadeca-9Z,17-diene-12,14-diyn-1-yl acetate exhibited inhibitory activity on COX-1 with IC50 values of 13.3 microM, 64.3 microM, 66.0 microM and 73.3 microM.

  14. Inhibitory effects of chickpea and Tribulus terrestris on lipase, α-amylase and α-glucosidase.

    Science.gov (United States)

    Ercan, Pınar; El, Sedef Nehir

    2016-08-15

    The total saponin content and its in vitro bioaccessibilities in Tribulus terrestris and chickpea were determined by a static in vitro digestion method (COST FA1005 Action INFOGEST). Also, in vitro inhibitory effects of the chosen food samples on lipid and starch digestive enzymes were determined by evaluating the lipase, α-amylase and α-glucosidase activities. The tested T. terrestris and chickpea showed inhibitory activity against α-glucosidase (IC50 6967 ± 343 and 2885 ± 85.4 μg/ml, respectively) and α-amylase (IC50 343 ± 26.2 and 167 ± 6.12 μg/ml, respectively). The inhibitory activities of T. terrestris and chickpea against lipase were 15.3 ± 2.03 and 9.74 ± 1.09 μg/ml, respectively. The present study provides the first evidence that these food samples (T. terrestris, chickpea) are potent inhibitors of key enzymes in digestion of carbohydrates and lipids in vitro. Copyright © 2016 Elsevier Ltd. All rights reserved.

  15. Evaluation of Traditional Indian Antidiabetic Medicinal Plants for Human Pancreatic Amylase Inhibitory Effect In Vitro

    Directory of Open Access Journals (Sweden)

    Sudha Ponnusamy

    2011-01-01

    Full Text Available Pancreatic α-amylase inhibitors offer an effective strategy to lower the levels of post prandial hyperglycemia via control of starch breakdown. Eleven Ayurvedic Indian medicinal plants with known hypoglycemic properties were subjected to sequential solvent extraction and tested for α-amylase inhibition, in order to assess and evaluate their inhibitory potential on pancreatic α-amylase. Analysis of 91 extracts, showed that 10 exhibited strong Human Pancreatic Amylase (HPA inhibitory potential. Of these, 6 extracts showed concentration dependent inhibition with IC50 values, namely, cold and hot water extracts from Ficus bengalensis bark (4.4 and 125 μgmL-1, Syzygium cumini seeds (42.1 and 4.1 μgmL-1, isopropanol extracts of Cinnamomum verum leaves (1.0 μgmL-1 and Curcuma longa rhizome (0.16 μgmL-1. The other 4 extracts exhibited concentration independent inhibition, namely, methanol extract of Bixa orellana leaves (49 μgmL-1, isopropanol extract from Murraya koenigii leaves (127 μgmL-1, acetone extracts from C. longa rhizome (7.4 μgmL-1 and Tribulus terrestris seeds (511 μgmL-1. Thus, the probable mechanism of action of the above fractions is due to their inhibitory action on HPA, thereby reducing the rate of starch hydrolysis leading to lowered glucose levels. Phytochemical analysis revealed the presence of alkaloids, proteins, tannins, cardiac glycosides, flavonoids, saponins and steroids as probable inhibitory compounds.

  16. Inhibitory effects of acyclic nucleoside phosphonates on human hepatitis B virus and duck hepatitis B virus infections in tissue culture

    NARCIS (Netherlands)

    R.A. Heijtink; J. Kruining; G.A. de Wilde; J. Balzarini; E. de Clercq; S.W. Schalm (Solko)

    1994-01-01

    textabstractThe inhibitory effects of the 9-(2-phosphonylmethoxyethyl)adenine-related compounds (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)-adenine, (S)-9-(3-fluoro-2-phosphonylmethoxypropyl)adenine, (R)-9-(2-phosphonylmethoxypropyl)adenine,

  17. Inhibitory effects of di-O-demethylcurcumin on interleukin-1β-induced interleukin-6 production from human gingival fibroblasts

    Directory of Open Access Journals (Sweden)

    Nuntana Aroonrerk

    2012-12-01

    Conclusion: Di-O-demethylcurcumin exhibited an inhibitory effect on the production of IL-6 by IL-1β-induced HGFs and can thus serve as a lead compound with its inhibiting property for IL-6 production.

  18. Prescription Stimulants' Effects on Healthy Inhibitory Control, Working Memory, and Episodic Memory: A Meta-analysis.

    Science.gov (United States)

    Ilieva, Irena P; Hook, Cayce J; Farah, Martha J

    2015-06-01

    The use of prescription stimulants to enhance healthy cognition has significant social, ethical, and public health implications. The large number of enhancement users across various ages and occupations emphasizes the importance of examining these drugs' efficacy in a nonclinical sample. The present meta-analysis was conducted to estimate the magnitude of the effects of methylphenidate and amphetamine on cognitive functions central to academic and occupational functioning, including inhibitory control, working memory, short-term episodic memory, and delayed episodic memory. In addition, we examined the evidence for publication bias. Forty-eight studies (total of 1,409 participants) were included in the analyses. We found evidence for small but significant stimulant enhancement effects on inhibitory control and short-term episodic memory. Small effects on working memory reached significance, based on one of our two analytical approaches. Effects on delayed episodic memory were medium in size. However, because the effects on long-term and working memory were qualified by evidence for publication bias, we conclude that the effect of amphetamine and methylphenidate on the examined facets of healthy cognition is probably modest overall. In some situations, a small advantage may be valuable, although it is also possible that healthy users resort to stimulants to enhance their energy and motivation more than their cognition.

  19. Inhibitory Effect of Curcumin on Candida-albicans compared with Nystatin: an in-vitro Study

    Directory of Open Access Journals (Sweden)

    Neda Babaii

    2016-10-01

    Full Text Available Introduction: Curcumin is the active ingredient in the traditional herbal remedy and dietary spice turmeric (Curcuma longa. Curcumin has a surprisingly wide range of beneficial properties, including anti-inflammatory, antioxidant, chemopreventive and chemotherapeutic activity. on basis of recent studies; it has antifungal and antibacterial effects. The aim of this study was in-vitro evaluation of antifungal effect of curcumin on candida albicans and comparing it with nystatin. Methods: after preparing curcumin powder, 3 laboratory methods were used to evaluate antifungal effect. The first method was cell count technique, used to evaluate the amount of candida albicans after time, in different concentrations of curcumin in Dimethyl sulfoxide (DMSO. The second was cup bioassay, in which inhibitory a zone of curcumin in DMSO was evaluated in sabouraud culture plates; and in third method, inhibitory zones of dried disks; which contained curcumin in DMSO were evaluated. Results: the result of all three methods showed that curcumin has antifungal effect and this effect increases in more concentrations. Conclusion: curcumin has apparent and dose dependent antifungal effect on candida albicans.

  20. Macrophage migration inhibitory factor inhibits the antiinflammatory effects of glucocorticoids via glucocorticoid-induced leucine zipper.

    Science.gov (United States)

    Fan, Huapeng; Kao, Wenping; Yang, Yuan H; Gu, Ran; Harris, James; Fingerle-Rowson, Günter; Bucala, Richard; Ngo, Devi; Beaulieu, Elaine; Morand, Eric F

    2014-08-01

    Glucocorticoids remain a mainstay in the treatment of rheumatoid arthritis (RA). Dose-dependent adverse effects highlight the need for therapies that regulate glucocorticoid sensitivity to enable dosage reduction. Macrophage migration inhibitory factor (MIF) is a proinflammatory protein that has been implicated in the pathogenesis of RA; it impairs glucocorticoid sensitivity via MAPK phosphatase 1 (MKP-1) inhibition. The intracellular protein glucocorticoid-induced leucine zipper (GILZ) mimics the effects of glucocorticoids in models of RA, but whether it represents a target for the modulation of glucocorticoid sensitivity remains unknown. We undertook this study to investigate whether GILZ is involved in the regulation of glucocorticoid sensitivity by MIF. GILZ expression was studied in the presence and absence of MIF, and the role of GILZ in the MIF-dependent regulation of the glucocorticoid sensitivity mediator MKP-1 was studied at the level of expression and function. GILZ expression was significantly inhibited by endogenous MIF, both basally and during responses to glucocorticoid treatment. The effects of MIF on GILZ were dependent on the expression and Akt-induced nuclear translocation of the transcription factor FoxO3A. GILZ was shown to regulate the expression of MKP-1 and consequent MAPK phosphorylation and cytokine release. MIF exerts its effects on MKP-1 expression and MAPK activity through inhibitory effects on GILZ. These findings suggest a previously unsuspected interaction between MIF and GILZ and identify GILZ as a potential target for the therapeutic regulation of glucocorticoid sensitivity. Copyright © 2014 by the American College of Rheumatology.

  1. Inhibitory effect of Lactobacillus rhamnosus on pathogenic bacteria isolated from women with bacterial vaginosis

    Directory of Open Access Journals (Sweden)

    Gita Eslami

    2014-06-01

    Full Text Available Background: Considering the high prevalence of bacterial vaginosis and its association with urinary tract infection in women and treatment of gynecologic problems occur when a high recurrence of bacterial vaginosis is often treated with antibiotics. The purpose of this study is to investigate the inhibitory effect of Lactobacillus rhamnosus on pathogenic bacteria isolated from women with bacterial vaginosis, respectively.Materials and Methods: 96 samples from women with bacterial vaginosis discharge referred to health centers dependent Shahid Beheshti University in 91-92 were taken by a gynecologist with a dacron swab and put in sterile tubes containing TSB broth and Thioglycollate broth and were immediately sent to the lab location in cold chain for the next stages of investigation. From Thioglycollate and TSB medium was cultured on blood agar and EMB and Palkam and Differential diagnosis environments, and then incubated for 24 h at 37°C. Strains of Lactobacillus rhamnosus were cultured in MRSA environment and were transfered to the lab. After purification of pathogenic bacteria, MIC methods and antibiogram, Lactobacillus rhamnosus inhibitory effect on pathogenic bacteria is checked. Statistical analysis was done by SPSS software v.16.Results: The results of this study show the inhibitory effect of Lactobacillus rhamnosus on some pathogenic bacteria that cause bacterial vaginosis, including Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus saprophyticus, Streptococcus agalactiae, Entrococcus, Listeria monocytogenes and E.Coli. Microscopic examination of stained smears of the large number of Lactobacillus and pathogenic bacteria showed reduced. The prevalence of abnormal vaginal discharge, history of drug use means of preventing pregnancy and douching, respectively, 61%, 55%, 42% and 13% respectively. Significant difference was observed between the use and non-use of IUD in women with bacterial vaginosis infection

  2. Diffusive versus Displacive Contact Plasticity of Nanoscale Asperities: Temperature- and Velocity-Dependent Strongest Size.

    Science.gov (United States)

    Guo, Wei; Wang, Zhao; Li, Ju

    2015-10-14

    We predict a strongest size for the contact strength when asperity radii of curvature decrease below 10 nm. The reason for such strongest size is found to be correlated with the competition between the dislocation plasticity and surface diffusional plasticity. The essential role of temperature is calculated and illustrated in a comprehensive asperity size-strength-temperature map taking into account the effect of contact velocity. Such a map should be essential for various phenomena related to nanoscale contacts such as nanowire cold welding, self-assembly of nanoparticles and adhesive nanopillar arrays, as well as the electrical, thermal, and mechanical properties of macroscopic interfaces.

  3. Inhibitory effect of celecoxib on agomelatine metabolism in vitro and in vivo

    Directory of Open Access Journals (Sweden)

    He JY

    2018-03-01

    Full Text Available Jiayang He,1 Ping Fang,2 Xiang Zheng,2 Chenchen Wang,2 Tenghui Liu,2 Bowen Zhang,2 Jian Wen,2 Ren-ai Xu3 1Department of Pharmacy, The First Hospital of Jiaxing, Jiaxing, Zhejiang, China; 2Department of Pharmacology, School of Pharmacy of Wenzhou Medical University, Wenzhou, Zhejiang, China; 3Department of Pharmacy, The First Affiliated Hospital of Wenzhou Medical University, Wenzhou, Zhejiang, China Aim: The aim of this study was to study the effect of celecoxib on agomelatine metabolism in vitro and in vivo. Methods: Ten healthy male Sprague–Dawley rats were randomly divided into 2 groups: Group A (control group and Group B (30 mg/kg celecoxib. Then a single dose of 20 mg/kg agomelatine was administered orally 30 min after administration of celecoxib. In an in vitro study, celecoxib with a series of concentrations was added to an incubation mixture containing recombinant human CYP2C9, human or rat liver microsomes to determine the half-maximal inhibitory concentration on the metabolism of agomelatine. Moreover, a mechanism study was performed to determine the inhibitory effect of celecoxib on CYP2C9. Results: The results showed that a single dose of 30 mg/kg celecoxib significantly increased the area under the concentration-time curve and maximum concentration of agomelatine. In addition, celecoxib inhibited the metabolism of agomelatine in the in vitro studies, which was determined to be by a competitive mechanism on CYP2C9. Those results indicated that celecoxib has an inhibitory effect on the metabolism of agomelatine both in vivo and in vitro. Conclusion: Thus, more attention should be paid when celecoxib is administered combined with agomelatine. Keywords: agomelatine, liver microsomes, pharmacokinetics, celecoxib, CYP2C9

  4. Considering body mass differences, who are the world's strongest women?

    Science.gov (United States)

    Vanderburgh, P M; Dooman, C

    2000-01-01

    Allometric modeling (AM) has been used to determine the world's strongest body mass-adjusted man. Recently, however, AM was shown to demonstrate body mass bias in elite Olympic weightlifting performance. A second order polynomial (2OP) provided a better fit than AM with no body mass bias for men and women. The purpose of this study was to apply both AM and 2OP models to women's world powerlifting records (more a function of pure strength and less power than Olympic lifts) to determine the optimal model approach as well as the strongest body mass-adjusted woman in each event. Subjects were the 36 (9 per event) current women world record holders (as of Nov., 1997) for bench press (BP), deadlift (DL), squat (SQ), and total (TOT) lift (BP + DL + SQ) according to the International Powerlifting Federation (IPF). The 2OP model demonstrated the superior fit and no body mass bias as indicated by the coefficient of variation and residuals scatterplot inspection, respectively, for DL, SQ, and TOT. The AM for these three lifts, however, showed favorable bias toward the middle weight classes. The 2OP and AM yielded an essentially identical fit for BP. Although body mass-adjusted world records were dependent on the model used, Carrie Boudreau (U.S., 56-kg weight class), who received top scores in TOT and DL with both models, is arguably the world's strongest woman overall. Furthermore, although the 2OP model provides a better fit than AM for this elite population, a case can still be made for AM use, particularly in light of theoretical superiority.

  5. Inhibitory effect of mycoplasma-released arginase. Activity in mixed-lymphocyte and tumour cell cultures

    DEFF Research Database (Denmark)

    Claesson, M H; Tscherning, T; Nissen, Mogens Holst

    1990-01-01

    inhibition can be reversed by addition of excess arginine to the culture medium. Antisera raised against non-fermenting, but not against fermenting, mycoplasma species block the inhibitory effect of MAE. SDS-PAGE separation of MAE disclosed a broad band at 60 kDa which contained arginase activity when...... assayed in MLC and cell proliferation culture. SDS-PAGE followed by western blotting and reaction with antisera raised against non-fermenting mycoplasma species demonstrated a band at 43 kDa common for these micro-organisms....

  6. Modulatory effect of caffeic acid on cholinesterases inhibitory properties of donepezil.

    Science.gov (United States)

    Agunloye, Odunayo Michael; Oboh, Ganiyu

    2017-09-22

    Background Donepezil hydrochloride commonly used in the management of Alzheimer's disease (AD), exhibiting its inhibitory effects on acetylcholinesterase and butyrylcholinesterase activity thereby enhance cognitive function. Caffeic acid member of hydroxycinnamic acid is widely present in human diet. This study aims to investigate influence of caffeic acid on acetylcholinesterase and butyrylcholinesterase inhibitory properties of donepezil (in vitro). Methods 5 mg of donepezil was dissolved in 50 mL distilled water while 10 mg of caffeic acid was dissolved in 100 mL distilled water. Therefore, mixtures of samples were prepared as follows: A2=donepezil 0.075 mg/mL+caffeic acid 0.025 mg/mL; A3=donepezil 0.050 mg/mL+caffeic acid 0.050 mg/mL; A4=donepezil 0.025 mg/mL+caffeic acid 0.075 mg/mL. All samples were kept in the refrigerator at 4 °C for subsequent analysis. Results The result showed that all the combinations show an inhibitory effect on acetylcholinesterase and butyrylcholinesterase activity in vitro, with the combination A4=donepezil 0.025 mg/mL+caffeic acid 0.075 mg/mL had significant (pdonepezil 0.025 mg/mL+caffeic acid 0.075 mg/mL and A3=donepezil 0.050 mg/mL+caffeic acid 0.050 mg/mL had highest inhibitory effect against FeSO4 and SNP induced lipid peroxidation in rat brain homogenate in vitro respectively. Moreover, all the samples exhibit antioxidant properties as typified by their ability to chelate iron (II) ion (Fe2+), hydroxyl radical (OH٭) radical scavenging ability and ferric reducing property (FRAP). Conclusions Therefore, the combination of caffeic acid with donepezil enhances the antioxidant properties of donepezil. The combination of caffeic acid with donepezil could be a therapeutic aid in the management of AD, possibly with fewer side effects of donepezil. Nevertheless, the combination donepezil 0.025 mg/mL+caffeic acid 0.075 mg/mL acid look promising.

  7. Renin inhibitory effect of synthetic phosphorylethanolamine (PE-104) in the rat.

    Science.gov (United States)

    Miyazaki, M; Yamamoto, K; Hosoki, K

    1976-12-01

    1. The renin inhibitory effect of 2-[4-(4'-chlorophenoxy)phenoxy - acetylamino]ethylphosphoryl-ethanolamine (PE-104) was examined both in vitro and in vivo. 2. PE-104 inhibited the rate of angiotensin formation from dog renin and renin substrate reaction. The Ki value was 2 mmol/l and the inhibition was competitive. 3. In normotensive rats, infusion of PE-104 abolished the increases of blood pressure and plasma angiotensin I concentration due to renin injection. In renal hypertensive rats, infusion of PE-104 decreased blood pressure and this was associated with a decrease of plasma angiotensin I concentration. 4. These observations confirm that PE-104 is a renin inhibitor.

  8. Inhibitory Effect of Chrysanthemum zawadskii Herbich var. latilobum Kitamura Extract on RANKL-Induced Osteoclast Differentiation

    Directory of Open Access Journals (Sweden)

    Dong Ryun Gu

    2013-01-01

    Full Text Available Chrysanthemum zawadskii Herbich var. latilobum Kitamura, known as “Gujulcho” in Korea, has been used in traditional medicine to treat various inflammatory diseases, including rheumatoid arthritis. However, these effects have not been tested on osteoclasts, the bone resorbing cells that regulate bone metabolism. Here, we investigated the effects of C. zawadskii Herbich var. latilobum Kitamura ethanol extract (CZE on osteoclast differentiation induced by treatment with the receptor activator of NF-κB ligand (RANKL. CZE inhibited osteoclast differentiation and formation in a dose-dependent manner. The inhibitory effect of CZE on osteoclastogenesis was due to the suppression of ERK activation and the ablation of RANKL-stimulated Ca2+-oscillation via the inactivation of PLCγ2, followed by the inhibition of CREB activation. These inhibitory effects of CZE resulted in a significant repression of c-Fos expression and a subsequent reduction of NFATc1, a key transcription factor for osteoclast differentiation, fusion, and activation in vitro and in vivo. These results indicate that CZE negatively regulates osteoclast differentiation and may be a therapeutic candidate for the treatment of various bone diseases, such as postmenopausal osteoporosis, rheumatoid arthritis, and periodontitis.

  9. Mechanistic Study of the Inhibitory Effect of Kaempferol on Uterine Fibroids In Vitro.

    Science.gov (United States)

    Li, Yanxia; Ding, Zhaoxia; Wu, Chuanzhong

    2016-12-08

    BACKGROUND This study examined the effect of kaempferol on uterine fibroids in vitro and the underlying mechanism, and investigated the potential of kaempferol as a clinical drug for the treatment of uterine fibroids. MATERIAL AND METHODS Uterine fibroid tissue and surrounding smooth muscle tissue were collected for primary culture. Different concentrations of kaempferol (12 μM, 24 μM, and 48 μM) were used to treat the cells for 24, 48, and 72 hours. Ethanol was used in the control group. A CCK-8 colorimetric assay was used to detect cell proliferation. Real-time PCR and immunoblot were used to detect estrogen receptor (ER), insulin-like growth factor-1 (IGF-1), and vascular endothelial growth factor (VEGF) levels in mRNA and protein. RESULTS The differences in proliferation at different time points and concentrations of kaempferol were statistically significant. The inhibitory effect of kaempferol on mRNA levels of ER and IGF, and protein levels of ER, VEGF, and IGF-1 were positively correlated with kaempferol concentration. Changes in kaempferol concentration showed no effect on VEGF mRNA expression. Treatment with kaempferol significantly lowered myocardin levels in uterine fibroid tissue compared to normal uterine smooth muscle (PKaempferol might be used for clinical treatment of uterine fibroids due to its inhibitory effect on the proliferation of uterine fibroids cells.

  10. Inhibitory effect of extracellular purine nucleotide and nucleoside concentrations on T cell proliferation

    Energy Technology Data Exchange (ETDEWEB)

    Weiler, Monica [Department of Medicine III and Transfusion Medicine, University Hospital Grosshadern, Ludwig-Maximilians-University, Munich (Germany); Schmetzer, Helga [Helmholtz Center Munich (Germany); German Research Center for Environmental Health, Munich (Germany); Braeu, Marion; Buhmann, Raymund [Helmholtz Center Munich (Germany); German Research Center for Environmental Health, Munich (Germany); Department of Medicine III and Transfusion Medicine, University Hospital Grosshadern, Ludwig-Maximilians-University, Munich (Germany)

    2016-11-15

    The release of nucleic acids and derivatives after tissue-injury may affect cellular immune-response. We studied the impact of extracellular ribo-, desoxyribonucleotides and nucleosides on T-cell immunity. Peripheral-blood-mononuclear-cells (PBMCs) or isolated CD3{sup +}T-cells obtained from 6 healthy donors were stimulated via CD3/CD28 Dynabeads or dendritic cells (DCs) in the presence or absence of pyrimidine-, purine-nucleotides and -nucleosides (range 2–200 µM). Addition of deoxy-, guanosine-triphosphate (dGTP, GTP) and guanosine resulted concentration dependent in a complete, adenosine-triphosphate (ATP) in a partial inhibition of the induced T-cell-proliferation. Deoxyadenosine-triphosphate (dATP), adenosine and the pyrimidine-ribo- and -deoxyribonucleotides displayed no inhibitory capacity. Inhibitory effects of dGTP and GTP, but not of guanosine and ATP were culture-media-dependent and could be almost abrogated by use of the serum-free lymphocyte-culture-media X-Vivo15 instead of RPMI1640 with standard-supplementation. In contrast to RPMI1640, X-Vivo15 resulted in a significant down-regulation of the cell-surface-located ectonucleotidases CD39 (Ecto-Apyrase) and CD73 (Ecto-5′-Nucleotidase), critical for the extracellular nucleotides-hydrolysis to nucleosides, explaining the loss of inhibition mediated by dGTP and GTP, but not Guanosine. In line with previous findings ATP was found to exert immunosuppressive effects on T-cell-proliferation. Purine-nucleotides, dGTP and GTP displayed a higher inhibitory capacity, but seem to be strictly dependent on the microenvironmental conditions modulating the responsiveness of the respective T-lymphocytes. Further evaluation of experimental and respective clinical settings should anticipate these findings.

  11. Inhibitory effect of extracellular purine nucleotide and nucleoside concentrations on T cell proliferation

    International Nuclear Information System (INIS)

    Weiler, Monica; Schmetzer, Helga; Braeu, Marion; Buhmann, Raymund

    2016-01-01

    The release of nucleic acids and derivatives after tissue-injury may affect cellular immune-response. We studied the impact of extracellular ribo-, desoxyribonucleotides and nucleosides on T-cell immunity. Peripheral-blood-mononuclear-cells (PBMCs) or isolated CD3 + T-cells obtained from 6 healthy donors were stimulated via CD3/CD28 Dynabeads or dendritic cells (DCs) in the presence or absence of pyrimidine-, purine-nucleotides and -nucleosides (range 2–200 µM). Addition of deoxy-, guanosine-triphosphate (dGTP, GTP) and guanosine resulted concentration dependent in a complete, adenosine-triphosphate (ATP) in a partial inhibition of the induced T-cell-proliferation. Deoxyadenosine-triphosphate (dATP), adenosine and the pyrimidine-ribo- and -deoxyribonucleotides displayed no inhibitory capacity. Inhibitory effects of dGTP and GTP, but not of guanosine and ATP were culture-media-dependent and could be almost abrogated by use of the serum-free lymphocyte-culture-media X-Vivo15 instead of RPMI1640 with standard-supplementation. In contrast to RPMI1640, X-Vivo15 resulted in a significant down-regulation of the cell-surface-located ectonucleotidases CD39 (Ecto-Apyrase) and CD73 (Ecto-5′-Nucleotidase), critical for the extracellular nucleotides-hydrolysis to nucleosides, explaining the loss of inhibition mediated by dGTP and GTP, but not Guanosine. In line with previous findings ATP was found to exert immunosuppressive effects on T-cell-proliferation. Purine-nucleotides, dGTP and GTP displayed a higher inhibitory capacity, but seem to be strictly dependent on the microenvironmental conditions modulating the responsiveness of the respective T-lymphocytes. Further evaluation of experimental and respective clinical settings should anticipate these findings.

  12. Inhibitory Effect of Nisin on Listeria monocytogenes Inoculated into Surimi and Minced Meat

    Directory of Open Access Journals (Sweden)

    Masoud Rezaei

    2012-02-01

    Full Text Available Background & Objective: Listeria monocytogenes has already established as an important food born pathogen which induce listeriosis in human. Use of bacteriocins to provide food safety has been increased dramatically. Nisin has a wide spectrum inhibitory effect than the other bacteriocins and inhibits food-borne pathogens such as L. monocytogenes and many other Gram-positive spoilage microorganisms. The purpose of this study was to investigate the inhibitory effect of Nisin on population of Listeria monocytogenes and the role of changes in food components on the antilisterial properties of Nisin. Materials & Methods: The minced meat and surimi samples were inoculated by 1×104 cfu/g of L. monocytogenes. Then samples exposed to Nisin at the levels of 500 or 1000 IU/g were prepared. All treatments after packaging in plastic bags were kept for 12 days at refrigerator temperature. Samples were cultured on CHROMagarTM Listeria every 2 days and the number of listeria monocytogenes was counted. Results: two different concentrations of Nisin (500 or 1000 IU/g was not able to inhibit L. monocytogenes below the acceptable level for raw food (100 cells per g in minced meat and surimi of silver carp. But the number of bacteria reduces more in fish surimi as compared to the mince meal. Also, antilisterial activity of Nisin was reduced during the storage period. Conclusion: Inhibitory property of Nisin against L. monocytogenes in surimi significantly was higher than the minced (P<0.05. So it is possible the antilisterial properties of Nisin will increase by elimination of some enzymes during processing.

  13. Effects of nanosuspension and inclusion complex techniques on the in vitro protease inhibitory activity of naproxen

    Energy Technology Data Exchange (ETDEWEB)

    Dharmalingam, Senthil Rajan; Chidambaram, Kumarappan; Srinivasan, Ramamurthy; Nadaraju, Shamala, E-mail: dsenthilrajan@yahoo.co.in [School of Pharmacy, International Medical University, Bukit Jalil, Kuala Lumpur (Malaysia)

    2014-01-15

    This study investigated the effects of nanosuspension and inclusion complex techniques on in vitro trypsin inhibitory activity of naproxen—a member of the propionic acid derivatives, which are a group of antipyretic, analgesic, and non-steroidal anti-inflammatory drugs. Nanosuspension and inclusion complex techniques were used to increase the solubility and anti-inflammatory efficacy of naproxen. The evaporative precipitation into aqueous solution (EPAS) technique and the kneading methods were used to prepare the nanosuspension and inclusion complex of naproxen, respectively. We also used an in vitro protease inhibitory assay to investigate the anti-inflammatory effect of modified naproxen formulations. Physiochemical properties of modified naproxen formulations were analyzed using UV, IR spectra, and solubility studies. Beta-cyclodextrin inclusion complex of naproxen was found to have a lower percentage of antitryptic activity than a pure nanosuspension of naproxen did. In conclusion, nanosuspension of naproxen has a greater anti-inflammatory effect than the other two tested formulations. This is because the nanosuspension formulation reduces the particle size of naproxen. Based on these results, the antitryptic activity of naproxen nanosuspension was noteworthy; therefore, this formulation can be used for the management of inflammatory disorders. (author)

  14. Inhibitory Effects of Thai Essential Oils on Potentially Aflatoxigenic Aspergillus parasiticus and Aspergillus flavus.

    Science.gov (United States)

    Jantapan, Kittika; Poapolathep, Amnart; Imsilp, Kanjana; Poapolathep, Saranya; Tanhan, Phanwimol; Kumagai, Susumu; Jermnak, Usuma

    2017-01-01

     The antiaflatoxigenic and antifungal activities of essential oils (EOs) of finger root (Boesenbergia rotunda (L.) Mansf.), pine (Pinus pinaster), rosewood (Aniba rosaedora), Siam benzoin (Styrax tonkinensis), Thai moringa (Moringa oleifera), and ylang ylang (Cananga odorata) were tested for Aspergillus parasiticus and Aspergillus flavus in potato dextrose broth. Aflatoxin B 1 (AFB 1 ) was extracted from culture using a QuEChERS-based extraction procedure and analyzed with high performance liquid chromatography (HPLC) coupled to a fluorescence detector. EO of pine showed the greatest inhibition of growth and AFB 1 production of A. parasiticus, followed by EOs of rosewood, finger root, Siam benzoin, and ylang ylang. EO of finger root gave the best inhibitory effects on A. flavus, followed by EOs of rosewood, pine, ylang ylang, and Siam benzoin. EO of Thai moringa did not show any significant inhibition of aflatoxigenic fungi. The antiaflatoxigenic activities of EOs correlated with their antifungal activities in the dosedependent manner. Comparison of the application of the five selected EOs in peanut pods by direct and vapor exposure indicated that the AFB 1 production inhibitory effects of the five EOs by direct exposure were faster and more effective than by vapor exposure. EO of finger root showed the best inhibition of AFB 1 production of A. flavus in peanut pods by direct exposure, followed by EOs of pine, rosewood, ylang ylang, and Siam benzoin.

  15. Role of histamine in the inhibitory effects of phycocyanin in experimental models of allergic inflammatory response

    Directory of Open Access Journals (Sweden)

    D. Remirez

    2002-01-01

    Full Text Available It has recently been reported that phycocyanin, a biliprotein found in the blue-green microalgae Spirulina, exerts anti-inflammatory effects in some animal models of inflammation. Taking into account these findings, we decided to elucidate whether phycocyanin might exert also inhibitory effects in the induced allergic inflammatory response and on histamine release from isolated rat mast cells. In in vivo experiments, phycocyanin (100, 200 and 300 mg/kg post-orally (p.o. was administered 1 h before the challenge with 1 μg of ovalbumin (OA in the ear of mice previously sensitized with OA. One hour later, myeloperoxidase activity and ear edema were assessed. Phycocyanin significantly reduced both parameters. In separate experiments, phycocyanin (100 and 200 mg/kg p.o. also reduced the blue spot area induced by intradermal injections of histamine, and the histamine releaser compound 48/80 in rat skin. In concordance with the former results, phyco-cyanin also significantly reduced histamine release induced by compound 48/80 from isolated peritoneal rat mast cells. The inhibitory effects of phycocyanin were dose dependent. Taken together, our results suggest that inhibition of allergic inflammatory response by phycocyanin is mediated, at least in part, by inhibition of histamine release from mast cells.

  16. The inhibitory effect of benzenethiol on the cresolase and catecholase activities of mushroom tyrosinase.

    Science.gov (United States)

    Saboury, A A; Zolghadri, S; Haghbeen, K; Moosavi-Movahedi, A A

    2006-12-01

    The inhibitory effect of benzenethiol on the cresolase and catecholase activities of mushroom tyrosinase (MT) have been investigated at two temperatures of 20 and 30 degrees C in 10 mM phosphate buffer solution, pHs 5.3 and 6.8. The results show that benzenethiol can inhibit both activities of mushroom tyrosinase competitively. The inhibitory effect of benzenethiol on the cresolase activity is more than the catecholase activity of MT. The inhibition constant (K(i)) value at pH 5.3 is smaller than that at pH 6.8 for both enzyme activities. However, the K(i) value increases in cresolase activity and decreases in catecholase activity due to the increase of temperature from 20 to 30 degrees C at both pHs. Moreover, the effect of temperature on K(i) value is more at pH 6.8 for both cresolase and catecholase activities. The type of binding process is different in the two types of MT activities. The binding process for catecholase inhibition is only entropy driven, which means that the predominant interaction in the active site of the enzyme is hydrophobic, meanwhile the electrostatic interaction can be important for cresolase inhibition due to the enthalpy driven binding process. Fluorescence and circular studies also show a minor change in the tertiary structure, without any change in the secondary structure, of the enzyme due to the electrostatic interaction in cresolase inhibition by benzenethiol at acidic pH.

  17. Effects of sleep deprivation on inhibitory biomarkers of schizophrenia: implications for drug development.

    Science.gov (United States)

    Ettinger, Ulrich; Kumari, Veena

    2015-11-01

    Development of drugs for the treatment of the clinical symptoms and cognitive deficits of schizophrenia is unsatisfactory, with many initially promising compounds not showing beneficial effects in clinical studies. Experimental model systems of schizophrenia combined with well-validated biomarkers are urgently needed to provide early indicators of effectiveness. Herein, we argue that experimentally controlled sleep deprivation represents a translational model system that can be studied in combination with neurocognitive biomarkers. Specifically, we review data on the psychotomimetic effects of sleep deprivation in healthy human beings and provide evidence of the psychosis-like deficits in translational inhibitory biomarkers-prepulse inhibition and antisaccades-that occur after sleep deprivation. These data support the use of the sleep deprivation model in combination with biomarkers with excellent psychometric properties and well-characterised neural mechanisms, such as prepulse inhibition and antisaccades, to substantially advance development of drugs with antipsychotic or pro-cognitive effects. Copyright © 2015 Elsevier Ltd. All rights reserved.

  18. Identification of tumor promoters by their inhibitory effect on intercellular transfer of lucifer yellow.

    Science.gov (United States)

    Budunova, I V; Mittelman, L A; Belitsky, G A

    1989-01-01

    The effect of the tumor promoters 12-O-tetradecanoylphorbol-13-acetate (TPA), mezerein, teleocidin, anthralin, the Ca2+-ionophore A23187, butylated hydroxytoluene (BHT), dichlorodiphenyltrichloroethane (DDT) and phenobarbital (PB) on lucifer yellow transfer in cultures of SV-40-transformed Djungarian hamster fibroblasts was studied. TPA, mezerein, teleocidin, A23187, DDT and BHT exerted a strong inhibitory effect on cell-to-cell dye transfer. Anthralin uncoupled cells in 3 experiments out of 6. PB appeared to enhance lucifer yellow transfer. Sodium nitrite, a substance with unknown promoting activity, effectively uncoupled cells. All the promoters investigated had a reversible effect on the dye transfer. The value of the dye transfer method for promoter screening is discussed.

  19. Tyrosinase Inhibitory and Anti-oxidative Effects of Lactic Acid Bacteria Isolated from Dairy Cow Feces.

    Science.gov (United States)

    Ji, Keunho; Cho, Youn Su; Kim, Young Tae

    2018-03-01

    Overproduction and accumulation of melanin cause a number of skin diseases. The inhibitors of tyrosinase are important for the treatment of skin diseases associated with hyper-pigmentation after UV exposure and application in cosmetics for whitening and depigmentation. Reactive oxygen species (ROS) including hydrogen peroxide are generated by chemical substances and metabolic intermediates and cause various diseases including cancer and heart diseases. We have isolated four different lactic acid bacteria (LAB) strains from dairy cow feces and investigated the tyrosinase inhibition and anti-oxidative effects of culture filtrates prepared from the isolated bacteria, which are designated as EA3, EB2, PC2, and PD3. To investigate optimal culture conditions isolated LAB strains, the measurements of tyrosinase inhibitory and anti-oxidative activities were performed. The results of tyrosinase inhibitory activities revealed that Enterococcus sp. EA3 showed about 65% at culture conditions (14 h, 30 °C, pH 8, and 0% NaCl), Enterococcus sp. EB2 about 65% at culture conditions (12 h, 30 °C, pH 9, and 0% NaCl), Pediococcus sp. PC2 about 80% at culture conditions (20 h, 30 °C, pH 6, and 0% NaCl), and Pediococcus sp. PD3 about 80% at culture conditions (20 h, 30 °C, pH 8, and 0% NaCl), respectively. In addition, anti-oxidative activities against four different LAB strains showed approximately more than 30% at optimal conditions for the measurements of tyrosinase inhibitory activities. From the results, we have suggested that the isolated four LAB strains could be useful for a potential agent for developing anti-oxidants and tyrosinase inhibitors.

  20. Inhibitory Effect and Mechanism of Arctium lappa Extract on NLRP3 Inflammasome Activation

    Directory of Open Access Journals (Sweden)

    Young-Kyu Kim

    2018-01-01

    Full Text Available Arctium lappa (A. lappa, Compositae, is considered a potential source of nutrition and is used as a traditional medicine in East Asian countries for centuries. Although several studies have shown its biological activities as an anti-inflammatory agent, there have been no reports on A. lappa with regard to regulatory role in inflammasome activation. The purpose of this study was to investigate the inhibitory effects of A. lappa extract (ALE on NLRP3 inflammasome activation and explore the underlying mechanisms. We found that ALE inhibited IL-1β secretion from NLRP3 inflammasome activated bone marrow derived macrophages but not that secreted by NLRC4 and AIM2 inflammasomes activation. Mechanistic studies revealed that ALE suppressed the ATPase activity of purified NLRP3 and reduced mitochondrial reactive oxygen species (mROS generated during NLRP3 activation. Therefore, the inhibitory effect of ALE on NLRP3 inflammasome might be attributed to its ability to inhibit the NLRP3 ATPase function and attenuated the mROS during inflammasome activation. In addition, ALE significantly reduced the LPS-induced increase of plasma IL-1β in mouse peritonitis model. These results provide evidence of novel anti-inflammatory mechanisms of A. lappa, which might be used for therapeutic applications in the treatment of NLRP3 inflammasome-associated inflammatory disorders.

  1. Inhibitory Effect and Mechanism of Arctium lappa Extract on NLRP3 Inflammasome Activation

    Science.gov (United States)

    Kim, Young-Kyu; Koppula, Sushruta; Shim, Do-Wan; In, Eun-Jung; Kwak, Su-Bin; Yu, Sang-Hyeun

    2018-01-01

    Arctium lappa (A. lappa), Compositae, is considered a potential source of nutrition and is used as a traditional medicine in East Asian countries for centuries. Although several studies have shown its biological activities as an anti-inflammatory agent, there have been no reports on A. lappa with regard to regulatory role in inflammasome activation. The purpose of this study was to investigate the inhibitory effects of A. lappa extract (ALE) on NLRP3 inflammasome activation and explore the underlying mechanisms. We found that ALE inhibited IL-1β secretion from NLRP3 inflammasome activated bone marrow derived macrophages but not that secreted by NLRC4 and AIM2 inflammasomes activation. Mechanistic studies revealed that ALE suppressed the ATPase activity of purified NLRP3 and reduced mitochondrial reactive oxygen species (mROS) generated during NLRP3 activation. Therefore, the inhibitory effect of ALE on NLRP3 inflammasome might be attributed to its ability to inhibit the NLRP3 ATPase function and attenuated the mROS during inflammasome activation. In addition, ALE significantly reduced the LPS-induced increase of plasma IL-1β in mouse peritonitis model. These results provide evidence of novel anti-inflammatory mechanisms of A. lappa, which might be used for therapeutic applications in the treatment of NLRP3 inflammasome-associated inflammatory disorders. PMID:29576797

  2. Inhibitory Effect and Mechanism ofArctium lappaExtracton NLRP3Inflammasome Activation.

    Science.gov (United States)

    Kim, Young-Kyu; Koppula, Sushruta; Shim, Do-Wan; In, Eun-Jung; Kwak, Su-Bin; Kim, Myong-Ki; Yu, Sang-Hyeun; Lee, Kwang-Ho; Kang, Tae-Bong

    2018-01-01

    Arctium lappa (A. lappa) , Compositae, is considered a potential source of nutrition and is used as a traditional medicine in East Asian countries for centuries. Although several studies have shown its biological activities as an anti-inflammatory agent, there have been no reports on A. lappa with regard to regulatory role in inflammasome activation. The purpose of this study was to investigate the inhibitory effects of A. lappa extract (ALE) on NLRP3 inflammasome activation and explore the underlying mechanisms. We found that ALE inhibited IL-1 β secretion from NLRP3 inflammasome activated bone marrow derived macrophages but not that secreted by NLRC4 and AIM2 inflammasomes activation. Mechanistic studies revealed that ALE suppressed the ATPase activity of purified NLRP3 and reduced mitochondrial reactive oxygen species (mROS) generated during NLRP3 activation. Therefore, the inhibitory effect of ALE on NLRP3 inflammasome might be attributed to its ability to inhibit the NLRP3 ATPase function and attenuated the mROS during inflammasome activation. In addition, ALE significantly reduced the LPS-induced increase of plasma IL-1 β in mouse peritonitis model. These results provide evidence of novel anti-inflammatory mechanisms of A. lappa , which might be used for therapeutic applications in the treatment of NLRP3 inflammasome-associated inflammatory disorders.

  3. Electrochemical evaluation of the inhibitory effects of weak acids on Zygosaccharomyces bailii.

    Science.gov (United States)

    Zhao, Jinsheng; Yang, Zhenyu; Wang, Min; Lu, Yao; Yang, Zhengyu

    2004-12-01

    The changes in intracellular redox activity or in mitochondrial electron transport could be taken as indications of the changes in the physiological state of living cells, based on which a mediated electrochemical method was purposed to evaluate the inhibitory effects of weak acids on Zygosaccharomyces bailii, a known food spoilage yeast. The dual mediator systems menadione/ferricyanide and 2,6-dichlorophenolindophenol/ferricyanide were employed as probes to detect the variance in intracellular redox activity and in mitochondrial electron flux, respectively. Measurements were made with a microelectrode voltammetric method to assay the ferrocyanide accumulations arising from menadione- or 2,6-dichlorophenolindophenol-mediated reduction of ferricyanide by Z. bailii suspensions by the presence or absence of increasing concentrations of weak acids. The results obtained from 2 h of incubation showed that the variance in electrochemical response revealed some physiological information underlying the inhibitory effects of weak acid on the yeast. For the first time, it was shown that the mediated electrochemical method provides an adjunct to the conventional method based on respiration inhibition for establishing levels for the utilization of preservatives in the food industry.

  4. The effects of inhibitory control training for preschoolers on reasoning ability and neural activity

    DEFF Research Database (Denmark)

    Liu, Qian; Zhu, Xinyi; Ziegler, Albert

    2015-01-01

    /week, for 3 weeks. Several cognitive tasks (involving inhibitory control, working memory, and fluid intelligence) were used to evaluate the transfer effects, and electroencephalography (EEG) was performed during a go/no-go task. Progress on the trained game was significant, while performance on a reasoning......Inhibitory control (including response inhibition and interference control) develops rapidly during the preschool period and is important for early cognitive development. This study aimed to determine the training and transfer effects on response inhibition in young children. Children...... in the training group (N = 20; 12 boys, mean age 4.87 ± 0.26 years) played “Fruit Ninja” on a tablet computer for 15 min/day, 4 days/week, for 3 weeks. Children in the active control group (N = 20; 10 boys, mean age 4.88 ± 0.20 years) played a coloring game on a tablet computer for 10 min/day, 1–2 days...

  5. Inhibitory effect of the essential oil from Eugenia caryophyllata Thumb leaves on coalho cheese contaminating microorganisms

    Directory of Open Access Journals (Sweden)

    Vinicius Nogueira Trajano

    2010-12-01

    Full Text Available Coalho cheese (a firm but very lightweight cheese produced in Brazil is widely produced and consumed in the Brazilian Northeast and its production has been mainly related to small farmers. This food has been frequently characterized as having high microbial load posing a risk for the health of consumers. This study aimed to indentify the chemical compounds of the essential oil from Eugenia caryophyllata leaves; to evaluate the inhibitory effect of the oil against coalho cheese contaminating microorganisms; and to assess its efficacy in inhibiting the autochthonous microflora of the cheese during refrigerated storage. Eugenol (74% was found to be the most prevalent compound in the essential oil. Minimum Inhibitory Concentration (MIC and Minimum Cidal Concentration (MCC in laboratorial broth were in the range of 2.5-5 and 5-20 µg.mL-1, respectively. Vaccum packed coalho cheese added with 5, 10, and 20 µg.g-1 of oil showed a lower growth rate (like-static effect against mesophilic bacteria during the time intervals evaluated. On the other hand, 2.5-10 µg.g-1 of oil provided a prominent decrease toward fungi count in cheese samples during storage. These results reveal the interesting antimicrobial property of the essential oil from E. caryophyllata leaves against a range of coalho cheese-related microorganisms in laboratorial media and in food matrix.

  6. In vitro inhibitory effect of miltefosine against strains of Histoplasma capsulatum var. capsulatum and Sporothrix spp.

    Science.gov (United States)

    Brilhante, Raimunda Sâmia Nogueira; Malaquias, Angela Donato Maia; Caetano, Erica Pacheco; Castelo-Branco, Débora de Souza Collares Maia; Lima, Rita Amanda Chaves de; Marques, Francisca Jakelyne de Farias; Silva, Natalya Fechine; Alencar, Lucas Pereira de; Monteiro, André Jalles; Camargo, Zoilo Pires de; Bandeira, Tereza de Jesus Pinheiro Gomes; Rodrigues, Anderson Messias; Cordeiro, Rossana de Aguiar; Moreira, José Luciano Bezerra; Sidrim, José Júlio Costa; Rocha, Marcos Fábio Gadelha

    2014-04-01

    Miltefosine (MIL), originally developed for use in cancer chemotherapy, has been shown to have important antifungal activity against several pathogenic fungi. Our aim in this study was to determine the in vitro activity of MIL against the dimorphic fungi Histoplasma capsulatum and Sporothrix spp. This was done using the broth microdilution method. MIL had an in vitro inhibitory effect against all strains of H. capsulatum var. capsulatum and Sporothrix spp. analyzed. The minimal inhibitory concentrations (MIC) varied from 0.25 μg/ml to 2 μg/ml for H. capsulatum var. capsulatum in the filamentous phase and from 0.125 μg/ml to 1 μg/ml in the yeast phase. The MIC interval for Sporothrix spp. in the filamentous phase was 0.25-2 μg/ml. The minimal fungicidal concentrations (MFCs) were ≤4 μg/ml for isolates of both analyzed species. This study demonstrates that MIL has an antifungal effect in vitro against two potentially pathogenic fungi and that more studies should be performed in order to evaluate its applicability in vivo.

  7. Inhibitory effects of NAMI-A-like ruthenium complexes on prion neuropeptide fibril formation.

    Science.gov (United States)

    Wang, Xuesong; Zhu, Dengsen; Zhao, Cong; He, Lei; Du, Weihong

    2015-05-01

    Prion diseases are a group of infectious and fatal neurodegenerative disorders caused by the conformational conversion of a cellular prion protein (PrP) into its abnormal isoform PrP(Sc). PrP106-126 resembles PrP(Sc) in terms of physicochemical and biological characteristics and is used as a common model for the treatment of prion diseases. Inhibitory effects on fibril formation and neurotoxicity of the prion neuropeptide PrP106-126 have been investigated using metal complexes as potential inhibitors. Nevertheless, the binding mechanism between metal complexes and the peptide remains unclear. The present study is focused on the interaction of PrP106-126 with NAMI-A and NAMI-A-like ruthenium complexes, including KP418, KP1019, and KP1019-2. Results demonstrated that these ruthenium complexes could bind to PrP106-126 in a distinctive binding mode through electrostatic and hydrophobic interactions. NAMI-A-like ruthenium complexes can also effectively inhibit the aggregation and fibril formation of PrP106-126. The complex KP1019 demonstrated the optimal inhibitory ability upon peptide aggregation, and cytotoxicity because of its large aromatic ligand contribution. The studied complexes could also regulate the copper redox chemistry of PrP106-126 and effectually inhibit the formation of reactive oxygen species. Given these findings, ruthenium complexes with relatively low cellular toxicity may be used to develop potential pharmaceutical products against prion diseases.

  8. Experimental study on the inhibitory effect of MSCs on radiationinduced thymoma in mice

    Directory of Open Access Journals (Sweden)

    Wen-Long Zhang

    2016-01-01

    Full Text Available Objective: To study the inhibitory effect of MSCs on radiation-induced thymoma in mice. Methods: C57BL/6 mice were selected as the research objects, model group and MSCs group induced thymoma by radiation, and MSCs group received intravenous injection of mesenchymal stem cell for therapy. Six months after treatment, macroscopic morphology of thymus tissue, contents of T lymphocyte subsets as well as expression of tumor suppressor gene PTEN and proliferation marker molecule Ki-67 were detected. Results: (1 macroscopic morphology: thymus tissue weight of model group was significantly greater than that of control group and thymus tissue weight of MSCs group was lower than that of control group; (2 cells and molecules: compared with control group, contents of CD4-CD8-, CD4+CD8- and CD4- CD8+ T cells as well as expression of PTEN in thymus tissue of model group significantly decreased, and CD4+CD8+ T cell content as well as Ki-67 expression significantly increased; compared with model group, contents of CD4-CD8-, CD4+CD8- and CD4-CD8+ T cells as well as expression of PTEN in thymus tissue of MSCs group significantly increased, and CD4+CD8+ T cell content as well as Ki-67 expression significantly decreased. Conclusions: MSCs have inhibitory effect on radiation-induced thymoma in mice, manifested as promoting CD4+CD8- and CD4-CD8+ T cell maturation as well as inhibiting cell proliferation.

  9. Effects of Different Working Modes of Ultrasound on Structural Characteristics of Zein and ACE Inhibitory Activity of Hydrolysates

    Directory of Open Access Journals (Sweden)

    Xiaofeng Ren

    2017-01-01

    Full Text Available Ultrasound was used as a new technology to pretreat protein prior to proteolysis to improve enzymolysis efficiency. The effects of different working modes of ultrasound on the angiotensin I-converting enzyme (ACE inhibitory activity of zein hydrolysates and the structural characteristics of zein were investigated. The solubility, surface hydrophobicity (H0, ultraviolet-visible (UV-Vis spectra, intrinsic fluorescence spectra, and circular dichroism (CD spectra of zein pretreated with ultrasound were determined. All ultrasound pretreatments significantly improved the ACE inhibitory activity of zein hydrolysates (p<0.05. The highest ACE inhibitory activity, representing an increase of 99.21% over the control, was obtained with dual sweeping frequency ultrasound of 33±2 and 68±2 kHz. The effects of single sweeping frequency and dual fixed frequency ultrasound were stronger than those of single fixed frequency ultrasound for improving the ACE inhibitory activity of zein. Structural changes in zein were induced by ultrasound, as confirmed by changes in the solubility, H0, UV-Vis spectra, intrinsic fluorescence spectra, and CD spectra of zein, and these were consistent with the corresponding ACE inhibitory activities of zein hydrolysates. Thus, ultrasound working mode and frequency have significant effects on the structure of zein and the ACE inhibitory activity of zein hydrolysates.

  10. Acute Modafinil Effects on Attention and Inhibitory Control in Methamphetamine-Dependent Humans*

    Science.gov (United States)

    Dean, Andy C.; Sevak, Rajkumar J.; Monterosso, John R.; Hellemann, Gerhard; Sugar, Catherine A.; London, Edythe D.

    2011-01-01

    Objective: Individuals who are methamphetamine dependent exhibit higher rates of cognitive dysfunction than healthy people who do not use methamphetamine, and this dysfunction may have a negative effect on the success of behavioral treatments for the disorder. Therefore, a medication that improves cognition, such as modafinil (Provigil), may serve as a useful adjunct to behavioral treatments for methamphetamine dependence. Although cognitive-enhancing effects of modafinil have been reported in several populations, little is known about the effects of modafinil in methamphetamine-dependent individuals. We thus sought to evaluate the effects of modafinil on the cognitive performance of methamphetamine-dependent and healthy individuals. Method: Seventeen healthy subjects and 24 methamphetamine-dependent subjects participated in this randomized, double-blind, placebo-controlled, crossover study. Effects of modafinil (200 mg, single oral dose) were assessed on participants’ performance on tests of inhibitory control, working memory, and processing speed/attention. Results: Across subjects, modafinil improved performance on a test of sustained attention, with no significant improvement on any other cognitive tests. However, within the methamphetamine-dependent group only, participants with a high baseline frequency of methamphetamine use demonstrated a greater effect of modafinil on tests of inhibitory control and processing speed than those participants with low baseline use of methamphetamine. Conclusions: Although modafinil produced limited effects across all participants, methamphetamine-dependent participants with a high baseline use of methamphetamine demonstrated significant cognitive improvement on modafinil relative to those with low baseline methamphetamine use. These results add to the findings from a clinical trial that suggested that modafinil may be particularly useful in methamphetamine-dependent subjects who use the drug frequently. PMID:22051208

  11. Inhibitory effect of aniracetam on N-type calcium current in acutely isolated rat neuronal cells.

    Science.gov (United States)

    Koike, H; Saito, H; Matsuki, N

    1993-04-01

    Effects of aniracetam on whole-cell calcium currents were studied in acutely isolated neuronal cells from postnatal rat ventromedial hypothalamus. There were three types of inward calcium currents, one low-threshold transient current and two high-threshold sustained currents. The nicardipine sensitive L-type current was activated at -20 mV or more depolarized potentials, and the omega-conotoxin sensitive N-type current was recorded at more positive potentials than the L-type. Aniracetam inhibited the N-type current in a dose-dependent manner without affecting the other two types of calcium currents. The effect appeared soon after the addition and lasted for several minutes during washing. Since the N-type current is thought to regulate the release of transmitters, the inhibitory effect may contribute to the nootropic property of aniracetam by modifying the neurotransmission.

  12. Inhibitory effect of 12C6+ ion and X-ray on angiogenesis in HMEC-1

    International Nuclear Information System (INIS)

    Liu Yuanyuan; Zhang Hong; Liu Yang; Wu Zhenhua; Sun Chao; Li Hongyan

    2013-01-01

    The study aims to explore the effect of 12 C 6+ ion and X-ray on proliferation, migration, tube formation and MMPS of human microvascular endothelial cells (HMEC-1). Transwell migration experiment showed that the radiation could inhibit the migration of HMEC-1 in sub-lethal dose 24 h after irradiation. Furthermore, the inhibition ability of 12 C 6+ ion was stronger than that of X-ray. Matrigel experiment indicated that 12 C 6+ ion suppressed the tube formation of HMEC-1 spontaneously. However, the inhibitory effect of X-ray had no significance. Meanwhile, Gelatin Zymography showed the expression of MMP-2 was inhibited obviously by 12 C 6+ ion, while X-ray had little effect on the expression of MMP-2. In conclusion, 12 C 6+ ion is superior to X-ray in radiotherapy of tumor. (authors)

  13. The Strength of the Strongest Ties in Collaborative Problem Solving

    DEFF Research Database (Denmark)

    de Montjoye, Yves-Alexandre; Stopczynski, Arkadiusz; Shmueli, Erez

    2014-01-01

    Complex problem solving in science, engineering, and business has become a highly collaborative endeavor. Teams of scientists or engineers collaborate on projects using their social networks to gather new ideas and feedback. Here we bridge the literature on team performance and information networks...... by studying teams' problem solving abilities as a function of both their within-team networks and their members' extended networks. We show that, while an assigned team's performance is strongly correlated with its networks of expressive and instrumental ties, only the strongest ties in both networks have......-significant in the statistical analysis. Our results have consequences for the organization of teams of scientists, engineers, and other knowledge workers tackling today's most complex problems....

  14. Inhibitory Effect of Camptothecin against Rice Bacterial Brown Stripe Pathogen Acidovorax avenae subsp. avenae RS-2.

    Science.gov (United States)

    Dong, Qiaolin; Luo, Ju; Qiu, Wen; Cai, Li; Anjum, Syed Ishtiaq; Li, Bin; Hou, Mingsheng; Xie, Guanlin; Sun, Guochang

    2016-07-27

    Camptothecin (CPT) has anticancer, antiviral, and antifungal properties. However, there is a dearth of information about antibacterial activity of CPT. Therefore, in this study, we investigated the inhibitory effect of CPT on Acidovorax avenae subsp. avenae strain RS-2, the pathogen of rice bacterial brown stripe, by measuring cell growth, DNA damage, cell membrane integrity, the expression of secretion systems, and topoisomerase-related genes, as well as the secretion of effector protein Hcp. Results indicated that CPT solutions at 0.05, 0.25, and 0.50 mg/mL inhibited the growth of strain RS-2 in vitro, while the inhibitory efficiency increased with an increase in CPT concentration, pH, and incubation time. Furthermore, CPT treatment affected bacterial growth and replication by causing membrane damage, which was evidenced by transmission electron microscopic observation and live/dead cell staining. In addition, quantitative real-time PCR analysis indicated that CPT treatment caused differential expression of eight secretion system-related genes and one topoisomerase-related gene, while the up-regulated expression of hcp could be justified by the increased secretion of Hcp based on the ELISA test. Overall, this study indicated that CPT has the potential to control the bacterial brown stripe pathogen of rice.

  15. Inhibitory Effect of Camptothecin against Rice Bacterial Brown Stripe Pathogen Acidovorax avenae subsp. avenae RS-2

    Directory of Open Access Journals (Sweden)

    Qiaolin Dong

    2016-07-01

    Full Text Available Camptothecin (CPT has anticancer, antiviral, and antifungal properties. However, there is a dearth of information about antibacterial activity of CPT. Therefore, in this study, we investigated the inhibitory effect of CPT on Acidovorax avenae subsp. avenae strain RS-2, the pathogen of rice bacterial brown stripe, by measuring cell growth, DNA damage, cell membrane integrity, the expression of secretion systems, and topoisomerase-related genes, as well as the secretion of effector protein Hcp. Results indicated that CPT solutions at 0.05, 0.25, and 0.50 mg/mL inhibited the growth of strain RS-2 in vitro, while the inhibitory efficiency increased with an increase in CPT concentration, pH, and incubation time. Furthermore, CPT treatment affected bacterial growth and replication by causing membrane damage, which was evidenced by transmission electron microscopic observation and live/dead cell staining. In addition, quantitative real-time PCR analysis indicated that CPT treatment caused differential expression of eight secretion system-related genes and one topoisomerase-related gene, while the up-regulated expression of hcp could be justified by the increased secretion of Hcp based on the ELISA test. Overall, this study indicated that CPT has the potential to control the bacterial brown stripe pathogen of rice.

  16. Inhibitory Effect of Arctigenin from Fructus Arctii Extract on Melanin Synthesis via Repression of Tyrosinase Expression

    Directory of Open Access Journals (Sweden)

    Hwayong Park

    2013-01-01

    Full Text Available To identify the active compound arctigenin in Fructus Arctii (dried seed of medicinal plant Arctium lappa and to elucidate the inhibitory mechanism in melanogenesis, we analyzed melanin content and tyrosinase activity on B16BL6 murine melanoma and melan-A cell cultures. Water extracts of Fructus Arctii were shown to inhibit tyrosinase activity in vitro and melanin content in α-melanocyte stimulating hormone-stimulated cells to similar levels as the well-known kojic acid and arbutin, respectively. The active compound arctigenin of Fructus Arctii displayed little or no cytotoxicity at all concentrations examined and decreased the relative melanin content and tyrosinase activity in a dose-dependent manner. Melanogenic inhibitory activity was also identified in vivo with zebrafish embryo. To determine the mechanism of inhibition, the effects of arctigenin on tyrosinase gene expression and tyrosinase promoter activity were examined. Also in addition, in the signaling cascade, arctigenin dose dependently decreased the cAMP level and promoted the phosphorylation of extracellular signal-regulated kinase. This result suggests that arctigenin downregulates cAMP and the tyrosinase enzyme through its gene promoter and subsequently upregulates extracellular signal-regulated kinase activity by increasing phosphorylation in the melanogenesis signaling pathway, which leads to a lower melanin content.

  17. Inhibitory Effect of Arctigenin from Fructus Arctii Extract on Melanin Synthesis via Repression of Tyrosinase Expression

    Science.gov (United States)

    Park, Hwayong; Song, Kwang Hoon; Jung, Pil Mun; Kim, Ji-Eun; Kim, Mi Yoon; Ma, Jin Yeul

    2013-01-01

    To identify the active compound arctigenin in Fructus Arctii (dried seed of medicinal plant Arctium lappa) and to elucidate the inhibitory mechanism in melanogenesis, we analyzed melanin content and tyrosinase activity on B16BL6 murine melanoma and melan-A cell cultures. Water extracts of Fructus Arctii were shown to inhibit tyrosinase activity in vitro and melanin content in α-melanocyte stimulating hormone-stimulated cells to similar levels as the well-known kojic acid and arbutin, respectively. The active compound arctigenin of Fructus Arctii displayed little or no cytotoxicity at all concentrations examined and decreased the relative melanin content and tyrosinase activity in a dose-dependent manner. Melanogenic inhibitory activity was also identified in vivo with zebrafish embryo. To determine the mechanism of inhibition, the effects of arctigenin on tyrosinase gene expression and tyrosinase promoter activity were examined. Also in addition, in the signaling cascade, arctigenin dose dependently decreased the cAMP level and promoted the phosphorylation of extracellular signal-regulated kinase. This result suggests that arctigenin downregulates cAMP and the tyrosinase enzyme through its gene promoter and subsequently upregulates extracellular signal-regulated kinase activity by increasing phosphorylation in the melanogenesis signaling pathway, which leads to a lower melanin content. PMID:23781272

  18. Flavonoids from Salvia chloroleuca with α-Amylsae and α-Glucosidase Inhibitory Effect.

    Science.gov (United States)

    Asghari, Behvar; Salehi, Peyman; Sonboli, Ali; Nejad Ebrahimi, Samad

    2015-01-01

    It is believed that the inhibition of carbohydrate hydrolyzing enzymes including α-amylase and α-glucosidase is one of the therapeutic approaches to decrease the postprandial glucose level after a meal, especially in the people with type 2 diabetes. Medicinal plants and their extracts are one of the main sources to find new inhibitors to the enzymes. In our study four flavonoids, namely luteolin 7-O-glucoside (1), luteolin 7-O-glucuronide (2), diosmetin 7-O-glucuronide (3) and salvigenin (4) were isolated from aerial parts of Salvia chloroleuca. The inhibitory activity of these compounds against α-amylase and α-glucosidase were evaluated. Compounds 1, 2 and 3 showed potent α-glucosidase inhibitory effect with IC50 values of 18.3, 14.7, and 17.1 µM, respectively. Also these compounds exhibited moderate α-amylase activity with IC50 values 81.7, 61.5, and 76.3 µM, respectively.

  19. Growth inhibitory effects of endotoxins from Bacteroides gingivalis and intermedius on human gingival fibroblasts in vitro

    International Nuclear Information System (INIS)

    Layman, D.L.; Diedrich, D.L.

    1987-01-01

    Purified endotoxin or lipopolysaccharide from Bacteroides gingivalis and Bacteroides intermedius caused a similar dose-dependent inhibition of growth of cultured human gingival fibroblasts as determined by 3 H-thymidine incorporation and direct cell count. Approximately 200 micrograms/ml endotoxin caused a 50% reduction in 3 H-thymidine uptake of logarithmically growing cells. Inhibition of growth was similar in cultures of fibroblasts derived from either healthy or diseased human gingiva. When examining the change in cell number with time of exposure in culture, the rate of proliferation was significantly suppressed during the logarithmic phase of growth. However, the cells recovered so that the rate of proliferation, although reduced, was sufficient to produce a cell density similar to the control cells with prolonged culture. The endotoxins were characterized by sodium dodecyl sulfate-polyacrylamide gel electrophoresis. The profiles of the Bacteroides endotoxins were different. B. gingivalis endotoxin showed a wide range of distinct bands indicating a heterogeneous distribution of molecular species. Endotoxin from B. intermedius exhibited a few discrete low molecular weight bands, but the majority of the lipopolysaccharides electrophoresed as a diffuse band of high molecular weight material. The apparent heterogeneity of the two Bacteroides endotoxins and the similarity in growth inhibitory capacity suggest that growth inhibitory effects of these substances cannot be attributed to any polysaccharide species of endotoxin

  20. Effects of multiple inhibitory components on anaerobic treatment processes in municipal solid waste incineration leachate.

    Science.gov (United States)

    Lei, Yuqing; Dang, Yan; Lan, Zhangheng; Sun, Dezhi

    2016-06-01

    This study served to investigate the comparative and combined effects of calcium, ammonia nitrogen, and aquatic humic substances (AHS) on specific methanogenic activity (SMA) in municipal solid waste leachate at mesophilic conditions. Using orthogonal experiments, anaerobic granular sludge was cultured with different concentrations combinations of the three added components for 13 days. The combination of 6000 mg/L calcium, 400 mg/L ammonia nitrogen, and 4000 mg/L AHS was the most inhibitory combination on the SMA of granular sludge, with a calculated 4.49 mL (standard temperature and atmospheric pressure) (STP) CH4/(gVSS·d) of SMA. The SMA with the addition of the inhibitory components was much lower than the control group's (1000 mg/L calcium, 200 mg/L ammonia nitrogen and 2000 mg/L AHS) with a calculated 12.97 mL (STP) CH4/(gVSS·d) of SMA. Calcium was the major inhibitor among the three components followed by AHS. High concentrations of calcium significantly inhibited the utilization of propionate and butyrate in the substrate and further affected the methanogenic process.

  1. Flavonoids from Machilus japonica Stems and Their Inhibitory Effects on LDL Oxidation

    Directory of Open Access Journals (Sweden)

    Se-Jin Joo

    2014-09-01

    Full Text Available Stems of Machilus japonica were extracted with 80% aqueous methanol (MeOH and the concentrated extract was successively extracted with ethyl acetate (EtOAc, normal butanol (n-BuOH, and water. Six flavonoids were isolated from the EtOAc fraction: (+-taxifolin, afzelin, (−-epicatechin, 5,3'-di-O-methyl-(−-epicatechin, 5,7,3'-tri-O-methyl-(−-epicatechin, and 5,7-di-O-methyl-3',4'-methylenedioxyflavan-3-ol. The chemical structures were identified using spectroscopic data including NMR, mass spectrometry and infrared spectroscopy. This is the first report of isolation of these six compounds from M. japonica. The compounds were evaluated for their diphenyl picryl hydrazinyl scavenging activity and inhibitory effects on low-density lipoprotein oxidation. Compounds 1 and 3–6 exhibited DPPH antioxidant activity equivalent with that of ascorbic acid, with half maximal inhibitory concentration (IC50 values of 0.16, 0.21, 0.17, 0.15 and 0.07 mM, respectively. The activity of compound 1 was similar to the positive control butylated hydroxytoluene, which had an IC50 value of 1.9 µM, while compounds 3 and 5 showed little activity. Compounds 1, 3, and 5 exhibited LDL antioxidant activity with IC50 values of 2.8, 7.1, and 4.6 µM, respectively.

  2. Cholecystokinin receptor-1 mediates the inhibitory effects of exogenous cholecystokinin octapeptide on cellular morphine dependence

    Directory of Open Access Journals (Sweden)

    Wen Di

    2012-06-01

    Full Text Available Abstract Background Cholecystokinin octapeptide (CCK-8, the most potent endogenous anti-opioid peptide, has been shown to regulate the processes of morphine dependence. In our previous study, we found that exogenous CCK-8 attenuated naloxone induced withdrawal symptoms. To investigate the precise effect of exogenous CCK-8 and the role of cholecystokinin (CCK 1 and/or 2 receptors in morphine dependence, a SH-SY5Y cell model was employed, in which the μ-opioid receptor, CCK1/2 receptors, and endogenous CCK are co-expressed. Results Forty-eight hours after treating SH-SY5Y cells with morphine (10 μM, naloxone (10 μM induced a cAMP overshoot, indicating that cellular morphine dependence had been induced. The CCK receptor and endogenous CCK were up-regulated after chronic morphine exposure. The CCK2 receptor antagonist (LY-288,513 at 1–10 μM inhibited the naloxone-precipitated cAMP overshoot, but the CCK1 receptor antagonist (L-364,718 did not. Interestingly, CCK-8 (0.1-1 μM, a strong CCK receptor agonist, dose-dependently inhibited the naloxone-precipitated cAMP overshoot in SH-SY5Y cells when co-pretreated with morphine. The L-364,718 significantly blocked the inhibitory effect of exogenous CCK-8 on the cAMP overshoot at 1–10 μM, while the LY-288,513 did not. Therefore, the CCK2 receptor appears to be necessary for low concentrations of endogenous CCK to potentiate morphine dependence in SH-SY5Y cells. An additional inhibitory effect of CCK-8 at higher concentrations appears to involve the CCK1 receptor. Conclusions This study reveals the difference between exogenous CCK-8 and endogenous CCK effects on the development of morphine dependence, and provides the first evidence for the participation of the CCK1 receptor in the inhibitory effects of exogenous CCK-8 on morphine dependence.

  3. Inhibitory effects of polysaccharides on the cariogenic activities of Streptococcus mutans.

    Science.gov (United States)

    Yano, Akira; Konno, Naotake; Imai, Susumu; Kato, Hirohisa

    2012-01-01

    Many carbohydrates are involved in the biofilm formation and activities of glucosyltransferases (Gtfs) of Streptococcus mutans, and the effects of various disaccharides and polysaccharides were investigated in this study, including the hot water-extracted glucan fraction of the Lentinula edodes fruiting body (HWG). HWG was found to inhibit the initial adhesion of S. mutans to saliva-coated hydroxyapatite (sHA), and also laminarin to inhibit glucan synthesis by Gtfs. However, sucrose-dependent biofilm formation by S. mutans was not inhibited by these materials. Interestingly, dextran was found to have an inhibitory effect on the sucrose-dependent biofilm formation. The data suggest that the presence of such an edible glucan as dextran in daily foods would act to some degree on S. mutans for suppressing the cariogenic activity.

  4. Tyrosinase inhibitory effects and antioxidative activities of saponins from Xanthoceras Sorbifolia nutshell.

    Directory of Open Access Journals (Sweden)

    Hongmei Zhang

    Full Text Available Certain saponins are bioactive compounds with anticancer, antivirus and antioxidant activities. This paper discussed inhibitory effects of saponins from Xanthoceras Sorbifolia on tyrosinase, through the research of the rate of tyrosinase catalyzed L-DOPA oxidation. The inhibition rate of tyrosinase activity presented non-linear changes with the saponins concentration. The rate reached 52.0% when the saponins concentration was 0.96 mg/ml. Antioxidant activities of saponins from Xanthoceras Sorbifolia were evaluated by using hydroxyl and superoxide radical scavenging assays. The hydroxyl radical scavenging effects of the saponins were 15.5-68.7%, respectively at the concentration of 0.18-2.52 mg/ml. The superoxide radical scavenging activity reduced from 96.6% to 7.05% with the time increasing at the concentration of 1.44 mg/ml. All the above antioxidant evaluation indicated that saponins from Xanthoceras Sorbifolia exhibited good antioxidant activity in a concentration- dependent manner.

  5. Growth-inhibitory effect of TGF-B on human fetal adrenal cells in primary monolayer culture.

    Science.gov (United States)

    Riopel, L; Branchaud, C L; Goodyer, C G; Adkar, V; Lefebvre, Y

    1989-08-01

    We examined the effects of transforming-growth factor-B (TGF-B) on growth ([3H]-thymidine uptake) and function (dehydroepiandrosterone sulfate [DHAS] and cortisol production) of human fetal zone adrenal cells. Results indicate that TGF-B significantly inhibits, in a dose-related manner, both basal and epidermal growth factor (EGF)-stimulated cell growth: IC50 = 0.1-0.25 ng/ml. EGF is ineffective in overcoming the inhibitory effect of TGF-B, suggesting a noncompetitive antagonism between the two factors. Also, the inhibitory effect of TGF-B is additive to that of adrenocorticotropic hormone (ACTH). On the other hand, TGF-B (1 ng/ml) does not significantly change basal or ACTH-stimulated DHAS or cortisol secretion. We conclude that, unlike its effect on other steroid-producing cells, TGF-B inhibits growth of fetal zone cells and does not appear to have a significant inhibitory effect on steroidogenesis.

  6. The effect of gastric inhibitory polypeptide on intestinal glucose absorption and intestinal motility in mice

    Energy Technology Data Exchange (ETDEWEB)

    Ogawa, Eiichi [Department of Diabetes and Clinical Nutrition, Graduate School of Medicine, Kyoto University (Japan); Hosokawa, Masaya [Department of Diabetes and Clinical Nutrition, Graduate School of Medicine, Kyoto University (Japan); Faculty of Human Sciences, Tezukayama Gakuin University, Osaka (Japan); Harada, Norio; Yamane, Shunsuke; Hamasaki, Akihiro; Toyoda, Kentaro; Fujimoto, Shimpei; Fujita, Yoshihito; Fukuda, Kazuhito [Department of Diabetes and Clinical Nutrition, Graduate School of Medicine, Kyoto University (Japan); Tsukiyama, Katsushi; Yamada, Yuichiro [Department of Diabetes and Clinical Nutrition, Graduate School of Medicine, Kyoto University (Japan); Department of Internal Medicine, Division of Endocrinology, Diabetes and Geriatric Medicine, Akita University School of Medicine, Akita (Japan); Seino, Yutaka [Department of Diabetes and Clinical Nutrition, Graduate School of Medicine, Kyoto University (Japan); Kansai Electric Power Hospital, Osaka (Japan); Inagaki, Nobuya, E-mail: inagaki@metab.kuhp.kyoto-u.ac.jp [Department of Diabetes and Clinical Nutrition, Graduate School of Medicine, Kyoto University (Japan); CREST of Japan Science and Technology Cooperation (JST), Kyoto (Japan)

    2011-01-07

    Research highlights: {yields} Exogenous GIP inhibits intestinal motility through a somatostatin-mediated pathway. {yields} Exogenous GIP inhibits intestinal glucose absorption by reducing intestinal motility. {yields} The GIP-receptor-mediated action in intestine does not involve in GLP-1-mediated pathway. -- Abstract: Gastric inhibitory polypeptide (GIP) is released from the small intestine upon meal ingestion and increases insulin secretion from pancreatic {beta} cells. Although the GIP receptor is known to be expressed in small intestine, the effects of GIP in small intestine are not fully understood. This study was designed to clarify the effect of GIP on intestinal glucose absorption and intestinal motility. Intestinal glucose absorption in vivo was measured by single-pass perfusion method. Incorporation of [{sup 14}C]-glucose into everted jejunal rings in vitro was used to evaluate the effect of GIP on sodium-glucose co-transporter (SGLT). Motility of small intestine was measured by intestinal transit after oral administration of a non-absorbed marker. Intraperitoneal administration of GIP inhibited glucose absorption in wild-type mice in a concentration-dependent manner, showing maximum decrease at the dosage of 50 nmol/kg body weight. In glucagon-like-peptide-1 (GLP-1) receptor-deficient mice, GIP inhibited glucose absorption as in wild-type mice. In vitro examination of [{sup 14}C]-glucose uptake revealed that 100 nM GIP did not change SGLT-dependent glucose uptake in wild-type mice. After intraperitoneal administration of GIP (50 nmol/kg body weight), small intestinal transit was inhibited to 40% in both wild-type and GLP-1 receptor-deficient mice. Furthermore, a somatostatin receptor antagonist, cyclosomatostatin, reduced the inhibitory effect of GIP on both intestinal transit and glucose absorption in wild-type mice. These results demonstrate that exogenous GIP inhibits intestinal glucose absorption by reducing intestinal motility through a somatostatin

  7. Growth Inhibitory Effects of Adhatoda vasica and Its Potential at Reducing Listeria monocytogenes in Chicken Meat

    Directory of Open Access Journals (Sweden)

    Shruti Shukla

    2017-07-01

    Full Text Available The inhibitory effects of Adhatoda vasica ethanolic leaf extract (AVELE against Listeria monocytogenes were examined to assess its potential to preserve minimally processed meat products safely. The total phenolic, flavonoid, and alkaloid levels in AVELE were 10.09 ± 4.52 mg of gallic acid equivalents (GAE/g, 22.43 ± 1.62 mg of quercetin equivalents/g, and 19.43 ± 3.90 mg/g, respectively. AVELE (1, 5, 10, or 20% had considerable antibacterial effects against L. monocytogenes NCIM 24563 in terms of the inhibitory zones (7.4–13.6 mm, MIC (100 mg/mL or 10% formulated solution, reduced cell viability, potassium ion efflux, and the release of 260-nm absorbing materials and extracellular ATP. AVELE was used as a rinse solution (5, 10, and 20% for raw chicken breast meat. A 20% rinsing solution applied for 60 min inhibited the L. monocytogenes NCIM 24563 counts significantly on raw chicken breast meat. Moreover, L. monocytogenes NCIM 24563 did not grow in the meat sample when the rinse time was increased to 90 min at the same concentration. L. monocytogenes showed a greater reduction to ~3 CFU/g after rinsing with a 10 and 20% AVELE solution for 30 min than with a 5% AVELE solution. The rinsing processes with AVELE produced the final cooked chicken products with higher sensory attribute scores, such as taste, juiciness, and tenderness, compared to the control group along with a decrease in microbial contamination. Chicken meat rinsed with AVELE (rinsing time of 90 min showed better sensory attribute scores of juiciness and tenderness, as well as the overall sensory quality compared to the untreated group. This research highlights the effectiveness of AVELE against L. monocytogenes NCIM 24563, suggesting that AVELE can be used as an effective antimicrobial marinade and/or a rinse for meat preservation.

  8. The effect of gastric inhibitory polypeptide on intestinal glucose absorption and intestinal motility in mice

    International Nuclear Information System (INIS)

    Ogawa, Eiichi; Hosokawa, Masaya; Harada, Norio; Yamane, Shunsuke; Hamasaki, Akihiro; Toyoda, Kentaro; Fujimoto, Shimpei; Fujita, Yoshihito; Fukuda, Kazuhito; Tsukiyama, Katsushi; Yamada, Yuichiro; Seino, Yutaka; Inagaki, Nobuya

    2011-01-01

    Research highlights: → Exogenous GIP inhibits intestinal motility through a somatostatin-mediated pathway. → Exogenous GIP inhibits intestinal glucose absorption by reducing intestinal motility. → The GIP-receptor-mediated action in intestine does not involve in GLP-1-mediated pathway. -- Abstract: Gastric inhibitory polypeptide (GIP) is released from the small intestine upon meal ingestion and increases insulin secretion from pancreatic β cells. Although the GIP receptor is known to be expressed in small intestine, the effects of GIP in small intestine are not fully understood. This study was designed to clarify the effect of GIP on intestinal glucose absorption and intestinal motility. Intestinal glucose absorption in vivo was measured by single-pass perfusion method. Incorporation of [ 14 C]-glucose into everted jejunal rings in vitro was used to evaluate the effect of GIP on sodium-glucose co-transporter (SGLT). Motility of small intestine was measured by intestinal transit after oral administration of a non-absorbed marker. Intraperitoneal administration of GIP inhibited glucose absorption in wild-type mice in a concentration-dependent manner, showing maximum decrease at the dosage of 50 nmol/kg body weight. In glucagon-like-peptide-1 (GLP-1) receptor-deficient mice, GIP inhibited glucose absorption as in wild-type mice. In vitro examination of [ 14 C]-glucose uptake revealed that 100 nM GIP did not change SGLT-dependent glucose uptake in wild-type mice. After intraperitoneal administration of GIP (50 nmol/kg body weight), small intestinal transit was inhibited to 40% in both wild-type and GLP-1 receptor-deficient mice. Furthermore, a somatostatin receptor antagonist, cyclosomatostatin, reduced the inhibitory effect of GIP on both intestinal transit and glucose absorption in wild-type mice. These results demonstrate that exogenous GIP inhibits intestinal glucose absorption by reducing intestinal motility through a somatostatin-mediated pathway rather

  9. Effect of pretreatment on enzymatic hydrolysis of bovine collagen and formation of ACE-inhibitory peptides

    DEFF Research Database (Denmark)

    Zhang, Yuhao; Olsen, Karsten; Grossi, Alberto Blak

    2013-01-01

    ACEinhibitory peptides. The highest ACE-inhibitory activity was obtained with Alcalase. Pretreatment significantly influenced the DH and ACE-inhibition. For most enzymes, boiling for 5 min resulted in a significantly higher DH and ACE-inhibitory activity. With Alcalase and collagenase, hydrolysis and release...... of ACE-inhibitory peptides occurred without any pretreatment, but HP-treatment significantly improved the DH and ACE-inhibitory activity. HP did not markedly affect the hydrolysis with the other enzymes. The major peptides obtained with Alcalase were identified; all were released from the triple helix...

  10. Inhibitory effect of Xenorhabdus nematophila TB on plant pathogens Phytophthora capsici and Botrytis cinerea in vitro and in planta.

    Science.gov (United States)

    Fang, Xiangling; Zhang, Manrang; Tang, Qian; Wang, Yonghong; Zhang, Xing

    2014-03-06

    Entomopathogenic bacteria Xenorhabdus spp. produce secondary metabolites with potential antimicrobial activity for use in agricultural productions. This study evaluated the inhibitory effect of X. nematophila TB culture on plant pathogens Botrytis cinerea and Phytophthora capsici. The cell-free filtrate of TB culture showed strong inhibitory effects (>90%) on mycelial growth of both pathogens. The methanol-extracted bioactive compounds (methanol extract) of TB culture also had strong inhibitory effects on mycelial growth and spore germinations of both pathogens. The methanol extract (1000 μg/mL) and cell-free filtrate both showed strong therapeutic and protective effects (>70%) on grey mold both in detached tomato fruits and plants, and leaf scorch in pepper plants. This study demonstrates X. nematophila TB produces antimicrobial metabolites of strong activity on plant pathogens, with great potential for controlling tomato grey mold and pepper leaf scorch and being used in integrated disease control to reduce chemical application.

  11. Inhibitory effect of aqueous dandelion extract on HIV-1 replication and reverse transcriptase activity

    Science.gov (United States)

    2011-01-01

    Background Acquired immunodeficiency syndrome (AIDS), which is caused by the human immunodeficiency virus (HIV), is an immunosuppressive disease that results in life-threatening opportunistic infections. The general problems in current therapy include the constant emergence of drug-resistant HIV strains, adverse side effects and the unavailability of treatments in developing countries. Natural products from herbs with the abilities to inhibit HIV-1 life cycle at different stages, have served as excellent sources of new anti-HIV-1 drugs. In this study, we aimed to investigate the anti-HIV-1 activity of aqueous dandelion extract. Methods The pseudotyped HIV-1 virus has been utilized to explore the anti-HIV-1 activity of dandelion, the level of HIV-1 replication was assessed by the percentage of GFP-positive cells. The inhibitory effect of the dandelion extract on reverse transcriptase activity was assessed by the reverse transcriptase assay kit. Results Compared to control values obtained from cells infected without treatment, the level of HIV-1 replication and reverse transcriptase activity were decreased in a dose-dependent manner. The data suggest that dandelion extract has a potent inhibitory activity against HIV-1 replication and reverse transcriptase activity. The identification of HIV-1 antiviral compounds from Taraxacum officinale should be pursued. Conclusions The dandelion extract showed strong activity against HIV-1 RT and inhibited both the HIV-1 vector and the hybrid-MoMuLV/MoMuSV retrovirus replication. These findings provide additional support for the potential therapeutic efficacy of Taraxacum officinale. Extracts from this plant may be regarded as another starting point for the development of an antiretroviral therapy with fewer side effects. PMID:22078030

  12. Inhibitory effect of aqueous dandelion extract on HIV-1 replication and reverse transcriptase activity

    Directory of Open Access Journals (Sweden)

    Han Huamin

    2011-11-01

    Full Text Available Abstract Background Acquired immunodeficiency syndrome (AIDS, which is caused by the human immunodeficiency virus (HIV, is an immunosuppressive disease that results in life-threatening opportunistic infections. The general problems in current therapy include the constant emergence of drug-resistant HIV strains, adverse side effects and the unavailability of treatments in developing countries. Natural products from herbs with the abilities to inhibit HIV-1 life cycle at different stages, have served as excellent sources of new anti-HIV-1 drugs. In this study, we aimed to investigate the anti-HIV-1 activity of aqueous dandelion extract. Methods The pseudotyped HIV-1 virus has been utilized to explore the anti-HIV-1 activity of dandelion, the level of HIV-1 replication was assessed by the percentage of GFP-positive cells. The inhibitory effect of the dandelion extract on reverse transcriptase activity was assessed by the reverse transcriptase assay kit. Results Compared to control values obtained from cells infected without treatment, the level of HIV-1 replication and reverse transcriptase activity were decreased in a dose-dependent manner. The data suggest that dandelion extract has a potent inhibitory activity against HIV-1 replication and reverse transcriptase activity. The identification of HIV-1 antiviral compounds from Taraxacum officinale should be pursued. Conclusions The dandelion extract showed strong activity against HIV-1 RT and inhibited both the HIV-1 vector and the hybrid-MoMuLV/MoMuSV retrovirus replication. These findings provide additional support for the potential therapeutic efficacy of Taraxacum officinale. Extracts from this plant may be regarded as another starting point for the development of an antiretroviral therapy with fewer side effects.

  13. Inhibitory effect of corcin on aggregation of 1N/4R human tau protein in vitro

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    Ali Mohammadi Karakani

    2015-05-01

    Full Text Available Objective(s:Alzheimer's disease (AD is the most common age-related neurodegenerative disorder. One of the hallmarks of AD is an abnormal accumulation of fibril forms of tau protein which is known as a microtubule associated protein. In this regard, inhibition of tau aggregation has been documented to be a potent therapeutic approach in AD and tauopathies. Unfortunately, the available synthetic drugs have modest beneficial efficacy with several side effects. Therefore, pipeline drugs from natural sources with anti-aggregation properties can be useful in the prevention and treatment of AD. Among medicinal plants, saffron (Crocus sativus, L., as a traditional herbal medicine has different pharmacological properties and can be used as treatment for several nervous system impairment including depression and dementia. Crocin as a major constituent of saffron is the glycosylated form of crocetin. Materials and Methods:  In this study, we investigated the inhibitory effect of crocin on aggregation of recombinant human tau protein 1N/4R isoform using biochemical methods and cell culture. Results:  Results revealed that tau protein under the fibrillation condition and in the presence of crocin had enough stability with low tendency for aggregation. Crocin inhibited tau aggregation with IC50 of 100 µg/ml.  Furthermore, transmission electron microscopy images confirmed that crocin could suppress the formation of tau protein filaments. Conclusion: Inhibitory effect of crocin could be related to its interference with nucleation phase that led to increases in monomer species of tau protein. Based on our results, crocin is recommended as a proper candidate to be used in AD treatment.

  14. Inhibitory effects of budesonide, desloratadine and dexamethasone on cytokine release from human mast cell line (HMC-1).

    Science.gov (United States)

    Zhao, Y; Leung, P C; Woo, K S; Chen, G G; Wong, Y O; Liu, S X; van Hasselt, C A

    2004-12-01

    To determine the inhibitory potency of budesonide on interleukin (IL)-4, 6 and 8, GM-CSF and TNF-alpha release from the human mast cell line (HMC-1) in comparison with the systemic glucocorticosteroid, dexamethasone, and H(1) antagonist, desloratadine. HMC-1 was stimulated with 25 ng/ml phorbol 12- myristate 13-acetate (PMA) and 2.5 x 10(-7) M ionomycin (A23187) for 6, 12 and 24 h in both the presence and absence of 10(-6)-10(-10) M concentrations of the test drugs. Culture supernatants were collected and assayed by ELISAs. HMC-1 produced substantial amounts of GM-CSF and IL-8 and smaller amounts of TNF-alpha, IL-4 and IL-6 after being stimulated with PMA together with A23187. Budesonide and dexamethasone had potent inhibitory effects and desloratadine had modest inhibitory effects on the release of these cytokines. Budesonide was more potent than dexamethasone at most concentrations and time points. IL-4 was the cytokine which was most susceptible to inhibition by the three tested drugs. The inhibitory effects, in some cases, were time- and concentration-dependent. Budesonide had a potent inhibitory effect on cytokine release from HMC-1. Its potency was greater than that of both dexamethasone and desloratadine.

  15. Inhibitory Effect of Plant Manilkara subsericea against Biological Activities of Lachesis muta Snake Venom

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    Eduardo Coriolano De Oliveira

    2014-01-01

    Full Text Available Snake venom is composed of a mixture of substances that caused in victims a variety of pathophysiological effects. Besides antivenom, literature has described plants able to inhibit injuries and lethal activities induced by snake venoms. This work describes the inhibitory potential of ethanol, hexane, ethyl acetate, or dichloromethane extracts and fractions from stem and leaves of Manilkara subsericea against in vivo (hemorrhagic and edema and in vitro (clotting, hemolysis, and proteolysis activities caused by Lachesis muta venom. All the tested activities were totally or at least partially reduced by M. subsericea. However, when L. muta venom was injected into mice 15 min first or after the materials, hemorrhage and edema were not inhibited. Thus, M. subsericea could be used as antivenom in snakebites of L. muta. And, this work also highlights Brazilian flora as a rich source of molecules with antivenom properties.

  16. Investigation of hydrazide derivatives inhibitory effect on peroxidase enzyme purified from turnip roots

    Science.gov (United States)

    Almaz, Züleyha; Öztekin, Aykut; Özdemir, Hasan

    2017-04-01

    Peroxidases (EC: 1.11.1.7) are haem proteins and contain iron (III) protoporphyrin IX (ferriprotoporphyrin IX) as the prosthetic group [1]. They are found in all cells and play a critical role in many biological processes, such as the host-defense mechanism [2]. Peroxidases (PODs) are widely used in clinical biochemistry, enzyme immunoassays, synthesis of various aromatic chemicals, treatment of waste water containing phenolic compounds [3, 4]. In this study, peroxidase enzyme was purified with Para amino benzohydrazide (PABH)-L-Tyrosine Sepharose 4B affinity chromatography to investigate the inhibitory effect of hydrazide derivatives on Turnip (Brassica rapa L.). IC50 values and Ki constants were calculated for the molecules of 6-Amino nicotinic hydrazide, 6-Amino-5-bromo nicotinic hydrazide, 2-Amino-5-hydroxy benzohydrazide, 4-Amino-3-hydroxy benzohydrazide on purified enzyme and inhibition type of these molecules were determined.

  17. Phytochemicals with NO inhibitory effects and interactions with iNOS protein from Trigonostemon howii.

    Science.gov (United States)

    Ma, Jun; Yang, Xueyuan; Wang, Peixia; Dong, Bangjian; Su, Guochen; Tuerhong, Muhetaer; Jin, Da-Qing; Xu, Jing; Lee, Dongho; Ohizumi, Yasushi; Lin, Jianping; Guo, Yuanqiang

    2017-12-01

    A phytochemical investigation to obtain new NO inhibitors led to the isolation of nine compounds including one new guaiane-type sesquiterpenoid (1) and two new cleistanthane diterpenoids (2 and 3) from the stems of Trigonostemon howii. Their structures were elucidated on the basis of extensive 1D and 2D NMR spectroscopic data analysis, and the absolute configurations of new compounds 1-3 were established via comparison of experimental and calculated electronic circular dichroism (ECD) spectra. Compounds 2 and 3 possess a rare 3,4-seco-cleistanthane diterpenoid skeleton. All of the compounds showed inhibitory effects on lipopolysaccharide-induced NO production in murine microglial BV-2 cells. The further molecular docking studies indicated the strong interactions between some bioactive compounds with the iNOS protein, which revealed the possible and potential mechanism of NO inhibition of bioactive compounds. Copyright © 2017 Elsevier Inc. All rights reserved.

  18. Inhibitory Effect of Triterpenoids from Panax ginseng on Coagulation Factor X

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    Lingxin Xiong

    2017-04-01

    Full Text Available Enzymes involved in the coagulation process have received great attention as potential targets for the development of oral anti-coagulants. Among these enzymes, coagulation factor Xa (FXa has remained the center of attention in the last decade. In this study, 16 ginsenosides and two sapogenins were isolated, identified and quantified. To determine the inhibitory potential on FXa, the chromogenic substrates method was used. The assay suggested that compounds 5, 13 and 18 were mainly responsible for the anti-coagulant effect. Furthermore, these three compounds also possessed high thrombin selectivity in the thrombin inhibition assay. Furthermore, Glide XP from Schrödinger was employed for molecular docking to clarify the interaction between the bioactive compounds and FXa. Therefore, the chemical and biological results indicate that compounds 5 (ginsenoside Rg2, 13 (ginsenoside Rg3 and 18 (protopanaxtriol, PPT are potential natural inhibitors against FXa.

  19. Inhibitory effect of gold nanoparticles on the D-ribose glycation of bovine serum albumin

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    Liu W

    2014-11-01

    Full Text Available Weixi Liu,1 Menashi A Cohenford,1–3 Leslie Frost,3 Champika Seneviratne,4 Joel A Dain1 1Department of Chemistry, University of Rhode Island, Kingston, RI, USA; 2Department of Integrated Science and Technology, 3Department of Chemistry, Marshall University, Huntington, WV, USA; 4Department of Chemistry, College of the North Atlantic, Labrador, NL, Canada Abstract: Formation of advanced glycation end products (AGEs by nonenzymatic glycation of proteins is a major contributory factor to the pathophysiology of diabetic conditions including senile dementia and atherosclerosis. This study describes the inhibitory effect of gold nanoparticles (GNPs on the D-ribose glycation of bovine serum albumin (BSA. A combination of analytical methods including ultraviolet–visible spectrometry, high performance liquid chromatography, circular dichroism, and matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF mass spectrometry were used to determine the extent of BSA glycation in the presence of citrate reduced spherical GNPs of various sizes and concentrations. GNPs of particle diameters ranging from 2 nm to 20 nm inhibited BSA’s AGE formation. The extent of inhibition correlated with the total surface area of the nanoparticles. GNPs of highest total surface area yielded the most inhibition whereas those with the lowest total surface area inhibited the formation of AGEs the least. Additionally, when GNPs’ total surface areas were set the same, their antiglycation activities were similar. This inhibitory effect of GNPs on BSA’s glycation by D-ribose suggests that colloidal particles may have a therapeutic application for the treatment of diabetes and conditions that promote hyperglycemia. Keywords: gold nanoparticles, glycation, AGEs, GNPs, BSA

  20. Inhibitory effect of select nitrocompounds on growth and survivability of Listeria monocytogenes in vitro.

    Science.gov (United States)

    Dimitrijevic, M; Anderson, R C; Callaway, T R; Jung, Y S; Harvey, R B; Ricke, S C; Nisbet, D J

    2006-05-01

    We report the effects of 2-nitro-1-propanol (2NPOH), 2-nitroethanol (2NEOH), and nitroethane (NE) on growth and survivability of Listeria monocytogenes. In all cases, inhibition was greatest with 2NPOH and least with NE. For example, specific growth rates of L. monocytogenes strain 18 declined (P nitrocompound was 0.62 +/- 0.02 h(-1). Specific growth rates of L. monocytogenes Scott A decreased (P < 0.05) 67, 45, and 11%, respectively, from controls (0.67 +/- 0.02 h(-1)) when cultured similarly. Specific growth rates for L. monocytogenes strain 18 incubated similarly except at 30 degrees C were reduced (P < 0.05) 76, 60, and 30%, respectively, and were reduced (P < 0.05) 78, 23, and 23% during anaerobic culture at 30 degrees C in brain heart infusion broth containing 15 mM 2NPOH, 2NEOH, or NE (control rates ranged from 0.37 +/- 0.07 to 0.74 +/- 0.05 h(-1)). Survivability of L. monocytogenes strain 18 was reduced (P < 0.05) during aerobic storage (4 months at 4 degrees C) in brain heart infusion broth containing 2NPOH or 2NEOH (by 7.8 and 1.9 log units, respectively) but not NE. The inhibitory effect of 2NPOH was approximately 20% greater during growth at pH 7.0 than at pH 5.6 or 8.0. These results demonstrate the differential inhibitory activity of 2NPOH, 2NEOH, and NE against L. monocytogenes in vitro.

  1. In vitro inhibitory effect on pancreatic lipase activity of subfractions from ethanol extracts of fermented Oats (Avena sativa L.) and synergistic effect of three phenolic acids.

    Science.gov (United States)

    Cai, Shengbao; Wang, Ou; Wang, Mengqian; He, Jianfeng; Wang, Yong; Zhang, Di; Zhou, Feng; Ji, Baoping

    2012-07-25

    The purpose of the present work is to study the pancreatic lipase inhibitory effects of different subfractions (n-hexane, ethyl acetate (EA), n-butanol, and water) from ethanol extracts of nonfermented and fungi-fermented oats and to delineate the interactions of three primary phenolic acids in the EA subfractions. The EA subfraction showed the highest inhibitory effect on pancreatic lipase activity at 1.5 mg/mL compared to the other subfractions, regardless of whether the oats were fermented. Meanwhile, both of the EA subfractions of two fungi-fermented oats demonstrated more effective inhibitory activity than that of nonfermented oats. A positive correlation between the total phenolics content and inhibitory activity was found. The inhibitory ability of the EA subfraction from nonfermented or fermented oats also displayed a dose-dependent effect. The standards of caffeic, ferulic, and p-coumaric acids, mainly included in EA subfractions of fermented oats, also displayed a dose-dependent inhibitory effect. A synergistic effect of each binary combination of p-coumaric, ferulic, and caffeic acids was observed, especially at 150.0 μg/mL. Those results indicate that fungi-fermented oats have a more effective inhibitory ability on pancreatic lipase and polyphenols may be the most effective component and could be potentially used for dietary therapy of obesity.

  2. Inhibitory effects of selected Thai medicinal plants on Na+,K+-ATPase.

    Science.gov (United States)

    Ngamrojanavanich, Nattaya; Manakit, Srinual; Pornpakakul, Surachai; Petsom, Amorn

    2006-09-01

    Extracts of ten Thai indigenous medicinal plants having ethnomedical application in the treatment of dysuria were tested for their Na(+),K(+)-ATPase inhibitory activity. The hexane extracts of Cyperus rotundus and Orthosiphon aristatus showed high potent inhibitory activity on crude enzyme Na(+),K(+)-ATPase from rat brain.

  3. Multilingual Stroop Performance: Effects of Trilingualism and Proficiency on Inhibitory Control

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    Marian, Viorica; Blumenfeld, Henrike K.; Mizrahi, Elena; Kania, Ursula; Cordes, Anne-Kristin

    2013-01-01

    Previous research suggests that multilinguals' languages are constantly co-activated and that experience managing this co-activation changes inhibitory control function. The present study examined language interaction and inhibitory control using a colour-word Stroop task. Multilingual participants were tested in their three most proficient…

  4. Antibacterial activities of coagulase-negative staphylococci from bovine teat apex skin and their inhibitory effect on mastitis-related pathogens.

    Science.gov (United States)

    Braem, G; Stijlemans, B; Van Haken, W; De Vliegher, S; De Vuyst, L; Leroy, F

    2014-05-01

    To explore antibacterial activities of coagulase-negative staphylococci (CoNS) from teat apices of dairy cows towards mastitis-causing pathogens. Of 254 CoNS, 38 displayed bacteriocin-like activity after a first screening. Seven of these strains displayed activity against at least one mastitis-related pathogen (Streptococcus uberis, Streptococcus dysgalactiae and Staphylococcus aureus). Staphylococcus chromogenes L217 displayed the strongest inhibitory effect, being active against all tested mastitis-related pathogens and most tested CoNS. Based on cation exchange and reversed-phase chromatography, in addition to N-terminal Edman degradation and PCR, the antibacterial peptide was identified as a nukacin-type bacteriocin and named nukacin L217. Although staphylococcal bacteriocins are generally found in the cell-free supernatants of liquid cultures, Staph. chromogenes L217 only led to detectable activity when grown on agar medium. Bacteriocin-like activities are not uncommon among CoNS from teat apices and may inhibit mastitis-causing pathogens, as found for nukacin L217 production by Staph. chromogenes L217. Nukacin L217 is the first identified bacteriocin of the species Staph. chromogenes and displays unusual production kinetics, that is, requiring surface growth of its producer. The fact that nukacins are produced by different CoNS species suggests a role in the teat skin ecosystem. © 2014 The Society for Applied Microbiology.

  5. Inhibitory Effect of Capparis spinosa Extract on Pancreatic Alpha-Amylase Activity

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    Mostafa Selfayan

    2016-04-01

    Full Text Available Background Diabetes mellitus is a metabolic disorder characterized by high blood glucose level caused due to deficiency of insulin secretion or insulin function. The inhibition of carbohydrate hydrolyzing enzymes such as α-amylase can be an important strategy for decrease postprandial blood glucose level in patients with type II diabetes. Plants contains different chemical constituents with potential for inhibition of α-amylase and hence maybe used as therapeutic. Objectives The aim of the present study is to investigate the effect of the ethanolic extract of Capparis spinosa on pancreatic α-amylase activities to find out the relevance of the plant in controlling blood sugar. Materials and Methods In this experimental study, root and leaves of C. spinosa were tested for α-amylase inhibition. Different concentrations (1.56, 3.12, 6.25, 12.5 and 25 mg/mL of extracts were incubated with enzyme substrate solution and the spectrometric method used for measure enzyme activity. Also acarbose was used as the standard inhibitor. Results Both root and leaves extracts showed inhibition of α-amylase (root = 97.31% and leaves = 98.92%. The root and leaves extracts of C. spinosa exhibited appreciable α-amylase inhibitory activity with an IC50 values 5.93 mg/mL and 3.89 mg/mL respectively, when compared with acarbose (IC50 value 0.038 mg/mL. Conclusions This study supports that root and leaves extracts of C. spinosa exhibit considerable α-amylase inhibitory activities. These results could be useful for developing functional foods by combination of plant-based foods for treatment of diabetes mellitus.

  6. Comparison of the acute effects of high-intensity interval training and continuous aerobic walking on inhibitory control.

    Science.gov (United States)

    Kao, Shih-Chun; Westfall, Daniel R; Soneson, Jack; Gurd, Brendon; Hillman, Charles H

    2017-09-01

    The purpose of this study was to investigate the effects of a single bout of high-intensity interval training (HIIT) and continuous aerobic exercise (CAE) on inhibitory control. The P3 component of the stimulus-locked ERP was collected in 64 young adults during a modified flanker task following 20 min of seated rest, 20 min of CAE, and 9 min of HIIT on separate days in counterbalanced order. Participants exhibited shorter overall reaction time following CAE and HIIT compared to seated rest. Response accuracy improved following HIIT in the task condition requiring greater inhibitory control compared to seated rest and CAE. P3 amplitude was larger following CAE compared to seated rest and HIIT. Decreased P3 amplitude and latency were observed following HIIT compared to seated rest. The current results replicated previous findings indicating the beneficial effect of acute CAE on behavioral and neuroelectric indices of inhibitory control. With a smaller duration and volume of exercise, a single bout of HIIT resulted in additional improvements in inhibitory control, paralleled by a smaller and more efficient P3 component. In sum, the current study demonstrated that CAE and HIIT differentially facilitate inhibitory control and its underlying neuroelectric activation, and that HIIT may be a time-efficient approach for enhancing cognitive health. © 2017 Society for Psychophysiological Research.

  7. Sorafenib Has sEH Inhibitory Activity Which Contributes to Its Effect Profile in vivo

    Science.gov (United States)

    Liu, Jun-Yan; Park, See-Hyoung; Morisseau, Christophe; Hwang, Sung Hee; Hammock, Bruce D.; Weiss, Robert H.

    2009-01-01

    The advent of multi-kinase inhibitors targeting the VEGF-receptor has revolutionized the treatment of highly angiogenic malignances such as renal cell carcinoma. Interestingly, several such inhibitors are commercially available, and they each possess diverse specific beneficial and adverse effect profiles. In examining the structure of sorafenib, it was hypothesized that this compound would possess inhibitory effects on the soluble epoxide hydrolase (sEH), an enzyme with pleiotropic effects on inflammation and vascular disease. We now show that sorafenib, but not another VEGF-receptor targeted inhibitor sunitinib, is a potent inhibitor of the human sEH in vitro (KI = 17 ± 4 nM). Furthermore, sorafenib causes the expected in vivo shift in oxylipid profile resulting from sEH inhibition, evidence of a reduction in the acute inflammatory response. Lipopolysaccharide (LPS)-induced hypotension was reversed with sorafenib, but not sunitinib, treatment, suggesting that sEH inhibition accounts for at least part of the anti-inflammatory effect of sorafenib. The pharmacokinetic studies presented here in light of the known potency of sorafenib as a sEH inhibitor indicate that the sEH will be largely inhibited at therapeutic doses of sorafenib. Thus it is likely that sEH inhibition contributes to the beneficial effects from the inhibition of the VEGF-receptor and other kinases during treatment with sorafenib. PMID:19671760

  8. Sorafenib has soluble epoxide hydrolase inhibitory activity, which contributes to its effect profile in vivo.

    Science.gov (United States)

    Liu, Jun-Yan; Park, See-Hyoung; Morisseau, Christophe; Hwang, Sung Hee; Hammock, Bruce D; Weiss, Robert H

    2009-08-01

    The advent of multikinase inhibitors targeting the vascular endothelial growth factor (VEGF) receptor has revolutionized the treatment of highly angiogenic malignancies such as renal cell carcinoma. Interestingly, several such inhibitors are commercially available, and they each possess diverse specific beneficial and adverse effect profiles. In examining the structure of sorafenib, it was hypothesized that this compound would possess inhibitory effects on the soluble epoxide hydrolase, an enzyme with pleiotropic effects on inflammation and vascular disease. We now show that sorafenib but not another VEGF receptor targeted inhibitor sunitinib is a potent inhibitor of the human soluble epoxide hydrolase in vitro (K(I) = 17 +/- 4 nmol/L). Furthermore, sorafenib causes the expected in vivo shift in oxylipid profile resulting from soluble epoxide hydrolase inhibition, evidence of a reduction in the acute inflammatory response. Lipopolysaccharide-induced hypotension was reversed with sorafenib but not sunitinib treatment, suggesting that soluble epoxide hydrolase inhibition accounts for at least part of the anti-inflammatory effect of sorafenib. The pharmacokinetic studies presented here in light of the known potency of sorafenib as a soluble epoxide hydrolase inhibitor indicate that the soluble epoxide hydrolase will be largely inhibited at therapeutic doses of sorafenib. Thus, it is likely that soluble epoxide hydrolase inhibition contributes to the beneficial effects from the inhibition of the VEGF receptor and other kinases during treatment with sorafenib.

  9. Inhibitory effect of angiostatins on activity of the plasminogen/plasminogen activator system.

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    Aisina, R B; Mukhametova, L I; Gulin, D A; Levashov, M Y; Prisyazhnaya, N V; Gershkovich, K B; Varfolomeyev, S D

    2009-10-01

    Angiostatins, kringle-containing fragments of plasminogen, are potent inhibitors of angiogenesis. Effects of three angiostatin forms, K1-3, K1-4, and K1-4.5 (0-2 microM), on the rate of native Glu-plasminogen activation by its physiological activators in the absence or presence of soluble fibrin were investigated in vitro. Angiostatins did not affect the intrinsic amidolytic activities of plasmin and plasminogen activators of tissue type (tPA) and urokinase type (single-chain scuPA and two-chain tcuPA), but inhibited conversion of plasminogen to plasmin in a dose-dependent manner. All three angiostatins suppressed Glu-plasminogen activation by tcuPA independently of the presence of fibrin, and the inhibitory effect increased in the order: K1-3 < K1-4 < K1-4.5. The inhibitory effects of angiostatins on the scuPA activator activity were lower and further decreased in the presence of fibrin. Angiostatin K1-3 (up to 2 microM) had no effect, while 2 microM angiostatins K1-4 and K1-4.5 inhibited the fibrin-stimulated Glu-plasminogen activation by tPA by 50 and 100%, respectively. The difference in effects of the three angiostatins on the Glu-plasminogen activation by scuPA, tcuPA, and tPA in the absence or presence of fibrin is due to the differences in angiostatin structures, mechanisms of action, and fibrin-specificity of plasminogen activators, as well as due to the influence of fibrin on the Glu-plasminogen conformation. Angiostatins in vivo, which mimic plasminogen-binding activity, can inhibit plasminogen activation stimulated by various proteins (including fibrin) of extracellular matrix, thereby blocking cell migration and angiogenesis. The data of this work indicate that the inhibition of Glu-plasminogen activation under the action of physiological plasminogen activators by angiostatins can be implicated in the complex mechanism of their antiangiogenic and antitumor action.

  10. Inhibitory effect of lidocaine on the sarcoplasmic reticulum Ca2+-dependent atpase from temporalis muscle.

    Science.gov (United States)

    Sánchez, Gabriel A; Casadoumecq, Ana C; Alonso, Guillermo L; Takara, Delia

    2010-01-01

    Myotoxic effects of local anesthetics on skeletal musclefibers involve the inhibition ofsarcoplasmic reticulum Ca2+ -dependent ATPase activity and Ca2 transport. Lidocaine is a local anesthetic frequently used to relieve the symptoms of trigeminal neuralgia. The aim of this work was to test the inhibitory and/or stimulatory effect of lidocaine on sarcoplasmic reticulum Ca2+ -dependent ATPase isolated from rabbit temporalis muscle. Ca2+ -dependent ATPase activity was determined by a colorimetric method Calcium-binding to the Ca dependent ATPase, Ca2+ transport, and phosphorylation of the enzyme by ATP were determined with radioisotopic techniques. Lidocaine inhibited the Ca2+ -dependent ATPase activity in a concentration-dependent manner. The preincubation of the sarcoplasmic reticulum membranes with lidocaine enhanced the Ca2+ dependent ATPase activity in the absence of calcium ionophore. Lidocaine also inhibited both Ca2+ uptake and enzyme phosphorylation by ATP but had no effect on Ca2+ -binding to the enzyme. We conclude that the effect of lidocaine on the sarcoplasmic reticulum Ca2+ -dependent ATPase from temporalis muscle is due to the drug's direct interaction with the enzyme and the increased permeability of the sarcoplasmic reticulum membrane to Ca.

  11. Inhibitory effect of synthetic cannabinoids on CYP1A activity in mouse liver microsomes.

    Science.gov (United States)

    Ashino, Takashi; Hakukawa, Kanae; Itoh, Yuka; Numazawa, Satoshi

    2014-01-01

    Synthetic cannabinoids developed by chemical modification are believed to bind to cannabinoid receptors and cause neurological effects similar to cannabis; however, their effects on drug metabolizing enzymes are unknown. This study aimed to elucidate the effect of synthetic cannabinoids on cytochrome P450 1A activity. Naphthoylindole, a basic structure of the major synthetic cannabinoids, strongly inhibited CYP1A activity in a competitive manner; the apparent Ki value was 0.40 μM. The N-Alkylated derivatives of naphthoylindole, MAM-2201 and JWH-019, also inhibited CYP1A activity in a concentration-dependent manner; however, their inhibitory effects were weaker than naphthoylindole. An adamantylamidoindole derivative, STS-135, showed inhibition of CYP1A activity in a concentrationdependent manner, but the adamantoylindole derivatives, AB-001 and AM-1248, did not. A tetramethylcyclopropanoylindole derivative, UR-144, showed a weak inhibition of CYP1A activity at high concentrations. These results suggest that synthetic cannabinoids and their basic molecules are capable of inhibiting CYP1A enzymatic activity.

  12. Acute inhibitory effect of alpha-mangostin on sarcoplasmic reticulum calcium-ATPase and myocardial relaxation.

    Science.gov (United States)

    Phungphong, Sukanya; Kijtawornrat, Anusak; de Tombe, Pieter P; Wattanapermpool, Jonggonnee; Bupha-Intr, Tepmanas; Suksamrarn, Sunit

    2017-10-01

    The benefits of α-mangostin for various tissues have been reported, but its effect on the heart has not been clarified. This study aimed to evaluate the effects of α-mangostin on cardiac function. Using a cardiac sarcoplasmic reticulum (SR) membrane preparation, α-mangostin inhibited SR Ca 2+ -ATPase activity in a dose-dependent manner (IC 50 of 6.47 ± 0.7 μM). Its suppressive effect was specific to SR Ca 2+ -ATPase but not to myofibrillar Ca 2+ -ATPase. Using isolated cardiomyocytes, 50 μM of α-mangostin significantly increased the duration of cell relengthening and increased the duration of Ca 2+ transient decay, suggesting altered myocyte relaxation. The relaxation effect of α-mangostin was also supported in vivo after intravenous infusion. A significant suppression of both peak pressure and rate of ventricular relaxation (-dP/dt) relative to DMSO infusion was observed. The results from the present study demonstrated that α-mangostin exerts specific inhibitory action on SR Ca 2+ -ATPase activity, leading to myocardial relaxation dysfunction. © 2017 Wiley Periodicals, Inc.

  13. Does Acupuncture Needling Induce Analgesic Effects Comparable to Diffuse Noxious Inhibitory Controls?

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    Juerg Schliessbach

    2012-01-01

    Full Text Available Diffuse noxious inhibitory control (DNIC is described as one possible mechanism of acupuncture analgesia. This study investigated the analgesic effect of acupuncture without stimulation compared to nonpenetrating sham acupuncture (NPSA and cold-pressor-induced DNIC. Forty-five subjects received each of the three interventions in a randomized order. The analgesic effect was measured using pressure algometry at the second toe before and after each of the interventions. Pressure pain detection threshold (PPDT rose from 299 kPa (SD 112 kPa to 364 kPa (SD 144, 353 kPa (SD 135, and 467 kPa (SD 168 after acupuncture, NPSA, and DNIC test, respectively. There was no statistically significant difference between acupuncture and NPSA at any time, but a significantly higher increase of PPDT in the DNIC test compared to acupuncture and NPSA. PPDT decreased after the DNIC test, whereas it remained stable after acupuncture and NPSA. Acupuncture needling at low pain stimulus intensity showed a small analgesic effect which did not significantly differ from placebo response and was significantly less than a DNIC-like effect of a painful noninvasive stimulus.

  14. An evaluation of the RNase H inhibitory effects of Vietnamese medicinal plant extracts and natural compounds.

    Science.gov (United States)

    Tai, Bui Huu; Nhut, Nguyen Duy; Nhiem, Nguyen Xuan; Quang, Tran Hong; Thanh Ngan, Nguyen Thi; Thuy Luyen, Bui Thi; Huong, Tran Thu; Wilson, Jennifer; Beutler, John A; Ban, Ninh Khac; Cuong, Nguyen Manh; Kim, Young Ho

    2011-10-01

    Acquired immune deficiency syndrome (AIDS) is a severe pandemic disease especially prevalent in poor and developing countries. Thus, developing specific, potent antiviral drugs that restrain infection by human immunodeficiency virus type 1 (HIV-1), a major cause of AIDS, remains an urgent priority. This study evaluated 32 extracts and 23 compounds from Vietnamese medicinal plants for their inhibitory effects against HIV-1 ribonuclease H (RNase H) and their role in reversing the cytopathic effects of HIV. The plants were air-dried and extracted in different solvent systems to produce plant extracts. Natural compounds were obtained as previously published. Samples were screened for RNase H inhibition followed by a cytopathic assay. Data were analyzed using the Microsoft Excel. At 50 μg/mL, 11 plant extracts and five compounds inhibited over 90% of RNase H enzymatic activity. Methanol extracts from Phyllanthus reticulatus and Aglaia aphanamixis leaves inhibited RNase H activity by 99 and 98%, respectively, whereas four extracts showed modest protection against the cytopathic effects of HIV. The screening results demonstrated that the butanol (BuOH) extract of Celastrus orbiculata leaves, methanol (MeOH) extracts of Glycosmis stenocarpa stems, Eurya ciliata leaves, and especially P. reticulatus leaves showed potential RNase H inhibition and protection against the viral cytopathic effects of HIV-1. Further chemical investigations should be carried out to find the active components of these extracts and compounds as potential anti-HIV drug candidates.

  15. Inhibitory effects of dietary Spirulina platensis on UVB-induced skin inflammatory responses and carcinogenesis.

    Science.gov (United States)

    Yogianti, Flandiana; Kunisada, Makoto; Nakano, Eiji; Ono, Ryusuke; Sakumi, Kunihiko; Oka, Sugako; Nakabeppu, Yusaku; Nishigori, Chikako

    2014-10-01

    Reactive oxygen species produced in response to UVR are important in skin tumor development. We have previously reported that deficiency of the Ogg1 gene, encoding the repair enzyme for 8-oxo-7,8-dihydroguanine (8-oxoG), increases skin tumor incidence in mice upon repetitive UVB exposure and modulation of UVB-induced inflammatory response. Spirulina platensis is used as a human food supplement because it contains abundant nutritional and antioxidant components. Therefore, we investigated the inhibitory effects of S. platensis on UVB-induced skin tumor development in Ogg1 knockout-(KO) mice and the wild-type (WT) counterpart. Dietary S. platensis suppressed tumor induction and development in both genotypes compared with our previous data without S. platensis. Induction of erythema and ear swelling, one of the hallmarks of UVB-induced inflammatory responses, was suppressed in the skin of Ogg1-KO mice and albino hairless mice fed with dietary S. platensis. Compared with untreated mice, S. platensis-administered mice showed significantly reduced 8-oxoG formation in the skin after UVB exposure. Moreover, we found that S. platensis effectively downregulated the signal proteins p38 mitogen-activated protein kinase, stress-activated protein kinase/c-Jun N-terminal kinase, and extracellular signal-regulated kinase after UVB exposure especially in Ogg1-KO mice. Our results suggest that S. platensis exerts antitumor effects against UVB irradiation in the skin through its anti-inflammatory and antioxidant effects.

  16. Inhibitory effects of four neonicotinoid active ingredients on acetylcholine esterase activity.

    Science.gov (United States)

    Győri, János; Farkas, Anna; Stolyar, Oksana; Székács, András; Mörtl, Mária; Vehovszky, Ágnes

    2017-12-01

    There is a great concern about the decline of pollinators, and neonicotinoids emerging bee disorders are assumed to play a significant role. Since changes in learning ability has been observed in honey bees exposed to some acetylcholine esterase (AChE) inhibitors, we therefore, tested in vitro the effect of four neonicotinoids on purified eel AChE. AChE activity was inhibited in a concentration-dependent manner, and calculated IC 50 values for thiamethoxam (IC 50 = 414 μM) and clothianidin (IC 50 = 160 μM) were found to be much higher compared to acetamiprid (IC 50 = 75.2 μM) and thiacloprid (IC 50 = 87.8 μM). The Lineweaver-Burk reciprocal plots for acetamiprid shows unchanged V max and increased K m values with inhibitor concentrations, while analysis of Michaelis-Menten plots shows predominantly competitive mechanism. The inhibition constant value (K i = 24.3 μM) indicates strong binding of the acetamiprid complex to AChE. Finally, the four tested neonicotinoids are not a uniform group regarding their blocking ability. Our results suggest a previously not established, direct AChE blocking mechanism of neonicotinoids tested, thus the neuronal AChE enzyme is likely among the direct targets of the neonicotinoid insecticides. We conclude, that these AChE inhibitory effects may also contribute to toxic effects on the whole exposed animal.

  17. Re-188 Enhances the Inhibitory Effect of Bevacizumab in Non-Small-Cell Lung Cancer

    Directory of Open Access Journals (Sweden)

    Jie Xiao

    2016-09-01

    Full Text Available The malignant behaviors of solid tumors such as growth, infiltration and metastasis are mainly nourished by tumor neovascularization. Thus, anti-angiogenic therapy is key to controlling tumor progression. Bevacizumab, a humanized anti-vascular endothelial growth factor (VEGF antibody, plus chemotherapy or biological therapy can prolong survival for cancer patients, but treatment-related mortality is a concern. To improve inhibitory effect and decrease side-effects on non-small-cell lung cancer (NSCLC, we used Re-188, which is a β emitting radionuclide, directly labeled with bevacizumab for radioimmunotherapy in a human A549 tumor model. Cytotoxic assay data showed that, after 188ReO4− or 188Re-bevacizumab at different concentration for 4 and 24 h, a time- and radioactivity does-dependent reduction in cell viability occurred. Also, an apoptosis assay conformed great apoptosis in the 188Re-bevacizumab group compared with controls and other treatment groups. In vivo, tumor volumes in the 188Re-bevacizumab (11.1 MBq/mice group were not reduced but growth was delayed compared with other groups. Thus, 188Re-bevacizumab enhanced the therapeutic effect of bevacizumab, suggesting a potential therapeutic strategy for NSCLC treatment.

  18. Medium Effects on Minimum Inhibitory Concentrations of Nylon-3 Polymers against E. coli

    Science.gov (United States)

    Choi, Heejun; Chakraborty, Saswata; Liu, Runhui; Gellman, Samuel H.; Weisshaar, James C.

    2014-01-01

    Minimum inhibitory concentrations (MICs) against E. coli were measured for three nylon-3 polymers using Luria-Bertani broth (LB), brain-heart infusion broth (BHI), and a chemically defined complete medium (EZRDM). The polymers differ in the ratio of hydrophobic to cationic subunits. The cationic homopolymer is inert against E. coli in BHI and LB, but becomes highly potent in EZRDM. A mixed hydrophobic/cationic polymer with a hydrophobic t-butylbenzoyl group at its N-terminus is effective in BHI, but becomes more effective in EZRDM. Supplementation of EZRDM with the tryptic digest of casein (often found in LB) recapitulates the LB and BHI behavior. Additional evidence suggests that polyanionic peptides present in LB and BHI may form electrostatic complexes with cationic polymers, decreasing activity by diminishing binding to the anionic lipopolysaccharide layer of E. coli. In contrast, two natural antimicrobial peptides show no medium effects. Thus, the use of a chemically defined medium helps to reveal factors that influence antimicrobial potency of cationic polymers and functional differences between these polymers and evolved antimicrobial peptides. PMID:25153714

  19. Inhibitory effect of essential oils against Trichosporon ovoides causing Piedra Hair Infection

    Directory of Open Access Journals (Sweden)

    Seema Saxena

    2012-12-01

    Full Text Available Piedra, is an asymptomatic fungal infection of the hair shaft, resulting in the formation of nodules of different hardness on the infected hair. The infection also known as Trichomycosis nodularis is a superficial fungal infection arising from the pathogen being restricted to the stratum corneum with little or no tissue reaction. The nodules are a concretion of hyphae and fruiting bodies of the fungus. Two varieties of Piedra may be seen, Black Piedra and White Piedra. The fungus Trichosporon ovoides is involved in the occurrence of both types of Piedras. The purpose of this study was to examine the effectiveness of selected essential oils for the control of growth of the fungus and to determine whether the antifungal effect was due to the major compounds of the oils. Two screening methods viz. Agar well diffusion assay and Minimum Inhibitory Concentration were adopted for the study. MIC and MFC were determined by tube dilution method. Essential oils from Eucalyptus, Ocimum basilicum, Mentha piperita, Cymbopogon flexuosus, Cymbopogon winterians, Trachyspermum ammi, Zingiber officinalis, Citrus limon, Cinnamomon zeylanicum, Salvia sclarea, Citrus aurantifolia, Melaleuca alternifolia, Citrus aurantium, Citrus bergamia, Pogostemon pathchouli, Cedrus atlantica, Jasminum officinale, Juniperus communis, Abelmoschus moschatus, Cyperus scariosus, Palargonium graveolens, Boswellia carterii, Rosa damascene, Veteveria zizanoides and Commiphora myrrha were evaluated. The essential oils of Cymbopogon winterians, Mentha piperita, Cinnamomum zeylanicum, Melaleuca alternifolia and Eucalyptus globulus were proved to be most effective against the fungus Trichosporon ovoides.

  20. Identification of ubiquitin in bovine milk and its growth inhibitory effects on human cancer cell lines.

    Science.gov (United States)

    Freiburghaus, C; Welinder, C; Tjörnstad, U; Lindmark-Månsson, H; Paulsson, M; Oredsson, S

    2010-08-01

    Bovine milk is associated with improved health and reduced risk of several diseases, among them cancer. Milk is a complex mixture of known and unknown components. The components and the mechanisms that contribute to the cancer-preventive effects are largely unknown. We set out to find new peptides in milk and identified ubiquitin (Ub) using matrix-assisted laser desorption ionization-time of flight mass spectrometry and Western blot. Using quantitative Western blot, we estimated the Ub concentration to be about 0.003 micromol/L in milk. We then decided to investigate the effect of treating human colon cancer CaCo-2 cells with Ub, using higher concentrations than in milk. CaCo-2 cells treated with 0.02 to 2.0 micromol/L Ub showed significantly decreased proliferation compared with untreated control cells. A higher growth inhibitory effect than in CaCo-2 cells was found in the neuroblastoma cell line SH-SY5Y treated with 0.02 to 0.2 micromol/L Ub. A bromodeoxyuridine DNA flow cytometric method was used to study cell cycle kinetics in Ub-treated CaCo-2 cells. The data point toward a prolongation of the G(1) phase. The levels of several cell cycle regulatory proteins were affected. Our data point to Ub possibly being one of the components in milk reducing the risk of cancer. Copyright (c) 2010 American Dairy Science Association. Published by Elsevier Inc. All rights reserved.

  1. Modeling of the Inhibitory Effect of Nanoparticles on Amyloid β Fibrillation.

    Science.gov (United States)

    Ramesh, Nirmal Kumar; Sudhakar, Swathi; Mani, Ethayaraja

    2018-03-22

    Experiments have shown that charged nanoparticles (NP) inhibit, partially or completely, the aggregation of Aβ protein monomers into fibrils. The equilibrium fibril content is found to be inversely proportional to the concentration of NP. In this work, we report a kinetic model for the fibrillation of Aβ protein in the presence of NP. In the model, apart from nucleation, elongation and fragmentation processes, the effect of NP is considered to cause a conformational change to the protein monomer, making the latter incompatible for aggregation. The simulated results explain the growth kinetics of pure Aβ (1-40) protein, and the kinetics in the presence of NP. The NP-monomer interaction considered in the model captures the significant effect of NP on the fibrillation process at a very molar ratio (NP to Aβ monomer) as low as 10 -4 . The model predictions are compared with two different NP systems, namely, gold and silica NP. The model can be applied to explain the inhibitory effect of other additives such as small molecules, NP, lipids, and surfactants that show a similar inhibition trend for fibril formation of Aβ and other proteins.

  2. Does inhibitory control training transfer?: behavioral and neural effects on an untrained emotion regulation task.

    Science.gov (United States)

    Beauchamp, Kathryn G; Kahn, Lauren E; Berkman, Elliot T

    2016-09-01

    Inhibitory control (IC) is a critical neurocognitive skill for successfully navigating challenges across domains. Several studies have attempted to use training to improve neurocognitive skills such as IC, but few have found that training generalizes to performance on non-trained tasks. We used functional magnetic resonance imaging (fMRI) to investigate the effect of IC training on a related but untrained emotion regulation (ER) task with the goal of clarifying how training alters brain function and why its effects typically do not transfer across tasks. We suggest hypotheses for training-related changes in activation relevant to transfer effects: the strength model and several plausible alternatives (shifting priorities, stimulus-response automaticity, scaffolding). Sixty participants completed three weeks of IC training and underwent fMRI scanning before and after. The training produced pre- to post-training changes in neural activation during the ER task in the absence of behavioral changes. Specifically, individuals in the training group demonstrated reduced activation during ER in the left inferior frontal gyrus and supramarginal gyrus, key regions in the IC neural network. This result is less consistent with the strength model and more consistent with a motivational account. Implications for future work aiming to further pinpoint mechanisms of training transfer are discussed. © The Author (2016). Published by Oxford University Press. For Permissions, please email: journals.permissions@oup.com.

  3. Medium effects on minimum inhibitory concentrations of nylon-3 polymers against E. coli.

    Science.gov (United States)

    Choi, Heejun; Chakraborty, Saswata; Liu, Runhui; Gellman, Samuel H; Weisshaar, James C

    2014-01-01

    Minimum inhibitory concentrations (MICs) against E. coli were measured for three nylon-3 polymers using Luria-Bertani broth (LB), brain-heart infusion broth (BHI), and a chemically defined complete medium (EZRDM). The polymers differ in the ratio of hydrophobic to cationic subunits. The cationic homopolymer is inert against E. coli in BHI and LB, but becomes highly potent in EZRDM. A mixed hydrophobic/cationic polymer with a hydrophobic t-butylbenzoyl group at its N-terminus is effective in BHI, but becomes more effective in EZRDM. Supplementation of EZRDM with the tryptic digest of casein (often found in LB) recapitulates the LB and BHI behavior. Additional evidence suggests that polyanionic peptides present in LB and BHI may form electrostatic complexes with cationic polymers, decreasing activity by diminishing binding to the anionic lipopolysaccharide layer of E. coli. In contrast, two natural antimicrobial peptides show no medium effects. Thus, the use of a chemically defined medium helps to reveal factors that influence antimicrobial potency of cationic polymers and functional differences between these polymers and evolved antimicrobial peptides.

  4. Inhibitory effect of essential oils against Trichosporon ovoides causing Piedra Hair Infection.

    Science.gov (United States)

    Saxena, Seema; Uniyal, Veena; Bhatt, R P

    2012-10-01

    Piedra, is an asymptomatic fungal infection of the hair shaft, resulting in the formation of nodules of different hardness on the infected hair. The infection also known as Trichomycosis nodularis is a superficial fungal infection arising from the pathogen being restricted to the stratum corneum with little or no tissue reaction. The nodules are a concretion of hyphae and fruiting bodies of the fungus. Two varieties of Piedra may be seen, Black Piedra and White Piedra. The fungus Trichosporon ovoides is involved in the occurrence of both types of Piedras. The purpose of this study was to examine the effectiveness of selected essential oils for the control of growth of the fungus and to determine whether the antifungal effect was due to the major compounds of the oils. Two screening methods viz. Agar well diffusion assay and Minimum Inhibitory Concentration were adopted for the study. MIC and MFC were determined by tube dilution method. Essential oils from Eucalyptus, Ocimum basilicum, Mentha piperita, Cymbopogon flexuosus, Cymbopogon winterians, Trachyspermum ammi, Zingiber officinalis, Citrus limon, Cinnamomon zeylanicum, Salvia sclarea, Citrus aurantifolia, Melaleuca alternifolia, Citrus aurantium, Citrus bergamia, Pogostemon pathchouli, Cedrus atlantica, Jasminum officinale, Juniperus communis, Abelmoschus moschatus, Cyperus scariosus, Palargonium graveolens, Boswellia carterii, Rosa damascene, Veteveria zizanoides and Commiphora myrrha were evaluated. The essential oils of Cymbopogon winterians, Mentha piperita, Cinnamomum zeylanicum, Melaleuca alternifolia and Eucalyptus globulus were proved to be most effective against the fungus Trichosporon ovoides.

  5. Inhibitory effect of essential oils against Trichosporon ovoides causing Piedra Hair Infection

    Science.gov (United States)

    Saxena, Seema; Uniyal, Veena; Bhatt, R.P.

    2012-01-01

    Piedra, is an asymptomatic fungal infection of the hair shaft, resulting in the formation of nodules of different hardness on the infected hair. The infection also known as Trichomycosis nodularis is a superficial fungal infection arising from the pathogen being restricted to the stratum corneum with little or no tissue reaction. The nodules are a concretion of hyphae and fruiting bodies of the fungus. Two varieties of Piedra may be seen, Black Piedra and White Piedra. The fungus Trichosporon ovoides is involved in the occurrence of both types of Piedras. The purpose of this study was to examine the effectiveness of selected essential oils for the control of growth of the fungus and to determine whether the antifungal effect was due to the major compounds of the oils. Two screening methods viz. Agar well diffusion assay and Minimum Inhibitory Concentration were adopted for the study. MIC and MFC were determined by tube dilution method. Essential oils from Eucalyptus, Ocimum basilicum, Mentha piperita, Cymbopogon flexuosus, Cymbopogon winterians, Trachyspermum ammi, Zingiber officinalis, Citrus limon, Cinnamomon zeylanicum, Salvia sclarea, Citrus aurantifolia, Melaleuca alternifolia, Citrus aurantium, Citrus bergamia, Pogostemon pathchouli, Cedrus atlantica, Jasminum officinale, Juniperus communis, Abelmoschus moschatus, Cyperus scariosus, Palargonium graveolens, Boswellia carterii, Rosa damascene, Veteveria zizanoides and Commiphora myrrha were evaluated. The essential oils of Cymbopogon winterians, Mentha piperita, Cinnamomum zeylanicum, Melaleuca alternifolia and Eucalyptus globulus were proved to be most effective against the fungus Trichosporon ovoides. PMID:24031963

  6. Inhibitory effects of antihistamines, diphenhydramine and chlorpheniramine, on proton currents in BV2 microglial cells.

    Science.gov (United States)

    Kim, Jiwon; Song, Jin-Ho

    2017-03-05

    Microglial NADPH oxidase is a major source of toxic reactive oxygen species produced during chronic neuroinflammation. Voltage-gated proton channel (H V 1) functions to maintain the intense activity of NADPH oxidase, and channel inhibition alleviates the pathology of neurodegenerative diseases such as ischemic stroke and multiple sclerosis associated with oxidative neuroinflammation. Antagonists of histamine H 1 receptors have beneficial effects against microglia-mediated oxidative stress and neurotoxicity. We examined the effects of the H 1 antihistamines, diphenhydramine and chlorpheniramine, on proton currents in BV2 microglial cells recorded using the whole-cell patch clamp technique. Diphenhydramine and chlorpheniramine reduced the proton currents with almost the same potency, yielding IC 50 values of 42 and 43μM, respectively. Histamine did not affect proton currents, excluding the involvement of histamine receptors in their action. Neither drug shifted the voltage-dependence of activation or the reversal potential of the proton currents, even though diphenhydramine slowed the activation and deactivation kinetics. The inhibitory effects of the two antihistamines on proton currents could be utilized to develop therapeutic agents for neurodegenerative diseases and other diseases associated with H V 1 proton channel abnormalities. Copyright © 2017 Elsevier B.V. All rights reserved.

  7. Inhibitory effect of leaf extract of Newbouldia laevis on the metabolic activities of alpha-glucosidase and alpha-amylase

    Directory of Open Access Journals (Sweden)

    Oyetunji T. Kolawole

    2013-12-01

    Full Text Available In this study, the effect of ethanol extract of the leaves of Newbouldia laevis on the activity of α-amylase and α-glucosidase was investigated. Inhibitory effect of N. laevis extract on α-glucosidase was tested in vitro using baker’s yeast α-glucosidase and rat intestinal α-glucosidase while α-amylase inhibitory effect was assayed using rat pancreatic α-amylase. α-Glucosidase inhibitory effect of the extract was also tested in vivo in diabetic and non-diabetic rats. N. laevis extract exhibited good α-glucosidase inhibitory activity in vitro with IC50 values of 2.2 µg/mL and 43.5 µg/mL for baker’s yeast and rat intestinal α-glucosidase respectively. The extract also inhibited rat pancreatic α-amylase activity with IC50 value of 58.7 µg/mL. In both diabetic and non-diabetic rats, N. laevis extract caused a significant reduction in postprandial blood glucose level after oral sucrose load. The results of this study indicate that N. laevis extract exerts its glucose-lowering effect through inhibition of α-glucosidase and α-amylase.

  8. Inhibitory Effect of Gallic acid on Production of Interleukins in Mouse Macrophage Stimulated by Lipopolysaccharide

    Directory of Open Access Journals (Sweden)

    Wansu Park

    2010-09-01

    Full Text Available Objectives: Gallic acid (GA is the major component of tannin which could be easily founded in various natural materials such as green tea, red tea, grape juice, and Corni Fructus. The purpose of this study is to investigate the effect of Gallic acid (GA on production of interleukin (IL in mouse macrophage Raw 264.7 cells stimulated by lipopolysaccharide (LPS. Methods: Productions of interleukins were measured by High-throughput Multiplex Bead based Assay with Bio-plex Suspension Array System based on xMAP (multi-analyte profiling beads technology. Firstly, cell culture supernatant was obtained after treatment with LPS and GA for 24 hour. Then, it was incubated with the antibody-conjugated beads for 30 minutes. And detection antibody was added and incubated for 30 minutes. And Strepavidin-conjugated Phycoerythrin (SAPE was added. After incubation for 30 minutes, the level of SAPE fluorescence was analyzed on Bio-plex Suspension Array System and concentration of interleukin was determined. Results: The results of the experiment are as follows. 1. GA significantly inhibited the production of IL-3, IL-10, IL-12p40, and IL-17 in LPS-induced mouse macrophage RAW 264.7 cells at the concentration of 25, 50, 100, 200 uM (p<0.05. 2. GA significantly inhibited the production of IL-6 in LPS-induced mouse macrophage RAW 264.7 cells at the concentration of 50, 100, 200 uM (p<0.05. 3. GA diminished the production of some cytokine such as IL-4, IL-5, and IL-13 in LPS-induced mouse macrophage RAW 264.7 cells. 4. GA did not show the inhibitory effect on the production of IL-1αand IL-9 in LPS-induced mouse macrophage RAW 264.7 cells. Conclusions: These results suggest that GA has anti-inflammatory activity related with its inhibitory effects on the production of interleukins such as IL-3, IL-10, IL-12p40, IL-17, and IL-6 in LPS-induced macrophages.

  9. Inhibitory noise

    Directory of Open Access Journals (Sweden)

    Alain Destexhe

    2010-03-01

    Full Text Available Cortical neurons in vivo may operate in high-conductance states, in which the major part of the neuron's input conductance is due to synaptic activity, sometimes several-fold larger than the resting conductance. We examine here the contribution of inhibition in such high-conductance states. At the level of the absolute conductance values, several studies have shown that cortical neurons in vivo are characterized by strong inhibitory conductances. However, conductances are balanced and spiking activity is mostly determined by fluctuations, but not much is known about excitatory and inhibitory contributions to these fluctuations. Models and dynamic-clamp experiments show that, during high-conductance states, spikes are mainly determined by fluctuations of inhibition, or by inhibitory noise. This stands in contrast to low-conductance states, in which excitatory conductances determine spiking activity. To determine these contributions from experimental data, maximum likelihood methods can be designed and applied to intracellular recordings in vivo. Such methods indicate that action potentials are indeed mostly correlated with inhibitory fluctuations in awake animals. These results argue for a determinant role for inhibitory fluctuations in evoking spikes, and do not support feed-forward modes of processing, for which opposite patterns are predicted.

  10. In vitro evaluation of capsaicin inhibitory effects on zonula occludens toxin in vibrio cholerae ATCC14035 strain

    Directory of Open Access Journals (Sweden)

    Soroor Erfanimanesh

    2014-10-01

    Conclusion: Capsaicin is one of the active compounds of red chili that can drastically suppress zot gene expression and shows promising inhibitory effect against V. cholerae zot production. Thus, routine intake of red chilli, which is easily available and inexpensive, may be an alternative approach to prevent and control symptoms of cholera.

  11. Central inhibitory effect of α-methyldopa on blood pressure, heart rate and body temperature of renal hypertensive rats

    NARCIS (Netherlands)

    Nijkamp, F.P.; Ezer, Joseph; Jong, Wybren de

    The central inhibitory effect of α-methyldopa on blood pressure, heart rate and body temperature was studied in conscious renal hypertensive rats. Systemic administration of α-methyldopa decreased mean arterial blood pressure and body temperature and caused a short lasting increase in heart rate

  12. Secretion of incretin hormones and the insulinotropic effect of gastric inhibitory polypeptide in women with a history of gestational diabetes

    DEFF Research Database (Denmark)

    Meier, J J; Gallwitz, B; Askenas, M

    2005-01-01

    AIMS/HYPOTHESIS: The insulinotropic effect of gastric inhibitory polypeptide (GIP) is reduced in patients with type 2 diabetes and around 50% of their first-degree relatives under hyperglycaemic conditions. It is unknown whether this is a result of a specific defect in GIP action or of a general ...

  13. Inhibitory effect of Raphanobrassica on Helicobacter pylori-induced gastritis in Mongolian gerbils.

    Science.gov (United States)

    Yamada, Takanori; Wei, Min; Toyoda, Takeshi; Yamano, Shoutaro; Wanibuchi, Hideki

    2014-08-01

    Helicobacter pylori (H. pylori) infection is well known to be associated with chronic gastritis and also development of gastric cancer. Raphanobrassica (RB) is an intergeneric hybrid of the genera Raphanus (radish) and Brassica (cabbages) containing appreciable amounts of glucoraphanin (GR) and glucoraphenin (GRe), which are actively hydrolyzed by the enzyme myrosinase to sulforaphane and sulforaphene, respectively. Both of these metabolites exert antimicrobial and anti-inflammatory activity. The purpose of the present study was to investigate the effect of two freeze-dried products of RB (RB1 and RB2) on H. pylori-induced gastritis in Mongolian gerbils. Six-week-old male Mongolian gerbils were inoculated orally with H. pylori (ATCC 43504), and 2weeks later were fed diets containing no additives or diets supplemented with 2% RB1 (containing both GR and GRe) or 2% RB2 (containing GR only) for 10weeks. In the RB1, but not the RB2 group, mononuclear cell infiltration, mRNA expression of IL-6, and cell proliferation in the gastric mucosa were significantly suppressed. These results indicate that RB1 containing both GR and GRe exerted significant inhibitory effects on H. pylori-induced gastritis in Mongolian gerbils apparently mediated via suppression of IL-6 expression and chronic inflammation. Copyright © 2014 Elsevier Ltd. All rights reserved.

  14. Composition Analysis and Inhibitory Effect of Sterculia lychnophora against Biofilm Formation by Streptococcus mutans

    Directory of Open Access Journals (Sweden)

    Yang Yang

    2016-01-01

    Full Text Available Pangdahai is a traditional Chinese drug, specifically described in the Chinese Pharmacopoeia as the seeds of Sterculia lychnophora Hance. Here, we separated S. lychnophora husk and kernel, analyzed the nutrient contents, and investigated the inhibitory effects of S. lychnophora ethanol extracts on cariogenic properties of Streptococcus mutans, important bacteria in dental caries and plaque formation. Ethanol extracts of S. lychnophora showed dose-dependent antibacterial activity against S. mutans with significant inhibition at concentrations higher than 0.01 mg/mL compared with the control group (p 0.03 mg/mL, while bacterial viability was decreased dose-dependently at high concentrations (0.04, 0.08, 0.16, and 0.32 mg/mL. Preliminary phytochemical analysis of the ethanol extract revealed a strong presence of alkaloid, phenolics, glycosides, and peptides while the presence of steroids, terpenoids, flavonoids, and organic acids was low. The S. lychnophora husk had higher moisture and ash content than the kernel, while the protein and fat content of the husk were lower (p<0.05 than those of the kernel. These results indicate that S. lychnophora may have antibacterial effects against S. mutans, which are likely related to the alkaloid, phenolics, glycosides, and peptides, the major components of S. lychnophora.

  15. Fish Oil and Adjuvant-Induced Arthritis: Inhibitory Effect on Leukocyte Recruitment.

    Science.gov (United States)

    Estevão-Silva, Camila Fernanda; Ames, Franciele Queiroz; Silva-Comar, Francielli Maria de Souza; Kummer, Raquel; Tronco, Rafael Prizon; Cuman, Roberto Kenji Nakamura; Bersani-Amado, Ciomar Aparecida

    2016-02-01

    Fish oil, a rich source of n-3 fatty acids, has been studied for its beneficial effects in many diseases. Recent studies have shown the robust anti-inflammatory activity of fish oil (FO), when administered orally to rats, in models of acute inflammation. Herein, we investigated if treatment with fish oil preparation (FOP) could interfere with the recruitment of leukocytes into the joint cavity of arthritic rats. We also evaluated the effect of treatment on rolling behavior and leukocyte adhesion in vivo and on leukocyte chemotaxis in vitro. Treatment with FOP (75, 150, and 300 mg/kg) initiated on the day of induction of arthritis (day 0) and maintained for 21 days reduced the total number of leukocytes recruited into the joint cavity, the number of rolling and adhered leukocytes in arthritic rats, and leukocyte migration in response to stimulation with N-formyl-methionyl-leucyl-phenylalanine (fMLP) and leukotriene B4 (LTB4). Together, our data provide evidence that FOP plays an important inhibitory role in the recruitment of leukocytes into the joint cavity of arthritic rats.

  16. Differential effects of lead and zinc on inhibitory avoidance learning in mice

    Directory of Open Access Journals (Sweden)

    F.S. de Oliveira

    2001-01-01

    Full Text Available We studied the effects of chronic intoxication with the heavy metals lead (Pb2+ and zinc (Zn2+ on memory formation in mice. Animals were intoxicated through drinking water during the pre- and postnatal periods and then tested in the step-through inhibitory avoidance memory task. Chronic postnatal intoxication with Pb2+ did not change the step-through latency values recorded during the 4 weeks of the test (ANOVA, P>0.05. In contrast, mice intoxicated during the prenatal period showed significantly reduced latency values when compared to the control group (day 1: q = 4.62, P<0.05; day 7: q = 4.42, P<0.05; day 14: q = 5.65, P<0.05; day 21: q = 3.96, P<0.05, and day 28: q = 6.09, P<0.05. Although chronic postnatal intoxication with Zn2+ did not alter a memory retention test performed 24 h after training, we noticed a gradual decrease in latency at subsequent 4-week intervals (F = 3.07, P<0.05, an effect that was not observed in the control or in the Pb2+-treated groups. These results suggest an impairment of memory formation by Pb2+ when the animals are exposed during the critical period of neurogenesis, while Zn2+ appears to facilitate learning extinction.

  17. Matrix metalloproteinases (MMPs) inhibitory effects of an octameric oligopeptide isolated from abalone Haliotis discus hannai.

    Science.gov (United States)

    Nguyen, Van-Tinh; Qian, Zhong-Ji; Ryu, Bomi; Kim, Kil-Nam; Kim, Daekyung; Kim, Young-Mog; Jeon, You-Jin; Park, Won Sun; Choi, Il-Whan; Kim, Geun Hyung; Je, Jae-Young; Jung, Won-Kyo

    2013-11-01

    Abalone (Haliotis discus hannai) is a marine gastropod, and an important fishery and food industrial resource that is massively maricultured in Asia, Africa, Australia and America. However, its health benefits have rarely been studied for nutraceutical and pharmaceutical application. In this study, the purified abalone oligopeptide (AOP) with anti-matrix metalloproteinases (anti-MMPs) effects was isolated from the digests of abalone intestine using recycle HPLC with a JAI W253 column and an OHpak SB-803 HQ column. The AOP was identified as Ala-Glu-Leu-Pro-Ser-Leu-Pro-Gly (MW=782.4 Da) with a de novo peptide sequencing technique using a tandem mass spectrometer. The AOP exhibited a specific inhibitory effect against MMP-2/-9 activity and attenuated protein expression of p50 and p65 in the human fibrosarcoma (HT1080) cells, dose-dependently. The results presented illustrate that the AOP could inhibit MMP-2/-9 expression in HT1080 cells via the nuclear factor-kappaB (NF-κB)-mediated pathway. This data suggest that the AOP from H. discus hannai intestine may possess therapeutic and preventive potential for the treatment of MMPs-related disorders such as angiogenesis and cardiovascular diseases. Copyright © 2013 Elsevier Ltd. All rights reserved.

  18. Effects of prenatal substance exposure on neurocognitive correlates of inhibitory control success and failure.

    Science.gov (United States)

    Roos, Leslie E; Beauchamp, Kathryn G; Pears, Katherine C; Fisher, Philip A; Berkman, Elliot T; Capaldi, Deborah

    2017-01-01

    Adolescents with prenatal substance (drug and alcohol) exposure exhibit inhibitory control (IC) deficits and aberrations in associated neural function. Nearly all research to date examines exposure to individual substances, and a minimal amount is known about the effects of heterogeneous exposure-which is more representative of population exposure levels. Using functional magnetic resonance imaging (fMRI), we investigated IC (Go/NoGo) in heterogeneously exposed (n = 7) vs. control (n = 7) at-risk adolescents (ages 13-17). The fMRI results indicated multiple IC processing differences consistent with a more immature developmental profile for exposed adolescents (Exposed  >  Nonexposed: NoGo > Go: right ventrolateral prefrontal cortex, right cuneus, and left inferior parietal lobe; NoGo > false alarm: occipital lobe; Go > false alarm: right anterior prefrontal cortex). Simple effects suggest exposed adolescents exhibited exaggerated correct trial but decreased incorrect trial activation. Results provide initial evidence that prenatal exposure across substances creates similar patterns of atypical brain activation to IC success and failure.

  19. Effects of aversive odour presentation on inhibitory control in the Stroop colour-word interference task.

    Science.gov (United States)

    Finkelmeyer, Andreas; Kellermann, Thilo; Bude, Daniela; Niessen, Thomas; Schwenzer, Michael; Mathiak, Klaus; Reske, Martina

    2010-10-18

    Due to the unique neural projections of the olfactory system, odours have the ability to directly influence affective processes. Furthermore, it has been shown that emotional states can influence various non-emotional cognitive tasks, such as memory and planning. However, the link between emotional and cognitive processes is still not fully understood. The present study used the olfactory pathway to induce a negative emotional state in humans to investigate its effect on inhibitory control performance in a standard, single-trial manual Stroop colour-word interference task. An unpleasant (H2S) and an emotionally neutral (Eugenol) odorant were presented in two separate experimental runs, both in blocks alternating with ambient air, to 25 healthy volunteers, while they performed the cognitive task. Presentation of the unpleasant odorant reduced Stroop interference by reducing the reaction times for incongruent stimuli, while the presentation of the neutral odorant had no effect on task performance. The odour-induced negative emotional state appears to facilitate cognitive processing in the task used in the present study, possibly by increasing the amount of cognitive control that is being exerted. This stands in contrast to other findings that showed impaired cognitive performance under odour-induced negative emotional states, but is consistent with models of mood-congruent processing.

  20. Inhibitory Effects of Probiotic Lactobacillus on the Growth of Human Colonic Carcinoma Cell Line HT-29.

    Science.gov (United States)

    Chen, Zhung-Yuan; Hsieh, You-Miin; Huang, Chun-Chih; Tsai, Cheng-Chih

    2017-01-10

    This study was conducted to investigate the inhibitory effect of Lactobacillus cells and supernatants on the growth of the human colon cancer cell line HT-29. Our study results indicated that the PM153 strain exhibits the best adhesion ability and the highest survival in the gastrointestinal tract simulation experiment. Furthermore, after an 8-h co-culture of PM153 and HT-29 cells, the PM153 strain can induce the secretion of nitric oxide from the HT-29 cells. In addition, after the co-culture of the BCRC17010 strain (10⁸ cfu/mL) and HT-29 cells, the Bax/Bcl-2 ratio in the HT-29 cells was 1.19, which showed a significant difference from the other control and LAB groups ( p strain exerts a pro-apoptotic effect on the HT-29 cells. Upon co-culture with HT-29 cells for 4, 8 and 12 h, the BCRC14625 strain (10⁸ cfu/mL) demonstrated a significant increase in lactate dehydrogenase (LDH) activity ( p strains have ability to inhibit the growth of the colorectal cancer cell line HT-29 Bax/Bcl-2 pathway or NO production. In summary, we demonstrated that the BCRC17010 strain, good abilities of adhesion and increased LDH release, was the best probiotic potential for inhibition of HT-29 growth amongst the seven LAB strains tested in vitro.

  1. Effects of aversive odour presentation on inhibitory control in the Stroop colour-word interference task

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    Nießen Thomas

    2010-10-01

    Full Text Available Abstract Background Due to the unique neural projections of the olfactory system, odours have the ability to directly influence affective processes. Furthermore, it has been shown that emotional states can influence various non-emotional cognitive tasks, such as memory and planning. However, the link between emotional and cognitive processes is still not fully understood. The present study used the olfactory pathway to induce a negative emotional state in humans to investigate its effect on inhibitory control performance in a standard, single-trial manual Stroop colour-word interference task. An unpleasant (H2S and an emotionally neutral (Eugenol odorant were presented in two separate experimental runs, both in blocks alternating with ambient air, to 25 healthy volunteers, while they performed the cognitive task. Results Presentation of the unpleasant odorant reduced Stroop interference by reducing the reaction times for incongruent stimuli, while the presentation of the neutral odorant had no effect on task performance. Conclusions The odour-induced negative emotional state appears to facilitate cognitive processing in the task used in the present study, possibly by increasing the amount of cognitive control that is being exerted. This stands in contrast to other findings that showed impaired cognitive performance under odour-induced negative emotional states, but is consistent with models of mood-congruent processing.

  2. Inhibitory effects of Iranian Thymus vulgaris extracts on in vitro growth of Entamoeba histolytica.

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    Behnia, Maryam; Haghighi, Ali; Komeylizadeh, Hossein; Tabaei, Seyyed-Javadi Seyyed; Abadi, Alireza

    2008-09-01

    One of the most common drugs used against a wide variety of anaerobic protozoan parasites is metronidazole. However, this drug is mutagenic for bacteria and is a potent carcinogen for rodents. Thymus vulgaris is used for cough suppression and relief of dyspepsia. Also it has antibacterial and antifungal properties. The aim of this study was to investigate antiamebic effect of Thymus vulgaris against Entamoeba histolytica in comparison with metronidazole. One hundred gram air-dried T. vulgaris plant was obtained and macerated at 25 degrees C for 14 days using n-hexane and a mixture of ethanol and water. For essential oil isolation T. vulgaris was subjected to hydrodistillation using a clevenger-type apparatus for 3 hr. E. histolytica, HM-1: IMSS strain was used in all experiments. It was found that the minimal inhibitory concentration (MIC) for T. vulgaris hydroalcoholic, hexanic extracts, and the essential oil after 24 hr was 4 mg/mL, 4 mg/mL, and 0.7 mg/mL, respectively. After 48 hr the MIC for T. vulgaris hydroalcoholic and hexanic extracts was 3 and 3 mg/mL, respectively. Therefore, it can be concluded that the Iranian T. vulgaris is effective against the trophozoites of E. histolytica.

  3. Inhibitory effect of combination of cetuximab and irradiation on colorectal carcinoma CL187 cells

    International Nuclear Information System (INIS)

    Wang Hao; Wang Junjie; Qu Ang; Liu Jingjia; Li Jin'na

    2012-01-01

    Objective: To investigate the combination effect of cetuximab and irradiation on colorectal carcinoma CL187 cell line and underlying molecular mechanism. Methods: CL187 cells with or without cetuximab treatment were irradiated by 0, 4 and 8 Gy X-rays, then cell death percentage was determined by MTT 24 and 48 h post-irradiation. Clone forming assay was used to evaluate the cell reproliferation ability. Cell cycle distribution, apoptosis, and necrosis were analyzed by flow cytometry. Western blot was used to detect the protein expressions of DNA-PKcs, Ku70 and Ku80. Results: The cetuximab enhanced the percentage of radiation-induced cell death, while decreased the cloning formation capacity and increased radiosensitivity (t=-6.14, -6.53, P<0.05). The SER of cetuximab on CL187 cell line approached to 1.38. In addition, cetuximab also increased radiation-induced G 0 /G 1 phase arrest (t=-4.64, P<0.05) and the percentage of apoptosis and necrosis (t=-9.16, P<0.05), but it decreased the expression levels of DNA-PKcs, Ku70 and Ku80 proteins. Conclusions: The cetuximab treatment might enhance the inhibitory effect of irradiation on colorectal carcinoma CL187 cell line by influencing cell cycle distribution, cell apoptosis, and the expression of DNA repair proteins. (authors)

  4. Inhibitory effects of silver nanoparticles against adenovirus type 3 in vitro.

    Science.gov (United States)

    Chen, Nana; Zheng, Yang; Yin, Jianjian; Li, Xiujing; Zheng, Conglong

    2013-11-01

    Adenoviruses are associated with respiratory, ocular, or gastrointestinal disease. With various species and high morbidity, adenoviruses are increasingly recognized as significant viral pathogen among pediatric and immunocompromised patients. However, there is almost no specific drug for treatment. Silver nanoparticles are demonstrated to be virucidal against influenza A (H1N1) virus, human immunodeficiency virus and Hepatitis B virus. Currently, there is no data regarding whether the silver nanoparticles inhibit the adenovirus or not. The aim of this study is to investigate the effect of silver nanoparticles on adenovirus type 3 (Ad3). The results revealed that HeLa cells infected with silver nanoparticles treated Ad3 did not show obvious CPE. The viability of HeLa cells infected with silver nanoparticles treated Ad3 was significantly higher than that of cells infected with untreated Ad3. There was a significant difference of fluorescence intensity between the cells infected with silver nanoparticles treated and untreated Ad3. The transmission electron microscopy (TEM) showed that silver nanoparticles could directly damage the structure of Ad3 particle. The PCR amplification products of DNA isolated from silver nanoparticles treated Ad3 was decreased in a dose-dependent manner. The decreased DNA loads were also confirmed by real-time PCR experiment. The present study indicates silver nanoparticles exhibit remarkably inhibitory effects on Ad3 in vitro, which suggests silver nanoparticles could be a potential antiviral agent for inhibiting Ad3 infection. Copyright © 2013 Elsevier B.V. All rights reserved.

  5. Increased sink strength offsets the inhibitory effect of sucrose on sugarcane photosynthesis.

    Science.gov (United States)

    Ribeiro, Rafael V; Machado, Eduardo C; Magalhães Filho, José R; Lobo, Ana Karla M; Martins, Márcio O; Silveira, Joaquim A G; Yin, Xinyou; Struik, Paul C

    2017-01-01

    Spraying sucrose inhibits photosynthesis by impairing Rubisco activity and stomatal conductance (g s ), whereas increasing sink demand by partially darkening the plant stimulates sugarcane photosynthesis. We hypothesized that the stimulatory effect of darkness can offset the inhibitory effect of exogenous sucrose on photosynthesis. Source-sink relationship was perturbed in two sugarcane cultivars by imposing partial darkness, spraying a sucrose solution (50mM) and their combination. Five days after the onset of the treatments, the maximum Rubisco carboxylation rate (V cmax ) and the initial slope of A-C i curve (k) were estimated by measuring leaf gas exchange and chlorophyll fluorescence. Photosynthesis was inhibited by sucrose spraying in both genotypes, through decreases in V cmax , k, g s and ATP production driven by electron transport (J atp ). Photosynthesis of plants subjected to the combination of partial darkness and sucrose spraying was similar to photosynthesis of reference plants for both genotypes. Significant increases in V cmax , g s and J atp and marginal increases in k were noticed when combining partial darkness and sucrose spraying compared with sucrose spraying alone. Our data also revealed that increases in sink strength due to partial darkness offset the inhibition of sugarcane photosynthesis caused by sucrose spraying, enhancing the knowledge on endogenous regulation of sugarcane photosynthesis through the source-sink relationship. Copyright © 2016 Elsevier GmbH. All rights reserved.

  6. Binding and Inhibitory Effect of the Dyes Amaranth and Tartrazine on Amyloid Fibrillation in Lysozyme.

    Science.gov (United States)

    Basu, Anirban; Suresh Kumar, Gopinatha

    2017-02-16

    Interaction of two food colorant dyes, amaranth and tartrazine, with lysozyme was studied employing multiple biophysical techniques. The dyes exhibited hypochromic changes in the presence of lysozyme. The intrinsic fluorescence of lysozyme was quenched by both dyes; amaranth was a more efficient quencher than tartrazine. The equilibrium constant of amaranth was higher than that of tartarzine. From FRET analysis, the binding distances for amaranth and tartrazine were calculated to be 4.51 and 3.93 nm, respectively. The binding was found to be dominated by non-polyelectrolytic forces. Both dyes induced alterations in the microenvironment surrounding the tryptophan and tyrosine residues of the protein, with the alterations being comparatively higher for the tryptophans than the tyrosines. The interaction caused significant loss in the helicity of lysozyme, the change being higher with amaranth. The binding of both dyes was exothermic. The binding of amaranth was enthalpy driven, while that of tartrazine was predominantly entropy driven. Amaranth delayed lysozyme fibrillation at 25 μM, while tartrazine had no effect even at 100 μM. Nevertheless, both dyes had a significant inhibitory effect on fibrillogenesis. The present study explores the potential antiamyloidogenic property of these azo dyes used as food colorants.

  7. The effects of stereotype threat and contextual cues on alcohol users' inhibitory control.

    Science.gov (United States)

    Pennington, Charlotte R; Qureshi, Adam; Monk, Rebecca L; Heim, Derek

    2016-03-01

    Previous research indicates that users of illicit substances exhibit diminished cognitive function under stereotype threat. Advancing this research, the current study aimed to examine the effects of stereotype threat on alcohol users' inhibitory control. It also examined whether drinkers demonstrate a greater approach bias towards alcohol-related relative to neutral stimuli. Fifty-five participants were assigned randomly to a stereotype threat condition, in which they were primed with a negative stereotype linking drinking behavior to cognitive decline, or a non-threat control condition. All participants then completed a modified version of the Cued Go/No-Go Association Test that exposed participants to alcohol-related and neutral pictorial stimuli and sound cues. Stereotype threatened participants demonstrated a speed-accuracy trade off, taking significantly longer to respond to go-trials with equivalent accuracy to the control condition. They also showed reduced response accuracy to both alcohol-related and neutral stimuli in reversed instruction trials. Participants in the control condition were both more accurate and quicker to respond to alcohol-related stimuli compared to neutral stimuli. These results suggest that awareness of negative stereotypes pertaining to alcohol-related impulsivity may have a harmful effect on inhibitive cognitive performance. This may have implications for public health campaigns and for methodological designs with high levels of procedural signaling with respect to not inadvertently inducing stereotype threat and impacting impulsivity. Copyright © 2015 Elsevier Ltd. All rights reserved.

  8. Direct inhibitory effects of pioglitazone on hepatic fetuin-A expression.

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    Akinobu Ochi

    Full Text Available Fetuin-A, a circulating glycoprotein synthesized in the liver, is involved in insulin resistance and type 2 diabetes. However, regulation of fetuin-A synthesis has remained obscure. We previously reported that pioglitazone treatment significantly reduced serum fetuin-A levels in patients with type 2 diabetes. To clarify whether pioglitazone can directory inhibit hepatic fetuin-A synthesis, we investigated the effects of pioglitazone on fetuin-A expression both in vitro and in vivo. Pioglitazone treatment suppressed mRNA and protein expression of fetuin-A in Fao hepatoma cells. Interestingly, rosiglitazone but not metformin, also inhibited fetuin-A expression. In addition, GW 9662, an inhibitor of peroxisome proliferator-activated receptor (PPAR γ, reversed pioglitazone-induced suppression of fetuin-A, suggesting that thiazolidinedione derivatives may have common characteristics with regard to fetuin-A suppression, possibly through PPARγactivation. Finally, oral administration of pioglitazone to mice for 8 weeks resulted in suppression of hepatic fetuin-A mRNA. These findings suggest that pioglitazone may partially ameliorate insulin resistance through its direct inhibitory effects on fetuin-A expression in the liver.

  9. Inhibitory Effect of Heracleum persicum and Ziziphus jujuba on Activity of Alpha-Amylase

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    Reza Afrisham

    2015-01-01

    Full Text Available Postprandial hyperglycemia plays an important role in the development of type 2 diabetes. Inhibition of alpha-amylase was led to a delay in breaks down of starch and glycogen and prevented a rapid rise in blood sugar. Alpha-amylase was isolated by gel filtration chromatography Sephadex G-75 from bovine pancreas. Then, total methanolic extracts of plants were prepared and IC50 values of extracts on alpha-amylase were obtained and compared with acarbose IC50. The polyphenolic content of extracts and antioxidant capacity were determined by Folin-Ciocalteu test and DPPH test, respectively. The specific activity of alpha-amylase was 48.2 U/mg. For inhibition of alpha-amylase, IC50 values of H. persicum, Z. jujuba, and acarbose were 307, 827, and 113 μg/ml, respectively. For inhibition of DPPH radical, IC50 values of extracts were 235 and 701 μg/ml. Total phenolic contents of methanol extracts were 73.8±3.2 and 44.2±1.8 μg tannic acid equivalent/mg extract. Acarbose causes gastrointestinal symptoms and liver toxicity, but H. persicum and Z. jujuba decrease these side effects and prevent gastrointestinal disorders. Due to the high polyphenolic content and antioxidant capacity of these plants and significant inhibitory effect of the plants on alpha-amylase, these plants can be proposed for treatment of diabetic patients.

  10. Tricyclic coumarin sulphonate derivatives with alkaline phosphatase inhibitory effects: in vitro and docking studies.

    Science.gov (United States)

    Iqbal, Jamshed; El-Gamal, Mohammed I; Ejaz, Syeda Abida; Lecka, Joanna; Sévigny, Jean; Oh, Chang-Hyun

    2018-12-01

    Tissue-nonspecific alkaline phosphatase (TNAP) is an important isozyme of alkaline phosphatases, which plays different pivotal roles within the human body. Most importantly, it is responsible for maintaining the balanced ratio of phosphate and inorganic pyrophosphate, thus regulates the extracellular matrix calcification during bone formation and growth. The elevated level of TNAP has been linked to vascular calcification and end-stage renal diseases. Consequently, there is a need to search for highly potent and selective inhibitors of alkaline phosphatases (APs) for treatment of disorders associated with the over-expression of APs. Herein, a series of tricyclic coumarin sulphonate 1a-za with known antiproliferative activity, was evaluated for AP inhibition against human tissue nonspecific alkaline phosphatase (h-TNAP) and human intestinal alkaline phosphatase (h-IAP). The methylbenzenesulphonate derivative 1f (IC 50  = 0.38 ± 0.01 μM) was found to be the most active h-TNAP inhibitor. Another 4-fluorobenzenesulphonate derivative 1i (IC 50  = 0.45 ± 0.02 μM) was found as the strongest inhibitor of h-IAP. Some of the derivatives were also identified as highly selective inhibitors of APs. Detailed structure-activity relationship (SAR) was investigated to identify the functional groups responsible for the effective inhibition of AP isozymes. The study was also supported by the docking studies to rationalise the most possible binding site interactions of the identified inhibitors with the targeted enzymes.

  11. Inhibitory and inductive effects of Phikud Navakot extract on human cytochrome P450.

    Science.gov (United States)

    Chiangsom, Abhiruj; Lawanprasert, Somsong; Oda, Shingo; Kulthong, Kornphimol; Luechapudiporn, Rataya; Yokoi, Tsuyoshi; Maniratanachote, Rawiwan

    2016-06-01

    Effects of the hydroethanolic extract of Phikud Navakot (PN), a Thai traditional remedy, on human cytochrome P450s (CYPs) were investigated in vitro. Selective substrates of CYPs were used to investigate the effects and kinetics of PN on CYP inhibition using human liver microsomes. Primary human hepatocytes were used to assess the inductive effects of PN on CYP enzyme activities and protein expressions. The results showed that PN inhibited the activities of CYP1A2, CYP2C9, CYP2D6, and CYP3A4 with half maximal inhibitory concentration (IC50) values of 13, 62, 67, and 88 μg/mL, respectively. Meanwhile, it had no effect on the activities of CYP2C19 and CYP2E1 (IC50 > 1 mg/mL). PN exhibited competitive inhibition of CYP1A2 (Ki = 34 μg/mL), mixed type inhibition of CYP2C9 and CYP2D6 (Ki = 80 and 12 μg/mL, respectively), and uncompetitive inhibition of CYP3A4 (Ki = 150 μg/mL). PN did not have an inductive effect on CYP1A2, CYP2C9, CYP2C19 and CYP3A4 in primary human hepatocytes, which is an advantageous characteristic of the extract. However the extract may cause herb-drug interactions via inhibition of CYP1A2, CYP2C9, CYP2D6 and CYP3A4, and precautions should be taken when PN is coadministered with drugs that are metabolized by these CYP enzymes. Copyright © 2016 The Japanese Society for the Study of Xenobiotics. Published by Elsevier Ltd. All rights reserved.

  12. The effect of STDP temporal kernel structure on the learning dynamics of single excitatory and inhibitory synapses.

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    Yotam Luz

    Full Text Available Spike-Timing Dependent Plasticity (STDP is characterized by a wide range of temporal kernels. However, much of the theoretical work has focused on a specific kernel - the "temporally asymmetric Hebbian" learning rules. Previous studies linked excitatory STDP to positive feedback that can account for the emergence of response selectivity. Inhibitory plasticity was associated with negative feedback that can balance the excitatory and inhibitory inputs. Here we study the possible computational role of the temporal structure of the STDP. We represent the STDP as a superposition of two processes: potentiation and depression. This allows us to model a wide range of experimentally observed STDP kernels, from Hebbian to anti-Hebbian, by varying a single parameter. We investigate STDP dynamics of a single excitatory or inhibitory synapse in purely feed-forward architecture. We derive a mean-field-Fokker-Planck dynamics for the synaptic weight and analyze the effect of STDP structure on the fixed points of the mean field dynamics. We find a phase transition along the Hebbian to anti-Hebbian parameter from a phase that is characterized by a unimodal distribution of the synaptic weight, in which the STDP dynamics is governed by negative feedback, to a phase with positive feedback characterized by a bimodal distribution. The critical point of this transition depends on general properties of the STDP dynamics and not on the fine details. Namely, the dynamics is affected by the pre-post correlations only via a single number that quantifies its overlap with the STDP kernel. We find that by manipulating the STDP temporal kernel, negative feedback can be induced in excitatory synapses and positive feedback in inhibitory. Moreover, there is an exact symmetry between inhibitory and excitatory plasticity, i.e., for every STDP rule of inhibitory synapse there exists an STDP rule for excitatory synapse, such that their dynamics is identical.

  13. Inhibitory effects of flavonoids extracted from Nepalese propolis on the LPS signaling pathway.

    Science.gov (United States)

    Funakoshi-Tago, Megumi; Ohsawa, Kentaro; Ishikawa, Toshiyuki; Nakamura, Fumika; Ueda, Fumihito; Narukawa, Yuji; Kiuchi, Fumiyuki; Tamura, Hiroomi; Tago, Kenji; Kasahara, Tadashi

    2016-11-01

    Flavonoids, particularly those derived from plants, harbor biological effects such as anti-inflammation and the inhibition of cancer progression. In the present study, we investigated the effects of 10 kinds of flavonoids isolated from Nepalese propolis on the LPS signaling pathway in order to clarify their anti-inflammatory activities. Five types of flavonoids: isoliquiritigenin, chrysin, 3',4'-dihydroxy-4-methoxydalbergione, 4-methoxydalbergion, and cearoin, markedly inhibited inflammatory responses including LPS-induced NO production by suppressing the expression of iNOS mRNA and LPS-induced mRNA expression of TNFα and CCL2. Their inhibitory effects on LPS-induced inflammatory responses correlated with the intensities of these flavonoids to suppress the LPS-induced activation of nuclear factor κB (NF-κB), an essential transcription factor for the mRNA expression of iNOS, TNFα, and CCL2. Among these flavonoids, 3',4'-dihydroxy-4-methoxydalbergione and 4-methoxydalbergion markedly inhibited the LPS-induced activation of IKK, thereby abrogating the degradation of IκBα and nuclear localization of NF-κB. On the other hand, isoliquiritigenin, chrysin, and cearoin failed to inhibit these signaling steps, but suppressed the transcriptional activity of NF-κB, which caused their anti-inflammatory effects. The results of the present study revealed that these five kinds of flavonoids are the components of Nepalese propolis that exhibit anti-inflammatory activities with a different regulatory mechanism for the activation of NF-κB. Copyright © 2016 Elsevier B.V. All rights reserved.

  14. Inhibitory effect on Streptococcus mutans and mechanical properties of the chitosan containing composite resin

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    Ji-Sun Kim

    2013-02-01

    Full Text Available Objectives This study evaluated the antibacterial effect and mechanical properties of composite resins (LCR, MCR, HCR incorporating chitosan with three different molecular weights (L, Low; M, Medium; H, High. Materials and Methods Streptococcus (S. mutans 100 mL and each chitosan powder were inoculated in sterilized 10 mL Brain-Heart Infusion (BHI solution, and was centrifuged for 12 hr. Absorbance of the supernatent was measured at OD660 to estimate the antibacterial activities of chitosan. After S. mutans was inoculated in the disc shaped chitosan-containing composite resins, the disc was cleansed with BHI and diluted with serial dilution method. S. mutans was spread on Mitis-salivarius bacitracin agar. After then, colony forming unit (CFU was measured to verify the inhibitory effect on S. mutans biofilm. To ascertain the effect on the mechanical properties of composite resin, 3-point bending and Vickers hardness tests were done after 1 and 3 wk water storage, respectively. Using 2-way analysis of variance (ANOVA and Scheffe test, statistical analysis was done with 95% significance level. Results All chitosan powder showed inhibition effect against S. mutans. CFU number in chitosan-containing composite resins was smaller than that of control resin without chitosan. The chitosan containing composite resins did not show any significant difference in flexural strength and Vickers hardness in comparison with the control resin. However, the composite resin, MCR showed a slightly decreased flexural strength and the maximum load than those of control and the other composite resins HCR and LCR. Conclusions LCR and HCR would be recommended as a feasible antibacterial restorative due to its antibacterial nature and mechanical properties.

  15. The Inhibitory Effects of Low-Dose Ionizing Radiation in IgE-Mediated Allergic Responses.

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    Hae Mi Joo

    Full Text Available Ionizing radiation has different biological effects according to dose and dose rate. In particular, the biological effect of low-dose radiation is unclear. Low-dose whole-body gamma irradiation activates immune responses in several ways. However, the effects and mechanism of low-dose radiation on allergic responses remain poorly understood. Previously, we reported that low-dose ionizing radiation inhibits mediator release in IgE-mediated RBL-2H3 mast cell activation. In this study, to have any physiological relevance, we investigated whether low-dose radiation inhibits allergic responses in activated human mast cells (HMC-1(5C6 and LAD2 cells, mouse models of passive cutaneous anaphylaxis and the late-phase cutaneous response. High-dose radiation induced cell death, but low-dose ionizing radiation of <0.5 Gy did not induce mast cell death. Low-dose ionizing radiation that did not induce cell death significantly suppressed mediator release from human mast cells (HMC-1(5C6 and LAD2 cells that were activated by antigen-antibody reaction. To determine the inhibitory mechanism of mediator released by low-dose ionizing radiation, we examined the phosphorylation of intracellular signaling molecules such as Lyn, Syk, phospholipase Cγ, and protein kinase C, as well as the intracellular free Ca2+ concentration ([Ca2+]i. The phosphorylation of signaling molecules and [Ca2+]i following stimulation of FcεRI receptors was inhibited by low dose ionizing radiation. In agreement with its in vitro effect, ionizing radiation also significantly inhibited inflammatory cells infiltration, cytokine mRNA expression (TNF-α, IL-4, IL-13, and symptoms of passive cutaneous anaphylaxis reaction and the late-phase cutaneous response in anti-dinitrophenyl IgE-sensitized mice. These results indicate that ionizing radiation inhibits both mast cell-mediated immediate- and delayed-type allergic reactions in vivo and in vitro.

  16. Inhibitory Effect of Alpha-Mangostin on Adhesion of Candida albicans to Denture Acrylic.

    Science.gov (United States)

    Kaomongkolgit, Ruchadaporn; Jamdee, Kusuma

    2015-01-01

    Candida-associated denture stomatitis is a very common disease affecting denture wearers. It is characterized by the presence of yeast biofilm on the denture, primarily associated with C. albicans. The investigation of agents that can reduce C. albicans adhesion may represent a significant advancement in the prevention and treatment of this disease. This study aims to investigate the effect of alpha-mangostin on the in vitro adhesion of C. albicans to denture acrylic and germ tube formation by C. albicans and to compare its activity with clotrimazole which is a topical antifungal agent commonly used for the treatment of Candida-associated denture stomatitis. Alpha-mangostin was extracted by thin layer chromatography. The effect of alpha-mangostin on adhesion of C. albicans to denture acrylic was determined by using a colorimetric tetrazolium assay and germ tube formation by C. albicans was determined by using the counting chamber. A significant reduction of C. albicans adhesion to denture acrylic was evident after exposure to 2,000 µg/ml of alpha-mangostin for only 15 min. In addition, the 2,000 µg/ml of the alpha-mangostin-treated C. albicans had a reduced ability for germ tube formation. These inhibitory effects of alpha-mangostin were as effective as clotrimazole. Alpha-mangostin has antifungal property against C. albicans by inhibiting the adhesion to denture acrylic and germ tube formation in vitro. These results suggest the potential application of alpha-mangostin as a topical medication or a natural oral hygiene product for treatment of Candida-associated denture stomatitis.

  17. Inhibitory Effects of Several Essential Oils towards Salmonella typhimurium, Salmonella paratyphi A and Salmonella paratyphi B

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    S.F. Mazhar

    2014-09-01

    Full Text Available Plant essential oils are natural products extracted from plants and because of their antimicrobial properties can be used as natural additives in foods. They are also useful for decontamination of food-borne pathogens and can be a safe additive in foods. The antimicrobial activities of essential oils belonging to Saturiea hortensis, Thymus vulgaris, Mentha polegium, Cuminum cyminum, Lavandula officinalis and Mentha viridis L. (spearmint were investigated at different concentrations (0.1, 0.3, 0.5, 1, 2, 5 and 10%v/v against Salmonella typhimurium, Salmonella paratyphi A and Salmonella paratyphi B by using the agar well diffusion method. Essential oils showed inhibitory effect on Salmonella spp. in the agar well diffusion assay. In addition, the capability of essential oils for decontamination of minced row beef, ground beef, minced raw chicken and minced raw fish inoculated with Salmonella spp. at 0.1 and 0.5%v/v were assessed. Reduction of the Salmonella spp. population was observed following the inoculation of the cultures with 0.1 and 0.5%v/v essential oils.

  18. Inhibitory effect of novel pyrimidines on ATP and ADP hydrolysis in synaptosomes from rat cerebral cortex.

    Science.gov (United States)

    Cechin, Sirlene R; Schetinger, Maria Rosa C; Zanatta, Nilo; Madruga, Claudia C; Pacholski, Iraci L; Flores, Darlene C; Bonacorso, Helio G; Martins, Marcos A P; Morsch, Vera M

    2003-11-01

    In this study, a new series of trihalomethyl-substituted pyrimidines and dihydropyrimidines were synthesized and tested as potential NTPDase inhibitors. For this purpose, synaptosomes from rat cerebral cortex were used as the enzyme source and ATP and ADP were used as the substrate. Among the new compounds, 4-methyl-2-methylsulfanyl-6-trichloromethylpyrimidine (2b) was found to be the most effective noncompetitive inhibitor, with an estimated K(i) value of 0.18 and 0.55 mM for ATP and ADP, respectively. Other pyrimidines inhibited NTPDase activity with the following rank order of inhibitory potency: 3,6-dimethyl-2-methylsulfanyl-4-trifluoromethyl-3,4-dihydro-pyrimidin-4-ol (3a) > 5-methyl-2-(4-methyl-6-trifluoromethyl-pyrimidin-2-yl)-3-trifluoromethyl-3,4-dihydro-2H-3-pyrazol-3-ol (6a) > 5-bromo-4,6-dimethoxy-4-trichloromethyl-1,2,3,4-tetrahydro-2-pyrimidin-2-one (9) for ATP and 6a > 9 > 3a for ADP. Our results demonstrate that a novel group of pyrimidines compounds can act as inhibitors of ATP and ADP hydrolysis in synaptosomes from rat cerebral cortex. These results can contribute for the understanding of the NTPDase activity and for further studies involving new compounds that can enlist as it inhibitors.

  19. Inhibitory effects of Lactobacillus rhamnosus and Lactobacillus casei on Candida biofilm of denture surface.

    Science.gov (United States)

    Song, Young-Gyun; Lee, Sung-Hoon

    2017-04-01

    Candida albicans biofilm is associated with denture-related stomatitis and oral candidiasis of elderly. Probiotics are beneficial bacteria and have antibacterial activity against pathogenic bacteria. The purpose of this study was to investigate the antifungal activity of various probiotics against C. albicans and the inhibitory effects of probiotics on Candida biofilm on the denture surface. The spent culture media of various probiotics were investigated the antifungal efficacy against C. albicans. Candida biofilm was formed on a denture base resin and was then treated with Lactobacillus rhamnosus and Lactobacillus casei. Also, the biofilms of L. rhamnosus and L. casei were formed and were sequentially treated with C. albicans. Colony-forming units of C. albicans on the denture surface were counted after spreading on agar plate. The denture base resin was treated with the spent culture media for 30days, after which the denture surface roughness was analyzed with an atomic force microscope. L. rhamnosus and L. casei exhibited stronger antifungal activity than other probiotics. The spent culture medium of L. rhamnosus and L. casei exhibited the antifungal activity against blastoconidia and biofilm of C. albicans. L. rhamnosus and L. casei showed the antifungal activity against Candida biofilm, and the biofilm of L. rhamnosus and L. casei inhibited formation of Candida biofilm on denture surface. Neither of the probiotics affected the surface roughness of the denture base resin. L. rhamnosus and L. casei may be the ideal probiotics for the prevention and treatment of denture-related stomatitis. Copyright © 2017 Elsevier Ltd. All rights reserved.

  20. [Inhibitory effect of kaempferol on inflammatory response of lipopolysaccharide-stimulated human mast cells].

    Science.gov (United States)

    Zhou, Yun-jiang; Wang, Hu; Li, Li; Sui, He-huan; Huang, Jia-jun

    2015-06-01

    This study is to investigate the inhibitory effect of kaempferol on inflammatory response of lipopolysaccharide(LPS)-stimulated HMC-1 mast cells. The cytotoxicity of kaempferol to HMC-1 mast cells were analyzed by using MTT assay and then the administration concentrations of kaempferol were established. Histamine, IL-6, IL-8, IL-1β and TNF-α were measured using ELISA assay in activated HMC-1 mast cells after incubation with various concentrations of kaempferol (10, 20 and 40 µmol.L-1). Western blot was used to test the protein expression of p-IKKβ, IκBα, p-IκBα and nucleus NF-κB of LPS-induced HMC-1 mast cells after incubation with different concentrations of kaempferol. The optimal concentrations of kaempferol were defined as the range from 5 µmol.L-1 to 40 µmol.L-1. Kaempferol significantly decreased the release of histamine, IL-6, IL-8, IL-1β and TNF-α of activated HMC-1 mast cells (Pkaempferol, the protein expression of p-IKKβ, p-IKBa and nucleus NF-κB (p65) markedly reduced in LPS-stimulated HMC-1 mast cells (Pkaempferol markedly inhibit mast cell-mediated inflammatory response. At the same time, kaempferol can inhibit the activation of IKKβ, block the phosphorylation of IκBα, prevent NF-KB entering into the nucleus, and then decrease the release of inflammatory mediators.

  1. Inhibitory effects of furan derivatives and phenolic compounds on dark hydrogen fermentation.

    Science.gov (United States)

    Lin, Richen; Cheng, Jun; Ding, Lingkan; Song, Wenlu; Zhou, Junhu; Cen, Kefa

    2015-11-01

    The inhibitory effects of furan derivatives [i.e. furfural and 5-hydroxymethylfurfural (5-HMF)] and phenolic compounds (i.e. vanillin and syringaldehyde) on dark hydrogen fermentation from glucose were comparatively evaluated. Phenolic compounds exhibited stronger inhibition on hydrogen production and glucose consumption than furan derivatives under the same 15mM concentration. Furan derivatives were completely degraded after 72h fermentation, while over 55% of phenolic compounds remained unconverted after 108h fermentation. The inhibition coefficients of vanillin (14.05) and syringaldehyde (11.21) were higher than those of 5-HMF (4.35) and furfural (0.64). Vanillin exhibited the maximum decrease of hydrogen yield (17%). The consumed reducing power by inhibitors reduction from R-CHO to RCH2OH was a possible reason contributed to the decreased hydrogen yield. Vanillin exhibited the maximum delay of peak times of hydrogen production rate and glucose consumption. Soluble metabolites and carbon conversion efficiency decreased with inhibitors addition, which were consistent with hydrogen production. Copyright © 2015 Elsevier Ltd. All rights reserved.

  2. [Estimates of the size of inhibitory areas in crowding effects in periphery].

    Science.gov (United States)

    Bondarko, V M; Danilova, M V; Solnushkin, S D; Chikhman, V N

    2014-01-01

    In psychophysical experiments we studied how surround influences recognition of test objects. The tests were low-contrast Landolt rings of the size 1.1, 1.5 and 2.3 deg. Their centers were located at 13.2 deg from the fixation point. The additional objects were similar Landolt rings or rings without gaps. The distance between the centers of the test and the additional objects varied from 2.2 to 13.2 deg. Inone experiment, the task of the observer was to identify both the test objects and the surrounding objects. In the second experiment the stimulus layout was the same, but'identification of only the test stimulus was required. In both experiments, deterioration of performance was found at all distances between the test objects and the surround, but the deterioration was more significant when the observer carried out the dual task. The data showed that the size of the inhibitory areas in our case does not comply with the Bouma low which states that the size of the interaction areas are equal to half of the eccentricity where the test is presented. Further deterioration of performance in the dual task reveals the contribution of attention into peripheral crowding effects.

  3. [Inhibitory effects of Scutellaria barbate extracts on diethylnitrosamine-induced hepatocarcinoma in rats].

    Science.gov (United States)

    Dai, Zhi-Jun; Wang, Xi-Jing; Ji, Zong-Zheng; Liu, Xiao-Xu; Kang, Hua-Feng; Diao, Yan; Ma, Xiao-Bin; Liu, Lei; Ren, Hong-Tao

    2009-04-01

    To investigate the inhibitory effects of Scutellaria barbate extracts on diethylnitrosamine-induced hepatocarcinoma in rats. Hepatocarcinoma model rats were induced by diethylnitrosamine (DEN). Sixty SD male rats were randomly divided into 4 groups: normal control group, hepatocarcinoma model group, ESB of high dose group and ESB of low dose group. All rats were killed in the 18th week, the levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), total bilirubin (TBIL), alkaline phosphatase (ALP), gamma-glutamyltransferase (gamma-GT) and alpha-L-fucosidase (AFU) in serum were measured by biochemical examinations; Hematoxy and eosin (HE) methods were used to examine the changes of liver pathology. The levels of ALT, AST, TBIL, ALP, gamma-GT, AFU in hepatocarcinoma model group and ESB groups were higher than that of control group (P < 0.05). ESB could relieve hepatic injures. The levels of liver function indexes in ESB groups were lower than that of model group. Histological examination demonstrated that the number of liver cancer nodus in ESB groups were lower than that of model group. Furthermore, ESB could attenuate the grade of cancer cell differentiation. ESB could inhibit experimental hepatocarcinoma and relieve hepatic injures in rats.

  4. Inhibitory effect of curcumin on angiogenesis in ectopic endometrium of rats with experimental endometriosis.

    Science.gov (United States)

    Zhang, Ying; Cao, Hong; Hu, Yue-Yue; Wang, Hua; Zhang, Chang-Jun

    2011-01-01

    The aim of this study was to observe the inhibitory effect of curcumin on endometriosis (EMS) and to determine its influence on vascular endothelial growth factor (VEGF) and microvessel density (MVD) in eutopic and ectopic endometrium of experimental rats, thus exploring the pathogenesis of EMS offering more experimental evidence for the clinical use of curcumin. Forty-eight female virgin rats were subjected to autotransplantation of endometrium during the estrus stage. After four weeks, 8 rats were randomly sacrificed to confirm that the rat model was successful. The remaining rats were randomly divided into four groups. Three groups were intragastrically administered curcumin (50, 100 and 150 mg/kg), and the model group was intragastrically administered vehicle alone. All rats were treated daily for four continuous weeks and examined by histology and immunohistochemical staining for MVD of eutopic and ectopic endometrium. Our results revealed that the cubic capacity of focal tissue in gross appearance was high in the model group and dose-dependently diminished after treatment with curcumin (Pcurcumin (PCurcumin decreased the quantity of microvessels and VEGF protein expression in the heterotopic endometrium of rats with EMS.

  5. In vitro inhibitory effects of plant-derived by-products against Cryptosporidium parvum

    Directory of Open Access Journals (Sweden)

    Teichmann Klaus

    2016-01-01

    Full Text Available Disposal of organic plant wastes and by-products from the food or pharmaceutical industries usually involves high costs. In the present study, 42 samples derived from such by-products were screened in vitro against Cryptosporidium parvum, a protozoan parasite that may contaminate drinking water and cause diarrhoea. The novel bioassay was previously established in the microtitre plate format. Human ileocaecal adenocarcinoma (HCT-8 cell cultures were seeded with C. parvum oocysts and parasite development was monitored by an indirect fluorescent antibody technique (IFAT and microscopic assessment for clusters of secondary infection (CSI. Minimum inhibitory concentrations (MICs and potential detrimental effects on the host cells were determined. An ethanolic extract from olive (Olea europaea pomace, after oil pressing and phenol recovery, reproducibly inhibited C. parvum development (MIC = 250–500 μg mL−1, IC50 = 361 (279–438 μg mL−1, IC90 = 467 (398–615 μg mL−1. Accordingly, tyrosol, hydroxytyrosol, trans-coniferyl alcohol and oleuropein were selected as reference test compounds, but their contributions to the observed activity of the olive pomace extract were insignificant. The established test system proved to be a fast and efficient assay for identifying anti-cryptosporidial activities in biological waste material and comparison with selected reference compounds.

  6. Antifungal properties and inhibitory effects upon aflatoxin production of Thymus vulgaris L. by Aspergillus flavus Link.

    Science.gov (United States)

    Kohiyama, Cássia Yumie; Yamamoto Ribeiro, Milene Mayumi; Mossini, Simone Aparecida Galerani; Bando, Erika; Bomfim, Natália da Silva; Nerilo, Samuel Botião; Rocha, Gustavo Henrique Oliveira; Grespan, Renata; Mikcha, Jane Martha Graton; Machinski, Miguel

    2015-04-15

    The antifungal and antiaflatoxigenic properties of Thymus vulgaris essential oil (TEO) were evaluated upon Aspergillus flavus "in vitro". Suspension containing 10(6) of A. flavus were cultivated with TEO in concentrations ranging from 50 to 500 μg/mL. TEO reached minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) at 250 μg/mL. Inhibition of ergosterol biosynthesis was detected at a concentration of 100 μg/mL of TEO. Morphological evaluation performed by both light microscopy and scanning electron microscopy showed that antifungal activity of TEO could be detected starting at a concentration of 50 μg/mL and the fungicide effect at a concentration of 250 μg/mL. TEO completely inhibited production of both B1 and B2 aflatoxins (AFB1 and AFB2) at a concentration of 150 μg/mL. This way, fungal biomass development and aflatoxin production were dependent on TEO concentration. Therefore, TEO was capable of controlling the growth of A. flavus and its production of aflatoxins. Copyright © 2014 Elsevier Ltd. All rights reserved.

  7. Inhibitory Effects of Pretreatment with Radon on Acute Alcohol-Induced Hepatopathy in Mice

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    Teruaki Toyota

    2012-01-01

    Full Text Available We previously reported that radon inhalation activates antioxidative functions in the liver and inhibits carbon tetrachloride-induced hepatopathy in mice. In addition, it has been reported that reactive oxygen species contribute to alcohol-induced hepatopathy. In this study, we examined the inhibitory effects of radon inhalation on acute alcohol-induced hepatopathy in mice. C57BL/6J mice were subjected to intraperitoneal injection of 50% alcohol (5 g/kg bodyweight after inhaling approximately 4000 Bq/m3 radon for 24 h. Alcohol administration significantly increased the activities of glutamic oxaloacetic transaminase (GOT, glutamic pyruvic transaminase (GPT in serum, and the levels of triglyceride and lipid peroxide in the liver, suggesting acute alcohol-induced hepatopathy. Radon inhalation activated antioxidative functions in the liver. Furthermore, pretreatment with radon inhibited the depression of hepatic functions and antioxidative functions. These findings suggested that radon inhalation activated antioxidative functions in the liver and inhibited acute alcohol-induced hepatopathy in mice.

  8. Obtaining of Solids With Potential Corrosion Inhibitory Effects by Electrocoagulation Vinasse Methods

    Directory of Open Access Journals (Sweden)

    Dra. Elaine Ojeda-Armaignac

    2015-11-01

    Full Text Available In this paper, electrocoagulation experiments are performed at different vinasse samples with a viewto obtaining solids with potential corrosion inhibitory effects. Experimental tests were performed with samples of complex sugar «Argeo Martínez» Guantánamo province, «Urbano Noris Holguín province, in the antique complex Destillery-Brewery «Hatuey» of the province of Santiago de Cuba and in the rum factory of Appleton» in Kingston Jamaica. Electrocoagulation preliminary tests performed with the vinasse from distilleries of Santiago de Cuba, Guantánamo and Holguín allowed the definition of thevariables and their domain, which were considered in the design of experiments to obtain the most favorable conditions of operation. Preliminary experiments corroborated that increasing the current density and pH, increase linearly solids obtained and current density values exceeding 0,194 5 A/cm2 are not feasible because they increase the energy consumption process and the increase of solids is negligible. Validation of electrocoagulation method was demonstrated with results of the experimentaldesign from Jamaica´s vinasse, that were similar to those obtained with Cuban vinasse; reaching favorable conditions for operation at current density of 0,194 5/cm2, pH equal to 8,97 and time 5,6 min, resulting in 15,42 g of total solids for a minimum consumption of 8,44 kW·h/kg.

  9. Inhibitory control in bilinguals and musicians: event related potential (ERP evidence for experience-specific effects.

    Directory of Open Access Journals (Sweden)

    Sylvain Moreno

    Full Text Available Bilinguals and musicians exhibit behavioral advantages on tasks with high demands on executive functioning, particularly inhibitory control, but the brain mechanisms supporting these differences are unclear. Of key interest is whether these forms of experience influence cognition through similar or distinct information processing mechanisms. Here, we recorded event-related potentials (ERPs in three groups - bilinguals, musicians, and controls - who completed a visual go-nogo task that involved the withholding of key presses to rare targets. Participants in each group achieved similar accuracy rates and responses times but the analysis of cortical responses revealed significant differences in ERP waveforms. Success in withholding a prepotent response was associated with enhanced stimulus-locked N2 and P3 wave amplitude relative to go trials. For nogo trials, there were altered timing-specific ERP differences and graded amplitude differences observed in the neural responses across groups. Specifically, musicians showed an enhanced early P2 response accompanied by reduced N2 amplitude whereas bilinguals showed increased N2 amplitude coupled with an increased late positivity wave relative to controls. These findings demonstrate that bilingualism and music training have differential effects on the brain networks supporting executive control over behavior.

  10. Inhibitory effect of cucurbitacin B on imiquimod-induced skin inflammation

    International Nuclear Information System (INIS)

    Li, Zheng Jun; Shin, Jung-Min; Choi, Dae-Kyoung; Lim, Seul Ki; Yoon, Tae-Jin; Lee, Young Ho; Sohn, Kyung-Cheol; Im, Myung; Lee, Young; Seo, Young-Joon; Kim, Chang Deok; Lee, Jeung-Hoon

    2015-01-01

    Psoriasis is a common skin disease, of which pathogenesis involves the increase of inflammatory reaction in epidermal cells. In an attempt to find therapeutics for psoriasis, we found that cucurbitacin B has an inhibitory potential on imiquimod-induced inflammation of keratinocytes. Cucurbitacin B significantly inhibited imiquimod-induced expression of crucial psoriatic cytokines, such as IL-8 and CCL20, via down-regulation of NF-κB and STAT3 signaling pathway in human keratinocytes. In addition, keratinocyte proliferation was markedly inhibited by cucurbitacin B. The potential beneficial effect of cucurbitacin B on psoriasis was further validated in imiquimod-induced psoriasiform dermatitis of experimental animal. Topical application of cucurbitacin B resulted in significant reduction of epidermal hyperplasia and inflammatory cytokines production, and ameliorated the psoriatic symptom. Taken together, these results suggest that cucurbitacin B may be a potential candidate for the treatment of psoriasis. - Highlights: • Cucurbitacin B has a potential for inhibiting the growth of keratinocytes. • Cucurbitacin B inhibits imiquimod-induced inflammatory reaction in keratinocytes. • Cucurbitacin B inhibits imiquimod-induced psoriasiform dermatitis in experimental animal

  11. Leucemia inhibitory factor; investigating the time-dependent effect on viability of vitrified bovine embryos.

    Science.gov (United States)

    Kocyigit, A; Cevik, M

    2017-12-01

    Leucemia inhibitory factor (LIF) is involved in various reproductive processes, including sperm development, regulation of ovulation, as well as blastocyst formation, hatching and implantation in embryos. Moreover, LIF has also been shown significantly to enhance the blastocyst formation rates of bovine embryos, a finding that remains controversial. Our purpose was to investigate time-dependent effect of LIF on bovine embryo culture, especially in terms of addition timing. Presumptive zygotes were cultured in five different groups. In this study, 100 ng/ml LIF was added to the culture medium were as follows; control: SOF alone, group A: at day 0 (fertilization day), group B: at day 4 post-insemination (p.i.), group C: at day 4 to 7 (p.i. before vitrification) and group D: at day 8 (p.i. after thawing). Addition of LIF to the culture medium at day 4 significantly increased the percentage of blastocyst rate when compared day 0, day 4 at 6/7 and control group (41.8% versus 24.3%, 19.7%, 34.6%). In conclusion, the addition of LIF only on day 4 (p.i.) to the culture medium was found to be beneficial for bovine embryonic development based on several measures, including blastocysts rate, re-expansion rate and cellular cryotolerance after vitrification. © 2017 Blackwell Verlag GmbH.

  12. Inhibitory effect of Allium sativum and Zingiber officinale extracts on clinically important drug resistant pathogenic bacteria.

    Science.gov (United States)

    Gull, Iram; Saeed, Mariam; Shaukat, Halima; Aslam, Shahbaz M; Samra, Zahoor Qadir; Athar, Amin M

    2012-04-27

    Herbs and spices are very important and useful as therapeutic agent against many pathological infections. Increasing multidrug resistance of pathogens forces to find alternative compounds for treatment of infectious diseases. In the present study the antimicrobial potency of garlic and ginger has been investigated against eight local clinical bacterial isolates. Three types of extracts of each garlic and ginger including aqueous extract, methanol extract and ethanol extract had been assayed separately against drug resistant Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, Staphylococcus aureus, Klebsiella pneumoniae, Shigella sonnei, Staphylococcusepidermidis and Salmonella typhi. The antibacterial activity was determined by disc diffusion method. All tested bacterial strains were most susceptible to the garlic aqueous extract and showed poor susceptibility to the ginger aqueous extract. The (minimum inhibitory concentration) MIC of different bacterial species varied from 0.05 mg/ml to 1.0 mg/ml. In the light of several socioeconomic factors of Pakistan mainly poverty and poor hygienic condition, present study encourages the use of spices as alternative or supplementary medicine to reduce the burden of high cost, side effects and progressively increasing drug resistance of pathogens.

  13. Inhibitory effect of Allium sativum and Zingiber officinale extracts on clinically important drug resistant pathogenic bacteria

    Directory of Open Access Journals (Sweden)

    Gull Iram

    2012-04-01

    Full Text Available Abstract Background Herbs and spices are very important and useful as therapeutic agent against many pathological infections. Increasing multidrug resistance of pathogens forces to find alternative compounds for treatment of infectious diseases. Methods In the present study the antimicrobial potency of garlic and ginger has been investigated against eight local clinical bacterial isolates. Three types of extracts of each garlic and ginger including aqueous extract, methanol extract and ethanol extract had been assayed separately against drug resistant Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, Staphylococcus aureus, Klebsiella pneumoniae, Shigella sonnei, Staphylococcusepidermidis and Salmonella typhi. The antibacterial activity was determined by disc diffusion method. Results All tested bacterial strains were most susceptible to the garlic aqueous extract and showed poor susceptibility to the ginger aqueous extract. The (minimum inhibitory concentration MIC of different bacterial species varied from 0.05 mg/ml to 1.0 mg/ml. Conclusion In the light of several socioeconomic factors of Pakistan mainly poverty and poor hygienic condition, present study encourages the use of spices as alternative or supplementary medicine to reduce the burden of high cost, side effects and progressively increasing drug resistance of pathogens.

  14. Smells like inhibition: The effects of olfactory and visual alcohol cues on inhibitory control.

    Science.gov (United States)

    Monk, R L; Sunley, J; Qureshi, A W; Heim, D

    2016-04-01

    How the smell of alcohol impacts alcohol-related thoughts and behaviours is unclear, though it is well-documented that alcohol-related stimuli and environments may trigger these. The current study, therefore, aimed to investigate the priming effects of both visual and olfactory alcohol cues on inhibitory control. Forty individuals (M age = 23.65, SD = 6.52) completed a go/no-go association task (GNAT) which measured reaction times, response accuracy and false alarm rates whilst being exposed to alcohol-related (or neutral) olfactory and visual cues. Alcohol-related visual cues elicited lower false alarm rates, slower reaction times and higher accuracy rates relative to neutral pictorial cues. False alarm rates were significantly higher for those exposed to alcohol as opposed to neutral olfactory cues. By highlighting that exposure to alcohol-related olfactory cues may impede response inhibition, the results indicate that exposure to such stimuli may contribute to the activation of cognitive responses which may drive consumption.

  15. Inhibitory effect of raspberry ketone on α-glucosidase: Docking simulation integrating inhibition kinetics.

    Science.gov (United States)

    Xiong, Shang-Ling; Yue, Li-Mei; Lim, Gyu Tae; Yang, Jun-Mo; Lee, Jinhyuk; Park, Yong-Doo

    2018-02-26

    Inhibition of α-glucosidase is directly associated with treatment of type 2 diabetes. In this regard, we conducted enzyme kinetics integrated with computational docking simulation to assess the inhibitory effect of raspberry ketone (RK) on α-glucosidase. RK bound to the active site of α-glucosidase and interacted with several key residues such as ASP68, TYR71, HIS111, PHE157, PHE158, PHE177, GLN181, ASP214, THR215, ASP349, ASP408, and ARG439, as detected by protein-ligand docking simulation. Subsequently, we confirmed the action of RK on α-glucosidase as the non-competitive type of inhibition in a reversible and rapidly binding manner. The relevant kinetic parameters were IC 50 =6.17±0.46mM and K i =7.939±0.211mM. Regarding the structure-activity relationship, the higher concentration of RK induced slight modulation of the shape of the active site as monitored by hydrophobic exposure. The tertiary conformational change was linked to RK inhibition, and mostly involved regional changes of the active site. Our study provides insight into the functional role of RK due to its structural property of a hydroxyphenyl ring that interacts with the active site of α-glucosidase. We suggest that similar hydroxyphenyl ring compounds targeting the key residues of the active site might be potential α-glucosidase inhibitors. Copyright © 2018. Published by Elsevier B.V.

  16. Lignan from Thyme Possesses Inhibitory Effect on ASIC3 Channel Current*

    Science.gov (United States)

    Dubinnyi, Maxim A.; Osmakov, Dmitry I.; Koshelev, Sergey G.; Kozlov, Sergey A.; Andreev, Yaroslav A.; Zakaryan, Naira A.; Dyachenko, Igor A.; Bondarenko, Dmitry A.; Arseniev, Alexander S.; Grishin, Eugene V.

    2012-01-01

    A novel compound was identified in the acidic extract of Thymus armeniacus collected in the Lake Sevan region of Armenia. This compound, named “sevanol,” to our knowledge is the first low molecular weight natural molecule that has a reversible inhibition effect on both the transient and the sustained current of human ASIC3 channels expressed in Xenopus laevis oocytes. Sevanol completely blocked the transient component (IC50 353 ± 23 μm) and partially (∼45%) inhibited the amplitude of the sustained component (IC50 of 234 ± 53 μm). Other types of acid-sensing ion channel (ASIC) channels were intact to sevanol application, except ASIC1a, which showed more than six times less affinity to it as compared with the inhibitory action on the ASIC3 channel. To elucidate the structure of sevanol, the set of NMR spectra in two solvents (d6-DMSO and D2O) was collected, and the complete chemical structure was confirmed by liquid chromatography-mass spectrometry with electrospray ionization (LC-ESI+-MS) fragmentation. This compound is a new lignan built up of epiphyllic acid and two isocitryl esters in positions 9 and 10. In vivo administration of sevanol (1–10 mg/kg) significantly reversed thermal hyperalgesia induced by complete Freund's adjuvant injection and reduced response to acid in a writhing test. Thus, we assume the probable considerable role of sevanol in known analgesic and anti-inflammatory properties of thyme. PMID:22854960

  17. Inhibitory effect of cucurbitacin B on imiquimod-induced skin inflammation

    Energy Technology Data Exchange (ETDEWEB)

    Li, Zheng Jun; Shin, Jung-Min; Choi, Dae-Kyoung; Lim, Seul Ki [Department of Dermatology, School of Medicine, Chungnam National University, Daejeon (Korea, Republic of); Yoon, Tae-Jin [Department of Dermatology, School of Medicine, Gyeongsang National University, Jinju (Korea, Republic of); Lee, Young Ho [Department of Anatomy, School of Medicine, Chungnam National University, Daejeon (Korea, Republic of); Sohn, Kyung-Cheol; Im, Myung; Lee, Young; Seo, Young-Joon; Kim, Chang Deok [Department of Dermatology, School of Medicine, Chungnam National University, Daejeon (Korea, Republic of); Lee, Jeung-Hoon, E-mail: jhoon@cnu.ac.kr [Department of Dermatology, School of Medicine, Chungnam National University, Daejeon (Korea, Republic of); Skin Med Company, Daejeon (Korea, Republic of)

    2015-04-17

    Psoriasis is a common skin disease, of which pathogenesis involves the increase of inflammatory reaction in epidermal cells. In an attempt to find therapeutics for psoriasis, we found that cucurbitacin B has an inhibitory potential on imiquimod-induced inflammation of keratinocytes. Cucurbitacin B significantly inhibited imiquimod-induced expression of crucial psoriatic cytokines, such as IL-8 and CCL20, via down-regulation of NF-κB and STAT3 signaling pathway in human keratinocytes. In addition, keratinocyte proliferation was markedly inhibited by cucurbitacin B. The potential beneficial effect of cucurbitacin B on psoriasis was further validated in imiquimod-induced psoriasiform dermatitis of experimental animal. Topical application of cucurbitacin B resulted in significant reduction of epidermal hyperplasia and inflammatory cytokines production, and ameliorated the psoriatic symptom. Taken together, these results suggest that cucurbitacin B may be a potential candidate for the treatment of psoriasis. - Highlights: • Cucurbitacin B has a potential for inhibiting the growth of keratinocytes. • Cucurbitacin B inhibits imiquimod-induced inflammatory reaction in keratinocytes. • Cucurbitacin B inhibits imiquimod-induced psoriasiform dermatitis in experimental animal.

  18. Effects of temperature and medium composition on inhibitory activities of gossypol-related compounds against aflatoxigenic fungi.

    Science.gov (United States)

    Mellon, J E; Dowd, M K; Beltz, S B

    2013-07-01

    To investigate the effects of temperature and medium composition on growth/aflatoxin inhibitory activities of terpenoids gossypol, gossypolone and apogossypolone against Aspergillus flavus and A. parasiticus. The compounds were tested at a concentration of 100 μg ml(-1) in a Czapek Dox (Czapek) agar medium at 25, 31 and 37°C. Increased incubation temperature marginally increased growth inhibition caused by these compounds, but reduced the aflatoxin inhibition effected by gossypol. Gossypolone and apogossypolone retained good aflatoxin inhibitory activity against A. flavus and A. parasiticus at higher incubation temperatures. However, increased temperature also significantly reduced aflatoxin production in control cultures. The effects of the terpenoids on fungal growth and aflatoxin production against the same fungi were also determined in Czapek, Czapek with a protein/amino acid addendum and yeast extract sucrose (YES) media. Growth of these fungi in the protein-supplemented Czapek medium or in the YES medium greatly reduced the growth inhibition effects of the terpenoids. Apogossypolone displayed strong anti-aflatoxigenic activity in the Czapek medium, but this activity was significantly reduced in the protein-amended Czapek and YES media. Gossypol, which displayed little to no aflatoxin inhibitory activity in the Czapek medium, did yield significant anti-aflatoxigenic activity in the YES medium. Incubation temperature and media composition are important parameters involved in the regulation of aflatoxin production in A. flavus and A. parasiticus. These parameters also affect the potency of growth and aflatoxin inhibitory activities of these gossypol-related compounds against aflatoxigenic fungi. Studies utilizing gossypol-related compounds as inhibitory agents of biological activities should be interpreted with caution due to compound interaction with multiple components of the test system, especially serum proteins. Published [2013]. This article is a

  19. Inhibitory effect of Hydrex anti-scalant on calcium scale deposition from seawater under multiple-effect distillers' conditions

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    Aiman Eid Al-Rawajfeh

    2015-09-01

    Full Text Available In this work, the inhibitory effect of a commercial anti-scalant (Veolia Hydrex® 9209 on the calcium minerals of carbonate, sulfate and hydrocalumite (Ca/Al clay deposition from seawater has been investigated. Different concentration factors and anti-scalant doses were studied by analyzing the water hardness and turbidity. The inhibitory effect of the investigated anti-scalant was efficient even at lower concentrations. The percentage inhibition decreases with increasing the temperature and increases with increasing the dose/amount of the anti-scalant. The carbonate scale inhibition was >99% and 98–99% at 50 and 70 °C, respectively. The percentage inhibition of sulfate from hemihydrate was ranged from 80% to 87% for 2 and 8 ppm anti-scalant at 50 °C. The inhibition of Ca/Al hydrocalumite deposition increases from 70% to 90% upon increasing the dose from 3 to 5 ppm, respectively. A recommended useful dose of antiscalant for seawater is 5 ppm.

  20. A cyclohexanecarboxamide derivative with inhibitory effects on Schistosoma mansoni cercarial serine protease and penetration of mice skin by the parasite.

    Science.gov (United States)

    Bahgat, Mahmoud; Aboul-Enein, Mohamed N; El Azzouny, Aida A; Maghraby, Amany; Ruppel, Andreas; Soliman, Wael M

    2009-01-01

    A cyclohexanecarboxamide derivative, N-phenyl-N-[1-(piperidine-1-carbonyl)cyclohexyl] benzamide (MNRC-5), was evaluated for its inhibitory effects on Schistosoma mansoni cercarial serine protease activity and cercarial penetration. MNRC-5 exerted an inhibitory effect on S. mansoni cercarial serine protease at serial concentrations of the specific chromogenic substrate Boc-Val-Leu-Gly-Arg-PNA for such enzyme family and the inhibitory coefficient (Ki) value was deduced. Moreover, topical treatment of mice tails with the most potent inhibitory concentration of MNRC-5 formulated in jojoba oil successfully blocked cercarial penetration as demonstrated by a significant reduction (75%; p jojoba oil base containing no MNRC-5. In addition, the IgM and IgG reactivities to crude S. mansoni cercarial, worm and egg antigens were generally lower in sera from treated infected mice than untreated infected mice. In conclusion, we report on a new serine protease inhibitor capable for blocking penetration of host skin by S. mansoni cercariae as measured by lowering worm burden and decrease in the levels of both IgM and IgG towards different bilharzial antigens upon topical treatment.

  1. Inhibitory effects of Urtica dioica L. root on electrophysiological properties of isolated rabbit atrioventricular node

    Directory of Open Access Journals (Sweden)

    A. Enayati

    2017-11-01

    Full Text Available Background and objectives: The ideal drug for treatment of a wide range of supraventricular arrhythmia hasn't yet been developed. Previous studies have shown antihypertensive and negative inotropic effects of the Urtica dioica L. (nettle. Therefore, the aim of present study is to determine the rate dependent inhibitory effects of ethanol extract of nettle root and investigate the role of adrenoceptors in the anti-arrhythmic mechanism of nettle on the isolated rabbit atrio-ventricular node. Methods: Urtica dioica roots were collected from Gorgan (Golestan, Iran. Male New Zealand rabbits (n=7 were used in all of the experiments. Experimental stimulation protocols (WBCL; Recovery, Facilitation, Fatigue were applied to assess electrophysiological properties of Node. All protocols were repeated in the presence and absence (control of different concentration (0.25-0.5 w/v % of nettle and 1 μM nadolol. Data were shown as Mean±SE, difference between groups statistically were assessed by SPSS software. Results: Nettle (0.5 w/v significantly decreased basic and functional properties of node as WBCL, ERP, FRP, AVCT and magnitude of fatigue (∆AH significantly increased but ∆FRP significantly decreased. In the presence of nadolol (1μM as a nonselective β-blocker, nettle (0.3 mg/L could not repeat its effects on electrophysiological properties of AV-node. Conclusion: The results showed the modifying properties of Urtica dioica root extract. It may be considered as a candidate for the treatment of supraventicular arrhythmias.

  2. Inhibitory effect of benzene metabolites on nuclear DNA synthesis in bone marrow cells

    International Nuclear Information System (INIS)

    Lee, E.W.; Johnson, J.T.; Garner, C.D.

    1989-01-01

    Effects of endogenously produced and exogenously added benzene metabolites on the nuclear DNA synthetic activity were investigated using a culture system of mouse bone marrow cells. Effects of the metabolites were evaluated by a 30-min incorporation of [ 3 H]thymidine into DNA following a 30-min interaction with the cells in McCoy's 5a medium with 10% fetal calf serum. Phenol and muconic acid did not inhibit nuclear DNA synthesis. However, catechol, 1,2,4-benzenetriol, hydroquinone, and p-benzoquinone were able to inhibit 52, 64, 79, and 98% of the nuclear DNA synthetic activity, respectively, at 24 μM. In a cell-free DNA synthetic system, catechol and hydroquinone did not inhibit the incorporation of [ 3 H]thymidine triphosphate into DNA up to 24 μM but 1,2,4-benzenetriol and p-benzoquinone did. The effect of the latter two benzene metabolites was completely blocked in the presence of 1,4-dithiothreitol (1 mM) in the cell-free assay system. Furthermore, when DNA polymerase α, which requires a sulfhydryl (SH) group as an active site, was replaced by DNA polymerase 1, which does not require an SH group for its catalytic activity, p-benzoquinone and 1,2,4-benzenetriol were unable to inhibit DNA synthesis. Thus, the data imply the p-benzoquinone and 1,2,4-benzenetriol inhibited DNA polymerase α, consequently resulting in inhibition of DNA synthesis in both cellular and cell-free DNA synthetic systems. The present study identifies catechol, hydroquinone, p-benzoquinone, and 1,2,4-benzenetriol as toxic benzene metabolites in bone marrow cells and also suggests that their inhibitory action on DNA synthesis is mediated by mechanism(s) other than that involving DNA damage as a primary cause

  3. TNF‐α has both stimulatory and inhibitory effects on mouse monocyte‐derived osteoclastogenesis

    Science.gov (United States)

    Jansen, Ineke D.C.; Sprangers, Sara; de Vries, Teun J.; Everts, Vincent

    2017-01-01

    Phenotypically different osteoclasts may be generated from different subsets of precursors. To what extent the formation of these osteoclasts is influenced or mediated by the inflammatory cytokine TNF‐α, is unknown and was investigated in this study. The osteoclast precursors early blasts (CD31hiLy‐6C−), myeloid blasts (CD31+Ly‐6C+), and monocytes (CD31−Ly‐6Chi) were sorted from mouse bone marrow using flow cytometry and cultured with M‐CSF and RANKL, with or without TNF‐α. Surprisingly, TNF‐α prevented the differentiation of TRAcP+ osteoclasts generated from monocytes on plastic; an effect not seen with early blasts and myeloid blasts. This inhibitory effect could not be prevented by other cytokines such as IL‐1β or IL‐6. When monocytes were pre‐cultured with M‐CSF and RANKL followed by exposure to TNF‐α, a stimulatory effect was found. TNF‐α also stimulated monocytes’ osteoclastogenesis when the cells were seeded on bone. Gene expression analysis showed that when TNF‐α was added to monocytes cultured on plastic, RANK, NFATc1, and TRAcP were significantly down‐regulated while TNF‐αR1 and TNF‐αR2 were up‐regulated. FACS analysis showed a decreased uptake of fluorescently labeled RANKL in monocyte cultures in the presence of TNF‐α, indicating an altered ratio of bound‐RANK/unbound‐RANK. Our findings suggest a diverse role of TNF‐α on monocytes’ osteoclastogenesis: it affects the RANK‐signaling pathway therefore inhibits osteoclastogenesis when added at the onset of monocyte culturing. This can be prevented when monocytes were pre‐cultured with M‐CSF and RANKL, which ensures the binding of RANKL to RANK. This could be a mechanism to prevent unfavorable monocyte‐derived osteoclast formation away from the bone. PMID:28543070

  4. Effect of chronic restraint stress on inhibitory gating in the auditory cortex of rats.

    Science.gov (United States)

    Ma, Lanlan; Li, Wai; Li, Sibin; Wang, Xuejiao; Qin, Ling

    2017-05-01

    A fundamental adaptive mechanism of auditory function is inhibitory gating (IG), which refers to the attenuation of neural responses to repeated sound stimuli. IG is drastically impaired in individuals with emotional and cognitive impairments (i.e. posttraumatic stress disorder). The objective of this study was to test whether chronic stress impairs the IG of the auditory cortex (AC). We used the standard two-tone stimulus paradigm and examined the parametric qualities of IG in the AC of rats by recording the electrophysiological signals of a single-unit and local field potential (LFP) simultaneously. The main results of this study were that most of the AC neurons showed a weaker response to the second tone than to the first tone, reflecting an IG of the repeated input. A fast negative wave of LFP showed consistent IG across the sampled AC sites, whereas a slow positive wave of LFP had less IG effect. IG was diminished following chronic restraint stress at both, the single-unit and LFP level, due to the increase in response to the second tone. This study provided new evidence that chronic stress disrupts the physiological function of the AC. Lay Summary The effects of chronic stress on IG were investigated by recording both, single-unit spike and LFP activities, in the AC of rats. In normal rats, most of the single-unit and N25 LFP activities in the AC showed an IG effect. IG was diminished following chronic restraint stress at both, the single-unit and LFP level.

  5. Solution NMR structure and inhibitory effect against amyloid-β fibrillation of Humanin containing a D-isomerized serine residue

    Energy Technology Data Exchange (ETDEWEB)

    Alsanousi, Nesreen [Institute for Protein Research, Osaka University, 3-2 Yamadaoka, Suita, Osaka 565-0871 (Japan); Sugiki, Toshihiko, E-mail: sugiki@protein.osaka-u.ac.jp [Institute for Protein Research, Osaka University, 3-2 Yamadaoka, Suita, Osaka 565-0871 (Japan); Furuita, Kyoko; So, Masatomo; Lee, Young-Ho; Fujiwara, Toshimichi [Institute for Protein Research, Osaka University, 3-2 Yamadaoka, Suita, Osaka 565-0871 (Japan); Kojima, Chojiro, E-mail: kojima-chojiro-xk@ynu.ac.jp [Institute for Protein Research, Osaka University, 3-2 Yamadaoka, Suita, Osaka 565-0871 (Japan); Graduate School of Engineering, Yokohama National University, Tokiwadai 79-5, Hodogaya-ku, Yokohama 240-8501 (Japan)

    2016-09-02

    Humanin comprising 24 amino acid residues is a bioactive peptide that has been isolated from the brain tissue of patients with Alzheimer's disease. Humanin reportedly suppressed aging-related death of various cells due to amyloid fibrils and oxidative stress. There are reports that the cytoprotective activity of Humanin was remarkably enhanced by optical isomerization of the Ser14 residue from L to D form, but details of the molecular mechanism remained unclear. Here we demonstrated that Humanin D-Ser14 exhibited potent inhibitory activity against fibrillation of amyloid-β and remarkably higher binding affinity for amyloid-β than that of the Humanin wild-type and S14G mutant. In addition, we determined the solution structure of Humanin D-Ser14 by nuclear magnetic resonance (NMR) and showed that D-isomerization of the Ser14 residue enables drastic conformational rearrangement of Humanin. Furthermore, we identified an amyloid-β-binding site on Humanin D-Ser14 at atomic resolution by NMR. These biophysical and high-resolution structural analyses clearly revealed structure–function relationships of Humanin and explained the driving force of the drastic conformational change and molecular basis of the potent anti-amyloid-β fibrillation activity of Humanin caused by D-isomerization of the Ser14 residue. This is the first study to show correlations between the functional activity, tertiary structure, and partner recognition mode of Humanin and may lead to elucidation of the molecular mechanisms of the cytoprotective activity of Humanin. - Highlights: • Humanin D-Ser14 showed the strongest inhibitory activity against Aβ40 fibrillation. • NMR structure of Humanin D-Ser14 was determined in alcohol/water mixture solution. • Humanin D-Ser14 directly bound Aβ40 stronger than Humanin wild-type and Humanin S14G. • Aβ40 and zinc ion binding sites of Humanin D-Ser14 were identified. • Structure around Ser14 of Humanin is critical for Aβ40 binding and

  6. The inhibitory effect of Penicillium camemberti and Geotruchum candidum on the associated funga of white mould cheese

    DEFF Research Database (Denmark)

    Decker, Marianne; Nielsen, P.V.

    2005-01-01

    effects of C. herbarum, and this was most pronounced in the early stages of growth. The interaction mechanism of C. herbarum was not affected by the choice of the strain of P. camemberti whereas the Penicillium contaminants were very sensitive to the choice of the R. camemberti strain. The presence of G...... contamination at the critical point of the salt brine. Pure P. camemberti had the largest inhibitory effect on the C. herbarum contaminant. Adding G. candidum in mixed cultures weakened the inhibitory effect of P. camemberti on C. herbarum. Low levels of G. candidum (10(3) spore/ml) promoted visible growth....... candidum in the mixed cultures seems to decrease the suppressing effect of pour-plated P. camemberti. No correlation of any kind was found in the pour-plated spore concentration totals by the inhibition of the C. herbarum and P. roqueforti contaminants whereas R. caseifulvum and P commune were sensitive...

  7. Inhibitory effect and molecular mechanism of mesenchymal stem cells on NSCLC cells.

    Science.gov (United States)

    Pan, Mengwu; Hou, Lingling; Zhang, Jingsi; Zhao, Diandian; Hua, Jilei; Wang, Ziling; He, Jinsheng; Jiang, Hong; Hu, Honggang; Zhang, Lishu

    2018-04-01

    Non-small-cell lung cancer (NSCLC) is still the main threat of cancer-associated death. Current treatment of NSCLC has limited effectiveness, and unfortunately, the prognosis of NSCLC remains poor. Therefore, a novel strategy for cancer therapy is urgently needed. Stem cell therapy has significant potential for cancer treatment. Mesenchymal stem cells (MSCs) with capacity for self-renewal and differentiation into various cells types exhibit the feature of homing to tumor site and immunosuppression, have been explored as a new treatment for various cancers. Studies revealed that the broad repertoire of trophic factors secreted by MSCs extensively involved in the interplay between MSCs and tumor cells. In this study, we confirmed that MSCs do have the paracrine effect on proliferation and migration of NSCLC cells (A549, NCI-H460, and SK-MES-1). Co-culture system and conditioned medium experiments results showed that soluble factors secreted by MSCs inhibited the proliferation of NSCLC cells in vitro. The scratch assay showed that conditioned medium of MSCs could suppress the migration of NSCLC cells in vitro. Western blot results showed that the expression of proteins relevant to cell proliferation, anti-apoptosis, and migration was remarkably decreased via MAPK/eIF4E signaling pathway. We speculated that soluble factors secreted by MSCs might be responsible for inhibitory mechanism of NSCLC cells. By Human Gene Expression Microarray Assay and recombinant Vascular Endothelial Growth Factor 165 (VEGF165) neutralizing experiment, we verified that VEGF might be responsible for the down-regulation of proteins related to cell proliferation, anti-apoptosis, and migration by suppressing translation initiation factor eIF4E via MAPK signaling pathway. Taken together, our study demonstrated that a possible trophic factor secreted by MSCs could manipulate translation initiation of NSCLC cells via MAPK signaling pathway, and significantly affect the fate of tumor cells, which

  8. Inhibitory effect of silver nanomaterials on transmissible virus-induced host cell infections.

    Science.gov (United States)

    Lv, Xiaonan; Wang, Peng; Bai, Ru; Cong, Yingying; Suo, Siqingaowa; Ren, Xiaofeng; Chen, Chunying

    2014-04-01

    Coronaviruses belong to the family Coronaviridae, which primarily cause infection of the upper respiratory and gastrointestinal tract of hosts. Transmissible gastroenteritis virus (TGEV) is an economically significant coronavirus that can cause severe diarrhea in pigs. Silver nanomaterials (Ag NMs) have attracted great interests in recent years due to their excellent anti-microorganism properties. Herein, four representative Ag NMs including spherical Ag nanoparticles (Ag NPs, NM-300), two kinds of silver nanowires (XFJ011) and silver colloids (XFJ04) were selected to study their inhibitory effect on TGEV-induced host cell infection in vitro. Ag NPs were uniformly distributed, with particle sizes less than 20 nm by characterization of environmental scanning electron microscope and transmission electron microscope. Two types of silver nanowires were 60 nm and 400 nm in diameter, respectively. The average diameter of the silver colloids was approximately 10 nm. TGEV infection induced the occurring of apoptosis in swine testicle (ST) cells, down-regulated the expression of Bcl-2, up-regulated the expression of Bax, altered mitochondrial membrane potential, activated p38 MAPK signal pathway, and increased expression of p53 as evidenced by immunofluorescence assays, real-time PCR, flow cytometry and Western blot. Under non-toxic concentrations, Ag NPs and silver nanowires significantly diminished the infectivity of TGEV in ST cells. Moreover, further results showed that Ag NPs and silver nanowires decreased the number of apoptotic cells induced by TGEV through regulating p38/mitochondria-caspase-3 signaling pathway. Our data indicate that Ag NMs are effective in prevention of TGEV-mediated cell infection as a virucidal agent or as an inhibitor of viral entry and the present findings may provide new insights into antiviral therapy of coronaviruses. Copyright © 2014 Elsevier Ltd. All rights reserved.

  9. Inhibitory effect of putranjivain A on allergic inflammation through suppression of mast cell activation

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Hui-Hun; Park, Seung-Bin; Lee, Soyoung [CMRI, Department of Pharmacology, School of Medicine, Kyungpook National University, Daegu 700-422 (Korea, Republic of); Kwon, Taeg Kyu [Department of Immunology, School of Medicine, Keimyung University, Daegu 704-701 (Korea, Republic of); Shin, Tae-Yong [College of Pharmacy, Woosuk University, Jeonju 565-701 (Korea, Republic of); Park, Pil-Hoon; Lee, Seung-Ho [College of Pharmacy, Youngnam University, Kyungsan 712-749 (Korea, Republic of); Kim, Sang-Hyun, E-mail: shkim72@knu.ac.kr [CMRI, Department of Pharmacology, School of Medicine, Kyungpook National University, Daegu 700-422 (Korea, Republic of)

    2014-02-01

    A great number of people are suffering from allergic inflammatory disease such as asthma, atopic dermatitis, and sinusitis. Therefore discovery of drugs for the treatment of these diseases is an important subject in human health. Putranjivain A (PJA), member of ellagitannin, is known to possess beneficial effects including anti-cancer and anti-viral activities. The aim of the present study was to elucidate whether PJA modulates the allergic inflammatory reaction and to study its possible mechanisms of action using mast cell-based in vitro and in vivo models. The study was performed in anaphylaxis mouse model and cultured mast cells. PJA inhibited the expression of pro-inflammatory cytokines in immunoglobulin E-stimulated mast cells. PJA reduced this expression by inhibiting nuclear factor (NF)-κB and nuclear factor of activated T cell. The oral administration of PJA reduced systemic and cutaneous anaphylaxis, the release of serum histamine, and the expression of the histamine H{sub 1} receptor. In addition, PJA attenuated the activation of mast cells. PJA inhibited the release of histamine from various types of mast cells by the suppression of intracellular calcium. The inhibitory activity of PJA on the allergic reaction was similar to that of disodium cromoglycate, a known anti-allergic drug. These results suggest that PJA can facilitate the prevention or treatment of allergic inflammatory diseases mediated by mast cells. - Highlights: • PJA reduced the degranulation of mast cells. • PJA inhibited the production of inflammatory cytokines. • The effect of PJA on allergic reaction was comparable to the DSCG. • PJA might be a candidate for the treatment of allergic inflammatory diseases.

  10. Inhibitory effects of organochlorine pesticides on intercellular transfer of Lucifer Yellow in cultured bovine oviductal cells.

    Science.gov (United States)

    Tiemann, U; Pöhland, R

    1999-01-01

    The present study investigated the effects of dichlorodiphenyltrichloroethane (DDT), methoxychlor (MXC), and gamma-hexachlorocyclohexane (gammaHCH, lindane) on gap junctional intercellular communication (GJIC) in cultured bovine oviductal cells. GJIC was evaluated by microinjecting fluorescent dye Lucifer Yellow and observing the inhibition of the spreading of dye into adjacent cells. After incubation for 1 h at 37 degrees C, a dose-dependent inhibition of GJIC was observed over a concentration range of 16 to 128 microM DDT, MXC, or gammaHCH compared with nonexposed controls. A significant inhibition began at 32 microM DDT, MXC, or gammaHCH. After incubation for 5 h, a dose-dependent inhibition of GJIC was obtained in the concentration range from 8 to 64 microM of the pesticides. The first significant inhibitory effect on GJIC was caused by 8 microM DDT, 16 microM MXC, and 32 microM gammaHCH. The 128 microM concentration of the pesticides was toxic. At pesticide concentration of 64 microM, the decrease in dye-coupling observed was not due to lethal cell injury, as is indicated by the use of trypan blue dye exclusion. After removal of 64 microM DDT from the culture medium, intercellular communication was reestablished within 3 h. Measurement of cytosolic free Ca2+ concentration [Ca2+]i in fura-2/AM-loaded oviductal cells showed that the inhibition of GJIC by addition of DDT, MXC, or gammaHCH was not associated with a detectable increase in [Ca2+]i. Coincubation of the DDT with dibutyryl-cAMP prevented the 64 microM DDT-induced inhibition of intercellular communication in adherent oviduct cells. It is suggested that organochlorine pesticides can influence cells responsible for reproduction.

  11. Inhibitory Effects of Probiotic Lactobacillus on the Growth of Human Colonic Carcinoma Cell Line HT-29

    Directory of Open Access Journals (Sweden)

    Zhung-Yuan Chen

    2017-01-01

    Full Text Available This study was conducted to investigate the inhibitory effect of Lactobacillus cells and supernatants on the growth of the human colon cancer cell line HT-29. Our study results indicated that the PM153 strain exhibits the best adhesion ability and the highest survival in the gastrointestinal tract simulation experiment. Furthermore, after an 8-h co-culture of PM153 and HT-29 cells, the PM153 strain can induce the secretion of nitric oxide from the HT-29 cells. In addition, after the co-culture of the BCRC17010 strain (109 cfu/mL and HT-29 cells, the Bax/Bcl-2 ratio in the HT-29 cells was 1.19, which showed a significant difference from the other control and LAB groups (p < 0.05, which therefore led to the inference that the BCRC17010 strain exerts a pro-apoptotic effect on the HT-29 cells. Upon co-culture with HT-29 cells for 4, 8 and 12 h, the BCRC14625 strain (109 cfu/mL demonstrated a significant increase in lactate dehydrogenase (LDH activity (p < 0.05, causing harm to the HT-29 cell membrane; further, after an 8-h co-culture with the HT-29 cells, it induced the secretion of nitric oxide (NO from the HT-29 cells. Some lactic acid bacteria (LAB strains have ability to inhibit the growth of the colorectal cancer cell line HT-29 Bax/Bcl-2 pathway or NO production. In summary, we demonstrated that the BCRC17010 strain, good abilities of adhesion and increased LDH release, was the best probiotic potential for inhibition of HT-29 growth amongst the seven LAB strains tested in vitro.

  12. Inhibitory Effects of Nitrite on Acid Production in Dental Plaque in Children.

    Science.gov (United States)

    Yamamoto, Yuji; Washio, Jumpei; Shimizu, Koichi; Igarashi, Koei; Takahashi, Nobuhiro

    To assess the inhibitory effects of nitrite on plaque acidogenicity and its relationship with caries experience. Plaque (2 μl) was collected from 76 children (age 5.8 ± 2.6 years, dmft 2.9 ± 3.5, DMTF 0.6 ± 1.4) and mixed with nitrite solution (final concentration = 0.63 mM) or distilled water (control). The initial pH (pH-0) of each sample was measured using a portable pH meter. The samples were incubated for 10 min, then their pH (pH-1) was measured again. Next, glucose (final concentration = 0.67%) was added to the samples, which were then incubated for a further 10 min before their pH was assessed for a third time (pH-2). The pH-0, pH-1, and pH-2 values of the control samples were 7.25 ± 0.16, 6.07 ± 0.44, and 5.11 ± 0.48, respectively, and those of the nitrite-treated samples were 7.26 ± 0.16, 6.37 ± 0.45, and 5.34 ± 0.48, respectively. The pH-1 and pH-2 values of the nitrite-treated samples were higher than those of the control samples (p plaque acid production was associated with stronger inhibition of plaque acid production by nitrite (p plaque acid production. Nitrite inhibited acid production more markedly in plaque that exhibited greater acid production, suggesting that nitrite might be effective at preventing caries, as it contributes to pH homeostasis in plaque by countering excess acidification.

  13. Inhibitory effects of regorafenib, a multiple tyrosine kinase inhibitor, on corneal neovascularization

    Directory of Open Access Journals (Sweden)

    Halil Ibrahim Onder

    2014-04-01

    Full Text Available AIM:To evaluate the inhibitory effects of regorafenib (BAY 73-4506, a multikinase inhibitor, on corneal neovascularization (NV.METHODS:Thirty adult male Sprague-Dawley rats weighing 250-300 g, were used. Corneal NV was induced by NaOH in the left eyes of each rat. Following the establishment of alkali burn, the animals were randomized into five groups according to topical treatment. Group 1 (n = 6 received 0.9% NaCl, Group 2 (n = 6 received dimethyl sulfoxide, Group 3 (n = 6 received regorafenib 1 mg/mL, Group 4 (n =6 received bevacizumab 5 mg/mL and Group 5 (n = 6 received 0.1% dexamethasone phosphate. On the 7d, the corneal surface covered with neovascular vessels was measured on photographs as the percentage of the cornea’s total area using computer-imaging analysis. The corneas obtained from rats were semiquantitatively evaluated for caspase-3 and vascular endothelial growth factor by immunostaining.RESULTS:A statistically significant difference in the percent area of corneal NV was found among the groups (P <0.001. Although the Group 5 had the smallest percent area of corneal NV, there was no difference among Groups 3, 4 and 5 (P >0.005. There was a statistically significant difference among the groups in apoptotic cell density (P = 0.002. The staining intensity of vascular endothelial growth factor in the epithelial and endothelial layers of cornea was significantly different among the groups (P <0.05. The staining intensity of epithelial and endothelial vascular endothelial growth factor was significantly weaker in Groups 3, 4 and 5 than in Groups 1 and 2.CONCLUSION: Topical administration of regorafenib 1 mg/mL is partly effective for preventing alkali-induced corneal NV in rats.

  14. Inhibitory Effect of β-Elemene on Human Airway Granulation Tissue in vivo and in vitro.

    Science.gov (United States)

    Hong, Lingling; Zeng, Yiming; Yang, Dongyong

    2016-01-01

    Recurrent airway granulation hyperplasia and scar formation make airway stenosis a clinical challenge. Therefore, a new approach for the treatment of airway stenosis is necessary. To explore the inhibitory effect of β-elemene on the proliferation of fibroblasts and airway granulation. In vivo: (1) study of the effect of local β-elemene injection by bronchoscopy. (2) During bronchoscopy, granulation tissues both before and after treatment were obtained. HE staining was performed and the result compared. In vitro: (1) human airway primary fibroblasts were purified and characterized. (2) Fibroblasts were treated with β-elemene and normal saline (NS) and then examined by optical and electron microscopy. (3) Fibroblasts treated with β-elemene or NS were assessed for viability by tetrazolium salt assay. (4) Apoptotic rates were determined by flow cytometry. In vivo: (1) after local injection of β- elemene, airway granulation tissue was reduced. (2) Granulation tissue was found to have less edema, and fibroblasts turned into mature fiber cells. In vitro: (1) human airway primary fibroblasts were successfully purified and cultured. (2) Compared with the control group, fibroblasts of the experimental group became clumped, the plasma granules were increased, and some fibroblasts lost their nucleus and organelles. (3) Compared with the control group, reduction of cell viability was detected with increased concentrations of β-elemene. (4) With increased concentrations of β-elemene, apoptotic rates of the fibroblasts were raised compared with the control group. β-Elemene may induce apoptosis and necrosis of airway primary fibroblasts and inhibit the proliferation of fibroblasts and airway granulation. The results provide a new approach for the treatment of airway stenosis. © 2016 S. Karger AG, Basel.

  15. Inhibitory effect of zinc oxide nanoparticles on pseudomonas aeruginosa biofilm formation

    Directory of Open Access Journals (Sweden)

    Mohammad Hassani Sangani

    2015-04-01

    Full Text Available Objective(s: Bacterial biofilm formation causes many persistent and chronic infections. The matrix protects biofilm bacteria from exposure to innate immune defenses and antibiotic treatments. The purpose of this study was to evaluate the biofilm formation of clinical isolates of Pseudomonas aeruginosa and the activity of zinc oxide nanoparticles (ZnO NPs on biofilm. Materials and Methods: After collecting bacteria from clinical samples of hospitalized patients, the ability of organisms were evaluated to create biofilm by tissue culture plate (TCP assay. ZnO NPs were synthesized by sol gel method and the efficacy of different concentrations (50- 350 µg/ml of ZnO NPs was assessed on biofilm formation and also elimination of pre-formed biofilm by using TCP method. Results:The average diameter of synthesized ZnO NPs was 20 nm. The minimum inhibitory concentration of nanoparticles was 150- 158 μg/ml and the minimum bactericidal concentration was higher (325 µg/ml. All 15 clinical isolates of P. aeruginosa were able to produce biofilm. Treating the organisms with nanoparticles at concentrations of 350 μg/ml resulted in more than 94% inhibition in OD reduction%. Molecular analysis showed that the presence of mRNA of pslA gene after treating bacteria with ZnO NPs for 30 minutes. Conclusion: The results showed that ZnO NPs can inhibit the establishment of P. aeruginosa biofilms and have less effective in removing pre-formed biofilm. However the tested nanoparticles exhibited anti-biofilm effect, but mRNA of pslA gene could be still detected in the medium by RT-PCR technique after 30 minutes treatment with ZnO.

  16. Inhibitory effect of tanshinone II A on TGF II-β1-induced cardiac fibrosis.

    Science.gov (United States)

    Zhou, Daixing; Li, Zhihui; Zhang, Liwei; Zhan, Chengye

    2012-12-01

    This study examined the effect of tanshinone II A (TSN II A) on the cardiac fibrosis induced by transforming growth factor β1 (TGF-β1) and the possible mechanisms. Cardiac fibroblasts were isolated from cardiac tissues of neonatal Sprague-Dawley (SD) rats by the trypsin digestion and differential adhesion method. The cells were treated with 5 ng/mL TGF-β1 alone or pretreated with TSN II A at different concentrations (10(-5) mol/L, 10(-4) mol/L). Immunocytochemistry was used for cell identification, RT-PCR for detection of the mRNA expression of connective tissue growth factor (CTGF) and collagen type I (COL I), Western blotting for detection of the protein expression of Smad7 and Smad3, and immunohistochemistry and immunofluorescence staining for detection of the protein expression of phosphorylated Smad3 (p-Smad3), CTGF and COLI. The results showed that TGF-β1 induced the expression of CTGF, COL I, p-Smad3 and Smad7 in a time-dependent manner. The mRNA expression of CTGF and COL I was significantly increased 24 h after TGF-β1 stimulation (PTSN A resulted in a decrease in the expression of p-Smad3, CTGF and COL I (PTSN II A as compared with that at 2 h post TGF-β1 stimulation (PTSN I IA; PTSN II A). It was concluded that TSN II A may exert an inhibitory effect on cardiac fibrosis by upregulating the expression of Smad7, suppressing the TGF-β1-induced phosphorylation of Smad3 and partially blocking the TGF-β1-Smads signaling pathway.

  17. Inhibitory Effect of Endostar on Specific Angiogenesis Induced by Human Hepatocellular Carcinoma

    Directory of Open Access Journals (Sweden)

    Qing Ye

    2015-01-01

    Full Text Available To investigate the effect of endostar on specific angiogenesis induced by human hepatocellular carcinoma, this research systematically elucidated the inhibitory effect on HepG2-induced angiogenesis by endostar from 50 ng/mL to 50000 ng/mL. We employed fluorescence quantitative Boyden chamber analysis, wound-healing assay, flow cytometry examination using a coculture system, quantitative analysis of tube formation, and in vivo Matrigel plug assay induced by HCC conditioned media (HCM and HepG2 compared with normal hepatocyte conditioned media (NCM and L02. Then, we found that endostar as a tumor angiogenesis inhibitor could potently inhibit human umbilical vein endothelial cell (HUVEC migration in response to HCM after four- to six-hour action, inhibit HCM-induced HUVEC migration to the lesion part in a dose-dependent manner between 50 ng/mL and 5000 ng/mL at 24 hours, and reduce HUVEC proliferation in a dose-dependent fashion. Endostar inhibited HepG2-induced tube formation of HUVECs which peaked at 50 ng/mL. In vivo Matrigel plug formation was also significantly reduced by endostar in HepG2 inducing system rather than in L02 inducing system. It could be concluded that, at cell level, endostar inhibited the angiogenesis-related biological behaviors of HUVEC in response to HCC, including migration, adhesion proliferation, and tube formation. At animal level, endostar inhibited the angiogenesis in response to HCC in Matrigel matrix.

  18. A simulated mucus layer protects Lactobacillus reuteri from the inhibitory effects of linoleic acid.

    Science.gov (United States)

    De Weirdt, R; Coenen, E; Vlaeminck, B; Fievez, V; Van den Abbeele, P; Van de Wiele, T

    2013-12-01

    Lactobacillus reuteri is a commensal, beneficial gut microbe that colonises the intestinal mucus layer, where it makes close contact with the human host and may significantly affect human health. Here, we investigated the capacity of linoleic acid (LA), the most common polyunsaturated fatty acid (PUFA) in a Western-style diet, to affect L. reuteri ATCC PTA 6475 prevalence and survival in a simulated mucus layer. Short-term (1 h) survival and mucin-agar adhesion assays of a log-phase L. reuteri suspension in intestinal water demonstrated that the simulated mucus layer protected L. reuteri against the inhibitory effects of LA by lowering its contact with the bacterial cell membrane. The protective effect of the simulated mucus layer was further evaluated using a more complex and dynamic model of the colon microbiota (SHIME®), in which L. reuteri survival was monitored during 6 days of daily exposure to LA in the absence (L-SHIME) and presence (M-SHIME) of a simulated mucus layer. After 6 days, luminal L- and M-SHIME L. reuteri plate counts had decreased by 3.1±0.5 and 2.6±0.9 log cfu/ml, respectively. Upon supplementation of 1.0 g/l LA, the decline in the luminal L. reuteri population started earlier than was observed for the control. In contrast, mucin-agar levels of L. reuteri (in the M-SHIME) remained unaffected throughout the experiment even in the presence of high concentrations of LA. Overall, the results of this study indicate the importance of the mucus layer as a protective environment for beneficial gut microbes to escape from stress by high loads of the antimicrobial PUFA LA to the colon, i.e. due to a Western-style diet.

  19. Inhibitory effects of Ponciri Fructus on testosterone-induced benign prostatic hyperplasia in rats.

    Science.gov (United States)

    Jeon, Woo-Young; Kim, Ohn Soon; Seo, Chang-Seob; Jin, Seong Eun; Kim, Jung-Ae; Shin, Hyeun-Kyoo; Kim, Yong-Ung; Lee, Mee-Young

    2017-08-03

    Benign prostatic hyperplasia (BPH) is non-cancerous condition of enlargement of the prostate, a common occurrence in older men. The immature fruits of Poncirus trifoliata (L.) Rafinesque (Rutaceae), Ponciri Fructus are widely used in traditional oriental medicine for the therapy of various diseases. However, little is known about the mechanism underlying the pathogenesis of BPH. In the present study, we investigated the protective effects of a Ponciri Fructus extract (PFE) on the development of BPH in a in a rat model of BPH induced by testosterone propionate (TP). Male Sprague Dawley rats were used as a model of BPH after its induction by daily subcutaneous injections of TP/corn oil, for a period of four weeks. PFE was administrated daily 1 h before TP/corn oil injection by oral gavage at a dose level of 200 mg/kg during the 4 weeks of TP/corn oil injections. All rats were sacrificed at the end of the experiment, we measured the relative prostate weight, the levels of testosterone and dihydrotestosterone (DHT), histological changes, activities of antioxidant enzymes (catalase, glutathione peroxidase, glutathione reductase, and superoxide dismutase), and expression of proliferating cell nuclear antigen (PCNA). In addition, we also measured the inhibition (%) of 5α-reductase in the prostatic tissue. Our findings indicate that PFE significantly inhibited the development of BPH; decreased the relative prostate weight, the level of testosterone and DHT in serum and prostatic tissue, prostatic hyperplasia, expression of PCNA, and increased the antioxidant enzymes. Moreover, PFE showed a weak inhibitory activity on 5α-reductase. These results suggest that PFE may be used as a therapeutic agent for BPH via antiproliferative and antioxidant effects.

  20. Antibacterial Inhibitory Effects of Punica Granatum Gel on Cariogenic Bacteria: An in vitro Study.

    Science.gov (United States)

    Millo, Grazielle; Juntavee, Apa; Ratanathongkam, Ariya; Nualkaew, Natsajee; Peerapattana, Jomjai; Chatchiwiwattana, Supaporn

    2017-01-01

    This study evaluated the in vitro antibacterial effects of the formulated Punica granatum (PG) gel against Streptococcus mutans, Streptococcus sanguinis, and Lactobacillus casei. The PG extract was dissolved in water at 500 mg/mL. High performance liquid chromatography (HPLC) was used for identification and quantification of chemical marker punicalagin. Minimum bactericidal concentration (MBC) and time-kill assay (TKA) were investigated. Antibacterial activities of the formulated PG gel, 2% chlorhexidine (CHX) gel and blank gel were tested by measuring the zones of inhibition through agar well diffusion method. The HPLC results showed presence of punicalagin at 2023.58 ± 25.29 pg/mL in the aqueous PG extract and at 0.234% (w/w) in the formulated PG gel. The MBC for S. mutans, S. Sanguinis, and L. casei were 250, 125, and 500 mg/mL respectively. The TKA of 500 mg/mL aqueous PG extract showed total inhibition of S. mutans, S. Sanguinis, and L. casei at 6, 1, and 24 hours contact time respectively. Agar well diffusion revealed that for S. mutans, CHX gel > PG gel > blank gel; for S. sanguinis, CHX gel = PG gel > blank gel; for L. casei, CHX gel > PG gel = blank gel. Comparison of the PG gel potency showed that S. sanguinis = S. mutans > L. casei. The PG gel equivalent to 0.234% punicalagin (w/w) inhibited S. mutans and S. sanguinis but not L. casei within 24 hours incubation period and has the potential to be used for caries prevention. Millo G, Juntavee A, Ratanathongkam A, Nualkaew N, Peerapattana J, Chatchiwiwattana S. Antibacterial Inhibitory Effects of Punica Granatum Gel on Cariogenic Bacteria: An in vitro Study. Int J Clin Pediatr Dent 2017;10(2):152-157.

  1. The effect of domestication on inhibitory control: wolves and dogs compared.

    Science.gov (United States)

    Marshall-Pescini, Sarah; Virányi, Zsófia; Range, Friederike

    2015-01-01

    Inhibitory control i.e. blocking an impulsive or prepotent response in favour of a more appropriate alternative, has been suggested to play an important role in cooperative behaviour. Interestingly, while dogs and wolves show a similar social organization, they differ in their intraspecific cooperation tendencies in that wolves rely more heavily on group coordination in regard to hunting and pup-rearing compared to dogs. Hence, based on the 'canine cooperation' hypothesis wolves should show better inhibitory control than dogs. On the other hand, through the domestication process, dogs may have been selected for cooperative tendencies towards humans and/or a less reactive temperament, which may in turn have affected their inhibitory control abilities. Hence, based on the latter hypothesis, we would expect dogs to show a higher performance in tasks requiring inhibitory control. To test the predictive value of these alternative hypotheses, in the current study two tasks; the 'cylinder task' and the 'detour task', which are designed to assess inhibitory control, were used to evaluate the performance of identically raised pack dogs and wolves. Results from the cylinder task showed a significantly poorer performance in wolves than identically-raised pack dogs (and showed that pack-dogs performed similarly to pet dogs with different training experiences), however contrary results emerged in the detour task, with wolves showing a shorter latency to success and less perseverative behaviour at the fence. Results are discussed in relation to previous studies using these paradigms and in terms of the validity of these two methods in assessing inhibitory control.

  2. The effect of domestication on inhibitory control: wolves and dogs compared.

    Directory of Open Access Journals (Sweden)

    Sarah Marshall-Pescini

    Full Text Available Inhibitory control i.e. blocking an impulsive or prepotent response in favour of a more appropriate alternative, has been suggested to play an important role in cooperative behaviour. Interestingly, while dogs and wolves show a similar social organization, they differ in their intraspecific cooperation tendencies in that wolves rely more heavily on group coordination in regard to hunting and pup-rearing compared to dogs. Hence, based on the 'canine cooperation' hypothesis wolves should show better inhibitory control than dogs. On the other hand, through the domestication process, dogs may have been selected for cooperative tendencies towards humans and/or a less reactive temperament, which may in turn have affected their inhibitory control abilities. Hence, based on the latter hypothesis, we would expect dogs to show a higher performance in tasks requiring inhibitory control. To test the predictive value of these alternative hypotheses, in the current study two tasks; the 'cylinder task' and the 'detour task', which are designed to assess inhibitory control, were used to evaluate the performance of identically raised pack dogs and wolves. Results from the cylinder task showed a significantly poorer performance in wolves than identically-raised pack dogs (and showed that pack-dogs performed similarly to pet dogs with different training experiences, however contrary results emerged in the detour task, with wolves showing a shorter latency to success and less perseverative behaviour at the fence. Results are discussed in relation to previous studies using these paradigms and in terms of the validity of these two methods in assessing inhibitory control.

  3. The Effect of Domestication on Inhibitory Control: Wolves and Dogs Compared

    Science.gov (United States)

    Marshall-Pescini, Sarah; Virányi, Zsófia; Range, Friederike

    2015-01-01

    Inhibitory control i.e. blocking an impulsive or prepotent response in favour of a more appropriate alternative, has been suggested to play an important role in cooperative behaviour. Interestingly, while dogs and wolves show a similar social organization, they differ in their intraspecific cooperation tendencies in that wolves rely more heavily on group coordination in regard to hunting and pup-rearing compared to dogs. Hence, based on the ‘canine cooperation’ hypothesis wolves should show better inhibitory control than dogs. On the other hand, through the domestication process, dogs may have been selected for cooperative tendencies towards humans and/or a less reactive temperament, which may in turn have affected their inhibitory control abilities. Hence, based on the latter hypothesis, we would expect dogs to show a higher performance in tasks requiring inhibitory control. To test the predictive value of these alternative hypotheses, in the current study two tasks; the ‘cylinder task’ and the ‘detour task’, which are designed to assess inhibitory control, were used to evaluate the performance of identically raised pack dogs and wolves. Results from the cylinder task showed a significantly poorer performance in wolves than identically-raised pack dogs (and showed that pack-dogs performed similarly to pet dogs with different training experiences), however contrary results emerged in the detour task, with wolves showing a shorter latency to success and less perseverative behaviour at the fence. Results are discussed in relation to previous studies using these paradigms and in terms of the validity of these two methods in assessing inhibitory control. PMID:25714840

  4. Inhibitory effect of gene combination in a mouse model of colon cancer with liver metastasis.

    Science.gov (United States)

    DU, Tong; Niu, Hongxin

    2014-09-01

    The aim of the present study was to establish an animal liver metastasis model with human colon cancer and investigate the inhibitory effect of the wild type (WT) p53 gene combined with thymidine kinase/ganciclovir (TK/GCV) and cytosine deaminase/5-fluorocytosine (CD/5-FC) systems on liver metastasis of colon cancer. A nude mouse liver metastasis model with human colon cancer was established via a spleen cultivation method. A total of 32 nude mice were randomly divided into four groups, each group with eight mice. Group 1 mice received splenic injections of SW480 cells (control group), while group 2 mice were injected with SW480/p53 cells in the spleen. Group 3 mice were administered splenic injections of SW480/TK-CD cells, and GCV and 5-FC were injected into the abdominal cavity. Finally, group 4 mice received splenic injections of SW480/p53 cells mixed in equal proportion with SW480/TK-CD cells, as well as GCV and 5-FC injections in the abdominal cavity. These cells described were constructed in our laboratory and other laboratories. The number of liver metastatic tumors, the liver metastasis rate, conventional pathology, electron microscopy and other indicators in the nude mice of each group were compared and observed. The nude mouse liver metastasis model with human colon cancer was successfully established; the liver metastasis rate of the control group was 100%. The results demonstrated that the rate of liver metastasis in the nude mice in each treatment group decreased, as well as the average number of liver metastatic tumors. Furthermore, the effect of the treatment group with genetic combination (group 4) was the most effective, demonstrating that WTp53 had a synergistic effect with TK/GCV and CD/5-FC. Therefore, the present study successfully established a mouse model of liver metastasis with colon cancer by injecting human colon cancer cells in the spleen. Combined gene therapy was shown to have a synergistic effect, which effectively inhibited the

  5. Inhibitory Effects ofPterodon emarginatusBean Oil and Extract onStaphylococcus aureus.

    Science.gov (United States)

    Mendes, V S; Sant'Anna, J B; Oliveira, S C C; Maldonade, Iriani Rodrigues; Machado, Eleuza Rodrigues

    2017-01-01

    that concentrations superior to 10% (v/v) using AC and 7.5% (v/v) using OE were necessary to eliminate colonies formedAccording to data of MIC, at 2.5% of AC and OE was enough to kill S. aureus The well diffusion technique demonstrated better performance than disc diffusion test for OE and AC extractsHydroalcoholic and oil extracts of sucupira beans had highest effect against Staphylococcus aureus Aqueous extract had no effect on bacterial growth in all microbial methods testedThe sucupira-based extracts is a promising source as herbal drug due to therapeutic value Abbreviations Used: OE: Essencial oil; AC: Hydroalcoholic oil extract; AQ: Aqueous extracts; MIC: Minimum inhibitory concentration; MBC: Minimum bactericidal concentration; CFU: Colony formed unit.

  6. Microbial transformation of isosteviol and inhibitory effects on Epstein-Barr virus activation of the transformation products.

    Science.gov (United States)

    Akihisa, Toshihiro; Hamasaki, Yusuke; Tokuda, Harukuni; Ukiya, Motohiko; Kimura, Yumiko; Nishino, Hoyoku

    2004-03-01

    Microbial transformation of isosteviol (2), a beyerane-type diterpenoid obtained from stevioside (1) by acid hydrolysis, yielded 7beta-hydroxyisosteviol (3), 11beta-hydroxyisosteviol (5), and 12beta-hydroxyisosteviol (6) by the fungus Aspergillus niger, 17-hydroxyisosteviol (7) by the fungus Glomerella cingulata, and 3 and 7-oxoisosteviol (4) by the fungus Mortierella elongate. The five metabolites, 3-7, along with 1 and 2 were evaluated for their inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) activation induced by the tumor promoter 12-O-tetradecanoylphorbol-13-acetate (TPA) in Raji cells as a primary screening test for inhibitors of tumor promoters. All the diterpenes tested showed potent inhibitory effects, with the five metabolites 3-7 exhibiting more potent effects.

  7. Inhibitory Effect of Nasal Intermittent Positive Pressure Ventilation on Gastroesophageal Reflux.

    Directory of Open Access Journals (Sweden)

    Danny Cantin

    Full Text Available Non-invasive intermittent positive pressure ventilation can lead to esophageal insufflations and in turn to gastric distension. The fact that the latter induces transient relaxation of the lower esophageal sphincter implies that it may increase gastroesophageal refluxes. We previously reported that nasal Pressure Support Ventilation (nPSV, contrary to nasal Neurally-Adjusted Ventilatory Assist (nNAVA, triggers active inspiratory laryngeal closure. This suggests that esophageal insufflations are more frequent in nPSV than in nNAVA. The objectives of the present study were to test the hypotheses that: i gastroesophageal refluxes are increased during nPSV compared to both control condition and nNAVA; ii esophageal insufflations occur more frequently during nPSV than nNAVA. Polysomnographic recordings and esophageal multichannel intraluminal impedance pHmetry were performed in nine chronically instrumented newborn lambs to study gastroesophageal refluxes, esophageal insufflations, states of alertness, laryngeal closure and respiration. Recordings were repeated without sedation in control condition, nPSV (15/4 cmH2O and nNAVA (~ 15/4 cmH2O. The number of gastroesophageal refluxes recorded over six hours, expressed as median (interquartile range, decreased during both nPSV (1 (0, 3 and nNAVA [1 (0, 3] compared to control condition (5 (3, 10, (p < 0.05. Meanwhile, the esophageal insufflation index did not differ between nPSV (40 (11, 61 h-1 and nNAVA (10 (9, 56 h-1 (p = 0.8. In conclusion, nPSV and nNAVA similarly inhibit gastroesophageal refluxes in healthy newborn lambs at pressures that do not lead to gastric distension. In addition, the occurrence of esophageal insufflations is not significantly different between nPSV and nNAVA. The strong inhibitory effect of nIPPV on gastroesophageal refluxes appears identical to that reported with nasal continuous positive airway pressure.

  8. The Effects of Excitatory and Inhibitory Social Cues on Cocaine-Seeking Behavior

    Directory of Open Access Journals (Sweden)

    Mark Andrew Smith

    2016-11-01

    Full Text Available Social partners influence the likelihood of using drugs, developing a substance use disorder, and relapse to drug use after a period of abstinence. Preclinical studies report that social cues influence the acquisition of cocaine use, the escalation of cocaine use over time, and the compulsive patterns of cocaine use that emerge during an extended binge. The purpose of this study was to examine the effects of social cues on the reinstatement of cocaine-seeking behavior after a period of abstinence. Male rats were obtained at weaning, assigned to triads (3 rats/cage, reared to adulthood, and implanted with intravenous catheters. Rats from each triad were then assigned to one of three conditions: (1 test rats were trained to self-administer cocaine and were tested for reinstatement, (2 cocaine partners were trained to self-administer cocaine and were predictive of response-contingent cocaine delivery, and (3 abstinent partners were not given access to cocaine and were predictive of extinction. Test rats alternated social partners every 5 days for 20 days such that responding was reinforced with cocaine in the presence of the cocaine partner (S+ for 10 days and not reinforced with cocaine in the presence of the abstinent partner (S- for 10 days. Responding of the test rats was then extinguished over 7 days under isolated conditions. Tests of reinstatement were then conducted in the presence of the cocaine partner and abstinent partner under extinction conditions. Neither social partner reinstated responding relative to that observed on the final day of extinction; however, responding was greater in the presence of the cocaine partner (S+ than the abstinent partner (S- during the reinstatement test. These data fail to demonstrate that a social partner reinstates cocaine-seeking behavior after a period of abstinence, but they do indicate that social partners can serve as either excitatory or inhibitory discriminative stimuli to influence drug

  9. No evidence for true training and transfer effects after inhibitory control training in young healthy adults.

    Science.gov (United States)

    Enge, Sören; Behnke, Alexander; Fleischhauer, Monika; Küttler, Lena; Kliegel, Matthias; Strobel, Alexander

    2014-07-01

    Recent studies reported that training of working memory may improve performance in the trained function and beyond. Other executive functions, however, have been rarely or not yet systematically examined. The aim of this study was to test the effectiveness of inhibitory control (IC) training to produce true training-related function improvements in a sample of 122 healthy adults using a randomized, double-blind pretest/posttest/follow-up design. Two groups performed either adaptive (training group) or nonadaptive (active control) versions of go/no-go and stop-signal tasks for 3 weeks. Training gains as well as near-transfer to an untrained Stroop task and far-transfer to psychometric fluid intelligence were explored. Although the adaptive group could substantially improve overall IC task performance after training, no differences to the active control group occurred, neither at posttest nor at follow-up testing. A large decrease in response latency from pre- to posttest (and from pretest to 4 months' follow-up testing) was found when the training group was compared to the passive control group, which, however, does not sufficiently control for possible confounds. Thus, no conclusive evidence was found that this performance increase mirrors a true increase in IC function. The fact that training improvement was mainly related to response latency may indicate that individuals were more focused on performance gains in the prepotent go trials but less on the stop trials to meet the requirements of the tasks as well as possible. The challenges for response inhibition training studies are extensively discussed. PsycINFO Database Record (c) 2014 APA, all rights reserved.

  10. Inhibitory effects of Tripterygium wilfordii multiglycoside on benign prostatic hyperplasia in rats.

    Science.gov (United States)

    Shen, Hai-Nan; Xu, Yuan; Jiang, Zhen-Zhou; Huang, Xin; Zhang, Lu-Yong; Wang, Tao

    2015-06-01

    The present study was designed to evaluate the inhibitory effects of Tripterygium wilfordii multiglycoside (GTW) against testosterone-induced benign prostatic hyperplasia (BPH) in rats. A total of 45 rats were randomly divided into five groups: Group I, vehicle control group (sham-operated and treated with vehicle); Group II, BPH group; Group III, BPH rats treated with finasteride at a dose of 5 mg·kg(-1); and Groups IV and V, BPH rats treated with GTW at dose levels of 10 and 20 mg·kg(-1), respectively. The drugs were administered orally once a day for 14 days. Prostate weight, prostatic index, and the testosterone and dihydrotestosterone (DHT) levels in serum and prostate, and the serum prostate specific antigen (PSA) levels were measured; prostate tissues were taken for histopathological examination; and serum biochemical analysis was also performed. The BPH rats displayed an increase in prostate weight, prostatic index with increased testosterone and DHT levels in both the serum and prostate, and increased serum PSA levels. GTW treatment at both doses resulted in significant reductions in prostate weight, prostatic index, testosterone and DHT levels in both the serum and prostate, and serum PSA levels, compared with BPH group. Histopathological examination also indicated that GTW treatment at both doses inhibited testosterone-induced prostatic hyperplasia. Serum biochemical analysis showed that the liver and renal functions were normal. In conclusion, GTW inhibited testosterone-induced prostatic hyperplasia in rats, without host toxicity, providing a basis for the development of GTW as a novel therapy for BPH. Copyright © 2015 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.

  11. Effects of brainstem lesions on the masseter inhibitory reflex. Functional mechanisms of reflex pathways

    NARCIS (Netherlands)

    Ongerboer de Visser, B. W.; Cruccu, G.; Manfredi, M.; Koelman, J. H.

    1990-01-01

    The masseter inhibitory reflex (MIR) was investigated in 16 patients with localized brainstem lesions involving the trigeminal system. The MIR consists of two phases of EMG silence (S1 and S2) evoked by stimulation of the mental nerve during maximal clenching of the teeth. The extent of the lesions

  12. Inhibitory effect of hexane fraction from Myagropsis myagroides on pancreatic α-amylase in vitro.

    Science.gov (United States)

    Pak, Won-Min; Kim, Koth-Bong-Woo Ri; Kim, Min-Ji; Cho, Ji-Young; Ahn, Dong-Hyun

    2015-03-01

    A Myagropsis myagroides (Mm) methanol extract showed α-amylase inhibitory activity of 13% at a concentration of 5 mg/ml. Results showed that the hexane fraction from the Mm methanol extract exhibited α-amylase inhibitory activity with an IC50 value of 4.24 mg/ml. The hexane fraction was separated using silica-gel column chromatography, and six subfractions were obtained. The fraction eluted with CHCl3:MeOH = 50:1 showed the highest α-amylase inhibitory activity with an IC50 value of 0.72 mg/ml. This fraction was purified using Sephadex LH-20 column chromatography and an octadecyl silica (ODS) Sepak cartridge, obtaining seven subfractions. Fraction (Fr.) 4 also showed a strong α-amylase inhibitory activity with an IC50 value of 0.75 mg/ml. Fr. 4 was purified by Sephadex LH-20 column chromatography and ODS Sepak cartridge, obtaining six subfractions. Fr. 4-2 was identified as sargachromanol I with an IC50 value of 0.40 mg/ml, and the inhibition pattern analyzed from Lineweaver-Burk plots revealed it to be an uncompetitive inhibitor. These results suggest that Mm has potential as a natural antidiabetes agent.

  13. [Inhibitory effect on Microcystis aeruginosa as well as separation and identification of the allelochemicals of welsh onion].

    Science.gov (United States)

    Zhou, Yang; Li, Yuan; Li, Cheng; Liu, Lu; Zhang, Tingting

    2013-11-01

    To study the inhibition of welsh onion on Microcystis aeruginosa, and separat and identify of the allelochemicals from welsh onion. METHEDS: The inhibitory effect of different concentrations of fistular onion stalk and fistular onion leaf water extracts on M. aeruginosa were studied; besides, separation and identification of the allelochemicals of welsh onion were also studied. Both fistular onion stalk and fistular onion leaf water extracts had, to different degree, inhibitory effect on the growth of M. aeruginosat. Compared with the control group, the fluorescence intensity of fistular onion stalk and fistular onion leaf were lower than the control group in the same period, and the inhibitory effect were more obvious with the increase of the water extract concentrations, to the fifth day, M. aeruginosa almost completely dead of the highest concentration(50 ml/L) of fistular onion stalk water extract treated group, the EC50 of water extract from fistular onion stalk to M. aeruginosa was 12.7 ml/L, equivalent to fresh weight 1.27 g/L. Main allelochemicals in fistular onion stalk includes allyl mercaptan, cyclopentyl mercaptan, and so on. The inhibiting assay on M. aeruginosa showed that the EC50 of allyl mercaptan and cyclopentyl mercaptan respectively were 0.03 and 0.02 g/L. The fistular onion stalk water extracts has very good algicidal effect, allelopathic algal inhibiting substances primarily are sulfocompound, which have the potential to develop into biological algicide.

  14. Inhibitory effects of phenolic compounds of rice straw formed by saccharification during ethanol fermentation by Pichia stipitis.

    Science.gov (United States)

    Wang, Xiahui; Tsang, Yiu Fai; Li, Yuhao; Ma, Xiubing; Cui, Shouqing; Zhang, Tian-Ao; Hu, Jiajun; Gao, Min-Tian

    2017-11-01

    In this study, it was found that the type of phenolic acids derived from rice straw was the major factor affecting ethanol fermentation by Pichia stipitis. The aim of this study was to investigate the inhibitory effect of phenolic acids on ethanol fermentation with rice straw. Different cellulases produced different ratios of free phenolic acids to soluble conjugated phenolic acids, resulting in different fermentation efficiencies. Free phenolic acids exhibited much higher inhibitory effect than conjugated phenolic acids. The flow cytometry results indicated that the damage to cell membranes was the primary mechanism of inhibition of ethanol fermentation by phenolic acids. The removal of free phenolic acids from the hydrolysates increased ethanol productivity by 2.0-fold, indicating that the free phenolic acids would be the major inhibitors formed during saccharification. The integrated process for ethanol and phenolic acids may constitute a new strategy for the production of low-cost ethanol. Copyright © 2017 Elsevier Ltd. All rights reserved.

  15. Comparative study of the inhibitory effects of wine polyphenols on the growth of enological lactic acid bacteria.

    Science.gov (United States)

    García-Ruiz, Almudena; Moreno-Arribas, M Victoria; Martín-Álvarez, Pedro J; Bartolomé, Begoña

    2011-02-28

    This paper reports a comparative study of the inhibitory potential of 18 phenolic compounds, including hydroxybenzoic acids and their derivatives, hydroxycinnamic acids, phenolic alcohols and other related compounds, stilbenes, flavan-3-ols and flavonols, on different lactic acid bacteria (LAB) strains of the species Oenococcus oeni, Lactobacillus hilgardii and Pediococcus pentosaceus isolated from wine. In general, flavonols and stilbenes showed the greatest inhibitory effects (lowest IC₅₀ values) on the growth of the strains tested (0.160-0.854 for flavonols and 0.307-0.855 g/L for stilbenes). Hydroxycinnamic acids (IC₅₀ > 0.470 g/L) and hydroxybenzoic acids and esters (IC₅₀ >1 g/L) exhibited medium inhibitory effect, and phenolic alcohols (IC₅₀ > 2 g/L) and flavanol-3-ols (negligible effect) showed the lowest effect on the growth of the LAB strains studied. In comparison to the antimicrobial additives used in winemaking, IC₅₀ values of most phenolic compounds were higher than those of potassium metabisulphite for O. oeni strains (e.g., around 4-fold higher for quercetin than for potassium metabisulphite), but lower for L. hilgardii and P. pentosaceus strains (e.g., around 2-fold lower for quercetin). Lysozyme IC₅₀ values were negligible for L. hilgardii and P. pentosaceus, and were higher than those corresponding to most of the phenolic compounds tested for O. oeni strains, indicating that lysozyme was less toxic for LAB than the phenolic compounds in wine. Scanning electron microscopy confirmed damage of the cell membrane integrity as a consequence of the incubation with antimicrobial agents. These results contribute to the understanding of the inhibitory action of wine phenolics on the progress of malolactic fermentation, and also to the development of new alternatives to the use of sulphites in enology. Copyright © 2011 Elsevier B.V. All rights reserved.

  16. Structure of constituents isolated from the flower buds of Cananga odorata and their inhibitory effects on aldose reductase.

    Science.gov (United States)

    Matsumoto, Takahiro; Nakamura, Seikou; Fujimoto, Katsuyoshi; Ohta, Tomoe; Ogawa, Keiko; Yoshikawa, Masayuki; Matsuda, Hisashi

    2014-10-01

    Three new terpenoid derivatives, canangaterpenes IV-VI, were isolated from the flower buds of Cananga odorata, cultivated in Thailand, together with eight known flavonoids. The chemical structures of the new compounds were elucidated on the basis of chemical and physicochemical evidence. The inhibitory effects of the isolated compounds on aldose reductase were also investigated. Several terpenoid derivatives and flavonoids were shown to inhibit aldose reductase.

  17. Inhibitory effect of Zataria multiflora Boiss. essential oil, alone and in combination with monolaurin, on Listeria monocytogenes

    OpenAIRE

    Raeisi, Mojtaba; Tajik, Hossein; Razavi Rohani, Seyed Mehdi; Tepe, Bektas; Kiani, Hossein; Khoshbakht, Rahem; Shirzad Aski, Hesamaddin; Tadrisi, Hamed

    2016-01-01

    Listeria monocytogenes is one of the major causes of infections in developing countries. In this study, chemical composition and anti-listerial effect of the essential oil of Zataria multiflora Boiss. alone and in combination with monolaurin were evaluated at different pH values (5, 6, and 7) and temperatures (5 ?C and 30 ?C). Chemical composition of Zataria multiflora Boiss. essential oil was evaluated by gas chromatography-mass spectrometry (GC-MS) analysis. Minimum inhibitory concentration...

  18. New 5-deoxyflavonoids and their inhibitory effects on protein tyrosine phosphatase 1B (PTP1B) activity

    DEFF Research Database (Denmark)

    Nguyen, Phi Hung; Dao, Trong Tuan; Kim, Jayeon

    2011-01-01

    , MS, CD, 1D- and 2D-NMR) and physicochemical analyses. All isolates exhibited moderate inhibitory effects on the enzyme assay with IC₅₀ values ranging from 14.9 ± 1.6 to 98.1 ± 11.3 μM. Compounds with prenyl and methoxy groups in the B ring (1, 2, 4, 8, and 13) possessed strong activity (IC(50) 14...

  19. α-Glucosidase and pancreatic lipase inhibitory activities and glucose uptake stimulatory effect of phenolic compounds from Dendrobium formosum

    Directory of Open Access Journals (Sweden)

    Prachyaporn Inthongkaew

    Full Text Available ABSTRACT A methanol extract from the whole plant of Dendrobium formosum Roxb. ex Lindl., Orchidaceae, showed inhibitory potential against α-glucosidase and pancreatic lipase enzymes. Chromatographic separation of the extract resulted in the isolation of twelve phenolic compounds. The structures of these compounds were determined through analysis of NMR and HR-ESI-MS data. All of the isolates were evaluated for their α-glucosidase and pancreatic lipase inhibitory activities, as well as glucose uptake stimulatory effect. Among the isolates, 5-methoxy-7-hydroxy-9,10-dihydro-1,4-phenanthrenequinone (12 showed the highest α-glucosidase and pancreatic lipase inhibitory effects with an IC50 values of 126.88 ± 0.66 µM and 69.45 ± 10.14 µM, respectively. An enzyme kinetics study was conducted by the Lineweaver-Burk plot method. The kinetics studies revealed that compound 12 was a non-competitive inhibitor of α-glucosidase and pancreatic lipase enzymes. Moreover, lusianthridin at 1 and 10 µg/ml and moscatilin at 100 µg/ml showed glucose uptake stimulatory effect without toxicity on L6 myotubes. This study is the first report on the phytochemical constituents and anti-diabetic and anti-obesity activities of D. formosum.

  20. [Inhibitory Effect of Decitabine on Proliferation of MDS-L Cells and Its Mechanism].

    Science.gov (United States)

    Wu, Dong; Zhang, Yao; Zhao, You-Shan; Guo, Juan; Chang, Chun-Kang

    2017-10-01

    To investigate the inhibitory effect of decitabine (DAC) in various dosages on the proliferention of MDS-RAEB cell line MDS-L and its mechanism. LC-MS/MS method was used to test the blood DAC concentration of 2 groups of MDS patients being treated with DAC 20 and 15 mg/m 2 ×5 d. In according to the various blood DAC concentration levels, the MDS-L cells were treated with different DAC dosages for 24, 48, 72 and 96 h, respectively. The CCK-8 method was applied to determine the cell proliferation, the flow cytometry was used to analyze the cell cycle and cell apoptosis changes, the P15 INK4B DNA methylation status was measured by methylation specific PCR using EZ DNA Methylation-Gold Kit. The blood DAC concentration of MDS patients treated with DAC 20 mg/m 2 ×5 d was 174.08±80.15(84.7-311) ng/ml, which was significantly higher than 89.87±32.94(43.2-165)ng/ml for the group treated with 15 mg/m 2 ×5 d (P=0.014). DAC could notably inhibit the proliferation of MDS-L cells, and the effect was in dose- and- time-dependent manner(r=0.786). However, when DAC concentration was ≥0.1 µg/ml, the proliferation inhibition rates were not significantly different between various dosages. After DAC treatment, MDS-L cells in G 1 phase increased notably, while cells in S phase decreased significantly. Also, the P15 INK4B DNA methylation status of MDS-L cells decreased after being treated with DAC for 96 h, but the difference was not significant between various dosages. DAC can significantly suppress MDS-L cell proliferation, block MDS-L cells in G 1 phase and induce the apoptosis at low concentration (0.1-0.2 µg/ml).

  1. The Philippine tobacco industry: "the strongest tobacco lobby in Asia"

    Science.gov (United States)

    Alechnowicz, K; Chapman, S

    2004-01-01

    Objective: To highlight revelations from internal tobacco industry documents about the conduct of the industry in the Philippines since the 1960s. Areas explored include political corruption, health, employment of consultants, resisting pack labelling, and marketing and advertising. Methods: Systematic keyword Minnesota depository website searches of tobacco industry internal documents made available through the Master Settlement Agreement. Results: The Philippines has long suffered a reputation for political corruption where collusion between state and business was based on the exchange of political donations for favourable economic policies. The tobacco industry was able to limit the effectiveness of proposed anti-tobacco legislation. A prominent scientist publicly repudiated links between active and passive smoking and disease. The placement of health warning labels was negotiated to benefit the industry, and the commercial environment allowed it to capitalise on their marketing freedoms to the fullest potential. Women, children, youth, and the poor have been targeted. Conclusion: The politically laissez faire Philippines presented tobacco companies with an environment ripe for exploitation. The Philippines has seen some of the world's most extreme and controversial forms of tobacco promotion flourish. Against international standards of progress, the Philippines is among the world's slowest nations to take tobacco control seriously. PMID:15564224

  2. Blandford's argument: The strongest continuous gravitational wave signal

    International Nuclear Information System (INIS)

    Knispel, Benjamin; Allen, Bruce

    2008-01-01

    For a uniform population of neutron stars whose spin-down is dominated by the emission of gravitational radiation, an old argument of Blandford states that the expected gravitational-wave amplitude of the nearest source is independent of the deformation and rotation frequency of the objects. Recent work has improved and extended this argument to set upper limits on the expected amplitude from neutron stars that also emit electromagnetic radiation. We restate these arguments in a more general framework, and simulate the evolution of such a population of stars in the gravitational potential of our galaxy. The simulations allow us to test the assumptions of Blandford's argument on a realistic model of our galaxy. We show that the two key assumptions of the argument (two dimensionality of the spatial distribution and a steady-state frequency distribution) are in general not fulfilled. The effective scaling dimension D of the spatial distribution of neutron stars is significantly larger than two, and for frequencies detectable by terrestrial instruments the frequency distribution is not in a steady state unless the ellipticity is unrealistically large. Thus, in the cases of most interest, the maximum expected gravitational-wave amplitude does have a strong dependence on the deformation and rotation frequency of the population. The results strengthen the previous upper limits on the expected gravitational-wave amplitude from neutron stars by a factor of 6 for realistic values of ellipticity.

  3. The Philippine tobacco industry: "the strongest tobacco lobby in Asia".

    Science.gov (United States)

    Alechnowicz, K; Chapman, S

    2004-12-01

    To highlight revelations from internal tobacco industry documents about the conduct of the industry in the Philippines since the 1960s. Areas explored include political corruption, health, employment of consultants, resisting pack labelling, and marketing and advertising. Systematic keyword Minnesota depository website searches of tobacco industry internal documents made available through the Master Settlement Agreement. The Philippines has long suffered a reputation for political corruption where collusion between state and business was based on the exchange of political donations for favourable economic policies. The tobacco industry was able to limit the effectiveness of proposed anti-tobacco legislation. A prominent scientist publicly repudiated links between active and passive smoking and disease. The placement of health warning labels was negotiated to benefit the industry, and the commercial environment allowed it to capitalise on their marketing freedoms to the fullest potential. Women, children, youth, and the poor have been targeted. The politically laissez faire Philippines presented tobacco companies with an environment ripe for exploitation. The Philippines has seen some of the world's most extreme and controversial forms of tobacco promotion flourish. Against international standards of progress, the Philippines is among the world's slowest nations to take tobacco control seriously.

  4. Four new compounds from the roots of Euphorbia ebracteolata and their inhibitory effect on LPS-induced NO production.

    Science.gov (United States)

    Bai, Jiao; Huang, Xue-Yan; Liu, Zhi-Guo; Gong, Chi; Li, Xin-Yu; Li, Da-Hong; Hua, Hui-Ming; Li, Zhan-Lin

    2018-03-01

    Three new diterpenoids, ebractenoids O~Q (1-3), and a new phenolic glucoside, γ-pyrone-3-O-β-d-(6-galloyl)-glucopyranoside (4), together with 6 known compounds, were isolated from the 95% ethanol extract of the roots of Euphorbia ebracteolata, and their structures were elucidated on the basis of spectroscopic data. The absolute configurations of 1-3 were determined by electronic circular dichroism (ECD) calculations. The inhibitory effects of all the isolates with exception of compounds 8 and 10 on the NO production in lipopolysaccharide (LPS)-induced macrophages were evaluated. All of them exhibited significant inhibitory activity. Copyright © 2017 Elsevier B.V. All rights reserved.

  5. Selective LXRα inhibitory effects observed in plant extracts of MEH184 (Parthenocissua tricuspidata) and MEH185 (Euscaphis japonica)

    International Nuclear Information System (INIS)

    Kim, Kang Ho; Choi, Seung Hyun; Lee, Thomas S.; Oh, Won Keun; Kim, Dong Sun; Kim, Jae Bum

    2006-01-01

    Liver X receptors (LXRs) are nuclear hormone receptors that behave as lipid sensors of cellular cholesterol and fatty acid. Although LXR activation can alleviate hypercholesterolemia by inducing cholesterol efflux, it also results in undesirable effects of fatty acid synthesis, resulting in hepatic steatosis and hyperlipidemia. Therefore, it is critical to identify LXRα inhibitory agents that would repress fatty acid synthesis and hepatic lipid accumulation. In current study, screening of plant extracts used for traditional oriental medicine resulted in the identification of two candidates demonstrating selective LXRα inhibitory activity. These were whole leaf methanol extracts of Parthenocissua tricuspidata (MEH184) and Euscaphis japonica (MEH185). Both MEH184 and MEH185 decreased transcriptional activity of LXRα and the expression of LXRα target genes, such as FAS and ADD1/SREBP1c. Additionally, MEH184 and MEH184 significantly reduced lipogenesis and adipocyte differentiation. Together, the data imply that MEH184 and MEH185 possess selective antagonistic properties on LXRα to downregulate lipogenesis

  6. Effects of vigorous walking exercise on core body temperature and inhibitory control in thermosensitive persons with multiple sclerosis.

    Science.gov (United States)

    Sandroff, Brian M; Motl, Robert W; Davis, Scott L

    2016-01-01

    Acute, moderate intensity aerobic exercise might improve cognition in multiple sclerosis (MS), but it is unknown if increases in core body temperature (Ctemp) that negates those effects in thermosensitive persons with MS. Fourteen fully ambulatory, thermosensitive persons with MS completed 20-min bouts of vigorous intensity treadmill walking exercise and seated quiet rest in a randomized, counterbalanced order. Ctemp was measured throughout each experimental condition. Inhibitory control (i.e., an executive function) was measured immediately prior to and following each condition. Ctemp was elevated (~0.6 °C) with vigorous exercise versus quiet rest (p control for vigorous exercise versus quiet rest (ηp(2) = 0.29). Exercise-related increases in Ctemp do not nullify the potential acute exercise benefits on inhibitory control in MS.

  7. Phytochemical screening of Nepeta cataria extracts and their in vitro inhibitory effects on free radicals and carbohydrate-metabolising enzymes.

    Science.gov (United States)

    Naguib, Abdel Moneam Mohamed; Ebrahim, Mohamed Elsayed; Aly, Hanan Farouk; Metawaa, Hemaia Mohamed; Mahmoud, Ahlam Hosni; Mahmoud, Ebtissam A; Ebrahim, Faten Mohamed

    2012-01-01

    This research was performed to investigate in vitro the biological activities of successive as well as 70% ethanol extracts of Nepeta cataria on some biochemical parameters including oxidative markers and carbohydrate-hydrolysing enzyme activities (α-amylase, β-galactosidase and α-glucosidase). Powdered N. cataria and its successive extracts were screened for their phytochemical constituents. Tests for tannins, carbohydrates, glycosides and flavonoids were positive in ethanolic extract, but those for steroids and terpenoids were positive in petroleum ether and chloroform extracts. Also, different extracts were chromatographically investigated. The results obtained demonstrated that different successive extracts of N. cataria exhibited an inhibitory effect on oxidative stress indices and carbohydrate-hydrolysing enzymes. It is observed that 70% ethanol, petroleum ether and chloroform extracts showed, respectively, the most potent inhibitory activities, while ethyl acetate and ethanol successive extracts appeared with moderate or low reducing activities.

  8. Inhibitory Effects of Pterodon emarginatus Bean Oil and Extract on Staphylococcus aureus

    Science.gov (United States)

    Mendes, V. S.; Sant'Anna, J. B.; Oliveira, S. C. C.; Maldonade, Iriani Rodrigues; Machado, Eleuza Rodrigues

    2017-01-01

    diffusion and microdilution) was evaluated on reducing CFUThe results showed by MBC that concentrations superior to 10% (v/v) using AC and 7.5% (v/v) using OE were necessary to eliminate colonies formedAccording to data of MIC, at 2.5% of AC and OE was enough to kill S. aureusThe well diffusion technique demonstrated better performance than disc diffusion test for OE and AC extractsHydroalcoholic and oil extracts of sucupira beans had highest effect against Staphylococcus aureusAqueous extract had no effect on bacterial growth in all microbial methods testedThe sucupira-based extracts is a promising source as herbal drug due to therapeutic value Abbreviations Used: OE: Essencial oil; AC: Hydroalcoholic oil extract; AQ: Aqueous extracts; MIC: Minimum inhibitory concentration; MBC: Minimum bactericidal concentration; CFU: Colony formed unit. PMID:29263627

  9. Inhibitory effect of Zataria multiflora Boiss. essential oil, alone and in combination with monolaurin, on Listeria monocytogenes.

    Science.gov (United States)

    Raeisi, Mojtaba; Tajik, Hossein; Razavi Rohani, Seyed Mehdi; Tepe, Bektas; Kiani, Hossein; Khoshbakht, Rahem; Shirzad Aski, Hesamaddin; Tadrisi, Hamed

    2016-01-01

    Listeria monocytogenes is one of the major causes of infections in developing countries. In this study, chemical composition and anti-listerial effect of the essential oil of Zataria multiflora Boiss. alone and in combination with monolaurin were evaluated at different pH values (5, 6, and 7) and temperatures (5 ˚C and 30 ˚C). Chemical composition of Zataria multiflora Boiss. essential oil was evaluated by gas chromatography-mass spectrometry (GC-MS) analysis. Minimum inhibitory concentration (MIC) of the essential oil and monolaurin were determined using microbroth dilution method and the interactions of essential oil and monolaurin were determined by the evaluation of fractional inhibitory concentrations (FIC) index. Carvacrol (63.20%) and thymol (15.10%) were found as the main components of the essential oil. The MIC values of the oil and monolaurin at pH 7 and 30 ˚C were measured as 312.50 µg mL(-1) and 125.00 µg mL(-1), respectively. Combination of monolaurin and Z. multiflora essential oil were found to act synergistically (FIC index essential oil. The lowest MIC value of monolaurin and essential oil was observed at pH 5 and 5 ˚C. According to our results, the oil alone or in combination with monolaurin at low pH and temperature conditions showed a promising inhibitory effect on L. monocytogenes.

  10. Inhibitory Effects of Physalis alkekengi L., Alcea rosea L., Bunium persicum B. Fedtsch. and Marrubium vulgare L. on Mushroom Tyrosinase.

    Science.gov (United States)

    Namjoyan, Foroogh; Jahangiri, Alireza; Azemi, Mohammad Ebrahim; Arkian, Elaheh; Mousavi, Hamideh

    2015-02-01

    The key enzyme in the process of melanin biosynthesis is tyrosinase. Skin hyperpigmentation and browning of foods are undesirable phenomena which tyrosinase represents. Therefore, tyrosinase inhibitors have been used increasingly for medicinal and cosmetic products. In this study, inhibitory effects of four plants including: physalis alkekengi L., Alcea rosea L., Bunium persicum B. Fedtsch. and Marrubium vulgare L. on diphenolase activity of mushroom tyrosinase were evaluated. The inhibitory activities of hydroalcoholic extracts of plants against oxidation of L-Dopa (as a substrate) by mushroom tyrosinase were investigated. The hydroalcoholic extract of P. alkekengi showed the most tyrosinase inhibitory effect with IC50 of 0.09 mg/mL vs. 0.38, 0.38 and 2.82 mg/mL of B. persicum, A. rosea and M. vulgare, respectively. M. vulgare exhibited uncompetitive inhibition and other plants showed mixed type inhibition on mushroom tyrosinase. All plants could inhibit mushroom tyrosinase, but more investigations on human tyrosinase and clinical studies are needed.

  11. Two New Monoterpene Glycosides from Qing Shan Lu Shui Tea with Inhibitory Effects on Leukocyte-Type 12-Lipoxygenase Activity

    Directory of Open Access Journals (Sweden)

    Ding Zhi Fang

    2013-04-01

    Full Text Available We evaluated the inhibitory effect of 12 Chinese teas on leukocyte-type 12-lipoxygenase (LOX activity. Tea catechins such as epigallocatechin gallate have been known to exhibit leukocyte-type 12-LOX inhibition. Qing Shan Lu Shui, which contains lower catechin levels than the other tested teas, suppressed leukocyte-type 12-LOX activity. To characterize the bioactive components of Qing Shan Lu Shui, leukocyte-type 12-LOX inhibitory activity–guided fractionation of the aqueous ethanol extract of the tea was performed, resulting in the isolation of two new monoterpene glycosides: liguroside A (1 and B (2. The structures of compounds 1 and 2 were characterized as (2E,5E-7-hydroperoxy-3,7-dimethyl-2,5-octadienyl-O-(α-L-rhamnopyranosyl-(1″→3′-(4′″-O-trans-p-coumaroyl-β-D-glucopyranoside and (2E,5E-7-hydroperoxy-3,7-dimethyl-2,5-octa-dienyl- O-(α-L-rhamnopyranosyl-(1″→3′-(4′″-O-cis-p-coumaroyl-β-D-glucopyranoside, respectively, based on spectral and chemical evidence. Ligurosides A (1 and B (2 showed inhibitory effects on leukocyte-type 12-LOX activity, with IC50 values of 1.7 and 0.7 μM, respectively.

  12. Inhibitory effects of edible seaweeds, polyphenolics and alginates on the activities of porcine pancreatic α-amylase

    DEFF Research Database (Denmark)

    Zaharudin, Nazikussabah Binti; Asunción Salmeán, Armando; Dragsted, Lars Ove

    2018-01-01

    Edible seaweeds are valuable because of their organoleptic properties and complex polysaccharide content. A study was conducted to investigate the potential of dried edible seaweed extracts, its potential phenolic compounds and alginates for α-amylase inhibitory effects. The kinetics of inhibitio...... information that crude extracts of brown edible seaweeds, phenolic compounds and alginates are potent α-amylase inhibitors, thereby potentially retarding glucose liberation from starches and alleviation of postprandial hyperglycaemia.......Edible seaweeds are valuable because of their organoleptic properties and complex polysaccharide content. A study was conducted to investigate the potential of dried edible seaweed extracts, its potential phenolic compounds and alginates for α-amylase inhibitory effects. The kinetics of inhibition...... was assessed in comparison with acarbose. The methanol extract of Laminaria digitata and the acetone extract of Undaria pinnatifida showed inhibitory activity against α-amylase, IC50 0.74 ± 0.02 mg/ml and 0.81 ± 0.03 mg/ml, respectively; both showed mixed-type inhibition. Phenolic compound, 2...

  13. Empirical prediction and validation of antibacterial inhibitory effects of various plant essential oils on common pathogenic bacteria.

    Science.gov (United States)

    Akdemir Evrendilek, Gulsun

    2015-06-02

    In this study, fractional compound composition, antioxidant capacity, and phenolic substance content of 14 plant essential oils-anise (Pimpinella anisum), bay leaves (Laurus nobilis), cinnamon bark (Cinnamomum verum), clove (Eugenia caryophyllata), fennel (Foeniculum vulgare), hop (Humulus lupulus), Istanbul oregano (Origanum vulgare subsp. hirtum), Izmir oregano (Origanum onites), mint (Mentha piperita), myrtus (Myrtus communis), orange peel (Citrus sinensis), sage (Salvia officinalis), thyme (Thymbra spicata), and Turkish oregano (Origanum minutiflorum)--were related to inhibition of 10 bacteria through multiple linear or non-linear (M(N)LR) models-four Gram-positive bacteria of Listeria innocua, coagulase-negative staphylococci, Staphylococcus aureus, and Bacillus subtilis, and six Gram-negative bacteria of Yersinia enterocolitica, Salmonella Enteritidis, Salmonella Typhimurium, Proteus mirabilis, Escherichia coli O157:H7, and Klebsiella oxytoca. A total of 65 compounds with different antioxidant capacity, phenolic substance content and antibacterial properties were detected with 14 plant essential oils. The best-fit M(N)LR models indicated that relative to anise essential oil, the essential oils of oreganos, cinnamon, and thyme had consistently high inhibitory effects, while orange peel essential oil had consistently a low inhibitory effect. Regression analysis indicated that beta-bisabolene (Turkish and Istanbul oreganos), and terpinolene (thyme) were found to be the most inhibitory compounds regardless of the bacteria type tested. Copyright © 2015 Elsevier B.V. All rights reserved.

  14. Inhibitory Effect of Arctigenin from Fructus Arctii Extract on Melanin Synthesis via Repression of Tyrosinase Expression

    OpenAIRE

    Park, Hwayong; Song, Kwang Hoon; Jung, Pil Mun; Kim, Ji-Eun; Ro, Hyunju; Kim, Mi Yoon; Ma, Jin Yeul

    2013-01-01

    To identify the active compound arctigenin in Fructus Arctii (dried seed of medicinal plant Arctium lappa) and to elucidate the inhibitory mechanism in melanogenesis, we analyzed melanin content and tyrosinase activity on B16BL6 murine melanoma and melan-A cell cultures. Water extracts of Fructus Arctii were shown to inhibit tyrosinase activity in vitro and melanin content in ? -melanocyte stimulating hormone-stimulated cells to similar levels as the well-known kojic acid and arbutin, respect...

  15. Inhibitory control effects in adolescent binge eating and consumption of sugar-sweetened beverages and snacks

    OpenAIRE

    Ames, Susan L.; Kisbu-Sakarya, Yasemin; Reynolds, Kim D.; Boyle, Sarah; Cappelli, Christopher; Cox, Matthew G.; Dust, Mark; Grenard, Jerry L.; Mackinnon, David P.; Stacy, Alan W.

    2014-01-01

    Inhibitory control and sensitivity to reward are relevant to the food choices individuals make frequently. An imbalance of these systems can lead to deficits in decision-making that are relevant to food ingestion. This study evaluated the relationship between dietary behaviors – binge eating and consumption of sweetened beverages and snacks - and behavioral control processes, among 198 ethnically diverse adolescents, ranging in age from 14 to 17, in Southern California. Neurocognitive control...

  16. Effects of reward and punishment on brain activations associated with inhibitory control in cigarette smokers.

    Science.gov (United States)

    Luijten, Maartje; O'Connor, David A; Rossiter, Sarah; Franken, Ingmar H A; Hester, Robert

    2013-11-01

    Susceptibility to use of addictive substances may result, in part, from a greater preference for an immediate small reward relative to a larger delayed reward or relative insensitivity to punishment. This functional magnetic resonance imaging (fMRI) study examined the neural basis of inhibiting an immediately rewarding stimulus to obtain a larger delayed reward in smokers. We also investigated whether punishment could modulate inhibitory control. The Monetary Incentive Go/NoGo (MI-Go/NoGo) task was administered that provided three types of reward outcomes contingent upon inhibitory control performance over rewarding stimuli: inhibition failure was either followed by no monetary reward (neutral condition), a small monetary reward with immediate feedback (reward condition) or immediate monetary punishment (punishment condition). In the reward and punishment conditions, successful inhibitory control resulted in larger delayed rewards. Community sample of smokers in the Melbourne (Australia) area. Nineteen smokers were compared with 17 demographically matched non-smoking controls. Accuracy, reaction times and brain activation associated with the MI-Go/NoGo task. Smokers showed hyperactivation in the right insula (P punishment condition in the right insula and dorsolateral prefrontal cortex, most probably as a result of increased activation in non-smoking controls. Compared with non-smokers, smokers showed increased neural activation when resisting immediately rewarding stimuli and may be less sensitive to punishment as a strategy to increase control over rewarding stimuli. © 2013 Society for the Study of Addiction.

  17. Tactile Ranschburg effects: facilitation and inhibitory repetition effects analogous to verbal memory.

    Science.gov (United States)

    Roe, Daisy; Miles, Christopher; Johnson, Andrew J

    2017-07-01

    The present paper examines the effect of within-sequence item repetitions in tactile order memory. Employing an immediate serial recall procedure, participants reconstructed a six-item sequence tapped upon their fingers by moving those fingers in the order of original stimulation. In Experiment 1a, within-sequence repetition of an item separated by two-intervening items resulted in a significant reduction in recall accuracy for that repeated item (i.e., the Ranschburg effect). In Experiment 1b, within-sequence repetition of an adjacent item resulted in significant recall facilitation for that repeated item. These effects mirror those reported for verbal stimuli (e.g., Henson, 1998a . Item repetition in short-term memory: Ranschburg repeated. Journal of Experimental Psychology: Learning, Memory, and Cognition, 24(5), 1162-1181. doi:doi.org/10.1037/0278-7393.24.5.1162). These data are the first to demonstrate the Ranschburg effect with non-verbal stimuli and suggest further cross-modal similarities in order memory.

  18. Inhibitory effect of bacteriocin-producing lactic acid bacteria against histamine-forming bacteria isolated from Myeolchi-jeot

    Directory of Open Access Journals (Sweden)

    Eun-Seo Lim

    2016-12-01

    Full Text Available Abstract The objectives of this study were to identify the histamine-forming bacteria and bacteriocin- producing lactic acid bacteria (LAB isolated from Myeolchi-jeot according to sequence analysis of the 16S rRNA gene, to evaluate the inhibitory effects of the bacteriocin on the growth and histamine accumulation of histamine-forming bacteria, and to assess the physico-chemical properties of the bacteriocin. Based on 16S rRNA gene sequences, histamine-forming bacteria were identified as Bacillus licheniformis MCH01, Serratia marcescens MCH02, Staphylococcus xylosus MCH03, Aeromonas hydrophila MCH04, and Morganella morganii MCH05. The five LAB strains identified as Pediococcus acidilactici MCL11, Leuconostoc mesenteroides MCL12, Enterococcus faecium MCL13, Lactobacillus sakei MCL14, and Lactobacillus acidophilus MCL15 were found to produce an antibacterial compound with inhibitory activity against the tested histamine-producing bacteria. The inhibitory activity of these bacteriocins obtained from the five LAB remained stable after incubation at pH 4.0–8.0 and heating for 10 min at 80 °C; however, the bacteriocin activity was destroyed after treatment with papain, pepsin, proteinase K, α-chymotrypsin, or trypsin. Meanwhile, these bacteriocins produced by the tested LAB strains also exhibited histamine-degradation ability. Therefore, these antimicrobial substances may play a role in inhibiting histamine formation in the fermented fish products and preventing seafood-related food-borne disease caused by bacterially generated histamine.

  19. Neuroprotective Effects of Acetylcholinesterase Inhibitory Peptides from Anchovy (Coilia mystus) against Glutamate-Induced Toxicity in PC12 Cells.

    Science.gov (United States)

    Zhao, Tiantian; Su, Guowan; Wang, Shuguang; Zhang, Qi; Zhang, Jianan; Zheng, Lin; Sun, Baoguo; Zhao, Mouming

    2017-12-27

    Ameliorations of cholinergic system dysfunction and oxidative stress in neurodegenerative diseases were main approaches to improve memory disorder. Our previous investigation showed that anchovy protein hydrolysate (APH) could attenuate scopolamine-induced memory deficits in mice by regulating acetylcholinesterase (AChE) activity. Therefore, peptides with AChE inhibitory activity in APH were explored and identified in this study, and their possible neuroprotective mechanisms on glutamate induced apoptosis in PC12 were also elucidated. Two peptides with strong AChE inhibitory capacity were identified as Pro-Ala-Tyr-Cys-Ser (PAYCS) and Cys-Val-Gly-Ser-Tyr (CVGSY) by ultraperformance liquid chromatography coupled with tandem mass spectrometry. The AChE inhibitory was 23.68 ± 0.97% and 6.08 ± 0.41%, respectively. Treatment with PAYCS and CVGSY could significantly (p < 0.05) increase cells viability, reduce lactate dehydrogenase release, reactive oxygen species (ROS) production, malondialdehyde content, and the ratio of Bax/Bcl-2 of glutamate-induced apoptosis PC12 cells (82.78 ± 6.58 and 109.94 ± 7.16% of control, respectively) as well as increase superoxide dismutase and GSH-px activities. In addition, both the peptides could inhibit Ca 2+ influx but have no effects on mitochondrial membrane potential. Results indicated that AChE inhibitory peptides (PAYCS and CVGSY) possibly protected the PC12 cells against glutamate-induced apoptosis via inhibiting ROS production and Ca 2+ influx. PAYCS and CVGSY might be considered as nutraceuticals for alleviating memory deficits.

  20. Effects of sub-inhibitory concentrations of German chamomile (Matricaria recotita extracts on the activity of catalase enzyme of S. aureus

    Directory of Open Access Journals (Sweden)

    gholamreza Goudarzi

    2005-12-01

    Findings: The extract showed growth inhibitory effect at dilution of and at dilution of showed bactericidal effect on standard strain. Dilutions of and as sub-inhibitory concentrations, decreased catalase activity prominently. Conclusion: Significant decrease of catalase activity at sub-inhibitory concentrations of this extract shows that this extract affects the production of catalase at different levels such as transcription, translation or transport and etc. Therefore, it is necessary to further study this extract. This enzyme can be a new target for production of novel antimicrobial agents.

  1. Effect of subinihibitory and inhibitory concentrations of Plectranthus amboinicus (Lour.) Spreng essential oil on Klebsiella pneumoniae.

    Science.gov (United States)

    Gonçalves, Thially Braga; Braga, Milena Aguiar; de Oliveira, Francisco F M; Santiago, Gilvandete M P; Carvalho, Cibele B M; Brito e Cabral, Paula; de Melo Santiago, Thiago; Sousa, Jeanlex S; Barros, Eduardo Bedê; do Nascimento, Ronaldo Ferreira; Nagao-Dias, Aparecida T

    2012-08-15

    We evaluated the antimicrobial activity and some mechanisms used by subinhibitory and inhibitory concentrations of the essential oil, obtained from leaves of Plectranthus amboinicus, against a standard strain of Klebsiella pneumoniae and 5 multiresistant clinical isolates of the bacteria. The minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC), the rate of kill and the pH sensitivity of the essential oil were determined by microdilution tests performed in 96-well plates. Subinhibitory and inhibitory concentrations of the essential oil were tested in order to check its action on K. pneumoniae membrane permeability, capsule expression, urease activity and cell morphology. The MIC and MBC of the essential oil were 0.09±0.01%. A complete inhibition of the bacterial growth was observed after 2 h of incubation with twice the MIC of the essential oil. A better MIC was found when neutral or alkaline pH broth was used. Alteration in membrane permeability was found by the increase of crystal violet uptake when the bacteria were incubated with twice the MIC levels of the essential oil. The urease activity could be prevented when all the subinhibitory concentrations were tested in comparison to the untreated group (p<0.001). Alteration of the bacterial morphology besides inhibition of the capsule expression was verified by atomic force microscopy, and Anthony's stain method, respectively. Our data allow us to conclude that the essential oil of P. amboinicus can be a good candidate for future research. Copyright © 2012 Elsevier GmbH. All rights reserved.

  2. Potent inhibitory effects of D-tagatose on the acid production and water-insoluble glucan synthesis of Streptococcus mutans GS5 in the presence of sucrose.

    Science.gov (United States)

    Sawada, Daijo; Ogawa, Takaaki; Miyake, Minoru; Hasui, Yoshinori; Yamaguchi, Fuminori; Izumori, Ken; Tokuda, Masaaki

    2015-01-01

    We examined and compared the inhibitory effects of D-tagatose on the growth, acid production, and water-insoluble glucan synthesis of GS5, a bacterial strain of Streptococcus mutans, with those of xylitol, D-psicose, L-psicose and L-tagatose. GS5 was cultured for 12h in a medium containing 10% (w/v) of xylitol, D-psicose, L-psicose, D-tagatose or L-tagatose, and the inhibitory effect of GS5 growth was assessed. Each sugar showed different inhibitory effects on GS5. Both D-tagatose and xylitol significantly inhibited the acid production and water-insoluble glucan synthesis of GS5 in the presence of 1% (w/v) sucrose. However, the inhibitory effect of acid production by D-tagatose was significantly stronger than that of xylitol in presence of sucrose.

  3. Anacardium occidentale Linn. (Anacardiaceae) stem bark extract induces hypotensive and cardio-inhibitory effects in experimental animal models.

    Science.gov (United States)

    Tchikaya, Francis Olivier; Bantsielé, Guy Bernard; Kouakou-Siransy, Gisèle; Datté, Jacques Yao; Yapo, Paul Angoue; Zirihi, Noel Guedé; Offoumou, Michel Atté

    2011-01-01

    Anacardium occidentale Linn. (Anacardiaceae) is a plant largely used in Africa for the treatment of different diseases. In Côte d'Ivoire it's commonly used for the treatment of hypertension. The present study was carried out in order to assess the effects of Anacardium occidentale extract (ANOE) on cardiovascular parameters in animal models. A mercury manometer kymograph of Ludwig was used to measure the blood pressure of normotensive rabbits in control conditions (normal physiological solution) and under the influence of ANOE. The contractile activity of an isolated rat heart was also measured in control conditions and under the influence of ANOE in different physiological media using a modified Langendhorff (1895) apparatus. The aqueous Anacardium occidentale (ANOE) bark extract applied intravenously in different doses (12, 40, 90, and 167 mg/kg b.w.), produced a significant dose-dependent decrease in blood pressure of previously normotensive rabbits (up to 89% vs control). Atropine (1 mg/ml) pre-treatment failed to reverse the hypotensive effects elicited by the extract. ANOE applied to isolated rat heart preparations in different concentrations (0.01, 0.1, 1.0, and 10 µg/ml) induced negative inotropic and chronotropic effects. Atropine pre-treatment of heart preparations (0.1 µg/ml) failed to reverse the negative effects induced by ANOE. The extract's action on heart contractile activity studied in modified culture media further confirmed its cardio-inhibitory effects. ANOE induced strong hypotensive and cardio-inhibitory effects in animal models.

  4. Inhibitory effect on nitric oxide production and free radical scavenging activity of Thai medicinal plants in osteoarthritic knee treatment.

    Science.gov (United States)

    Anuthakoengkun, Areeya; Itharat, Arunporn

    2014-08-01

    Thai medicine plants used for Osteoarthritis of knee (OA) treatment consist of twelve plants such as Crinumn asiaticum, Cleome viscosa, Drypetes roxburghii, Piper longum, Piper nigrum, Plumbago indica, Alpinia galanga, Curcuma aromatica, Globba malaccensis, Zingiber montanum, Zingiber officinale andZingiberzerumbet. They showedhighfrequency in OA formula. To investigate inhibitory effect on LPS-induced nitric oxide (NO) release from RAW264. 7 cell and free radical scavenging activity usingDPPH assay of these ethanolic plant extracts. Plant materials were extracted by maceration in 95% ethanol. Anti-inflammatory activity were tested on LPS-induced NO production. Free radical scavenging activity was performed by DPPH assay. All of ethanolic extracts exhibited potent inhibitory effect on NO release. The ethanolic extract of Z. zerumbet exhibited the highest inhibitory effect followed by Z. montanum and G. malaccensis, respectively. Except A. galanga and C. viscosa, all extracts possessed more influential than indomethacin (IC50 = 20.32±3.23 μLg/ml), a positive control. The investigation on antioxidant activity suggested that the ethanolic extracts of D. roxburghii, Z. officinale, Z. montanum, C. aromatic, A. galanga, P indica, G malaccensis, P nigrum exhibited antioxidant activity. By means ofD. roxburghii had the highest electron donating activity,followed by Z. officinale. Moreover both extracts were more effective than BHT apositive control (EC50 = 14.04±1.95 μg/ml). Thai medicinal plants had anti-inflammatory activity and could inhibit destruction of articular cartilage that corresponded to the traditional medicine and supported using these medicinal plants for OA treatment.

  5. Gastric inhibitory polypeptide analogues

    DEFF Research Database (Denmark)

    Holst, Jens Juul

    2002-01-01

    Gastric inhibitory polypeptide (GIP, also called glucose-dependent insulinotropic polypeptide) and glucagon-like peptide-1 (GLP-1) are peptide hormones from the gut that enhance nutrient-stimulated insulin secretion (the 'incretin' effect). Judging from experiments in mice with targeted deletions...

  6. Hypocholesterolemic Effect and In Vitro Pancreatic Lipase Inhibitory Activity of an Opuntia ficus-indica Extract

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    Eduardo Padilla-Camberos

    2015-01-01

    Full Text Available Cholesterol control is fundamental for prevention of cardiovascular disorders. In this work, the hypocholesterolemic activity of an aqueous Opuntia ficus-indica extract (AOE was tested in triton-induced mice. The inhibitory activity on pancreatic lipase enzyme was evaluated in vitro by the same extract. Furthermore, polyphenol content of the extract was evaluated. Hypercholesterolemia was induced in three groups of mice by intraperitoneal administration of Triton WR-1339. After induction of hypercholesterolemia, the groups were treated with an AOE (500 mg/kg and saline solution and the positive control group with orlistat, respectively. Cholesterol levels were measured 24 h later in peripheral blood. The levels of blood cholesterol after administration of AOE significantly decreased compared to negative control. The inhibitory activity of AOE on pancreatic lipase enzyme was evaluated at concentrations from 60 to 1000 μg/mL. The AOE inhibited the pancreatic lipase with an IC50 = 588.5 μg/mL. The AOE had a high content of polyphenolic compounds. These results show that AOE is able to prevent hypercholesterolemia by pancreatic lipase inhibition, in part due to its polyphenolic compounds.

  7. Hypocholesterolemic Effect and In Vitro Pancreatic Lipase Inhibitory Activity of an Opuntia ficus-indica Extract

    Science.gov (United States)

    Flores-Fernandez, Jose Miguel; Fernandez-Flores, Ofelia; Gutierrez-Mercado, Yanet; Carmona-de la Luz, Joel; Sandoval-Salas, Fabiola; Mendez-Carreto, Carlos

    2015-01-01

    Cholesterol control is fundamental for prevention of cardiovascular disorders. In this work, the hypocholesterolemic activity of an aqueous Opuntia ficus-indica extract (AOE) was tested in triton-induced mice. The inhibitory activity on pancreatic lipase enzyme was evaluated in vitro by the same extract. Furthermore, polyphenol content of the extract was evaluated. Hypercholesterolemia was induced in three groups of mice by intraperitoneal administration of Triton WR-1339. After induction of hypercholesterolemia, the groups were treated with an AOE (500 mg/kg) and saline solution and the positive control group with orlistat, respectively. Cholesterol levels were measured 24 h later in peripheral blood. The levels of blood cholesterol after administration of AOE significantly decreased compared to negative control. The inhibitory activity of AOE on pancreatic lipase enzyme was evaluated at concentrations from 60 to 1000 μg/mL. The AOE inhibited the pancreatic lipase with an IC50 = 588.5 μg/mL. The AOE had a high content of polyphenolic compounds. These results show that AOE is able to prevent hypercholesterolemia by pancreatic lipase inhibition, in part due to its polyphenolic compounds. PMID:26078966

  8. Cognitive-electrophysiological indices of attentional and inhibitory processing in adults with ADHD: familial effects

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    McLoughlin Gráinne

    2011-07-01

    Full Text Available Abstract Background Attention deficit hyperactivity disorder (ADHD is a common neurodevelopmental disorder that starts in childhood and frequently persists in adults. In a comparison of adults with ADHD and a matched control sample, we previously showed that abnormal inhibitory processing is typically preceded or accompanied by other processing deficits in adult ADHD. We now compare these data further to additional data from first-degree relatives (fathers of children with ADHD to identify whether this pattern of abnormal processing shares familial influences with ADHD in adults. Methods Using a family design, we compared 20 fathers of children with the combined subtype of ADHD with 21 adults with ADHD combined subtype and 20 controls in event-related potential indices of preparatory states and subsequent response inhibition processing as elicited by a cued continuous performance task. Results Fathers of children with ADHD exhibited significantly weaker orienting attention to cues and inhibitory processing than the controls but not the ADHD sample. Conclusions These findings provide evidence for the familial association of attentional orienting and response inhibition processes with ADHD in adults and indicate a familial and neurobiological link between ADHD in children and adults.

  9. Papain-like protease (PLpro) inhibitory effects of cinnamic amides from Tribulus terrestris fruits.

    Science.gov (United States)

    Song, Yeong Hun; Kim, Dae Wook; Curtis-Long, Marcus John; Yuk, Heung Joo; Wang, Yan; Zhuang, Ningning; Lee, Kon Ho; Jeon, Kwon Seok; Park, Ki Hun

    2014-01-01

    Tribulus terrestris fruits are well known for their usage in pharmaceutical preparations and food supplements. The methanol extract of T. terrestris fruits showed potent inhibition against the papain-like protease (PLpro), an essential proteolylic enzyme for protection to pathogenic virus and bacteria. Subsequent bioactivity-guided fractionation of this extract led to six cinnamic amides (1-6) and ferulic acid (7). Compound 6 emerged as new compound possessing the very rare carbinolamide motif. These compounds (1-7) were evaluated for severe acute respiratory syndrome coronavirus (SARS-CoV) PLpro inhibitory activity to identify their potencies and kinetic behavior. Compounds (1-6) displayed significant inhibitory activity with IC50 values in the range 15.8-70.1 µM. The new cinnamic amide 6 was found to be most potent inhibitor with an IC50 of 15.8 µM. In kinetic studies, all inhibitors exhibited mixed type inhibition. Furthermore, the most active PLpro inhibitors (1-6) were proven to be present in the native fruits in high quantities by HPLC chromatogram and liquid chromatography with diode array detection and electrospray ionization mass spectrometry (LC-DAD-ESI/MS).

  10. Litter Decomposition in a Semiarid Dune Grassland: Neutral Effect of Water Supply and Inhibitory Effect of Nitrogen Addition.

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    Yulin Li

    Full Text Available The decomposition of plant material in arid ecosystems is considered to be substantially controlled by water and N availability. The responses of litter decomposition to external N and water, however, remain controversial, and the interactive effects of supplementary N and water also have been largely unexamined.A 3.5-year field experiment with supplementary nitrogen and water was conducted to assess the effects of N and water addition on mass loss and nitrogen release in leaves and fine roots of three dominant plant species (i.e., Artemisia halondendron, Setaria viridis, and Phragmites australis with contrasting substrate chemistry (e.g. N concentration, lignin content in this study in a desertified dune grassland of Inner Mongolia, China. The treatments included N addition, water addition, combination of N and water, and an untreated control. The decomposition rate in both leaves and roots was related to the initial litter N and lignin concentrations of the three species. However, litter quality did not explain the slower mass loss in roots than in leaves in the present study, and thus warrant further research. Nitrogen addition, either alone or in combination with water, significantly inhibited dry mass loss and N release in the leaves and roots of the three species, whereas water input had little effect on the decomposition of leaf litter and fine roots, suggesting that there was no interactive effect of supplementary N and water on litter decomposition in this system. Furthermore, our results clearly indicate that the inhibitory effects of external N on dry mass loss and nitrogen release are relatively strong in high-lignin litter compared with low-lignin litter.These findings suggest that increasing precipitation hardly facilitates ecosystem carbon turnover but atmospheric N deposition can enhance carbon sequestration and nitrogen retention in desertified dune grasslands of northern China. Additionally, litter quality of plant species

  11. The Inhibitory Effects of 2 Commercial Probiotic Strains on the Growth of Staphylococcus aureus and Gene Expression of Enterotoxin A

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    Mahnoosh Parsaeimehr

    2017-08-01

    Full Text Available Background: Food-borne intoxications are current problems in human society and most of them are caused by the enterotoxins of Staphylococcus aureus. Staphylococcal enterotoxin A (SEA is the most frequently responsible for staphylococcal food poisoning outbreaks. From a food safety and human health point of view, lactic acid bacteria (LAB may provide a promising strategy to combat the pathogenic bacteria, particularly S. aureus. Objective: The objective of this study was to evaluate the inhibitory activity of two commercial lactobacillus strains on growth and enterotoxin A production by S. aureus. Moreover, the inhibitory effect of these strains on gene expression of enterotoxin type A was assessed using real-time Polymerase chain reaction (PCR. Materials and Methods: In this study the inhibitory effect of two commercial probiotic strains, Lactobacillus acidophilus (LA5 and Lactobacillus casei 01 on the growth and enterotoxin production of S. aureus was evaluated at 25 and 35°C. The gene expression of SEA of S. aureus was also evaluated by real time (RT PCR technique. Results: The lactobacillus strains decreased the bacterial count at both temperatures compared with the control group. This reduced effect was greater at 25°C (3 log/CFU than 35°C (2 log/CFU. The production of SEA, SEC and SEE was inhibited by the lactobacillus strains. Furthermore, the gene expression of SEA was significantly suppressed in S. aureus co cultured with studied lactobacillus strains and the greatest down-regulation of sea (10.31 fold was observed in co-incubation of S. aureus with LC01 at 25°C. Conclusion: This research raises important implications for the potential use of LAB as a natural preservative in foodstuffs by correct microbial ecology of the environment and a new approach for biocontrol of S. aureus.

  12. Differential inhibitory effect of fondaparinux on the procoagulant potential of intact monocytes and monocyte-derived microparticles.

    Science.gov (United States)

    Ben-Hadj-Khalifa-Kechiche, Sonia; Hezard, Nathalie; Poitevin, Stephane; Remy, Marie-Geneviève; Florent, Bernadette; Mahjoub, Touhami; Nguyen, Philippe

    2010-11-01

    Monocytes and monocyte-derived microparticles (MMPs) play a major role in acute coronary syndrome (ASC). Activated monocytes (ac-M) and MMPs support thrombin generation via tissue factor (TF). The aim of this study was to evaluate the inhibitory effect of fondaparinux, a selective Xa inhibitor, on thrombin generation supported by activated monocytes and MMPs. Monocytes were purified by elutriation. They were activated by LPS, allowing to obtain both ac-M and MMPs. Thrombin generation was performed using Fluoroscan(®) in these two cell models, in comparison with a cell-free model (TF 5 pM final). Two concentrations of ac-M (0.2 × 10⁶ and 1 × 10⁶/well) and four concentrations of MMPs (40,000; 80,000; 120,000 and 160,000/well) were tested. TGT was evaluated for increasing fondaparinux concentrations (0, 0.1, 0.4, 0.7 and 1.2 μg/ml). Without fondaparinux, 0.2 × 10⁶ ac-M and 160,000 MMPs induced comparable results. Fondaparinux inhibited thrombin generation in the three models. Inhibition was fondaparinux concentration dependent. Rate index was the most sensitive parameter, compared to lag-time, peak and endogenous thrombin potential. The rate index IC(50) were 0.69 ± 0.03 μg/ml for ac-M, 0.20 ± 0.03 μg/ml for MMPs, and 0.22 ± 0.02 μg/ml for cell-free model. Fondaparinux exerted an inhibitory effect at all concentrations, including the lowest (0.1 μg/ml). The extend of inhibition was similar between MMPs and cell-free models, and stronger than ac-M model. We assume that the efficacy of fondaparinux 2.5 mg once daily in ACS patients may be in part attributed to its inhibitory effect on MMPs.

  13. Effects of chloroquine, mefloquine and quinine on natural killer cell activity in vitro. An analysis of the inhibitory mechanism

    DEFF Research Database (Denmark)

    Pedersen, B K; Bygbjerg, I C; Theander, T G

    1986-01-01

    Natural killer (NK) cell activity against K 562 target cells was inhibited by pharmacological concentrations of chloroquine, mefloquine and quinine. The most potent were mefloquine and quinine. The drug-induced inhibition of the NK cell activity was abolished by addition of alpha-interferon (IF...... NK cell enriched populations in a single cell agarose assay, it was shown that the inhibitory effects of mefloquine, but not of chloroquine and quinine were due to an inhibition of the formation of effector/target cell conjugates....

  14. Phenolic amides from Tribulus terrestris and their inhibitory effects on nitric oxide production in RAW 264.7 cells.

    Science.gov (United States)

    Kim, Hyung Sik; Lee, Jin Woo; Jang, Hari; Le, Thi Phuong Linh; Kim, Jun Gu; Lee, Moon Soon; Hong, Jin Tae; Lee, Mi Kyeong; Hwang, Bang Yeon

    2018-02-01

    A new phenolic amide, named cis-terrestriamide (7), together with ten known compounds (1-6, 8-11), were isolated from the methanolic extract of the fruits of Tribulus terrestris. The structure of 7 was elucidated on the basis of extensive analyses of 1D and 2D nuclear magnetic resonance spectroscopic and high resolution mass spectrometry data. Compounds 1, 2, 5, 6, 8, 9, and 11 exhibited inhibitory effects on the lipopolysaccharide-stimulated nitric oxide production in RAW 264.7 cells, with IC 50 values of 18.7-49.4 μM.

  15. Inhibitory effects of Ganoderma applanatum on rat lens aldose reductase and sorbitol accumulation in streptozotocin-induced diabetic rat tissues.

    Science.gov (United States)

    Jung, Sang Hoon; Lee, Yeon Sil; Shim, Sang Hee; Lee, Sanghyun; Shin, Kuk Hyun; Kim, Ju Sun; Kim, Yeong Shik; Kang, Sam Sik

    2005-06-01

    Aldose reductase, the key enzyme of the polyol pathway, is known to play important roles in diabetic complications. Therefore, inhibitors of aldose reductase would be potential agents for the prevention of diabetic complications. To evaluate the inhibitory potential of aldose reductase from Ganoderma applanatum (Polyporaceae), methanol (MeOH) and water extracts were tested for their effects on rat lens aldose reductase (RLAR). The effects of both extracts on streptozotocin (STZ)-induced diabetes in rats were also investigated. The MeOH extract exhibited a potent rat lens aldose reductase (RLAR) inhibition in vitro, and showed a significant inhibition, of not only serum glucose concentrations, but also of sorbitol accumulations in the lens, red blood cells (RBC) and sciatic nerves in STZ-induced diabetic rats. Associated with a reduction in serum glucose concentration in STZ-induced diabetic rats, this extract was found to cause a significant glucose tolerance effect. These results suggested that G. applanatum might possess constituents with antidiabetic and inhibitory effects on diabetic complications. Copyright (c) 2005 John Wiley & Sons, Ltd.

  16. The inhibitory effect of progesterone on lactogenesis during pregnancy is already evident by mid- to late gestation in rodents.

    Science.gov (United States)

    López-Fontana, Constanza M; Maselli, María E; Salicioni, Ana M; Carón, Rubén W

    2012-01-01

    Lactogenesis is a very complex process highly dependent on hormonal regulation. In the present study the time-course of the inhibitory actions of progesterone on prolactin secretion, mammary gland morphology and lactogenesis from mid- to late gestation in rodents was investigated. Groups of pregnant rats were luteectomised or administered with mifepristone on Day 10, 13, 15 or 17 of gestation and decapitated 28 or 48h later. Whole-blood samples and the inguinal mammary glands were taken for determinations of hormone levels and for measurement of mammary content of casein and lactose and for tissue morphology analyses, respectively. Luteectomy or mifepristone evoked prolactin increases only after Day 17 of gestation. Mammary content of casein was increased by both treatments regardless of timing or duration. Mifepristone was less effective than luteectomy in inducing lactose production and the effect was only observed after Day 15 of gestation. Analysis of mammary gland morphology confirmed the observed effect of progesterone on lactogenesis. Both treatments triggered remarkable secretory activity in the mammary gland, even without a parallel epithelial proliferation, demonstrating that the mammary epithelium is able to synthesise milk compounds long before its full lobulo-alveolar development is achieved, provided that progesterone action is abolished. Thus, the present study demonstrates that progesterone is a potent hormonal switch for the prolactin and prolactin-like effects on mammary gland development and its milk-synthesising capacity during pregnancy, and that its inhibitory action is already evident by mid-pregnancy in rodents.

  17. Inhibitory effects of different forms of tocopherols, tocopherol phosphates, and tocopherol quinones on growth of colon cancer cells.

    Science.gov (United States)

    Dolfi, Sonia C; Yang, Zhihong; Lee, Mao-Jung; Guan, Fei; Hong, Jungil; Yang, Chung S

    2013-09-11

    Tocopherols are the major source of dietary vitamin E. In this study, the growth inhibitory effects of different forms of tocopherols (T), tocopheryl phosphates (TP), and tocopherol quinones (TQ) on human colon cancer HCT116 and HT29 cells were investigated. δ-T was more active than γ-T in inhibiting colon cancer cell growth, decreasing cancer cell colony formation, and inducing apoptosis; however, α-T was rather ineffective. Similarly, the rate of cellular uptake also followed the ranking order δ-T > γ-T ≫ α-T. TP and TQ generally had higher inhibitory activities than their parent compounds. Interestingly, the γ forms of TP and TQ were more active than the δ forms in inhibiting cancer cell growth, whereas the α forms were the least effective. The potencies of γ-TQ and δ-TQ (showing IC50 values of ∼0.8 and ∼2 μM on HCT116 cells after a 72 h incubation, respectively) were greater than 100-fold and greater than 20-fold higher, respectively, than those of their parent tocopherols. Induction of cancer cell apoptosis by δ-T, γ-TP, and γ-TQ was characterized by the cleavage of caspase 3 and PARP1 and DNA fragmentation. These studies demonstrated the higher growth inhibitory activity of δ-T than γ-T, the even higher activities of the γ forms of TP and TQ, and the ineffectiveness of the α forms of tocopherol and their metabolites against colon cancer cells.

  18. Effects of Subminimum Inhibitory Concentrations of Antibiotics on the Pasteurella multocida Proteome: A Systems Approach

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    Bindu Nanduri

    2008-01-01

    Full Text Available To identify key regulators of subminimum inhibitory concentration (sub-MIC antibiotic response in the Pasteurella multocida proteome, we applied systems approaches. Using 2D-LC-ESI-MS2, we achieved 53% proteome coverage. To study the differential protein expression in response to sub-MIC antibiotics in the context of protein interaction networks, we inferred P. multocida Pm70 protein interaction network from orthologous proteins. We then overlaid the differential protein expression data onto the P. multocida protein interaction network to study the bacterial response. We identified proteins that could enhance antimicrobial activity. Overall compensatory response to antibiotics was characterized by altered expression of proteins involved in purine metabolism, stress response, and cell envelope permeability.

  19. Enzymatic synthesis of arbutin undecylenic acid ester and its inhibitory effect on mushroom tyrosinase.

    Science.gov (United States)

    Tokiwa, Y; Kitagawa, M; Raku, T

    2007-03-01

    A novel tyrosinase inhibitor, an arbutin derivative having undecylenic acid at the 6-position of its glucose moiety, was enzymatically synthesized. Its inhibitory activity was studied in vitro by using catechol and phenol as substrates. The IC(50) value of the arbutin ester on tyrosinase using catechol (4 x 10(-4) M) was 1% of that when arbutin (4 x 10(-2) M) was used. Using phenol, IC(50) of the arbutin ester (3 x 10(-4) M) as substrate was 10% of that of arbutin (3 x 10(-3) M). These results suggest that the arbutin ester inhibits the latter part of the tyrosinase reaction, which consists of hydroxylation and oxidation.

  20. Sesquiterpenes from the essential oil of Curcuma wenyujin and their inhibitory effects on nitric oxide production.

    Science.gov (United States)

    Xia, Guiyang; Zhou, Li; Ma, Jianghao; Wang, Ying; Ding, Liqin; Zhao, Feng; Chen, Lixia; Qiu, Feng

    2015-06-01

    Three new sesquiterpenes including a new elemane-type sesquiterpene, 5βH-elem-1,3,7,8-tetraen-8,12-olide (1), and two new carabrane-type sesquiterpenes, 7α,11-epoxy-6α-methoxy-carabrane-4,8-dione (2) and 8,11-epidioxy-8-hydroxy-4-oxo-6-carabren (3), together with eight known sesquiterpenes (4-11) were isolated from Curcuma wenyujin Y. H. Chen et C. Ling. Their structures were elucidated based on extensive spectroscopic analyses. A possible biogenetic scheme for the related compounds was postulated. All of the isolated compounds were tested for inhibitory activity against LPS-induced nitric oxide production in RAW 264.7 macrophages. Meanwhile, preliminary structure-activity relationships for these compounds are discussed. Copyright © 2015 Elsevier B.V. All rights reserved.

  1. Inhibitory effects of small molecular peptides from Spirulina (Arthrospira) platensis on cancer cell growth.

    Science.gov (United States)

    Wang, Zhujun; Zhang, Xuewu

    2016-02-01

    In this study, the whole proteins of Spirulina (Arthrospira) platensis were extracted, hydrolysis with three proteases (trypsin, alcalase and papain) was performed, and gel filtration chromatography was employed to separate hydrolysates. Totally, 15 polypeptides were isolated, which showed anti-proliferation activities on five cancer cells (HepG-2, MCF-7, SGC-7901, A549 and HT-29), with the IC50 values between <31.25 and 336.57 μg mL(-1). Moreover, a new peptide YGFVMPRSGLWFR was identified from papain-digested hydrolysates. It also exhibited inhibitory activities on cancer cells, and the best activity was observed on A549 cancer cells (IC50 values 104.05 μg mL(-1)). In other words, these polypeptides exhibited anti-proliferation activities on cancer cells, and low toxicity or stimulatory activity on normal cells, suggesting that they are promising ingredients in food and pharmaceutical applications.

  2. Antifungal Effects of Zataria multiflora Essential Oil on the Inhibitory Growth of some Postharvest Pathogenic Fungi

    Directory of Open Access Journals (Sweden)

    Mahboobeh NASSERI

    2015-12-01

    Full Text Available The present study aimed to determine minimum inhibitory concentration and minimum fungicidal concentration of the essential oil of Zataria multiflora to control Alternaria solani, Rhizoctonia solani, Rhizopus stolonifer, Aspergillus flavus, Aspergillus ochraceus and Aspergillus niger. The essential oil of Zataria multiflora was tested in vitro on PDA (malt extract agar medium with eight concentrations: 0, 10, 50, 100, 200, 300, 400, 500, 600, 700, 800, 900 and 1000 ppm. This investigation followed the completely randomized design (CRD with three replications. GC-MS evaluations of the essential oil revealed that thymol (35%, carvacrol (34%, cymene-p (9.89%, gamma-terpinene (5.88% and alpha-pinene (4.22% were the main compounds of Zataria multiflora oil. The results showed that the essential oil of Zataria multiflora has antifungal activity; the lowest inhibition (75% was observed in the A. niger, while the highest inhibition (95.3% was observed in A. solani. Minimum inhibitory concentration for A. solani, R. solani, R. stolonifer, A. flavus, A. ochraceus and A. niger was 200, 200, 200, 300, 300 and 200 ppm respectively. In addition, the present results showed that minimum fungicidal concentration (MFC for A. solani, R. solani, R .stolonifer, A. niger and A.ochraceus was 600, 400, 300, 900 and 700 ppm respectively and none of the tested concentrations were fatal for A. flavus. A. solani and R. solani showed a strong sensitivity to Zataria multiflora essential oil at all concentrations. Findings of the current study suggest that essential oils of Zataria multiflora could be used for control of postharvest phytopathogenic fungi on fruits or vegetables.

  3. Antioxidative Characteristics of Anisomeles indica Extract and Inhibitory Effect of Ovatodiolide on Melanogenesis

    Directory of Open Access Journals (Sweden)

    Li-Ling Chang

    2012-05-01

    Full Text Available The purpose of the study was to investigate the antioxidant characteristics of Anisomeles indica methanol extract and the inhibitory effect of ovatodiolide on melanogenesis. In the study, the antioxidant capacities of A. indica methanol extract such as DPPH assay, ABTS radical scavenging assay, reducing capacity and metal ion chelating capacity as well as total phenolic content of the extract were investigated. In addition, the inhibitory effects of ovatodiolide on mushroom tyrosinase, B16F10 intracellular tyrosinase and melanin content were determined spectrophotometrically. Our results revealed that the antioxidant capacities of A. indica methanol extract increased in a dose-dependent pattern. The purified ovatodiolide inhibited mushroom tyrosinase activity (IC50 = 0.253 mM, the compound also effectively suppressed intracellular tyrosinase activity (IC50 = 0.469 mM and decreased the amount of melanin (IC50 = 0.435 mM in a dose-dependent manner in B16F10 cells. Our results concluded that A. indica methanol extract displays antioxidant capacities and ovatodiolide purified from the extract inhibited melanogenesis in B16F10 cells. Hence, A. indica methanol extract and ovatodiolide could be applied as a type of dermatological whitening agent in skin care products.

  4. Lignan dicarboxylates and terpenoids from the flower buds of Cananga odorata and their inhibitory effects on melanogenesis.

    Science.gov (United States)

    Matsumoto, Takahiro; Nakamura, Seikou; Nakashima, Souichi; Fujimoto, Katsuyoshi; Yoshikawa, Masayuki; Ohta, Tomoe; Ogawa, Keiko; Matsuda, Hisashi

    2014-04-25

    The methanolic extract from the flower buds of Cananga odorata showed an inhibitory effect on melanogenesis in theophylline-stimulated murine B16 melanoma 4A5 cells. From the methanolic extract, two new lignan dicarboxylates, canangalignans I and II, three new terpenoids, canangaterpenes I, II, and III, and eight known compounds were isolated. The structures of these compounds were elucidated on the basis of chemical/physicochemical evidence. Several mono- and sesquiterpene analogues significantly inhibited melanogenesis. In particular, canangaterpene I and (3R,3aR,8aS)-3-isopropyl-8a-methyl-8-oxo-1,2,3,3a,6,7,8,8a-octahydroazulene-5-carbaldehyde exhibited a potent inhibitory effect on melanogenesis [inhibition (%): 34.7±4.2 (p<0.01), 45.5±5.7 (p<0.01) at 1 μM, respectively] without inducing cytotoxicity. Moreover, the biological effect of these compounds was much stronger than that of the reference compound, arbutin. Thus, these isolated terpenoid derivatives may be promising therapeutic agents for the treatment of several skin disorders.

  5. Phytochemical composition, protective and therapeutic effect on gastric ulcer and α-amylase inhibitory activity of Achillea biebersteinii Afan.

    Science.gov (United States)

    Abd-Alla, Howaida I; Shalaby, Nagwa M M; Hamed, Manal A; El-Rigal, Nagy Saba; Al-Ghamdi, Samira N; Bouajila, Jalloul

    2016-01-01

    Three sesquiterpene lactones [two germacranolides (micranthin and sintenin) and one guaianolide (4β,10α-dihydroxy-5β,7β,8βH-guaia-1,11(13)dien-12,8α-olide)] and four derivatives of 3-methoxy flavones (santin, quercetagetin-3,6,3'-trimethyl ether, quercetagetin-3,6-dimethyl ether, and 5,7 dihydroxy 3,3',4'-trimethoxy flavone) were isolated from the ethyl acetate extract (EAE) of the aerial parts of Achillea biebersteinii Afan. (Asteraceae). Evaluation of protective and therapeutic effects of EAE against ethanol-induced gastric ulcer in rats was carried. Antiulcer activity evaluation was done through measuring ulcer indices, stomach acidity, gastric volume and lesion counts. Oxidative stress markers; malondialdehyde, glutathione and superoxide dismutase were also estimated. The work was extended to determine the histopathological assessment of the stomach. Gastric ulcer exhibited a significant elevation of the ulcer index and oxidative stress markers. The extract attenuated these increments and recorded protective and therapeutic effects against gastric ulcer. Hyperglycaemia increases the mucosal susceptibility to ulcerogenic stimuli and predisposes gastric ulceration. In vitro α-amylase inhibitory assay was applied to evaluate the post prandial antihyperglycaemia activity. The result showing that the EAE has the ability to reduce starch-induced postprandial glycaemic excursions by virtue of potent intestinal α-amylase inhibitory activity. These findings demonstrated the remarkable potential of A. biebersteinii as valuable source of antiulcer agent with post prandial hyperglycaemia lowering effect.

  6. Inhibitory effect of Zataria multiflora Boiss and carvacrol on histamine (H(1) ) receptors of guinea-pig tracheal chains.

    Science.gov (United States)

    Boskabady, Mohammad Hossein; Tabanfar, Hengameh; Gholamnezhad, Zahra; Sadeghnia, Hamid Reza

    2012-10-01

    The inhibitory effect of aqueous-ethanolic extract of Zataria multiflora Boiss (Labiatae) and carvacrol on histamine (H(1) ) receptors was examined on tracheal chains of guinea-pigs. The effects of three concentrations of aqueous-ethanolic extract, carvacrol, 10 nm chlorpheniramine, and saline on histamine (H(1) ) receptors were tested on three groups of guinea-pig tracheal chains as follows: incubated trachea with (i) indomethacin (n = 9), (ii) indomethacin, propranolol, and atropine (n = 7), and (iii) indomethacin and propranolol (n = 6). The EC(50) (effective concentration of histamine causing 50% of maximum response) obtained in the presence of chlorpheniramine for all concentrations of the extract and carvacrol in all three groups was significantly higher than that of saline (P effect of Z. multiflora and its constituent carvacrol on histamine H(1) receptors. © 2011 The Authors Fundamental and Clinical Pharmacology © 2011 Société Française de Pharmacologie et de Thérapeutique.

  7. The bacterial biofilms in dialysis water systems and the effect of the sub inhibitory concentrations of chlorine on them.

    Science.gov (United States)

    Suman, Ethel; Varghese, Benji; Joseph, Neethu; Nisha, Kumari; Kotian, M Shashidhar

    2013-05-01

    The presence of bacteria in the form of biofilms poses a problem in the fluid pathways of haemodialysis plants and procedures which are aimed to detach and neutralize biofilms are necessary to improve the patient safety and the quality of the healthcare. The present study was therefore aimed at isolating the organisms which colonized dialysis water systems as biofilms, as well as to study the effect of the sub inhibitory concentrations of chlorine on the biofilms which were produced by these isolates. Swabs were used to collect the biofilms which were produced on the internal surface of the dialysis tubing from the dialysis units. This study was conducted at the Department of Microbiology, Kasturba Medical College (KMC), Mangalore, India. The cultures were performed on MacConkey's agar and blood agar. The organisms which were isolated were identified and antibiotic sensitivity tests were performed. The biofilm production was done by the microtitre plate method of O'Toole and Kolter. The biofilm production was also studied in the presence of sub inhibitory concentrations of chlorine. Acinetobacter spp and Pseudomonas aeruginosa were the two predominant organisms which colonized the dialysis water systems as biofilms. The sub inhibitory concentrations of chlorine did not bring about any decrease in the biofilm production by the isolates. On the contrary, there was an increase in the biofilm production. Our study highlighted the importance of using appropriate methods to improve the quality of the water in dialysis units. This in turn, may help in reducing the biofilm formation in the water systems of dialysis units and thus, contribute to the prevention of hospital acquired infections in the patients who need haemodialysis.

  8. Inhibitory effect of ethanol extract of Nannochloropsis oceanica on lipopolysaccharide-induced neuroinflammation, oxidative stress, amyloidogenesis and memory impairment.

    Science.gov (United States)

    Choi, Ji Yeon; Hwang, Chul Ju; Lee, Hee Pom; Kim, Hee Sik; Han, Sang-Bae; Hong, Jin Tae

    2017-07-11

    Oxidative stress and neuroinflammation is implicated in the pathogenesis and development of Alzheimer's disease (AD). Here, we investigated the suppressive possibility of ethanol extract of Nannochloropsis oceanica (N. oceanica) on memory deficiency along with the fundamental mechanisms in lipopolysaccharide (LPS)-treated mice model. Among several extracts of 32 marine microalgae, ethanol extract of N. oceanica showed the most significant inhibitory effect on nitric oxide (NO) generation, NF-κB activity and β-secretase activity in cultured BV-2 cells, neuronal cells and Raw 264.7 cells. Ethanol extract of N. oceanica (50, 100 mg/kg) also ameliorated LPS (250 μg/kg)-induced memory impairment. We also found that ethanol extract of N. oceanica inhibited the LPS-induced expression of iNOS and COX-2. Furthermore, the production of reactive oxygen species (ROS), malondialdehyde (MDA) level as well as glutathione (GSH) level was also decreased by treatment of ethanol extract of N.oceanica. The ethanol extract of N. oceanica also suppresses IκB degradation as well as p50 and p65 translocation into the nucleus in LPS-treated mice brain. Associated with the inhibitory effect on neuroinflammation and oxidative stress, ethanol extract of N. oceanica suppressed Aβ1-42 generation through down-regulation of APP and BACE1 expression in in vivo. These results suggest that ethanol extract of N. oceanica ameliorated memory impairment via anti-inflammatory, anti-oxidant and anti-amyloidogenic mechanisms.

  9. Inhibitory effect of nicotinamide on in vitro and in vivo production of tumor necrosis factor-alpha.

    Science.gov (United States)

    Fukuzawa, M; Satoh, J; Muto, G; Muto, Y; Nishimura, S; Miyaguchi, S; Qiang, X L; Toyota, T

    1997-10-01

    Nicotinamide, a pellagra-preventive factor, has multiple functions such as inhibition of poly-ADP-ribose synthetase, inhibition of inducible nitric oxide synthase, free radical scavenging and suppression of major histocompatibility complex class II expression and ICAM-1 expression on endothelial cells. In addition to these, we have found an inhibitory effect of nicotinamide on production of tumor necrosis factor-alpha (TNF-alpha) in vitro and in vivo. Lipopolysaccharide (LPS)-induced in vitro TNF-alpha production by human peripheral blood mononuclear cells, measured by enzyme-linked immunosorbent assay (ELISA), was significantly inhibited with more than 1 x 10(-3) mol/l of nicotinamide, while interleukin-1-beta was not inhibited and interleukin-6 was slightly inhibited even with 10(-2) mol/l. Oral administration of nicotinamide with more than 62.5 mg/kg also significantly inhibited LPS-induced serum TNF-alpha production measured by ELISA and bioassay in Balb/c mice. Thus, nicotinamide has an inhibitory effect on TNF-alpha production that may be beneficial to TNF-alpha-mediated diseases.

  10. Inhibition of BCL2 expression and activity increases H460 sensitivity to the growth inhibitory effects of polyphenon E.

    Science.gov (United States)

    Borgovan, Theodor; Bellistri, John-Paul S; Slack, Kristen N; Kopelovich, Levy; Desai, Manisha; Joe, Andrew K

    2009-01-01

    The anti-cancer properties of the green tea-derived mixture Polyphenon E (Poly E) have been demonstrated in a variety of cell culture and animal models. We recently discovered that the H460 lung cancer cell line is markedly resistant to the growth inhibitory effects of Poly E compared with SW480 colon and Flo-1 esophageal cancer cells. We investigated the mechanism of H460 resistance by comparing gene expression profiles of Poly E-sensitive and -resistant cells. Unsupervised hierarchical clustering revealed that Poly E-sensitive cells clustered separately from Poly E-resistant cells, and 6,242 genes were differentially expressed between the two groups at the 0.01 level of significance. We discovered that BCL2 gene and protein expression were significantly higher in H460 cells compared with SW480 and Flo-1 cells (10.60-fold higher gene expression; P < 0.0001). Inhibition of BCL2 expression and activity, using siRNA and the small molecule inhibitor HA14-1 respectively, restored sensitivity to Poly E and induced BCL2-related apoptosis by decreasing mitochondrial membrane potential and inducing PARP cleavage. Our results suggest that increased BCL2 expression may contribute to H460 resistance to the growth inhibitory effects of Poly E. If validated in additional laboratory and clinical models, BCL2 could ultimately be used as a marker of Poly E resistance.

  11. [Synthesis of colon-specific prodrug of indomethacin and its inhibitory effect on liver metastasis from colon cancer].

    Science.gov (United States)

    Peng, Ning-fu; Yang, Li-qun; Chen, Ru-fu; Cai, Xiang; Li, Le-qun; Li, Zhi-hua; Zhou, Quan-bo; Zhou, Jia-jia; Jiang, Zhi-peng

    2010-03-01

    To develop a colon-specific prodrug of Indomethacin microbially triggered, carry out in vitro/in vivo evaluation of drug release, and appraise its inhibitory effect on liver metastasis from colon cancer. Indomethacin prodrugs were synthesized and characterized by FTIR and NMR, and dissolution test simulating gastrointestinal tract was employed to screen the colon-specific prodrug. Then, the pharmacokinetic profile of portal vein and peripheral blood in Sprague-Dawley rats was studied. Lastly, the inhibitory effect on liver metastasis from colon cancer in nude mice was observed. The chemical structure characterized by FTIR and NMR demonstrated that six kinds of indomethacin-block-amylose with different drug loading (IDM-AM-1-6) were synthesized, among which IDM-AM-3 was degraded 1.3%, 9.3% and 95.3%, respectively, in simulated gastric fluid for 4 h, small intestine for 6 h, and colon for 36 h. The pharmacokinetic test of IDM-AM-3 showed that absorption was delayed significantly (P IDM regarding to portal vein. Additionally, its AUC(0-t) in peripheral blood was remarkably lower than that in Portal vein (P IDM (P IDM-AM-3 possesses advantage of sustained release in portal vein providing some experimental basis for colon-specific delivery system applied to sustained release in the portal vein.

  12. Inhibitory effects of oxaliplatin in experimental radiation treatment of colorectal carcinoma: does oxaliplatin improve 5-fluorouracil-dependent radiosensitivity?

    International Nuclear Information System (INIS)

    Folkvord, Sigurd; Flatmark, Kjersti; Seierstad, Therese; Roe, Kathrine; Rasmussen, Heidi; Ree, Anne Hansen

    2008-01-01

    Background and purpose: New chemoradiotherapy regimens for rectal cancer with integration of oxaliplatin with 5-fluorouracil-based therapy are being actively investigated. However, only limited preclinical data are available on oxaliplatin as radiosensitizer in colorectal carcinoma. Materials and methods: A human colorectal carcinoma cell line (HT29) was exposed to ionizing radiation with or without oxaliplatin and/or 5-fluorouracil, upon which clonogenicity and cell cycle profiles were analyzed. HT29 xenografts were treated for two weeks with daily radiation and/or the oral 5-fluorouracil analog capecitabine with or without oxaliplatin once weekly, and tumor volumes were followed for up to 60 days. Results: Pretreatment of HT29 cells with oxaliplatin for 2 h, followed by radiation and a 48-h exposure to 5-fluorouracil, resulted in increased radiocytotoxicity, and combination index analysis indicated synergistic effects. Ionizing radiation and oxaliplatin induced cell cycle G 2 /M phase arrest in HT29 cells at distinctly different time points. Growth of HT29 xenografts was clearly inhibited by radiation. Capecitabine and oxaliplatin together significantly improved the inhibitory effect, but oxaliplatin did not add to the growth inhibitory response induced by radiation plus capecitabine. Conclusions: The combination of oxaliplatin and 5-fluorouracil sensitized colorectal carcinoma cells to ionizing radiation in vitro. In vivo, however, oxaliplatin did not convincingly improve the increased radiocytotoxicity conferred by capecitabine treatment. In the absence of conclusive clinical evidence, the integration of OXA into combined-modality treatment of rectal cancer must remain controversial

  13. Effect of steeping temperature on antioxidant and inhibitory activities of green tea extracts against α-amylase, α-glucosidase and intestinal glucose uptake.

    Science.gov (United States)

    Liu, Shuyuan; Ai, Zeyi; Qu, Fengfeng; Chen, Yuqiong; Ni, Dejiang

    2017-11-01

    The objective of the present study was to evaluate the effect of steeping temperature on the biological activities of green tea, including the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical-scavenging capacity, α-glucosidase and α-amylase inhibitory activities, and glucose uptake inhibitory activity in Caco-2 cells. Results showed that, with increasing extraction temperature, the polyphenol content increased, which contributed to enhance antioxidant activity and inhibitory effects on α-glucosidase and α-amylase. Green tea steeped at 100°C showed the highest DPPH radical-scavenging activity and inhibitory effects on α-glucosidase and α-amylase activities with EC 50 or IC 50 values of 6.15μg/mL, 0.09mg/mL, and 6.31mg/mL, respectively. However, the inhibitory potential on glucose uptake did not show an upward trend with increasing extraction temperature. Green tea steeped at 60°C had significantly stronger glucose uptake inhibitory activity (ptea. Copyright © 2017 Elsevier Ltd. All rights reserved.

  14. Antimicrobial and selected in vitro enzyme inhibitory effects of leaf extracts, flavonols and indole alkaloids isolated from Croton menyharthii.

    Science.gov (United States)

    Aderogba, Mutalib A; Ndhlala, Ashwell R; Rengasamy, Kannan R R; Van Staden, Johannes

    2013-10-11

    Croton species are used in folk medicine in the management of infections, inflammation and oxidative stress-related diseases. In order to isolate, characterize and evaluate the bioactive constituents of Croton menyharthii Pax leaf extracts, repeated column fractionation of the ethyl acetate fraction from a 20% aqueous methanol crude extract afforded three flavonols identified by NMR (1D and 2D) spectroscopic methods as myricetrin-3-O-rhamnoside (myricetrin, 1), quercetin-3-O-rhamnoside (2) and quercetin (3) along with an indole alkaloid, (E)-N-(4-hydroxycinnamoyl)-5-hydroxytryptamine, [trans-N-(p-coumaroyl) serotonin, 4]. All the compounds are reported from the leaf extract of this plant for the first time. The crude extracts, four solvent fractions (hexane, DCM, ethyl acetate and butanol) and isolated compounds obtained from the leaves were evaluated for their inhibitory effects on selected bacteria, a fungus (Candida albicans), cyclooxygenase (COX-2), α-glucosidase and acetylcholinesterase (AChE). Amongst the compounds, quercetin (3) was the most active against Bacillus subtilis and Candida albicans while myricetrin-3-O-rhamnoside (1) and trans-N-(p-coumaroyl) serotonin (4) were the most active compounds against Escherichia coli, Klebsiella pneumonia and Staphylococcus aureus. The inhibitory activity of myricetrin-3-O-rhamnoside (1) against COX-2 was insignificant while that of the other three compounds 2-4 was low. The AChE inhibitory activity of the alkaloid, trans-N-(p-coumaroyl) serotonin was high, with a percentage inhibitory activity of 72.6% and an IC50 value of 15.0 µg/mL. The rest of the compounds only had moderate activity. Croton menyharthii leaf extracts and isolated compounds inhibit α-glucosidase at very low IC50 values compared to the synthetic drug acarbose. Structure activity relationship of the isolated flavonols 1-3 is briefly outlined. Compounds 1-4 and the leaf extracts exhibited a broad spectrum of activities. This validates the

  15. In vitro inhibitory effects of farnesol and interactions between farnesol and antifungals against biofilms of Candida albicans resistant strains.

    Science.gov (United States)

    Xia, Jinping; Qian, Fang; Xu, Wenqian; Zhang, Zhenzhen; Wei, Xin

    2017-04-01

    Antifungal resistance is a serious problem in clinical infections. Farnesol, which is a potential antifungal agent against biofilms formed by Candida albicans resistant strains (a fluconazole-resistant isolate derived from SC5314 and two clinical Candida resistant isolates), was investigated in this study. The inhibitory effects of farnesol on biofilms were examined by XTT assay. The morphological changes and biofilm thicknesses were analyzed by scanning electron microscopy and confocal laser scanning microscopy, respectively. Additionally, the checkerboard microdilution method was used to investigate the interactions between farnesol and antifungals (fluconazole, amphotericin B, caspofungin, itraconazole, terbinafine and 5-flurocytosine) against biofilms. The results showed decreased SMICs of farnesol and thinner biofilms in the farnesol-treated groups, indicating that farnesol inhibited the development of biofilms formed by the resistant strain. Furthermore, there were synergistic effects between farnesol and fluconazole/5-flurocytosine, while there were antagonistic effects between farnesol and terbinafine/itraconazole, respectively, on the biofilms formed by the resistant strains.

  16. Increased Excretion of C4-Carnitine Species after a Therapeutic Acetylsalicylic Acid Dose: Evidence for an Inhibitory Effect on Short-Chain Fatty Acid Metabolism

    Science.gov (United States)

    Mels, Catharina M. C.; Jansen van Rensburg, Peet; van der Westhuizen, Francois H.; Pretorius, Pieter J.; Erasmus, Elardus

    2011-01-01

    Acetylsalicylic acid and/or its metabolites are implicated to have various effects on metabolism and, especially, on mitochondrial function. These effects include both inhibitory and stimulatory effects. We investigated the effect of both combined and separate oral acetylsalicylic acid and acetaminophen administration at therapeutic doses on the urinary metabolite profile of human subjects. In this paper, we provided in vivo evidence, in human subjects, of a statistically significant increase in isobutyrylcarnitine after the administration of a therapeutic dose of acetylsalicylic acid. We, therefore, propose an inhibitory effect of acetylsalicylic acid on the short-chain fatty acid metabolism, possibly at the level of isobutyryl-CoA dehydrogenase. PMID:22084721

  17. Effect of cortisol on gonadotropin inhibitory hormone (GnIH) in the cinnamon clownfish, Amphiprion melanopus.

    Science.gov (United States)

    Choi, Young Jae; Habibi, Hamid R; Kil, Gyung-Suk; Jung, Min-Min; Choi, Cheol Young

    2017-04-01

    Hypothalamic peptides, gonadotropin-releasing hormone (GnRH) and gonadotropin inhibitory hormone (GnIH), play pivotal roles in the control of reproduction and gonadal maturation in fish. In the present study we tested the possibility that stress-mediated reproductive dysfunction in teleost may involve changes in GnRH and GnIH activity. We studied expression of brain GnIH, GnIH-R, seabream GnRH (sbGnRH), as well as circulating levels of follicle stimulating hormone (FSH), and luteinizing hormone (LH) in the cinnamon clownfish, Amphiprion melanopus. Treatment with cortisol increased GnIH mRNA level, but reduced sbGnRH mRNA and circulating levels of LH and FSH in cinnamon clownfish. Using double immunofluorescence staining, we found expression of both GnIH and GnRH in the diencephalon region of cinnamon clownfish brain. These findings support the hypothesis that cortisol, an indicator of stress, affects reproduction, in part, by increasing GnIH in cinnamon clownfish which contributes to hypothalamic suppression of reproductive function in A. melanopus, a protandrous hermaphroditic fish. Copyright © 2017 Elsevier Inc. All rights reserved.

  18. Secondary metabolites from Glycine soja and their growth inhibitory effect against Spodoptera litura.

    Science.gov (United States)

    Zhou, Yan-Ying; Luo, Shi-Hong; Yi, Ting-Shuang; Li, Chun-Huan; Luo, Qian; Hua, Juan; Liu, Yan; Li, Sheng-Hong

    2011-06-08

    The wild soybean (Glycine soja Sieb. et Zucc) has been reported to be relatively resistant to insect and pathogenic pests. However, the responsible secondary metabolites in the aerial part of this important plant are largely unknown. From the aerial part of G. soja, 13 compounds were isolated and identified, including seven isoflavonoids (1-7), a cyclitol (8), two sterol derivatives (9 and 10), and three triterpenoids (11-13). Compound 7 is a new isoflavonoid, and compounds 9 and 10 are reported as natural products for the first time. The growth inhibitory activity of 1, 3, 4, and 8 against the larvae of Spodoptera litura was investigated. The most abundant isoflavonoid in the aerial part of G. soja, daidzein (1), which could not be metabolized by S. litura, was found to inhibit the insect larvae growth significantly in 3 days after feeding diets containing the compound. Compounds 3, 4, and 8, which could be partially or completely metabolized, were inactive. Our results suggested that the isoflavonoid daidzein (1) might function as a constitutive defense component in G. soja against insect pests.

  19. Inhibitory effect of phloretin on α-glucosidase: Kinetics, interaction mechanism and molecular docking.

    Science.gov (United States)

    Han, Lin; Fang, Chun; Zhu, Ruixue; Peng, Qiang; Li, Ding; Wang, Min

    2017-02-01

    As the aglycone of phloridzin, phloretin belongs to dihydrochalcone with antioxidant, anti-inflammatory and antimicrobial activities. In this study, multispectroscopic techniques and molecular docking analysis were used to investigate the inhibitory activity and mechanisms of phloretin on α-glucosidase. The results showed that phloretin reversibly inhibited α-glucosidase in a mixed-type manner and the value of IC 50 was 31.26μgL -1 . The intrinsic fluorescence of α-glucosidase was quenched by the interactions with phloretin through a static quenching mechanism and spontaneously formed phloretin-α-glucosidase complex by the driving forces of van der Waals force and hydrogen bond. Atomic force microscope (AFM) studies and FT-IR measurements suggested that the interactions could change the micro-environments and conformation of the enzymes and the molecular docking analysis displayed the exact binding site of phloretin on α-glucosidase. These results indicated that phloretin is a strong α-glucosidase inhibitor, thus could be contribute to the improvement of diabetes mellitus. Copyright © 2016 Elsevier B.V. All rights reserved.

  20. Citrus pectin: characterization and inhibitory effect on fibroblast growth factor-receptor interaction.

    Science.gov (United States)

    Liu, Y; Ahmad, H; Luo, Y; Gardiner, D T; Gunasekera, R S; McKeehan, W L; Patil, B S

    2001-06-01

    This study was undertaken to characterize the pectin from four citrus species and to determine their in vitro inhibitory activities on the binding of fibroblast growth factor (FGF) to the FGF receptor (FGFR). Pectin from various parts of lemon, grapefruit, tangerine, and orange were isolated and characterized. Tangerine had the highest pectin content among the four citrus species. Segment membrane contained as much as or more pectin than flavedo/albedo. Anhydrogalacturonic content was highest in pectin from segment membrane of tangerine and flavedo/albedo of grapefruit. Lemon pectin contained the highest methoxyl content (MC), and grapefruit contained the largest proportion of lower molecular weight (lemon was the most potent inhibitor. The inhibition activity was significantly correlated with sugar content, MC, and size of pectin. Kinetic studies revealed a competitive nature of pectin inhibition with the heparin, a crucial component of the FGF signal transduction process. The observation that the heparin-dependent biological activity of FGF signal transduction is antagonized by citrus pectin should be further investigated for the use of these pectins as anti-growth factor agents for potential health benefits.

  1. Inhibitory effects of telmisartan on culture and proliferation of and Kv1.3 potassium channel expression in peripheral blood CD4+ T lymphocytes from Xinjiang Kazakh patients with hypertension

    Directory of Open Access Journals (Sweden)

    Sha-Sha Huang

    2016-10-01

    Full Text Available Introduction: Activation of T lymphocytes, for which potassium channels are essential, is involved in the development of hypertension. In this study, we explored the inhibitory effects of telmisartan on the culture and proliferation of and Kv1.3 potassium channel expression in peripheral blood CD4+ T lymphocytes derived from Xinjiang Kazakh patients with hypertension. Methods: CD4+ T-cell samples from hypertensive Kazakh patients and healthy Kazakh people were divided into healthy control, case control, telmisartan, and 4-aminopytidine groups. Changes in the expression levels of interleukin (IL-6 and IL-17 in the blood of the healthy control and case control subjects were detected by enzyme-linked immunosorbent assay. Peripheral blood CD4+ T lymphocytes were first activated and proliferated in vitro and then incubated for 0, 24, and 48 h under various treatment conditions. Thereafter, changes in CD4+ T-lymphocytic proliferation were determined using Cell Counting Kit-8 and microscope photography. Changes in messenger RNA (mRNA and protein expression of the Kv1.3 potassium channel in CD4+ T lymphocytes were detected using real-time quantitative polymerase chain reaction and Western blots, respectively. Results: The IL-6 and IL-17 expression levels were significantly higher in the blood of the hypertensive Kazakh patients than in the healthy Kazakh people. Telmisartan inhibited T-lymphocytic proliferation, as well as the mRNA and protein expression of the Kv1.3 potassium channel in CD4+ T lymphocytes, and the inhibitory effects were time-dependent, with the strongest inhibition observed after 48 h and significantly weaker inhibition observed after 24 h of treatment. Conclusions: Telmisartan may potentially regulate hypertensive inflammatory responses by inhibiting T-lymphocytic proliferation and Kv1.3 potassium channel expression in CD4+ T lymphocytes.

  2. Degree of synchronization modulated by inhibitory neurons in clustered excitatory-inhibitory recurrent networks

    Science.gov (United States)

    Li, Huiyan; Sun, Xiaojuan; Xiao, Jinghua

    2018-01-01

    An excitatory-inhibitory recurrent neuronal network is established to numerically study the effect of inhibitory neurons on the synchronization degree of neuronal systems. The obtained results show that, with the number of inhibitory neurons and the coupling strength from an inhibitory neuron to an excitatory neuron increasing, inhibitory neurons can not only reduce the synchronization degree when the synchronization degree of the excitatory population is initially higher, but also enhance it when it is initially lower. Meanwhile, inhibitory neurons could also help the neuronal networks to maintain moderate synchronized states. In this paper, we call this effect as modulation effect of inhibitory neurons. With the obtained results, it is further revealed that the ratio of excitatory neurons to inhibitory neurons being nearly 4 : 1 is an economic and affordable choice for inhibitory neurons to realize this modulation effect.

  3. A comparative study between inhibitory effect of L. lactis and nisin on important pathogenic bacteria in Iranian UF Feta cheese

    Directory of Open Access Journals (Sweden)

    Saeed Mirdamadi

    2015-02-01

    Full Text Available   Introduction : In the present study, the inhibitory effect of nisin-producing Lactococcus lactis during co-culture and pure standard nisin were assessed against selected foodborne pathogenes in growth medium and Iranian UF Feta cheese. In comparison L lactis, not only proves flavor but also plays a better role in microbial quality of Iranian UF Feta cheese as a model of fermented dairy products.   Materials and method s: L. lactis subsp. lactis as nisin producer strain, Listeria monocytogenes, Escherichia coli and Staphylococcus aureus as pathogenic strains were inoculated in Ultra-Filtered Feta cheese. Growth curve of bacterial strains were studied by colony count method in growth medium and UF Feta cheese separately and during co-culture with L. lactis. Nisin production was determined by agar diffusion assay method against susceptible test strain and confirmed by RP-HPLC analysis method.   Results : Counts of L. monocytogenes decreased in cheese sample containing L. lactis and standard nisin, to 103 CFU/g after 7 days and it reached to undetectable level within 2 weeks. S. aureus counts remained at its initial number, 105 CFU/g, after 7 days then decreased to 104 CFU/g on day 14 and it was not detectable on day 28. E. coli numbers increased in both treatments after 7 days and then decreased to 104 CFU/g after 28 days. Despite the increasing number of E. coli in growth medium containing nisin, due to the synergistic effect of nisin and other metabolites produced by Lactococcus lactis and starter cultures, the number of E. coli decreased with slow rate . Discussion and conclusion : The results showed, L. monocytogenes was inhibited by L. lactis before entering the logarithmic phase during co-culture. S. aureus was also inhibited during co-culture, but it showed less sensitivity in comparison with L. monocytogenes. However, the number of E. coli remained steady in co-culture with L. lactis. Also, we found that, in all cheese samples, E

  4. Inhibitory Effects of Soyeum Pharmacopuncture (SPP on LPS-induced Inflammation Related Cytokine Expressions of RAW 264.7 cells

    Directory of Open Access Journals (Sweden)

    Yoon Mi-Young

    2007-12-01

    Full Text Available Aim : This study was done to investigate whether SPP has inhibitory effects on the activation of RAW 264.7 cells. Method : In tumor necrosis factor-a (TNF-a/ interleukin-1b (IL-1b and IL-6, the mRNA expression of molecular indicators related to inflammatory changes of the Reumatoid Arthritis (RA were examined using quantitative real-time PCR. Results : The treatment of SPP significantly suppressed the expression of proinflammatory cytokines and chemokines such as TNF-a, IL-1b, IL-6 compared with the control. The expression of NOS-II was considerably reduced, which was accompanied by a reduction in the production of nitric oxide (NO. It also reduced the expression of TNF-αin serum of Balb/c mice compared with control group. Conclusion : SPP is an effective herbal material for suppressing the inflammation related cytokines of RAW 264.7 cells.

  5. Strongest Tropical cyclones: 1980-2009: A 30-year collage of Hurricane Satellite (HURSAT) data

    Data.gov (United States)

    National Oceanic and Atmospheric Administration, Department of Commerce — Strongest Tropical Cyclones: 1980-2009 poster - a 30-year collage of Hurricane Satellite (HURSAT) data. This poster depicts a series of 5 degree grids where within...

  6. Effects of curcuminoids identified in rhizomes of Curcuma longa on BACE-1 inhibitory and behavioral activity and lifespan of Alzheimer’s disease Drosophila models

    Science.gov (United States)

    2014-01-01

    Background Alzheimer’s disease (AD) is the most common type of presenile and senile dementia. The human β-amyloid precursor cleavage enzyme (BACE-1) is a key enzyme responsible for amyloid plaque production, which implicates the progress and symptoms of AD. Here we assessed the anti-BACE-1 and behavioral activities of curcuminoids from rhizomes of Curcuma longa (Zingiberaceae), diarylalkyls curcumin (CCN), demethoxycurcumin (DMCCN), and bisdemethoxycurcumin (BDMCCN) against AD Drosophila melanogaster models. Methods Neuro-protective ability of the curcuminoids was assessed using Drosophila melanogaster model system overexpressing BACE-1 and its substrate APP in compound eyes and entire neurons. Feeding and climbing activity, lifespan, and morphostructural changes in fly eyes also were evaluated. Results BDMCCN has the strongest inhibitory activity toward BACE-1 with 17 μM IC50, which was 20 and 13 times lower than those of CCN and DMCCN respectively. Overexpression of APP/BACE-1 resulted in the progressive and measurable defects in morphology of eyes and locomotion. Remarkably, supplementing diet with either 1 mM BDMCCN or 1 mM CCN rescued APP/BACE1-expressing flies and kept them from developing both morphological and behavioral defects. Our results suggest that structural characteristics, such as degrees of saturation, types of carbon skeleton and functional group, and hydrophobicity appear to play a role in determining inhibitory potency of curcuminoids on BACE-1. Conclusion Further studies will warrant possible applications of curcuminoids as therapeutic BACE-1 blockers. PMID:24597901

  7. Inhibitory effects of herbal constituents on P-glycoprotein in vitro and in vivo: Herb–drug interactions mediated via P-gp

    Energy Technology Data Exchange (ETDEWEB)

    Li, Xue, E-mail: lixue@imm.ac.cn; Hu, Jinping, E-mail: hujp@imm.ac.cn; Wang, Baolian, E-mail: wangbaolian@imm.ac.cn; Sheng, Li, E-mail: shengli@imm.ac.cn; Liu, Zhihao, E-mail: liuzhihao@imm.ac.cn; Yang, Shuang, E-mail: yangsh@imm.ac.cn; Li, Yan, E-mail: yanli@imm.ac.cn

    2014-03-01

    Modulation of drug transporters via herbal medicines which have been widely used in combination with conventional prescription drugs may result in herb–drug interactions in clinical practice. The present study was designed to investigate the inhibitory effects of 50 major herbal constituents on P-glycoprotein (P-gp) in vitro and in vivo as well as related inhibitory mechanisms. Among these herbal medicines, four constituents, including emodin, 18β-glycyrrhetic acid (18β-GA), dehydroandrographolide (DAG), and 20(S)-ginsenoside F{sub 1} [20(S)-GF{sub 1}] exhibited significant inhibition (> 50%) on P-gp in MDR1-MDCKII and Caco-2 cells. Emodin was the strongest inhibitor of P-gp (IC{sub 50} = 9.42 μM), followed by 18β-GA (IC{sub 50} = 21.78 μM), 20(S)-GF{sub 1} (IC{sub 50} = 76.08 μM) and DAG (IC{sub 50} = 77.80 μM). P-gp ATPase activity, which was used to evaluate the affinity of substrates to P-gp, was stimulated by emodin and DAG with K{sub m} and V{sub max} values of 48.61, 29.09 μM and 71.29, 38.45 nmol/min/mg protein, respectively. However, 18β-GA and 20(S)-GF{sub 1} exhibited significant inhibition on both basal and verapamil-stimulated P-gp ATPase activities at high concentration. Molecular docking analysis (CDOCKER) further elucidated the mechanism for structure–inhibition relationships of herbal constituents with P-gp. When digoxin was co-administered to male SD rats with emodin or 18β-GA, the AUC{sub 0−t} and Cmax of digoxin were increased by approximately 51% and 58%, respectively. Furthermore, 18β-GA, DAG, 20(S)-GF{sub 1} and Rh{sub 1} at 10 μM significantly inhibited CYP3A4/5 activity, while emodin activated the metabolism of midazolam in human liver microsomes. In conclusion, four herbal constituents demonstrated inhibition of P-gp to specific extents in vitro and in vivo. Taken together, our findings provided the basis for the reliable assessment of the potential risks of herb–drug interactions in humans. - Highlights: • Emodin, 18

  8. Inhibitory effects of herbal constituents on P-glycoprotein in vitro and in vivo: Herb–drug interactions mediated via P-gp

    International Nuclear Information System (INIS)

    Li, Xue; Hu, Jinping; Wang, Baolian; Sheng, Li; Liu, Zhihao; Yang, Shuang; Li, Yan

    2014-01-01

    Modulation of drug transporters via herbal medicines which have been widely used in combination with conventional prescription drugs may result in herb–drug interactions in clinical practice. The present study was designed to investigate the inhibitory effects of 50 major herbal constituents on P-glycoprotein (P-gp) in vitro and in vivo as well as related inhibitory mechanisms. Among these herbal medicines, four constituents, including emodin, 18β-glycyrrhetic acid (18β-GA), dehydroandrographolide (DAG), and 20(S)-ginsenoside F 1 [20(S)-GF 1 ] exhibited significant inhibition (> 50%) on P-gp in MDR1-MDCKII and Caco-2 cells. Emodin was the strongest inhibitor of P-gp (IC 50 = 9.42 μM), followed by 18β-GA (IC 50 = 21.78 μM), 20(S)-GF 1 (IC 50 = 76.08 μM) and DAG (IC 50 = 77.80 μM). P-gp ATPase activity, which was used to evaluate the affinity of substrates to P-gp, was stimulated by emodin and DAG with K m and V max values of 48.61, 29.09 μM and 71.29, 38.45 nmol/min/mg protein, respectively. However, 18β-GA and 20(S)-GF 1 exhibited significant inhibition on both basal and verapamil-stimulated P-gp ATPase activities at high concentration. Molecular docking analysis (CDOCKER) further elucidated the mechanism for structure–inhibition relationships of herbal constituents with P-gp. When digoxin was co-administered to male SD rats with emodin or 18β-GA, the AUC 0−t and Cmax of digoxin were increased by approximately 51% and 58%, respectively. Furthermore, 18β-GA, DAG, 20(S)-GF 1 and Rh 1 at 10 μM significantly inhibited CYP3A4/5 activity, while emodin activated the metabolism of midazolam in human liver microsomes. In conclusion, four herbal constituents demonstrated inhibition of P-gp to specific extents in vitro and in vivo. Taken together, our findings provided the basis for the reliable assessment of the potential risks of herb–drug interactions in humans. - Highlights: • Emodin, 18β-GA, DAG, and 20(S)-GF 1 significantly inhibited P-gp in vitro

  9. From cookies to carrots; the effect of inhibitory control training on children's snack selections.

    Science.gov (United States)

    Porter, L; Bailey-Jones, C; Priudokaite, G; Allen, S; Wood, K; Stiles, K; Parvin, O; Javaid, M; Verbruggen, F; Lawrence, N S

    2018-05-01

    Children consume too much sugar and not enough fruit and vegetables, increasing their risk of adverse health outcomes. Inhibitory control training (ICT) reduces children's and adults' intake of energy-dense foods in both laboratory and real-life settings. However, no studies have yet examined whether ICT can increase healthy food choice when energy-dense options are also available. We investigated whether a food-specific Go/No-Go task could influence the food choices of children aged 4-11, as measured by a hypothetical food choice task using healthy and unhealthy food images printed on cards. Participants played either an active game (healthy foods = 100% go, unhealthy foods = 100% no-go; Studies 1 & 2), a food control game (both healthy and unhealthy foods = 50% go, 50% no-go; Studies 1 & 2) or a non-food control game (sports equipment = 100% go, technology = 100% no-go; Study 2 only) followed by the choice task. In Study 2, food card choices were also measured before training to examine change in choices. A post-training real food choice task was added to check that choices made in the card-based task were representative of choices made when faced with real healthy and unhealthy foods. Overall, the active group chose the greatest number of healthy food cards. Study 2 confirmed that this was due to increases in healthy food card choice in this group only. Active group participants chose a greater number of healthy foods in the real food choice task compared to children in the non-food control group only. The results are discussed with reference to methodological issues and the development of future healthy eating interventions. Copyright © 2017 The Authors. Published by Elsevier Ltd.. All rights reserved.

  10. Anti-Oxidative and Cholinesterase Inhibitory Effects of Leaf Extracts and Their Isolated Compounds from Two Closely Related Croton Species

    Directory of Open Access Journals (Sweden)

    Johannes Van Staden

    2013-02-01

    Full Text Available A comparative evaluation of the antioxidant and acetylcholinesterase inhibitory activity of the leaf extracts of Croton gratissimus and Croton zambesicus (subgratissimus and compounds isolated from the extracts was carried out to determine their potential and suitability or otherwise as a substitute for each other in the management of oxidative and neurodegenerative conditions. Different antioxidant assays (DPPH, FRAP, β-carotene-linoleic and the lipid peroxidation models and the microplate assay for acetylcholinesterase (AChE inhibition were carried out separately to study the activities of the crude leaf extracts and four solvent fractions from each of the two Croton species. Bioassay guided fractionation was used to target antioxidant constituents of the crude extracts and ethyl acetate fractions of 20% aqueous methanol extract of C. gratissimus on silica gel and Sephadex LH-20 columns resulted in the isolation of kaempferol-3-O-β-6''(p-coumaroyl glucopyranoside (tiliroside, 2, apigenin-6-C-glucoside (isovitexin, 3 and kampferol (4. The extract of C. zambesicus yielded quercetin-3-O-β-6''(p-coumaroyl glucopyranoside-3'-methyl ether (helichrysoside- 3'-methyl ether, 1, kaempferol-3-O-β-6''(p-coumaroyl glucopyranoside (tiliroside, 2 and apigenin-6-C-glucoside (isovitexin, 3. Three of the isolated compounds and their different combinations were also included in the bioassays. In all the assays performed, the antioxidant capacity and AChE inhibitory effects of C. zambesicus extracts were weaker than those of C. gratissimus. This suggests that C. gratissimus may not be substituted by C. zambesicus, despite the similarity in some of their constituents. Generally, the combinations made from the isolated compounds showed better activities in most of the assays compared to the individual isolated compounds. This suggests mechanisms such as synergism and/or additive effects to be taking place. This study established low, moderate and high

  11. The inhibitory effect of Houttuynia cordata extract on stem cell factor-induced HMC-1 cell migration.

    Science.gov (United States)

    Kim, In Sik; Kim, Joo-Hwan; Kim, Jin Sook; Yun, Chi-Young; Kim, Dong-Hee; Lee, Ji-Sook

    2007-05-30

    Hottuynia cordata Thunb (Saururaceae; HC) is known as a therapeutic drug that has been used in traditional oriental medicine for the treatment of allergy. Mast cells play an important role in a variety of inflammatory diseases, and specifically asthma and atopy. In the present study, we investigated the effect of HC extracts on the migration of the human mast cell line, HMC-1, in response to stem cell factor (SCF). Treatment with HC extracts at a concentration of 10mug/ml for 24h showed no significant decrease in the survival rate of the HMC-1 cells. SCF showed the typical bell-shape curve for the HMC-1 cell chemoattraction with the peak of the curve at the SCF concentration of 100ng/ml. HC-1, which was the whole plant (Houttuynia cordata) extracted with 80% EtOH, and HC-3, which was the residue successively partitioned with EtOAc, both had inhibitory effects on HMC-1 cell movement. After the treatment with 10mug/ml HC-1 extract for 6 and 24h, the chemotactic index (CI) of HMC-1 cells decreased up to 74 and 63%, respectively. HC-3 extract treatment for 6 and 24h lowered the CI to 72 and 44%, respectively. The HC-1 and HC-3 extracts had no inhibitory effect on the mRNA and surface protein expressions of c-kit, SCF receptor. SCF mediated the chemotaxis signaling via NF-kappaB activation, and both extracts inhibited the activation. Therefore, our results indicate that HC-1 and HC-3 extracts decrease the chemotactic ability of HMC-1 cells in response to SCF by inhibiting the NF-kappaB activation, and these substances may be useful for treating mast cell-induced inflammatory diseases.

  12. A Bioactivity-Based Method for Screening, Identification of Lipase Inhibitors, and Clarifying the Effects of Processing Time on Lipase Inhibitory Activity of Polygonum Multiflorum

    Directory of Open Access Journals (Sweden)

    Yan-xu Chang

    2016-01-01

    Full Text Available Traditional Chinese medicine (TCM has been used for the treatment of many complex diseases. However, the bioactive components are always undefined. In this study, a bioactivity-based method was developed and validated to screen lipase inhibitors and evaluate the effects of processing on the lipase inhibitory activity of TCM by ultrahigh performance liquid chromatography coupled with quadrupole-time-of-flight mass spectrometry and fraction collector (UHPLC/Q-TOF-MS-FC. The results showed that both Polygonum multiflorum and processed P. multiflorum extracts had inhibitory effect against lipase with IC50 values of 38.84 μg/mL and 190.6 μg/mL, respectively. Stilbenes, phenolic acid, flavonoids, and anthraquinones were considered to be the potential lipase inhibitors. Eleven potential lipase inhibitors were simultaneously determined by UHPLC. Principal component analysis (PCA was employed in exploring the effects of processing time on lipase inhibitory activity of P. multiflorum. Compared with conventional methods, a bioactivity-based method could quantitatively analyze lipase inhibitory activity of individual constituent and provide the total lipase inhibitory activity of the samples. The results demonstrated that the activity integrated UHPLC/Q-TOF-MS-FC method was an effective and powerful tool for screening and identifying lipase inhibitors from traditional Chinese medicines.

  13. A Bioactivity-Based Method for Screening, Identification of Lipase Inhibitors, and Clarifying the Effects of Processing Time on Lipase Inhibitory Activity of Polygonum Multiflorum

    Science.gov (United States)

    Chang, Yan-xu; Ge, Ai-hua; Jiang, Yan; Teye Azietaku, John; Li, Jin; Gao, Xiu-mei

    2016-01-01

    Traditional Chinese medicine (TCM) has been used for the treatment of many complex diseases. However, the bioactive components are always undefined. In this study, a bioactivity-based method was developed and validated to screen lipase inhibitors and evaluate the effects of processing on the lipase inhibitory activity of TCM by ultrahigh performance liquid chromatography coupled with quadrupole-time-of-flight mass spectrometry and fraction collector (UHPLC/Q-TOF-MS-FC). The results showed that both Polygonum multiflorum and processed P. multiflorum extracts had inhibitory effect against lipase with IC50 values of 38.84 μg/mL and 190.6 μg/mL, respectively. Stilbenes, phenolic acid, flavonoids, and anthraquinones were considered to be the potential lipase inhibitors. Eleven potential lipase inhibitors were simultaneously determined by UHPLC. Principal component analysis (PCA) was employed in exploring the effects of processing time on lipase inhibitory activity of P. multiflorum. Compared with conventional methods, a bioactivity-based method could quantitatively analyze lipase inhibitory activity of individual constituent and provide the total lipase inhibitory activity of the samples. The results demonstrated that the activity integrated UHPLC/Q-TOF-MS-FC method was an effective and powerful tool for screening and identifying lipase inhibitors from traditional Chinese medicines. PMID:26925151

  14. In vitro inhibitory effects of plumbagin, the promising antimalarial candidate, on human cytochrome P450 enzymes.

    Science.gov (United States)

    Sumsakul, Wiriyaporn; Chaijaroenkul, Wanna; Na-Bangchang, Kesara

    2015-11-01

    To investigate the propensity of plumbagin to inhibit the three isoforms of human cytochrome P450 (CYP), i.e., CYP1A2, CYP2C19, and CYP3A4 using human liver microsomes in vitro. Inhibitory effects of plumbagin on the three human CYP isoforms were investigated using pooled human liver microsomes. Phenacetin O-deethylation, omeprazole hydroxylation and nifedipine oxidation were used as selective substrates for CYP1A2, CYP2C19 and CYP3A4 activities, respectively. Concentrations of paracetamol, 5-hydroxyomeprazole, and oxidized nifedipine were determined in microsomal incubation mixture using high-performance liquid chromatography. Plumbagin showed significant inhibitory effects on all CYP isoforms, but with the most potent activity on CYP2C19-mediated omeprazole hydroxylation. The IC50 (concentration that inhibits enzyme activity by 50%) values of plumbagin and nootkatone (selective inhibitor) for CYP2C19 were (0.78 ± 0.01) and (27.31 ± 0.66) μM, respectively. The inhibitory activities on CYP1A2-mediated phenacetin O-deethylation and CYP3A4-mediated nifedipine oxidation were moderate. The IC50 values of plumbagin and α-naphthoflavone (selective inhibitor) for CYP1A2 were (1.39 ± 0.01) and (0.02 ± 0.36) μM, respectively. The corresponding IC50 values of plumbagin and ketoconazole (selective inhibitor) for CYP3A4 were (2.37 ± 0.10) and (0.18 ± 0.06) μM, respectively. Clinical relevance of the interference of human drug metabolizing enzymes should be aware of for further development scheme of plumbagin as antimalarial drug when used in combination with other antimalarial drugs which are metabolized by these CYP isoforms. Copyright © 2015 Hainan Medical College. Production and hosting by Elsevier B.V. All rights reserved.

  15. Effects of excitatory and inhibitory neurotransmission on motor patterns of human sigmoid colon in vitro

    Science.gov (United States)

    Aulí, M; Martínez, E; Gallego, D; Opazo, A; Espín, F; Martí-Gallostra, M; Jiménez, M; Clavé, P

    2008-01-01

    Background and purpose: To characterize the in vitro motor patterns and the neurotransmitters released by enteric motor neurons (EMNs) in the human sigmoid colon. Experimental approach: Sigmoid circular strips were studied in organ baths. EMNs were stimulated by electrical field stimulation (EFS) and through nicotinic ACh receptors. Key results: Strips developed weak spontaneous rhythmic contractions (3.67±0.49 g, 2.54±0.15 min) unaffected by the neurotoxin tetrodotoxin (TTX; 1 μM). EFS induced strong contractions during (on, 56%) or after electrical stimulus (off, 44%), both abolished by TTX. Nicotine (1–100 μM) inhibited spontaneous contractions. Latency of off-contractions and nicotine responses were reduced by NG-nitro-L-arginine (1 mM) and blocked after further addition of apamin (1 μM) or the P2Y1 receptor antagonist MRS 2179 (10 μM) and were unaffected by the P2X antagonist NF279 (10 μM) or α-chymotrypsin (10 U mL−1). Amplitude of on- and off-contractions was reduced by atropine (1 μM) and the selective NK2 receptor antagonist Bz-Ala-Ala-D-Trp-Phe-D-Pro-Pro-Nle-NH2 (1 μM). MRS 2179 reduced the amplitude of EFS on- and off-contractions without altering direct muscular contractions induced by ACh (1 nM–1 mM) or substance P (1 nM–10 μM). Conclusions and implications: Latency of EFS-induced off-contractions and inhibition of spontaneous motility by nicotine are caused by stimulation of inhibitory EMNs coreleasing NO and a purine acting at muscular P2Y1 receptors through apamin-sensitive K+ channels. EFS-induced on- and off-contractions are caused by stimulation of excitatory EMNs coreleasing ACh and tachykinins acting on muscular muscarinic and NK2 receptors. Prejunctional P2Y1 receptors might modulate the activity of excitatory EMNs. P2Y1 and NK2 receptors might be therapeutic targets for colonic motor disorders. PMID:18846038

  16. Inhibitory effects of food additives derived from polyphenols on staphylococcal enterotoxin A production and biofilm formation by Staphylococcus aureus.

    Science.gov (United States)

    Shimamura, Yuko; Hirai, Chikako; Sugiyama, Yuka; Shibata, Masaharu; Ozaki, Junya; Murata, Masatsune; Ohashi, Norio; Masuda, Shuichi

    2017-12-01

    In this study, we examined the inhibitory effects of 14 food additives derived from polyphenol samples on staphylococcal enterotoxin A (SEA) production and biofilm formation by Staphylococcus aureus. Tannic acid AL (TA), Purephenon 50 W (PP) and Polyphenon 70A (POP) at 0.25 mg/mL and Gravinol®-N (GN), Blackcurrant polyphenol AC10 (BP), and Resveratrol-P5 (RT) at 1.0 mg/mL significantly decreased SEA production by S. aureus C-29 (p additives derived from polyphenols have viability to be used as a means to inhibit the enterotoxin production and control the biofilm formation of foodborne pathogens.

  17. The inhibitory effects of pudendal nerve stimulation on bladder overactivity in spinal cord injury dogs: is early stimulation necessary?

    Science.gov (United States)

    Chen, Guoqing; Liao, Limin; Dong, Qian; Ju, Yanhe

    2012-01-01

    To determine the inhibitory effects of pudendal nerve stimulation (5 Hz) on bladder overactivity at early and late stages of spinal cord injury in dogs. The study was performed in eight dogs with chronic spinal cord transection at the T9-T10 level. Group 1 (four dogs) underwent electrical stimulation of pudendal nerve one month after spinal cord transection. Group 2 (four dogs) underwent stimulation six months after spinal cord transection. The bladders were removed for histological examination of fibrosis after the stimulation. The bladder capacity and the compliance were significantly increased (p stimulation in group 1, but not in group 2. The nonvoiding contractions were inhibited in both groups by electrical stimulation. Collagen fiber was increased, while elastic fiber was significantly decreased (p stimulation can increase the bladder capacity and compliance only during the early period before the bladder wall becomes fibrosit and can inhibit the nonvoiding contraction during two stages. © 2012 International Neuromodulation Society.

  18. 5-Substituted-benzylsulfanyl-thiophene-2-sulfonamides with effective carbonic anhydrase inhibitory activity: Solution and crystallographic investigations.

    Science.gov (United States)

    Ivanova, Jekaterīna; Balode, Agnese; Žalubovskis, Raivis; Leitans, Janis; Kazaks, Andris; Vullo, Daniela; Tars, Kaspars; Supuran, Claudiu T

    2017-02-01

    A series of 5-substituted-benzylsulfanyl-thiophene-2-sulfonamides was prepared by reacting 5-bromo-thiophene-2-sulfonamide with 5-substituted-benzyl mercaptans. The new compounds were investigated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. The cytosolic human (h) isoforms hCA I was poorly inhibited by the new sulfonamides (K I s in the range of 683-4250nM), whereas hCA II, and the transmembrane, tumor associated isoforms hCA IX and XII were effectively inhibited in the subnanomolar-nanomolar range. A high resolution X-ray crystal structure of the adduct of hCA II with one of the new sulfonamides allowed us to rationalize the excellent inhibitory activity of these heterocyclic sulfonamides. Copyright © 2016 Elsevier Ltd. All rights reserved.

  19. Inhibitory effect of n-hexane: ethyl acetate fraction from Artemisia vulgaris L. on cell culture of oral epithelial carcinoma

    Directory of Open Access Journals (Sweden)

    Ira Arundina

    2009-03-01

    Full Text Available Background: Sudamala herb (Artemisia vulgaris L. is often used in society as an anti tumor for organs of digestive system including oral cavity. Nevertheless, there are still no further scientific researches on active materials which can be used as anti carcinogen in oral cavity. Most of anti carcinogens are actually obtained from the genus Artemisia. Moreover, in Indonesia, the species of the genus Artemisia that grows the most is Artemisia vulgaris L. The problem of this research, however, is that the effect of n-hexane fraction: ethyl acetate from Artemisia vulgaris L. towards the decreasing of oncogene in oral squamous cell carcinoma is still indefinite. Purpose: The objective of this research is to explain the effect of giving n-hexane : ethyl acetate (3:7 fraction containing terpenoid from Artemisia vulgaris L. towards the decreasing of oncogene in oral epithelial carcinoma cell line. Methods: The method of this research is laboratory experimental research by using squamous cell carcinoma of oral cavity on cell culture. The inhibitory percentage test in vitro, furthermore, is taken during the analysis. The result then is analyzed by probit analysis with drawing relation curve between the inhibitory percentage and concentration. Result: The result of n-hexane : ethyl acetate (3:7 fraction containing terpenoid from Artemisia vulgaris L. has the smallest IC50, 3.902 μg/ml, less than 20 μg/ml suitable with NCI criteria; thus, it can potentially be used as anti carcinogen. Conclusion: There is the decreasing of oncogenes after being given n-hexane : ethyl acetate (3:7 fraction containing terpenoid from Artemisia vulgaris L. towards oral epithelial carcinoma cell line.

  20. Caregiver burden: the strongest predictor of self-rated health in caregivers of patients with dementia.

    Science.gov (United States)

    Abdollahpour, Ibrahim; Nedjat, Saharnaz; Noroozian, Maryam; Salimi, Yahya; Majdzadeh, Reza

    2014-09-01

    People having dementia need help and supervision to perform their activities of daily living. This responsibility is usually imposed on family members who endure a great burden, leading to undesirable health outcomes. The aims of our study were to measure caregivers' health as well as identify its adjusted relevant predictors. One hundred and fifty three registered patients and their caregivers from Iranian Alzheimer Association were included in this cross-sectional study through sequential sampling. Self-rated health (SRH) was measured using a single question with Likert-type scale ranging from very bad (1) to very good (5). The multiple linear regression model was applied to determine the adjusted associations between independent variables under study and SRH. The mean caregiver SRH level was 3.03. Of the participant caregivers, 29% were either unsatisfied or very unsatisfied with their health level. In the final regression model, SRH showed a direct significant association with the patient's number of children but an inverse significant association with the marital status (married patients), patient's age, and caregiver burden. Caregiver burden was not only significantly associated with poor SRH after removing the effect of the other covariates but it was also recognized as the strongest predictor of caregivers' SRH. Therefore, it seems that development of intervention programs, in order to reduce caregiver burden, can be considered as important step in promoting caregivers' health level. © The Author(s) 2014.

  1. Effects of incentives, age, and behavior on brain activation during inhibitory control: A longitudinal fMRI study

    Directory of Open Access Journals (Sweden)

    David J. Paulsen

    2015-02-01

    Full Text Available We investigated changes in brain function supporting inhibitory control under age-controlled incentivized conditions, separating age- and performance-related activation in an accelerated longitudinal design including 10- to 22-year-olds. Better inhibitory control correlated with striatal activation during neutral trials, while Age X Behavior interactions in the striatum indicated that in the absence of extrinsic incentives, younger subjects with greater reward circuitry activation successfully engage in greater inhibitory control. Age was negatively correlated with ventral amygdala activation during Loss trials, suggesting that amygdala function more strongly mediates bottom-up processing earlier in development when controlling the negative aspects of incentives to support inhibitory control. Together, these results indicate that with development, reward-modulated cognitive control may be supported by incentive processing transitions in the amygdala, and from facilitative to obstructive striatal function during inhibitory control.

  2. Combined EGFR- and notch inhibition display additive inhibitory effect on glioblastoma cell viability and glioblastoma-induced endothelial cell sprouting in vitro

    DEFF Research Database (Denmark)

    Staberg, Mikkel; Michaelsen, Signe Regner; Olsen, Louise Stobbe

    2016-01-01

    . Inhibition of EGFR and Notch signaling was achieved using either Iressa (gefitinib) or the gamma-secretase inhibitor DAPT. Our data showed that DAPT combined with Iressa treatment displayed increased inhibitory effect on cell viability and abrogated expression and activation of major pro-survival pathways....... Similarly, the combinational treatment significantly increased abrogation of GBM-induced endothelial cell sprouting suggesting reduced GBM angiogenesis. CONCLUSION: This study finds that simultaneous targeting of notch and EGFR signaling leads to enhanced inhibitory effects on GBM-induced angiogenesis...

  3. Inhibitory Effect of the root of Polygala tenuifolia on Bradykinin and ...

    African Journals Online (AJOL)

    Results: Administration of the Polygala tenuifolia extract at 100 mg/kg dose produced significant analgesic effect on acetic acid-induced writhing (97 % inhibition) but its effect in the tail-flick test was not significant (p < 0.05). In addition, the extract exerted significant anti-inflammatory effect in the rat paw edema model (8 to 33 ...

  4. Annona muricata leaves have strongest cytotoxic activity against breast cancer cells

    Directory of Open Access Journals (Sweden)

    Susi Endrini

    2014-12-01

    Full Text Available Background Plant-derived herbal compounds have a long history of clinical use, better patient tolerance and acceptance. They are freely available natural compounds that can be safely used to prevent various ailments. Plants have been the basis of traditional medicine throughout the world for thousands of years and are providing mankind with new remedies. The objective of this study was to determine the cytotoxicity of soursop (Anona muricata Linn leaves and pearl grass (Hedyotis corymbosa (L. Lam. on the hormone-dependent human breast carcinoma Michigan Cancer Foundation-7 (MCF-7 cell line. Methods This study used two types of solvents (water and ethanol in the extraction process and two incubation times (24 hours and 48 hours in the MTT assays to analyze the cytotoxic effects of both plants. Results Preliminary results showed that the ethanolic extract of soursop leaves (SE displayed cytotoxic effects against MCF-7 on 24- and 48-hour incubation times with IC50 values of 88.788 ìg/ml and 14.678 mg/ml, respectively. Ethanolic pearl grass extract (PE showed similar results, with IC50 values of 65.011 mg/ml on 24-hour incubation time and 52.329 mg/ml on 48-hour incubation time against MCF-7 cell line. However, the water extract of both plants displayed lower cytotoxic effect against MCF-7 cell line. Conclusion The ethanolic extract of both plants displayed cytotoxic effect against MCF-7. Soursop (Anona muricata Linn leaves have the strongest cytotoxic activity against MCF-7 breast cancer cell line.

  5. Annona muricata leaves have strongest cytotoxic activity against breast cancer cells

    Directory of Open Access Journals (Sweden)

    Susi Endrini

    2015-12-01

    Full Text Available BACKGROUND Plant-derived herbal compounds have a long history of clinical use, better patient tolerance and acceptance. They are freely available natural compounds that can be safely used to prevent various ailments. Plants have been the basis of traditional medicine throughout the world for thousands of years and are providing mankind with new remedies. The objective of this study was to determine the cytotoxicity of soursop (Anona muricata Linn leaves and pearl grass (Hedyotis corymbosa (L. Lam. on the hormone-dependent human breast carcinoma Michigan Cancer Foundation-7 (MCF-7 cell line. METHODS This study used two types of solvents (water and ethanol in the extraction process and two incubation times (24 hours and 48 hours in the MTT assays to analyze the cytotoxic effects of both plants. RESULTS Preliminary results showed that the ethanolic extract of soursop leaves (SE displayed cytotoxic effects against MCF-7 on 24- and 48-hour incubation times with IC50 values of 88.788 μg/ml and 14.678 μg/ml, respectively. Ethanolic pearl grass extract (PE showed similar results, with IC50 values of 65.011 μg/ ml on 24-hour incubation time and 52.329 μg/ml on 48-hour incubation time against MCF-7 cell line. However, the water extract of both plants displayed lower cytotoxic effect against MCF-7 cell line. CONCLUSION The ethanolic extract of both plants displayed cytotoxic effect against MCF-7. Soursop (Anona muricata Linn leaves have the strongest cytotoxic activity against MCF-7 breast cancer cell line.

  6. Comparative evaluation of inhibitory effect of curcumin and doxycycline on matrix metalloproteinase-9 activity in chronic periodontitis

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    Sanjeela Rakshith Guru

    2017-01-01

    Full Text Available Background and Objectives: The pathogenesis of inflammatory periodontal diseases essentially involves degradation of extracellular matrix molecules, and collagen breakdown and matrix metalloproteinases (MMPs are proteinases primarily involved in this process. It is known that doxycycline downregulates MMP activity. Curcumin has anti-inflammatory effect and also downregulates MMP activity. Thus, a study was conducted to evaluate the anti-inflammatory effect of curcumin by its inhibition of MMP-9 activity and compare the same with doxcycline, which has known anticollagenase activity. Subjects and Methods: Gingival tissue samples were obtained from thirty patients diagnosed with chronic periodontitis. The tissue extracts were treated with Curcumin and doxycycline and inhibition of MMP-9 analyzed by gelatinzymography. Gels obtained were stained with Coomassie Brilliant Blue, and enzymatic activities detected as bands of gelatinlysis against blue background. Relative MMP-9 levels were measured by scanning the clear zones and analyzing the percentage inhibition. Results: Results showed that MMP-9 activity was significantly decreased by both the drugs. Curcumin showed 61.01% reduction in the MMP-9 activity at 1500 μg/ml concentration and doxycycline showed 59.58% reduction in the MMP-9 activity at 300 μg/ml concentration. Conclusion: The current study showed that curcumin has inhibitory effect on polymorphonuclear leukocyte-type MMP-9 involved in matrix degradation in periodontitis. Since Curcumin has a potent anti-inflammatory effect, it may have therapeutic potential as a host modulation agent in periodontal diseases.

  7. A comparison inhibitory effects of cisplatin and MNPs-PEG-cisplatin on the adhesion capacity of bone metastatic breast cancer.

    Science.gov (United States)

    Mokhtari, Mohammad Javad; Koohpeima, Fatemeh; Mohammadi, Hadi

    2017-10-01

    To date, high mortality in women due to malignancy breast cancer related to the metastasis to the bone is a significant challenge. As, magnetic nanoparticles (MNPs) conjugated with the biocompatible polymers was employed for the delivery of some hydrophobic anticancer agents, the main aim of the current research was to assess whether cisplatin-loaded MNPs enhanced the anticancer effect of free cisplatin in breast cancer cells. MNPs decorated with PEG were synthesized by an improved coprecipitation technique, and then cisplatin was loaded onto the MNPs via a simple mixing method. Afterward, its morphology, size, chemical structure, magnetic property, hydrodynamic diameter, zeta potential, and crystal structure were characterized by scanning and transmittance electron microscopy, Fourier transforms infrared spectroscopy, vibrating sample magnetometer, dynamic light scattering, and X-ray powder diffraction and flame atomic absorption spectroscopy respectively. Additionally, the effects of cisplatin and MNPs-PEG-cisplatin on viability, migration and adhesion capacity of T47D cells were investigated by evaluating α2-integrin and β1-integrin; mRNAs were assessed by real-time RT-PCR. Consequently, the in vitro assay results showed a considerable dose-dependent inhibitory effect of cisplatin and MNPs-PEG-cisplatin on proliferation, migration, and adhesion of T47D cells. Finally, current research was shown that MNPs-PEG-cisplatin strongly increased anticancer effects compared with free cisplatin in the T47D cell line. © 2017 John Wiley & Sons A/S.

  8. Inhibitory effect of 660-nm LED on melanin synthesis in in vitro and in vivo.

    Science.gov (United States)

    Oh, Chang Taek; Kwon, Tae-Rin; Choi, Eun Ja; Kim, Soon Re; Seok, Joon; Mun, Seog Kyun; Yoo, Kwang Ho; Choi, Yeon Shik; Choi, Sun Young; Kim, Beom Joon

    2017-01-01

    Skin hyperpigmentary disorders including postinflammatory hyperpigmentation, melasma, solar lentigines, and conditions like freckles are common. The light-emitting diodes (LEDs) are the latest category of nonthermal and noninvasive phototherapy to be considered in skin pigmentation disorder treatment. The purpose of this study was to investigate the effects of 660-nm LED on inhibition of melanogenesis. We investigated whether a 660-nm LED affected melanin synthesis in in vitro and in vivo models, and we explored the mechanisms involved. The inhibitory effect of 660-nm LED on melanin synthesis was evaluated in B16F10 cells and HRM-2 melanin-possessing hairless mice were used to evaluate the antimelanogenic effects of 660-nm LED. Interestingly, 660-nm LED inhibited alpha-melanocyte-stimulating hormone-induced tyrosinase activity in B16F10 cells. We also found that 660-nm LED decreased MITF and tyrosinase expression and induced the activation of ERK. These findings suggest that the depigmenting effects of 660-nm LED result from downregulation of MITF and tyrosinase expression due to increased ERK activity. The 660-nm LED reduced UVB-induced melanogenesis in the skin of HRM-2 via downregulation of tyrosinase and MITF. These findings suggest 660-nm LED is a potentially depigmentation strategy. © 2016 John Wiley & Sons A/S. Published by John Wiley & Sons Ltd.

  9. The growth inhibitory effects of cadmium and copper on the MDA-MB468 human breast cancer cells

    Directory of Open Access Journals (Sweden)

    Mojtaba Panjehpour

    2010-01-01

    Full Text Available Background: Cadmium chloride is an important occupational and environmental pollutant. However, it can also be anti-carcinogenic under certain conditions. Copper, an essential trace element, has the ability to generate reactive oxygen species and induce cell apoptosis. This study was aimed to determine the growth inhibitory effects of cadmium and copper on the MDA-MB468 human breast cancer cells. Methods: By using MTT cell viability test, treatment of monolayer cell cultures with different metal concentrations (1-1000 μM showed a significant dose dependent decrease (p < 0.05 of viable cells in different times. Results: A considerable cytotoxicity was observed for CdCl2 at 200 μM and 1 μM after 48 and 72 hours incubations, respectively. The highest concentration of CuCl2 (1000 μM had little cytotoxic effects after 48 hours incubation period, but 1 μM of CuCl2 revealed a considerable cytotoxicity after 72 hours. The maximum synergic cytotoxic effect was observed at 0.5 μM of both metals. Conclusions: The results of the present study indicate that cytotoxic effect of CuCl2 is somehow lesser than that of CdCl2. This may be due to vital role of copper which is not known for cadmium so far.

  10. ON POTENTIAL REPRESENTATIONS OF THE DISTRIBUTION LAW OF RARE STRONGEST EARTHQUAKES

    Directory of Open Access Journals (Sweden)

    M. V. Rodkin

    2014-01-01

    'bend-down' is described by the finite distribution law, i.e. the bend-down occurs more efficiently than it is envisaged in the commonly used model developed by Y. Kagan (which treats the bend-dawn as an exponential decay law. However, despite the finiteness of the distribution law, density of magnitudes decline quite slowly in the area close to the maximum possible Мmах event as (Мmах – Mn, where n varies in the range between 4 and 6 in the majority of cases. As a result Мmах value can be estimated only with a large error. In rare cases, if the space-and-time area under study contains higher number of strongest earthquakes, the empirical distribution law becomes close to the exponential law; in this case n value is quite high, and Мmах values becomes unstable and tend to infinite growth.In our study, the distribution law of strongest earthquakes was investigated by the methods based on the extreme values theory (world data and several regional catalogues were examined, and the results of calculation do not reveal cases of  occurrence of characteristic events. However, such a seismic regime was revealed in a number of cases from paleoseismicity data and from some instrumental regional catalogues. Conditions providing for the occurrence of characteristic earthquakes are studied here using the multiplicative cascade model. According to [Rodkin, 2011], this model provides the simulation of all known regularities of seismic regime, such as a decrease in b-value in the vicinity of strong earthquakes, development of aftershock power cascade, and existence of seismic cycle and foreshock activity. This article considers an extension of the cascade model by adding of non-linear members in the kinetic cascade equation in order to describe effects of the 'bend-down' of the earthquake recurrence curve and the characteristic earthquakes occurrence. It is shown that in terms of the multiplicative cascade model, the occurrence of characteristic earthquakes is connected

  11. Neuroprotective effect of seaweeds inhabiting South Indian coastal area (Hare Island, Gulf of Mannar Marine Biosphere Reserve): Cholinesterase inhibitory effect of Hypnea valentiae and Ulva reticulata.

    Science.gov (United States)

    Suganthy, N; Karutha Pandian, S; Pandima Devi, K

    2010-01-14

    Alzheimer's disease (AD) is the most common form of dementia, which is one of the four leading causes of death in developed nations. Until date the only symptomatic treatment for this disease is based on the "cholinergic hypothesis" where the drugs enhance acetylcholine levels in the brain by inhibiting acetylcholinesterase (AChE). In the course for screening cholinesterase inhibitors about eight seaweeds, with wide pharmaceutical applications, were collected from Hare Island, Gulf of Mannar, Marine Biosphere Reserve, Tamil Nadu, India. Inhibitory effect of methanol extract of the seaweeds was studied in vitro by incubating various concentration of the extract with AChE or butyryl cholinesterase (BuChE) and assessing their activities by Ellman's colorimetric method. Kinetic parameters like IC(50), K(i) and V(max) were also analyzed. The results showed that of the eight seaweeds screened Hypnea valentiae, Padina gymnospora, Ulva reticulata and Gracilaria edulis exhibited inhibitory activity to AChE with IC(50) value of 2.6, 3.5, 10 and 3mg/ml respectively, while H. valentiae, Enteromorpha intestinalis, Dictyota dichotoma and U. reticulata showed 50% inhibition to BuChE at concentration 3.9, 7, 6.5 and 10mg/ml respectively. The inhibitory activities of the seaweed extracts were comparable to the standard drug donepezil. Enzyme kinetic analysis showed that algal extracts exhibited mixed type inhibition (partial noncompetitive inhibition). Copyright 2009 Elsevier Ireland Ltd. All rights reserved.

  12. Effects of Nicotine on Attention and Inhibitory Control in Healthy Nonsmokers

    OpenAIRE

    Wignall, Nicholas D.; de Wit, Harriet

    2011-01-01

    Nicotine improves cognitive functioning in smokers and psychiatric populations, but its cognitive-enhancing effects in healthy nonsmokers are less well understood. Nicotine appears to enhance certain forms of cognition in nonsmokers, but its specificity to subtypes of cognition is not known. This study sought to replicate and extend previous findings on the effects of nicotine on cognitive performance in healthy nonsmokers. Healthy young adults (N=40, 50% female) participated in a placebo-con...

  13. PPAR-gamma-independent inhibitory effect of rosiglitazone on glucose synthesis in primary cultured rabbit kidney-cortex tubules.

    Science.gov (United States)

    Derlacz, Rafal A; Hyc, Karol; Usarek, Michal; Jagielski, Adam K; Drozak, Jakub; Jarzyna, Robert

    2008-10-01

    Therapeutic effect of rosiglitazone has been reported to result from an improvement of insulin sensitivity and inhibition of glucose synthesis. As the latter process occurs in both liver and kidney cortex the aim of this study was to elucidate the rosiglitazone action on glucose formation in both tissues. Primary cultured cells of both liver and kidney cortex grown in defined medium were use throughout. To identify the mechanism responsible for drug-induced changes, intracellular gluconeogenic intermediates and enzyme activities were determined. In contrast to hepatocytes, the administration of a 10 micromol/L concentration of rosiglitazone to renal tubules resulted in about a 70% decrease in the rate of gluconeogenesis, accompanied by an approximately 75% decrease in alanine utilization and a 35% increase in lactate synthesis. The effect of rosiglitazone was not abolished by GW9662, the PPAR-gamma irreversible antagonist, indicating that this action is not dependent on PPAR-gamma activation. In view of rosiglitazone-induced changes in gluconeogenic intermediates and a diminished incorporation of 14CO2 into pyruvate, it is likely that the drug causes a decline in flux through pyruvate carboxylase and (or) phosphoenolpyruvate carboxykinase. It is likely that the hypoglycemic action of rosiglitazone is PPAR-gamma independent and results mainly from its inhibitory effects on renal gluconeogenesis.

  14. The inhibitory effect of Thymus vulgaris extracts on the planktonic form and biofilm structures of six human pathogenic bacteria.

    Science.gov (United States)

    Mohsenipour, Zeinab; Hassanshahian, Mehdi

    2015-01-01

    Microorganisms are responsible for many problems in industry and medicine because of biofilm formation. Therefore, this study was aimed to examine the effect of Thymus vulgaris (T. vulgaris) extracts on the planktonic form and biofilm structures of six pathogenic bacteria. Antimicrobial activities of the plant extracts against the planktonic form of the bacteria were determined using the disc diffusion method. MIC and MBC values were evaluated using macrobroth dilution technique. Anti-biofilm effects were assessed by microtiter plate method. According to disc diffusion test (MIC and MBC), the ability of Thymus vulgaris (T. vulgaris ) extracts for inhibition of bacteria in planktonic form was confirmed. In dealing with biofilm structures, the inhibitory effect of the extracts was directly correlated to their concentration. Except for the inhibition of biofilm formation, efficacy of each extract was independent from type of solvent. According to the potential of Thymus vulgaris (T. vulgaris) extracts to inhibit the test bacteria in planktonic and biofilm form, it can be suggested that Thymus vulgaris (T. vulgaris) extracts can be applied as antimicrobial agents against the pathogenic bacteria particularly in biofilm forms.

  15. Phorbol ester potentiates the growth inhibitory effects of troglitazone via up-regulation of PPARγ in A549 cells

    International Nuclear Information System (INIS)

    Kim, Hyo Jung; Woo, Im Sun; Kang, Eun Sil; Eun, So Young; Kim, Gil Hyeong; Ham, Sun Ah; Kim, Hye Jung; Lee, Jae Heun; Chang, Ki Churl; Kim, Jin-Hoi; Lee, Hoon Taek; Seo, Han Geuk

    2006-01-01

    The activation of peroxisome proliferator-activated receptor gamma (PPARγ) has been shown to induce growth arrest and differentiation of various cancer cells. In the current study, we investigated the effect of 12-O-tetradecanoylphorbol-13-acetate (TPA) on the expression of PPARγ and proliferation of A549 cells. TPA elicited a dose- and time-dependent increase in PPARγ mRNA and protein levels. PPARγ expression in response to TPA was attenuated by pretreatment with bisindolylmaleimide I, N-acetyl-L-cysteine (NAC) and PD98059. TPA-induced protein kinase C (PKC) activation was linked to the generation of reactive oxygen species (ROS), both of which were indispensable for PPARγ expression in A549 cells. Pretreatment with bisindolylmaleimide I or NAC blocked TPA-induced phosphorylation of extracellular signal-regulated kinase (ERK), suggesting that ERK-mediated signaling is also involved in the induction of PPARγ. Furthermore, the growth inhibitory effect of troglitazone was significantly potentiated by prolonged incubation with TPA and was attenuated in the presence of GW9662, a specific inhibitor of PPARγ. These effects were associated with an induction of cell cycle arrest at G /G 1 phase, which was accompanied by the induction of p21 Waf1/Cip1 expression and decreased cyclin D1 expression. Taken together, these observations indicate that TPA synergizes with PPARγ ligand to inhibit cell growth through up-regulation of PPARγ expression

  16. The Inhibitory Effects of Aqueous Extract from Guava Twigs, Psidium guajava L., on Mutation and Oxidative Damage

    Directory of Open Access Journals (Sweden)

    Zhi-Chyang Kang

    2013-01-01

    Full Text Available This study examines the inhibitory effects of the aqueous extract from guava twigs (GTE, Psidium guajava L., on mutation and oxidative damage. The results show that GTE inhibits the mutagenicity of 4-nitroquinoline-N-oxide (4-NQO, a direct mutagen, and 2-aminoanthracene (2-AA, an indirect mutagen, toward Salmonella typhimurium TA 98 and TA 100. In addition, GTE shows radical scavenging, reducing activities, tyrosinase inhibition, and liposome protection effects. Meanwhile, GTE in the range of 0.1–0.4 mg/mL protects liver cells from tert-butyl-hydroperoxide-(t-BHP- induced cytotoxicity. Furthermore, the cytotoxicity inhibition of GTE in the t-BHP-treated cells was demonstrated in a dose-dependent manner. High-performance liquid chromatography analysis suggests that the major phenolic constituents in GTE are gallic acid, ferulic acid, and myricetin. These active phenolic components may contribute to the biological protective effects of GTE in different models. The data suggest that GTE exhibiting biological activities can be applied to antimutation, antityrosinase, and antioxidative damage.

  17. [Inhibitory effect of 17-AAG combined with paclitaxel on proliferation of esophageal squamous cell carcinoma Eca-109 cells in vitro].

    Science.gov (United States)

    Chen, Size; Chen, Xuemei; Li, Yuqi; Yang, Shu; Mo, Xianyi; Zhang, Fan; Mo, Kailan; Ding, Ying

    2015-06-01

    To investigate the effect of 17-AAG combined with paclitaxel (PTX) on the proliferation and apoptosis of esophageal squamous cell carcinoma cell line Eca-109 in vitro. Eca-109 cells were treated with 17-AAG and PTX either alone or in combination. The proliferation of Eca-109 cells was detected by MTT assay, and the cell cycle changes and cell apoptosis were determined by flow cytometry. Compared with the control group, both 17-AAG and PTX significantly inhibited the proliferation of Eca-109 cells. A combined treatment of the cells with 0.5 µmol/L PTX and 0.625 µmol/L 17-AAG produced an obviously stronger inhibitory effect on the cell proliferation than either of the agents used alone (PAAG and PTX used alone caused Eca-109 cell cycle arrest in G2/M phase and S phase, respectively, and their combined use caused cell cycle arrest in both G2/M and S phases. The cell apoptosis rates of Eca-109 cells treated with 17-AAG, PTX and their combination were 4.52%, 10.91%, and 29.88%, respectively, all significantly higher than that in the control group (1.32%); the combined treatment resulted in a distinct apoptotic peak that was significantly higher than that caused by either of the agents alone. 17-AAG and PTX can inhibit cell proliferation and promote apoptosis of Eca-109 cells, and their combination produces stronger effects in inhibiting cell proliferation and increasing cell apoptosis.

  18. The inhibitory effect of different concentrations of KH902 eye drops on corneal neovascularization induced by alkali burn

    Directory of Open Access Journals (Sweden)

    Yan Wu

    2017-01-01

    Full Text Available Purpose: The aim of this study was to evaluate the inhibitory effect of different concentrations of KH902 eye drops on rabbit corneal neovascularization (CNV induced by alkali burn. Methods: Forty-eight adult rabbits were randomized into four groups after alkali burning: Group A (2.5 mg/ml, Group B (5 mg/ml, and Group C (10 mg/ml by different concentrations of KH902 eye drops and Group D by saline solution as control with three times a day for 2 weeks. At days 7, 14, and 28, the anterior segment photographs, confocal microscopy, and histopathology were performed to evaluate corneal opacity, neovascularization, inflammatory cell density, vessel size, and edema. Immunohistochemistry was applied to analyze the vascular endothelial growth factor (VEGF level. Results: (1 The CNV in the medicine-treated groups showed a reduction without obvious corneal side effects histologically. (2 Compared to the control group, the three medicine-treated groups showed a reduction in the VEGF levels and CNV areas on days 7, 14, and 28 and in the inflammatory cell density on days 14 and 28 (P 0.05. Conclusion: KH902 eye drops in lower concentration showed an obvious reduction of the CNV growing for rabbit corneal alkali burn without side effects.

  19. Inhibitory effect of cranberry extract on periodontopathogenic biofilm: An integrative review

    Directory of Open Access Journals (Sweden)

    Annie Karoline Bezerra de Medeiros

    2016-01-01

    Full Text Available Background: Combating biofilm-dependent oral infections involves the use of synthetic antibiotics, which are often associated with bacterial resistance and adverse effects. As a result, herbs such as cranberry have emerged as an alternative treatment. The aim of this study was to evaluate, through an integrative literature review, the effectiveness of cranberry extract on cultures and biofilms of periodontopathogenic bacteria. Materials and Methods: In vitro and in vivo studies evaluating the action of cranberry extract on the growth, coaggregation and formation of periodontopathogenic bacteria and periodontal biofilm were identified. Searches were carried out in the “Cochrane Library,” “MEDLINE,” “Web of Science,” “Scopus,” “LILACS,” “Scielo,” and “Google Scholar” databases, using the terms: “vaccinium macrocarpon;” “cranberries;” “cranberry;” “biofilms;” “periodontitis;” “chronic periodontitis;” “aggressive periodontitis;” “periodontal diseases;” and “periodont*.” Results: a low number of studies evaluating the effectiveness of cranberry extract on periodontal disease were found, and no human studies were identified. In general, the eight studies included in the revision found that the compounds effectively inhibited the formation of a biofilm of Porphyromonas gingivalis and Fusobacterium nucleatum at concentrations equal or superior to 62.5 μg/ml, but did not significantly inhibit bacterial growth or promote the breakdown of preformed biofilm. Conclusions: while most of the studies presented certain methodological limitations, they did identify an inhibiting effect of cranberry on periodontal bacteria. These results serve as support for the development of further studies evaluating the most effective vehicle and ideal concentration that can be used without causing adverse effects on oral tissues.

  20. Study of Possible Mechanisms Involved in the Inhibitory Effects of Coumarin Derivatives on Neutrophil Activity

    Science.gov (United States)

    Drábiková, Katarína; Perečko, Tomáš; Nosál', Radomír; Harmatha, Juraj; Šmidrkal, Jan; Jančinová, Viera

    2013-01-01

    To specify the site of action of the synthetic coumarin derivatives 7-hydroxy-3-(4′-hydroxyphenyl) coumarin (HHC) and 7-hydroxy-3-(4′-hydroxyphenyl) dihydrocoumarin (HHDC), we evaluated their effects on extra- and intracellular reactive oxygen species (ROS) formation in phorbol-myristate-13-acetate (PMA) stimulated human neutrophils. We studied also the effects of HHC and HHDC on possible molecular mechanisms which participate in the activation of NADPH oxidase, that is, on PKC activity, on phosphorylation of some PKC isoforms (α, βII, and δ), and on phosphorylation of the NADPH oxidase subunit p40phox. Without affecting cytotoxicity, both coumarines tested were effective inhibitors/scavengers of ROS produced by neutrophils on extracellular level. HHC markedly diminished oxidant production and also, intracellularly, decreased PKC activity and partly phosphorylation of PKCα, βII. On the other hand, we did not observe any effect of coumarin derivatives on phosphorylation of PKCδ and on phosphorylation of the NADPH oxidase subunit p40phox, which were suggested to be involved in the PMA-dependent intracellular activation process. In agreement with our previous findings, we assume that the different molecular structures of HHC and HHDC with their different physicochemical and free radical scavenging characteristics are responsible for their diverse effects on the parameters tested. PMID:24349608

  1. Inhibitory effects of imperatorin on voltage-gated K(+) channels and ATP-sensitive K(+) channels.

    Science.gov (United States)

    Wang, Yu-Wen; Yang, Chin-Tsang; Chen, Yi-Hung; Gong, Chi-Li; Chen, Yu-Fang; Kuo, Yueh-Hsiung; Leung, Yuk-Man

    2015-02-01

    Imperatorin is a furocoumarin isolated from Angelica archangelica and Cnidium monnieri. It has multiple neuromodulatory actions such as anticonvulsant effects, anxiolytic effects and anti-nociceptive effects. Although there have been reports demonstrating its effects on voltage-gated Na(+) channels (VGSC) and transient reversal potential (TRP) V1 channels in neurons, there is hitherto no work showing whether this compound affects voltage-gated K(+) (Kv) channels and ATP-sensitive K(+) (KATP) channels. We investigated the effects of imperatorin on K(+) channels using whole-cell configuration voltage-clamp technique. Imperatorin inhibited Kv channels in differentiated neuronal NG108-15 cells, and caused a left shift in the steady-state inactivation curve without affecting activation gating. Imperatorin also inhibited heterologously expressed wild type Kv1.2 and Kv2.1 channels, but became much less potent in inhibiting Kv1.2 V370G, a mutant defective in C-type inactivation, implying that drug inhibition depends on C-type inactivation. At a high concentration (100μM), imperatorin also suppressed KATP channels. Our results suggest that imperatorin inhibited both Kv and KATP channels. Copyright © 2014 Institute of Pharmacology, Polish Academy of Sciences. Published by Elsevier Urban & Partner Sp. z o.o. All rights reserved.

  2. Inhibitory effect of maple syrup on the cell growth and invasion of human colorectal cancer cells.

    Science.gov (United States)

    Yamamoto, Tetsushi; Uemura, Kentaro; Moriyama, Kaho; Mitamura, Kuniko; Taga, Atsushi

    2015-04-01

    Maple syrup is a natural sweetener consumed by individuals of all ages throughout the world. Maple syrup contains not only carbohydrates such as sucrose but also various components such as organic acids, amino acids, vitamins and phenolic compounds. Recent studies have shown that these phenolic compounds in maple syrup may possess various activities such as decreasing the blood glucose level and an anticancer effect. In this study, we examined the effect of three types of maple syrup, classified by color, on the cell proliferation, migration and invasion of colorectal cancer (CRC) cells in order to investigate whether the maple syrup is suitable as a phytomedicine for cancer treatment. CRC cells that were administered maple syrup showed significantly lower growth rates than cells that were administered sucrose. In addition, administration of maple syrup to CRC cells caused inhibition of cell invasion, while there was no effect on cell migration. Administration of maple syrup clearly inhibited AKT phosphorylation, while there was no effect on ERK phosphorylation. These data suggest that maple syrup might inhibit cell proliferation and invasion through suppression of AKT activation and be suitable as a phytomedicine for CRC treatment, with fewer adverse effects than traditional chemotherapy.

  3. Inhibitory effect of esculentoside A on tumour necrosis factor α production by human monocytes

    Directory of Open Access Journals (Sweden)

    H-B. Wang

    1996-01-01

    Full Text Available Esculentoside A (EsA is a saponin isolated from the roots of Phytolacca esculenta. Previous experiments have shown that it has strong anti-inflammatory effects. Tumour necrosis factor (TNF is a very important inflammatory mediator. It is known that there are two types of TNF—TNFα is from macrophages/monocytes and TNFβ is from activated lymphocytes. In order to study the mechanism of the anti-inflammatory effect of EsA, it was determined whether TNFα production from human peripheral monocytes was altered by EsA under lipopolysaccharide (LPS-stimulated conditions. EsA was found to decrease TNFα production in a dose-dependent manner at concentrations higher than 1 μmol/l EsA. Recent studies have shown that EsA has a curative effect on chocolate cyst and other inflammatory diseases. Our previous studies have shown that EsA could reduce the release of platelet activating factor (PAF from rat macrophages, and inhibit interleukin-1 and interleukin-6 production from routine macrophages. The reducing effects of EsA on the release of TNFα, IL-1, IL-6 and PAF may explain its anti-inflammatory effect.

  4. Inhibitory effects of (-)-epigallocatechin gallate on the life cycle of human immunodeficiency virus type 1 (HIV-1).

    Science.gov (United States)

    Yamaguchi, Koushi; Honda, Mitsuo; Ikigai, Hajime; Hara, Yukihiko; Shimamura, Tadakatsu

    2002-01-01

    Epigallocatechin gallate (EGCg), the major tea catechin, is known as a potent anti-bacterial agent. In addition, anti-tumor promoting, anti-inflammatory, anti-oxidative and antiviral activities have been reported. In the present study, we investigated possible anti-human immunodeficiency virus type-1 (HIV-1) activity of EGCg and its mechanisms of action in the viral life cycle. EGCg impinges on each step of the HIV life cycle. Thus, destruction of the viral particles, viral attachment to cells, post-adsorption entry into cells, reverse transcription (RT), viral production from chronically-infected cells, and the level of expression of viral mRNA, were analyzed using T-lymphoid (H9) and monocytoid (THP-1) cell systems, and antiviral protease activity was measured using a cell-free assay. Inhibitory effects of EGCg on specific binding of the virions to the cellular surfaces and changes in the steady state viral regulation (mRNA expression) due to EGCg were not observed. However, EGCg had a destructive effect on the viral particles, and post-adsorption entry and RT in acutely infected monocytoid cells were significantly inhibited at concentrations of EGCg greater than 1 microM, and protease kinetics were suppressed at a concentration higher than 10 microM in the cell-free study. Viral production by THP-1 cells chronically-infected with HIV-1 was also inhibited in a dose-dependent manner and the inhibitory effect was enhanced by liposome modification of EGCg. As expected, increased viral mRNA production was observed in lipopolysaccharide (LPS)-activated chronically HIV-1-infected cells. This production was significantly inhibited by EGCg treatment of THP-1 cells. In contrast, production of HIV-1 viral mRNA in unstimulated or LPS-stimulated T-lymphoid cells (H9) was not inhibited by EGCg. Anti-HIV viral activity of EGCg may thus result from an interaction with several steps in the HIV-1 life cycle.

  5. Inhibitory effect and mechanism of azo dyes on anaerobic methanogenic wastewater treatment: Can redox mediator remediate the inhibition?

    Science.gov (United States)

    Dai, Ruobin; Chen, Xiaoguang; Luo, Ying; Ma, Puyue; Ni, Shengsheng; Xiang, Xinyi; Li, Gang

    2016-11-01

    Inhibitory effect of azo dyes on anaerobic methanogenic wastewater treatment (AMWT) has been studied mainly focusing on biological toxicity in the batch test with simulated sole co-substrate. Detailed information on inhibitory effect and mechanism of azo dyes during the long-term operation with real complex co-substrate is limited. Moreover, whether redox mediator (RM) could remediate the inhibition is still unclear in previous studies, especially under the complex scenario. In this study, the real textile wastewater with alternative concentrations of azo dyes (0-600 mg/L) were used to operate a lab-scale high-rate anaerobic methanogenic bioreactor for 127 days, and 50 μM anthraquinone-2-sulfonate (AQS) as RM was added at the last period of operation. Azo dyes with concentration of 600 mg/L could cause significant inhibition on overall (decolorizing and methanogenic) performance of AMWT. Specific methanogenic activity assays showed that acetoclastic methanogens was more susceptible to high concentration azo dyes than hydrogenotrophic methanogens. The spatial distribution of extracellular polymeric substance in the anaerobic granular sludge (AGS) showed that the high biological toxicity of azo dyes was mainly attributed to enrichment effect in tightly bound-EPS (TB-EPS). The channels of AGS was clogged by azo dyes, which was evidenced by the hard release of aromatic amines in EPSs as well as decreased porosity of AGS and scanning electron microscope images. Meanwhile, the settling ability, particle size and strength of AGS all deteriorated after azo dyes concentration exceeded 450 mg/L. The dosing of AQS could mostly remediate overall performance of the bioreactor even if the recovery of acetoclastic methanogens was slow. However, except for the porosity with a part of recovery, physical characteristics of AGS hardly recovered, and washout of sludge from the bioreactor was still happening. It suggested that additional attention should be paid to prevent sludge

  6. Tumor-inhibitory effect of intralesional injection of bradykinin and immunostimulants in mice.

    Science.gov (United States)

    Mashiba, H; Matsunaga, K

    1985-11-01

    Intralesional injection of bradykinin at the dose of 500 micrograms or 1000 micrograms in oil or gelatin was effective in inhibiting the growth of Sa 180 cells in ddY mice. Ulcer formation in tumor was observed at a high rate in these bradykinin-treated groups. Combined use of bradykinin with a streptococcal preparation (OK-432) was more effective in inhibition of tumor growth compared with that in oil. Similar bradykinin-induced inhibition was observed in a spontaneous mammary tumor of C3H (MM 46) mice. These results suggest that increase in cellular influx and activation of infiltrated cells within a tumor are important factors to induce tumor inhibition effectively.

  7. Inhibitory effects of kratom leaf extract (Mitragyna speciosa Korth.) on the rat gastrointestinal tract.

    Science.gov (United States)

    Chittrakarn, Somsmorn; Sawangjaroen, Kitja; Prasettho, Supaporn; Janchawee, Benjamas; Keawpradub, Niwat

    2008-02-28

    Kratom (Mitragyna speciosa Korth.) is an indigenous plant of Thailand used traditionally in folk medicine although it is claimed to cause addiction. It is used to treat diarrhea, however, there is no scientific evidence to support the use. The aim of this study is to investigate the effect of methanolic extract of kratom leaves on the rat gastrointestinal tract. Kratom extract at 50, 100, 200 and 400 mg/kg (p.o.) caused a dose dependent protection against castor oil-induced diarrhea in rats and also inhibited intestinal transit. The antidiarrheal effect was not antagonized by naloxzone. The inhibition of intestinal transit by kratom extract was significantly different from the control when treated with a single dose for 1 day. For longer-term treatments of 15 and 30 days, kratom extract did not decrease the intestinal transit time indicating that adaptation had occurred. Kratom extract at a dose level of 200 and 400 mg/kg for 30 days and morphine at 3 mg/kg (i.p.) caused a decrease in the increment of body weight that was significantly different from the control and kratom extract at lower doses (50 and 100 mg/kg). However it had no effect on the level of plasma cholecystokinin. The results suggested that methanolic kratom extract exhibited its antidiarrheal effect on rat gastrointestinal tract. The effects may occur via pathways in addition to the action on opioid receptors. High does of kratom extract decreased the increment of body weight similar to the effect of morphine.

  8. Synergistic inhibitory effect of berberine and d-limonene on human gastric carcinoma cell line MGC803.

    Science.gov (United States)

    Zhang, Xiu-Zhen; Wang, Ling; Liu, Dong-Wu; Tang, Guang-Yan; Zhang, Hong-Yu

    2014-09-01

    This study aims at evaluating the anticancer effects of berberine hydrochloride (berberine) and d-limonene, alone and in combination, on human gastric carcinoma cell line MGC803 to determine whether berberine and d-limonene work synergistically and elucidate their mechanisms. MGC803 cells were treated with berberine and d-limonene, alone and in combination, for 24-48 h. The inhibitory effects of these drugs on growth were determined by MTT assay. The combination index and drug reduction index were calculated with the Chou-Talalay method based on the median-effect principle. Flow cytometry and laser scanning confocal microscopy were employed to evaluate the effects of both drugs on cell-cycle perturbation and apoptosis, generation of reactive oxygen species (ROS), mitochondrial membrane potential, and expression of Bcl-2 and caspase-3 in MGC803 cells. Berberine or d-limonene alone can inhibit the growth of MGC803 cells in a dose- and time-dependent manner. Berberine and d-limonene at a combination ratio of 1:4 exhibited a synergistic effect on anti-MGC803 cells. The two drugs distinctly induced intracellular ROS generation, reduced the mitochondrial transmembrane potential (ΔΨm), enhanced the expression of caspase-3, and decreased the expression of Bcl-2. The combination of berberine and d-limonene showed more remarkable effects compared with drugs used singly in MGC803 cells. The combination of berberine and d-limonene exerted synergistic anticancer effects on MGC803 cells by cell-cycle arrest, ROS production, and apoptosis induction through the mitochondria-mediated intrinsic pathway.

  9. Synergistic cancer growth-inhibitory effect of emodin and low-dose ...

    African Journals Online (AJOL)

    Purpose: To investigate the anti-cancer activity of emodin and its combination with low-dose cisplatin against human gastric cancer (SNU-5), including their effects on cell cycle phase distribution, apoptosis and cancer cell morphology. Methods: The anti-cancer activity of emodin, cisplatin and their combination against ...

  10. Inhibitory effects of brown algae extracts on histamine production in mackerel muscle via inhibition of growth and histidine decarboxylase activity of Morganella morganii.

    Science.gov (United States)

    Kim, Dong Hyun; Kim, Koth Bong Woo Ri; Cho, Ji Young; Ahn, Dong Hyun

    2014-04-01

    This study was performed to investigate the inhibitory effects of brown algae extracts on histamine production in mackerel muscle. First, antimicrobial activities of brown algae extracts against Morganella morganii were investigated using a disk diffusion method. An ethanol extract of Ecklonia cava (ECEE) exhibited strong antimicrobial activity. The minimum inhibitory concentration (MIC) of ECEE was 2 mg/ml. Furthermore, the brown algae extracts were examined for their ability to inhibit crude histidine decarboxylase (HDC) of M. morganii. The ethanol extract of Eisenia bicyclis (EBEE) and ECEE exhibited significant inhibitory activities (19.82% and 33.79%, respectively) at a concentration of 1 mg/ml. To obtain the phlorotannin dieckol, ECEE and EBEE were subjected to liquid-liquid extraction, silica gel column chromatography, and HPLC. Dieckol exhibited substantial inhibitory activity with an IC50 value of 0.61 mg/ml, and exhibited competitive inhibition. These extracts were also tested on mackerel muscle. The viable cell counts and histamine production in mackerel muscle inoculated with M. morganii treated with ≥2.5 MIC of ECEE (weight basis) were highly inhibited compared with the untreated sample. Furthermore, treatment of crude HDC-inoculated mackerel muscle with 0.5% ECEE and 0.5% EBEE (weight basis), which exhibited excellent inhibitory activities against crude HDC, reduced the overall histamine production by 46.29% and 56.89%, respectively, compared with the untreated sample. Thus, these inhibitory effects of ECEE and EBEE should be helpful in enhancing the safety of mackerel by suppressing histamine production in this fish species.

  11. [Investigation the Inhibitory Effects of Kaempferol on Rat Renalmesangial Cells Proliferation under High Glucose Condition].

    Science.gov (United States)

    Chen, Ni; Han, Peng-Ding; Chen, Wen; Deng, Yan

    2017-07-01

    To investigate the protective effects of kaempferol on rat renal mesangial cells under high glucose condition and explore its mechanism. The HBZY-1 cells were divided into normal glucose group (5.5 mmol/L), high glucose group (25 mmol/L), 10 μmol/L kaempferol+high glucose group, and 30 μmol/L kaempferol+high glucose group. Cell proliferative ability was measured by MTT; cell cycle was analyzed by flow cytometry; mRNA and protein levels were determined by Real-time PCR and Western blot, respectively. Kaempferol had no effect on the proliferative ability of rat renal mesangial cells under normal glucose (5.5 mmol/L) condition. High glucose (25 mmol/L) enhanced the cell proliferative ability, and this effect was antagonized by kaempferol (10-30 μmol/L) treatment. High glucose reduced the cell population at G 0 /G 1 phase with an associated increase in S phase, and had no effect on G₂/M phase; and kaempferol treatment restored high glucose-induced changes in cell cycle. Kaempferol also prevented high glucose-induced increase in fibronectin and connective tissue growth factor mRNA and protein expression levels. Kaempferol also prevented high glucose-induced increase in fibronectin and connective tissue growth factor mRNA and protein expression levels. Further, high glucose caused an increase in protein level of phosphorylated p38 mitogen-activated protein kinases (p38 MAPK), which was antagonized by kaempferol treatment. Our results suggest that kaempferol exerts its protective effect on rat renal mesangial cells under high glucose condition via p38 MAPK signaling pathway.

  12. Synthesis, characterization and inhibitory effects of crocetin derivative compounds in cancer and inflammation.

    Science.gov (United States)

    Chu, Yang; Gao, Jin; Niu, Jie; Huang, Yan-Fen; Chen, Ming; Wang, Mao-Ze; Shang, Qiang; Lu, Wen-Qi; Peng, Li-Hua; Jiang, Zhi-Hong

    2018-02-01

    Crocetin is a natural product possessing extraordinary therapeutic effects for various diseases. However, its extremely low solubility limits its application greatly. Conjugation of organic compounds containing heteroatoms such as N to poor soluble molecules can help the synthesized derivative to form stable hydrogen bonds by lowering the salvation energy, which will improve the solubility of the synthesized compounds. Herein, crocetin was modified by conjugating with piperidyl, diethylin and benzylamine to improve their solubility and bioactivities. In the present study, the conjugation of crocetin with piperidyl, diethylin and benzylamine and their influence on the solubility and the pharmacological effects of crocetin were investigated. With the described strategy, crocetin derivatives were synthesized and their structures were elucidated by 1 H NMR, 13 C NMR and UPLC-MS spectroscopic analysis. The solubility of crocetin and its derivatives were identified. Upon that, the pharmacological effects of the crocetin derivatives on the tumor and inflammation treatment were investigated. It was shown that, in contrast to crocetin, of which, the solubility and pharmacological effects were low and limited, the synthesized compounds have significantly higher solubility and possess broad spectrum of anticancer effects in multiple tumor cell lines, including B16F10, MCF-7, A549 and SKOV3, as well as enhanced anti-inflammation efficacy in macrophage (RAW264.7) without causing cells damage. Conjugation of piperidyl, diethylin and benzylamine with the crocetin was demonstrated to be a highly efficient strategy to improve the solubility of crocetin. The synthesized crocetin derivatives were shown the promising therapeutics for the tumor and inflammation treatment with high safety. Copyright © 2017 Elsevier Masson SAS. All rights reserved.

  13. Inhibitory effect of green coffee bean extract on fat accumulation and body weight gain in mice

    Directory of Open Access Journals (Sweden)

    Aitani Michio

    2006-03-01

    Full Text Available Abstract Background An epidemiological study conducted in Italy indicated that coffee has the greatest antioxidant capacity among the commonly consumed beverages. Green coffee bean is rich in chlorogenic acid and its related compounds. The effect of green coffee bean extract (GCBE on fat accumulation and body weight in mice was assessed with the objective of investigating the effect of GCBE on mild obesity. Methods Male ddy mice were fed a standard diet containing GCBE and its principal constituents, namely, caffeine and chlorogenic acid, for 14 days. Further, hepatic triglyceride (TG level was also investigated after consecutive administration (13 days of GCBE and its constituents. To examine the effect of GCBE and its constituents on fat absorption, serum TG changes were evaluated in olive oil-loaded mice. In addition, to investigate the effect on hepatic TG metabolism, carnitine palmitoyltransferase (CPT activity in mice was evaluated after consecutive ingestion (6 days of GCBE and its constituents (caffeine, chlorogenic acid, neochlorogenic acid and feruloylquinic acid mixture. Results It was found that 0.5% and 1% GCBE reduced visceral fat content and body weight. Caffeine and chlorogenic acid showed a tendency to reduce visceral fat and body weight. Oral administration of GCBE (100 and 200 mg/kg· day for 13 days showed a tendency to reduce hepatic TG in mice. In the same model, chlorogenic acid (60 mg/kg· day reduced hepatic TG level. In mice loaded with olive oil (5 mL/kg, GCBE (200 and 400 mg/kg and caffeine (20 and 40 mg/kg reduced serum TG level. GCBE (1%, neochlorogenic acid (0.028% and 0.055% and feruloylquinic acid mixture (0.081% significantly enhanced hepatic CPT activity in mice. However, neither caffeine nor chlorogenic acid alone was found to enhance CPT activity. Conclusion These results suggest that GCBE is possibly effective against weight gain and fat accumulation by inhibition of fat absorption and activation of fat

  14. Inhibitory effect of a triterpenoid compound, with or without alpha interferon, on hepatitis C virus infection.

    Science.gov (United States)

    Watanabe, Takako; Sakamoto, Naoya; Nakagawa, Mina; Kakinuma, Sei; Itsui, Yasuhiro; Nishimura-Sakurai, Yuki; Ueyama, Mayumi; Funaoka, Yusuke; Kitazume, Akiko; Nitta, Sayuri; Kiyohashi, Kei; Murakawa, Miyako; Azuma, Seishin; Tsuchiya, Kiichiro; Oooka, Shinya; Watanabe, Mamoru

    2011-06-01

    A lack of patient response to alpha interferon (α-IFN) plus ribavirin (RBV) treatment is a major problem in eliminating hepatitis C virus (HCV). We screened chemical libraries for compounds that enhanced cellular responses to α-IFN and identified a triterpenoid, toosendanin (TSN). Here, we studied the effects and mechanisms of action of TSN on HCV replication and its effect on α-IFN signaling. We treated HCV genotype 1b replicon-expressing cells and HCV-J6/JFH-infected cells with TSN, with or without α-IFN, and the level of HCV replication was quantified. To study the effects of TSN on α-IFN signaling, we detected components of the interferon-stimulated gene factor 3 (ISGF3), phosphorylated signal transducer and activator of transcription 1 (STAT1), and STAT2 by Western blotting analysis; expression levels of mRNA of interferon regulatory factor 9 using real-time reverse transcription-PCR (RT-PCR); and interferon-stimulated response element reporter activity and measured the expression levels of interferon-inducible genes for 2',5'-oligoadenylate synthetase, MxA, protein kinase R, and p56 using real-time RT-PCR. TSN alone specifically inhibited expression of the HCV replicon (50% effective concentration = 20.6 nM, 50% cytotoxic concentration > 3 μM, selectivity index > 146). Pretreatment with TSN prior to α-IFN treatment was more effective in suppressing HCV replication than treatment with either drug alone. Although TSN alone did not activate the α-IFN pathway, it significantly enhanced the α-IFN-induced increase of phosphorylated STATs, interferon-stimulated response element activation, and interferon-stimulated gene expression. TSN significantly increased baseline expression of interferon regulatory factor 9, a component of interferon-stimulated gene factor 3. Antiviral effects of treatment with α-IFN can be enhanced by pretreatment with TSN. Its mechanisms of action could potentially be important to identify novel molecular targets to treat HCV

  15. Pharmacodynamic modeling of the acid inhibitory effect of ranitidine in patients in an intensive care unit during prolonged dosing: characterization of tolerance

    NARCIS (Netherlands)

    Mathôt, R. A.; Geus, W. P.

    1999-01-01

    To characterize the relationship between the pharmacokinetics and the acid inhibitory effect of ranitidine during prolonged dosing on the basis of a physiologic indirect-response model. Multiple doses of ranitidine were administered to 18 patients in an intensive care unit in an open randomized

  16. Physicochemical Basis for the Inhibitory Effects of Organic and Inorganic Salts on the Growth of Pectobacterium carotovorum subsp. carotovorum and Pectobacterium atrosepticum▿

    OpenAIRE

    Yaganza, Elian-Simplice; Tweddell, Russell J.; Arul, Joseph

    2008-01-01

    Twenty-one salts were tested for their effects on the growth of Pectobacterium carotovorum subsp. carotovorum and Pectobacterium atrosepticum. In liquid medium, 11 salts (0.2 M) exhibited strong inhibition of bacterial growth. The inhibitory action of salts relates to the water-ionizing capacity and the lipophilicity of their constituent ions.

  17. Physicochemical basis for the inhibitory effects of organic and inorganic salts on the growth of Pectobacterium carotovorum subsp. carotovorum and Pectobacterium atrosepticum.

    Science.gov (United States)

    Yaganza, Elian-Simplice; Tweddell, Russell J; Arul, Joseph

    2009-03-01

    Twenty-one salts were tested for their effects on the growth of Pectobacterium carotovorum subsp. carotovorum and Pectobacterium atrosepticum. In liquid medium, 11 salts (0.2 M) exhibited strong inhibition of bacterial growth. The inhibitory action of salts relates to the water-ionizing capacity and the lipophilicity of their constituent ions.

  18. Physicochemical Basis for the Inhibitory Effects of Organic and Inorganic Salts on the Growth of Pectobacterium carotovorum subsp. carotovorum and Pectobacterium atrosepticum▿

    Science.gov (United States)

    Yaganza, Elian-Simplice; Tweddell, Russell J.; Arul, Joseph

    2009-01-01

    Twenty-one salts were tested for their effects on the growth of Pectobacterium carotovorum subsp. carotovorum and Pectobacterium atrosepticum. In liquid medium, 11 salts (0.2 M) exhibited strong inhibition of bacterial growth. The inhibitory action of salts relates to the water-ionizing capacity and the lipophilicity of their constituent ions. PMID:19114504

  19. Inhibitory effects of simvastatin on oxidative stress of patients with type 2 diabetes mellitus

    International Nuclear Information System (INIS)

    Su Ying; Liu Xiaomin; Wang Yueying; Sun Yanming; Luan Ying

    2008-01-01

    To study the effects of simvastatin on oxidative stress and blood lipid metabolism of patients with type 2 diabetes mellitus, 168 diabetic patients were randomly divided into simvastatin group and placebo group. The serum levels of SOD and MDA, as well as the lipid profile in patients were observed before and after 12 weeks treatment, respectively. The results showed that the serum levels of SOD in diabetic patients before treatment were significantly lower, and whereas level of MDA was higher than that of controls (P 0.05). The serum levels of HDL-C in patients after treatment with simvastatin were higher, and while the serum levels of TG, TC, LDL-C and VLDL-C were significantly lower than that of before the treatment (P 0.05). Therefore, the simvastatin could significantly inhibit oxidative stress provoked by hyperglycemia and had beneficial effects on the lipid homeostasis of diabetic patients. (authors)

  20. Rho-kinase inhibitors augment the inhibitory effect of propofol on rat bronchial smooth muscle contraction.

    Science.gov (United States)

    Hanazaki, Motohiko; Yokoyama, Masataka; Morita, Kiyoshi; Kohjitani, Atsushi; Sakai, Hiroyasu; Chiba, Yoshihiko; Misawa, Miwa

    2008-06-01

    Airway smooth muscle contraction is not caused by the increase in intracellular Ca(2+) ([Ca(2+)](i)) alone because agonist stimulation increases tension at the same [Ca(2+)](i) (increase in Ca(2+) sensitivity). The small G protein Rho A and Rho-kinase (ROCK) play important roles in the regulation of Ca(2+) sensitivity. In this study, we investigated the effects of three ROCK inhibitors (fasudil, Y-27632, and H-1152) on rat airway smooth muscle contraction and the effects of ROCK inhibitors on propofol-induced bronchodilatory effects. Ring strips from intrapulmonary bronchus of male Wistar rats were placed in 400-microL organ baths containing Krebs-Henseleit solution. After obtaining stable contraction with 30 microM acetylcholine, (1) propofol (1 microM-1 mM) was cumulatively applied; (2) cumulative doses of Y-27632 (0.01-300 microM), fasudil (0.01-100 microM), or H-1152 (0.01-100 microM) were applied; (3) propofol (1 microM-1 mM), with Y-27632, fasudil or H-1152 (0.03 microM or 0.1 microM), was cumulatively applied. (1) Propofol produced concentration-dependent relaxation of rat bronchial smooth muscle. (2) All ROCK inhibitors produced concentration-dependent relaxation. (3) 0.03 microM Y-27632 and fasudil had no significant effect on the concentration-response curve for propofol, while 0.1 microM of both agents significantly shifted concentration-response curves to the left and decreased EC(50). H-1152 (both 0.03 microM and 0.1 microM) significantly sifted the concentration-response curve for propofol to the left and decreased EC(50). ROCK inhibitors, especially H-1152, can attenuate the contraction of rat airway smooth muscle. The combined use of ROCK inhibitors and propofol causes greater relaxation.

  1. The inhibitory effect of simvastatin and aspirin on histamine responsiveness in human vascular endothelial cells.

    Science.gov (United States)

    Absi, Mais; Bruce, Jason I; Ward, Donald T

    2014-04-01

    Statins and aspirin deliver well-established cardiovascular benefits resulting in their increased use as combined polypills to decrease risk of stroke and heart disease. However, the direct endothelial effect of combined statin/aspirin cotreatment remains unclear. Histamine is an inflammatory mediator that increases vascular permeability, and so we examined the effect of treating human umbilical vein endothelial cells (HUVECs) for 24 h with 1 μM simvastatin and 100 μM aspirin on histamine responsiveness. Subsequent histamine (1 μM) challenge increased intracellular calcium (Ca(2+)i) concentration, an effect that was significantly inhibited by combined simvastatin/aspirin pretreatment but not when then the compounds were given separately, even at 10-fold higher concentrations. In contrast, the Ca(2+)i mobilization response to ATP challenge (10 μM) was not inhibited by combined simvastatin/aspirin pretreatment. The H1 receptor antagonist pyrilamine significantly inhibited both histamine-induced Ca(2+)i mobilization and extracellular signal-regulated kinase (ERK) activation, whereas ranitidine (H2 receptor antagonist) was without effect. However, combined simvastatin/aspirin pretreatment failed to decrease H1 receptor protein expression ruling out receptor downregulation as the mechanism of action. Histamine-induced ERK activation was also inhibited by atorvastatin pretreatment, while simvastatin further inhibited histamine-induced vascular endothelial cadherin phosphorylation as well as altered HUVEC morphology and inhibited actin polymerization. Therefore, in addition to the known therapeutic benefits of statins and aspirin, here we provide initial cellular evidence that combined statin/aspirin treatment inhibits histamine responsiveness in HUVECs.

  2. Inhibitory effect of trichothecene mycotoxins on bovine platelets stimulated by platelet activating factor.

    OpenAIRE

    Gentry, P A; Ross, M L; Bondy, G S

    1987-01-01

    Several species of fungi, which infect cereals and grains, can produce a class of compounds, known as trichothecene mycotoxins, which is characterized by a substituted epoxy-trichothecene ring structure. Cattle are susceptible to intoxication from feeds contaminated with T-2 toxin, one of the more potent trichothecene mycotoxins, while swine refuse to ingest feed contaminated with T-2 toxin. The bovine platelet has been used as a model cell system to evaluate the effects of T-2 toxin and its ...

  3. Effects of aversive odour presentation on inhibitory control in the Stroop colour-word interference task

    OpenAIRE

    Finkelmeyer, Andreas; Kellermann, Thilo; Bude, Daniela; Nie?en, Thomas; Schwenzer, Michael; Mathiak, Klaus; Reske, Martina

    2010-01-01

    Abstract Background Due to the unique neural projections of the olfactory system, odours have the ability to directly influence affective processes. Furthermore, it has been shown that emotional states can influence various non-emotional cognitive tasks, such as memory and planning. However, the link between emotional and cognitive processes is still not fully understood. The present study used the olfactory pathway to induce a negative emotional state in humans to investigate its effect on i...

  4. Inhibitory effects of lactoferrin on growth and biofilm formation of Porphyromonas gingivalis and Prevotella intermedia.

    Science.gov (United States)

    Wakabayashi, Hiroyuki; Yamauchi, Koji; Kobayashi, Tetsuo; Yaeshima, Tomoko; Iwatsuki, Keiji; Yoshie, Hiromasa

    2009-08-01

    Lactoferrin (LF) is an iron-binding antimicrobial protein present in saliva and gingival crevicular fluids, and it is possibly associated with host defense against oral pathogens, including periodontopathic bacteria. In the present study, we evaluated the in vitro effects of LF-related agents on the growth and biofilm formation of two periodontopathic bacteria, Porphyromonas gingivalis and Prevotella intermedia, which reside as biofilms in the subgingival plaque. The planktonic growth of P. gingivalis and P. intermedia was suppressed for up to 5 h by incubation with >or=130 microg/ml of human LF (hLF), iron-free and iron-saturated bovine LF (apo-bLF and holo-bLF, respectively), and >or=6 microg/ml of bLF-derived antimicrobial peptide lactoferricin B (LFcin B); but those effects were weak after 8 h. The biofilm formation of P. gingivalis and P. intermedia over 24 h was effectively inhibited by lower concentrations (>or=8 microg/ml) of various iron-bound forms (the apo, native, and holo forms) of bLF and hLF but not LFcin B. A preformed biofilm of P. gingivalis and P. intermedia was also reduced by incubation with various iron-bound bLFs, hLF, and LFcin B for 5 h. In an examination of the effectiveness of native bLF when it was used in combination with four antibiotics, it was found that treatment with ciprofloxacin, clarithromycin, and minocycline in combination with native bLF for 24 h reduced the amount of a preformed biofilm of P. gingivalis compared with the level of reduction achieved with each agent alone. These results demonstrate the antibiofilm activity of LF with lower iron dependency against P. gingivalis and P. intermedia and the potential usefulness of LF for the prevention and treatment of periodontal diseases and as adjunct therapy for periodontal diseases.

  5. Inhibitory Effect of Alpha-Mangostin on Adhesion of Candida albicans to Denture Acrylic

    OpenAIRE

    Kaomongkolgit, Ruchadaporn; Jamdee, Kusuma

    2015-01-01

    Objective: Candida-associated denture stomatitis is a very common disease affecting denture wearers. It is characterized by the presence of yeast biofilm on the denture, primarily associated with C. albicans. The investigation of agents that can reduce C. albicans adhesion may represent a significant advancement in the prevention and treatment of this disease. This study aims to investigate the effect of alpha-mangostin on the in vitro adhesion of C. albicans to denture acrylic and germ tube ...

  6. Inhibitory Effect of Enterococcus faecium WB2000 on Volatile Sulfur Compound Production by Porphyromonas gingivalis

    OpenAIRE

    Suzuki, Nao; Higuchi, Takuya; Nakajima, Masato; Fujimoto, Akie; Morita, Hiromitsu; Yoneda, Masahiro; Hanioka, Takashi; Hirofuji, Takao

    2016-01-01

    Volatile sulfur compounds (VSCs) produced by oral anaerobes are the major compounds responsible for oral malodor. Enterococcus faecium WB2000 is recognized as an antiplaque probiotic bacterium. In this study, the effect of E. faecium WB2000 on VSC production by Porphyromonas gingivalis was evaluated, and the mechanism of inhibition of oral malodor was investigated. P. gingivalis ATCC 33277 was cultured in the presence of four lactic acid bacteria, including E. faecium WB2000. Subsequently, P....

  7. Synergistic inhibitory effect of hyperbaric oxygen combined with sorafenib on hepatoma cells.

    Directory of Open Access Journals (Sweden)

    Hai-Shan Peng

    Full Text Available OBJECTIVES: Hypoxia is a common phenomenon in solid tumors, associated with chemotherapy and radiotherapy resistance, recurrence and metastasis. Hyperbaric oxygen (HBO therapy can increase tissue oxygen pressure and content to prevent the resistance, recurrence and metastasis of cancer. Presently, Sorafenib is a first-line drug, targeted for hepatocellular carcinoma (HCC but effective in only a small portion of patients and can induce hypoxia. The purpose of this study is to investigate the effect of HBO in combination with sorafenib on hepatoma cells. METHODS: Hepatoma cell lines (BEL-7402 and SK-Hep1 were treated with HBO at 2 atmosphere absolute pressure for 80 min per day or combined with sorafenib or cisplatin. At different time points, cells were tested for cell growth, colony formation, apoptosis, cell cycle and migration. Finally, miRNA from the hepatoma cells was detected by microRNA array and validated by qRT-PCR. RESULTS: Although HBO, sorafenib or cisplatin alone could inhibit growth of hepatoma cells, HBO combined with sorafenib or cisplatin resulted in much greater synergistic growth inhibition (cell proliferation and colony formation in hepatoma cells. Similarly, the synergistic effect of HBO and sorafenib on induction of apoptosis was also observed in hepatoma cells. HBO induced G1 arrest in SK-Hep1 not in BEL-7402 cells, but enhanced cell cycle arrest induced by sorafenib in BEL-7402 treated cells. However, HBO had no obvious effect on the migration of hepatoma cells, and microRNA array analysis showed that hepatoma cells with HBO treatment had significantly different microRNA expression profiles from those with blank control. CONCLUSIONS: We show for the first time that HBO combined with sorafenib results in synergistic growth inhibition and apoptosis in hepatoma cells, suggesting a potential application of HBO combined with sorafenib in HCC patients. Additionally, we also show that HBO significantly altered microRNA expression

  8. Inhibitory effect of TCCE on CCl4-induced overexpression of IL-6 in acute liver injury.

    Science.gov (United States)

    Gao, Jing; Dou, Huan; Tang, Xin-Hui; Xu, Li-Zhi; Fan, Yi-Mei; Zhao, Xiao-Ning

    2004-11-01

    Terminalia catappa L. leaves have been shown to protect against acute liver injury produced by some hepatotoxicants, but the active components and mechanisms are not clear. This study was designed to characterize the protective effects of the chloroform fraction of the ethanol extract of T. catappa leaves (TCCE) against carbon tetrachloride (CCl4)-induced hepatotoxicity in mice, and analyze the changes in expression level of interleukin-6 (IL-6) in the process. It was found that TCCE pretreatment (10 or 30 mg/kg, ig) protected mice from CCl4 toxicity, as evidenced by the reversed alterations in serum alanine aminotransferase (sALT) and serum aspartate aminotransferase (sAST) activities. Additionally liver tissues were subjected to RT-PCR, Western blot and immunohistochemistry to analyze changes in IL-6 expression. It was found that TCCE markedly suppressed the CCl4-induced over-transcription of IL-6 gene. Consistent with the result, the expression of IL-6 protein was also blocked by TCCE in CCl4-stimulated mice, especially in the area around central vein on liver tissue section. In conclusion, TCCE is effective in protecting mice from the hepatotoxicity produced by CCl4, and the mechanisms underlying its protective effects may be related to the inhibition on the overexpression of IL-6 mainly around terminal hepatic vein.

  9. Inhibitory effect of totarol on exotoxin proteins hemolysin and enterotoxins secreted by Staphylococcus aureus.

    Science.gov (United States)

    Shi, Ce; Zhao, Xingchen; Li, Wenli; Meng, Rizeng; Liu, Zonghui; Liu, Mingyuan; Guo, Na; Yu, Lu

    2015-10-01

    Staphylococcus aureus (S. aureus) causes a wide variety of infections, which are of major concern worldwide. S. aureus produces multiple virulence factors, resulting in food infection and poisoning. These virulence factors include hyaluronidases, proteases, coagulases, lipases, deoxyribonucleases and enterotoxins. Among the extracellular proteins produced by S. aureus that contribute to pathogenicity, the exotoxins α-hemolysin, staphylococcal enterotoxin A (SEA) and staphylococcal enterotoxin B (SEB) are thought to be of major significance. Totarol, a plant extract, has been revealed to inhibit the proliferation of several pathogens effectively. However, there are no reports on the effects of totarol on the production of α-hemolysin, SEA or SEB secreted by S. aureus. The aim of this study was to evaluate the effects of totarol on these three exotoxins. Hemolysis assay, western blotting and real-time reverse transcriptase-PCR assay were performed to identify the influence of graded subinhibitory concentrations of totarol on the production of α-hemolysin and the two major enterotoxins, SEA and SEB, by S. aureus in a dose-dependent manner. Moreover, an enzyme linked immunosorbent assay showed that the TNF-α production of RAW264.7 cells stimulated by S. aureus supernatants was inhibited by subinhibitory concentrations of totarol. Form the data, we propose that totarol could potentially be used as a promising natural compound in the food and pharmaceutical industries.

  10. Inhibitory effects and molecular mechanisms of tetrahydrocurcumin against human breast cancer MCF-7 cells

    Directory of Open Access Journals (Sweden)

    Xiao Han

    2016-02-01

    Full Text Available Background: Tetrahydrocurcumin (THC, an active metabolite of curcumin, has been reported to have similar biological effects to curcumin, but the mechanism of the antitumor activity of THC is still unclear. Methods: The present study was to investigate the antitumor effects and mechanism of THC in human breast cancer MCF-7 cells using the methods of MTT assay, LDH assay, flow cytometry analysis, and western blot assay. Results: THC was found to have markedly cytotoxic effect and antiproliferative activity against MCF-7 cells in a dose-dependent manner with the IC50 for 24 h of 107.8 μM. Flow cytometry analysis revealed that THC mediated the cell-cycle arrest at G0/G1 phase, and 32.8% of MCF-7 cells entered the early phase of apoptosis at 100 μM for 24 h. THC also dose-dependently led to apoptosis in MCF-7 cells via the mitochondrial pathway, as evidenced by the activation of caspase-3 and caspase-9, the elevation of intracellular ROS, a decrease in Bcl-2 and PARP expression, and an increase in Bax expression. Meanwhile, cytochrome C was released to cytosol and the loss of mitochondria membrane potential (Δψm was observed after THC treatment. Conclusion: THC is an excellent source of chemopreventive agents in the treatment of breast cancer and has excellent potential to be explored as antitumor precursor compound.

  11. Inhibitory effects and molecular mechanisms of tetrahydrocurcumin against human breast cancer MCF-7 cells

    Science.gov (United States)

    Han, Xiao; Deng, Shan; Wang, Ning; Liu, Yafei; Yang, Xingbin

    2016-01-01

    Background Tetrahydrocurcumin (THC), an active metabolite of curcumin, has been reported to have similar biological effects to curcumin, but the mechanism of the antitumor activity of THC is still unclear. Methods The present study was to investigate the antitumor effects and mechanism of THC in human breast cancer MCF-7 cells using the methods of MTT assay, LDH assay, flow cytometry analysis, and western blot assay. Results THC was found to have markedly cytotoxic effect and antiproliferative activity against MCF-7 cells in a dose-dependent manner with the IC50 for 24 h of 107.8 μM. Flow cytometry analysis revealed that THC mediated the cell-cycle arrest at G0/G1 phase, and 32.8% of MCF-7 cells entered the early phase of apoptosis at 100 μM for 24 h. THC also dose-dependently led to apoptosis in MCF-7 cells via the mitochondrial pathway, as evidenced by the activation of caspase-3 and caspase-9, the elevation of intracellular ROS, a decrease in Bcl-2 and PARP expression, and an increase in Bax expression. Meanwhile, cytochrome C was released to cytosol and the loss of mitochondria membrane potential (Δψm) was observed after THC treatment. Conclusion THC is an excellent source of chemopreventive agents in the treatment of breast cancer and has excellent potential to be explored as antitumor precursor compound. PMID:26899573

  12. Inhibitory effect of liposomal solutions of grape seed extract on the formation of heterocyclic aromatic amines.

    Science.gov (United States)

    Natale, Daniela; Gibis, Monika; Rodriguez-Estrada, Maria Teresa; Weiss, Jochen

    2014-01-08

    The effectiveness of grape seed extract (GSE) encapsulated in liposomes to inhibit the formation of heterocyclic aromatic amines (HAA) during frying of beef patties was assessed. All liposomal systems were prepared by high pressure homogenization at 22 500 psi. A total of six samples (rapeseed oil (control), GSE at 0.1% and 0.2%, and GSE-containing liposomes with 1%, 2%, and 5% soy lecithin) were investigated. MeIQx (2-amino-3,8-dimethylimidazo[4,5-f]quinoxaline), PhIP (2-amino-1-methyl-6-phenylimidazo[4,5b]pyridine), Norharman, and Harman were found after the marinade application and frying. PhIP concentrations decreased upon marination with GSE (0.1%) and GSE-containing liposomes (1% and 5%) (p oil control (p < 0.01) while no effect on β-carboline formation was observed. Results are in contrast to previous studies that had shown that liposomal encapsulation may enhance effectiveness of polyphenols to inhibit radical reactions. A mechanistic model was proposed to explain the observed differences.

  13. Evaluation of Inhibitory Effect of Recreational Drugs on Dopaminergic Terminal Neuron by PET and Whole-Body Autoradiography

    Directory of Open Access Journals (Sweden)

    Skye Hsin-Hsien Yeh

    2014-01-01

    Full Text Available There is little investigation for the functional roles of peripheral dopamine. [18F]FDOPA has been used in cancer imaging (i.e., neuroendocrine and tumors pancreatic tumors and neuroimaging (i.e., Parkinson’s disease and Huntington’s disease. Here, we accessed side effects of recreational drugs such as ketamine, cocaine, and methamphetamine on dopamine neurons in peripheral organs by using positron emission tomography (PET imaging and quantitative whole-body autoradiography (QWBAR with [18F]FDOPA. The images were applied for the measurement of specific binding ratios (SBRs of striatum with the cerebellum as the reference region. Clear striatal [18F]FDOPA-derived radioactivity was observed. Moderate level of radiotracer accumulation was presented in the mucosal layers of the stomach and small intestine. The medulla layers of kidney had higher radioactivity than that of the cortex. Blocking images markedly eliminated the specific binding of [18F]FDOPA in the striatum and in peripheral organs such as stomachs, intestines, and kidney. Ketamine showed the highest inhibitory effect on striatal [18F]FDOPA-derived radioactivity followed by cocaine and methamphetamine. The current results demonstrated a useful crossing-validating tool that enhances the capability of [18F]FDOPA for further investigations of the alteration of dopaminergic neurons in the brain disorder or cancer diseases in peripheral tissues.

  14. Method for Bacterial Growth and Ammonia Production and Effect of Inhibitory Substances in Disposable Absorbent Hygiene Products.

    Science.gov (United States)

    Forsgren-Brusk, Ulla; Yhlen, Birgitta; Blomqvist, Marie; Larsson, Peter

    The purpose of this study was to evaluate a pragmatic laboratory method to provide a technique for developing incontinence products better able to reduce malodor when used in the clinical setting. Bacterial growth and bacterially formed ammonia in disposable absorbent incontinence products was measured by adding synthetic urine inoculated with bacteria to test samples cut from the crotch area of the product. The inhibitory effect's of low pH (4.5 and 4.9) and 3 antimicrobial substances-chlorhexidine, polyhexamethylene biguanide (PHMB), and thymol-at 2 concentrations each, were studied. From the initial inocula of 3.3 log colony-forming units per milliliter (cfu/mL) at baseline, the bacterial growth of the references increased to 5.0 to 6.0 log cfu/mL at 6 hours for Escherichia coli, Proteus mirabilis, and Enterococcus faecalis. At 12 hours there was a further increase to 7.0 to 8.9 log cfu/mL. Adjusting the pH of the superabsorbent in the incontinence product from 6.0 to pH 4.5 and pH 4.9 significantly (P bacterial growth rates, in most cases, both at 6 and 12 hours. The effect was most pronounced at pH 4.5. Chlorhexidine had significant (P bacterial growth and ammonia production. This technique, we describe, provides a pragmatic method for assessing the odor-inhibiting capacity of specific incontinence products.

  15. Inhibitory effects of rHP-NAP IgY against Helicobacter pylori attachment to AGS cell line.

    Science.gov (United States)

    Borhani, Katayoun; Mohabati Mobarez, Ashraf; Khabiri, Ali Reza; Behmanesh, Mehrdad; Khoramabadi, Nima

    2016-08-01

    Helicobacter pylori is a major human pathogen related to gastric adenocarcinoma and gastroduodenal diseases. Treatment of H. pylori infections is complicated by the rise of antibiotic resistance, necessitating investigation of alternative therapies. One such alternative is passive immunization by oral administration of antibacterial immunoglobulin. In the present study, chicken immunoglobulin (IgY) was used for passive immunotherapy against a major virulence factor of H. pylori, namely recombinant HP-Nap protein. Recombinant HP-Nap was prepared and used to immunize hens. IgY was purified from the eggs by polyethylene glycol precipitation method with a total IgY-HP-NAP yield of 30 mg per egg. The inhibitory effect of specific IgY on H. pylori attachment was investigated in AGS cell line infected by the bacteria. The results demonstrate the potent effect of IgY- HP-NAP in inhibition of H. pylori attachment to the AGS cells. Copyright © 2016 Elsevier Ltd. All rights reserved.

  16. Isolation and identification of an anti-algal compound from Artemisia annua and mechanisms of inhibitory effect on algae.

    Science.gov (United States)

    Ni, Lixiao; Acharya, Kumud; Hao, Xiangyang; Li, Shiyin

    2012-08-01

    The goals of this work were to isolate and identify an anti-algal compound from extracts of Artemisia annua and study its mode of action on Microcystis aeruginosa. The anti-algal compound was isolated from the extracts using column chromatography and activity-guided fractionation methods. Artemisinin with strong anti-algal activity was identified by gas chromatography-mass spectrometry and (1)H Nuclear Magnetic Resonance. The EC(50) of artemisinin on M. aeruginosa was 3.2mg L(-1). Artemisinin decreased the soluble protein content and increased the superoxide dismutase activity and ascorbic acid content of M. aeruginosa, but exerted no effect on soluble sugar content. The results suggested the mode of action of artemisinin on algae may primarily be the increasing level of reactive oxygen species in algae cells. The results of our research could aid in the development of new anti-algal substances and lead to further study of mechanisms of inhibitory effect on algae. Copyright © 2012 Elsevier Ltd. All rights reserved.

  17. Inhibitory effect of live-attenuated Listeria monocytogenes-based vaccines expressing MIA gene on malignant melanoma.

    Science.gov (United States)

    Qian, Yue; Zhang, Na; Jiang, Ping; Chen, Siyuan; Chu, Shujuan; Hamze, Firas; Wu, Yan; Luo, Qin; Feng, Aiping

    2012-08-01

    Listeria monocytogenes (LM), a Gram-positive facultative intracellular bacterium, can be used as an effective exogenous antigen expression vector in tumor-target therapy. But for successful clinical application, it is necessary to construct attenuated LM stain that is safe yet retains the potency of LM based on the full virulent pathogen. In this study, attenuated LM and recombinants of LM expressing melanoma inhibitory activity (MIA) were constructed successfully. The median lethal dose (LD(50)) and invasion efficiency of attenuated LM strains were detected. The recombinants were utilized for immunotherapy of animal model of B16F10 melanoma. The level of MIA mRNA expression in tumor tissue was detected by using real-time polymerase chain reaction (PCR) with specific sequence, meanwhile the anti-tumor immune response was assayed by flow cytometric analysis and enzyme-linked immunosorbent spot (ELISPOT) assay. The results showed the toxicity and invasiveness of attenuated LM were decreased as compared with LM, and attenuated LM expressing MIA, especially the double-genes attenuated LM recombinant, could significantly induce anti-tumor immune response and inhibit tumor growth. This study implicates attenuated LM may be a safer and more effective vector for immunotherapy of melanoma.

  18. Mechanism of inhibitory effect of atorvastatin on resistin expression induced by tumor necrosis factor-α in macrophages

    Directory of Open Access Journals (Sweden)

    Chua Su-Kiat

    2009-05-01

    Full Text Available Abstract Atorvastatin has been shown to reduce resistin expression in macrophages after pro-inflammatory stimulation. However, the mechanism of reducing resistin expression by atorvastatin is not known. Therefore, we sought to investigate the molecular mechanisms of atorvastatin for reducing resistin expression after proinflammatory cytokine, tumor necrosis factor-α (TNF-α stimulation in cultured macrophages. Cultured macrophages were obtained from human peripheral blood mononuclear cells. TNF-α stimulation increased resistin protein and mRNA expression and atorvastatin inhibited the induction of resistin by TNF-α. Addition of mevalonate induced resistin protein expression similar to TNF-α stimulation. However, atorvastatin did not have effect on resistin protein expression induced by mevalonate. SP600125 and JNK small interfering RNA (siRNA completely attenuated the resistin protein expression induced by TNF-α and mevalonate. TNF-α induced phosphorylation of Rac, while atorvastatin and Rac-1 inhibitor inhibited the phosphorylation of Rac induced by TNF-α. The gel shift and promoter activity assay showed that TNF-α increased AP-1-binding activity and resistin promoter activity, while SP600125 and atorvastatin inhibited the AP-1-binding activity and resistin promoter activity induced by TNF-α. Recombinant resistin and TNF-α significantly reduced glucose uptake in cultured macrophages, while atorvastatin reversed the reduced glucose uptake by TNF-α. In conclusion, JNK and Rac pathway mediates the inhibitory effect of atorvastatin on resistin expression induced by TNF-α.

  19. EFFECTIVENESS OF INTEGRATED NEUROMUSCULAR INHIBITORY TECHNIQUE (INIT WITH SPECIFIC STRENGTH TRAINING EXERCISES IN SUBJECTS WITH UPPER TRAPEZIUS TRIGGER POINTS

    Directory of Open Access Journals (Sweden)

    B. Jyothirmai

    2015-10-01

    Full Text Available Background: Upper trapezius trigger points is a common cause for neck pain, decreased cervical range of motion and functional activities. The purpose of the study was to evaluate the effectiveness of integrated neuromuscular inhibitory technique (INIT along with specific strength training exercises in reducing pain, improving ROM and functional activities in subjects with upper trapezius trigger point. Methods: Thirty subjects were diagnosed with upper trapezius trigger points were included in the study. These patients were randomly allocated to intervention group (n=15, which underwent a 4- weeks training program of INIT along with specific strength training & control group (n=15 that received INIT alone. The outcome measures were taken before and after treatment. Outcomes were measured by visual analogue scale, cervical range of motion and neck disability index. Within the groups VAS, NDI, and cervical lateral flexion and rotation showed significant change in the mean value. The comparison of pre and post VAS in experimental group and control group showed a significant change in the experimental group .Paired sample t- test was used to analyze changes from before and after intervention programmed. Results: There is a statistically significant (p<0.00 improvement in both variables from baseline to 4th week in experimental group and control group but compared to control group, experimental group shows highly significant values in all parameters. Conclusion: INIT along with specific strength training is proved to be effective in reducing pain, decreasing disability and improving range of motion in individuals with upper trapezius trigger points.

  20. Inhibitory effects of propyl gallate on tyrosinase and its application in controlling pericarp browning of harvested longan fruits.

    Science.gov (United States)

    Lin, Yi-Fen; Hu, Yong-Hua; Lin, He-Tong; Liu, Xuan; Chen, Yi-Hui; Zhang, Shen; Chen, Qing-Xi

    2013-03-20

    Tyrosinase (EC 1.14.18.1), also known as polyphenol oxidase (PPO), is a key enzyme in pigment biosynthesis of organisms. The inhibitory effects of propyl gallate on the activity of mushroom tyrosinase and effects of propyl gallate on pericarp browning of harvested longan fruits in relation to phenolic metabolism were investigated. The results showed that propyl gallate could potently inhibit diphenolase activity of tyrosinase. The inhibitor concentration leading to 50% activity lost (IC50) was determined to be 0.685 mM. Kinetic analyses showed that propyl gallate was a reversible and mixed type inhibitor on this enzyme. The inhibition constants (K(IS) and K(I)) were determined to be 2.135 and 0.661 mM, respectively. Furthermore, the results also showed that propyl gallate treatment inhibited activities of PPO and POD in pericarp of harvested longan fruits, and maintained higher contents of total phenol and flavonoid of longan pericarp. Moreover, propyl gallate treatment also delayed the increases of browning index and browning degree in pericarp of harvested longan fruits. Therefore, application of propyl gallate may be a promising method for inhibiting tyrosinase activity, controlling pericarp browning, and extending shelf life of harvested longan fruits.

  1. [The molecular mechanisms of curcuma wenyujin extract-mediated inhibitory effects on human esophageal carcinoma cells in vitro].

    Science.gov (United States)

    Jing, Zhao; Zou, Hai-Zhou; Xu, Fang

    2012-09-01

    To study the molecular mechanisms of Curcuma Wenyujin extract-mediated inhibitory effects on human esophageal carcinoma cells. The Curcuma Wenyujin extract was obtained by supercritical carbon dioxide extraction. TE-1 cells were divided into 4 groups after adherence. 100 microL RMPI-1640 culture medium containing 0.1% DMSO was added in Group 1 as the control group. 100 microL 25, 50, and 100 mg/L Curcuma Wenyujin extract complete culture medium was respectively added in the rest 3 groups as the low, middle, and high dose Curcuma Wenyujin extract groups. The effects of different doses of Curcuma Wenyujin extract (25, 50, and 100 mg/L) on the proliferation of human esophageal carcinoma cell line TE-1 in vitro were analyzed by MTT assay. The gene expression profile was identified by cDNA microarrays in esophageal carcinoma TE-1 cells exposed to Curcuma Wenyujin extract for 48 h. The differential expression genes were further analyzed by Gene Ontology function analysis. Compared with the control group, MTT results showed that Curcuma Wenyujin extract significantly inhibited the proliferation of TE-1 cells in a dose-dependent manner (PCurcuma Wenyujin extract could inhibit the growth of human esophageal carcinoma cell line TE-1 in vitro. The molecular mechanisms might be associated with regulating genes expressions at multi-levels.

  2. Inhibitory effect of leptin on rosiglitazone-induced differentiation of primary adipocytes prepared from TallyHO/Jng mice

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Ki Young; Kim, Joo Young; Sung, Yoon-Young; Jung, Won Hoon; Kim, Hee-Youn; Park, Ji Seon; Cheon, Hyae Gyeong [Medicinal Science Division, Korea Research Institute of Chemical Technology, 100 Jang-dong, Yuseong, 305-600 Daejon (Korea, Republic of); Rhee, Sang Dal, E-mail: sdrhee@krict.re.kr [Medicinal Science Division, Korea Research Institute of Chemical Technology, 100 Jang-dong, Yuseong, 305-600 Daejon (Korea, Republic of)

    2011-03-25

    Research highlights: {yields} In this study, we investigated the effects of leptin on adipocyte differentiation prepared from subcutaneous fat of TallyHo mice. {yields} Leptin inhibited the adipocytes differentiation at physiological concentration via inhibition of PPAR{gamma} expression. {yields} Inhibitors of ERK and STAT1 restored the leptin's inhibitory activity both in vitro and in vivo. -- Abstract: The effects of leptin on rosiglitazone-induced adipocyte differentiation were investigated in the primary adipocytes prepared from subcutaneous fat of TallyHO/Jng (TallyHO) mouse, a recently developed model animal for type 2 diabetes mellitus (T2DM). The treatment of leptin inhibited the rosiglitazone-induced adipocyte differentiation with a decreased expression of peroxisome proliferator-activated receptor {gamma} (PPAR{gamma}) a key adipogenic transcription factor, both in mRNA and protein levels. Leptin (10 nM) was sufficient to inhibit the adipocyte differentiation, which seemed to come from increased expression of leptin receptor genes in the fat of TallyHO mice. The inhibition of adipogenesis by leptin was restored by the treatment of inhibitors for extracellular-signal-regulated kinase (ERK) (PD98059) and signal transducer and activator of transcription-1 (STAT1) (fludarabine). Furthermore, in vivo intraperitoneal administration of PD98059 and fludarabine increased the PPAR{gamma} expression in the subcutaneous fat of TallyHO mice. These data suggest that leptin could inhibit the PPAR{gamma} expression and adipocyte differentiation in its physiological concentration in TallyHO mice.

  3. Phytochemical profile of a blend of black chokeberry and lemon juice with cholinesterase inhibitory effect and antioxidant potential.

    Science.gov (United States)

    Gironés-Vilaplana, Amadeo; Valentão, Patrícia; Andrade, Paula B; Ferreres, Federico; Moreno, Diego A; García-Viguera, Cristina

    2012-10-15

    In this study, black chokeberry concentrate was added (5% w/v) to lemon juice, since previous reports suggested potential health benefits of this blend. The phytochemical composition, antioxidant capacity (scavenging of DPPH, superoxide and hydroxyl radicals, and hypochlorous acid), and inhibitory activity against cholinesterase of the new blend were determined and compared with those of lemon juice and chokeberry in citric acid (5%). The chokeberry concentrate, rich in cyanidin-glycosides, quercetin derivatives, and 3-O-caffeoylquinic acid, and lemon juice, possessing flavones, flavanones, quercetin derivates, and hydroxycinnamic acids, were characterised. The new drink showed a higher antioxidant effect than the chokeberry or lemon controls for all the tested methods, except for hypochlorous acid, in which lemon juice displayed higher activity. Both the lemon juice and chokeberry controls inhibited acetylcholinesterase and butyrylcholinesterase, and this effect was increased in the new mixtures. The results of the different radical scavenging assays indicate that the lemon-black chokeberry (5% w/v) mixture was more antioxidative than the respective controls separately. Moreover, their inhibition of cholinesterase is of interest regarding neurodegenerative disorders such as Alzheimer's disease, Parkinson's disease, or senile dementia. Copyright © 2012 Elsevier Ltd. All rights reserved.

  4. Colorimetric sensing of oxalate based on its inhibitory effect on the reaction of Fe (III) with curcumin nanoparticles

    Science.gov (United States)

    Pourreza, Nahid; Lotfizadeh, Neda; Golmohammadi, Hamed

    2018-03-01

    In this research, a new colorimetric method for the determination of oxalate using curcumin nanoparticles (CURNs) in the presence Fe (III) is introduced. The method is based on the inhibitory effect of oxalate ion on the reaction of (CURNs) with Fe (III) in acidic media. This reaction was monitored by measuring the increase in absorbance of CURNs-Fe3 + complex in the presence of oxalate ion at 427 nm. The effect of different parameters such as the pH of the sample solution, concentration of Fe (III), concentration of CURNs and the reaction time was examined and optimized. Under optimum experimental conditions, the absorption intensity was linear with the concentration of oxalate in the range of 0.15 to 1.70 μg mL- 1. The limit of detection (LOD) was 0.077 μg mL- 1 and the relative standard deviations (RSD) for 8 replicate measurements of 0.40 and 1.05 μg mL- 1 of oxalate were 4.20% and 2.74%, respectively. The developed method was successfully employed to the determination of oxalate in water, food and urine samples with satisfactory results.

  5. Phenolic Constituents and Inhibitory Effects of Hibiscus sabdariffa L. (Sorrel) Calyx on Cholinergic, Monoaminergic, and Purinergic Enzyme Activities.

    Science.gov (United States)

    Oboh, Ganiyu; Adewuni, Taiwo M; Ademiluyi, Adedayo O; Olasehinde, Tosin A; Ademosun, Ayokunle O

    2018-01-17

    This study revealed the effect of phenolic extract from Hibiscus sabdariffa L. (sorrel) calyx on acetylcholinesterase (AChE), butyrylcholinesterase (BChE), monoamine oxidase (MAO), and ecto-5' nucleotidase (E-NTDase) activities as well as pro-oxidant-induced oxidative damage in rat brain in vitro. Sorrel extract inhibited AChE (EC 50 = 46.96 µg/mL), BChE (EC 50 = 40.38 µg/mL), MAO (EC 50 = 43.69 µg/mL), and E-NTDase (EC 50 = 40.52 µg/mL) and stimulated Na + /K + -ATPase (EC 50 = 22.01 µg/mL) activities. The phenolic extract also reduced Fe 2+ - (EC 50 = 22.37 µg/mL) and sodium nitroprusside- (SNP-) (21.46 µg/mL) induced malondialdehyde (MDA) production in rat brain homogenates. Catechin (53.12 mg/g), chlorogenic (67.12 mg/g), rutin (16.25 mg/g), and caffeic acid (15.38 mg/g) were the most abundant phenolic compounds in the extract. The synergistic effects of the phenolic compounds may contribute to the enzyme inhibitory and stimulatory activities of the extract. Our findings suggest that sorrel extract shows promising potential for the treatment and/or management of some neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease.

  6. Biosynthesis of Silver Nanoparticles Using Carum carvi Extract and its Inhibitory Effect on Growth of Candida albicans

    Directory of Open Access Journals (Sweden)

    Nasiri

    2016-08-01

    Full Text Available Background Biological synthesis of nanoparticles has emerged as a promising field of biotechnology. Various biological systems including fungi, yeasts, bacteria, and plants have been used for biosynthesis of nanoparticles. Silver nanoparticles have unique properties that make them ideal for various medical and industrial applications. Owing to high levels of organic reducing agents and ease of manipulation, plant extracts are widely used for biological generation of various types of metal nanoparticles. Objectives The objective of the present study was to evaluate efficacy of Carum carvi extract in biosynthesis of silver nanoparticles and to investigate antifungal effects of the biosynthesized nanoparticles. Methods Silver nanoparticles were synthesized by addition of silver nitrate solution into fresh extract of C. carvi. Characterization of the synthesized silver nanoparticles was performed by transmission electron microscopy (TEM, scanning electron microscopy (SEM, energy dispersive spectrometry (EDS, and X-ray diffraction analysis (XRD. Inhibitory effect of silver nanoparticles on Candida albicans growth was evaluated by serial microdilution method. Results The results revealed the formation of spherical silver nanoparticles with an average size of 10 nm. Moreover, concentration of SNPs in a 25 mL sample containing both SNPs and plant extract biomass was 2.934 mg/L on average. Serial microdilution test showed that SNPs at the concentration of 50 μg/mL can inhibit growth of the pathogen. Conclusions The present study extends the existing literature about green synthesis of nanoparticles using plant tissues and extracts.

  7. Studies on inhibitory effect of Baicalein on MCF-7 Cells and its mechanism of action

    International Nuclear Information System (INIS)

    Gandhi, N.M.

    2013-01-01

    Acute toxicity to the normal cells from the conventional chemotherapeutic drugs has been one of the stumbling blocks for effective therapy. Further, increased acidity and hypoxia in solid tumour decreases the therapeutic effectiveness of radiotherapy and chemotherapy. The transcriptional response to cellular hypoxia is primarily mediated by the transcription factor hypoxia-inducible factor-1 (HIF-1). Thus, controlling HIF-1 could be an attractive target for cancer therapy. In view of the above considerations studies were undertaken to identify the phytoceutical which can be effective for cancer therapy. One of the phytoceutical being studied is Saicalein (BA), a compound extracted from the root of Scutellaria boicalensis, which is an active flavonoid extensively used in traditional Chinese medicine. In the present study the effects of BA on toxicity to the MCF-7 line was tested. MCF-7 cells when treated with BA exhibited concentration dependent toxicity. MCF-7 cells when treated with BA at the concentration of 50 μM, 50% cells lost viability. Further, it was shown that BA radio-sensitize the MCF-7 cells in vitro, as tested by LDH leakage assay. Radiation (4 Gy) alone did not show marked LDH leakage, however post radiation exposure treatment with BA (50 μM) of MCF-7 cells resulted in increased LDH leakage. In vitro wound healing assay was performed - which is the test for cell migration and cell proliferation. BA inhibited the wound closure by 97%. Overall the results demonstrate the anticancer potential of BA. In order to determine the effect of BA on transcription activation by HIF-1, a cell-based reporter assay for HIF-1 functional antagonist in MCF-7 cells was established. A luciferase reporter gene under the control of HRE from the erythropoietin gene (pTK-HRE3-luc) was employed to monitor HIF-1 activity. MCF-7 cells were transiently transfected with aforementioned plasmid followed by growing them in the presence of CoCl 2 , (hypoxia mimetic agent) and under

  8. Spatial coherence resonance and spatial pattern transition induced by the decrease of inhibitory effect in a neuronal network

    Science.gov (United States)

    Tao, Ye; Gu, Huaguang; Ding, Xueli

    2017-10-01

    Spiral waves were observed in the biological experiment on rat brain cortex with the application of carbachol and bicuculline which can block inhibitory coupling from interneurons to pyramidal neurons. To simulate the experimental spiral waves, a two-dimensional neuronal network composed of pyramidal neurons and inhibitory interneurons was built. By decreasing the percentage of active inhibitory interneurons, the random-like spatial patterns change to spiral waves and to random-like spatial patterns or nearly synchronous behaviors. The spiral waves appear at a low percentage of inhibitory interneurons, which matches the experimental condition that inhibitory couplings of the interneurons were blocked. The spiral waves exhibit a higher order or signal-to-noise ratio (SNR) characterized by spatial structure function than both random-like spatial patterns and nearly synchronous behaviors, which shows that changes of the percentage of active inhibitory interneurons can induce spatial coherence resonance-like behaviors. In addition, the relationship between the coherence degree and the spatial structures of the spiral waves is identified. The results not only present a possible and reasonable interpretation to the spiral waves observed in the biological experiment on the brain cortex with disinhibition, but also reveal that the spiral waves exhibit more ordered degree in spatial patterns.

  9. Algal testing of titanium dioxide nanoparticles-Testing considerations, inhibitory effects and modification of cadmium bioavailability

    International Nuclear Information System (INIS)

    Hartmann, N.B.; Von der Kammer, F.; Hofmann, T.; Baalousha, M.; Ottofuelling, S.; Baun, A.

    2010-01-01

    The ecotoxicity of three different sizes of titanium dioxide (TiO 2 ) particles (primary particles sizes: 10, 30, and 300 nm) to the freshwater green alga Pseudokirchneriella subcapitata was investigated in this study. Algal growth inhibition was found for all three particle types, but the physiological mode of action is not yet clear. It was possible to establish a concentration/dose-response relationship for the three particle sizes. Reproducibility, however, was affected by concentration-dependent aggregation of the nanoparticles, subsequent sedimentation, and possible attachment to vessel surfaces. It is also believed that heteroaggregation, driven by algal exopolymeric exudates, is occurring and could influence the concentration-response relationship. The ecotoxicity of cadmium to algae was investigated both in the presence and absence of 2 mg/L TiO 2 . The presence of TiO 2 in algal tests reduced the observed toxicity due to decreased bioavailability of cadmium resulting from sorption/complexation of Cd 2+ ions to the TiO 2 surface. However, for the 30 nm TiO 2 nanoparticles, the observed growth inhibition was greater than what could be explained by the concentration of dissolved Cd(II) species, indicating a possible carrier effect, or combined toxic effect of TiO 2 nanoparticles and cadmium. These results emphasize the importance of systematic studies of nanoecotoxicological effects of different sizes of nanoparticles and underline the fact that, in addition to particle toxicity, potential interactions with existing environmental contaminants are also of crucial importance in assessing the potential environmental risks of nanoparticles.

  10. Enhancement of inhibitory neurotransmission and inhibition of excitatory mechanisms underlie the anticonvulsant effects of Mallotus oppositifolius

    Directory of Open Access Journals (Sweden)

    Kennedy Kwami Edem Kukuia

    2016-01-01

    Full Text Available Context: Mallotus oppositifolius is a shrub that is used traditionally to treat epilepsy, but its potential has not been scientifically validated. Aims: This study investigated the anticonvulsant properties and possible mechanism of action of the 70% v/v hydroalcoholic extract of the leaves of M. oppositifolius.Materials and Methods: Inprinting control region (ICR mice (25–30 g were pretreated with the M. oppositifolius leaf extract (10–100 mg/kg before administering the respective convulsants (pentylenetetrazole [PTZ], picrotoxin [PTX], strychnine [STR], 4-aminopyridine [4-AP], and pilocarpine. The effect of the extract in maximal electroshock seizure (MES model was investigated also. Statistical Analysis: Data were presented as mean ± standard error of the mean and were analyzed with one-way analysis of variance (ANOVA or two-way ANOVA where appropriate with Newman–Keuls or Bonferroni post hoc test respectively. P< 0.05 was considered significant. Results: In both PTX