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Sample records for profound inhibitory effect

  1. Children with profound intellectual and multiple disabilities : the effects of functional movement activities

    NARCIS (Netherlands)

    van der Putten, A; Vlaskamp, C; Reynders, K; Nakken, H

    Objective: To determine the effect of functional movement activities within the MOVE ( Mobility Opportunities Via Education) curriculum on the independence of children with profound intellectual and multiple disabilities. Subjects: Forty-four children with profound intellectual and multiple

  2. Nanotechnological Inventions and Nanomaterials Produce A Profound Effect

    Directory of Open Access Journals (Sweden)

    VLASOV Vladimir Alexeevich

    2015-02-01

    Full Text Available The inventions in the area of nanotechnologies and nanomaterials produce a profound effect in construction, housing and communal services and adjacent economic fields as they allow us: to increase mechanical strength, coefficient of elasticity, alkali resistance and temperature of products vitrification; to obtain nanostructured coatings with the property of shape memory on the steel; to raise the dynamics of coal burning and its full burnout in the boilers of thermoelectric power station; to produce metal nanopowders with increased stored energy 10–15% etc. For example, the invention «Epoxy composition for high strength, alkali resistant structures» refers to epoxy composition used as a binder for production of high strength, thermal- and alkali-resistant glass-fiber material which can be applied in the manufacture process of construction reinforcement to strengthen concrete structures. The invention «The method to produce nanostructured reaction foil» can be used to join different materials including metal alloys, ceramics, amorphous materials and elements of microelectronic devices that are sensible to the heating. This process provides decreased labour-output ratio and energy consumption as well as the condition to manufacture foil with specified stored energy and high mechanical properties. The invention «The method of intensification of burning lowreactionary coal in the boilers of thermoelectric power station» refers to the thermal energy and can be implemented at the thermal plants. The increased dynamics of inflaming and burning leads to full burnout of powdered-coal low-reactionary fuel and decreased mechanical underfiring. The specialists may be also interested in the following inventions: fine dispersed organic suspension of carbon metal-containing nanostructures and the method to produce it; the dispersion of carbon nanotubes; the composition for reinforcement of building structures; the reinforced plate element made of

  3. EFFECT OF JUMPS IN PROFOUNDNESS ON THE FOOTBALLER REFLECTION

    Directory of Open Access Journals (Sweden)

    Nebojša Đošić

    2011-09-01

    Full Text Available The treatment endured one month. For this time 8 trainings and totally 322 jums in profoundness were done with differant altitudes from 42 cm to 105 cm. The complete time of work with time-out between sequences was about 120 minutes. The time-out between the sequences was from 2 ' til 6'. The pause between the training was from 2 to 5 days. The puls after 30 '' from the finishing of the jums in th sequence was from 100 to 140 pulsation in the minute measured by palpation. On the finaly measurement is constated that the two leg jump from place in height was better for 7 cm , and the one leg jump with three footsteps spring was better for 2 cm. This such result indicate on the assumption that the progress must bi greater if the program would be longer , for example two, three months and if this program should be done by footbalers which are active and in the best player years i.e. between 18 -30 year. The author was by this time 40 years old.

  4. 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.

  5. DMPD: Gram-negative endotoxin: an extraordinary lipid with profound effects oneukaryotic signal transduction. [Dynamic Macrophage Pathway CSML Database

    Lifescience Database Archive (English)

    Full Text Available 1916089 Gram-negative endotoxin: an extraordinary lipid with profound effects oneuk...ep;5(12):2652-60. (.png) (.svg) (.html) (.csml) Show Gram-negative endotoxin: an extraordinary lipid with profound effect...tive endotoxin: an extraordinary lipid with profound effects oneukaryotic signal transduction. Authors Raetz

  6. The effects of an environmental "enrichment" program on the behavior of institutionalized profoundly retarded children.

    OpenAIRE

    Horner, R D

    1980-01-01

    This study determined the effects of procedures designed to "enrich" the physical and social environment of an institutional ward on the "adaptive" and "maladaptive" child, adult, self, and object-directed behaviors of five profoundly retarded ambulatory females. Behavior observed in two treatment conditions, an environment "enriched" with toys and objects and an "enriched" environment coupled with differential reinforcement of adaptive behavior, was compared to behavior occurring in correspo...

  7. Effect of profound normovolemic hypotension and moderate hypothermia on circulating cytokines and adhesion molecules.

    Science.gov (United States)

    Hansen, D; Bogatzki, S; Syben, R; Bechrakis, N E; Dopjans, D; Spies, C; Welte, M; Schaffartzik, W

    1999-11-01

    Hypotension caused by hypovolemic, hemorrhagic shock induces disturbances in the immune system that may contribute to an increased susceptibility to sepsis. The effect of chemically induced hypotension on circulating cytokines and adhesion molecules has not been investigated yet. In 21 patients scheduled for resection of malignant choroidal melanoma of the eye the perioperative serum levels of the cytokines IL-1beta, IL-6, IL-10, TNF-alpha, and the adhesion molecules sE-Selectin and sICAM-1 were investigated. Moderate hypothermia of 32 degrees C was induced in all patients. In 14 patients profound hypotension (mean arterial blood pressure 35-40 mmHg, hypotension group) was induced by enalapril and nitroglycerin for a mean duration of 71 min. In 7 patients the tumor was not resectable, and hypotension was not induced (controls). We did not detect significant differences in serum levels of cytokines or sE-Selectin perioperatively in patients with profound hypotension compared with controls. In both groups IL-6 serum levels increased significantly and reached a maximum after rewarming (17 +/- 6 and 16 +/- 5 pg/dL, respectively, P < 0.001). IL-1beta, IL-10, and TNF-alpha did not change perioperatively in both groups. On the first postoperative day sICAM-1 serum levels were significantly increased in both groups (mean increase of 96 and 54 ng/mL, respectively, P < 0.01 and P < 0.05). We conclude from this study that profound normovolemic arterial hypotension does not seem to have effects on serum levels of circulating IL-1beta, IL-6, IL-10, TNF-alpha, and sE-Selectin. Perioperative moderate hypothermia may be the reason for the postoperative increase in sICAM-1 levels independent of the blood pressure.

  8. The Differential Effects of Attentional Focus in Children with Moderate and Profound Visual Impairments

    Directory of Open Access Journals (Sweden)

    Scott W. T. McNamara

    2017-10-01

    Full Text Available It has been consistently reported that an external focus of attention leads to better motor performance than an internal focus, but no research to date has explored this effect in a population with visual impairments (VI. External focus statements typically reference something in the environment (e.g., target that may be difficult to conceptualize for people with VI since they cannot generate a visual representation of the object of focus. Internal focus statements could be more closely identifiable with proprioception that is not impaired in this population. Recent studies have reported that sighted adults with temporarily obstructed vision are able to receive an external focus benefit when performing discrete tasks (i.e., golf putt and vertical jump, however, it is unclear if those with VI would experience the same benefit. The purpose of this investigation was to compare how an internal focus and external focus impact the balance of children with VI. Eighteen children with VI were grouped into a moderate (n = 11 and a profound VI group (n = 7. Participants completed a familiarization trial, an internal focus trial (i.e., focusing on feet and an external focus trial (i.e., focusing on markers in a counterbalanced order. The moderate VI group had a lower root mean square error while using an external focus (p = 0.04, while the profound VI group did not differ between conditions (p > 0.05. These results suggest that while performing a task reliant on sensory feedback, an external focus benefit may be dependent on the severity of VI. Further research is needed to examine whether external focus statements can be presented in a way that may be more intuitive to those with profound VI. These findings may help to influence how professionals in health-related fields (e.g., physical therapist and physical educators give instructions on motor performance to populations with VI.

  9. Profound effects of population density on fitness-related traits in an invasive freshwater snail.

    Directory of Open Access Journals (Sweden)

    Nicholas Zachar

    Full Text Available Population density can profoundly influence fitness-related traits and population dynamics, and density dependence plays a key role in many prominent ecological and evolutionary hypotheses. Here, we evaluated how individual-level changes in population density affect growth rate and embryo production early in reproductive maturity in two different asexual lineages of Potamopyrgus antipodarum, a New Zealand freshwater snail that is an important model system for ecotoxicology and the evolution of sexual reproduction as well as a potentially destructive worldwide invader. We showed that population density had a major influence on individual growth rate and early-maturity embryo production, effects that were often apparent even when comparing treatments that differed in population density by only one individual. While individual growth rate generally decreased as population density increased, we detected a hump-shaped relationship between embryo production and density, with females from intermediate-density treatments producing the most embryos and females from low- and high-density treatments producing the fewest embryos. The two lineages responded similarly to the treatments, indicating that these effects of population density might apply more broadly across P. antipodarum. These results indicate that there are profound and complex relationships between population density, growth rate, and early-maturity embryo production in at least two lineages of this important model system, with potential implications for the study of invasive populations, research on the maintenance of sex, and approaches used in ecotoxicology.

  10. Inhibitory effect of cyanide on wastewater nitrification ...

    Science.gov (United States)

    The effect of CN- (CN-) on nitrification was examined with samples from nitrifying wastewater enrichments using two different approaches: by measuring substrate (ammonia) specific oxygen uptake rates (SOUR), and by using RT-qPCR to quantify the transcripts of functional genes involved in nitrification. The nitrifying bioreactor was operated as a continuous reactor with a 24 h hydraulic retention time. The samples were exposed in batch vessels to cyanide for a period of 12 h. The concentrations of CN- used in the batch assays were 0.03, 0.06, 0.1 and 1.0 mg/L. There was considerable decrease in SOUR with increasing dosages of CN-. A decrease of more than 50% in nitrification activity was observed at 0.1 mg/L CN-. Based on the RT-qPCR data, there was notable reduction in the transcript levels of amoA and hao for increasing CN- dosage, which corresponded well with the ammonia oxidation activity measured via SOUR. The inhibitory effect of cyanide may be attributed to the affinity of cyanide to bind ferric heme proteins, which disrupt protein structure and function. The correspondence between the relative expression of functional genes and SOUR shown in this study demonstrates the efficacy of RNA based function-specific assays for better understanding of the effect of toxic compounds on nitrification activity in wastewater. Nitrification is the first step of nitrogen removal is wastewater, and it is susceptible to inhibition by many industrial chemical. We looked at

  11. Long-term effect of Helicobacter pylori eradication on the reversibility of acid secretion in profound hypochlorhydria.

    Science.gov (United States)

    Iijima, K; Sekine, H; Koike, T; Imatani, A; Ohara, S; Shimosegawa, T

    2004-06-01

    Although profound hypochlorhydria is considered to be an important risk factor for development of gastric cancer, long-term effect of Helicobacter pylori eradication on its reversibility remains uncertain. To clarify the change in acid secretion after eradication in a long-term follow-up over 5 years in patients with profound hypochlorhydria. Twenty-three H. pylori-positive patients with hypochlorhydria (hypochlorhydria.

  12. 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 ...

  13. Acetyl-cholinesterase Enzyme Inhibitory Effect of Calophyllum species

    African Journals Online (AJOL)

    acetylcholinesterase (AChE) enzyme using Ellman's method. Results: Most of the extracts showed promising inhibitory activity against AChE at concentrations of. 100 µg/mL, with the methanol extract of C. inophyllum demonstrating the strongest inhibitory effect of. 81.28 % followed by the methanol extract of C. benjaminum ...

  14. Acetyl-cholinesterase Enzyme Inhibitory Effect of Calophyllum species

    African Journals Online (AJOL)

    : Most of the extracts showed promising inhibitory activity against AChE at concentrations of 100 μg/mL, with the methanol extract of C. inophyllum demonstrating the strongest inhibitory effect of 81.28 % followed by the methanol extract of C.

  15. The effects of a power-assisted exercise intervention on alertness in people with profound intellectual and multiple disabilities

    NARCIS (Netherlands)

    Wessels, Marleen D.; Bossink, Leontien W.M.; van der Putten, Annette A.J.

    2017-01-01

    One of the benefits of physical activity in people with profound intellectual and multiple disabilities (PIMD) is an increase in alertness. This study investigated the effect of a power-assisted exercise intervention on alertness and the relationship of this effect to the level of additional motor

  16. Motor interventions in children with severe or profound intellectual disabilities: motor, cognitive and social effects

    NARCIS (Netherlands)

    Houwen, Suzanne; van der Putten, Annette; Vlaskamp, Carla

    2014-01-01

    Background: It is generally agreed that motor activity promotes motor, cognitive, and social development, but the specific benefits in children with severe or profound intellectual disabilities (S-PID) are as yet unknown. The aim of this study was to systematically review the evidence related to

  17. The Effects of Governing Board Configuration on Profound Organizational Change in Hospitals

    Science.gov (United States)

    Alexander, Jeffrey A.; Ye, Yining; Lee, Shoou-Yih D.; Weiner, Bryan J.

    2006-01-01

    This study extends the literature on governing boards and organizational change by examining how governing board configurations have influenced profound organizational change in U.S. hospitals, and the conditions under which such change occurs. Hospitals governed by boards that more closely resembled a corporate governance model were more likely…

  18. The causal effect of profound organizational change when job insecurity is low – a quasi-experiment analysing municipal mergers

    DEFF Research Database (Denmark)

    Bhatti, Yosef; Gørtz, Mette; Pedersen, Lene Holm

    2015-01-01

    The present article finds that the causal effect of profound organizational change on employee health can be very low, if job insecurity is mitigated. We demonstrate this by investigating a rare case of a large-scale radical public sector reform with low job insecurity, in which a large number of...

  19. Profound Effects of Population Density on Fitness-Related Traits in an Invasive Freshwater Snail

    OpenAIRE

    Nicholas Zachar; Maurine Neiman

    2013-01-01

    Population density can profoundly influence fitness-related traits and population dynamics, and density dependence plays a key role in many prominent ecological and evolutionary hypotheses. Here, we evaluated how individual-level changes in population density affect growth rate and embryo production early in reproductive maturity in two different asexual lineages of Potamopyrgus antipodarum, a New Zealand freshwater snail that is an important model system for ecotoxicology and the evolution o...

  20. 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.

  1. A comparison of the effects of four therapy procedures on concentration and responsiveness in people with profound learning disabilities.

    Science.gov (United States)

    Lindsay, W R; Pitcaithly, D; Geelen, N; Buntin, L; Broxholme, S; Ashby, M

    1997-06-01

    This paper is an investigation into the efficacy of four therapeutic treatment procedures increasingly used with people with profound learning disabilities: snoezelen, hand massage/aromatherapy, relaxation, and active therapy (a bouncy castle). In particular, the effects of these procedures on concentration and responsiveness were examined. Eight subjects with profound learning disabilities took part in the study and each subject received each of the treatments. To assess the effects of the treatments, simple concentration tasks were administered and the subjects' responsiveness to each treatment was rated by independent observers. The results suggest that both snoezelen and relaxation had a positive effect on concentration and seemed to be the most enjoyable therapies for clients, whereas hand massage/aromatherapy and active therapy had no or even negative effects on concentration and appeared less enjoyable.

  2. Inhibitory Effect of Glycerin on Vibrio parahaemolyticus and Salmonella

    Science.gov (United States)

    Chun, Doki; Seol, Sung Yong; Tak, Ryunbin; Park, Cheong Kyu

    1972-01-01

    In a study of the effect of glycerin in transport media on Vibrio parahaemolyticus and Salmonella, it was found that a concentration of 30% glycerin was highly inhibitory for V. parahaemolyticus and to a lesser degree for Salmonella. The incorporation of peptone or human feces in media did not reduce the inhibitory effect of glycerin. In media with 15% glycerin, viable counts of V. parahaemolyticus and Salmonella increased after 24 hr of incubation both in the presence and absence of feces. Due to the concurrent increase in the total bacterial count in the media containing feces, no enrichment effect was noted. PMID:4565633

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

    African Journals Online (AJOL)

    Aghomotsegin

    2015-07-29

    Jul 29, 2015 ... The abundance of second generation feedstock reinforces the consideration of biofuel over fossil fuel, ..... cells size.Comparing the effects of the two inhibitors, it can be observed that in general vanillin has a pronounced inhibitory effect than acetic acid; ..... furans and linoleic acid on hydrogen production.

  4. Antioxidant properties and inhibitory effect of ethanolic extract of ...

    African Journals Online (AJOL)

    Recent studies have shown that vegetables consumption could lower the risk of diabetes mellitus. Therefore, this study sought to investigate the inhibitory effect of Struchium sparganophora (Ewuro Odo) leaf on key enzyme linked to type-2 diabetes (á-amylase and á-glucosidase) as well as assessing the effect of blanching ...

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

    African Journals Online (AJOL)

    Recently, there has been increasing interest in Ficus deltoidea (Moracea) due to its chemical composition and the potential health benefits. The leaves of the plant have been suggested to have potential antidiabetic effects. Inhibition of carbohydrate-hydrolysing enzymes, such as α-glucosidase and α-amylase is one of the ...

  6. Inhibitory Effect of Aspirin on Cholangiocarcinoma Cells

    Science.gov (United States)

    Boueroy, Parichart; Aukkanimart, Ratchadawan; Boonmars, Thidarut; Sriraj, Pranee; Ratanasuwan, Panaratana; Juasook, Amornrat; Wonkchalee, Nadchanan; Vaeteewoottacharn, Kulthida; Wongkham, Sopit

    2017-11-26

    Aspirin and other non-steroidal anti-inflammatory drugs reduce the risk of cancer due to their anti-proliferative and apoptotic effects, which are the important mechanisms for their anti-tumor activity. Here, the effect of aspirin on human cholangiocarcinoma cells (KKU-214) and the underlying mechanisms of its action were explored. Cell proliferation was measured by sulforhodamine B (SRB) assay, while cell cycle distribution and apoptosis were determined by flow cytometry. Western blotting was used to explore protein expression underlying molecular mechanisms of anti-cancer treatment of aspirin. Aspirin reduced cell proliferation in a dose- and time-dependent manner, and altered the cell cycle phase distribution of KKU-214 cells by increasing the proportion of cells in the G0/G1 phase and reducing the proportion in the S and G2/M phases. Consistent with its effect on the cell cycle, aspirin also reduced the expression of cyclin D1 and cyclin‑dependent kinase 4 (Cdk-4), which are important for G0/G1 cell cycle progression. Treatment with aspirin led to increased induction of apoptosis in a dose-dependent manner. Further analysis of the mechanism underlying the effect of this drug showed that aspirin induced the expression of the tumor-suppressor protein p53 while inhibiting the anti-apoptotic protein B‑cell lymphoma-2 (Bcl-2). Correspondingly, the activation of caspase-9 and -3 was also increased. These findings suggest that aspirin causes cell cycle arrest and apoptosis, both of which could contribute to its anti-proliferative effect. Creative Commons Attribution License

  7. Narcissus tazetta lectin shows strong inhibitory effects against ...

    Indian Academy of Sciences (India)

    Prakash

    early stem and progenitor cells, and expansion of lineage- committed cells in prolonged culture could be developed for clinical expansion of CD34+ cells for transplantation and use of these cells for other cell therapy strategies. In this study, we investigated the inhibitory effect of a novel mannose- binding lectin isolated ...

  8. Inhibitory effect of essential oil on aflatoxin activities

    African Journals Online (AJOL)

    STORAGESEVER

    2010-04-19

    Apr 19, 2010 ... Inhibitory effects of Thyme oils on growth and aflatoxin production by Aspergillus parasiticus. Food Control,15: 479-483. Rasoli I, Fakoor MH, Yadegarinia D, Gachkar L, Allameh A, Rezaei MB. (2008). Antimycotoxigenic characteristics of Rosmarinus officinalis and Trachyspermum copticum L. essential oils.

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

    African Journals Online (AJOL)

    Cold extracts of five fungicidal plants (Aloe barbadensis, Azdrichta indica, Nicotiana tabacum, Tridax precubens and Carica papaya) were screened for in vitro inhibitory effects on Fusarium oxysporium, using 25, 50, 75 and 100% concentrations of each extract. The four different concentrations of N. tabacum completely ...

  10. 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 ...

  11. 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 ...

  12. Inhibitory effect of Taraxacum officinale L (Compositae) aqueous ...

    African Journals Online (AJOL)

    Conclusion: T. officinale root aqueous extract has inhibitory effects on spermatogenesis. Further studies are required to identify specific ingredient(s) in T. officinale that may be useful as male contraceptive(s). Keywords: Taraxacum officinale, Dandelion, GDNF family receptor alpha 1, Macrophage Colony- Stimulating Factor ...

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

    African Journals Online (AJOL)

    The Inhibitory Effects of Neem Oil against the Development of Plasmodium berghei in Mice. 'C. I. NYAMWANGE, J. O. MAINA AND H. S. NYANDIEKA*. Department of Medical Biochemistry, School of Medicine, Moi Teaching and Referral Hospital, Moi. University, P. O. Box 4606-30100, Eldoret, Kenya. Although neem oil ...

  14. Antioxidant Activity and Inhibitory Effect of Some Commonly used ...

    African Journals Online (AJOL)

    Antioxidant Activity and Inhibitory Effect of Some Commonly used Medicinal Plants against Lipid Per-Oxidation in Mice Brain. ... oxidative stress in brain could be potentially prevented by the intake of these plants. Key words: Antioxidant activity, Balb c mice, iron chelation, phenolics, oxidative stress, medicinal plants.

  15. 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 ...

  16. 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.

  17. In vitro inhibitory effect of methanol leaf extract of Stachytarpheta ...

    African Journals Online (AJOL)

    In the fourth and final phases, the second phase experiments were repeated in a calcium-free medium and in the absence and presence of propranolol (1.54 mM) respectively. Results: SJ exhibited significant inhibitory effects on OT and CaCl2 induced uterine contractions (p < 0.05). The EC50 for OT increased from 1.92 ...

  18. 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 ...

  19. What is profound?

    DEFF Research Database (Denmark)

    Sobisch, Jan-Ulrich

    2013-01-01

    Discussing the question, which elements on the path are to be considered profound. While a general view is that the most subtle practises are also the most profound, 'Jig-rten-mgon-po maintains that the most fundamental one's are to be considered the most profound.......Discussing the question, which elements on the path are to be considered profound. While a general view is that the most subtle practises are also the most profound, 'Jig-rten-mgon-po maintains that the most fundamental one's are to be considered the most profound....

  20. 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.

  1. 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.

  2. Inhibitory effects of arbutin-beta-glycosides synthesized from enzymatic transglycosylation for melanogenesis.

    Science.gov (United States)

    Jun, So-Young; Park, Kyung-Min; Choi, Ki-Won; Jang, Min Kyung; Kang, Hwan Yul; Lee, Sang-Hyeon; Park, Kwan-Hwa; Cha, Jaeho

    2008-04-01

    To develop a new skin whitening agent, arbutin-beta-glycosides were synthesized and evaluated for their melanogenesis inhibitory activities. Three active compounds were synthesized via the transglycosylation reaction of Thermotoga neapolitana beta-glucosidase and purified by recycling preparative HPLC. As compared with arbutin (IC(50 )= 6 mM), the IC(50 )values of these compounds were 8, 10, and 5 mM for beta-D -glucopyranosyl-(1-->6)-arbutin, beta-D: -glucopyranosyl-(1-->4)-arbutin, and beta-D -glucopyranosyl-(1-->3)-arbutin, respectively. beta-D: -Glucosyl-(1-->3)-arbutin also exerted the most profound inhibitory effects on melanin synthesis in B16F10 melanoma cells. Melanin synthesis was inhibited to a significant degree at 5 mM, at which concentration the melanin content was reduced to below 70% of that observed in the untreated cells. Consequently, beta-D: -glucopyranosyl-(1-->3)-arbutin is a more effective depigmentation agent and is also less cytotoxic than the known melanogenesis inhibitor, arbutin.

  3. 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.

  4. Inhibitory effect of furosemide on histamine release from human basophils

    OpenAIRE

    貴谷, 光; 草浦, 康浩; 本家, 尚子; 谷水, 将邦; 光延, 文裕; 御舩, 尚志; 岡崎, 守宏; 谷崎, 勝朗

    1992-01-01

    Inhibitory effect of furosemide on histamine release from basophils induced by anti-IgE was examined in 4 healthy subjects and 8 patients with atopic asthma. The experiments of basophil histamine release were carried out by using whole blood method. The mean values of histamine release after 15 min preincubation with furosemide atvarious concentrations were not significantly decreased, in both healthy and asthmatic subjects compared to those of histamine release without furosemide. The result...

  5. Inhibitory Effect of Corn Silk on Skin Pigmentation

    Directory of Open Access Journals (Sweden)

    Sang Yoon Choi

    2014-03-01

    Full Text Available In this study, the inhibitory effect of corn silk on melanin production was evaluated. This study was performed to investigate the inhibitory effect of corn silk on melanin production in Melan-A cells by measuring melanin production and protein expression. The corn silk extract applied on Melan-A cells at a concentration of 100 ppm decreased melanin production by 37.2% without cytotoxicity. This was a better result than arbutin, a positive whitening agent, which exhibited a 26.8% melanin production inhibitory effect at the same concentration. The corn silk extract did not suppress tyrosinase activity but greatly reduced the expression of tyrosinase in Melan-A cells. In addition, corn silk extract was applied to the human face with hyperpigmentation, and skin color was measured to examine the degree of skin pigment reduction. The application of corn silk extract on faces with hyperpigmentation significantly reduced skin pigmentation without abnormal reactions. Based on the results above, corn silk has good prospects for use as a material for suppressing skin pigmentation.

  6. Effects of early identification and intervention on language development in Japanese children with prelingual severe to profound hearing impairment.

    Science.gov (United States)

    Kasai, Norio; Fukushima, Kunihiro; Omori, Kana; Sugaya, Akiko; Ojima, Toshiyuki

    2012-04-01

    Early identification and intervention for prelingual bilateral severe to profound hearing loss is supposed to reduce the delay in language development. Many countries have implemented early detection and hearing intervention and conducted regional universal newborn hearing screening (UNHS). However, the benefits of UNHS in later childhood have not yet been confirmed, although language development at school age has a lifelong impact on children's future. Our Research on Sensory and Communicative Disorders project attempted to reveal the effects of UNHS and those of early intervention on the development of verbal communication in Japanese children. In this study, 319 children with prelingual bilateral severe to profound hearing loss, 4 to 10 years of age, were evaluated with the Test of Question-Answer Interaction Development used as an objective variable. Participation in UNHS and early intervention were used as explanatory variables. The adjusted odds ratio (AOR) was calculated after adjusting several confounding factors with use of logistic regression analysis. In addition, caregivers' answers were obtained by a questionnaire, and the process of diagnosis with and without UNHS was analyzed retrospectively. Early intervention was significantly associated with better language development (AOR, 3.23; p identification leads directly to early intervention.

  7. Profound Effects of Aggregatibacter actinomycetemcomitans Leukotoxin Mutation on Adherence Properties Are Clarified in in vitro Experiments.

    Directory of Open Access Journals (Sweden)

    Senthil Kumar Velusamy

    Full Text Available Leukotoxin (Ltx is a prominent virulence factor produced by Aggregatibacter actinomycetemcomitans, an oral microorganism highly associated with aggressive periodontitis. Ltx compromises host responsiveness by altering the viability of neutrophils, lymphocytes, and macrophages. Previously, we developed a Rhesus (Rh monkey colonization model designed to determine the effect of virulence gene mutations on colonization of A. actinomycetemcomitans. Unexpectedly, an A. actinomycetemcomitans leukotoxin (ltxA mutant (RhAa-VS2 failed to colonize in the Rh model. No previous literature suggested that Ltx was associated with A. actinomycetemcomitans binding to tooth surfaces. These results led us to explore the broad effects of the ltxA mutation in vitro. Results indicated that LtxA activity was completely abolished in RhAa-VS2 strain, while complementation significantly (P<0.0001 restored leukotoxicity compared to RhAa-VS2 strain. RT-PCR analysis of ltx gene expression ruled out polar effects. Furthermore, binding of RhAa-VS2 to salivary-coated hydroxyapatite (SHA was significantly decreased (P<0.0001 compared to wild type RhAa3 strain. Real time RT-PCR analysis of the genes related to SHA binding in RhAa-VS2 showed that genes related to binding were downregulated [rcpA (P = 0.018, rcpB (P = 0.02, tadA (P = 0.002] as compared to wild type RhAa3. RhAa-VS2 also exhibited decreased biofilm depth (P = 0.008 and exo-polysaccharide production (P<0.0001. Buccal epithelial cell (BEC binding of RhAa-VS2 was unaffected. Complementation with ltxA restored binding to SHA (P<0.002 but had no effect on biofilm formation when compared to RhAa3. In conclusion, mutation of ltxA diminished hard tissue binding in vitro, which helps explain the previous in vivo failure of a ltxA knockout to colonize the Rh oral cavity. These results suggest that; 1 one specific gene knockout (in this case ltxA could affect other seemingly unrelated genes (such as rcpA, rcpB tadA etc, and 2

  8. Glutamatergic modulation of separation distress: profound emotional effects of excitatory amino acids in chicks.

    Science.gov (United States)

    Normansell, Larry; Panksepp, Jaak

    2011-10-01

    Pre-clinical models of brain affective circuits provide relevant evidence for understanding the brain systems that figure heavily in psychiatric disorders. Social isolation and the resulting separation distress contribute to the onset of depression. In this work, the effects of excitatory amino acids (EAA) on isolation-induced distress vocalization (DV) were assessed in young domestic chicks. Both glutamate and quisqualate (QA) produced dose-dependent reductions in DVs, while N-methyl-d-aspartate (NMDA) and kainate (KA) increased DVs. Such a differential pattern of responsiveness may indicate the presence of reciprocal or interacting EAA systems in the brain control of separation distress. Administration of either the NMDA receptor antagonist 2-amino-5-phosphonovalerate (APV) or the broad-spectrum antagonist gamma-d-glutamylglycine (DGG) greatly reduced DVs, as did the antagonist 2-amino-4-phosphonobutyrate (APB). APV did not attenuate the increase in vocalizations seen after NMDA or KA administration. DGG, however, was able to block the increase in calling produced by either of these agonists, suggesting a KA receptor mechanism. KA treatment inhibited the ability of other chicks, or auditory and somatosensory information, to suppress DVs. KA-treated animals exhibited a hyperemotional behavior pattern during which a variety of motivated behaviors were disrupted including reactions to novel objects, approaching the flock, and foraging. They could not sustain a coherent flock-like social cohesion, but exhibited strong fixed-action patterns of flight interspersed with hiding and crouching behaviors. The evident behavioral changes suggest that glutamatergic synapses directly influence sensory, motor and emotional processes in the brain and may be especially important in the integration of environmental stimuli with emotional central state processes of animals. Considering that unresolved social loss and grief have been deemed to be among the main precipitating causes

  9. The effectiveness of bilateral cochlear implants for severe-to-profound deafness in adults: a systematic review.

    Science.gov (United States)

    van Schoonhoven, Jelmer; Sparreboom, Marloes; van Zanten, Bert G A; Scholten, Rob J P M; Mylanus, Emmanuel A M; Dreschler, Wouter A; Grolman, Wilko; Maat, Bert

    2013-02-01

    Assessment of the clinical effectiveness of bilateral cochlear implantation compared with unilateral cochlear implantation or bimodal stimulation, in adults with severe-to-profound hearing loss. In 2007, the National Institute for Health and Clinical Excellence (NICE) in the U.K. conducted a systematic review on cochlear implantation. This study forms an update of the adult part of the NICE review. The electronic databases MEDLINE and Embase were searched for English language studies published between October 2006 and March 2011. Studies were included that compared bilateral cochlear implantation with unilateral cochlear implantation and/or with bimodal stimulation, in adults with severe-to-profound sensorineural hearing loss. Speech perception in quiet and in noise, sound localization and lateralization, speech production, health-related quality of life, and functional outcomes were analyzed. Data extraction forms were used to describe study characteristics and the level of evidence. The effect size was calculated to compare different outcome measures. Pooling of data was not possible because of the heterogeneity of the studies. As in the NICE review, the level of evidence of the included studies was low, although some of the additional studies showed less risk of bias. All studies showed a significant bilateral benefit in localization over unilateral cochlear implantation. Bilateral cochlear implants were beneficial for speech perception in noise under certain conditions and several self-reported measures. Most speech perception in quiet outcomes did not show a bilateral benefit. The current review provides additional evidence in favor of bilateral cochlear implantation, even in complex listening situations.

  10. The effects of profound hypothermia on pancreas ischemic injury: a new experimental model.

    Science.gov (United States)

    Rocha-Santos, Vinicius; Ferro, Oscar Cavalcante; Pantanali, Carlos Andrés; Seixas, Marcel Povlovistsch; Pecora, Rafael Antonio Arruda; Pinheiro, Rafael Soares; Claro, Laura Carolina López; Abdo, Emílio Elias; Chaib, Eleazar; D'Albuquerque, Luiz Augusto Carneiro

    2014-08-01

    Pancreatic ischemia-reperfusion (IR) has a key role in pancreas surgery and transplantation. Most experimental models evaluate the normothermic phase of the IR. We proposed a hypothermic model of pancreas IR to evaluate the benefic effects of the cold ischemic phase. We performed a reproducible model of hypothermic pancreatic IR. The ischemia was induced in the pancreatic tail portion (1-hour ischemia, 4-hour reperfusion) in 36 Wistar rats. They are divided in 3 groups as follows: group 1 (control), sham; group 2, normothermic IR; and group 3, hypothermic IR. In group 3, the temperature was maintained as close to 4.5°C. After reperfusion, serum amylase and lipase levels, inflammatory mediators (tumor necrosis factor α, interleukin 6), and pancreas histology were evaluated. In pancreatic IR groups, amylase, cytokines, and histological damage were significantly increased when compared with group 1. In the group 3, we observed a significant decrease in tumor necrosis factor α (P = 0.004) and interleukin 6 (P = 0.001) when compared with group 2. We did not observe significant difference in amylase (P = 0.867), lipase (P = 0.993), and histology (P = 0.201). In our experimental model, we reproduced the cold phase of pancreas IR, and the pancreas hypothermia reduced the inflammatory mediators after reperfusion.

  11. Bacterial mechanisms to overcome inhibitory effects of dietary tannins.

    Science.gov (United States)

    Smith, Alexandra H; Zoetendal, Erwin; Mackie, Roderick I

    2005-08-01

    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 anti-nutritional effects. The reason for the protective effect is unclear, but could be elucidated if the mechanism(s) by which tannins inhibit bacteria and the mechanisms of tannin resistance were understood. A review of the literature indicates that the ability of tannins to complex with polymers and minerals is the basis of the inhibitory effect on gastrointestinal bacteria. Mechanisms by which bacteria can overcome inhibition include tannin modification/degradation, dissociation of tannin-substrate complexes, tannin inactivation by high-affinity binders, and membrane modification/repair and metal ion sequestration. Understanding the mechanism of action of tannins and the mechanism(s) bacteria use to overcome the inhibitory effects will allow better management of the rumen ecosystem to reduce the anti-nutritional effects of tannin-rich fodder plants and thereby improve ruminant production.

  12. Inhibitory effect of tenomodulin versus ranibizumab on in vitro angiogenesis

    Directory of Open Access Journals (Sweden)

    Wei Wang

    2017-08-01

    Full Text Available AIM: To evaluate anti-angiogenic effect of tenomodulin (TNMD and ranibizumab on cell proliferation and capillary-like morphogenesis of vascular endothelial cells under the stimulation of vascular endothelial growth factor (VEGF in vitro. METHODS: The effects of TNMD and ranibizumab on VEGF-induced proliferation of human umbilical vein endothelial cells (HUVECs were evaluated by MTT assay, and the effects of TNMD and ranibizumab on capillary-like structures formed by HUVECs under the stimulation of VEGF were examined in culture. Capillary-like morphogenesis of HUVECs was quantitatively evaluated, and total lengths of tube-like structures per field were measured in a masked way. RESULTS: HUVECs with both ranibizumab and TNMD protein showed MTT reduction in VEGF-stimulated cell proliferation as expected, while MTT absorbance in the HUVECs with TNMD was significantly declined than that with ranibizumab (P<0.01. The capillary-like structures formed by HUVECs were markedly impaired by the presence of both TNMD and ranibizumab in the culture medium. The total length of the capillary-like structures per field was significantly shorter in the medium with TNMD than that of ranibizumab (P<0.01. The inhibitory effect of TNMD on tube formation in vitro angiogenesis was significantly stronger than that of ranibizumab. CONCLUSION: TNMD may have stronger inhibitory effect than ranibizumab on in vitro angiogenesis.

  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 hydroxycinnamic acids on Dekkera spp.

    Science.gov (United States)

    Harris, Victoria; Jiranek, Vladimir; Ford, Christopher M; Grbin, Paul R

    2010-03-01

    Simple phenolic components of wine, hydroxycinnamic acids (HCAs) are known to have antimicrobial properties. This study sought to determine the potential of ferulic acid as an antifungal agent for the control of Dekkera. Growth was inhibited by all HCAs examined in this study, with ferulic acid being the most potent at all concentrations. In the presence of ethanol, the inhibitory effects of ferulic acid were amplified. Scanning electron microscopy images reveal cellular damage upon exposure to ferulic acid. Thus, manipulation of ferulic acid concentrations could be of industrial significance for control of Dekkera and may be the basis for differences in susceptibility of wines to Dekkera spoilage.

  15. In vitro inhibitory effect of methanol leaf extract of Stachytarpheta ...

    African Journals Online (AJOL)

    and presence of propranolol (1.54 mM) respectively. Results: SJ exhibited significant inhibitory effects on OT and CaCl2 induced uterine contractions (p <. 0.05). The EC50 for OT increased from 1.92 ± 0.12 to 7.16 ± 0.16 nM and that for CaCl2 increased from. 0.19 ± 0.09 to 0.76 ± 0.11 mM in the presence of the extract.

  16. Effects of music on seizure frequency in institutionalized subjects with severe/profound intellectual disability and drug-resistant epilepsy.

    Science.gov (United States)

    D'Alessandro, Patrizia; Giuglietti, Marta; Baglioni, Antonella; Verdolini, Norma; Murgia, Nicola; Piccirilli, Massimo; Elisei, Sandro

    2017-09-01

    Approximately one-third of patients with epilepsy continue to experience seizures despite adequate therapy with antiepileptic drugs. Drug-resistant epilepsy is even more frequent in subjects with intellectual disability. As a result, several non-pharmacological interventions have been proposed to improve quality of life in patients with intellectual disability and drug-resistant epilepsy. A number of studies have demonstrated that music can be effective at reducing seizures and epileptiform discharges. In particular, Mozart's sonata for two pianos in D major, K448, has been shown to decrease interictal EEG discharges and recurrence of clinical seizures in patients with intellectual disability and drug-resistant epilepsy as well. The aim of this study is to investigate the influence of Mozart's music on seizure frequency in institutionalized epileptic subjects with profound/severe intellectual disability. Twelve patients (10 males and 2 females) with a mean age of 21.6 years were randomly assigned to two groups in a cross-over design; they listened to Mozart K448 once a day for six months. A statistically significant difference was observed between the listening period and both baseline and control periods. During the music period, none of the patients worsened in seizure frequency; one patient was seizure-free, five had a greater than 50% reduction in seizure frequency and the remaining showed minimal (N=2) or no difference (N=4). The average seizure reduction compared to the baseline was 20.5%. Our results are discussed in relation to data in the literature considering differences in protocol investigation. Music may be considered a useful approach as add-on therapy in some subjects with profound intellectual disability and drug-resistant epilepsy and can provide a new option for clinicians to consider, but further large sample, multicenter studies are needed to better understand the characteristics of responders and non-responders to this type of non

  17. Effects of living room, Snoezelen room, and outdoor activities on stereotypic behavior and engagement by adults with profound mental retardation.

    Science.gov (United States)

    Cuvo, A J; May, M E; Post, T M

    2001-01-01

    Two experiments were conducted to test the effect of a room with sensory equipment, or Snoezelen room, on the stereotypic behavior and engagement of adults with profound mental retardation. In Experiment 1, participants were observed in their living room before and after attending the Snoezelen room. Results showed that there tended to be a reduction in stereotypy and increase in engagement when participants went from their living room to the Snoezelen room, and a return of these behaviors to pre-Snoezelen levels in the living room. Positive effects in the Snoezelen room did not carryover to the living room. In Experiment 2, the living and Snoezelen rooms were compared to an outdoor activity condition with the same participants and target behaviors. Results showed that the outdoor condition was superior, the Snoezelen condition intermediate, and the living room least effective in their impact on stereotypic behavior and engagement. Conceptualizations regarding factors that maintain stereotypic behavior and engagement were discussed in the context of the three experimental conditions.

  18. Inhibitory Effect of Baicalin and Baicalein on Ovarian Cancer Cells

    Directory of Open Access Journals (Sweden)

    Gary O. Rankin

    2013-03-01

    Full Text Available Ovarian cancer is one of the primary causes of death for women all through the Western world. Baicalin and baicalein are naturally occurring flavonoids that are found in the roots and leaves of some Chinese medicinal plants and are thought to have antioxidant activity and possible anti-angiogenic, anti-cancer, anxiolytic, anti-inflammatory and neuroprotective activities. Two kinds of ovarian cancer (OVCAR-3 and CP-70 cell lines and a normal ovarian cell line (IOSE-364 were selected to be investigated in the inhibitory effect of baicalin and baicalein on cancer cells. Largely, baicalin and baicalein inhibited ovarian cancer cell viability in both ovarian cancer cell lines with LD50 values in the range of 45–55 µM for baicalin and 25–40 µM for baicalein. On the other hand, both compounds had fewer inhibitory effects on normal ovarian cells viability with LD50 values of 177 µM for baicalin and 68 µM for baicalein. Baicalin decreased expression of VEGF (20 µM, cMyc (80 µM, and NFkB (20 µM; baicalein decreased expression of VEGF (10 µM, HIF-1α (20 µM, cMyc (20 µM, and NFkB (40 µM. Therefore baicalein is more effective in inhibiting cancer cell viability and expression of VEGF, HIF-1α, cMyc, and NFκB in both ovarian cancer cell lines. It seems that baicalein inhibited cancer cell viability through the inhibition of cancer promoting genes expression including VEGF, HIF-1α, cMyc, and NFκB. Overall, this study showed that baicalein and baicalin significantly inhibited the viability of ovarian cancer cells, while generally exerting less of an effect on normal cells. They have potential for chemoprevention and treatment of ovarian cancers.

  19. Family influences on the cognitive development of profoundly deaf children: exploring the effects of socioeconomic status and siblings.

    Science.gov (United States)

    Macaulay, Catrin E; Ford, Ruth M

    2013-10-01

    We evaluated the cognitive development of 48 profoundly deaf children from hearing families (born 1994-2002, mean age M = 8.0 years at time of test, none of whom had received early auditory-verbal therapy) as a function of family socioeconomic status and number of siblings. Overall, the deaf children matched a younger group of 47 hearing controls (M = 4.6 years) on verbal ability, theory of mind, and cognitive inhibition. Partial correlations (controlling for age) revealed positive relations in the hearing group between maternal education and inhibition, between number of younger siblings and references to emotions, and between number of close-in-age siblings and references to desires and false beliefs. In the deaf group, there were positive relations between household income and memory span, between maternal education and references to false beliefs, and between number of younger siblings and nonverbal ability. In contrast, deaf children with a greater number of older siblings aged ≤12 years showed inferior memory span, inhibition, belief understanding, picture-sequencing accuracy, and mental-state language, suggesting that they failed to compete successfully with older siblings for their parents' attention and material resources. We consider the implications of the findings for understanding birth-order effects on deaf and language-impaired children.

  20. Systematic Moiety Variations of Ultrashort Peptides Produce Profound Effects on Self-Assembly, Nanostructure Formation, Hydrogelation, and Phase Transition

    KAUST Repository

    Chan, Kiat Hwa

    2017-10-04

    Self-assembly of small biomolecules is a prevalent phenomenon that is increasingly being recognised to hold the key to building complex structures from simple monomeric units. Small peptides, in particular ultrashort peptides containing up to seven amino acids, for which our laboratory has found many biomedical applications, exhibit immense potential in this regard. For next-generation applications, more intricate control is required over the self-assembly processes. We seek to find out how subtle moiety variation of peptides can affect self-assembly and nanostructure formation. To this end, we have selected a library of 54 tripeptides, derived from systematic moiety variations from seven tripeptides. Our study reveals that subtle structural changes in the tripeptides can exert profound effects on self-assembly, nanostructure formation, hydrogelation, and even phase transition of peptide nanostructures. By comparing the X-ray crystal structures of two tripeptides, acetylated leucine-leucine-glutamic acid (Ac-LLE) and acetylated tyrosine-leucine-aspartic acid (Ac-YLD), we obtained valuable insights into the structural factors that can influence the formation of supramolecular peptide structures. We believe that our results have major implications on the understanding of the factors that affect peptide self-assembly. In addition, our findings can potentially assist current computational efforts to predict and design self-assembling peptide systems for diverse biomedical applications.

  1. The inhibitory effect of ethylenediamine on mushroom tyrosinase.

    Science.gov (United States)

    Alijanianzadeh, Mahdi; Saboury, Ali Akbar; Ganjali, Mohammad Reza; Hadi-Alijanvand, Hamid; Moosavi-Movahedi, Ali Akbar

    2012-04-01

    The inhibitory effect of ethylenediamine on both activities of mushroom tyrosinase (MT) at 20 °C in a 10 mM phosphate buffer solution (pH 6.8), was studied. L-DOPA and L-tyrosine were used as substrates of catecholase and cresolase activities, respectively. The results showed that ethylenediamine competitively inhibits both activities of the enzyme with inhibition constants (K(i)) of 0.18±0.05 and 0.14±0.01 μM for catecholase and cresolase respectively, which are lower than the reported values for other MT inhibitors. For further insight a docking study between tyrosinase and ethylenediamine was performed. The docking simulation showed that ethylenediamine binds in the active site of the enzyme near the Cu atoms and makes 3 hydrogen bonds with two histidine residues of active site. Copyright © 2012 Elsevier B.V. All rights reserved.

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

    National Research Council Canada - National Science Library

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

    2015-01-01

    .... Inhibitory effects of the oils were assessed on periodontopathic Porphyromonas gingivalis and Aggregatibacter actinomycetemcomitans and cariogenic Streptococcus mutans and Lactobacillus acidophilus...

  3. The Hands with Eyes and Nose in the Palm: As Effective Communication Alternatives for Profoundly Deaf People in Zimbabwe

    Science.gov (United States)

    Mutswanga, Phillipa

    2017-01-01

    Drawing from the experiences and testimonies of people with profound deafness, the study qualitatively explored the use of the hands with eyes and nose in the palm as communication alternatives in the field of deafness. The study was prompted by the 27 year old lady, Leah Katz-Hernandez who is deaf who got engaged in March 2015 as the 2016…

  4. The False-Friend Effect in Three Profoundly Deaf Learners of French: Disentangling Morphology, Phonology and Orthography

    Science.gov (United States)

    Janke, Vikki; Kolokonte, Marina

    2015-01-01

    Three profoundly deaf individuals undertook a low-frequency backward lexical translation task (French/English), where morphological structure was manipulated and orthographic distance between test items was measured. Conditions included monomorphemic items (simplex), polymorphemic items (complex), items whose French morphological structure…

  5. The Effect of Frequency Transposition on Speech Perception in Adolescents and Young Adults with Profound Hearing Loss

    Science.gov (United States)

    Gou, J.; Smith, J.; Valero, J.; Rubio, I.

    2011-01-01

    This paper reports on a clinical trial evaluating outcomes of a frequency-lowering technique for adolescents and young adults with severe to profound hearing impairment. Outcomes were defined by changes in aided thresholds, speech perception, and acceptance. The participants comprised seven young people aged between 13 and 25 years. They were…

  6. Normalization of Institutional Mealtimes for Profoundly Retarded Persons: Effects and Noneffects of Teaching Family-Style Dining.

    Science.gov (United States)

    Wilson, Philip G.; And Others

    1984-01-01

    The study evaluated a program for teaching family-style mealtime skills to four profoundly retarded institutionalized adolescents. The program used forward chaining with a less-to-more intrusive prompting sequence and contingent reinforcement to teach the skills. (Author/DB)

  7. Multi-Sensory Rooms: Comparing Effects of the Snoezelen and the Stimulus Preference Environment on the Behavior of Adults with Profound Mental Retardation

    Science.gov (United States)

    Fava, Leonardo; Strauss, Kristin

    2010-01-01

    The present study examined whether Snoezelen and Stimulus Preference environments have differential effects on disruptive and pro-social behaviors in adults with profound mental retardation and autism. In N = 27 adults these target behaviors were recorded for a total of 20 sessions using both multi-sensory rooms. Three comparison groups were…

  8. Inhibitory effects of Sudanese plant extracts on HIV-1 replication and HIV-1 protease.

    Science.gov (United States)

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

    1999-02-01

    Forty-eight methanol and aqueous extracts from Sudanese plants were screened for their inhibitory activity on viral replication. Nineteen extracts showed inhibitory effects on HIV-induced cytopathic effects (CPE) on MT-4 cells. The extracts were further screened against HIV-1 protease (PR) using an HPLC assay method. Of the tested extracts, the methanol extracts of Acacia nilotica (bark and pods), Euphorbia granulata (leaves), Maytenus senegalensis (stem-bark) and aqueous extracts of A. nilotica (pods) and M. senegalensis (stem-bark) showed considerable inhibitory effects against HIV-1 PR. Inhibitory principles were isolated from M. senegalensis and their activities were also discussed.

  9. 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.

  10. Acetylcholinesterase inhibitory effects of some plants from Rosaceae

    Directory of Open Access Journals (Sweden)

    S. Esmaeili

    2015-10-01

    Full Text Available Background and objectives: Alzheimer's disease (AD is an age dependent disorder. AD is associated with decrease of brain acetylcholine level. Nowadays, one of the methods for progression inhibition of AD is using acetylcholinesterase inhibitors. Rosaceae is a large plant family. Different biological effects of some species of this family have been reported. The aim of the present study was to assess the acetylcholinesterase inhibitory (AChEI activity of the selected plants belonging to Rosaceae family. Methods: AChEI activity of six species from Rosaceae including Cotoneaster nummularia, Cerasus microcarpa, Amygdalus scoparia, Agrimonia eupatoria, Rosa canina and Rosa damascena were evaluated based on Ellman’s method in concentration of 300 µg/mL using total extracts and methanol fractions which were obtained by maceration. Results: The results showed that the total extract and methanol fraction of the aerial parts of A. eupatoria demonstrated significant AChEI activity with 46.5% and 56.2% inhibition of the enzyme, respectively. Conclusion: According to the results of the AChEI activity of the methanol fraction of A. eupatoria, it seems that the polar components of the species such as flavonoids may be responsible for its effectiveness.

  11. 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.

  12. Inhibitory Effect of Heparin on Gentamicin Concentrations in Blood

    Science.gov (United States)

    Regamey, Claude; Schaberg, Dennis; Kirby, William M. M.

    1972-01-01

    In monitoring gentamicin concentrations in the blood of patients with renal insufficiency, the assayed antibiotic concentration was found to be lower when the sample was drawn as heparinized plasma rather than as serum. This lowering of gentamicin concentrations by heparin was studied further by adding increasing doses of heparin and various amounts of gentamicin to human serum. With a range of 2 to 100 units of heparin per ml, gentamicin concentrations in the serum were lowered by 9 to 14%; with higher heparin concentrations, an even greater and increasing inhibition was noticed, reaching 56% for 1,000 units/ml. This inhibitory effect of heparin on gentamicin was reversible by dilution, indicating that it was not due to degradation or to formation of an inactive chemical complex. Underestimation by the laboratory of gentamicin concentrations in blood is likely to be greatest with capillary tubes, with which the concentration of heparin is especially high. With clinical heparinization, the amount of active heparin in the blood does not exceed 10 units/ml and is for the most part under 3 units/ml; thus, therapeutically significant inhibition of the antibiotic is unlikely in patients receiving anticoagulation. PMID:4670696

  13. 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.

  14. 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.

  15. Inhibitory Effects of Respiration Inhibitors on Aflatoxin Production

    Science.gov (United States)

    Sakuda, Shohei; Prabowo, Diyan Febri; Takagi, Keiko; Shiomi, Kazuro; Mori, Mihoko; Ōmura, Satoshi; Nagasawa, Hiromichi

    2014-01-01

    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. PMID:24674936

  16. Inhibitory effects of capsaicinoids on fatty acid desaturation in a rat liver cell line.

    Science.gov (United States)

    Nakano, N; Shirasaka, N; Masuoka, K; Murakami, T; Watanabe, T; Kobata, K; Shimizu, S; Yoshizumi, H

    2001-08-01

    The inhibitory effects of such vanillylamides as capsaicin and nine capsaicinoids on fatty acid desaturation in liver cells were investigated by using the cultured rat liver cell line, BRL-3A. When capsaicin was added to the medium, it had a relatively strong inhibitory effect on delta6 desaturation and clear inhibitory effects on delta5 and C24delta16 desaturation (delta16 desaturation of C24-polyunsaturated fatty acids). Capsaicinoids with side carbon chain lengths of C10:0 and C12:0 expressed the maximum inhibitory effects of the nine capsaicinoids on fatty acid desaturation in the BRL-3A cells. The inhibitory effects of the capsaicinoids were not correlated with their pungency.

  17. 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.

  18. 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...

  19. 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 ...

  20. Inhibitory Effect of Cow Urine against Colletotrichum capsici Isolated ...

    African Journals Online (AJOL)

    Cow urine has got several applications in agriculture. It is shown to possess inhibitory activity against many phytopathogenic fungi and bacteria. Among various diseases of Chilli, anthracnose is the most important disease which results in drastic reduction in yield. The present study was conducted with an aim to determine ...

  1. Growth inhibitory and cytotoxic effects of the methanol extract of ...

    African Journals Online (AJOL)

    inflammatory, anti-malaria, anti-diabetics, and antihypertensive properties in combination with other plants. The seeds have particularly served as thickener in certain soups like 'egusi' and 'ogbono' in the eastern part of Nigeria. The growth inhibitory and ...

  2. 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

  3. Inhibitory effect of artocarpanone from Artocarpus heterophyllus on melanin biosynthesis.

    Science.gov (United States)

    Arung, Enos Tangke; Shimizu, Kuniyoshi; Kondo, Ryuichiro

    2006-09-01

    In our previous efforts to find new tyrosinase inhibitory materials, we investigated 44 Indonesian medicinal plants belonging to 24 families. Among those plants, the extract of Artocarpus heterophyllus was one of the strongest inhibitors of tyrosinase activity. By activity-guided fractionation of A. heterophyllus wood extract, we isolated artocarpanone, which inhibited both mushroom tyrosinase activity and melanin production in B16 melanoma cells. This compound is a strong candidate as a remedy for hyperpigmentation in human skin.

  4. Human ACAT inhibitory effects of shikonin derivatives from Lithospermum erythrorhizon.

    Science.gov (United States)

    An, Sojin; Park, Yong-Dae; Paik, Young-Ki; Jeong, Tae-Sook; Lee, Woo Song

    2007-02-15

    Three naphthoquinones were isolated by bioassay-guided fractionation from the CHCl(3) extracts of roots of Lithospermum erythrorhizon. They were identified as acetylshikonin (1), isobutyrylshikonin (2), and beta-hydroxyisovalerylshikonin (3) on the basis of their spectroscopic analyses. The compounds 1-3 were tested for their inhibitory activities against human ACAT-1 (hACAT-1) or human ACAT-2 (hACAT-2). Compound 2 preferentially inhibited hACAT-2 (IC(50)=57.5microM) than hACAT-1 (32% at 120microM), whereas compounds 1 and 3 showed weak inhibitory activities in both hACAT-1 and -2. To develop more potent hACAT inhibitor, shikonin derivatives (5-11) were synthesized by semi-synthesis of shikonin (4), which was prepared by hydrolysis of 1-3. Among them, compounds 5 and 7 exhibited the strong inhibitory activities against hACAT-1 and -2. Furthermore, we demonstrated that compound 7 behaved as a potent ACAT inhibitor in not only in vitro assay system but also cell-based assay system.

  5. Telomerase Inhibitory Effects of Red Pigment Rubropunctatin and Statin Monacolin L Isolated from Red Yeast Rice.

    Science.gov (United States)

    Xu, Baojun; Wang, Qijun; Sung, Changkeun

    2017-04-26

    In addition to the cholesterol-lowering activity of red yeast rice (RYR), its anticancer activities have been frequently reported. However, the mechanism of action of the anticancer activity of RYR is not yet fully understood. The objective of the current study was to elucidate anticancer compositions and anticancer mechanism of actions of RYR. The isolated compounds from RYR were subjected to anti-proliferation assay, apoptosis assay via flow cytometry, and telomerase inhibitory assay via telomeric repeat amplification protocol-PCR (TRAP-PCR) assay, and Western blotting assay in an in vitro cell culture system. The results showed that a statin, monacolin L, and a red pigment, rubropunctatin, from RYR exhibited very strong cancer cell proliferation inhibitory effects; the rubropunctatin was comparable with anticancer drug cis-platinum, taxol, and 10-hydroxy-camptothecin (HCPT) in their IC50 values. Monacolin L and rubropunctatin exerted their anticancer activity via telomerase inhibitory effects. Monacolin L and rubropunctatin presented the similar telomerase inhibitory effects as the anticancer drug cis-platinum, while the anticancer drug HCPT presented a weak telomerase inhibitory effect in the TRAP-PCR assay. Meanwhile, rubropunctatin and cis-platinum did not present strong apoptosis induction activity as the momacolin L and HCPT did. These results indicate that the RYR may exert anticancer effects through the telomerase inhibitory effect of rubropunctatin and the apoptosis-induction effect of monacolin L.

  6. Inhibitory effects of Taraxacum mongolicum with phreatic water on melanin synthesis

    OpenAIRE

    Jang, Moon-Hee; Ahn, Taek-Won

    2014-01-01

    Background: Recently, people have begun showing heightened interest in skin whitening. Melanin is an important factor that determines skin color. The purpose of this study is to investigate the inhibitory effect of Taraxacum mongolicum (TAM) with phreatic water (PW) from Dogo Hot Springs on melanin synthesis. Methods: We assessed the inhibitory effects of TAM on melanin synthesis in B16F10 mouse melanoma cells. The mRNA levels of tyrosinase related protein (TRP)-1, TRP-2, tyrosinase, MITF,...

  7. 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.

  8. 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.

  9. Telomerase-inhibitory effects of sugar-modified nucleotide analogs.

    Science.gov (United States)

    Jinmei, Hiroshi; Takahashi, Hazuki; Amano, Rie; Suzuki, Kaori; Saneyoshi, Mineo; Yamaguchi, Toyofumi

    2002-01-01

    Telomerase is an endogenous reverse transcriptase that uses its internal RNA moiety as a template for the synthesis of telomere repeats, thus maintaining telomere length. To study the susceptibility of telomerase to sugar-modified nucleotide analogs, inhibition by arabinofuranosylguanine 5'-triphosphate (araGTP), 3'-azido-2',3'-dideoxyguanosine 5'-triphosphate (AZdGTP), 2',3'-dideoxy-2'-fluoroarabino-furanosylguanine 5'-triphosphate (FaraGTP), and their thymine counterparts was investigated. Among these compounds, all dGTP analogs showed potent inhibitory activity against human telomerase. Conversely, dTTP analogs showed moderate or weak inhibition. Partially purified telomerase from cherry salmon testis utilized ddGTP and AZdGTP as substrates into the 3'-terminus of DNA.

  10. Inhibitory effect of Lactobacillus salivarius on Streptococcus mutans biofilm formation.

    Science.gov (United States)

    Wu, C-C; Lin, C-T; Wu, C-Y; Peng, W-S; Lee, M-J; Tsai, Y-C

    2015-02-01

    Dental caries arises from an imbalance of metabolic activities in dental biofilms developed primarily by Streptococcus mutans. This study was conducted to isolate potential oral probiotics with antagonistic activities against S. mutans biofilm formation from Lactobacillus salivarius, frequently found in human saliva. We analysed 64 L. salivarius strains and found that two, K35 and K43, significantly inhibited S. mutans biofilm formation with inhibitory activities more pronounced than those of Lactobacillus rhamnosus GG (LGG), a prototypical probiotic that shows anti-caries activity. Scanning electron microscopy showed that co-culture of S. mutans with K35 or K43 resulted in significantly reduced amounts of attached bacteria and network-like structures, typically comprising exopolysaccharides. Spot assay for S. mutans indicated that K35 and K43 strains possessed a stronger bactericidal activity against S. mutans than LGG. Moreover, quantitative real-time polymerase chain reaction showed that the expression of genes encoding glucosyltransferases, gtfB, gtfC, and gtfD was reduced when S. mutans were co-cultured with K35 or K43. However, LGG activated the expression of gtfB and gtfC, but did not influence the expression of gtfD in the co-culture. A transwell-based biofilm assay indicated that these lactobacilli inhibited S. mutans biofilm formation in a contact-independent manner. In conclusion, we identified two L. salivarius strains with inhibitory activities on the growth and expression of S. mutans virulence genes to reduce its biofilm formation. This is not a general characteristic of the species, so presents a potential strategy for in vivo alteration of plaque biofilm and caries. © 2014 John Wiley & Sons A/S. Published by John Wiley & Sons Ltd.

  11. [Inhibitory effects of natural plant extracts on Verticillium albo-atrum].

    Science.gov (United States)

    Zhang, Shuhong; Zhou, Baoli; Zhang, Lei; Fu, Yawen

    2006-06-01

    This paper studied the inhibitory effects of 54 kinds of ethanol-extracted plant solutions on Verticillium albo-atrum. The results showed that 15 kinds of these extracts could inhibit the growth of verticillium albo-atrum mycelium, with an inhibitory rate more than 50%, among which, the inhibitory rate of Asarum sieboldii, Coptis chinensis, Magnolia officinalis, Acacia catechu, Sophora flavescens, Glycyrrhiza uralensis, Cnidium monnieri, Platycodon grandiflorum and Allium. cepa. extracts was higher than 65%, and that of Cnidium monnieri extract reached 86.84%. A total of 16 kinds of plant extracts decreased the spore germination of V. albo-atrum, with the inhibitory rate higher than 70%, and there were 7 kinds of plant extracts whose inhibitory rate reached 95%. Almost no spore bourgeon was found after treated with Asarum sieboldii, Coptis chinensis, and Magnolia officinalis extracts. The extract of Acacia catechu did not inhibit the growth of mycelium, but restrained the spore germination by 100%. Cnidium monnieri extract could strongly inhibit the growth of mycelium, but had a less effect on spore germination rate (only by 11.3%). The active substances found in natural plant extracts which had the inhibitory effects on pathogen brought us a new and promising method to deal with V. albo-atrum and other vegetable diseases.

  12. 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.

  13. Inhibitory effects of pomegranate extracts on recombinant human maltase-glucoamylase.

    Science.gov (United States)

    Kawakami, Kayoko; Li, Peng; Uraji, Misugi; Hatanaka, Tadashi; Ito, Hideyuki

    2014-09-01

    α-Glucosidase inhibitors are currently used in the treatment of type 2 diabetes. In this study, we investigated the inhibitory activities of aril and pericarp extracts from pomegranates obtained various regions against recombinant human maltase-glucoamylase (MGAM). The inhibitory activities of the aril extracts tended to be stronger than those of the pericarp extracts. The Iranian aril extract was the most effective inhibitor. We investigated the polyphenol content of the pomegranate extracts using the Folin-Ciocalteu method. Among the aril extracts, the Iranian aril extract showed the highest polyphenol content. We further evaluated inhibitory activity against α-glucosidase from the rat small intestine. Pomegranate extract used in this study showed slightly different inhibitory activities according to α-glucosidase origin. Iranian aril extract was the most effective inhibitor of α-glucosidases, especially recombinant human MGAM. Bioassay-guided fractionation of the pomegranate arils led to identification of punicalagin and oenothein B as potent inhibitors of α-glucosidase. Oenothein B showed inhibitory activity with a half-maximal inhibitory concentration (IC(50)) value of 174 μM. Its potency was comparable to that of the α-glucosidase inhibitor acarbose with an IC(50) value of 170 μM. Dixon plot kinetic analysis of oenothein B showed a noncompetitive inhibition with a K(i) value of 102 μM. These results suggest that pomegranate arils would be useful for suppressing postprandial hyperglycemia. © 2014 Institute of Food Technologists®

  14. 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.

  15. 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

  16. 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.

  17. Effectiveness of a nurse-led preadmission intervention for parents of children with profound multiple disabilities undergoing hip-joint surgery: A quasi-experimental pilot study.

    Science.gov (United States)

    Seliner, Brigitte; Latal, Beatrice; Spirig, Rebecca

    2017-07-01

    The aim of this study was to assess the effectiveness of a family-centered care (FCC) intervention provided by an advanced practice nurse (APN) for parents of children with profound disabilities undergoing surgery. In a quasi-experimental design, we used the MPOC-20 to assess satisfaction with FCC and interviews to identify potential mechanisms for improving satisfaction. There was a positive effect on the MPOC-20 domain "general information," albeit with a small effect size (Cohen's d = 0.35). The interviewed parents expected additional support. Emphasis should be placed on providing comprehensive care coordination by an experienced APN. Shared care management is crucial in improving FCC. © 2017 Wiley Periodicals, Inc.

  18. 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.

  19. The effect of amitriptyline on inhibitory avoidance in mice is dose-dependent.

    Science.gov (United States)

    Parra, Andrés; Vinader-Caerols, Concepción; Ferrer-Añó, Aránzazu; Urquiza, Adoración; Monleón, Santiago

    2009-11-01

    The purpose of the present work was to study the dose-effect relationship of the antidepressant amitriptyline on inhibitory avoidance in male and female mice. Subjects received physiological saline or 2.5, 5, 10 or 20 mg/kg of amitriptyline hydrochloride 30 min before the training phase, and were subjected to the test phase 24 h later. Results showed a clear impairing effect of amitriptyline on inhibitory avoidance in both male and female mice, and that the effect is dose-dependent.

  20. 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.

  1. 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.

  2. 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

  3. Inhibitory effects of xanthones from guttiferae plants on PAF-induced hypotension in mice.

    Science.gov (United States)

    Oku, Hisae; Ueda, Yoshimi; Iinuma, Munekazu; Ishiguro, Kyoko

    2005-01-01

    The inhibitory effects of 22 xanthones from three Guttiferae plants (Hypericum patulum, Calophyllum inophyllum and C. austroindium) on exogenous platelet activating factor (PAF)-induced hypotension were examined using a blood pressure monitoring in vivo assay method. Guanandin (2), caloxanthone E (3), 1,3,5,6-tetrahydroxy-2-isoprenylxanthone (8), 6-deoxyjacareubin (11) and patulone (18) showed strong inhibition of PAF-induced hypotension, with inhibitory effects of more than 60 %. Their ID50 values were greater than that of ginkgolide B (BN-52 021), a natural PAF-antagonist from the Ginkgo biloba.

  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

    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 trai......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....... Furthermore, gender differences in the training-induced changes in neural activity were found in preschoolers....

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

    Directory of Open Access Journals (Sweden)

    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

  6. Profound effect of profiling platform and normalization strategy on detection of differentially expressed microRNAs--a comparative study.

    Directory of Open Access Journals (Sweden)

    Swanhild U Meyer

    Full Text Available BACKGROUND: Adequate normalization minimizes the effects of systematic technical variations and is a prerequisite for getting meaningful biological changes. However, there is inconsistency about miRNA normalization performances and recommendations. Thus, we investigated the impact of seven different normalization methods (reference gene index, global geometric mean, quantile, invariant selection, loess, loessM, and generalized procrustes analysis on intra- and inter-platform performance of two distinct and commonly used miRNA profiling platforms. METHODOLOGY/PRINCIPAL FINDINGS: We included data from miRNA profiling analyses derived from a hybridization-based platform (Agilent Technologies and an RT-qPCR platform (Applied Biosystems. Furthermore, we validated a subset of miRNAs by individual RT-qPCR assays. Our analyses incorporated data from the effect of differentiation and tumor necrosis factor alpha treatment on primary human skeletal muscle cells and a murine skeletal muscle cell line. Distinct normalization methods differed in their impact on (i standard deviations, (ii the area under the receiver operating characteristic (ROC curve, (iii the similarity of differential expression. Loess, loessM, and quantile analysis were most effective in minimizing standard deviations on the Agilent and TLDA platform. Moreover, loess, loessM, invariant selection and generalized procrustes analysis increased the area under the ROC curve, a measure for the statistical performance of a test. The Jaccard index revealed that inter-platform concordance of differential expression tended to be increased by loess, loessM, quantile, and GPA normalization of AGL and TLDA data as well as RGI normalization of TLDA data. CONCLUSIONS/SIGNIFICANCE: We recommend the application of loess, or loessM, and GPA normalization for miRNA Agilent arrays and qPCR cards as these normalization approaches showed to (i effectively reduce standard deviations, (ii increase sensitivity

  7. Eye Gaze and Aging: Selective and Combined Effects of Working Memory and Inhibitory Control

    Directory of Open Access Journals (Sweden)

    Trevor J. Crawford

    2017-11-01

    Full Text Available Eye-tracking is increasingly studied as a cognitive and biological marker for the early signs of neuropsychological and psychiatric disorders. However, in order to make further progress, a more comprehensive understanding of the age-related effects on eye-tracking is essential. The antisaccade task requires participants to make saccadic eye movements away from a prepotent stimulus. Speculation on the cause of the observed age-related differences in the antisaccade task largely centers around two sources of cognitive dysfunction: inhibitory control (IC and working memory (WM. The IC account views cognitive slowing and task errors as a direct result of the decline of inhibitory cognitive mechanisms. An alternative theory considers that a deterioration of WM is the cause of these age-related effects on behavior. The current study assessed IC and WM processes underpinning saccadic eye movements in young and older participants. This was achieved with three experimental conditions that systematically varied the extent to which WM and IC were taxed in the antisaccade task: a memory-guided task was used to explore the effect of increasing the WM load; a Go/No-Go task was used to explore the effect of increasing the inhibitory load; a ‘standard’ antisaccade task retained the standard WM and inhibitory loads. Saccadic eye movements were also examined in a control condition: the standard prosaccade task where the load of WM and IC were minimal or absent. Saccade latencies, error rates and the spatial accuracy of saccades of older participants were compared to the same measures in healthy young controls across the conditions. The results revealed that aging is associated with changes in both IC and WM. Increasing the inhibitory load was associated with increased reaction times in the older group, while the increased WM load and the inhibitory load contributed to an increase in the antisaccade errors. These results reveal that aging is associated with

  8. Simultaneous presence of endogenous retrovirus and herpes virus antigens has profound effect on cell-mediated immune responses

    DEFF Research Database (Denmark)

    Brudek, Tomasz; Christensen, Tove; Hansen, Hans Jacob

    2004-01-01

    Retroviruses have been suggested as possible pathogenic factors in multiple sclerosis (MS), supported by the observation that endogenous retroviruses are activated in MS patients. Different members of the herpes family of which several are neurotropic have also been suggested as factors in MS...... pathogenesis. Further, interactions between retroviruses and herpes viruses have been implied in the development of MS. The objective of the study was investigation of cell-mediated immune responses of MS patients to retrovirus and herpes virus antigens, particularly antigen combinations, with analyses...... retrovirus HERV-H and herpes virus antigens resulted in highly increased cellular immune responses among both the MS patients and healthy subjects. The increase was synergistic in character in most samples. Very pronounced effects were obtained using HHV-6A and HSV-1 antigens. Blast transformation assays...

  9. 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 ...

  10. 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

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

    African Journals Online (AJOL)

    mammary carcinoma cell line [14]. In addition, emodin has been found to show cytotoxic effects against human oral squamous cell carcinoma. (HSC-2) and ... cancer: epidemiology, pathology and treatment. Ann. Oncol 2003; 14(2): ii31–36. 2. Wu B, Zhang Q, Shen W, Zhu J. Anti-proliferative and chemosensitizing effects of ...

  12. PROFOUND AND SEXUALLY DIMORPHIC EFFECTS OF CLINICALLY-RELEVANT LOW DOSE SCATTER IRRADIATION ON THE BRAIN AND BEHAVIOR

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    Anna eKovalchuk

    2016-06-01

    Full Text Available Irradiated cells can signal damage and distress to both close and distant neighbors that have not been directly exposed to the radiation (naïve bystanders. While studies have shown that such bystander effects occur in the shielded brain of animals upon body irradiation, their mechanism remains unexplored. Observed effects may be caused by some blood-borne factors; however they may also be explained, at least in part, by very small direct doses received by the brain that result from scatter or leakage. In order to establish the roles of low doses of scatter irradiation in the brain response, we developed a new model for scatter irradiation analysis whereby one rat was irradiated directly at the liver and the second rat was placed adjacent to the first and received a scatter dose to its body and brain. This work focuses specifically on the response of the latter rat brain to the low scatter irradiation dose. Here, we provide the first experimental evidence that very low, clinically relevant doses of scatter irradiation alter gene expression, induce changes in dendritic morphology, and lead to behavioral deficits in exposed animals. The results showed that exposure to radiation doses as low as 0.115 cGy caused changes in gene expression and reduced spine density, dendritic complexity, and dendritic length in the prefrontal cortex tissues of females, but not males. In the hippocampus, radiation altered neuroanatomical organization in males, but not in females. Moreover, low dose radiation caused behavioral deficits in the exposed animals. This is the first study to show that low dose scatter irradiation influences the brain and behavior in a sex-specific way.

  13. Inhibitory Effect of Interferons on Contractive Activity of Bovine Mesenteric Lymphatic Vessels and Nodes.

    Science.gov (United States)

    Unt, D V; Lobov, G I

    2017-12-01

    We studied the effect of IFNα-2b and IFNβ-1a on phasic and tonic contractions of isolated bovine mesenteric lymphatic vessels and nodes. IFNα-2b and IFNβ-1a in concentrations of 250-1000 U/ml produced dose-dependent negative chronotropic and inotropic effects on spontaneous phasic contractions and tonus of lymphatic vessels and nodes. In de-endothelialized lymphatic vessels and nodes, IFNα-2b and IFNβ-1a in the same concentrations had less pronounced inhibitory effect on spontaneous contraction and tonus. L-NAME (100 μM) and charybdotoxin (0.1 μM with 0.5 μM apamine) significantly attenuated the inhibitory effect of IFNα-2b on phasic and tonic contractions of lymph nodes. L-NAME (100 μM) and indomethacin (10 μM) significantly reduced the IFNα-2b-induced inhibitory effect on phasic and tonic contractions of lymph node. These results indicate that IFNα-2b and IFNβ-1a have a pronounced inhibitory effect on the phasic and tonic contractions of bovine mesenteric lymphatic vessels and nodes. The responses are endothelium-dependent and are determined by production of NO and endothelium-dependent hyperpolarizing factor by endotheliocytes in lymphatic vessels and by production of NO and prostacyclin by endotheliocytes in the lymphatic nodes.

  14. 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.

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

    Science.gov (United States)

    Hsieh, I-Ju; Chen, Yung Y

    2017-01-01

    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.

  16. The Divergent Effects of Fear and Disgust on Inhibitory Control: An ERP Study.

    Directory of Open Access Journals (Sweden)

    Mengsi Xu

    Full Text Available Negative emotional stimuli have been shown to attract attention and impair executive control. However, two different types of unpleasant stimuli, fearful and disgusting, are often inappropriately treated as a single category in the literature on inhibitory control. Therefore, the present study aimed to investigate the divergent effects of fearful and disgusting distracters on inhibitory control (both conscious and unconscious inhibition. Specifically, participants were engaged in a masked Go/No-Go task superimposed on fearful, disgusting, or neutral emotional contexts, while event-related potentials were measured concurrently. The results showed that for both conscious and unconscious conditions, disgusting stimuli elicited a larger P2 than fearful ones, and the difference waves of P3 amplitude under disgusting contexts were smaller than that under fearful contexts. These results suggest that disgusting distracters consume more attentional resources and therefore impair subsequent inhibitory control to a greater extent. This study is the first to provide electrophysiological evidence that fear and disgust differently affect inhibitory control. These results expand our understanding of the relationship between emotions and inhibitory control.

  17. 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.

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

    African Journals Online (AJOL)

    -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 ...

  19. Blocking the interleukin 2 (IL2)-induced systemic autophagic syndrome promotes profound antitumor effects and limits toxicity.

    Science.gov (United States)

    Lotze, Michael T; Buchser, William J; Liang, Xiaoyan

    2012-08-01

    Cancer is the leading cause of death in the United States in those dying under the age of 85. Although cancer is increasingly controlled as a chronic disease, true cures of patients with metastatic epithelial malignancies have rarely been obtained with currently available systemic therapies. For example, administration of high-dose recombinant interleukin 2 (IL2), enhancing cytolytic immune cell proliferation and delivery, promotes complete antitumor responses in IL2 promotes both T-cell and NK cell induction of immune cell-mediated autophagy (iC-MA) in tumor targets. We have demonstrated that HMGB1 is detected at high levels in the serum of IL2-treated mice with translocation to the cytoplasm from the nucleus in the liver, consistent with HMGB1's release in response to stress, and ability to sustain autophagy. Limiting autophagy in mice with coadministration of chloroquine (CQ) diminishes serum levels of HMGB1, cytokines (IFNG and IL6 but not IL18), and autophagic flux, attenuating weight gain, enhancing DC, T-cell and NK cell numbers, and promoting long-term tumor control in a murine hepatic metastases model. Autophagy (programmed cell survival) is a metabolic process associated with promotion of late cancer growth. In tumor cell lines, CQ treatment limits ATP production through inhibition of oxidative phosphorylation and promotion of apoptosis. CQ increases autophagic vacuoles and LC3-II levels in tumor cells, associated with increased annexin V(+)/PI(-) cells, cleaved-PARP, cleaved-CASP3, and cytochrome c release from mitochondria. These observations, limiting toxicity and prolonging antitumor effects, with a combination of IL2 and autophagy inhibition in murine models are now being tested by the Cytokine Working Group in patients with advanced renal cell carcinoma.

  20. Antiplatelet effects of clopidogrel compared with aspirin after myocardial infarction: enhanced inhibitory effects of combination therapy.

    Science.gov (United States)

    Moshfegh, K; Redondo, M; Julmy, F; Wuillemin, W A; Gebauer, M U; Haeberli, A; Meyer, B J

    2000-09-01

    We sought to compare the inhibitory effects of the combination of two doses of aspirin plus clopidogrel with either drug alone on platelet aggregation and activation. Enhanced platelet inhibitory effects of clopidogrel by aspirin on platelet aggregation and activation are suggested by experimental studies but have not been shown in humans. The effects of clopidogrel 75 mg or aspirin 100 (300) mg on platelet aggregation and activation by flow cytometry after stimulation with various agonists were determined in 30 patients with a past history of myocardial infarction. Clopidogrel alone or in combination with aspirin markedly inhibited adenosine diphosphate (ADP)-mediated platelet aggregation compared with monotherapy with aspirin (24.6 +/- 3.3% or 26.6 +/- 2.7% vs. 44.7 +/- 2.9%; p after stimulation with ADP or thrombin (p after activation with low dose thrombin (p after stimulation with collagen and thrombin compared with monotherapies. Thus, this dual antiplatelet treatment strategy deserves further evaluation in clinical trials for secondary prevention of acute myocardial infarction or unstable angina.

  1. Inhibitory Aromatase Effects of Flavonoids from Ginkgo Biloba Extracts on Estrogen Biosynthesis.

    Science.gov (United States)

    Park, Yong Joo; Choo, Wun Hak; Kim, Ha Ryong; Chung, Kyu Hyuck; Oh, Seung Min

    2015-01-01

    Ginkgo biloba extract (GBE) is a popular phytomedicine and has been used for disorders of the central nervous system, cardiovascular, renal, respiratory, and circulatory diseases. Although GBE is a complex mixture of over 300 compounds, its major components are 24% flavonoids and 6% terpene lactones. In this study, we tested the inhibitory effects of the three major flavonoids (kaempferol, quercetin, and isorhamnetin) from GBE, independently and as mixtures, on aromatase activity using JEG-3 cells (human placental cells) and recombinant proteins (human placental microsome). In both systems, kaempferol showed the strongest inhibitory effects among the three flavonoids; the flavanoid mixtures exerted increased inhibitory effects. The results of exon I.1-driven luciferase reporter gene assays supported the increased inhibitory effects of flavonoid mixtures, accompanied by suppression of estrogen biosynthesis. In the RT-PCR analysis, decreased patterns of aromatase promoter I.1 mRNA expressions were observed, which were similar to the aromatase inhibition patterns of flavonoids and their mixtures. The present study demonstrated that three flavonoids synergistically inhibit estrogen biosynthesis through aromatase inhibition, decrease CYP19 mRNA, and induce transcriptional suppression. Our results support the usefulness of flavonoids in adjuvant therapy for breast cancer by reducing estrogen levels with reduced adverse effects due to estrogen depletion.

  2. [Study of inhibitory effect of extracts from Actinidia arguta on human carcinoma of esophagus cells].

    Science.gov (United States)

    Zhang, Li; Guo, Hong-Li; Tian, Lin; Cao, Shu-Fen; Du, Chang-Hai

    2007-05-01

    To study the inhibitory effect of extracts from Actinidia arguta by n-butyl alcohol on human carcinoma of esophagus cells (Eca-109) and Its mechanism. MTT colonmetric assay was used to examine the growth inhibitory of concentration-effect (1 microg/ml, 10 microg/ml,100 microg/ml) and time-effect (24 h, 48 h, 72 h) of extracts from Actinidia arguta by n-butyl alcohol on Eca-109 cells. TUNEL test were performed to observe the apoptosis induced by the extracts (1 microg/ml, 10 microg/ml, 100 microg/ml) on Eca-109 cells. The inhibitory effect of the extracts on Eca-109 cells increased in a dose-time Manner and the highest rate of inhibition was 87.2%. The extracts could significantly induce apoptosis of Eca-109 cells, but in control group, apoptosis wasn't observed. The extracts from Actinidia arguta by n-butyl alcohol have good inhibitory effect on Eca-109 cells.

  3. 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.

  4. The Bacterial and Fungal inhibitory effect of extracts from ...

    African Journals Online (AJOL)

    Welcome

    2013-04-24

    Apr 24, 2013 ... Figure 1. The effect of maackiain acetate,formononetin,chlorophorin and Iroko on. F. moniliforme. ... of which display therapeutic activity (Yoon et al., 2007; Ja. Kim et al., 2006; ..... may explain the mechanism of action of the plant extracts. .... Relationships between the structures and bactericidal properties of ...

  5. Inhibitory Effect of Berberine on Zeste Homolog 2 (Ezh2 ...

    African Journals Online (AJOL)

    Histone methylation inhibitor, 3-deazaneoplanocin A (DZNep), also led to a similar effect on cell proliferation of KYSE450 cells. Berberine treatment also resulted in strong transcriptional reduction of the AXL receptor kinase. The results of qRT-PCR and FACS analyses showed significant inhibition of AXL mRNA and protein ...

  6. Simulated Inhibitory Effects of Typical Byproducts of Biomass ...

    African Journals Online (AJOL)

    The viability test has shown that in the presence of lower concentrations of inhibitors, S. cerevisiae can adapt for the first 12 h of fermentation and then may improve ethanol production yield overtime. At lower concentrations (2 g/l vanillin and 4 g/l acetic acid) the effect of inhibitors on the viability of S. cerevisiae and ethanol ...

  7. Study on the inhibitory effect of total alkaloids of Sophora ...

    African Journals Online (AJOL)

    Background: Ku Dou Zi is the dried whole plant, roots and seeds of Sophora alopecuroides L. in the genus Sophora of family Leguminosae. The entire plant is bitter in taste, cold in nature, and has the heat clearing, detoxifying, pathogenic wind dispelling dampness, analgesic, and insecticidal effects. Modern ...

  8. 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 ...

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

    African Journals Online (AJOL)

    Balmoori J, Stohs SJ. Protective effects of grape seed proanthocyanidins and selected antioxidants against. TPA-induced hepatic and brain lipid peroxidation and. DNA fragmentation, and peritoneal macrophage activation in mice. Gen Pharmacol: The Vascular. System 1998; 30(5): 771-776. 17. Cheung LM, Cheung PCK.

  10. 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 ...

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

    African Journals Online (AJOL)

    STORAGESEVER

    2010-02-08

    Feb 8, 2010 ... 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.

  12. 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).

  13. 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 ...

  14. 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 ...

  15. The inhibitory effect of Lactobacillus sakei KBL isolated from kimchi ...

    African Journals Online (AJOL)

    Aghomotsegin

    2015-08-26

    Aug 26, 2015 ... was to investigate whether extracts from Lactobacillus sakei KBL cells isolated from kimchi could exert anti-adipogenic ... preadipocytes. Key words: Lactobacillus sakei KBL, 3T3-L1 cells, adipocyte differentiation, obesity. ..... Effect of dietary inclusion of Lactobacillus acidophilus ATCC 43121 on cholesterol.

  16. Inhibitory effect of stevioside on calcium influx to produce antihypertension.

    Science.gov (United States)

    Lee, C N; Wong, K L; Liu, J C; Chen, Y J; Cheng, J T; Chan, P

    2001-12-01

    Stevioside is a sweet-tasting glycoside occurring abundantly in the leaves of Stevia rebaudiana (Compositae). It has been used popularly in Japan and Brazil as a sugar substitute for decades. Previous study has shown that it lowered blood pressure in spontaneously hypertensive rats (SHRs) when administered intravenously. This study shows that intraperitoneal injection of stevioside 25 mg/kg also has antihypertensive effect in SHRs. In isolated aortic rings from normal rats, stevioside could dose-dependently relax the vasopressin-induced vasoconstriction in both the presence and absence of endothelium. However, stevioside had no effect on phenylephrine- and KCl-induced phasic vasoconstriction. In addition, stevioside lost its influence on vasopressin-induced vasoconstriction in Ca(2+)-free medium. The results indicate that stevioside caused vasorelaxation via an inhibition of Ca(2+) influx into the blood vessel. This phenomenon was further confirmed in cultured aortic smooth muscle cells (A7r5). Using 10(-5) M methylene blue for 15 min, stevioside could still relax 10(-8) M vasopressin-induced vasoconstriction in isolated rat aortic rings, showing that this vasorelaxation effect was not related to nitric oxide. The present data show that the vasorelexation effect of stevioside was mediated mainly through Ca(2+) influx inhibition.

  17. 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.

  18. 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.

  19. Rat liver mitochondrial membrane characteristics and mitochondrial functions are more profoundly altered by dietary lipid quantity than by dietary lipid quality: effect of different nutritional lipid patterns.

    Science.gov (United States)

    Aoun, Manar; Feillet-Coudray, Christine; Fouret, Gilles; Chabi, Béatrice; Crouzier, David; Ferreri, Carla; Chatgilialoglu, Chryssostomos; Wrutniak-Cabello, Chantal; Cristol, Jean Paul; Carbonneau, Marie-Annette; Coudray, Charles

    2012-03-01

    Dietary lipids are known to affect the composition of the biological membrane and functions that are involved in cell death and survival. The mitochondrial respiratory chain enzymes are membrane protein complexes whose function depends on the composition and fluidity of the mitochondrial membrane lipid. The present study aimed at investigating the impact of different nutritional patterns of dietary lipids on liver mitochondrial functions. A total of forty-eight Wistar male rats were divided into six groups and fed for 12 weeks with a basal diet, lard diet or fish oil diet, containing either 50 or 300 g lipid/kg. The 30 % lipid intake increased liver NEFA, TAG and cholesterol levels, increased mitochondrial NEFA and TAG, and decreased phospholipid (PL) levels. SFA, PUFA and unsaturation index (UI) increased, whereas MUFA and trans-fatty acids (FA) decreased in the mitochondrial membrane PL in 30 % fat diet-fed rats compared with 5 % lipid diet-fed rats. PL UI increased with fish oil diet v. basal and lard-rich diets, and PL trans-FA increased with lard diet v. basal and fish oil diets. The 30 % lipid diet intake increased mitochondrial membrane potential, membrane fluidity, mitochondrial respiration and complex V activity, and decreased complex III and IV activities. With regard to lipid quality effects, β-oxidation decreased with the intake of basal or fish oil diets compared with that of the lard diet. The intake of a fish oil diet decreased complex III and IV activities compared with both the basal and lard diets. In conclusion, the characteristics and mitochondrial functions of the rat liver mitochondrial membrane are more profoundly altered by the quantity of dietary lipid than by its quality, which may have profound impacts on the pathogenesis and development of non-alcoholic fatty liver disease.

  20. 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 ...

  1. 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 ...

  2. 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 ...

  3. 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…

  4. 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.

  5. 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

  6. 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.

  7. 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 ...

  8. Inhibitory Effect of Helicteres gardneriana Ethanol Extract on Acute Inflammation

    Directory of Open Access Journals (Sweden)

    Juliana Oliveira de Melo

    2012-01-01

    Full Text Available The anti-inflammatory effect of an ethanol extract of Helicteres gardneriana (Nees Castiglioni was assayed in experimental models of pleurisy and microcirculation in situ. Treatment of animals with 500 mg/kg body weight reduced the exudate volume (35% reduction induced by intrapleural injection of carrageenan and the migration of polymorphonuclear cells into the inflamed pleural cavity of rats (40%. Additionally, rolling and adhesion of leukocytes and the number of leukocytes that migrated toward the perivascular space in response to the carrageenan injection were decreased by the extract (500 mg/kg. These data demonstrate the anti-inflammatory effect of the ethanol extract of Helicteres gardneriana and imply that inhibition of leukocyte-endothelial interactions is important in the extract's mechanism of action.

  9. Inhibitory Effects of Arginine on the Aggregation of Bovine Insulin

    OpenAIRE

    Varughese, Michael M.; Jay Newman

    2012-01-01

    Static and dynamic light scattering were used to investigate the effects of L-arginine, commonly used to inhibit protein aggregation, on the initial aggregation kinetics of solutions of bovine insulin in 20% acetic acid and 0.1 M NaCl as a model system for amyloidosis. Measurements were made as a function of insulin concentration (0.5–2.0 mM), quench temperature (60–85°C), and arginine concentration (10–500 mM). Aggregation kinetics under all conditions had a lag phase, whose duration decreas...

  10. Inhibitory effects of ameloblastin on epithelial cell proliferation.

    Science.gov (United States)

    Saito, Noriko; Ariyoshi, Wataru; Okinaga, Toshinori; Kamegawa, Mariko; Matsukizono, Miho; Akebiyama, Yasuo; Kitamura, Chiaki; Nishihara, Tatsuji

    2014-08-01

    Ameloblastin is an enamel matrix protein expressed in several tissues. Many potential mechanisms have been identified by which ameloblastin functions as an extracellular matrix protein. However, the biological effects of ameloblastin on gingival epithelial cells remain unclear. In the present study, we established a novel system to purify recombinant human ameloblastin and clarified its biological functions in epithelial cells in vitro. Recombinant human ameloblastin was isolated from COS-7 cells overexpressing HaloTag-fused human ameloblastin by the HaloTag system and then purified further by reverse-phase high-performance liquid chromatography. SCC-25 cells, derived from human oral squamous cell carcinoma, were treated with recombinant ameloblastin and then cell survival was assessed by a WST-1 assay. Cell cycle analysis was performed by flow cytometry. The novel purification system allowed effective recovery of the recombinant ameloblastin proteins at a high purity. Recombinant ameloblastin protein was found to suppress the proliferation of SCC-25 cells. Flow cytometric analysis showed that ameloblastin treatment induced cell cycle arrest G1 phase. We developed a procedure for production of highly purified recombinant human ameloblastin. Biological analyses suggest that ameloblastin induces cell cycle arrest in epithelial cells and regulates the progression of periodontitis. Copyright © 2014 Elsevier Ltd. All rights reserved.

  11. 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.

  12. 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.

  13. Inhibitory Effects of Arginine on the Aggregation of Bovine Insulin

    Directory of Open Access Journals (Sweden)

    Michael M. Varughese

    2012-01-01

    Full Text Available Static and dynamic light scattering were used to investigate the effects of L-arginine, commonly used to inhibit protein aggregation, on the initial aggregation kinetics of solutions of bovine insulin in 20% acetic acid and 0.1 M NaCl as a model system for amyloidosis. Measurements were made as a function of insulin concentration (0.5–2.0 mM, quench temperature (60–85°C, and arginine concentration (10–500 mM. Aggregation kinetics under all conditions had a lag phase, whose duration decreased with increasing temperature and with increasing insulin concentration but which increased by up to a factor of 8 with increasing added arginine. Further, the initial growth rate after the lag phase also slowed by up to a factor of about 20 in the presence of increasing concentrations of arginine. From the temperature dependence of the lag phase duration, we find that the nucleation activation energy doubles from 17±5 to 36±3 kcal/mol in the presence of 500 mM arginine.

  14. Inhibitory effect of chlorogenic acid on digestion of potato starch.

    Science.gov (United States)

    Karim, Zida; Holmes, Melvin; Orfila, Caroline

    2017-02-15

    The effect of the chlorogenic acid isomer 5-O-caffeoylquinic acid (5-CQA) on digestion of potato starch by porcine pancreatic alpha amylase (PPAA) was investigated using isolated starch and cooked potato tuber as substrates. In vitro digestion was performed on five varieties of potato with varying phenolic content. Co- and pre-incubation of PPAA with 5-CQA significantly reduced PPAA activity in a dose dependent manner with an IC50 value of about 2mgmL(-1). Lineweaver-Burk plots indicated that 5-CQA exerts a mixed type inhibition as km increased and Vmax decreased. The total polyphenol content (TPC) of peeled tuber tissue ranged from 320.59 to 528.94mg 100g(-1)dry weight (DW) in raw tubers and 282.03-543.96mg 100g(-1)DW in cooked tubers. With the exception of Désirée, TPC and 5-CQA levels decreased after cooking. Principle component analysis indicated that digestibility is affected by multiple factors including phenolic, dry matter and starch content. Copyright © 2016 Elsevier Ltd. All rights reserved.

  15. 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.

  16. Inhibitory effect of coumarin derivatives on apple (cv. Idared polyphenol oxidase

    Directory of Open Access Journals (Sweden)

    I. Strelec

    2017-01-01

    Full Text Available Inhibitory effect of 32 coumarin derivatives (20 Schiff bases, 5 thiosemicarbazides, 5 thiazolidinones, and their precursors, 7-hydroxy-4-methylcoumarin and 4-methylcoumarin-7-yl hydrazine carboxylate on partially purified apple polyphenol oxidase was investigated. Thirteen coumarin derivatives inhibited polyphenol oxidase (5 Schiff bases, 5 thiosemicarbazides, 1 thiazolidinone, 4-methyl-7-hydroxycoumarin and 4-methylcoumarin-7-yl hydrazine carboxylate, while 19 derivatives showed no effect on enzyme activity. The most effective inhibitors were thiosemicarbazides, with 4-methyl-1-(2-(4-methyl-2-oxo-2H-chromen-7-yloxyacetyl thiosemicarbazide (compound C23 being the most prominent inhibitor (IC50 = 10.45 µM. The importance of thiosemicarbazide moiety as crucial structure element for strong apple PPO inhibition was confirmed by its cyclisation to thiazolidinone bearing the same substituents as corresponding thiosemicarbazide. Capture of the sulphur atom of thiosemicarbazide group within tiazolidinone ring caused significant loss of inhibitory effect against apple PPO.

  17. Inhibitory effects of phloroglucinol derivatives isolated from Ecklonia stolonifera on Fc(epsilon)RI expression.

    Science.gov (United States)

    Shim, Sun-Yup; Choi, Jae-Sue; Byun, Dae-Seok

    2009-07-01

    Two bioactive phloroglucinol derivatives, dioxinodehydroeckol (DHE) and phlorofucofuroeckol A (PFF-A) were isolated from edible marine brown alga, Ecklonia stolonifera, and evaluated for effects on cell surface Fc(epsilon)RI expression in KU812F cells. DHE and PFF-A were found to reduce the cell surface expression, and total cellular protein and mRNA levels for the Fc(epsilon)RI alpha chain. Moreover, both compounds exerted inhibitory effects against the elevation of intracellular calcium concentration [Ca(2+)](i) and histamine release from anti-Fc(epsilon)RI alpha chain antibody (CRA-1)-stimulated cells. These inhibitory effects were stronger for PFF-A than for DHE. These results show that two phloroglucinol derivatives, DHE and PFF-A, may exert anti-allergic effects via the inhibition of Fc(epsilon)RI expression, calcium influx, and degranulation in basophils, and contributes to the pharmacological activities of marine brown alga, including E. stolonifera.

  18. Inhibitory effect of goat and cow milk fermented with Bifidobacterium longum bb-46 on growth of uropathogenic Candida albicans

    Directory of Open Access Journals (Sweden)

    Vedran Slačanac

    2004-10-01

    Full Text Available The study was carried out to determine the antagonistic influence of goat and cow milk fermented with Bifidobacterium longum Bb-46 on uropathogenic Candida albicans strain. The hypothesis of this study was that fermented goat milk could have possible stronger inhibitory effect on the growth of uropathogenic yeast Candida albicans than fermented cow milk. The correlation between the inhibitory effect and the time of fermentation (number of viable Bifidobacterium longum Bb-46 cells and pH of fermented milk was also determined. The obtained results have shown considerably higher inhibitory effect of fermented goat milk on the growth of Candida albicans compared with fermented cow milk. There was no significant correlation between number of Bifidobacterium longum Bb-46 cells in fermented and the inhibitory effect; as well as between changes in pH during fermentation and inhibitory effect of fermented goat or cow milk.

  19. Adenosine effects on inhibitory synaptic transmission and excitation–inhibition balance in the rat neocortex

    Science.gov (United States)

    Zhang, Pei; Bannon, Nicholas M; Ilin, Vladimir; Volgushev, Maxim; Chistiakova, Marina

    2015-01-01

    Abstract Adenosine might be the most widespread neuromodulator in the brain: as a metabolite of ATP it is present in every neuron and glial cell. However, how adenosine affects operation of neurons and networks in the neocortex is poorly understood, mostly because modulation of inhibitory transmission by adenosine has been so little studied. To clarify adenosine's role at inhibitory synapses, and in excitation–inhibition balance in pyramidal neurons, we recorded pharmacologically isolated inhibitory responses, compound excitatory–inhibitory responses and spontaneous events in layer 2/3 pyramidal neurons in slices from rat visual cortex. We show that adenosine (1–150 μm) suppresses inhibitory transmission to these neurons in a concentration-dependent and reversible manner. The suppression was mediated by presynaptic A1 receptors (A1Rs) because it was blocked by a selective A1 antagonist, DPCPX, and associated with changes of release indices: paired-pulse ratio, inverse coefficient of variation and frequency of miniature events. At some synapses (12 out of 24) we found evidence for A2ARs: their blockade led to a small but significant increase of the magnitude of adenosine-mediated suppression. This effect of A2AR blockade was not observed when A1Rs were blocked, suggesting that A2ARs do not have their own effect on transmission, but can modulate the A1R-mediated suppression. At both excitatory and inhibitory synapses, the magnitude of A1R-mediated suppression and A2AR–A1R interaction expressed high variability, suggesting high heterogeneity of synapses in the sensitivity to adenosine. Adenosine could change the balance between excitation and inhibition at a set of inputs to a neuron bidirectionally, towards excitation or towards inhibition. On average, however, these bidirectional changes cancelled each other, and the overall balance of excitation and inhibition was maintained during application of adenosine. These results suggest that changes of adenosine

  20. 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. PMID:26170872

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

    Directory of Open Access Journals (Sweden)

    Francis Ocheng

    2015-01-01

    Full Text Available 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.

  2. Inhibitory effects of nisin against Clostridium perfringens food poisoning and nonfood-borne isolates.

    Science.gov (United States)

    Udompijitkul, Pathima; Paredes-Sabja, Daniel; Sarker, Mahfuzur R

    2012-01-01

    The enterotoxigenic Clostridium perfringens type A is the causative agent of C. perfringens type A food poisoning (FP) and nonfood-borne (NFB) human gastrointestinal diseases. Due to its ability to form highly resistant endospores, it has become a great concern to the meat industry to produce meat free of C. perfringens. In this study, we evaluated the antimicrobial effect of nisin against C. perfringens FP and NFB isolates. No inhibitory effect of nisin was observed against germination of spores of both FP and NFB isolates in laboratory medium. However, nisin effectively arrested outgrowth of germinated spores of C. perfringens in rich medium. Interestingly, germinated spores of NFB isolates possessed higher resistance to nisin than that of FP isolates. Furthermore, nisin exhibited inhibitory effect against vegetative growth of both FP and NFB isolates in laboratory medium, with vegetative cells of NFB isolates showing higher resistance than that of FP isolates. However, the antimicrobial activity of nisin against C. perfringens was significantly decreased in a meat model system. In conclusion, although nisin showed inhibitory effect against spore outgrowth and vegetative cells of C. perfringens FP and NFB isolates in laboratory conditions, no such effect was observed against C. perfringens spores inoculated into a meat model system. © 2011 Institute of Food Technologists®

  3. Inhibitory effects of cinnamon-water extract on human tumor cell lines

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    Nazila Ariaee-Nasab

    2014-09-01

    Full Text Available Objective: To question the inhibitory effect of cinnamon-water extract (CWE on four human tumor cell lines (AGs, HeLa, MCF-7 and MDA-MB234. Naturally, compounds are an important source for clinical proposes. Cinnamon, a plant-derived spice, is widely used as a food additive and has been attracted many researches in recent years to find its pharmaceutical benefits. Methods: In order to find the answer to this subject, the water extract of cinnamon was prepared and cell proliferation was evaluated using MTT assay. The effect of apoptosis was investigated by DNA fragmentation analysis. Results: The inhibitory effect of CWE on the growth of the cells was significant. DNA fragmentation was found in cultured AGs and MCF-7 cell lines treated by CWE. Conclusions: This study showed the anti-neoplastic activity of CWE on tumor cell lines.

  4. 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.

  5. 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.

  6. The inhibitory effects of sorbate and benzoate against Clostridium perfringens type A isolates.

    Science.gov (United States)

    Alnoman, Maryam; Udompijitkul, Pathima; Paredes-Sabja, Daniel; Sarker, Mahfuzur R

    2015-06-01

    This study evaluated the inhibitory effects of sorbate and benzoate against Clostridium perfringens type A food poisoning (FP) and non-food-borne (NFB) disease isolates. No significant inhibition of germination of spores of both FP and NFB isolates was observed in rich medium (pH 7.0) supplemented with permissive level of sodium sorbate (0.3% ≈ 0.13 mM undissociated sorbic acid) or sodium benzoate (0.1% ≈ 0.01 mM undissociated benzoic acid) used in foods. However, these levels of sorbate and benzoate effectively arrested outgrowth of germinated C. perfringens spores in rich medium. Lowering the pH of the medium increases the inhibitory effects of sorbate and benzoate against germination of spores of NFB isolates, and outgrowth of spores of both FP and NFB isolates. Furthermore, sorbate and benzoate inhibited vegetative growth of C. perfringens isolates. However, the permissible levels of these organic salts could not control the growth of C. perfringens spores in chicken meat stored under extremely abusive conditions. In summary, although sorbate and benzoate showed inhibitory activities against C. perfringens in the rich medium, no such effect was observed in cooked chicken meat. Therefore, caution should be taken when applying these organic salts into meat products to reduce or eliminate C. perfringens spores. Copyright © 2014 Elsevier Ltd. All rights reserved.

  7. Structure-activity relationship of citrus polymethoxylated flavones and their inhibitory effects on Aspergillus niger.

    Science.gov (United States)

    Liu, Li; Xu, Xiaoyun; Cheng, Dan; Yao, Xiaolin; Pan, Siyi

    2012-05-02

    Citrus peels are rich in polymethoxylated flavones (PMFs) and are potential sources of natural preservatives. Six PMFs extracts, isolated and purified from the peels of three mandarins (Citrus reticulata) and three sweet oranges (Citrus sinensis), were identified and quantitated. Their inhibitory effects on Aspergillus niger were evaluated using a microbroth dilution assay. The Red tangerine variety exhibited the greatest antifungal activity (MIC = 0.2 mg/mL), while Jincheng showed the lowest activity (MIC = 1.8 mg/mL). An analysis of principal components was applied to the results in order to elucidate the structure-activity relationships of the citrus PMFs. The structure-activity relationship analysis revealed that, for good inhibitory effect, the 5-OH, 3-OCH₃, and 8-OCH₃ functionalities were essential, while the presence of 3-OH and 3'-OCH₃ greatly reduced inhibition. The findings of this study provide important information for the exploitation and utilization of citrus PMFs as natural biopreservatives.

  8. 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.

  9. [Study the inhibitory effects of three oral actinomyces on growth of oral Candida albicans in vitro].

    Science.gov (United States)

    Li, Duo; Xiao, Xiao-rong; Zhu, Zhu; Ren, Qian; Hu, Tao; Gong, Qi-mei; Zhou, Hong-mei

    2008-10-01

    The aim of this study was to investigate whether the three species of oral Actinomyces have inhibitory effects on the growth of oral Candida albicans in vitro. Straight o'clock method was used to observe the bacteriostasis circle. Reverse o'clock and mixed culture method were used to study the quantitative changes of Candida albicans colony respectively. (1) None of the groups had been viewed the bacteriostasis circle. (2) Compared with control groups, there was a significant decrease of Candida albicans colony on Actinomyces viscosus TPY soft agar (P Actinomyces naeslundii and Actinomyces odontolyticus TPY soft agar were both devoid of obvious Candida albicans colony (P Actinomyces viscosus) and the two latter groups (Actinomyces naeslundii and Actinomyces odontolyticus) showed a striking contrast (P 0.05). Oral Actinomyces viscosus, Actinomyces naeslundii and Actinomyces odontolyticus could inhibit the growth of Candida albicans in vitro. However, which of them contributed more to the inhibitory effects was still not affirmed.

  10. 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.

  11. 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 ...

  12. Inhibitory effect of aqueous extract of Echinacea purpurea and Nerium oleander on HSV-1 multiplication

    OpenAIRE

    Maliheh Farahani

    2014-01-01

    Background: Treatment of HSV-1 infections with the available chemical drugs may have some problems such as drug resistance and virus latency. Therefore, there is a requirement for new antiherpes drugs in today's world. The present study was carried out to analyze the inhibitory effect of Echinacea purpurea and Nerium oleander plants with ethnomedical background on HSV-1 replication. Methods: Plants were extracted by decoction method to obtain aqueous extract. These extracts were screened f...

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

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    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.

  14. Profound climatic effects on two East Asian black-throated tits (Ave: Aegithalidae), revealed by ecological niche models and phylogeographic analysis.

    Science.gov (United States)

    Dai, Chuanyin; Zhao, Na; Wang, Wenjuan; Lin, Congtian; Gao, Bin; Yang, Xiaojun; Zhang, Zhengwang; Lei, Fumin

    2011-01-01

    Although a number of studies have assessed the effects of geological and climatic changes on species distributions in East Asian, we still have limited knowledge of how these changes have impacted avian species in south-western and southern China. Here, we aim to study paleo-climatic effects on an East Asian bird, two subspecies of black-throated tit (A. c. talifuensis-concinnus) with the combined analysis of phylogeography and Ecological Niche Models (ENMs). We sequenced three mitochondrial DNA markers from 32 populations (203 individuals) and used phylogenetic inferences to reconstruct the intra-specific relationships among haplotypes. Population genetic analyses were undertaken to gain insight into the demographic history of these populations. We used ENMs to predict the distribution of target species during three periods; last inter-glacial (LIG), last glacial maximum (LGM) and present. We found three highly supported, monophyletic MtDNA lineages and different historical demography among lineages in A. c. talifuensis-concinnus. These lineages formed a narrowly circumscribed intra-specific contact zone. The estimated times of lineage divergences were about 2.4 Ma and 0.32 Ma respectively. ENMs predictions were similar between present and LGM but substantially reduced during LIG. ENMs reconstructions and molecular dating suggest that Pleistocene climate changes had triggered and shaped the genetic structure of black-throated tit. Interestingly, in contrast to profound impacts of other glacial cycles, ENMs and phylogeographic analysis suggest that LGM had limited effect on these two subspecies. ENMs also suggest that Pleistocene climatic oscillations enabled the formation of the contact zone and thus support the refuge theory.

  15. Profound Climatic Effects on Two East Asian Black-Throated Tits (Ave: Aegithalidae), Revealed by Ecological Niche Models and Phylogeographic Analysis

    Science.gov (United States)

    Wang, Wenjuan; Lin, Congtian; Gao, Bin; Yang, Xiaojun; Zhang, Zhengwang; Lei, Fumin

    2011-01-01

    Although a number of studies have assessed the effects of geological and climatic changes on species distributions in East Asian, we still have limited knowledge of how these changes have impacted avian species in south-western and southern China. Here, we aim to study paleo-climatic effects on an East Asian bird, two subspecies of black-throated tit (A. c. talifuensis–concinnus) with the combined analysis of phylogeography and Ecological Niche Models (ENMs). We sequenced three mitochondrial DNA markers from 32 populations (203 individuals) and used phylogenetic inferences to reconstruct the intra-specific relationships among haplotypes. Population genetic analyses were undertaken to gain insight into the demographic history of these populations. We used ENMs to predict the distribution of target species during three periods; last inter-glacial (LIG), last glacial maximum (LGM) and present. We found three highly supported, monophyletic MtDNA lineages and different historical demography among lineages in A. c. talifuensis–concinnus. These lineages formed a narrowly circumscribed intra-specific contact zone. The estimated times of lineage divergences were about 2.4 Ma and 0.32 Ma respectively. ENMs predictions were similar between present and LGM but substantially reduced during LIG. ENMs reconstructions and molecular dating suggest that Pleistocene climate changes had triggered and shaped the genetic structure of black-throated tit. Interestingly, in contrast to profound impacts of other glacial cycles, ENMs and phylogeographic analysis suggest that LGM had limited effect on these two subspecies. ENMs also suggest that Pleistocene climatic oscillations enabled the formation of the contact zone and thus support the refuge theory. PMID:22195047

  16. 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.

  17. 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.

  18. DNA damage inhibitory effect and phytochemicals of fermented red brown rice extract

    Directory of Open Access Journals (Sweden)

    Ee-Ling Kong

    2015-09-01

    Full Text Available Objective: To determine the polyphenol compounds (phenolic and flavonoid compounds, antioxidant activity [1,1-diphenylpicryl-2-picrylhydrazyl (DPPH radical scavenging activity] and DNA damage inhibitory effect of fermented local red brown rice. Methods: DNA nicking assay was employed to determine the antioxidant activity of the fermented rice extract. Phytochemical screening was completed using standard methods and DPPH radical assays were used to confirm the antioxidant properties of the extracts. Results: After four days of fermentation, fermented red brown rice had more polyphenol compounds compared to unfermented counterpart. Fermented red brown rice showed greater antioxidant properties with EC50 value of DPPH radical scavenging of 43.00 mg extract/mL or 8 mg quercetin equivalent antioxidant activity. In addition, fermented rice extract showed DNA damage inhibitory effect to a certain extent. It protected DNA from reactive oxygen species; however, at high concentration it might induce reductive damage to DNA, whereas, unfermented red brown rice showed weak DNA damage inhibitory effect. Conclusions: Fermented red brown rice could protect DNA from oxidative damage but might induce reductive damage to DNA at high concentrations.

  19. Neurofeedback training effects on inhibitory brain activation in ADHD: A matter of learning?

    Science.gov (United States)

    Baumeister, Sarah; Wolf, Isabella; Holz, Nathalie; Boecker-Schlier, Regina; Adamo, Nicoletta; Holtmann, Martin; Ruf, Matthias; Banaschewski, Tobias; Hohmann, Sarah; Brandeis, Daniel

    2016-09-19

    Neurofeedback training (NF) is a promising non-pharmacological treatment for ADHD that has been associated with improvement of attention-deficit/hyperactivity disorder (ADHD)-related symptoms as well as changes in electrophysiological measures. However, the functional localization of neural changes following NF compared to an active control condition, and of successful learning during training (considered to be the critical mechanism for improvement), remains largely unstudied. Children with ADHD (N=16, mean age: 11.81, SD: 1.47) were randomly assigned to either slow cortical potential (SCP, n=8) based NF or biofeedback control training (electromyogram feedback, n=8) and performed a combined Flanker/NoGo task pre- and post-training. Effects of NF, compared to the active control, and of learning in transfer trials (approximating successful transfer to everyday life) were examined with respect to clinical outcome and functional magnetic resonance imaging (fMRI) changes during inhibitory control. After 20 sessions of training, children in the NF group presented reduced ADHD symptoms and increased activation in areas associated with inhibitory control compared to baseline. Subjects who were successful learners (n=9) also showed increased activation in an extensive inhibitory network irrespective of the type of training. Activation increased in an extensive inhibitory network following NF training, and following successful learning through NF and control biofeedback. Although this study was only powered to detect large effects and clearly requires replication in larger samples, the results suggest a crucial role for learning effects in biofeedback trainings. Copyright © 2016 IBRO. Published by Elsevier Ltd. All rights reserved.

  20. Clotrimazole potentiates the inhibitory effects of ATP on the key glycolytic enzyme 6-phosphofructo-1-kinase.

    Science.gov (United States)

    Marcondes, Mariah Celestino; Sola-Penna, Mauro; Zancan, Patricia

    2010-05-01

    Clotrimazole (CTZ) has been proposed as a potential anti-neoplastic agent, which inhibits glucose metabolism. The present work aimed to evaluate the effects of CTZ on the kinetic mechanism of 6-phosphofructo-1-kinase (PFK). We show that CTZ promotes a dose-dependent inhibition of PFK, presenting a K(i) of 28 +/- 2 microM. Inhibition occurs through the dissociation of the enzyme tetramers, as demonstrated through fluorescence spectroscopy and gel filtration chromatography. Moreover, the affinities of the enzyme for ATP and fructose-6-phosphate are reduced 50% and 30%, respectively. Furthermore, the affinity of PFK for ATP at the inhibitory site becomes 2-fold higher. Altogether, the results presented here suggest that PFK inhibition by CTZ involves a decrease in the affinity of PFK for its substrates at the catalytic site with the concomitant potentiation of the inhibitory properties of ATP. Copyright 2010 Elsevier Inc. All rights reserved.

  1. 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

  2. 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 (MBIC50 - 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 MBIC50 values than their respective glycone forms. The lowest MBIC50 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.

  3. Controlled versus automatic processes: which is dominant to safety? The moderating effect of inhibitory control.

    Science.gov (United States)

    Xu, Yaoshan; Li, Yongjuan; Ding, Weidong; Lu, Fan

    2014-01-01

    This study explores the precursors of employees' safety behaviors based on a dual-process model, which suggests that human behaviors are determined by both controlled and automatic cognitive processes. Employees' responses to a self-reported survey on safety attitudes capture their controlled cognitive process, while the automatic association concerning safety measured by an Implicit Association Test (IAT) reflects employees' automatic cognitive processes about safety. In addition, this study investigates the moderating effects of inhibition on the relationship between self-reported safety attitude and safety behavior, and that between automatic associations towards safety and safety behavior. The results suggest significant main effects of self-reported safety attitude and automatic association on safety behaviors. Further, the interaction between self-reported safety attitude and inhibition and that between automatic association and inhibition each predict unique variances in safety behavior. Specifically, the safety behaviors of employees with lower level of inhibitory control are influenced more by automatic association, whereas those of employees with higher level of inhibitory control are guided more by self-reported safety attitudes. These results suggest that safety behavior is the joint outcome of both controlled and automatic cognitive processes, and the relative importance of these cognitive processes depends on employees' individual differences in inhibitory control. The implications of these findings for theoretical and practical issues are discussed at the end.

  4. Inhibitory effect of allicin on the growth of Babesia and Theileria equi parasites.

    Science.gov (United States)

    Salama, Akram Ahmed; AbouLaila, Mahmoud; Terkawi, Mohamad Alaa; Mousa, Ahmed; El-Sify, Ahmed; Allaam, Mahmoud; Zaghawa, Ahmed; Yokoyama, Naoaki; Igarashi, Ikuo

    2014-01-01

    Allicin is an active ingredient of garlic that has antibacterial, antifungal, antiviral, and antiprotozoal activity. However, the inhibitory effects of allicin on Babesia parasites have not yet been examined. In the present study, allicin was tested as a potent inhibitor against the in vitro growth of bovine and equine Babesia parasites and the in vivo growth of Babesia microti in a mouse model. The in vitro growth of Babesia bovis, Babesia bigemina, Babesia caballi, or Theileria equi was inhibited by allicin in a dose-dependent manner and had IC50 values of 818, 675, 470, and 742 μM, respectively. Moreover, allicin significantly inhibited (P allicin for 5 days significantly (P allicin with diminazene aceturate, growth inhibitory assays were performed in vitro and in vivo. Interestingly, combinations of diminazene aceturate with allicin synergistically potentiated its inhibitory effects in vitro and in vivo. These results indicate that allicin might be beneficial for the treatment of babesiosis, particularly when used in combination with diminazene aceturate.

  5. A good read : A study into the use and effects of multi-sensory storytelling; a storytelling method for persons with profound intellectual and multiple disabilities.

    NARCIS (Netherlands)

    ten Brug, Annet

    2015-01-01

    In order to include persons with profound intellectual and multiple disabilities (PIMD) into our storytelling culture, multi-sensory storytelling (MSST) has been developed. In a multi-sensory book, verbal text is supported by sensory stimuli, the form and content of the book are adjusted to the

  6. A systematic review of the effects of motor interventions to improve motor, cognitive, and/or social functioning in people with severe or profound intellectual disabilities

    NARCIS (Netherlands)

    Houwen, Suzanne; van der Putten, Annette; Vlaskamp, Carla

    While if is generally agreed that motor activity promotes motor, cognitive, and social development, the specific benefits in people with severe or profound intellectual disabilities (S-PID) are as yet unknown. The aim of this study was to systematically review the evidence related to motor

  7. Relabelling Behaviour. The Effects of Psycho-Education on the Perceived Severity and Causes of Challenging Behaviour in People with Profound Intellectual and Multiple Disabilities

    Science.gov (United States)

    Poppes, P.; van der Putten, A.; Post, W.; Frans, N.; ten Brug, A.; van Es, A.; Vlaskamp, C.

    2016-01-01

    Background: Prevalence rates of challenging behaviour are high in children and adults with profound intellectual and multiple disabilities (PIMD). Moreover, many of these behaviours are observed daily. Direct support staff report that most challenging behaviour identified has little impact on the person with PIMD and attribute challenging…

  8. Effects of Inservice Teacher Training on Correct Implementation of Assessment and Instructional Procedures for Teachers of Students with Profound Multiple Disabilities

    Science.gov (United States)

    Horrocks, Erin L.; Morgan, Robert L.

    2011-01-01

    A multicomponent training package (live training, video modeling, role playing, and feedback) was used to train teachers to conduct assessment and to instruct students with profound multiple disabilities. Phase 1 of the study involved training seven teachers to conduct assessment in three areas: (a) preference assessment (i.e., identification of…

  9. In vitro inhibitory effect of cranberry (Vaccinium macrocarpom Ait.) juice on pathogenic microorganisms.

    Science.gov (United States)

    Magariños, H L E; Sahr, C; Selaive, S D C; Costa, M E; Figuerola, F E; Pizarro, O A

    2008-01-01

    The purpose of this study was to determine the inhibitory effects of cranberry juice on pathogenic microorganisms. The microorganisms analyzed were Escherichia coli from patients with urinary infections, Salmonella spp., Listeria monocytogenes, Pseudomonas aeruginosa, and Staphylococcus aureus. The disc method was used to determine the sensitivity of bacteria to cranberry juice (CJ, both concentrated and diluted). A lawn of 10(6) cfu/ml was grown on agar surfaces in Petri dishes and on Whatman discs that had been previously saturated with CJ and CJ : water 1 : 1 to 1 : 50 juice solutions had been placed on the discs, which were cultured and incubated. The results indicated that S. aureus was more susceptible to cranberry juice inhibition than the other microorganisms. L. monocytogenes was the most resistant to the inhibitory action of cranberry juice, showing a significant difference from the inhibition of P. aeruginosa, uropathogenic E. coli, Salmonella spp., and S. aureus. This study also demonstrated that the inhibitory activity of cranberry juice for E. coli took place up to a dilution of 1 : 20.

  10. Inhibitory effect of eupatilin and jaceosidin isolated from Artemisia princeps in IgE-induced hypersensitivity.

    Science.gov (United States)

    Lee, Seung Hoon; Bae, Eun-Ah; Park, Eun-Kyung; Shin, Yong-Wook; Baek, Nam-In; Han, Eun-Joo; Chung, Hae-Gon; Kim, Dong-Hyun

    2007-12-15

    To understand the antiallergic effect of Artemisia princeps (AP), which has been found to show inhibitory activity against degranulation and a passive cutaneous anaphylaxis (PCA) reaction, eupatilin and jaceosidin, as the active components, were isolated by degranulation-inhibitory activity-guided fractionation, with their antiallergic activity investigated. These isolated components potently inhibited the release of beta-hexosaminidase from RBL-2H3 cells induced by the IgE-antigen complex, with IC(50) values of 3.4 and 4.5muM, respectively. Eupatilin and jaceosidin potently inhibited the PCA reaction and scratching behaviors induced by IgE- antigen complex and compound 48/80, respectively. Orally administered jaceosidin more potently inhibited the PCA reaction than that of eupatilin, although the PCA reaction-inhibitory activity of intraperitoneally administered jaceosidin was nearly the same as that of eupatilin. Eupatilin and jaceosidin inhibited the gene expressions of TNF-alpha and IL-4 in RBL-2H3 cells stimulated by IgE-antigen complex. Eupatilin and jaceosidin inhibited the activation of NF-kB. Based on these findings, eupatilin and jaceosidin may be useful for protection from the PCA and itching reactions, which are IgE-mediated representative skin allergic diseases.

  11. Inhibitory effects of sanguinarine against the cyanobacterium Microcystis aeruginosa NIES-843 and possible mechanisms of action

    Energy Technology Data Exchange (ETDEWEB)

    Shao, Jihai [College of Resources and Environment, Hunan Agricultural University, Changsha 410128 (China); Hunan Provincial Key Laboratory of Farmland Pollution Control and Agricultural Resources Use, Hunan Agricultural University, Changsha 410128 (China); Liu, Deming [State Key Laboratory Breeding Base of Crop Germplasm Innovation and Resource Utilization, Hunan Agricultural University, Changsha 410128 (China); Gong, Daoxin; Zeng, Qingru; Yan, Zhiyong [College of Resources and Environment, Hunan Agricultural University, Changsha 410128 (China); Gu, Ji-Dong, E-mail: jdgu@hku.hk [Hunan Provincial Key Laboratory of Farmland Pollution Control and Agricultural Resources Use, Hunan Agricultural University, Changsha 410128 (China); Laboratory of Environmental Microbiology and Toxicology, School of Biological Sciences, The University of Hong Kong, Hong Kong SAR (China)

    2013-10-15

    Highlights: •Sanguinarine was found as a strong algicidal biologically derived substance. •Sanguinarine can induce oxidative stress in the cells of Microcystis aeruginosa. •Photosystem is a target of toxicity of sanguinarine on M. aeruginosa. •Sanguinarine can induce DNA damage and inhibit cell division. -- Abstract: Sanguinarine showed strong inhibitory effect against Microcystis aeruginosa, a typical water bloom-forming and microcystins-producing cyanobacterium. The EC50 of sanguinarine against the growth of M. aeruginosa NIES-843 was 34.54 ± 1.17 μg/L. Results of chlorophyll fluorescence transient analysis indicated that all the electron donating side, accepting side, and the reaction center of the Photosystem II (PS II) were the targets of sanguinarine against M. aeruginosa NIES-843. The elevation of reactive oxygen species (ROS) level in the cells of M. aeruginosa NIES-843 upon exposure indicated that sanguinarine induced oxidative stress in the active growing cells of M. aeruginosa NIES-843. Further results of gene expression analysis indicated that DNA damage and cell division inhibition were also involved in the inhibitory action mechanism of sanguinarine against M. aeruginosa NIES-843. The inhibitory characteristics of sanguinarine against M. aeruginosa suggest that the ecological- and public health-risks need to be evaluated before its application in cyanobacterial bloom control to avoid devastating events irreversibly.

  12. 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.

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

    Science.gov (United States)

    Ponnusamy, Sudha; Ravindran, Remya; Zinjarde, Smita; Bhargava, Shobha; Ravi Kumar, Ameeta

    2011-01-01

    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. PMID:20953430

  14. Inhibitory effects of Korean medicinal plants and camelliatannin H from Camellia japonica on human immunodeficiency virus type 1 protease.

    Science.gov (United States)

    Park, Jong Cheol; Hur, Jong Moon; Park, Ju Gwon; Hatano, Tsutomu; Yoshida, Takashi; Miyashiro, Hirotsugu; Min, Byung Sun; Hattori, Masao

    2002-08-01

    To identify substances with anti-human immunodeficiency virus (HIV) activity in traditional medicines, 101 extracts of Korean medicinal plants were screened for their inhibitory effects on HIV type 1 protease (PR). The enzyme activity was determined by HPLC. Of the extracts tested, strong inhibitory effects were observed in the acetone extracts of the pericarp and leaves of Camellia japonica, the water extract of the leaves of Sageretia theezans and the methanol extract of the aerial part of Sophora flavescens. Camelliatannin H from the pericarp of C. japonica, showed a potent inhibitory activity on HIV-1 PR with IC(50) of 0.9 microM. Copyright 2002 John Wiley & Sons, Ltd.

  15. Inhibitory Effect of Apigenin on Losartan Metabolism and CYP2C9 Activity in vitro.

    Science.gov (United States)

    Wang, Zhe; Gong, Yun; Zeng, Da-Li; Chen, Lian-Guo; Lin, Gao-Tong; Huang, Cheng-Ke; Sun, Wei; Chen, Meng-Chun; Hu, Guo-Xin; Chen, Rui-Jie

    2016-01-01

    CYP2C9 is one of the most important phase I drug-metabolizing enzymes in liver. The objective of this work was to investigate the effects of apigenin on the metabolism of losartan and human CYP2C9 and rat CYP2C11 activity in vitro. Different concentrations of apigenin were added to a 100 mmol/l Tris-HCl reaction mixture containing 2 pmol/ml recombinant human CYP2C9.1, 0.25 mg/ml human liver microsomes or 0.5 mg/ml rat liver microsomes to determine the half maximal inhibition or a half-maximal inhibitory concentration (IC50) on the metabolism of losartan. In addition, diclofenac used as CYP2C9 substrate was performed to determine the effects of apigenin on CYP2C9. The results showed that apigenin has the inhibitory effect on the metabolism of losartan in vitro, the IC50 was 7.61, 4.10 and 11.07 μmol/l on recombinant CYP2C9 microsomes, human liver microsomes and rat liver microsomes, respectively. Meanwhile, apigenin's mode of action on human CYP2C9 activity was competitive for the substrate diclofenac. In contrast to its potent inhibition of CYP2C9 in humans (9.51 μmol/l), apigenin had lesser effects on CYP2C11 in rat (IC50 = 15.51 μmol/l). The observations imply that apigenin has the inhibitory effect on the metabolism of losartan and CYP2C9 activity in vitro. More attention should be paid as to when losartan should be administrated combined with apigenin. © 2016 S. Karger AG, Basel.

  16. Effect of xenon on excitatory and inhibitory transmission in rat spinal ventral horn neurons.

    Science.gov (United States)

    Yamamoto, Tomohiro; Honda, Hiroyuki; Baba, Hiroshi; Kohno, Tatsuro

    2012-05-01

    The minimum alveolar concentration is determined in the spinal cord rather than in the brain. Xenon inhibits glutamatergic excitatory synaptic transmission in the dorsal horn neurons. However, its actions in the ventral horn neurons have not been investigated. The effects of 50 or 75% xenon on excitatory and inhibitory synaptic transmission were examined in the spinal lamina IX neurons of neonatal rats by using a whole cell patch clamp technique. Fifty percent xenon inhibited the α-amino-3-hydroxy-5-methyl-4-isoxazole-4-propionic acid-induced currents (amplitudes = 72 ± 9% and integrated area = 73 ± 13% of the control values), and α-amino-3-hydroxy-5-methyl-4-isoxazole-4-propionic acid receptor-mediated electrically evoked excitatory postsynaptic currents (amplitudes = 69 ± 13% of the control values). Seventy-five percent xenon similarly inhibited α-amino-3-hydroxy-5-methyl-4-isoxazole-4-propionic acid-induced currents. However, xenon had no effect on the N-methyl-D-aspartate-induced currents or N-methyl-D-aspartate receptor-mediated electrically evoked excitatory postsynaptic currents. Xenon decreased the amplitude, but not the frequency, of miniature excitatory postsynaptic currents. There were no discernible effects on the currents induced by γ-aminobutyric acid or glycine or on miniature inhibitory postsynaptic currents. Xenon inhibits α-amino-3-hydroxy-5-methyl-4-isoxazole-4-propionic acid receptor-mediated glutamatergic excitatory transmission in the spinal lamina IX neurons via a postsynaptic mechanism. In contrast, there are no substantial effects on N-methyl-D-aspartate receptor-mediated or inhibitory synaptic transmission. The suppressive effects on excitatory synaptic transmission in the ventral horn neurons partly account for the mechanism behind xenon's ability to produce immobility in response to noxious stimuli and to determine the minimum alveolar concentration.

  17. Inhibitory effect of Rosa damascena Mill flower essential oil, geraniol and citronellol on rat ileum contraction.

    Science.gov (United States)

    Sadraei, H; Asghari, G; Emami, S

    2013-01-01

    Flower of Rosa damascena Mill is widely used in Iran for gastrointestinal (GI) disorders. However, its pharmacological action on ileum contraction has not been studied. In this research we have investigated ileum motility effect of essential oil of flower petals of R. damascena growing in Kashan, Iran, and two of its constituents. The essential oils obtained by hydrodistillation were investigated by a combination of GC and GC/MS. More than 34 compounds have been identified. The main constituents of the essential oil were β-citronellol (23%), nonadecane (16%), geraniol (16%) and heneicosane (5%). A portion of rat isolated ileum was suspended under 1g tension in Tyrode's solution at 37°C and gassed with O2. Effect of the R. damascena essential oil (2.5-160 μg/ml), geraniol (0.2-3.2 μg/ml) and citronellol (0.8-6.4 μg/ml) were studied on ileum contractions induced by KCl, acetylcholine (ACh) and electrical field stimulation (EFS) and compared with standard drugs atropine and loperamide. The contractile response of EFS was mediated mainly through the intramural nerve plexuses, because its response was inhibited by loperamide and partially reduced by atropine. The essential oil concentration dependently inhibited the response to KCl (IC50=67 ± 8.4μg/ml) and EFS (IC50=47 ± 10.6 μg/ml). Geraniol (IC50=1.7 ± 0.15 μg/ml for KCl) and citronellol (IC50=2.9 ± 0.3 μg/ml for KCl) also had inhibitory effect of ileum contraction and both were more potent than the essential oil. It was concluded that R. damascena essential oil mainly had an inhibitory effect on ileum contractions and geraniol and citronellol had a major role in inhibitory effect of the essential.

  18. 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,

  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. The effects of PDE5 inhibitory drugs on renal ischemia/reperfusion injury in rats.

    Science.gov (United States)

    Küçük, A; Yucel, M; Erkasap, N; Tosun, M; Koken, T; Ozkurt, M; Erkasap, S

    2012-10-01

    The aim of the present study was to evaluate the effects of phosphodiesterase type 5 (PDE5) inhibitory drugs, Tadalafil and Sildenafil, on inducible NOS (iNOS), endothelial NOS (eNOS) and p53 genes expressions and apoptosis in ischemia/reperfusion (I/R) induced oxidative injury in rat renal tissue. Eighty Sprague-Dawley rats (300-350 g) were divided into four groups. In ischemia/reperfusion group, rats were subjected to renal ischemia by clamping the left pedicle for 60 min, and then reperfused for 90 min. On the other hand, in other two groups the rats were individually pretreated with Tadalafil and Sildenafil 1 h before the induction of ischemia. Malondialdehyde (MDA) is determined in renal tissue homogenates by high-performance liquid chromatography, the number of apoptotic cell were calculated by TUNEL method and p53 and eNOS expression were detected with immunohistochemistry. On the other hand, myeloperoxidase (MPO) levels were measured by spectrophotometric method and the mRNA level of iNOS in renal tissue was determined by Real-time PCR (RT-PCR). Our results indicate that MDA and MPO levels were increased in the I/R group than those in the control group. Both Tadalafil and Sildenafil treatment decreased the MDA levels in ischemia/reperfusion group, whereas this effect was more potent with Sildenafil. RT-PCR results showed that, iNOS gen expression increased in the I/R group, but decreased in the PDE5 inhibitory drugs treated group. Apoptotic cells, eNOS levels and p53 positive cells were also decreased in PDE5 inhibitory drugs treated group. We suggest that Tadalafil and Sildenafil have beneficial effects against I/R related renal tissue injury and this protective effect is clearer for Sildenafil than Tadalafil.

  1. When Lightning Strikes Twice: Profoundly Gifted, Profoundly Accomplished.

    Science.gov (United States)

    Makel, Matthew C; Kell, Harrison J; Lubinski, David; Putallaz, Martha; Benbow, Camilla P

    2016-07-01

    The educational, occupational, and creative accomplishments of the profoundly gifted participants (IQs ⩾ 160) in the Study of Mathematically Precocious Youth (SMPY) are astounding, but are they representative of equally able 12-year-olds? Duke University's Talent Identification Program (TIP) identified 259 young adolescents who were equally gifted. By age 40, their life accomplishments also were extraordinary: Thirty-seven percent had earned doctorates, 7.5% had achieved academic tenure (4.3% at research-intensive universities), and 9% held patents; many were high-level leaders in major organizations. As was the case for the SMPY sample before them, differential ability strengths predicted their contrasting and eventual developmental trajectories-even though essentially all participants possessed both mathematical and verbal reasoning abilities far superior to those of typical Ph.D. recipients. Individuals, even profoundly gifted ones, primarily do what they are best at. Differences in ability patterns, like differences in interests, guide development along different paths, but ability level, coupled with commitment, determines whether and the extent to which noteworthy accomplishments are reached if opportunity presents itself. © The Author(s) 2016.

  2. Selective and potent inhibitory effect of docosahexaenoic acid (DHA) on U46619-induced contraction in rat aorta

    Science.gov (United States)

    Sato, Kyosuke; Chino, Daisuke; Kobayashi, Tomoya; Obara, Keisuke; Miyauchi, Seiji; Tanaka, Yoshio

    2013-01-01

    Inhibitory effects of docosahexaenoic acid (DHA) on blood vessel contractions induced by various constrictor stimulants were investigated in the rat thoracic aorta. The inhibitory effects of DHA were also compared with those of eicosapentaenoic acid (EPA) and linoleic acid (LA). DHA exhibited a strong inhibitory effect on the sustained contractions induced by U46619, a TXA2 mimetic. This inhibitory effect of DHA was not affected by removal of the endothelium or by treatment with either indomethacin or Nω-nitro-l-arginine. DHA also significantly diminished PGF2α-induced contraction but did not show any appreciable inhibitory effects on the contractions to both phenylephrine (PE) and high-KCl. Similarly, EPA exhibited significant inhibitory effects against the contractions induced by both U46619 and PGF2α without substantially affecting either PE- or high-KCl-induced contractions. However, both DHA and EPA generated more potent inhibitions against contractions induced by U46619 than those by PGF2α. In contrast, LA did not show significant inhibitory effects against any contractions, including those induced by U46619. The present findings suggest that DHA and EPA elicit more selective inhibition against blood vessel contractions that are mediated through stimulation of prostanoid receptors than those through α-adrenoceptor stimulation or membrane depolarization. Although DHA and EPA have similar inhibitory potencies against prostanoid receptor-mediated contractions, they had a more potent inhibition against TXA2 receptor (TP receptor)-mediated contractions than against PGF2α receptor (FP receptor)-mediated responses. Selective inhibition by either DHA or EPA of prostanoid receptor-mediated blood vessel contractions may partly underlie the mechanisms by which these ω-3 polyunsaturated fatty acids exert their circulatory-protective effects. PMID:24304639

  3. 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

  4. 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.

  5. Mechanism of growth inhibitory effect of cape aloe extract in ehrlich ascites tumor cells.

    Science.gov (United States)

    Kametani, Saeda; Oikawa, Tomoko; Kojima-Yuasa, Akiko; Kennedy, David Opare; Norikura, Toshio; Honzawa, Mayumi; Matsui-Yuasa, Isao

    2007-12-01

    Cape aloe (Aloe ferox Miller) has been a herb well known for its cathartic properties and has also been used popularly as a health drink (juice, tea and tonic) in the United States and in Europe. Cape aloe extract also has been reported to possess several pharmacological effects, such as anti-inflammatory, anti-bacterial, anti-fungal and protective effect against liver injury. However, the investigations on an anti-tumor activity in cape aloe extract are very few and subsequent mechanisms have not been well elucidated. In this study, we examined the effect of the selective growth inhibitory activity of cape aloe extract and found that the cape aloe extract, especially the dichloromethane (CH(2)Cl(2)) extract, caused a dose-dependent growth inhibitory effect in Ehrlich ascites tumor cells (EATC), but not in mouse embryo fibroblast (NIH3T3) cells, which was used as a normal cell model. Furthermore, the CH(2)Cl(2) extract caused an accumulation of cells in the G1 phase and a decrease of cells in the S and G2/M phase of the cell cycle and inhibited DNA synthesis in a dose-dependent manner. In addition, other results suggest that cell cycle arrest and inhibition of proliferation in EATC by the CH(2)Cl(2 )extract are associated with decreased retinoblastoma protein (Rb) phosphorylation.

  6. The Inhibitory Effect of Haloxylon salicornicum on Contraction of the Mouse Uterus

    Directory of Open Access Journals (Sweden)

    Nabila H. Saleem

    2013-01-01

    Full Text Available Haloxylon salicornicum (H. salicornicum is a plant that is frequently taken as a tea by Bedouin women in Egypt who are experiencing difficulties during pregnancy, as well as to provide relief from dysmenorrhoea. Despite its medical use, there has been no detailed evaluation of the effect of this plant on uterine tissue. Therefore, the initial aim of this study was to determine whether H. salicornicum affected the contraction of the mouse uterus in vitro. The crude aqueous extract of H. salicornicum was found to inhibit the spontaneous contractions of the uterus, with the effect being rapid in onset and completely reversible upon washout. Subsequent purification of the plant extract resulted in the identification of synephrine and N-methyltyramine, both of which were found to have inhibitory effects on the spontaneous contractions of the uterus. The EC50 for the purified constituent identified as synephrine was 0.82 ± 0.24 μg/mL. The inhibitory activity of crude H. salicornicum, as well as the isolated constituents, could be prevented by pretreatment of the uterus with the β-adrenoceptor antagonist propranolol. In conclusion, the use of H. salicornicum during preterm labour appears to be justified, and its pharmacologic effect is consistent with it acting as a β-adrenoceptor agonist.

  7. The Inhibitory Effect of Haloxylon salicornicum on Contraction of the Mouse Uterus

    Science.gov (United States)

    Saleem, Nabila H.; Ferro, Valerie A.; Simpson, Ann M.; Gray, Alexander I.; Drummond, Robert M.

    2013-01-01

    Haloxylon salicornicum (H. salicornicum) is a plant that is frequently taken as a tea by Bedouin women in Egypt who are experiencing difficulties during pregnancy, as well as to provide relief from dysmenorrhoea. Despite its medical use, there has been no detailed evaluation of the effect of this plant on uterine tissue. Therefore, the initial aim of this study was to determine whether H. salicornicum affected the contraction of the mouse uterus in vitro. The crude aqueous extract of H. salicornicum was found to inhibit the spontaneous contractions of the uterus, with the effect being rapid in onset and completely reversible upon washout. Subsequent purification of the plant extract resulted in the identification of synephrine and N-methyltyramine, both of which were found to have inhibitory effects on the spontaneous contractions of the uterus. The EC50 for the purified constituent identified as synephrine was 0.82 ± 0.24 μg/mL. The inhibitory activity of crude H. salicornicum, as well as the isolated constituents, could be prevented by pretreatment of the uterus with the β-adrenoceptor antagonist propranolol. In conclusion, the use of H. salicornicum during preterm labour appears to be justified, and its pharmacologic effect is consistent with it acting as a β-adrenoceptor agonist. PMID:24174981

  8. Triterpenoids from Calophyllum inophyllum and their growth inhibitory effects on human leukemia HL-60 cells.

    Science.gov (United States)

    Li, Yan-Zhi; Li, Zhan-Lin; Yin, Shi-Liang; Shi, Guang; Liu, Ming-Sheng; Jing, Yong-Kui; Hua, Hui-Ming

    2010-09-01

    A new friedelane-type triterpene (1), along with seven known triterpenoids, was isolated from the stems and leaves of Calophyllum inophyllum Linn. Their structures were established as 3beta, 23-epoxy-friedelan-28-oic acid (1), friedelin (2), epifriedelanol (3), canophyllal (4), canophyllol (5), canophyllic acid (6), 3-oxo-friedelan-28-oic acid (7), and oleanolic acid (8) by spectroscopic methods (NMR, EI-MS). The growth inhibitory effects of these triterpenoids on human leukemia HL-60 cells were determined. Crown Copyright (c) 2010. Published by Elsevier B.V. All rights reserved.

  9. 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.

  10. Inhibitory effect of melatonin on testosterone synthesis is mediated via GATA-4/SF-1 transcription factors.

    Science.gov (United States)

    Qin, Fenju; Zhang, Jie; Zan, Linsen; Guo, Weiqiang; Wang, Jin; Chen, Lili; Cao, Yi; Shen, Ouxi; Tong, Jian

    2015-11-01

    The aim of the present study was to elucidate whether the GATA-4/SF-1 signalling pathway is involved in the inhibitory effects of melatonin on testosterone production in both the TM3 Leydig cell line and in C57BL/6J mice. In-vitro experiments demonstrated that melatonin treatment significantly reduced testosterone levels in cell culture medium (P testosterone production (P testosterone production are mediated via down-regulation of GATA-4 and SF-1 expression. Copyright © 2015 Reproductive Healthcare Ltd. Published by Elsevier Ltd. All rights reserved.

  11. 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.

  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. 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.

  14. Inhibitory effects of different fractions of Nepeta satureioides on melanin synthesis through reducing oxidative stress.

    Science.gov (United States)

    Emami, Seyed Ahmad; Yazdian-Robati, Rezvan; Sadeghi, Mohammad; Baharara, Javad; Amini, Elaheh; Salek, Farzaneh; Tayarani-Najaran, Zahra

    2017-04-01

    Nepeta satureioides Boiss. has been used in traditional medicine of eastern countries and is famous for its medicinal properties. The aim of this study was to evaluate the effect of methanol (MeOH), n-hexane and dichloromethane (CH2Cl2) fractions of the extract on melanin synthesis and oxidative stress in B16F10 melanoma cell line. The B16F10 cell line viability after treatment with increasing concentrations of different fractions of the plant (5-60 μg/mL) was measured using MTT assay. The inhibitory effect on synthesis of melanin, mushroom tyrosinase activity, cellular tyrosinase and oxidative stress were determined by the colorimetric and fluorometric methods. The data showed that at concentrations below 60 μg/mL, fractions did not show significant toxicity on melanoma cells. The amount of melanin synthesis by MeOH and CH2Cl2 fractions and mushroom tyrosinase activity by the MeOH fraction declined in B16F10 cells. In addition to the capacity of MeOH, n-hexane and CH2Cl2 fractions in decreasing the amount of reactive oxygen species (ROS) in melanoma cells, all fractions revealed remarkable antioxidant activity. The melanogenesis inhibitory and antioxidant effects of N. satureioides on B16F10 cells may suggest this plant as a new pharmaceutical agent in reducing skin pigment and skin aging in cosmetic industry.

  15. 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.

  16. 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)

  17. Inhibitory effects of kale ingestion on metabolism by cytochrome P450 enzymes in rats.

    Science.gov (United States)

    Yamasaki, Izumi; Yamada, Masayoshi; Uotsu, Nobuo; Teramoto, Sachiyuki; Takayanagi, Risa; Yamada, Yasuhiko

    2012-01-01

    Kale (Brassica oleracea L. var acephala DC) is a leafy green vegetable belonging to the cabbage family (Brassicaceae) that contains a large amount of health-promoting phytochemicals. There are any reports about the effects of kale ingestion on the chemoprevention function and mechanism, but the interactions between kale and drugs have not been researched. We investigated the effects of kale intake on cytochrome P450 (CYP) metabolism by using cocktail probe drugs, including midazolam (for CYP3A4), caffeine (for CYP1A2), dextromethorphan (for CYP2D6), tolbutamide (for CYP2C9), omeprazole (for CYP2C19), and chlorzoxazone (for CYP2E1). Cocktail drugs were administered into rats treated with kale and cabbage (2000 mg/kg) for a week. The results showed that kale intake induced a significant increase in plasma levels and the AUC of midazolam, caffeine, and dextromethorphan. In addition, the plasma concentration and AUC of omeprazole tended to increase. Additionally, no almost differences in the mRNA expression levels of CYP enzymes in the liver were observed. In conclusion, kale ingestion was considered to have an inhibitory effect on the activities of CYP3A4, 1A2, 2D6, and 2C19 for a reason competitive inhibition than inhibitory changes in the mRNA expressions.

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

    Science.gov (United States)

    Remirez, D; Ledón, N; González, R

    2002-01-01

    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 300mg/kg post-orally (p.o.)) was administered 1 h before the challenge with 1 microg 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, phycocyanin 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. PMID:12061428

  19. Inhibitory Effects of Spices on Biogenic Amine Accumulation during Fish Sauce Fermentation.

    Science.gov (United States)

    Zhou, Xuxia; Qiu, Mengting; Zhao, Dandan; Lu, Fei; Ding, Yuting

    2016-04-01

    The presence of high levels of biogenic amines is detrimental to the quality and safety of fish sauce. This study investigated the effects of ethanol extracts of spices, including garlic, ginger, cinnamon, and star anise extracts, in reducing the accumulation of biogenic amines during fish sauce fermentation. The concentrations of biogenic amines, which include histamine, putrescine, tyramine, and spermidine, all increased during fish sauce fermentation. When compared with the samples without spices, the garlic and star anise extracts significantly reduced these increases. The greatest inhibitory effect was observed for the garlic ethanolic extracts. When compared with controls, the histamine, putrescine, tyramine, and spermidine contents and the overall biogenic amine levels of the garlic extract-treated samples were reduced by 30.49%, 17.65%, 26.03%, 37.20%, and 27.17%, respectively. The garlic, cinnamon, and star anise extracts showed significant inhibitory effects on aerobic bacteria counts. Furthermore, the garlic and star anise extracts showed antimicrobial activity against amine producers. These findings may be helpful for enhancing the safety of fish sauce. © 2016 Institute of Food Technologists®

  20. [The inhibitory effects of Realgar bioleaching solution on S180 ascites-tumor and its toxicity].

    Science.gov (United States)

    Xie, Qin-Jian; Zhang, Xu; Wang, Xin; Bai, Lu; Li, Hong-Yu

    2009-06-01

    To investigate the inhibitory effect of Realgar bioleaching solution (RBS) on tumor S180 cells line and estimate its toxicity, to provide experimental evidence for the further exploit of Realgar. 24 hours after the models of ascites-tumor bearing mice were established, the mice were injected RBS once a day. The survival rates of S180 ascites-tumor bearing mice injected in RBS was studied, and the RBS acute toxicity of mice produced by oral, intraperitoneal or intravenous was evaluated by Drug Median Lethal Dose (LD50). The inhibitory effect of S180 cells in vivo had a dose-dependent manner. The survival rates of mice were 10% - 60% in the different dose in 15 days. The LD50 values of RBS by oral, intraperitoneal or intravenous were 5.27 mg/kg, 3.63 mg/kg and 2.68 mg/kg, respectively. RBS has potent antitumor effect, LD50 value of RBS is lower than that of traditional medicine.

  1. 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.

  2. 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.

  3. Taurin-conjugated ursodeoxycholic acid has a reversible inhibitory effect on human keratinocyte growth.

    Science.gov (United States)

    Yamaguchi, Y; Itami, S; Nishida, K; Ando, Y; Okamoto, S; Hosokawa, K; Yoshikawa, K

    1998-09-01

    Tauroursodeoxycholic acid (TUDC) is one of the most hydrophilic taurin conjugated bile acids. TUDC has a suppressive effect on DNA synthesis in primary cultured rat hepatocytes. In this study, we investigated the growth inhibitory effect of TUDC on cultured human keratinocytes. TUDC suppressed the proliferation of keratinocytes in a dose dependent fashion, as measured by both cell counts and 5-bromo-2'-deoxyuridine (BrdU) uptake. Keratinocytes reproliferated and reached almost the same cell number as control after removal of TUDC from the medium. TUDC (1 mM) had no effect on the cell viability, as measured by the dye exclusion test. Epidermal sheets stratified in the presence of TUDC appeared thinner than those stratified without TUDC. These results suggest that TUDC has a reversible growth suppressive effect on human keratinocytes through the mechanism other than cytotoxicity and would be applicable for the treatment of hyperproliferative skin disorders such as psoriasis.

  4. 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.

  5. 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

    2017-05-06

    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.

  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 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.

  8. The effect of electromagnetic field emitted by a mobile phone on the inhibitory control of saccades.

    Science.gov (United States)

    Okano, Tomoko; Terao, Yasuo; Furubayashi, Toshiaki; Yugeta, Akihiro; Hanajima, Ritsuko; Ugawa, Yoshikazu

    2010-04-01

    To investigate whether exposure to a pulsed high-frequency electromagnetic field (pulsed EMF) emitted by a mobile phone has short-term effects on the inhibitory control of saccades. A double-blind, counterbalanced crossover study design was employed. We assessed the performance of 10 normal subjects on antisaccade (AS) and cued saccade (CUED) tasks as well as two types of overlap saccade (OL1, OL2) task before and after 30 min of exposure to EMF emitted by a mobile phone or sham exposure. After EMF or sham exposure, we observed a slight but significant shortening of latency in the CUED and OL2 tasks. AS amplitude decreased as well as the saccade velocities in the AS, CUED, and OL1 tasks after exposure. These changes occurred regardless of whether exposure was real or sham. The frequencies of pro-saccades in the AS task, saccades to cue in the CUED task, and prematurely initiated saccades in the overlap (OL2) task did not change significantly after real or sham EMF exposure. Thirty minutes of mobile phone exposure has no significant short-term effect on the inhibitory control of saccades. The cortical processing responsible for saccade inhibition is not affected by exposure to EMF emitted by a mobile phone. 2009 International Federation of Clinical Neurophysiology. Published by Elsevier Ireland Ltd. All rights reserved.

  9. Effects of inhibitory compounds in lignocellulosic hydrolysates on Mortierella isabellina growth and carbon utilization.

    Science.gov (United States)

    Ruan, Zhenhua; Hollinshead, Whitney; Isaguirre, Christine; Tang, Yinjie J; Liao, Wei; Liu, Yan

    2015-05-01

    Oleaginous fungus Mortierella isabellina showed excellent lipid conversion on non-detoxified lignocellulosic hydrolysate. This study investigated the effects of inhibitory compounds (furfural, hydroxymethylfurfural, and ferulic and coumaric acids) in lignocellulosic hydrolysate on M. isabellina growth and lipid production. M. isabellina can tolerate furfural (∼1 g/L), hydroxymethylfurfural (∼2.5 g/L), ferulic (∼0.5 g/L) and coumaric acid (∼0.5 g/L) with normal growth rates. Synergistic effect of these inhibitors (2 g/L furfural, 0.4 g/L hydroxymethylfurfural, 0.02 g/L ferulic acid and 0.02 g/L coumaric acid) moderately reduces total fungal growth (by 28%), while the presence of these inhibitors has minor impact on cell lipid contents and lipid profiles. In the presence of inhibitory compounds, (13)C-tracing has revealed that M. isabellina can simultaneously utilize glucose and acetate, and acetate is mainly assimilated for synthesis of lipid and TCA cycle amino acids. The results also demonstrate that glucose has strong catabolite repression for xylose utilization for biomass and lipid production in the presence of inhibitors. Copyright © 2015 Elsevier Ltd. All rights reserved.

  10. Interaction between Various Apple Procyanidin and Staphylococcal Enterotoxin A and Their Inhibitory Effects on Toxin Activity

    Science.gov (United States)

    Shimamura, Yuko; Hirai, Chikako; Sugiyama, Yuka; Utsumi, Mio; Yanagida, Akio; Murata, Masatsune; Ohashi, Norio; Masuda, Shuichi

    2017-01-01

    In this study, we investigated the interaction between apple polyphenols (AP; mainly consisting of procyanidin (PC) from an apple) and staphylococcal enterotoxin A (SEA), and the inhibitory effects of AP on SEA activity. According to the degree of polymerization, in particularly highly polymerized PC (more than pentamer) strongly interacted with SEA. The binding affinity of AP with SEA molecules was determined using Biacore analysis. AP reacted with SEA immobilized on a Biacore sensor chip. After treatment with pepsin and pancreatin, to examine the changes of binding affinity of AP in intragastric conditions, AP maintained interaction with SEA. We examined whether AP inhibits the proliferation and interferon-γ (IFN-γ) production induced by SEA in mouse spleen cells. AP strongly inactivated the proliferation and IFN-γ production induced by SEA. These results suggest that AP, which has a higher degree of polymerization, inactivates stronger biological activity of SEA through interaction with SEA. Our studies are the first to demonstrate the relationship between the degree of polymerization of AP and the inhibitory effects on SEA activities. PMID:28783092

  11. 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.

  12. Effects of oxotremorine and physostigmine on the inhibitory avoidance impairment produced by amitriptyline in male and female mice.

    Science.gov (United States)

    Monleón, Santiago; Urquiza, Adoración; Vinader-Caerols, Concepción; Parra, Andrés

    2009-12-28

    We have previously observed that amitriptyline and other antidepressants produce impairing effects on inhibitory avoidance (also called passive avoidance) in mice of both sexes. In the present study we investigated the involvement of the cholinergic system in the inhibitory avoidance impairment produced by acute amitriptyline in male and female CD1 mice. For this purpose, the effects on said task of acute i.p. administration of several doses of amitriptyline, either alone or in combination with the cholinergic agonists oxotremorine and physostigmine, were evaluated. Pre-training administration of 5, 7.5, 10 or 15 mg/kg of amitriptyline produced a significant impairment of inhibitory avoidance in both males and females. When oxotremorine (0.05 or 0.1 mg/kg) was co-administered with amitriptyline, the antidepressant's impairing effect was partially counteracted, although inhibitory avoidance learning was not significant. Physostigmine (0.15, 0.3 or 0.6 mg/kg) counteracted the impairment produced by amitriptyline, as mice treated with both drugs exhibited inhibitory avoidance learning. These results show that the inhibitory avoidance impairment produced by amitriptyline in male and female mice is mediated, at least partially, by the cholinergic system.

  13. 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

  14. Acute effects of alcohol on inhibitory control and simulated driving in DUI offenders.

    Science.gov (United States)

    Van Dyke, Nicholas; Fillmore, Mark T

    2014-06-01

    The public health costs associated with alcohol-related traffic accidents have prompted considerable research aimed at identifying characteristics of individuals who drive under the influence (DUI) in order to improve treatment and prevention strategies. Survey studies consistently show that DUI offenders self-report higher levels of impulsivity compared to their nonoffending counterparts. However, little is known about how individuals with a DUI history respond under alcohol. Inhibitory control is a behavioral component of impulsivity thought to underlie risky drinking and driving behaviors. The present study examined the degree to which DUI drivers display deficits of inhibitory control in response to alcohol and the degree to which alcohol impaired their simulated driving performance. It was hypothesized that DUI offenders would display an increased sensitivity to the acute impairing effects of alcohol on simulated driving performance. Young adult drivers with a history of DUI and a demographically-comparable group of drivers with no history of DUI (controls) were tested following a 0.65 g/kg dose of alcohol and a placebo. Inhibitory control was measured by using a cued go/no-go task. Drivers then completed a driving simulation task that yielded multiple indicators of driving performance, such as within-lane deviation, steering rate, centerline crossings and road edge excursions, and drive speed. Results showed that although DUI offenders self-reported greater levels of impulsivity than did controls, no group differences were observed in the degree to which alcohol impaired inhibitory control and driving performance. The findings point to the need to identify other aspects of behavioral dysfunction underlying the self-reported impulsivity among DUI offenders, and to better understand the specific driving situations that might pose greater risk to DUI offenders. The systematic study of candidate cognitive deficits in DUI offenders will provide important

  15. Inhibitory effect of calcium channel blockers on proliferation of human glioma cells in vitro

    Energy Technology Data Exchange (ETDEWEB)

    Kunert-Radek, J.; Stepien, H.; Lyson, K.; Pawlikowski, M.; Radek, A.

    1989-01-01

    The effects of 2 specific calcium channel blockers, verapamil and nimodipine, on the proliferation of human glioma tumour cells were investigated in vitro. Tumour tissues for primary cell cultures were obtained bioptically from 3 patients with the histopathological diagnosis of glioblastoma. The (/sup 3/H)-thymidine incorporation into glioma tumour cells DNA was used as a sensitive index of the cell proliferation. It was found that varapamil (10/sup 4/-10/sup 5/M) and nimodipine (10/sup 4/-10/sup 6/M) significantly inhibited the (/sup 3/H)-thymidine uptake in a dose-related manner. The inhibitory effect of both calcium channel antagonists was reversed by stimultancous addition of calcium chloride (5x10/sup 3/M). These results indicate that verapamil and nimodipine may exert an antiproliferative effect on glioma cells growth acting through a blokade of specific voltage-dependent calcium channels.

  16. In vitro study on the inhibitory effect of ketamine to LPS-induced apoptosis in HUVEC culture

    Directory of Open Access Journals (Sweden)

    Aswoco Andyk Asmoro

    2015-12-01

    Full Text Available Objective: To determine the effect of lipopolysaccharide (LPS exposure and treatment with ketamine to the levels of nitric oxide, intracellular calcium and caspase-3 of human umbilical vein endothelial cell culture. Methods: This research used the human umbilical vein endothelial cell culture with LPS induction. ELISA was conducted to measure the levels of apoptosis markers such as nitric oxide, intracellular calcium and caspase-3. Results: The results showed significant elevation of all parameters after LPS induction. Ketamine addition resulted in various effects. Measurement of intracellular calcium and caspase-3 showed similar result, in which the inhibitory effect of ketamine was more effective when added at the same time as LPS. Vice versa, in nitric oxide measurement, the highest inhibitory effect of ketamine was obtained when added 6 h after LPS induction. Conclusions: At least in part, ketamine was suggested to have inhibitory effect in apoptosis mechanism.

  17. Inhibitory effect of mTOR activator MHY1485 on autophagy: suppression of lysosomal fusion.

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    Yeon Ja Choi

    Full Text Available Autophagy is a major degradative process responsible for the disposal of cytoplasmic proteins and dysfunctional organelles via the lysosomal pathway. During the autophagic process, cells form double-membraned vesicles called autophagosomes that sequester disposable materials in the cytoplasm and finally fuse with lysosomes. In the present study, we investigated the inhibition of autophagy by a synthesized compound, MHY1485, in a culture system by using Ac2F rat hepatocytes. Autophagic flux was measured to evaluate the autophagic activity. Autophagosomes were visualized in Ac2F cells transfected with AdGFP-LC3 by live-cell confocal microscopy. In addition, activity of mTOR, a major regulatory protein of autophagy, was assessed by western blot and docking simulation using AutoDock 4.2. In the result, treatment with MHY1485 suppressed the basal autophagic flux, and this inhibitory effect was clearly confirmed in cells under starvation, a strong physiological inducer of autophagy. The levels of p62 and beclin-1 did not show significant change after treatment with MHY1485. Decreased co-localization of autophagosomes and lysosomes in confocal microscopic images revealed the inhibitory effect of MHY1485 on lysosomal fusion during starvation-induced autophagy. These effects of MHY1485 led to the accumulation of LC3II and enlargement of the autophagosomes in a dose- and time-dependent manner. Furthermore, MHY1485 induced mTOR activation and correspondingly showed a higher docking score than PP242, a well-known ATP-competitive mTOR inhibitor, in docking simulation. In conclusion, MHY1485 has an inhibitory effect on the autophagic process by inhibition of fusion between autophagosomes and lysosomes leading to the accumulation of LC3II protein and enlarged autophagosomes. MHY1485 also induces mTOR activity, providing a possibility for another regulatory mechanism of autophagy by the MHY compound. The significance of this study is the finding of a novel

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

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    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.

  19. 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; 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 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.

  20. In vitro inhibitory effect on digestive enzymes and antioxidant potential of commonly consumed fruits.

    Science.gov (United States)

    Podsędek, Anna; Majewska, Iwona; Redzynia, Małgorzata; Sosnowska, Dorota; Koziołkiewicz, Maria

    2014-05-21

    Dietary inhibitors of fats and carbohydrates degrading enzymes can reduce obesity and type 2 diabetes. In this study, we screened crude extracts from 30 commonly consumed fruits to test their in vitro inhibitory effect against key enzymes relevant for obesity (pancreatic lipase) and type 2 diabetes (α-glucosidase and α-amylase), total phenolic content (Folin-Ciocalteu method), and antioxidant capacity (ABTS and FRAP). The IC50 values of the fruits tested varied from 39.91 to >400 mg/mL, from 1.04 to >80 mg/mL, and from 0.72 to 135.07 mg/mL against α-glucosidase, α-amylase, and pancreatic lipase, respectively. Antioxidant capacity ranged from 0.66 to 124.66 μmol of TE/g of fruit and strongly correlated with phenolic content, while the enzyme inhibition was poorly correlated with total phenolic and antioxidant capacity. Among fruits tested, blue honeysuckle and red gooseberry exhibited the highest inhibitory activity with respect to the carbohydrate degrading enzymes, while lingonberry had the strongest anti-lipase activity.

  1. Inhibitory effects of sea buckthorn procyanidins on fatty acid synthase and MDA-MB-231 cells.

    Science.gov (United States)

    Wang, Yi; Nie, Fangyuan; Ouyang, Jian; Wang, Xiaoyan; Ma, Xiaofeng

    2014-10-01

    Fatty acid synthase (FAS) is overexpressed in many human cancers including breast cancer and is considered to be a promising target for therapy. Sea buckthorn has long been used to treat a variety of maladies. Here, we investigated the inhibitory effect of sea buckthorn procyanidins (SBPs) isolated from the seeds of sea buckthorn on FAS and FAS overexpressed human breast cancer MDA-MB-231 cells. The FAS activity and FAS inhibition were measured by a spectrophotometer at 340 nm of nicotinamide adenine dinucleotide phosphate (NADPH) absorption. We found that SBP potently inhibited the activity of FAS with a half-inhibitory concentration (IC50) value of 0.087 μg/ml. 3-4,5-Dimethylthiazol-2-yl-2,3-diphenyl tetrazolium bromide (MTT) assay was used to test the cell viability. SBP reduced MDA-MB-231 cell viability with an IC50 value of 37.5 μg/ml. Hoechst 33258/propidium iodide dual staining and flow cytometric analysis showed that SBP induced MDA-MB-231 cell apoptosis. SBP inhibited intracellular FAS activity with a dose-dependent manner. In addition, sodium palmitate could rescue the cell apoptosis induced by SBP. These results showed that SBP was a promising FAS inhibitor which could induce the apoptosis of MDA-MB-231 cells via inhibiting FAS. These findings suggested that SBP might be useful for preventing or treating breast cancer.

  2. 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.

  3. 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

  4. Inhibitory effect of Disulfiram/copper complex on non-small cell lung cancer cells

    Energy Technology Data Exchange (ETDEWEB)

    Duan, Lincan [Department of Thoracic Surgery, The Third Affiliated Hospital of Kunming Medical University, Kunming (China); Shen, Hongmei [Cancer Center of Integrative Medicine, The Third Affiliated Hospital of Kunming Medical University, Kunming (China); Zhao, Guangqiang [Department of Thoracic Surgery, The Third Affiliated Hospital of Kunming Medical University, Kunming (China); Yang, Runxiang [Cancer Chemotherapy Center, The Third Affiliated Hospital of Kunming Medical University, Kunming (China); Cai, Xinyi [Colorectal Cancer Center, The Third Affiliated Hospital of Kunming Medical University, Kunming (China); Zhang, Lijuan [Department of Pathology, The Third Affiliated Hospital of Kunming Medical University, Kunming (China); Jin, Congguo [Cancer Institute, The Third Affiliated Hospital of Kunming Medical University, Kunming (China); Huang, Yunchao, E-mail: daliduanlincan@163.com [Department of Thoracic Surgery, The Third Affiliated Hospital of Kunming Medical University, Kunming (China)

    2014-04-18

    Highlights: • Disulfiram and copper synergistically inhibit lung cancer cell proliferation. • Lung cancer cell colony formation ability is inhibited by Disulfiram/copper. • Disulfiram/copper increases the sensitivity of cisplatin to lung cancer cells. • Lung cancer stem cells are specifically targeted by Disulfiram/copper complex. - Abstract: Non-small cell lung cancer (NSCLC) is the most common cause of cancer-related death in both men and women worldwide. Recently, Disulfiram has been reported to be able to inhibit glioblastoma, prostate, or breast cancer cell proliferation. In this study, the synergistic effect of Disulfiram and copper on NSCLC cell growth was investigated. Inhibition of cancer cell proliferation was detected by 1-(4,5-Dimethylthiazol-2-yl)-3,5-diphenylformazan (MTT) assay and cell cycle analysis. Liquid colony formation and tumor spheroid formation assays were used to evaluate their effect on cancer cell clonogenicity. Real-time PCR was performed to test the mRNA level of cancer stem cell related genes. We found that Disulfiram or copper alone did not potently inhibit NSCLC cell proliferation in vitro. However, the presence of copper significantly enhanced inhibitory effect of Disulfiram on NSCLC cell growth, indicating a synergistic effect between Disulfiram and copper. Cell cycle analysis showed that Disulfiram/copper complex caused NSCLC cell cycle arrest in G2/M phase. Furthermore, Disulfiram/copper significantly increased the sensitivity of cisplatin in NSCLC cells tested by MTT assay. Liquid colony formation assay revealed that copper dramatically increased the inhibitory effect of Disulfiram on NSCLC cell colony forming ability. Disulfiram combined with copper significantly attenuated NSCLC cell spheroid formation and recuded the mRNA expression of lung cancer stem cell related genes. Our data suggest that Disulfiram/copper complex alone or combined with other chemotherapy is a potential therapeutic strategy for NSCLC patients.

  5. The inhibitory effect of a polymerisable cationic monomer on functional matrix metalloproteinases.

    Science.gov (United States)

    Liu, Ning; Li, Fang; Chen, Yu-Jiang; Zhang, Ling; Lu, Shuai; Kang, Jun-Jun; Chen, Ji-Hua

    2013-11-01

    This study examined the use of methacryloxylethyl cetyl dimethyl ammonium chloride (DMAE-CB) as a potential matrix metalloproteinases (MMPs) inhibitor on both soluble recombinant and dentine matrix-bound endogenous MMPs, meanwhile attempted to determine the effective anti-MMP group of quaternary ammonium methacrylates (QAMs). The possible inhibitory effects of five DMAE-CB mass concentrations (0.1%, 0.5%, 1%, 3%, 5%) on soluble rhMMP-9 were measured using a colorimetic assay kit. Methyl methacrylate (MMA) and [2-(methacryloyloxy)ethyl] trimethylammonium chloride (METMAC) were also screened against rhMMP-9 to compare the inhibitory effect with DMAE-CB. Matrix-bound endogenous MMP-activity was evaluated in completely demineralized dentine beams. Thirty beams were randomly divided into three groups (N=10) and respectively placed into 500μL of calcium- and zinc-containing media (CM; control), 0.2% chlorhexidine or 3% DMAE-CB in CM aged for 30 days. The changes in modulus of elasticity, loss of dry mass and solubilization of collagen peptides were measured via three-point bending, precision weighing and hydroxyproline assay, respectively. 0.5-5% mass concentrations of DMAE-CB were highly effective (Peffect of MMA was much lower than that of METMAC and DMAE-CB at the same concentration (Peffective in inhibiting both soluble recombinant MMPs and matrix-bound dentine MMPs. Quaternary ammonium group is the effective anti-MMP group of QAMs. The incorporation of DMAE-CB into dental adhesives has the potential to enhance the durability of dentine bonding and thus increases the longevity of restorations. Copyright © 2013 Elsevier Ltd. All rights reserved.

  6. [Study on proteomics of inhibitory effects of elemene on proliferation of human lens epithelial cell].

    Science.gov (United States)

    Hu, Yan-hong; Huang, Xiu-rong; Qi, Ming-xin; Hou, Bu-yuan

    2010-05-01

    To investigate the inhibitory effects of natural medicinal monomer elemene (Ele) on proliferation of human lens epithelial cells B3 (HLE-B3) inducing by recombinant human basic fibroblast growth factor(rhbFGF) and to pursue the proteomics regularity of the inhibitory effects of Ele on proliferation of HLE-B3. Experimental study. This study is divided into three group: control group, rhbFGF group and Ele group. Using 10 microg/L rhbFGF to induce proliferation of HLE-B3. Proliferative HLE-B3 were incubated with 80 mg/L Ele in CO2 incubator for 24 hours. Then the inhibitory effects of Ele on proliferation of HLE-B3 was detected by methyl thiazolyl tetrazolium (MTT). The change of expressions of all protein in HLE-B3 was assayed and analyzed by protein array and surface-enhanced laser desorption ionization time of flight mass spectrometry (SELDI-TOF-MS) proteomics technology. MTT test showed that the A values of rhbFGF (0.599+/-0.053) group were higher than that of control group (0.409+/-0.042) remarkably. The A values of Ele group (0.450+/-0.061) decreased obviously compared to rhbFGF group, the inhibition rates were 24.90% (F=28.886, P=0.000). Five different protein spots were obtained in proliferative HLE-B3 induced by rhbFGF. The expressions were up-regulated in two of the five protein spots at the ratios of mass/charge (m/z) of 8093 and 9516, while the expressions were down-regulated in three of the five protein spots at m/z of 5361, 9666 and 13 767. Ten different protein spots were obtained in HLE-B3 incubated with Ele. The expressions were up-regulated in four of the ten protein spots at m/z of 2487, 4392, 8566 and 11 600, while the expressions were down-regulated in six of the ten protein spots at m/z of 3679, 4826, 6861, 9516, 9557 and 9672. Ele could effectively inhibit HLE-B3 proliferation induced by rhbFGF. The protein spot at m/z of 9516 might be the target of proliferative inhibition in HLE-B3 by Ele.

  7. Carbon tetrachloride-induced hepatic and renal damages in rat: inhibitory effects of cacao polyphenol.

    Science.gov (United States)

    Suzuki, Koichiro; Nakagawa, Kiyotaka; Yamamoto, Takayuki; Miyazawa, Taiki; Kimura, Fumiko; Kamei, Masanori; Miyazawa, Teruo

    2015-01-01

    Here, we investigated the protective effect of cacao polyphenol extract (CPE) on carbon tetrachloride (CCl4)-induced hepato-renal oxidative stress in rats. Rats were administered CPE for 7 days and then received intraperitoneal injection of CCl4. Two hours after injection, we found that CCl4 treatment significantly increased biochemical injury markers, lipid peroxides (phosphatidylcholine hydroperoxide (PCOOH) and malondialdehyde (MDA)) and decreased glutathione peroxidase activity in kidney rather than liver, suggesting that kidney is more vulnerable to oxidative stress under the present experimental conditions. CPE supplementation significantly reduced these changes, indicating that this compound has antioxidant properties against CCl4-induced oxidative stress. An inhibitory effect of CPE on CCl4-induced CYP2E1 mRNA degradation may provide an explanation for CPE antioxidant property. Together, these results provide quantitative evidence of the in vivo antioxidant properties of CPE, especially in terms of PCOOH and MDA levels in the kidneys of CCl4-treated rats.

  8. 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.

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

    Science.gov (United States)

    Zhang, Hongmei; Zhou, Quancheng

    2013-01-01

    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.

  10. Inhibitory effects of veterinary antibiotics on anammox activity: short- and long-term tests.

    Science.gov (United States)

    Sguanci, S; Lotti, T; Caretti, C; Caffaz, S; Dockhorn, T; Lubello, C

    2017-11-01

    The suitability of the anammox process for the treatment of swine digester liquor was assessed through the evaluation of the short- and long-term inhibitory effect of three veterinary antibiotics commonly administered to Italian swine livestock. The toxicity of doxycycline, tiamulin and enrofloxacin was evaluated through batch tests designed to estimate specific anammox activity. Moreover, the short-term toxicity of combined concentrations of doxycycline and enrofloxacin was evaluated so as to verify whether a synergistic effect could be established. According to the inhibition recorded in the presence of the maximum antibiotics concentrations predicted for digester liquor, target compounds do not seem to represent a real hazard for anammox bacteria because at those concentration levels, the activity was just slightly reduced. Moreover, in granular systems, inhibition could be easily counterbalanced by increasing the biomass concentration in the reactor, thus assuring the design treatment capacity for antibiotic-rich wastewaters.

  11. 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

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

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    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.

  13. Simultaneous quantification and inhibitory effect on LDL oxidation of the traditional Korean medicine, Leejung-tang

    Science.gov (United States)

    2014-01-01

    Background Leejung-tang (LJT) is a traditional Korean herbal medicine for the treatment of gastrointestinal disorders. In this study, we performed quantification analysis of five marker components, liquiritin (1), ginsenoside Rg1 (2), ginsenoside Rb1 (3), glycyrrhizin (4), and 6-gingerol (5) in LJT using a high performance liquid chromatography-photodiode array (HPLC–PDA). In addition, we investigated the inhibitory effect on low-density lipoprotein (LDL) oxidation by the LJT sample. Methods Compounds 1–5 were separated within 35 min using a Gemini C18 column. The mobile phase used gradient elution with 1.0% (v/v) aqueous acetic acid (A) and 1.0% (v/v) acetic acid in acetonitrile (B). The flow rate was 1.0 mL/min and the detector was a photodiode array (PDA) set at 203 nm, 254 nm, and 280 nm. The inhibitory effect on LDL oxidation conduct an experiment on thiobarbituric acid reactive substance (TBARS) assay, relative electrophoretic mobility (REM) assay, and electrophoresis of ApoB fragmentation of LJT. Results Calibration curves of compounds 1–5 showed good linearity (r2 ≥0.9995) in different concentration ranges. The recoveries of compounds 1–5 were in the range of 98.90–103.39%, with relative standard deviations (RSD) below 3.0%. The RSDs (%) of intra-day and inter-day precision were 0.10–1.08% and 0.29–1.87%, respectively. The inhibitory effect of LJT on Cu2+-induced LDL oxidation was defined by TBARS assay (IC50: 165.7 μg/mL) and REM of oxLDL (decrease of 50% at 127.7 μg/mL). Furthermore LJT reduced the fragmentation of ApoB of oxLDL in a dose-dependent manner. Conclusions The established HPLC-PDA method will be helpful to improve quality control of LJT. In addition, LJT is a potential LDL oxidation inhibitor. PMID:24383717

  14. Inhibitory effects of neurotransmitters and steroids on human CYP2A6.

    Science.gov (United States)

    Higashi, Eriko; Nakajima, Miki; Katoh, Miki; Tokudome, Shogo; Yokoi, Tsuyoshi

    2007-04-01

    Human CYP2A6 catalyzes the metabolism of nicotine, cotinine, and coumarin as well as some pharmaceutical drugs. CYP2A6 is highly expressed in liver and, also, in brain and steroid-related tissues. In this study, we investigated the inhibitory effects of neurotransmitters and steroid hormones on CYP2A6 activity. We found that coumarin 7-hydroxylation and cotinine 3'-hydroxylation by recombinant CYP2A6 expressed in baculovirus-infected insect cells were competitively inhibited by tryptamine (both K(i) = 0.2 microM), serotonin (K(i) = 252 microM and 167 microM), dopamine (K(i) = 49 microM and 22 microM), and histamine (K(i) = 428 microM and 359 microM). Cotinine formation from nicotine was inhibited by tryptamine (K(i) = 0.7 microM, competitive), serotonin (K(i) = 272 microM, noncompetitive), dopamine, noradrenaline, and adrenaline (K(i) = 11 microM, 54 microM, and 81 microM, uncompetitive). Estrogens (K(i) = 0.6-3.8 microM), androgens (K(i) = 60-149 microM), and corticosterone (K(i) = 36 microM) also inhibited cotinine formation, but coumarin 7-hydroxylation and cotinine 3'-hydroxylation did not. Nicotine-Delta(5'(1'))-iminium ion formation from nicotine was not affected by these steroid hormones, indicating that the inhibition of cotinine formation was due to the inhibitory effects on aldehyde oxidase. The nicotine-Delta(5'(1'))-iminium ion formation was competitively inhibited by tryptamine (K(i) = 0.3 microM), serotonin (K(i) = 316 microM), dopamine (K(i) = 66 microM), and histamine (K(i) = 209 microM). Thus, we found that some neurotransmitters inhibit CYP2A6 activity, being related with inter- and intraindividual differences in CYP2A6-dependent metabolism. The inhibitory effects of steroid hormones on aldehyde oxidase may also contribute to interindividual differences in nicotine metabolism.

  15. 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.

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

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    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.

  17. Multiple inhibitory effects of genistein on stimulus-secretion coupling in rat pancreatic acini.

    Science.gov (United States)

    Duan, R D; Wagner, A C; Yule, D I; Williams, J A

    1994-02-01

    Genistein, a tyrosine kinase inhibitor, inhibited cholecystokinin (CCK)-induced maximal amylase release from rat pancreatic acini by 18, 31, and 46% at concentrations of 100, 300, and 750 microM, respectively, after 30 min preincubation. Genistein similarly decreased amylase release stimulated by bombesin but not that stimulated by secretin or vasoactive intestinal peptide. The steps of stimulus-secretion coupling affected by genistein were further evaluated. We found genistein dose dependently suppressed CCK-as well as NaF-induced polyphosphoinositide hydrolysis with a 50% inhibitory concentration of 380 and 400 microM, respectively, but only slightly suppressed the increase of intracellular Ca2+ concentration in response to either low or high concentrations of CCK. Genistein at 300 microM also decreased incorporation of [3H]inositol into phosphatidylinositol 4,5-bisphosphate. Most strikingly, 300 microM genistein inhibited Ca(2+)-stimulated amylase release by 85% in streptolysin O-permeabilized acini and thapsigargin-stimulated amylase release by 69% in intact acini. Daidzein, the inactive analogue of genistein, had no effect on any of the above parameters. Genistein, up to 750 microM, did not affect amylase release in response to phorbol ester. To relate these inhibitory effects of genistein to its inhibition of tyrosine phosphorylation, Western blotting was performed with an anti-phosphotyrosine monoclonal antibody. Genistein at 100 microM partly and at 300 microM completely inhibited CCK-induced tyrosine phosphorylation. In conclusion, genistein inhibits amylase release at multiple stages of stimulus-secretion coupling. These effects most likely involve both tyrosine kinase-dependent and -independent mechanisms.

  18. 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

  19. 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.

  20. Triterpenoid saponins from the roots of Cyathula officinalis and their inhibitory effects on nitric oxide production.

    Science.gov (United States)

    Jiang, Yun-Tao; Yan, Wen-Jing; Qi, Chu-Lu; Hou, Ji-Qin; Zhong, Yan-Ying; Li, Hui-Jun; Wang, Hao; Li, Ping

    2017-06-01

    The present study was designed to investigate the chemical constituents of the roots of Cyathula officinalis. Compounds were isolated by silica gel, Sephadex LH-20, ODS column chromatography, and preparative HPLC. Their structures were determined on the basis of 1D and 2D NMR techniques, mass spectrometry, and chemical methods. One new oleanane-type triterpenoid saponin, 28-O-[α-L-rhamnopyranosyl-(1→3)-β-D-glucuronopyranosyl-(1→3)-β-D-glucopyranosyl] hederagenin (1), was isolated from the roots of Cyathula officinalis. The anti-inflammatory activities of the isolates were evaluated for their inhibitory effects against LPS-induced nitric oxide (NO) production in RAW 264.7 macrophages cells. Compounds 2, 4, and 6 exhibited moderate anti-inflammatory activities. Copyright © 2017 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.

  1. 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.

  2. 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.

  3. INHIBITORY EFFECT OF CHITOSAN OLIGOSACCHARIDE ON HUMAN HEPATOMA CELLS IN VITRO.

    Science.gov (United States)

    Liu, Likun; Xin, Yi; Liu, Jia; Zhang, Ershao; Li, Weiling

    2017-01-01

    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. MTT assay was applied to detect cell viability of the human hepatoma cells treated with Chitosan oligosaccharide. Flow cytometric analysis was used to investigate the apoptosis of the human hepatoma cells treated with Chitosan oligosaccharide. We employed western blot to investigate the underlying mechanisms involved in the apoptosis. Our data indicated that chitosan oligosaccharide dose-dependently inhibited the growth of hepatoma cells and induced apoptosis. On the molecular level, chitosan oligosaccharide decreased Bcl-2 and increased Caspase-3 expression which may be related to the apoptosis of hepatoma cells. Our results provide an experimental basis for the clinical development of Chitosan oligosaccharide as a novel anti-hepatoma drug.

  4. 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.

  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

    Non-fermenting mycoplasma species deplete culture media for arginine through arginase activity linked to their arginine deiminase pathway, resulting in proliferation arrest and cell death in mycoplasma-contaminated cell cultures. The presence of only 2-3 Mycoplasma (M.) arginini-contaminated T...... cells in a one-way allogeneic mixed-lymphocyte culture (MLC) significantly inhibits development of cytotoxic T-cell activity. Likewise, strong degrees of inhibition are observed after addition of nanogram doses of M. arginini extracts (MAE) to MLC or cell proliferation cultures. M. arginini-induced cell...... 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...

  6. 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.

  7. Inhibitory effect of valproic acid on cytochrome P450 2C9 activity in epilepsy patients.

    Science.gov (United States)

    Gunes, Arzu; Bilir, Erhan; Zengil, Hakan; Babaoglu, Melih O; Bozkurt, Atila; Yasar, Umit

    2007-06-01

    Drug interactions constitute a major problem in the treatment of epilepsy because drug combinations are so common. Valproic acid is a widely used anticonvulsant drug with a broad therapeutic spectrum. Case reports suggest interaction between valproic acid and other drugs metabolized mainly by cytochrome P450 isoforms. The aim of this study was to evaluate the inhibitory effect of valproic acid on cytochrome P450 2C9 (CYP2C9) activity by using losartan oxidation as a probe in epilepsy patients. Patients were prescribed sodium valproate (mean 200 mg/day for the first week and 400 mg/day in the following period) according to their clinical need. A single oral dose of 25 mg losartan was given to patients before and after the first dose, first week and 4 weeks of valproic acid treatment. Losartan and E3174, the CYP2C9-derived carboxylic acid metabolite of losartan in 8 hr urine were assayed by using high pressure liquid chromatography. Urinary losartan/E3174 ratio did not change significantly on the first day (0.9, 0.3-3.5; median, range), and first week (0.6, 0.2-3.8; median, range), while a significant increase was observed after 4 weeks of valproic acid treatment (1.1, 0.3-5.7; median, range) as compared to that of measured before valproic acid administration (0.6, 0.1-2.1; median, range) (P = 0.039). The degree of inhibition was correlated with the steady-state plasma concentrations of valproic acid (r(2) = 0.70, P = 0.04). The results suggest an inhibitory effect of valproic acid on CYP2C9 enzyme activity in epilepsy patients at steady state. The risk of pharmacokinetic drug-drug interactions should be taken into account during concomitant use of valproic acid and CYP2C9 substrates.

  8. Inhibitory effect and mechanism of metformin on human ovarian cancer cells SKOV-3 and A2780.

    Science.gov (United States)

    Huo, J; Bian, X-H; Huang, Y; Miao, Z-C; Song, L-H

    2017-02-01

    Ovarian cancer is the most common malignant tumor in female reproductive system. Metformin is an orally taken hypoglycemic agent, which is extensively applied in the clinic. Clinical trials find that there may be a certain degree of action of the metformin in inhibiting malignant tumors. This paper aims to investigate the inhibitory effect and mechanism of metformin on human ovarian cancer cells. Through in vitro cell experiment, the influences of metformin on the proliferation, colony formation and apoptosis of ovarian carcinoma cells were studied. Ovarian cancer cells SKOV-3 and A2780 in logarithmic growth phase were selected and cell proliferation was measured by MTT method. The metformin was processed for 48 h to calculate the survival rate of cells. Also, metformin was processed for 24 h and two weeks or stained with crystal violet, after which Quantity One (Bio-Rad, Hercules, CA, USA) method was used to quantitatively analyze the cell clone formation, meanwhile, the FCM (flow cytometry) was used for the detection and analysis. Intervened by metformin with different concentrations for 48 h, the cell viabilities of SKOV-3 and A2780 cells were respectively reduced by 19.49 ± 2.92%, 45.41 ± 7.95%, 53.84 ± 5.53%, 64.04 ± 4.36% and 11.45 ± 3.12%, 35.42 ± 7.55%, 43.77 ± 5.77%, 53.05 ± 5.55% as compared with that in the control group with statistical significances. After processed by metformin with different concentrations for two weeks, the cells clone numbers of SKOV-3 and A2780 were significantly reduced. Treatment of metformin on SKOV-3 and A2780 cells of human ovarian cancer showed significant apoptosis. The metformin has the inhibitory effect on the cells of human ovarian cancer, which may be through inducing ovarian cancer cell apoptosis.

  9. Ginsenoside Rg3 enhances the inhibitory effects of chemotherapy on esophageal squamous cell carcinoma in mice.

    Science.gov (United States)

    Chang, Liang; Huo, Bingjie; Lv, Yalei; Wang, Yudong; Liu, Wei

    2014-11-01

    The present study was conducted in order to investigate the inhibitory effects of ginsenoside Rg3 combined with chemotherapy on Eca-109 esophageal squamous cell carcinoma (ESCC) in mice. Tumor xenograft models were established in the right forelimb of 20 BALB/c nude mice by subcutaneous injection. The tumor-bearing mice were randomly assigned to 4 treatment groups (n=5 per group) as follows: the control group (saline), the ginsenoside Rg3 alone group (6 mg/kg/day, once a day for 3 weeks), the chemotherapy alone group (paclitaxel 10 mg/kg/day + cisplatin 5 mg/kg/day on days 1, 7, 14 and 21) and the chemotherapy + Rg3 group (combined treatment). The length and width of the tumor were directly measured with calipers at different time points and the tumor volume (cm 3 ) was calculated using the formula 0.52 × length × width 2 every other day. The mice were sacrificed by cervical dislocation following completion of therapy, the tumors were removed and weighed and the expression levels of Ki-67 were determined by immunohistochemistry. The results indicated that the coadministration of ginsenoside Rg3 significantly enhanced the inhibitory effects of chemotherapy on tumor growth. In addition, the expression levels of Ki-67 in the chemotherapy + Rg3 group were significantly lower compared to those in the other 3 groups. The chemotherapy + Rg3 group also exhibited the lowest microvascular density among all four groups. These findings suggested that ginsenoside Rg3 may improve the antitumor efficacy of chemotherapy in Eca-109 ESCC in mice.

  10. Inhibitory effect of piperine on Helicobacter pylori growth and adhesion to gastric adenocarcinoma cells.

    Science.gov (United States)

    Tharmalingam, Nagendran; Kim, Sa-Hyun; Park, Min; Woo, Hyun Jun; Kim, Hyun Woo; Yang, Ji Yeong; Rhee, Ki-Jong; Kim, Jong Bae

    2014-01-01

    Piperine is a compound comprising 5-9% of black pepper (Piper nigrum), which has a variety of biological roles related to anticancer activities. Helicobacter pylori has been classified as a gastric carcinogen, because it causes gastritis and gastric cancer by injecting the virulent toxin CagA and translocating VacA. The present study investigated the inhibitory action of piperine on H. pylori growth and adhesion. Inhibition of H. pylori growth was determined by the broth macrodilution method, and adhesion to gastric adenocarcinoma cells validated by urease assay. Motility test was performed by motility agar and the expression of adhesion gene and flagellar gene in response to the piperine treatment was assessed by RT-PCR and immunoblotting. Administrated piperine suppressed the level of H. pylori adhesion to gastric adenocarcinoma cells in a dose dependent manner and the inhibition was statistically significant as determined by Student's t-test. In addition, piperine treatment effects on the flagellar hook gene flgE and integral membrane component of the export apparatus gene flhA expression to be suppressed and piperine diminished the H. pylori motility. flhA, encodes an integral membrane component of the export apparatus, which is also one of the regulatory protein in the class 2 genes expression and flgE is one of them that encodes hook part of the flagella. Suppression of both genes, leads to less motility results in the organism attracted less towards to the gastric epithelial cells might be the possible reason in the adhesion inhibition. To our knowledge, this is the first report published on the inhibitory effects of piperine against the adhesion of H. pylori to gastric adenocarcinoma cells.

  11. [Inhibitory effect of DMPP on soil nitrification as affected by soil moisture content, pH and organic matter].

    Science.gov (United States)

    Xue, Yan; Wu, Zhi-Jie; Zhang, Li-Li; Gong, Ping; Dong, Xin-Xin; Nie, Yan-Xia

    2012-10-01

    A laboratory incubation test with meadow brown soil was conducted to study the inhibitory effect of 3,4-dimethylpyrazole phosphate (DMPP) on soil nitrification as affected by soil moisture content (40%, 60% and 80% of the maximum field capacity), pH (4, 7 and 10), and organic matter (retained and removal). With the decrease of soil moisture content, the degradation of DMPP in soil tended to slow down, and the oxidation of soil NH4+ was more inhibited. At pH 10, more DMPP was remained in soil, and had the greatest inhibitory effect; at pH 7 and pH 4, the DMPP was lesser remained, with a smaller inhibitory effect. The removal of organic matter prolonged the remaining time of DMPP in soil, and decreased the apparent soil nitrification rate significantly.

  12. Inhibitory effect of aqueous extract of Echinacea purpurea and Nerium oleander on HSV-1 multiplication

    Directory of Open Access Journals (Sweden)

    Maliheh Farahani

    2014-02-01

    Full Text Available Background: Treatment of HSV-1 infections with the available chemical drugs may have some problems such as drug resistance and virus latency. Therefore, there is a requirement for new antiherpes drugs in today's world. The present study was carried out to analyze the inhibitory effect of Echinacea purpurea and Nerium oleander plants with ethnomedical background on HSV-1 replication. Methods: Plants were extracted by decoction method to obtain aqueous extract. These extracts were screened for their cytotoxicity against Hep-2 cell line by CPE (cytopathic effect assay. Antiviral effect of the plant extracts were determined by the virus cytopathic effect inhibition assay. Results: Nerium oleander extract had the highest toxicity (>0.1 μg/ml on Hep-2 cells and Echinacea purpurea extract exhibited significant antiherpes effect at nontoxic concentrations used on the cell lines. Findings indicated that Echinacea purpurea extract inhibited HSV-1 multiplication at concentrations >400 μg/ml. Conclusion: Echinacea purpurea plant had no any effect on cells at nontoxic concentrations and inhibited HSV-1 multiplication at concentrations >400 μg/ml. Further research is needed to find out the anti herpetic mechanism of this plant.

  13. The Effect of Inhibitory Control on General Mathematics Achievement and Fraction Comparison in Middle School Children

    Science.gov (United States)

    Gómez, David Maximiliano; Jiménez, Abelino; Bobadilla, Roberto; Reyes, Cristián; Dartnell, Pablo

    2015-01-01

    Individual differences in inhibitory control have been shown to relate to general mathematics achievement, but whether this relation varies for specific areas within mathematics is a question that remains open. Here, we evaluate if inhibitory processes play a specific role in the particular case of fraction comparison, where learners must ignore…

  14. 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…

  15. Inhibitory effect of added adenosine diphosphate on palmitate oxidation in mitochondria from rat brain

    Energy Technology Data Exchange (ETDEWEB)

    Kawamura, N.

    1986-05-01

    It is generally accepted that fatty acids are poor substrates for the oxidation in brain because plasma fatty acids do not traverse the blood-brain barrier. However, a regional difference in the barrier suggests that fatty acids are available for oxidation. Why most of fatty acids are not oxidized is not certain. For this reason, regulation of oxidation of (1-/sup 14/C)palmitate (pal) in rat brain has been studied in nonsynaptic mitochondria (mit) prepared by use of Ficoll/sucrose density gradient. The authors found two contrasting oxidations with respect to ATP concentration; Type A at 2 mM and Type B at 0.5 mM. The rate of Type A was 50% of the level of B. Type A was inhibited by high levels of L-carnitine (car) and Mg/sup 2 +/. Added ADP inhibited Type A, but stimulated B. Addition of carboxyatractyloside was stimulatory for Type A, but inhibitory for B. The rate of Type A showed a downward curvature with increasing protein concentration while that of B showed a linear relationship. Addition of NH/sub 4//sup +/ to Type A stimulated the rate and reduced the inhibitory effects of both added ADP and high levels of car. These results suggest that under the normal level of ATP, the carnitine-dependent transport of pal is inhibited (thereby resulting in the inhibition in pal oxidation) by the transport of ADP into mit mediated by the ATP-ADP translocase, but that the inhibition is not observed under the specified conditions or regions where ATP levels are low or ammonia levels are high.

  16. Fungal inhibitory effect of Citrus Limon peel essential oil on Candida albicans

    Directory of Open Access Journals (Sweden)

    Iwan Hernawan

    2015-06-01

    Full Text Available Background: Oral candidiasis is an opportunistic infections due to Candida albicans that often found in people with HIV/AIDS. Anti-fungi, polyne and azole, are used in the treatment of oral candidiasis, but often cause persistence and recurrence. Citrus Limon peel contains terpenoids capable of inhibiting the synthesis of ergosterol, a component of the fungal cell wall that helps to maintain cell membrane permeability. Essential oil derived from citrus limon peel, thus, is expected to inhibit the growth of Candida albicans. Purpose: This research was aimed to know how essential oil derived from citrus Limon peel can inhibit the growth of Candida albicans. Method: This research was a laboratory experimental research carried out in three phases. First, essential oil was made with cold pressing method, and then the concentration of 100% was diluted to 50%, 12.5%, 6.25%, 3.125%, 1.56% and 0.78%. A test was conducted on the culture of Candida albicans in Sabouraud broth, accompanied by control (+ and (-. Second, the dilution of essential oil was conducted to alter the concentration with inhibitory power, from the strongest one to the weakest one, and then it was tested on the culture of Candida albicans. Third, spreading was carried out from liquid culture to agar media in order to measure the number of colonies. Result: Candida albicans did not grow on media with 100% essential oil treatment, but it grew on media with 50% essential oil treatment. In the second phase, dilution of 100%, 90%, 80%, 70%, 60% and 50% was conducted. The growth of Candida albicans was found on the treatment media of 60% and 50%. On the agar media, the growth occurred in the cultured medium treated with 70%. Conclusion: The minimum inhibitory power of essential oil derived from citrus Limon peel against Candida albicans was in the concentration of 80%. Essential oil derived from citrus Limon peel has antifungal effect and potential as a therapeutic agent for oral candidiasis.

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

    Directory of Open Access Journals (Sweden)

    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.

  18. 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.

  19. The Inhibitory Effect of Doxycycline on Cisplatin-Sensitive and -Resistant Epithelial Ovarian Cancer

    Science.gov (United States)

    Ma, Bei; Xu, Ming-juan

    2014-01-01

    Background Detecting a new effective and hypotoxic anticancer drug is an emerging new strategy for cancer chemotherapy. Doxycycline (DC) is a kind of antibiotics but also inhibits tumorigenesis. Methods MTT and cell invasion assay, flow cytometry, western-blot analysis and nude mice were used to investigate the effects and underlying mechanisms of doxycycline on epithelial ovarian cancer cells. Results Doxycycline inhibited the proliferation and invasion of SKOV3 and SKOV3/DDP; induced moderate apoptosis of SKOV3/DDP. CXCR4 expression at both mRNA and protein levels was downregulated in both cell lines when treated with doxycycline. Akt and ERK1/2 were involved in doxycycline effect on cell proliferation of SKOV3 but not of SKOV3/DDP. Akt and EKR1/2 phosphorylation were activated by SDF-1α, which was then inhibited by doxycycline in SKOV3. Pro-caspase-3 expression was significantly higher in SKOV3 than that in SKOV3/DDP which was upregulated when treated with doxycycline. In vivo, doxycycline inhibited peritoneal tumor xenograft and decreased malignant ascites. Conclusion Doxycycline not only has an inhibitory effect on ovarian cancer, but also can increase sensitivity to cisplatin. SDF-1α/CXCR4-regulated Akt and ERK 1/2 activations are probably involved in the antitumor effect of doxycycline on SKOV3 cells, while upregulation of pro-caspase-3 may be the main mechanism involved in SKOV3/DDP cells. PMID:24598933

  20. Growth inhibitory effects of the dual ErbB1/ErbB2 tyrosine kinase inhibitor PKI-166 on human prostate cancer xenografts.

    Science.gov (United States)

    Mellinghoff, Ingo K; Tran, Chris; Sawyers, Charles L

    2002-09-15

    Experiments with human prostate cancer cell lines have shown that forced overexpression of the ErbB2-receptor tyrosine kinase (RTK) promotes androgen-independent growth and increases androgen receptor-transcriptional activity in a ligand-independent fashion. To investigate the relationship between ErbB-RTK signaling and androgen in genetically unmanipulated human prostate cancer, we performed biochemical and biological studies with the dual ErbB1/ErbB2 RTK inhibitor PKI-166 using human prostate cancer xenograft models with isogenic sublines reflecting the transition from androgen-dependent to androgen-independent growth. In the presence of low androgen concentrations, PKI-166 showed profound growth-inhibitory effects on tumor growth, which could be partially reversed by androgen add-back. At physiological androgen concentrations, androgen withdrawal greatly enhanced the ability of PKI-166 to retard tumor growth. The level of extracellular signal-regulated kinase activation correlated with the response to PKI-166 treatment, whereas the expression levels of ErbB1 and ErbB2 did not. These results suggest that ErbB1/ErbB2 RTKs play an important role in the biology of androgen-independent prostate cancer and provide a rationale for clinical evaluation of inhibitors targeted to this pathway.

  1. 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.

  2. 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.

  3. The inhibitory effect of locally injected dexmedetomidine on carrageenan-induced nociception in rats.

    Science.gov (United States)

    Honda, Yuka; Higuchi, Hitoshi; Matsuoka, Yoshikazu; Yabuki-Kawase, Akiko; Ishii-Maruhama, Minako; Tomoyasu, Yumiko; Maeda, Shigeru; Morimatsu, Hiroshi; Miyawaki, Takuya

    2015-10-05

    Recent studies showed that the administration of dexmedetomidine relieved hyperalgesia in the presence of neuropathic pain. These findings have led to the hypothesis that the local administration of dexmedetomidine is useful for relieving acute inflammatory nociception, such as postoperative pain. Thus, we evaluated the inhibitory effect of locally injected dexmedetomidine on acute inflammatory nociception. Acute inflammatory nociception was induced by an intraplantar injection of 1% carrageenan into the hindpaws of rats, and dexmedetomidine was also injected combined with carrageenan. The paw withdrawal threshold based on von Frey filament stimulation was measured until 12 h after injection. We compared the area under the time-curve (AUC) between carrageenan and carrageenan with dexmedetomidine. To clarify that the action of dexmedetomidine was via α2-adrenoceptors, we evaluated the effect of yohimbine, a selective antagonist of α2-adrenoceptors, on the anti-nociception of dexmedetomidine. As the results, the intraplantar injection of carrageenan with over 10 μM dexmedetomidine significantly increased AUC, compared to that with only carrageenan injection. This effect of dexmedetomidine was reversed by the addition of yohimbine to carrageenan and dexmedetomidine. These results demonstrated that the locally injected dexmedetomidine was effective against carrageenan-induced inflammatory nociception via α2-adrenoceptors. The findings suggest that the local injection of dexmedetomidine is useful for relieving local acute inflammatory nociception. Copyright © 2015 Elsevier B.V. All rights reserved.

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

    Directory of Open Access Journals (Sweden)

    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.

  5. Central administration of obestatin fails to show inhibitory effects on food and water intake in mice.

    Science.gov (United States)

    Van Dijck, Annemie; Annemie, Van Dijck; Van Dam, Debby; Debby, Van Dam; Vergote, Valentijn; Valentijn, Vergote; De Spiegeleer, Bart; Bart, De Spiegeleer; Luyten, Walter; Walter, Luyten; Schoofs, Liliane; Liliane, Schoofs; De Deyn, Peter Paul; Peter Paul, De Deyn

    2009-08-07

    Obestatin is a ghrelin-associated peptide hormone with presumed anorexigenic and inhibitory effect on gastric propulsive motility activity. Recent literature, however, discloses much contestation over satiety and gastrointestinal motility-related functionalities of obestatin. In addition, antidipsinogenic effects in rodents by obestatin were recently reported. The present study was set up to bring more clarity into the contested effects of obestatin on food and water intake. Additionally, the stability of obestatin in brain tissue homogenate was investigated. The in vitro incubation of obestatin in brain homogenates revealed disappearance half-life times of 19 min for crude brain homogenate to 27 min for brain membrane homogenate. For the behavioural studies, male C57Bl/6 mice were intracerebroventricularly treated with 0.2 nmol murine amidated obestatin or vehicle at the age of 3 months. An additional group of mice was treated with 0.3 nmol of corticotropin releasing factor (CRF) as a positive control of suppression of food intake. Food and water intake were studied over a period of 5 h in metabolic cages. Under our experimental conditions, no suppressive effects of obestatin on food or water intake were observed, whereas CRF evoked a significant suppression of food intake, which proves the internal validity of the study design.

  6. Topochemical synthesis of Co-Fe layered double hydroxides at varied Fe/Co ratios: unique intercalation of triiodide and its profound effect.

    Science.gov (United States)

    Ma, Renzhi; Liang, Jianbo; Takada, Kazunori; Sasaki, Takayoshi

    2011-01-26

    Co-Fe layered double hydroxides at different Fe/Co ratios were synthesized from brucite-like Co(2+)(1-x)Fe(2+)(x)(OH)(2) (0 ≤ x ≤ 1/3) via oxidative intercalation reaction using an excess amount of iodine as the oxidizing agent. A new redoxable species: triiodide (I(3)(-)), promoted the formation of single-phase Co-Fe LDHs. The results point to a general principle that LDHs with a characteristic ratio of total trivalent and divalent cations (M(3+)/M(2+)) at 1/2 may be the most stable in the oxidative intercalation procedure. At low Fe content, e.g., starting from Co(2+)(1-x)Fe(2+)(x)(OH)(2) (x triiodide and iodide into the interlayer gallery of as-transformed LDH phase, which profoundly impacted the relative intensity ratio of basal Bragg peaks as a consequence of the significant X-ray scattering power of triiodide. In combination with XRD simulation, the LDH structure model was constructed by considering both the host layer composition/charge and the arrangement of interlayer triiodide/iodide. The work provides a clear understanding of the thermodynamic and kinetic factors associated with the oxidative intercalation reaction and is helpful in elucidating the formation of LDH structure in general.

  7. 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

    structure of collagen. Many of these peptides had C-terminal sequences similar to known ACE-inhibitory peptides. The present results suggest that collagen-rich food materials are good substrates for the release of potent ACE-inhibitory peptides, when proper pre-treatment and enzymatic treatment is applied.......Bovine collagen was pre-treated (boiled or high pressure (HP)-treated) and then hydrolysed by 6 proteases. The degree of hydrolysis (DH) and the angiotensin-converting enzyme (ACE)-inhibitory activity of hydrolysates were measured. All enzymes used were able to partly degrade collagen and release...

  8. Inhibitory Effect of Sophorolipid on Candida albicans Biofilm Formation and Hyphal Growth.

    Science.gov (United States)

    Haque, Farazul; Alfatah, Md; Ganesan, K; Bhattacharyya, Mani Shankar

    2016-03-31

    Candida albicans causes superficial and life-threatening systemic infections. These are difficult to treat often due to drug resistance, particularly because C. albicans biofilms are inherently resistant to most antifungals. Sophorolipid (SL), a glycolipid biosurfactant, has been shown to have antimicrobial and anticancer properties. In this study, we investigated the effect of SL on C. albicans biofilm formation and preformed biofilms. SL was found to inhibit C. albicans biofilm formation as well as reduce the viability of preformed biofilms. Moreover, SL, when used along with amphotericin B (AmB) or fluconazole (FLZ), was found to act synergistically against biofilm formation and preformed biofilms. Effect of SL on C. albicans biofilm formation was further visualized by scanning electron microscopy (SEM) and confocal laser scanning microscopy (CLSM), which revealed absence of hyphae, typical biofilm architecture and alteration in the morphology of biofilm cells. We also found that SL downregulates the expression of hypha specific genes HWP1, ALS1, ALS3, ECE1 and SAP4, which possibly explains the inhibitory effect of SL on hyphae and biofilm formation.

  9. Inhibitory effect of cholesteryl gamma-aminobutyrate on evoked activity in rat hippocampal slices.

    Science.gov (United States)

    Hesse, G W; Shashoua, V E; Jacob, J N

    1985-02-01

    Cholesteryl gamma-aminobutyrate (C-G) readily crosses the blood-brain barrier and has properties that suggest that it may be a potential gamma-aminobutyric acid (GABA)-mimetic compound. The effect of this compound on the orthodromically-evoked discharge of hippocampal pyramidal cells was investigated using slices of rat hippocampus maintained in vitro. The compound produced dose-dependent inhibition of the discharge of pyramidal cells. The magnitude of the inhibitory effect was somewhat less than that produced by a similar dose of GABA, but the duration of the inhibition was prolonged by about 10-fold over that produced by GABA. The inhibition produced by cholesteryl gamma-aminobutyrate was blocked by the addition of picrotoxin to the incubation medium, and by replacement of chloride with isethionate. In addition, pretreatment of slices with the irreversible esterase inhibitor, phenylmethylsulfonylfluoride, attenuated the effects of cholesteryl gamma-aminobutyrate, but not that of GABA. These results suggest that cholesteryl gamma-aminobutyrate has GABA-like actions in the CNS, and that its activity is largely dependent upon enzymatic release of GABA from the compound by esterases present in the tissue.

  10. 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.

  11. 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.

  12. 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.

  13. 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.

  14. Analysis of the inhibitory effects of chloropicrin fumigation on nitrification in various soil types.

    Science.gov (United States)

    Yan, Dongdong; Wang, Qiuxia; Li, Yuan; Ouyang, Canbin; Guo, Meixia; Cao, Aocheng

    2017-05-01

    Chloropicrin retards the conversion of ammonia to nitrite during the nitrification process in soil. In our study, the dynamic effect of chloropicrin fumigation on soil nitrification was evaluated in five different soil types to identify relationships between soil properties and the effect of fumigation on nitrification. Chloropicrin significantly inhibited nitrification in all soils; however, the recovery of nitrification varied greatly between the soils. Following chloropicrin fumigation, nitrification recovered to the control level in all soils, except in the acidic Guangxi soil. Nitrification recovered faster in fumigated sandy loam Beijing soil than in the other four fumigated soils. Soil texture and pH were two important factors that influenced chloropicrin's inhibitory effect on nitrification. An S-shaped function was fitted to soil NO3(-)-N content to assess the nitrification recovery tendency in different soils. The time taken to reach maximum nitrification (tmax) ranged from 2.4 to 3.0 weeks in all unfumigated soils. Results demonstrated that tmax was greater in all fumigated soils than in untreated soils. Correlation calculations showed that tmax was strongly correlated to soil texture. The correlation analysis results indicated that the recovery rate of nitrification after chloropicrin fumigation is much faster in sandy loam soil than silty loam soil. Copyright © 2017. Published by Elsevier Ltd.

  15. 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

  16. The inhibitory effect of vitamin K on RANKL-induced osteoclast differentiation and bone resorption.

    Science.gov (United States)

    Wu, Wei-Jie; Kim, Min Seuk; Ahn, Byung-Yong

    2015-10-01

    To further understand the correlation between vitamin K and bone metabolism, the effects of vitamins K1, menaquinone-4 (MK-4), and menaquinone-7 (MK-7) on RANKL-induced osteoclast differentiation and bone resorption were comparatively investigated. Vitamin K2 groups (MK-4 and MK-7) were found to significantly inhibit RANKL-medicated osteoclast cell formation of bone marrow macrophages (BMMs) in a dose-dependent manner, without any evidence of cytotoxicity. The mRNA expression of specific osteoclast differentiation markers, such as c-Fos, NFATc1, OSCAR, and TRAP, as well as NFATc1 protein expression and TRAP activity in RANKL-treated BMMs were inhibited by vitamin K2, although MK-4 exhibited a significantly greater efficiency compared to MK-7. In contrast, the same dose of vitamin K1 had no inhibitory effect on RANKL-induced osteoclast cell formation, but increased the expression of major osteoclastogenic genes. Interestingly, vitamins K1, MK-4 and MK-7 all strongly inhibited osteoclastic bone resorption (p vitamins K1, MK-4 and MK-7 have anti-osteoporotic properties, while their regulation effects on osteoclastogenesis are somewhat different.

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

    Science.gov (United States)

    Xiao, Jie; Xu, Xiaobo; Li, Xiao; Li, Yanli; Liu, Guobing; Tan, Hui; Shen, Hua; Shi, Hongcheng; Cheng, Dengfeng

    2016-09-30

    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.

  19. 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 (HV1) 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 H1 receptors have beneficial effects against microglia-mediated oxidative stress and neurotoxicity. We examined the effects of the H1 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 IC50 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 HV1 proton channel abnormalities. Copyright © 2017 Elsevier B.V. All rights reserved.

  20. 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.

  1. Genetic variants on rat chromosome 8 exhibit profound effects on hypertension severity and survival during nitric oxide inhibition in spontaneously hypertensive rats.

    Science.gov (United States)

    Schulz, Angela; Schütten-Faber, Sabrina; Schulte, Leonard; Unland, Johannes; Kossmehl, Peter; Kreutz, Reinhold

    2014-03-01

    Hypertension and mortality is aggravated by nitric oxide inhibition with N(G)-nitro-L-arginine methyl ester (L-NAME) in spontaneously hypertensive rats (SHRs) but not in Munich Wistar Frömter (MWF) rats. MWF rats carry major albuminuria quantitative trait loci on rat chromosome (RNO) 6 and RNO8; susceptibility of SHRs to L-NAME is enhanced by transfer of RNO6 from MWF rats into the SHR background. Here, we tested whether the sensitivity to L-NAME in SHRs is affected by transfer of RNO8 from MWF rats in consomic SHR-8(MWF) rats. In study 1, we analyzed survival in male SHR and SHR-8(MWF) rats in response to 18 weeks of treatment with either normal drinking water (vehicle-treated) or water containing 20mg/L L-NAME. In study 2, we analyzed blood pressure and renal damage in both strains in response to 6 weeks of treatment with L-NAME compared with vehicle-treated groups. In study 1, starting after 6 weeks of treatment with L-NAME, mortality reached 90% in SHRs in contrast with the group of L-NAME treated SHR-8(MWF) rats (P rats survived similar to vehicle-treated rats. In study 2, L-NAME resulted in a more pronounced increase in mean arterial blood pressures in SHRs compared with SHR-8(MWF) rats (216 ± 6 vs. 180 ± 11 mm Hg; P rats after L-NAME treatment (P < 0.05), whereas albuminuria was not different between strains. The blood pressure increase and impaired survival of SHRs in response to nitric oxide inhibition is profoundly influenced by genes on RNO8.

  2. The effects of environmental enrichment and age-related differences on inhibitory avoidance in zebrafish (Danio rerio Hamilton)

    NARCIS (Netherlands)

    Manuel, R.; Gorissen, M.; Stokkermans, M.; Zethof, J.; Ebbesson, L.O.E.; Vis, van de J.W.; Flik, G.; Bos, van den R.

    2015-01-01

    The inhibitory avoidance paradigm allows the study of mechanisms underlying learning and memory formation in zebrafish (Danio rerio Hamilton). For zebrafish, the physiology and behavior associated with this paradigm are as yet poorly understood. We therefore assessed the effects of environmental

  3. 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

  4. 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.

  5. 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.

  6. Growth inhibitory effect of grape phenolics against wine spoilage yeasts and acetic acid bacteria.

    Science.gov (United States)

    Pastorkova, E; Zakova, T; Landa, P; Novakova, J; Vadlejch, J; Kokoska, L

    2013-02-15

    This paper investigates the in vitro antimicrobial potential of 15 grape phenolic compounds of various chemical classes (phenolic acids, stilbenes and flavonoids) using the broth microdilution method against yeasts and acetic acid bacteria frequently occurring in deteriorated wine. Pterostilbene (MICs=32-128 μg/mL), resveratrol (MICs=256-512 μg/mL) and luteolin (MICs=256-512 μg/mL) are among six active compounds that possessed the strongest inhibitory effects against all microorganisms tested. In the case of phenolic acids, myricetin, p-coumaric and ferulic acids exhibited selective antimicrobial activity (MICs=256-512 μg/mL), depending upon yeasts and bacteria tested. In comparison with potassium metabisulphite, all microorganisms tested were more susceptible to the phenolics. The results revealed the antibacterial and antiyeast effects against wine spoilage microorganisms of several highly potent phenolics naturally occurring in grapes. These findings also provide arguments for further investigation of stilbenes as prospective compounds reducing the need for the use of sulphites in winemaking. Copyright © 2012 Elsevier B.V. All rights reserved.

  7. Inhibitory effects of polyphosphates on Clostridium perfringens growth, sporulation and spore outgrowth.

    Science.gov (United States)

    Akhtar, Saeed; Paredes-Sabja, Daniel; Sarker, Mahfuzur R

    2008-09-01

    This study evaluated the effects of various polyphosphates (SPP, STPP, SAPP and TSPP) on growth, sporulation and spore germination of Clostridium perfringens, and germination and outgrowth of C. perfrinegns spores in poultry meat. We have found that the requirements of polyP (0.8-1.0%) to inhibit C. perfringens bacterial growth were higher than those reported for other bacteria. Sub-lethal concentrations of polyP significantly (pperfringens by reducing sporulating cells (heat-resistant cells) approximately 5-6 log(10). While C. perfringens spores were able to germinate in the presence of 1% STPP, their outgrowth was significantly (pperfringens was observed when meat samples contaminated with a cocktail of spores of C. perfringens isolates carrying enterotoxin gene on the chromosome were treated with 1% STPP. Collectively, this study demonstrated the inhibitory effects of polyP on growth, sporulation and spore outgrowth of C. perfringens, and suggests that polyP can be used not only as an enhancer of the functional properties of meat products, but also as a promising C. perfringens antimicrobial agent.

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

    Science.gov (United States)

    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.

  9. 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.

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

    Directory of Open Access Journals (Sweden)

    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.

  11. Antioxidant and tyrosinase inhibitory effects of neolignan glycosides from Crataegus pinnatifida seeds.

    Science.gov (United States)

    Huang, Xiao-Xiao; Liu, Qing-Bo; Wu, Jie; Yu, Li-Hong; Cong, Qian; Zhang, Yan; Lou, Li-Li; Li, Ling-Zhi; Song, Shao-Jiang

    2014-12-01

    In our efforts to find an inhibitor of melanin formation and develop potential depigmenting agents for skin-protecting cosmetics and medicinal products from natural resources, we focused on the seeds of Crataegus pinnatifida which showed antioxidant and tyrosinase-inhibiting activities. By activity-guided fractionation of an extract of C. pinnatifida seeds, four new neolignan glycosides, pinnatifidaninsides A-D (1-4), along with two known compounds (5-6), were isolated. Their structures were elucidated by spectroscopic analyses, especially 1D, 2D NMR and CD spectra. The antioxidant and tyrosinase-inhibiting activities of all isolates were assayed. Compound 6 showed good activity against 2,2-diphenyl-1-pikrylhydrazyl, while compounds 1, 2, 5, and 6 exhibited strong 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) free radical scavenging activity, being as effective as, or even more effective than the positive control Trolox. Moreover, compounds 5 and 6 displayed a moderate mushroom tyrosinase inhibitory activity. Georg Thieme Verlag KG Stuttgart · New York.

  12. 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.

  13. 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.

  14. Inhibitory effect of Newcastle disease virus on hepatic fibrosis induced by CCl4

    Directory of Open Access Journals (Sweden)

    Ya-lin LI

    2013-11-01

    Full Text Available Objective To explore the inhibitory effect of Newcastle diseases virus (NDV on CCl4-induced liver fibrosis in mice. Methods Liver fibrosis model was reproduced in 30 Kunming mice by intraperitoneal injection of CCl4/peanut oil solution for 2 times a week, and the total treatment lasted for 8 weeks. Three days after last injection, NDV was injected through tail vein for 1 or 3 times (24h intervals. Twenty-four hours after NDV infusion, mice were sacrificed and the livers were removed for gross morphology observation. The liver tissue sections were stained by HE and Sirius red dyeing. α-smooth muscle actin (α-SMA expression was detected by Western blotting. Results After CCl4 induction for 8 weeks, obvious fibrosis symptoms appeared in the liver of model mice, and the surface of liver tissue became hard with rough, with white patches on it. HE staining showed that there was loosening of tissue and enlarged perisinusoidal spaces in liver with fibrosis. Sirius red dyeing displayed abnormal collagen deposition in the fibrotic liver tissues. After NDV injection for 3 times, white spots on the surface of mouse liver were significantly reduced, and collagen deposition was lowered. Western blotting showed that α-SMA levels decreased with increasing frequency of NDV injection. Conclusion NDV may effectively suppress the development of CCl4-induced liver fibrosis in mice. DOI: 10.11855/j.issn.0577-7402.2013.11.003

  15. 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 (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 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 (Vcmax) and the initial slope of A-Ci curve (k) were estimated by measuring leaf gas exchange and chlorophyll fluorescence. Photosynthesis was inhibited by sucrose spraying in both genotypes, through decreases in Vcmax, k, gs and ATP production driven by electron transport (Jatp). 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 Vcmax, gs and Jatp 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.

  16. Inhibitory Effects of Constituents from the Aerial Parts of Rosmarinus officinalis L. on Triglyceride Accumulation.

    Science.gov (United States)

    Li, Jian; Adelakun, Tiwalade Adegoke; Wang, Sijian; Ruan, Jingya; Yang, Shengcai; Li, Xiaoxia; Zhang, Yi; Wang, Tao

    2017-01-17

    Sixteen flavonoids (1-16) including two new ones, named officinoflavonosides A (1) and B (2) were obtained from the aerial parts of Rosmarinus officinalis. Among the known ones, 6, 10, and 13 were isolated from the rosmarinus genus for the first time. Their structures were elucidated by chemical and spectroscopic methods. Moreover, the effects on sodium oleate-induced triglyceride accumulation (TG) in HepG2 cells of the above-mentioned compounds and 16 other isolates (17-32) reported previously to have been obtained in the plant were analyzed. Results show that eight kinds of flavonoids (compounds 1, 2, 3, 6-9 and 11) and seven kinds of other known isolates (compounds 17-20, 23, 26 and 31) possessed significant inhibitory effects on intracellular TG content in HepG2 cells. Among them, the activities of compounds 1 and 20 were comparable to that of orlistat, which suggested that these compounds in this plant might be involved in lipid metabolism.

  17. 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.

  18. 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.

  19. 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.

  20. 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.

  1. In vitro inhibitory effects of tea polyphenols on the proliferation of Chlamydia trachomatis and Chlamydia pneumoniae.

    Science.gov (United States)

    Yamazaki, Tsutomu; Inoue, Miyuki; Sasaki, Nozomu; Hagiwara, Toshikatsu; Kishimoto, Toshio; Shiga, Sadashi; Ogawa, Motohiko; Hara, Yukihiko; Matsumoto, Takaaki

    2003-08-01

    In vitro inhibitory effects of tea polyphenols on Chlamydia trachomatis and C. pneumoniae were investigated. A product of tea polyphenols, Polyphenon 70S was used. Chlamydial strains used were C. trachomatis D/UW-3/Cx and L(2)/434/Bu, and C. pneumoniae AR-39 and AC-43 strains. HeLa229 cells and HL cells were used for cultivation of C. trachomatis and C. pneumoniae, respectively. In the post-inoculation method, no inclusions of C. trachomatis were observed at 0.5 mg/ml of Polyphenon 70S. However, the toxicity of Polyphenon 70S was noted in HeLa229 cells and HL cells at a concentration of 0.25 mg/ml. In the pre-inoculation method, no toxic effects of Polyphenon 70S on the cells were noted. Complete inhibition of C. trachomatis D and L(2) was noted at concentrations of 1.6 and 0.4 mg/ml, respectively. With C. pneumoniae strains, the end points were 0.8 and 1.6 mg/ml for AR-39 and AC-43, respectively. Our findings encouraged the application of tea polyphenols for topical usage.

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

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    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.

  3. 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.

  4. [Inhibitory effect of thalidomide combined with interferon on the proliferation of Kasumi-1 cells].

    Science.gov (United States)

    Xu, Hao; Mi, Ruihua; Fan, Ruihua; Yin, Qingsong; Wang, Xiaojiao; Wei, Xudong

    2015-09-01

    To explore the inhibitory effect of thalidomide combined with interferon (IFN) on the human acute myeloid leukemia cell line Kasumi- 1 and its mechanism. The inhibitiory effect of Kasumi- 1 cells by thalidomide, interferon or combination was detected by CCK- 8 method, the apoptosis by flow cytometry, the expression of apoptosis related proteins by Western blot, vascular endothelial growth factor (VEGF) concentration in culture supernatant by ELISA. Thalidomide inhibited the proliferation of Kasumi- 1 in a dose- dependent manner from 50 μg/ml to 500 μg/ml with an IC₅₀ of (451.13 ± 6.92)μg/ml at 24 h and (362.50 ± 14.52)μg/ml at 48 h. IFN also demonstrated the inhibitory capacity in a dose-dependent manner from 500 U/ml to 5 000 U/ml, with an IC₅₀ of (2 209 ± 127) U/ml at 24 h and (1 393±63) U/ml at 48 h. The apoptosis rates of Kasumi-1 cells treated with thalidomide 350 μg/ml or IFN 1 400 U/ml for 48 h were (14.68 ± 2.61) % and (21.71 ± 0.71)%, respectively, significantly higher than control group (Pthalidomide group [(141.11 ± 3.70) ng/L and IFN group [(119.90 ± 2.00) ng/L (P thalidomide 350 μg/ml or IFN 1 400 U/ml for 48 h. When treated with the combination agents, the expression of Bcl-2 further decreased and p-P38, Bax, cytochrome C, cleaved-Caspase-3, 8, 9 further increased as compared with each single agent (P Thalidomide and IFN could synergistically inhibit the proliferation of Kasumi-1 cells probably through inducing apoptosis via the mitochondrial pathway, death receptor pathway and P38 MAPK pathway, as well as inhibiting VEGF secretion.

  5. Inhibitory effect of mitragynine on human cytochrome P450 enzyme activities.

    Science.gov (United States)

    Hanapi, N A; Ismail, S; Mansor, S M

    2013-10-01

    To date, many findings reveal that most of the modern drugs have the ability to interact with herbal drugs. This study was conducted to determine the inhibitory effects of mitragynine on cytochrome P450 2C9, 2D6 and 3A4 activities. The in vitro study was conducted using a high-throughput luminescence assay. Statistical analysis was conducted using one-way ANOVA and Dunnett's test with P GraphPad Prism(®) 5 (Version 5.01, GraphPad Software, Inc., USA). Assessment using recombinant enzymes showed that mitragynine gave the strongest inhibitory effect on CYP2D6 with an IC50 value of 0.45±0.33 mM, followed by CYP2C9 and CYP3A4 with IC50 values of 9.70±4.80 and 41.32±6.74 μM respectively. Positive inhibitors appropriate for CYP2C9, CYP2D6, and CYP3A4 which are sulfaphenazole, quinidine and ketoconazole were used respectively. Vmax values of CYP2C9, CYP2D6 and CYP3A4 were 0.0005, 0.01155 and 0.0137 μM luciferin formed/pmol/min respectively. Km values of CYP2C9, CYP2D6, and CYP3A4 were 32.65, 56.01, and 103.30 μM respectively. Mitragynine noncompetitively inhibits CYP2C9 and CYP2D6 activities with the Ki values of 61.48 and 12.86 μM respectively. On the other hand, mitragynine inhibits CYP3A4 competitively with a Ki value of 379.18 μM. The findings of this study reveal that mitragynine might inhibit cytochrome P450 enzyme activities, specifically CYP2D6. Therefore, administration of mitragynine together with herbal or modern drugs which follow the same metabolic pathway may contribute to herb-drug interactions.

  6. HIV-1 protease inhibitory effects of some selected plants in Caesalpiniaceae and Papilionaceae families

    OpenAIRE

    Pranee Rattanasuwan; Sanan Subhadhirasakul; Supinya Tewtrakul

    2003-01-01

    Fifty-two ethanol and water extracts of the plants in Caesalpiniaceae and Papilionaceae families were screened for their HIV-1 protease (HIV-1 PR) inhibitory activities using high performance liquid chromatography (HPLC) technique. Among the tested extracts, Cassia garrettiana (wood, water extract) showed the most potent inhibitory activity against HIV-1 PR, followed by Cassia garrettiana (wood, EtOH extract) and Caesalpinia sappan (wood, EtOH extract) with IC50 of 18, 32 and 75 μg/ml, respec...

  7. 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.

  8. The direct inhibitory effect of dutasteride or finasteride on androgen receptor activity is cell line specific.

    Science.gov (United States)

    Chhipa, Rishi Raj; Halim, Danny; Cheng, Jinrong; Zhang, Huan Yi; Mohler, James L; Ip, Clement; Wu, Yue

    2013-10-01

    Finasteride and dutasteride were developed originally as 5α-reductase inhibitors to block the conversion of testosterone to dihydrotestosterone (DHT). These drugs may possess off-target effects on the androgen receptor (AR) due to their structural similarity to DHT. A total of four human prostate cancer cell models were examined: LNCaP (T877A mutant AR), 22Rv1 (H874Y mutant AR), LAPC4 (wild-type AR), and VCaP (wild-type AR). Cells were cultured in 10% charcoal-stripped fetal bovine serum, either with or without DHT added to the medium. AR activity was evaluated using the ARE-luciferase assay or the expression of AR regulated genes. Dutasteride was more potent than finasteride in interfering with DHT-stimulated AR signaling. Disruption of AR function was accompanied by decreased cell growth. Cells that rely on DHT for protection against death were particularly vulnerable to dutasteride. Different prostate cancer cell models exhibited different sensitivities to dutasteride and finasteride. LNCaP was most sensitive, LAPC4 and VCaP were intermediate, while 22Rv1 was least sensitive. Regardless of the AR genotype, if AR was transfected into drug-sensitive cells, AR was inhibited by drug treatment; and if AR was transfected into drug-resistant cells, AR was not inhibited. The direct inhibitory effect of dutasteride or finasteride on AR signaling is cell line specific. Mutations in the ligand binding domain of AR do not appear to play a significant role in influencing the AR antagonistic effect of these drugs. Subcellular constituent is an important factor in determining the drug effect on AR function. Copyright © 2013 Wiley Periodicals, Inc.

  9. 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.

  10. 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.

  11. 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.

  12. 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.

  13. 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

  14. A novel polyherbal microbicide with inhibitory effect on bacterial, fungal and viral genital pathogens.

    Science.gov (United States)

    Talwar, G P; Dar, Sajad A; Rai, Mahendra K; Reddy, K V R; Mitra, Debashis; Kulkarni, Sujata V; Doncel, Gustavo F; Buck, Christopher B; Schiller, John T; Muralidhar, Sumathi; Bala, Manju; Agrawal, S S; Bansal, Kavita; Verma, Jitendra K

    2008-08-01

    A polyherbal cream (Basant) has been formulated using diferuloylmethane (curcumin), purified extracts of Emblica officinalis (Amla), purified saponins from Sapindus mukorossi, Aloe vera and rose water along with pharmacopoeially approved excipients and preservatives. Basant inhibits the growth of WHO strains and clinical isolates of Neisseria gonorrhoeae, including those resistant to penicillin, tetracycline, nalidixic acid and ciprofloxacin. It has pronounced inhibitory action against Candida glabrata, Candida albicans and Candida tropicalis isolated from women with vulvovaginal candidiasis, including three isolates resistant to azole drugs and amphotericin B. Basant displayed a high virucidal action against human immunodeficiency virus HIV-1NL4.3 in CEM-GFP reporter T and P4 (Hela-CD4-LTR-betaGal) cell lines with a 50% effective concentration (EC50) of 1:20000 dilution and nearly complete (98-99%) inhibition at 1:1000 dilution. It also prevented the entry of HIV-1(IIIB) virus into P4-CCR5 cells (EC50 approximately 1:2492). Two ingredients, Aloe and Amla, inhibited the transduction of human papillomavirus type 16 (HPV-16) pseudovirus in HeLa cells at concentrations far below those that are cytotoxic and those used in the formulation. Basant was found to be totally safe according to pre-clinical toxicology carried out on rabbit vagina after application for 7 consecutive days or twice daily for 3 weeks. Basant has the potential of regressing vulvovaginal candidiasis and preventing N. gonorrhoeae, HIV and HPV infections.

  15. 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.

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

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    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.

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

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    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.

  18. 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.

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

    Science.gov (United States)

    Moreno, Sylvain; Wodniecka, Zofia; Tays, William; Alain, Claude; Bialystok, Ellen

    2014-01-01

    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.

  20. 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.

  1. Transcriptome analysis of phycocyanin inhibitory effects on SKOV-3 cell proliferation.

    Science.gov (United States)

    Ying, Jun; Wang, Jian; Ji, Huijuan; Lin, Chaoqing; Pan, Ruowang; Zhou, Li; Song, Yulong; Zhang, Enyong; Ren, Ping; Chen, Jishun; Liu, Qian; Xu, Teng; Yi, Huiguang; Li, Jinsong; Bao, Qiyu; Hu, Yunliang; Li, Peizhen

    2016-07-01

    Phycocyanin (PC) from Spirulina platensis has inhibitory effects on tumor cell growth. In this research, the transcriptome study was designed to investigate the underlying molecular mechanisms of PC inhibition on human ovarian cancer cell SKOV-3 proliferation. The PC IC50 was 216.6μM and 163.8μM for 24h and 48h exposure, respectively, as determined by CCK-8 assay. The morphological changes of SKOV-3 cells after PC exposure were recorded using HE staining. Cells arrested in G2/M stages as determined by flow cytometry. The transcriptome analysis showed that 2031 genes (with > three-fold differences) were differentially expressed between the untreated and the PC-treated cells, including 1065 up-regulated and 966 down-regulated genes. Gene ontology and KEGG pathway analysis identified 18 classical pathways that were remarkably enriched, such as neurotrophin signaling pathway, VEGF signaling pathway and P53 signaling pathway. qPCR results further showed that PTPN12, S100A2, RPL26, and LAMA3 increased while HNRNPA1P10 decreased in PC-treated cells. Molecules and genes in those pathways may be potential targets to develop treatments for ovarian cancer. Copyright © 2016 Elsevier B.V. All rights reserved.

  2. Inhibitory effect of Eleutherine americana Merr. extract on Staphylococcus aureus isolated from food.

    Science.gov (United States)

    Ifesan, B O T; Hamtasin, C; Mahabusarakam, W; Voravuthikunchai, S P

    2009-01-01

    About 106 samples of ready-to-eat foods were purchased over a period of 3 mo out of which 76 (71.69%) were contaminated with Staphylococcus aureus. S. aureus isolated from the food samples were characterized phenotypically using traditional biochemical methods. Ninety-four percent of the isolates were mannitol fermenters, 86% positive for coagulase test, while 80% produced lipase enzyme. Antibiotic susceptibility test revealed that 21% and 63% of the food isolates were resistant to oxacillin and penicillin, respectively. The antibacterial activity of the bulb of Eleutherine americana used in Thai cuisine was investigated by agar disc diffusion using 2.5 mg of the crude extract and produced inhibition zone between 14.5 and 15.7 mm, while the minimum inhibitory concentration (MIC) value ranged from 0.06 to 1.00 mg/mL on both food isolates and reference strains. Growth curve in the presence of the crude ethanol extract at 4 MIC showed bacteriostatic effect by 5 log reduction relative to the control. Partially purified fractions tentatively identified by column chromatography were suspected to be responsible for the antibacterial property. This study suggests that E. americana bulb has potential for application as a natural preservative in foods.

  3. Inhibitory effects of oral Actinomyces on the proliferation, virulence and biofilm formation of Candida albicans.

    Science.gov (United States)

    Guo, Yiqing; Wei, Changlei; Liu, Chuanxia; Li, Duo; Sun, Jun; Huang, Haiyun; Zhou, Hongmei

    2015-09-01

    The pathogenesis of Candida-associated stomatitis involves the dysfunction of flora antagonistic to Candida. Oral Actinomyces species play an important role in regulating the oral microecological balance. The objective of this study was to investigate the antagonism of three oral Actinomyces against Candida albicans. Suspensions, culture supernatants and bacterial lysates of Actinomyces viscosus, Actinomyces naeslundii and Actinomyces odontolyticus were investigated for their actions upon C. albicans. In addition to a commercial strain, six clinical strains of C. albicans were also tested. The proliferation of C. albicans was assessed using a liquid co-cultivation assay. The adhesion, acid protease and extracellular phospholipase activity, hyphae growth, and biofilm formation of C. albicans were measured. The results showed that the suspensions, culture supernatants and cell lysates of 10(8) colony forming units/ml oral Actinomyces significantly inhibited the proliferation of C. albicans (all PActinomyces have inhibitory effects on the proliferation, adhesion, metabolic enzyme activity, hyphae formation and biofilm development of C. albicans. Copyright © 2015 Elsevier Ltd. All rights reserved.

  4. 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.

  5. [Growth inhibitory effects of lipofectamine-mediated DCC gene on ovarian epithelial carcinoma].

    Science.gov (United States)

    Li, Pei-ling; Hu, Chun-jie; Li, Chang-min; Meng, Chun-yan; Gao, Lei

    2006-03-01

    To study the inhibitory effects of lipofectamine-mediated deleted colorectal carcinoma gene on ovarian epithelial carcinoma (ovarian cancer) cell line SKOV3. We constructed a recombinant eukaryotic expression vector pcDNA3.1 (+)-DCC containing exogenous human DCC cDNA and vector with neomycin resistance gene, which were introduced by lipofectamine-mediated gene transfection into SKOV3 cell line that does not express DCC endogenously, thus forming SKOV3/DCC. Therefore, the experimental cells were classified into SKOV3/DCC, SKOV3/Neo and SKOV3. By using reverse transcriptase-polymerase chain reaction and immunocytochemistry, the expression of DCC mRNA and its protein were examined. Exogenous DCC had successfully been transferred into SKOV3 cells and obtained permanent expression. The growth speed of SKOV3/DCC was slower than the other two groups, there was significant difference between them (P < 0.01). SKOV3/DCC clones number was 38 +/- 8, while SKOV3 and SKOV3/Neo were 192 +/- 8 and 186 +/- 10, respectively, there was significant difference between them (P < 0.01). The percentage of G(1) phase cells increased to 78.0%, which that of S phase decreased to 5.3% by analyzing cell cycle, there was significant difference between them (20.0% and 3.2%, P < 0.01). The ultrastructural changes of the cells were observed under electron microscope, revealing growth retardation. DCC gene played an important role in generation and development of ovarian carcinomas.

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

    Directory of Open Access Journals (Sweden)

    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.

  7. 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.

  8. Inhibitory effect of isoflavones on peroxynitrite-mediated low-density lipoprotein oxidation.

    Science.gov (United States)

    Lai, Hsi-Huai; Yen, Gow-Chin

    2002-01-01

    Peroxynitrite, a potent oxidant formed in vivo from the reaction of nitric oxide with superoxide, can mediate low-density liprotein (LDL) oxidation which is thought to increase the risk of atherosclerosis. This study investigates the inhibitory effect of the isoflavones, genistein and daidzein, together with their glycosidic forms, genistin and daidzin, on the peroxynitrite-mediated LDL oxidation and nitration of tyrosine. Genistein and daidzein were observed to dose-dependently inhibit peroxynitrite-mediated LDL oxidation, while their glucoside conjugates showed less activity. Moreover, all the isoflavones used in this study were found to be potent peroxynitrite scavengers, preventing the nitration of tyrosine. The ability of the isoflavones at 50 microM to decrease the tyrosine nitration induced by peroxynitrite (1 mM) was in the ratios of genistein (49%), daidzein (40%), daidzin (41%) and genistin (42%) when compared to the control (tyrosine incubated only with peroxynitrite). These results suggest that an intake of isoflavones could contribute to protecting against cardiovascular diseases and chronic inflammatory diseases.

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

    Directory of Open Access Journals (Sweden)

    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.

  10. Inhibitory Effect of Furanic and Phenolic Compounds on Exoelectrogenesis in a Microbial Electrolysis Cell Bioanode.

    Science.gov (United States)

    Zeng, Xiaofei; Borole, Abhijeet P; Pavlostathis, Spyros G

    2016-10-18

    The objective of this study was to systematically investigate the inhibitory effect of furfural (FF), 5-hydroxymethylfurfural (HMF), syringic acid (SA), vanillic acid (VA), and 4-hydroxybenzoic acid (HBA), which are problematic lignocellulose-derived byproducts, on exoelectrogenesis in the bioanode of a microbial electrolysis cell. The five compound mixture at an initial total concentration range from 0.8 to 8.0 g/L resulted in an up to 91% current decrease as a result of exoelectrogenesis inhibition; fermentative, nonexoelectrogenic biotransformation pathways of the five compounds were not affected. Furthermore, the parent compounds at a high concentration, as opposed to their biotransformation products, were responsible for the observed inhibition. All five parent compounds contributed to the observed inhibition of the mixture. The IC50 (i.e., concentration resulting in 50% current decrease) of individually tested parent compounds was 2.7 g/L for FF, 3.0 g/L for HMF, 1.9 g/L for SA, 2.1 g/L for VA and 2.0 g/L for HBA. However, the parent compounds, when tested below their respective noninhibitory concentration, jointly resulted in significant inhibition as a mixture. Catechol and phenol, which were persistent biotransformation products, inhibited exoelectrogenesis only at high concentrations, but to a lesser extent than the parent compounds. Exoelectrogenesis recovery from inhibition by all compounds was observed at different rates, with the exception of catechol, which resulted in irreversible inhibition.

  11. New stilbenoids from Pholidota yunnanensis and their inhibitory effects on nitric oxide production.

    Science.gov (United States)

    Guo, Xiao-Yu; Wang, Jue; Wang, Nai-Li; Kitanaka, Susumu; Liu, Hong-Wei; Yao, Xin-Sheng

    2006-01-01

    Six new stilbenoids, a (bibenzyldihydrophenanthrene) ether designated phoyunnanin D (1), a bis(dihydrophenanthrene) ether designated phoyunnanin E (2), and four stilbenes designated phoyunbene A-D (3-6), were isolated from the air-dried whole plant of Pholidota yunnanensis ROLFE. The new compounds were identified as 7-[2-(3-hydroxyphenethyl)-4-hydroxy-6-methoxyphenoxy]-4-hydroxy-2-methoxy-9,10-dihydrophenanthrene (1), 1-[(9,10-dihydro-4-hydroxy-2-methoxy-7-phenanthrenyl)oxy]-4,7-dihydroxy-2-methoxy-9,10-dihydrophenanthrene (2), trans-3,3'-dihydroxy-2',4',5-trimethoxystilbene (3), trans-3,4'-dihydroxy-2',3',5-trimethoxystilbene (4), trans-3,3'-dihydroxy-2',5-dimethoxystilbene (5), and trans-3-hydroxy-2',3',5-trimethoxystilbene (6) based on spectroscopic evidence. Furthermore, the inhibitory effects of compounds 1-6 on nitric oxide production in a murine macrophage-like cell line (RAW 264.7) activated by lipopolysaccharide and interferon-gamma were examined.

  12. 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

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

    Directory of Open Access Journals (Sweden)

    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.

  14. 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.

  15. Inhibitory effect of propylene glycol mannate sulfate on growth of rabbit lens epithelial cells in vitro

    Science.gov (United States)

    Huang, Jin; Xie, Li-Na

    2010-01-01

    AIM To investigate the inhibitory effect of rabbit lens epithelial cell (RLEC) survival and growth by propylene glycol mannate sulfate (PGMS) on the rabbit capsular bag in vitro. METHODS Capsular bags were prepared from rabbit eyes after extracapsular cataract extraction (ECCE) and incubated in 0.2, 0.4, 0.8g/L PGMS in 2, 5, 10 minutes incubation periods. After treatment, the capsular bags were cultured for 7 days in Dulbecco minimum essential medium (DMEM) supplemented with 50mL/L fetal calf serum (FCS). The specimens were examined with light microscopy and transmission electron microscopy (TEM). Capsular bags without receiving PGMS only served as controls. RESULTS PGMS inhibited the proliferation of RLEC in the manner of concentration and time dependent. At the threshold protocol of incubation in PGMS at 0.8g/L for 5 or 10 minutes, proliferative activity of cells were largely arrested and nearly no RLEC was seen on the posterior capsule (P<0.05). Control group had no effect on structure and proliferative activity of RLEC, and the growth proceeded rapidly so that the posterior capsule were totally covered by a confluent monolayer of cell by the end of 7 days. Under TEM, the cells in the control group were tightly arrayed with clearly defined cellular boundary and structure; while cellular deformity and undefined intracellular structure could be seen in the 0.4g/L and 0.8g/L experimental groups. CONCLUSION PGMS can effectively inhibit the proliferation of RLEC. PMID:22553517

  16. 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.

  17. 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

  18. 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.

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

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    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.

  20. Antibacterial Inhibitory Effects ofPunica GranatumGel on Cariogenic Bacteria: Anin vitroStudy.

    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. 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.

  2. 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.

  3. Effect of vancomycin minimal inhibitory concentration on the outcome of methicillin-susceptible Staphylococcus aureus endocarditis.

    Science.gov (United States)

    Cervera, Carlos; Castañeda, Ximena; de la Maria, Cristina Garcia; del Rio, Ana; Moreno, Asunción; Soy, Dolors; Pericas, Juan Manuel; Falces, Carlos; Armero, Yolanda; Almela, Manel; Ninot, Salvador; Pare, Juan Carlos; Mestres, Carlos A; Gatell, Jose M; Marco, Francesc; Miro, Jose M

    2014-06-01

    Staphylococcus aureus endocarditis has a high mortality rate. Vancomycin minimum inhibitory concentration (MIC) has been shown to affect the outcome of methicillin-resistant S. aureus bacteremia, and recent data point to a similar effect on methicillin-susceptible S. aureus bacteremia. We aimed to evaluate the effect of vancomycin MIC on left-sided S. aureus infective endocarditis (IE) treated with cloxacillin. We analyzed a prospectively collected cohort of patients with IE in a single tertiary-care hospital. Vancomycin, daptomycin, and cloxacillin MIC was determined by E-test. S. aureus strains were categorized as low vancomycin MIC (cloxacillin, of whom 53 (57%) had a vancomycin MIC < 1.5 µg/mL and 40 (43%) a vancomycin MIC ≥ 1.5 µg/mL. In-hospital mortality was 30% (n = 16/53) in patients with a low vancomycin MIC and 53% (n = 21/40) in those with a high vancomycin MIC (P = .03). No correlation was found between oxacillin MIC and vancomycin or daptomycin MIC. Logistic regression analysis showed that higher vancomycin MIC increased in-hospital mortality 3-fold (odds ratio, 3.1; 95% confidence interval, 1.2-8.2) after adjustment for age, year of diagnosis, septic complications, and nonseptic complicated endocarditis. Our results indicate that vancomycin MIC could be used to identify a subgroup of patients with methicillin-susceptible S. aureus IE at risk of higher mortality. The worse outcome of staphylococcal infections with a higher vancomycin MIC cannot be explained solely by suboptimal pharmacokinetics of antibiotics. © The Author 2014. Published by Oxford University Press on behalf of the Infectious Diseases Society of America. All rights reserved. For Permissions, please e-mail: journals.permissions@oup.com.

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

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    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.

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

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    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.

  6. The Inhibitory Effects of Aqueous Extract from Guava Twigs, Psidium guajava L., on Mutation and Oxidative Damage

    OpenAIRE

    Zhi-Chyang Kang; Ming-Tsung Yen; Chih-Kwang Chiu; Horng-Cherng Wu; Shu-Ling Huang; Shan-Pao Tai; Bor-Sen Wang

    2013-01-01

    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...

  7. Inhibitory effect of eugenol on seed germination and pre-harvest sprouting of hybrid rice (Oryza sativa L.)

    OpenAIRE

    Hu, Qijuan; Lin, Cheng; Guan, Yajing; Sheteiwy, Mohamed Salah; Hu, Weimin; Hu, Jin

    2017-01-01

    Pre-harvest sprouting (PHS) is a constrain problem in hybrid rice production. The present study was conducted to investigate the inhibitory effect of eugenol on seed germination and PHS of hybrid rice variety (Qian You 1). The results showed that seed germination speed and the activities of ?-amylase were inhibited by eugenol pre-soaking and these effects enhanced with the increasing of eugenol concentrations; while seedling growth was not negatively affected. In field trials, eugenol applica...

  8. Inhibitory effect of Azadirachta indica A. juss leaf extract on the activities of alpha-amylase and alpha-glucosidase.

    Science.gov (United States)

    Kazeem, M I; Dansu, T V; Adeola, S A

    2013-11-01

    In recent decades, there has been a drastic increase in the incidence and prevalence of diabetic mellitus. The aim of this study was to evaluate the in vitro inhibitory effect of Azadirachita indica leaf extract on the activity of alpha-amylase and alpha-glucosidase as a means of alleviating hyperglycemia and managing diabetes mellitus. Aqueous extract of Azadirachita indica exhibited most potent alpha-amylase inhibitory activity with IC50 value of 9.15 mg mL(-1) and acetone extract exhibited most potent alpha-glucosidase inhibitory activity with IC50 value of 5.00 mg mL(-1). Kinetic studies revealed both acetone and aqueous extract to exhibit mixed non-competitive inhibition for alpha-amylase and alpha-glucosidase. It can be concluded that the antidiabetic potential of Azadirachta indica may be due to its ability to inhibit both alpha-amylase and alpha-glucosidase. The presence of phytochemicals such as flavonoids, tannins and saponins in this plant may be responsible for its inhibitory activity on the two enzymes studied.

  9. 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.

  10. 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.

  11. 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

  12. HIV-1 protease inhibitory effects of some selected plants in Caesalpiniaceae and Papilionaceae families

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    Pranee Rattanasuwan

    2003-07-01

    Full Text Available Fifty-two ethanol and water extracts of the plants in Caesalpiniaceae and Papilionaceae families were screened for their HIV-1 protease (HIV-1 PR inhibitory activities using high performance liquid chromatography (HPLC technique. Among the tested extracts, Cassia garrettiana (wood, water extract showed the most potent inhibitory activity against HIV-1 PR, followed by Cassia garrettiana (wood, EtOH extract and Caesalpinia sappan (wood, EtOH extract with IC50 of 18, 32 and 75 μg/ml, respectively. The isolation of active substances against HIV-1 PR of these two plants will be further investigated.

  13. Profound Hypoglycemia with Ecstasy Intoxication

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    Perliveh Carrera

    2015-01-01

    Full Text Available Background. 3,4-Methylenedioxymethamphetamine (MDMA or ecstasy is a synthetic drug that is commonly abused for its stimulant and euphoric effects. Adverse MDMA effects include hyperthermia, psychomotor agitation, hemodynamic compromise, renal failure, hyponatremia, and coma. However, endogenous hyperinsulinemia with severe persistent hypoglycemia has not been reported with MDMA use. Case Report. We report the case of a 29-year-old woman who remained severely hypoglycemic requiring continuous intravenous infusion of high-dose dextrose solutions for more than 24 hours after MDMA intoxication. Serum insulin and C-peptide levels confirmed marked endogenous hyperinsulinemia as the cause of the severe hypoglycemia. Why Should an Emergency Physician Be Aware of This? Immediate and frequent monitoring of blood glucose should be instituted in patients presenting with MDMA ingestion particularly if found to be initially hypoglycemic. Early recognition can help prevent the deleterious effects of untreated hypoglycemia that can add to the morbidity from MDMA use. Clinicians need to be aware of this side effect of MDMA so they can carefully monitor and treat it, especially in patients presenting with altered mental status.

  14. Phenolic acids in some cereal grains and their inhibitory effect on starch liquefaction and saccharification.

    Science.gov (United States)

    Kandil, Amin; Li, Jihong; Vasanthan, Thava; Bressler, David C

    2012-08-29

    The presence of phenolic acids in cereal grain is thought to influence starch hydrolysis during liquefaction and saccharification of grain flours in the bioethanol industry. As a basis for remodeling starch hydrolysis systems and understanding inhibition mechanisms, the composition and concentration of phenolic acids in whole grain flours of triticale, wheat, barley, and corn were analyzed by high-performance liquid chromatography. The total phenolic acid contents (sum of nine phenolic acids) in the four grains were 1.14, 1.70, 0.90, and 1.25 mg/g, respectively, with more than 90% found in the bound form. Ferulic, coumaric, and protocatechuic acids were the major phenolic acids in triticale and wheat. Gallic acid was also rich in triticale. Ferulic, coumaric, hydroxybenzoic, and gallic acids were predominant in barley. In corn, ferulic, coumaric, gallic, and syringic acids were abundant. On the basis of these profiles, pure phenolic acids were added individually and collectively to isolated starches at amounts either equivalent to or 3 times those in the whole grains for hydrolysis. The degree of starch hydrolysis with α-amylase and amyloglucosidase decreased up to 8% when individual phenolic acids were present in cooked starch slurry. The decreases were more pronounced when phenolic acids were added collectively (4-5% with α-amylase and 9-13% with sequential α-amylase and amyloglucosidase). The study of a phenolic acid-starch-enzyme model system indicated that the interactions of phenolic acid-enzyme and phenolic acid-starch significantly contributed to the inhibitory effect of starch hydrolysis. Heating facilitated the interactions. Phenolic acids thus play a significant role in the resistance of starch to enzyme and/or the loss of enzyme activity during starch hydrolysis.

  15. In vitro inhibitory effects of pristimerin on human liver cytochrome P450 enzymes.

    Science.gov (United States)

    Hao, Xiaoyi; Yuan, Jianlei; Xu, Yansen; Wang, Zhao; Hou, Jianzhang; Hu, Tao

    2017-04-07

    1. Pristimerin (PTM) is a biological component isolated from Chinese herbal plant Celastrus and Maytenus spp and it possesses numerous pharmacological activities. However, whether PTM affects the activity of human liver cytochrome P450 (CYP) enzymes remains unclear. 2. In this study, the inhibitory effects of PTM on the eight human liver CYP isoforms (i.e., 1A2, 3A4, 2A6, 2E1, 2D6, 2C9, 2C19, and 2C8) were investigated in vitro using human liver microsomes (HLMs). 3. The results showed that PTM inhibited the activity of CYP1A2, 3A4, and 2C9, with IC50 values of 21.74, 15.88, and 16.58 μM, respectively, but that other CYP isoforms were not affected. Enzyme kinetic studies showed that PTM was not only a non-competitive inhibitor of CYP3A4, but also a competitive inhibitor of CYP1A2 and 2C9, with Ki values of 7.33, 11.60, and 8.09 μM, respectively. In addition, PTM is a time-dependent inhibitor for CYP3A4 with Kinact/KI value of 0.049/11.62 μM-1min-1. 4. The in vitro studies of PTM with CYP isoforms indicate that PTM has the potential to cause pharmacokinetic drug interactions with other co-administered drugs metabolized by CYP1A2, 3A4, and 2C9. Further clinical studies are needed to evaluate the significance of this interaction.

  16. Inhibitory Effect of Bridged Nucleosides on Thermus aquaticus DNA Polymerase and Insight into the Binding Interactions.

    Science.gov (United States)

    Kim, Sung-Kun; Castro, Aaron; Kim, Edward S; Dinkel, Austin P; Liu, Xiaoyun; Castro, Miguel

    2016-01-01

    Modified nucleosides have the potential to inhibit DNA polymerases for the treatment of viral infections and cancer. With the hope of developing potent drug candidates by the modification of the 2',4'-position of the ribose with the inclusion of a bridge, efforts were focused on the inhibition of Taq DNA polymerase using quantitative real time PCR, and the results revealed the significant inhibitory effects of 2',4'-bridged thymidine nucleoside on the polymerase. Study on the mode of inhibition revealed the competitive mechanism with which the 2',4'-bridged thymidine operates. With a Ki value of 9.7 ± 1.1 μM, the 2',4'-bridged thymidine proved to be a very promising inhibitor. Additionally, docking analysis showed that all the nucleosides including 2',4'-bridged thymidine were able to dock in the active site, indicating that the substrate analogs reflect a structural complementarity to the enzyme active site. The analysis also provided evidence that Asp610 was a key binding site for 2',4'-bridged thymidine. Molecular dynamics (MD) simulations were performed to further understand the conformational variations of the binding. The root-mean-square deviation (RMSD) values for the peptide backbone of the enzyme and the nitrogenous base of the inhibitor stabilized within 0.8 and 0.2 ns, respectively. Furthermore, the MD analysis indicates substantial conformational change in the ligand (inhibitor) as the nitrogenous base rotated anticlockwise with respect to the sugar moiety, complemented by the formation of several new hydrogen bonds where Arg587 served as a pivot axis for binding formation. In conclusion, the active site inhibition of Taq DNA polymerase by 2',4'-bridged thymidine suggests the potential of bridged nucleosides as drug candidates.

  17. Inhibitory Effect of Bridged Nucleosides on Thermus aquaticus DNA Polymerase and Insight into the Binding Interactions.

    Directory of Open Access Journals (Sweden)

    Sung-Kun Kim

    Full Text Available Modified nucleosides have the potential to inhibit DNA polymerases for the treatment of viral infections and cancer. With the hope of developing potent drug candidates by the modification of the 2',4'-position of the ribose with the inclusion of a bridge, efforts were focused on the inhibition of Taq DNA polymerase using quantitative real time PCR, and the results revealed the significant inhibitory effects of 2',4'-bridged thymidine nucleoside on the polymerase. Study on the mode of inhibition revealed the competitive mechanism with which the 2',4'-bridged thymidine operates. With a Ki value of 9.7 ± 1.1 μM, the 2',4'-bridged thymidine proved to be a very promising inhibitor. Additionally, docking analysis showed that all the nucleosides including 2',4'-bridged thymidine were able to dock in the active site, indicating that the substrate analogs reflect a structural complementarity to the enzyme active site. The analysis also provided evidence that Asp610 was a key binding site for 2',4'-bridged thymidine. Molecular dynamics (MD simulations were performed to further understand the conformational variations of the binding. The root-mean-square deviation (RMSD values for the peptide backbone of the enzyme and the nitrogenous base of the inhibitor stabilized within 0.8 and 0.2 ns, respectively. Furthermore, the MD analysis indicates substantial conformational change in the ligand (inhibitor as the nitrogenous base rotated anticlockwise with respect to the sugar moiety, complemented by the formation of several new hydrogen bonds where Arg587 served as a pivot axis for binding formation. In conclusion, the active site inhibition of Taq DNA polymerase by 2',4'-bridged thymidine suggests the potential of bridged nucleosides as drug candidates.

  18. Investigation of the inhibitory effects of various drugs on the hepatic uptake of fexofenadine in humans.

    Science.gov (United States)

    Matsushima, Soichiro; Maeda, Kazuya; Ishiguro, Naoki; Igarashi, Takashi; Sugiyama, Yuichi

    2008-04-01

    Fexofenadine (FEX), an H(1)-receptor antagonist, is eliminated from the liver mainly in an unchanged form. Our previous study suggested that organic anion-transporting polypeptide (OATP) 1B3 contributes mainly to the hepatic uptake of FEX. On the other hand, a clinical report demonstrated that a T521C mutation of OATP1B1 increased its plasma area under the plasma concentration-time curve. Several compounds are reported to have a drug interaction with FEX, and some of this may be caused by the inhibition of its hepatic uptake. We determined which transporters are involved in the hepatobiliary transport of FEX by using double transfectants and examined whether clinically reported drug interactions with FEX could be explained by the inhibition of its hepatic uptake. Vectorial basal-to-apical transport of FEX was observed in double transfectants expressing OATP1B1/multidrug resistance-associated protein 2 (MRP2) and OATP1B3/MRP2, suggesting that OATP1B1 as well as OATP1B3 is involved in the hepatic uptake of FEX and that MRP2 can recognize FEX as a substrate. The inhibitory effects of compounds on FEX uptake in OATP1B3-expressing HEK293 cells were investigated, and the maximal degree of increase in plasma AUC of FEX by drug interaction in clinical situations was estimated. As a result, cyclosporin A and rifampicin were found to have the potential to interact with OATP1B3-mediated uptake at clinical concentrations. From these results, most of the reported drug interaction cannot be explained by the inhibition of hepatic uptake of FEX, and different mechanisms such as the inhibition of intestinal efflux should be considered.

  19. 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

  20. Study on the inhibitory effect of allicin on human gastric cancer cell line SGC-7901 and its mechanism.

    Science.gov (United States)

    Tao, Mei; Gao, Linghan; Pan, Jie; Wang, Xiaoye

    2014-01-01

    Allicin is the main active constituent of Allium sativum L., which is characterized by broad antibacterial spectrum (MarkosN et al., 2008; Chen et al., 2008); it also has apparent inhibitory effects on a variety of tumors. The Objective of the paper is to study the inhibitory effect of allicin on human gastric cancer cell line SGC-7901. MTT assay and flow cytometry technique were applied to determine the inhibition rate of allicin on human gastric cancer cell line SGC-7901. The results shows that different concentrations of allicin apparently inhibited the gastric cancer SGC7901 cells, cell growth inhibition rates in the experimental groups showed an upward trend with increased allicin concentration, which were concentration-dependent. Flow cytometry results found that the cell cycle was arrested in the G2/M phase. Allicin has an apparent inhibitory effect on proliferation of gastric cancer cells, and can induce their apoptosis. Compared with other chemotherapeutic drugs, allicin's anti-tumor effect is better; and toxic and side effects are relatively small.

  1. Inhibitory effects of Chinese nutritional herbs in isogenic breast carcinoma cells with modulated estrogen receptor function.

    Science.gov (United States)

    Telang, Nitin; Li, Guo; Katdare, Meena; Sepkovic, Daniel; Bradlow, Leon; Wong, George

    2016-11-01

    In estrogen receptor (ER)+ MCF-7 cells, ER represents a ligand-activated transcription factor, and 17β-estradiol (E2) represents its physiological ligand. Maintenance of the human breast carcinoma-derived MCF-7 cells with 0.7% serum selected a proliferative sub-population of E2-responsive cells with transiently non-functional ER due to limited availability of E2. Culture of MCF-7 cells in the presence of either 0.7% serum, herbs on ER-NF and ER-F cells identified the inhibitory concentration (IC)50 values for these herbs, while the IC50 ratios for the ER-NF:ER-F phenotypes facilitated their rank ordering in terms of efficacy. Out of the 11 efficacious herbs tested, five herbs exhibited ER-F > ER-NF inhibitory activity, four exhibited ER-F = ER-NF inhibitory activity and two exhibited ER-NF > ER-F inhibitory activity. Extracts from representative herbs, Lycium barbarum bark, Epimedium grandiflorum and Cornus officinalis, from each of the three groups inhibited anchorage-independent growth, induced G1 or G2/M arrest and/or apoptosis, and generated anti-proliferative E2 metabolites. The differential growth inhibition in ER-NF and ER-F phenotypes, together with the mechanistic efficacy of representative herbs, identified potential leads for their efficacy on ER+ and/or ER- breast cancer.

  2. [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.

  3. 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.

  4. 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

  5. Inhibitory effect of the recombinant Phoneutria nigriventer Tx1 toxin on voltage-gated sodium channels.

    Science.gov (United States)

    Silva, Anita O; Peigneur, Steve; Diniz, Marcelo R V; Tytgat, Jan; Beirão, Paulo S L

    2012-12-01

    Phoneutria nigriventer toxin Tx1 (PnTx1, also referred to in the literature as Tx1) exerts inhibitory effect on neuronal (Na(V)1.2) sodium channels in a way dependent on the holding potential, and competes with μ-conotoxins but not with tetrodotoxin for their binding sites. In the present study we investigated the electrophysiological properties of the recombinant toxin (rPnTx1), which has the complete amino acid sequence of the natural toxin with 3 additional residues: AM on the N-terminal and G on the C-terminal. At the concentration of 1.5 μM, the recombinant toxin inhibits Na(+) currents of dorsal root ganglia neurons (38.4 ± 6.1% inhibition at -80 mV holding potential) and tetrodotoxin-resistant Na(+) currents (26.2 ± 4.9% at the same holding potential). At -50 mV holding potential the inhibition of the total current reached 71.3 ± 2.3% with 1.5 μM rPnTx1. The selectivity of rPnTx1 was investigated on ten different isoforms of voltage-gated sodium channels expressed in Xenopus oocytes. The order of potency for rPnTx1 was: rNa(V)1.2 > rNa(V)1.7 ≈ rNa(V)1.4 ≥ rNa(V)1.3 > mNa(V)1.6 ≥ hNa(V)1.8. No effect was seen on hNa(V)1.5 and on the arthropods isoforms (DmNa(V)1, BGNa(V)1.1a and VdNa(V)1). The IC(50) for Na(V)1.2 was 33.7 ± 2.9 nM with a maximum inhibition of 83.3 ± 1.9%. The toxin did not alter the voltage-dependence of channel gating and was effective on Na(V)1.2 channels devoid of inactivation. It was ineffective on neuronal calcium channels. We conclude that rPnTx1 has a promising selectivity, and that it may be a valuable model to achieve pharmacological activities of interest for the treatment of channelopathies and neuropathic pain. Copyright © 2012 Elsevier Masson SAS. All rights reserved.

  6. [Inhibitory effect of quercetin on the biofilm formation of Streptococcus mutans].

    Science.gov (United States)

    Yue, J X; Yang, H Y; Han, L; Zhu, M Y; Song, F F; Huang, C

    2016-06-01

    To observe the inhibitory effect of quercetin on the biofilm formation of Streptococcus mutans(Sm), to preliminarily reveal the possible underlying mechanisms, and to evaluate the cytotoxicity of quercetion to human dental pulp cells so as to provide the theoretical basis for the application of quercetin in oral biomaterials. Quercetin storage solution was diluted to 0, 3.125, 6.25, 12.5, 25, 50, 100, 200, 400 and 800 mg/L, and added into Sm medium for 4 h and 24 h, crystal violet staining was used to evaluate the biofilm volume. In subsequent detections, three groups were set: control(0 mg/L), 200 mg/L quercetin and 400 mg/L quercetin. Confocal laser scanning microscopy was used to observe the morphology of the biofilm; qPCR for gtfB, gtfC, comD, comE, and luxS were assessed to preliminarily investigate the mechanisms. Finally, the methyl thiazolyl tetrazolium(MTT)test using human dental pulp cells was used to investigate cytotoxicity. Quercetin could significantly inhibit up to(86.16±0.45)% of the biofilm formation of Sm(Compared with the control group P=0.00)and effectively removed(43.04±0.53)% of the mature biofilm(Compared with the control group P=0.00). Confocal laser scanning microscopy photographs showed that after co-incubated for 24 h, the dense biofilm structures of the experimental group were destroyed by quercetin both at 200 mg/L and 400 mg/L. Quercetin suppressedover 50% of the expression of gtfB, gtfC, comD, comE(compared with the control group P<0.05)and promoted the expression of luxS up to 2.18 ± 0.24 and 2.84 ± 0.26 after 4 h and 24 h, respectively(compared with the control group P<0.05). Quercetin also exhibited acceptable compatibility for human dental pulp cells. Quercetin could effectively reduce the biofilm formation of Sm by inhibiting the expression of the related genes, and exhibited no cytotoxicity for human dental pulp cells. Quercetin has good potential to be applied in oral biological materials.

  7. In Vitro Inhibitory Effects of Cyandin-3-rutinoside on Pancreatic α-Amylase and Its Combined Effect with Acarbose

    Directory of Open Access Journals (Sweden)

    Sarinya Akkarachiyasit

    2011-03-01

    Full Text Available The inhibitory activity on pancreatic α-amylase by cyanidin-3-rutinoside was examined in vitro. The IC50 value of cyanidin-3-rutinoside against pancreatic α-amylase was 24.4 ± 0.1 μM. The kinetic analysis revealed that pancreatic α-amylase was inhibited by cyanidin-3-rutinoside in a non-competitive manner. The additive inhibition of a combination of cyanidin-3-rutinoside with acarbose against pancreatic α-amylase was also found. These results provide the first evidence for the effect of cyanidin-3-rutinoside in a retarded absorption of carbohydrates by inhibition of pancreatic α-amylase which may be useful as a potential inhibitor for prevention and treatment of diabetes mellitus.

  8. Inhibitory effect of essential oils obtained from plants grown in Colombia on yellow fever virus replication in vitro

    OpenAIRE

    Martínez Jairo R; Ocazionez Raquel E; Meneses Rocío; Stashenko Elena E

    2009-01-01

    Abstract Background An antiviral drug is needed for the treatment of patients suffering from yellow fever. Several compounds present in plants can inactive in vitro a wide spectrum of animal viruses. Aim In the present study the inhibitory effect of essential oils of Lippia alba, Lippia origanoides, Oreganum vulgare and Artemisia vulgaris on yellow fever virus (YFV) replication was investigated. Methods The cytotoxicity (CC50) on Vero cells was evaluated by the MTT reduction method. The minim...

  9. QUANTITATVE ANALYSIS OF PUNGENT COMPONENTS DURING THE RED PEPPER GROWTH AND VERIFICATION OF ITS INHIBITORY EFFECTS ON PLANT PATHOGENS

    OpenAIRE

    渡辺, 信平

    2016-01-01

    Red peppers are very popular seasonings in the world because of their strong pungency. The pungent components, named apsaicinoids, are said to have a strong antibiological activity, as well. In this study, I quantified the amount of capsaicinoids during the growth of chili pepper (Capsicum annuum) and examined their inhibitory effects on the growth of plant pathogens. Capsaicinoids has been shown to accumulate in placenta mostly 30 to 40 days after flowering, which was accompanied by indu...

  10. Strong inhibitory effect of pre-eclampsia serum on angiogenesis detected in vitro by human cell-based angiogenesis tests.

    Science.gov (United States)

    Virtanen, Anita; Toimela, Tarja; Tihtonen, Kati; Sarkanen, Jertta-Riina; Huttala, Outi; Heinonen, Tuula; Uotila, Jukka

    2016-10-01

    To explore in vitro angiogenic properties of maternal and umbilical cord blood sera from women with symptomatic pre-eclampsia in comparison with sera from women with normotensive pregnancies. Maternal and umbilical blood serum samples were collected from eleven primiparous women with pre-eclampsia and ten healthy gestational-age-matched primiparous controls. The samples were tested for tubule formation in two different types of in vitro angiogenesis tests. The first test (fibroblast-HUVEC) showed effects on angiogenesis and the second test (hASC-HUVEC), in addition to angiogenesis, also showed effects on vasculogenesis. The pro-angiogenic and inhibitory properties of the samples were microscopically quantified after immunostaining tubular structures, using markers for von Willebrand factor (vWf) and collagen IV. Serum samples from pre-eclamptic women inhibited tubule formation in both models, while those from normal pregnancy didn't. Umbilical blood samples were inhibitory both after pre-eclampsia and normal pregnancy. In the fibroblast-HUVEC model the inhibition was stronger after preeclampsia pregnancy, and the difference between groups was statistically significant. In the pre-eclampsia group a correlation between the inhibitory effect of umbilical blood and birth weight adjusted to gestational age was found. No clear correlation between sera from pregnant women and corresponding umbilical sera was found. The strong inhibitory effect of maternal serum samples on tubule formation reflects the anti-angiogenic state that is present in pre-eclampsia. Copyright © 2016 International Society for the Study of Hypertension in Pregnancy. Published by Elsevier B.V. All rights reserved.

  11. 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.

  12. [The relationship between inhibitory effect of xuanfuguilian prescription on the growth of esophageal cells ECA9706 and its components].

    Science.gov (United States)

    Ma, Jun-Hua; Chen, Yu-Long; Wang, Hai-Bo; Yin, Su-Gai; Wu, Yao-Song

    2013-02-01

    To discuss the relationship between inhibitory effect of different concentration ethanol extracts from Xuanfuguilian prescription on the growth of esophageal cells ECA9706 and its components. The drug was extracted with anhydrous ethanol, 95%, 85%, 75%, 50%, 25% ethanol or water, the cell proliferation inhibitory rate of different solvent extracts were detected with MTT assay, and IC50 was calculated. The components of the drug were determined by LC/MS. Based on the inhibitory rate and the components peak area, the samples were hierarchy clustered respectively. The correlation of components peak area and inhibition rate was analyzed with Pearson Correlation. The components peak area and inhibition rate were analyzed using PLS. The IC50 of the 7 extracts on esophageal carcinoma cell ECA9706 were respectively 46.361, 52.67, 58.11, 78.26, 93.10, 2579.43 and 3953.34 microg/ mL 22 stable peaks were determined by LC-MS. Based on the inhibition rate and the components peak area, the clustering results of the two samples were similar. The 10 peaks areaes were closely related to inhibition rate (P ethanol have different effects, and their curative effects are closely related to components.

  13. [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/m2×5 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 P15INK4B 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/m2×5 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/m2×5 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 G1 phase increased notably, while cells in S phase decreased significantly. Also, the P15INK4B 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 G1 phase and induce the apoptosis at low concentration (0.1-0.2 µg/ml).

  14. 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 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.

  15. 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.

  16. 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.

  17. Effects of emotional reactivity on inhibitory avoidance in the elevated T-maze

    Directory of Open Access Journals (Sweden)

    C. Conde

    2000-02-01

    Full Text Available The possibility of the presence of inter-individual emotional differences and the memory performance of rats was examined in the elevated T-maze. Two kinds of aversively motivated behaviors, inhibitory avoidance and escape learning, were measured. Based on the number of trials to achieve a learning criterion, rats were divided into two subgroups with either low or high avoidance reactivity (LAR or HAR, respectively. Retention test avoidance latencies showed that HAR animals had better avoidance memory (Mann-Whitney rank sum test, P = 0.0035. No such differences were found for the escape component of this test. These data suggest that individual emotional differences affect inhibitory avoidance performance, which may help to explain the dispersion of the data observed in other studies using this paradigm.

  18. 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.

  19. 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.

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

    OpenAIRE

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

    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...

  1. Modelling inhibitory effects of long chain fatty acids in the anaerobic digestion process

    OpenAIRE

    Flotats Ripoll, Xavier

    2013-01-01

    Mathematical modelling of anaerobic digestion process has been used to give new insights regarding dynamics of the long chain fatty acids (LCFA) inhibition. Previously published experimental data, including batch tests with clay mineral bentonite additions, were used for parameter identification. New kinetics were considered to describe the bio-physics of the inhibitory process, including: i) adsorption of LCFA over granular biomass and ii) specific LCFA substrate (saturated/unsaturated) a...

  2. Inhibitory effect of isoprenoid-substituted flavonoids isolated from Artocarpus heterophyllus on melanin biosynthesis.

    Science.gov (United States)

    Arung, Enos Tangke; Shimizu, Kuniyoshi; Kondo, Ryuichiro

    2006-07-01

    Isoprenoid-substituted flavonoids were isolated from the wood of Artocarpus heterophyllus by means of activity-guided fractionation. Artocarpin (1), cudraflavone C (2), 6-prenylapigenin (3), kuwanon C (4), norartocarpin (5) and albanin A (6) inhibited melanin biosynthesis in B16 melanoma cells without inhibiting tyrosinase. A structure-activity investigation indicated that the presence of the isoprenoid-substituted moiety enhanced the inhibitory activity on melanin production in B16 melanoma cells.

  3. Evaluation of inhibitory effect and apoptosis induction of Zyzyphus Jujube on tumor cell lines, an in vitro preliminary study

    OpenAIRE

    Vahedi, Fatemeh; Fathi Najafi, Mohsen; Bozari, Kazem

    2008-01-01

    In the present study, water extract of dried fruit of Zyzyphus Jujube was tested for its possible anticancer effect and induction of apoptosis on human tumor cell lines, HEp-2, HeLa and Jurkat cell lines. The inhibitory effect of water extract of this fruit on cell proliferation was assessed by MTT colorimetric assay. The induction of apoptosis of this extract was analyzed by DNA fragmentation analysis. Zyzyphus Jujube extract showed inhibitory effects on mentioned cell lines. Jurkat leukemic...

  4. 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.

  5. Profound thrombocytopenia after primary exposure to eptifibatide

    Directory of Open Access Journals (Sweden)

    Nicholas B Norgard

    2010-09-01

    Full Text Available Nicholas B Norgard, Brian T BadgleyUniversity at Buffalo, School of Pharmacy and Pharmaceutical Sciences, Buffalo, NY, USAAbstract: Eptifibatide is a glycoprotein IIb/IIIa receptor antagonist used to reduce the incidence of ischemic events in patients with acute coronary syndromes and those undergoing percutaneous coronary intervention. A minority of patients given eptifibatide develop acute, profound thrombocytopenia (<20,000 cells/mm3 within a few hours of receiving the drug. This case report discusses a patient who developed profound thrombocytopenia within hours of receiving eptifibatide for the first time. The Naranjo algorithm classified the likelihood that this patient’s thrombocytopenia was related to eptifibatide as probable. Profound thrombocytopenia is an uncommon but clinically important complication of eptifibatide. This case report emphasizes the importance of monitoring platelet counts routinely at baseline and within 2–6 hours of eptifibatide administration.Keywords: drug-induced thrombocytopenia, glycoprotein IIb/IIIa antagonists, eptifibatide, thrombocytopenia

  6. 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.

  7. Profound thrombocytopenia after primary exposure to eptifibatide.

    Science.gov (United States)

    Norgard, Nicholas B; Badgley, Brian T

    2010-01-01

    Eptifibatide is a glycoprotein IIb/IIIa receptor antagonist used to reduce the incidence of ischemic events in patients with acute coronary syndromes and those undergoing percutaneous coronary intervention. A minority of patients given eptifibatide develop acute, profound thrombocytopenia (eptifibatide for the first time. The Naranjo algorithm classified the likelihood that this patient's thrombocytopenia was related to eptifibatide as probable. Profound thrombocytopenia is an uncommon but clinically important complication of eptifibatide. This case report emphasizes the importance of monitoring platelet counts routinely at baseline and within 2-6 hours of eptifibatide administration.

  8. Glycolic acid chemical peeling improves inflammatory acne eruptions through its inhibitory and bactericidal effects on Propionibacterium acnes.

    Science.gov (United States)

    Takenaka, Yuko; Hayashi, Nobukazu; Takeda, Mikiko; Ashikaga, Sayaka; Kawashima, Makoto

    2012-04-01

    Glycolic acid chemical peeling is effective for treating comedones, and some clinical data show that it also improves inflammatory eruptions. The purpose of this study was to identify the mechanism of glycolic acid chemical peeling to improve inflammatory acne. To assess growth inhibitory and bactericidal effects of glycolic acid on Propionibacterium acnes in vitro, we used an agar diffusion method and a time-kill method. To reveal bactericidal effects in vivo, we established an agar-attached method which correlated well with the ordinary swab-wash method, and we used the agar-attached method to compare the numbers of propionibacteria on the cheek treated with glycolic acid chemical peeling. Our results show that 30% glycolic acid (at pH 1.5, 3.5 and 5.5) formed growth inhibitory circles in the agar diffusion method, but the diameters of those circles were smaller than with 1% nadifloxacin lotion or 1% clindamycin gel. In the time-kill method, 30% glycolic acid (at pH 1.5 and 3.5) or 1% nadifloxacin lotion reduced the number of P. acnes to less than 100 CFU/mL within 5 min. In contrast, in 30% glycolic acid (at pH 5.5) or in 1% clindamycin gel, P. acnes survived for more than 4 h. Chemical peeling with 35% glycolic acid (at pH 1.2) decreased the number of propionibacteria on the cheeks of patients compared with untreated controls (P glycolic acid has moderate growth inhibitory and bactericidal effects on P. acnes, and that chemical peeling with glycolic acid works on inflammatory acne via those effects. © 2011 Japanese Dermatological Association.

  9. 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 rewarding stimulus to obtain a larger delayed reward, and during inhibition of neutral stimuli. Group differences in brain activity were not significant in the 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.

  10. Postantibiotic effect and postantibiotic sub-minimum inhibitory concentration effect of valnemulin against Staphylococcus aureus isolates from swine and chickens.

    Science.gov (United States)

    Zhao, D H; Yu, Y; Zhou, Y F; Shi, W; Deng, H; Liu, Y H

    2014-02-01

    The postantibiotic effect (PAE) and postantibiotic sub-minimum inhibitory concentration (MIC) effect (PA-SME) of valnemulin against Staphylococcus aureus were investigated in vitro using a spectrophotometric technique and classic viable count method. A standard curve was constructed by regression analysis of the number of colonies and the corresponding optical density (OD) at 630 nm of the inoculum. After exposure to valnemulin at different concentrations for an hour, the antibiotic was removed by centrifuging and washing. The PA-SMEs were measured after initial exposure to valnemulin at 4 × the MIC, and then, valnemulin was added to reach corresponding desired concentrations in the resuspended culture. Samples were collected hourly until the culture became turbid. The results were calculated by converting the OD values into the counts of bacteria in accordance with the curve. The MIC of valnemulin against eight strains was identically 0.125 μg ml(-1) . The mean PAEs were 2.12 h (1 × MIC) and 5.06 h (4 × MIC), and the mean PA-SMEs were 6.85 h (0.1 × MIC), 9.12 h (0.2 × MIC) and 10.8 h (0.3 × MIC). The results showed that the strains with identical MICs exhibited different PAEs and PA-SMEs. Valnemulin produced prolonged PAE and PA-SME periods for Staph. aureus, supporting a longer dosing interval while formulating a daily administration dosage. In this study, valnemulin demonstrated prolonged postantibiotic effects and postantibiotic sub-MIC effects on strains of Staphylococcus aureus. The strains with identical MICs of valnemulin exhibited different PAEs and PA-SMEs. Staphylococcus aureus isolated from different species has little impact on the postantibiotic effect of valnemulin. The result suggests a longer dosing interval while formulating a daily administration dosage, and it may play a valuable role of valnemulin in treating Staph. aureus infections in animals. © 2013 The Society for Applied Microbiology.

  11. Litter Decomposition in a Semiarid Dune Grassland: Neutral Effect of Water Supply and Inhibitory Effect of Nitrogen Addition.

    Directory of Open Access Journals (Sweden)

    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

  12. Litter Decomposition in a Semiarid Dune Grassland: Neutral Effect of Water Supply and Inhibitory Effect of Nitrogen Addition.

    Science.gov (United States)

    Li, Yulin; Ning, Zhiying; Cui, Duo; Mao, Wei; Bi, Jingdong; Zhao, Xueyong

    2016-01-01

    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 should be considered

  13. Curcumin synergistically potentiates the growth-inhibitory and pro-apoptotic effects of celecoxib in osteoarthritis synovial adherent cells.

    Science.gov (United States)

    Lev-Ari, S; Strier, L; Kazanov, D; Elkayam, O; Lichtenberg, D; Caspi, D; Arber, N

    2006-02-01

    Osteoarthritis (OA) is the Western world's leading cause of disability. Cyclo-oxygenase-2 (COX-2) inhibitors are efficient anti-inflammatory agents commonly used in the treatment of osteoarthritis. However, recent studies have shown that their long-term use may be limited due to cardiovascular toxicity. The anti-inflammatory efficacy of the phytochemical curcumin has been demonstrated in several in vitro and animal models. This study was undertaken to investigate whether curcumin augments the growth-inhibitory and pro-apoptotic effects of celecoxib in OA synovial adherent cells. OA synovial adherent cells were prepared from human synovial tissue collected during total knee replacement surgery. The cells were exposed to different concentrations of celecoxib (0-40 mum), curcumin (0-20 mum) and their combination. Flow cytometric analysis was used to measure the percentage of cells with a subdiploid DNA content, the hallmark of apoptosis. COX-2 activity was assessed by measuring production of prostaglandin E(2) by enzyme-linked immunoassay. A synergistic effect was observed in inhibition of cell growth when the cells were exposed to various concentrations of celecoxib combined with curcumin. The inhibitory effect of the combination on cell growth was associated with an increased induction of apoptosis. The synergistic effect was mediated through a mechanism that involves inhibition of COX-2 activity. This effect may enable the use of celecoxib at lower and safer concentrations, and may pave the way for a novel combination treatment in osteoarthritis and other rheumatological disorders.

  14. Hypocholesterolemic Effect and In Vitro Pancreatic Lipase Inhibitory Activity of an Opuntia ficus-indica Extract

    Directory of Open Access Journals (Sweden)

    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.

  15. Hypocholesterolemic Effect and In Vitro Pancreatic Lipase Inhibitory Activity of an Opuntia ficus-indica Extract.

    Science.gov (United States)

    Padilla-Camberos, Eduardo; Flores-Fernandez, Jose Miguel; Fernandez-Flores, Ofelia; Gutierrez-Mercado, Yanet; Carmona-de la Luz, Joel; Sandoval-Salas, Fabiola; Mendez-Carreto, Carlos; Allen, Kirk

    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.

  16. 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...

  17. In vitro α-amylase inhibitory activity and in vivo hypoglycemic effect of methanol extract of Citrus macroptera Montr. fruit.

    Science.gov (United States)

    Uddin, Nizam; Hasan, Md Rakib; Hossain, Md Monir; Sarker, Arjyabrata; Hasan, A H M Nazmul; Islam, A F M Mahmudul; Chowdhury, Mohd Motaher H; Rana, Md Sohel

    2014-06-01

    To investigate the therapeutic effects of methanol extract of Citrus macroptera Montr.fruit in α-amylase inhibitory activity (in vitro) and hypoglycemic activity in normal and glucose induced hyperglycemic rats (in vivo). Fruits of Citrus macroptera without rind was extracted with pure methanol following cold extraction and tested for presence of phytochemical constituents, α-amylase inhibitory activity, and hypoglycemic effect in normal rats and glucose induced hyperglycemic rats. Presence of saponin, steroid and terpenoid were identified in the extract. The results showed that fruit extract had moderate α-amylase inhibitory activity [IC50 value=(3.638±0.190) mg/mL] as compared to acarbose. Moreover at 500 mg/kg and 1 000 mg/kg doses fruit extract significantly (P<0.05 and P<0.01 respectively) reduced fasting blood glucose level in normal rats as compared to glibenclamide (5 mg/kg). In oral glucose tolerance test, 500 mg/kg dose significantly reduced blood glucose level (P<0.05) at 2 h but 1 000 mg/kg dose significantly reduced blood glucose level at 2 h and 3 h (P<0.05 and P<0.01 respectively) whereas glibenclamide (5 mg/kg) significantly reduced glucose level at every hour after administration. Overall time effect is also considered extremely significant with F value=23.83 and P value=0.0001 in oral glucose tolerance test. These findings suggest that the plant may be a potential source for the development of new oral hypoglycemic agent.

  18. The Inhibitory Effects of 2 Commercial Probiotic Strains on the Growth of Staphylococcus aureus and Gene Expression of Enterotoxin A

    Directory of Open Access Journals (Sweden)

    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.

  19. The inhibitory effects of quercetin on obesity and obesity-induced inflammation by regulation of MAPK signaling.

    Science.gov (United States)

    Seo, Min-Jung; Lee, Yeon-Joo; Hwang, Ji-Hyun; Kim, Kui-Jin; Lee, Boo-Yong

    2015-11-01

    Quercetin is a flavonoid found in fruits, vegetables, leaves and grains. It has inhibitory, antiviral, antiasthma, anticancer and antiinflammatory effects. Research has suggested that obesity is linked to metabolic disorders. In this study, we examined the inhibitory effect of quercetin on lipid accumulation and obesity-induced inflammation using 3T3-L1, RAW264.7, zebrafish and mouse models. Quercetin suppressed protein levels of the key adipogenic factors C/EBPβ, C/EBPα, PPARγ and FABP4 and the TG-synthesis enzymes lipin1, DGAT1 and LPAATθ. Activation of m-TOR and p70S6K, which are related to insulin and adipogenesis, was down-regulated during adipogenesis in 3T3-L1 cells. Recent research suggested that MAPK signaling factors were involved in adipogenesis and inflammation and that the adipokines MCP-1 and TNF-α attracted macrophages into adipose tissue. Our data showed that quercetin inhibited the MAPK signaling factors ERK1/2, JNK and p38MAPK and MCP-1 and TNF-α in adipocytes and macrophages. Quercetin also inhibited secretion of the inflammatory cytokines IL-1β and IL-6 and stimulated that of IL-10, an antiinflammatory cytokine. In this study, we confirmed the inhibitory effects of quercetin in adipogenesis and inflammation using a mouse model. In mice, quercetin reduced body weight (almost 40%) and suppressed expression of adipogenic, lipogenic and inflammation-related cytokines. Our data demonstrated that quercetin inhibits lipid accumulation and obesity-induced inflammation in the cell and animal models. Our study suggested that quercetin may represent a potential therapeutic agent for other metabolic disorders by regulating obesity and obesity-induced inflammation. Copyright © 2015 Elsevier Inc. All rights reserved.

  20. The inhibitory effects of bupivacaine, levobupivacaine, and ropivacaine on K2P (two-pore domain potassium) channel TREK-1.

    Science.gov (United States)

    Shin, Hye Won; Soh, Jeong Seop; Kim, Hee Zoo; Hong, Jinpyo; Woo, Dong Ho; Heo, Jun Young; Hwang, Eun Mi; Park, Jae-Yong; Lee, C Justin

    2014-02-01

    Bupivacaine, levobupivacaine, and ropivacaine are amide local anesthetics. Levobupivacaine and ropivacaine are stereoisomers of bupivacaine and were developed to circumvent the bupivacaine's severe toxicity. The recently characterized background potassium channel, K(2P) TREK-1, is a well-known target for various local anesthetics. The purpose of study is to investigate the differences in inhibitory potency and stereoselectivity among bupivacaine, levobupivacaine, and ropivacaine on K(2P) TREK-1 channels overexpressed in COS-7 cells. We investigated the effects of bupivacaine, levobupivacaine, and ropivacaine (10, 50, 100, 200, and 400 μM) on TREK-1 channels expressed in COS-7 cells by using the whole cell patch clamp technique with a voltage ramp protocol ranging from -100 to 100 mV for 200 ms from a holding potential of -70 mV. Bupivacaine, levobupivacaine, and ropivacaine showed reversible inhibition of TREK-1 channels in a concentration-dependent manner. The half-maximal inhibitory concentrations (IC(50)) of bupivacaine, levobupivacaine, and ropivacaine were 95.4 ± 14.6, 126.1 ± 24.5, and 402.7 ± 31.8 μM, respectively. IC(50) values indicated a rank order of potency (bupivacaine > levobupivacaine > ropivacaine) with stereoselectivity. Hill coefficients were 0.84, 0.93, and 0.89 for bupivacaine, levobupivacaine, and ropivacaine, respectively. Inhibitory effects on TREK-1 channels by bupivacaine, levobupivacaine, and ropivacaine demonstrated stereoselectivity: bupivacaine was more potent than levobupivacaine and ropivacaine. Inhibition of TREK-1 channels and consecutive depolarization of the cell membrane by bupivacaine, levobupivacaine, and ropivacaine may contribute to the blockade of neuronal conduction and side effects.

  1. General and Food-Specific Inhibitory Control As Moderators of the Effects of the Impulsive Systems on Food Choices

    Directory of Open Access Journals (Sweden)

    Xuemeng Zhang

    2017-05-01

    Full Text Available The present study aimed to extend the application of the reflective-impulsive model to restrained eating and explore the effect of automatic attention (impulsive system on food choices. Furthermore, we examined the moderating effects of general inhibitory control (G-IC and food-specific inhibitory control (F-IC on successful and unsuccessful restrained eaters (US-REs. Automatic attention was measured using “the EyeLink 1000,” which tracked eye movements during the process of making food choices, and G-IC and F-IC were measured using the Stop-Signal Task. The results showed that food choices were related to automatic attention and that G-IC and F-IC moderated the predictive relationship between automatic attention and food choices. Furthermore, among successful restrained eaters (S-REs, automatic attention to high caloric foods did not predict food choices, regardless of whether G-IC or F-IC was high or low. Whereas food choice was positively correlated with automatic attention among US-REs with poor F-IC, this pattern was not observed in those with poor G-IC. In conclusion, the S-REs had more effective self-management skills and their food choices were affected less by automatic attention and inhibitory control. Unsuccessful restrained eating was associated with poor F-IC (not G-IC and greater automatic attention to high caloric foods. Thus, clinical interventions should focus on enhancing F-IC, not G-IC, and on reducing automatic attention to high caloric foods.

  2. Inhibitory effects of Citrus flavonoids on starch digestion and antihyperglycemic effects in HepG2 cells.

    Science.gov (United States)

    Shen, Wei; Xu, Ying; Lu, Yan-Hua

    2012-09-26

    Flavonoids are a class of important bioactive natural products and are being extensively used in functional foods. In the present study, the effects of four Citrus flavonoids (i.e., hesperidin, naringin, neohesperidin, and nobiletin) on amylase-catalyzed starch digestion, major digestive enzyme activities (e.g., pancreatic α-amylase and α-glucosidase), and glucose use in HepG2 cells were investigated. The results showed that all of the tested Citrus flavonoids significantly inhibited amylase-catalyzed starch digestion. Moreover, naringin and neohesperidin mainly inhibited amylose digestion, whereas hesperidin and nobiletin inhibited both amylose and amylopectin digestion. However, these flavonoids showed weak inhibitory activities against digestive enzymes. Furthermore, glucose consumption, glycogen concentration, and glucokinase activity were significantly elevated, and glucose-6-phosphatase activity was markedly decreased by Citrus flavonoids. These results demonstrate that Citrus flavonoids play important roles in preventing the progression of hyperglycemia, partly by binding to starch, increasing hepatic glycolysis and the glycogen concentration, and lowering hepatic gluconeogenesis. This work suggests that Citrus flavonoids might be potentially used for the prevention of postprandial hyperglycemia.

  3. Inhibitory effect of endostatin gene therapy combined with phosphorus-32 colloid on tumour growth in Wistar rats.

    Science.gov (United States)

    Gao, Huiqi; Zhu, Jing; Li, Yong; Fu, Peng; Shen, Baozhong

    2016-07-01

    Eighty healthy male Wistar rats, aged 5 weeks, weighing 100-120 g, were utilized for establishing tumour-bearing models by immediate Walker-256 cancerous ascites injection and randomly divided to four groups (n=20) treated with 0.2 ml solution containing saline, (32)P-colloid (0.3 mCi), endostatin gene (20 μg), endostatin gene combined with colloid (32)P. The effect of endostatin combined with a small dose of (32)P-colloidal on tumour growth in vivo was evaluated and the potential mechanism underlying the combined therapy was explored. We found that (32)P-colloid combined with endostatin exhibited higher inhibitory effect upon tumour growth compared with application of (32)P-colloid or endostatin alone, although three therapies all significantly inhibited tumour growth compared with saline control group. The higher inhibitory effect of (32)P-colloid combined with endostatin upon tumour growth might be attributed to a synergistic effect of inhibiting angiogenesis by endostatin and inducing apoptosis by (32)P-colloid, as demonstrated by microvessel density (MVD) and apoptotic index (AI) measurement. Combined therapy of (32)P-colloid and endostatin probably serves as a novel and efficacious therapy of tumour growth. © 2016 The Author(s).

  4. Caveolin-1 is essential for metformin inhibitory effect on IGF1 action in non-small-cell lung cancer cells.

    Science.gov (United States)

    Salani, Barbara; Maffioli, Sara; Hamoudane, Meriem; Parodi, Alessia; Ravera, Silvia; Passalacqua, Mario; Alama, Angela; Nhiri, Mohamed; Cordera, Renzo; Maggi, Davide

    2012-02-01

    Metformin causes an AMP/ATP ratio increase and AMP-activated protein kinase (AMPK) activation. Since caveolin-1 (Cav-1) plays a role in AMPK activation and energy balance, we investigated whether Cav-1 could participate in metformin's inhibitory effect on IGF1 signaling. The effect of metformin was studied in two non-small-cell lung cancer (NSCLC) cell lines, Calu-1 and Calu-6, expressing higher and lower amounts of Cav-1, respectively. In Calu-1, but not in Calu-6 cells, metformin reduced phosphorylation of type 1 insulin-like growth factor receptor (IGF-IR) substrates Akt and Forkhead transcription factor 3a (FOXO3a), inhibited IGF1-dependent FOXO3a nuclear exit, and decreased IGF1-dependent cell proliferation. Here, we show that sensitivity of NSCLC cells to metformin was dependent on Cav-1 expression and that metformin required Cav-1 to induce AMPK phosphorylation and AMP/ATP ratio increase. Cav-1 silencing in Calu-1 and overexpression in Calu-6 reduced and improved, respectively, the inhibitory effect of metformin on IGF1-dependent Akt phosphorylation. Prolonged metformin treatment in Calu-6 cells induced a dose-dependent expression increase of Cav-1 and OCT1, a metformin transporter. Cav-1 and OCT1 expression was associated with the antiproliferative effect of metformin in Calu-6 cells (IC(50)=18 mM). In summary, these data suggest that Cav-1 is required for metformin action in NSCLC cells.

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

    Science.gov (United States)

    Decker, Marianne; Nielsen, Per Vaeggemose

    2005-09-25

    The diameter of pinpoint inoculated cheese contaminates (Cladosporium herbarum, Penicillium roqueforti, Penicillium caseifulvum and Penicillium commune), isolated from either the dairy environment or directly from cheese, were inoculated 24 h after inoculation of the secondary starters to simulate 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 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 P. camemberti strain. The presence of G. 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 P. caseifulvum and P. commune were sensitive to this.

  6. 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.

  7. Green synthesis of silver nanoparticles and characterization of their inhibitory effects on AGEs formation using biophysical techniques.

    Science.gov (United States)

    Ashraf, Jalaluddin M; Ansari, Mohammad Azam; Khan, Haris M; Alzohairy, Mohammad A; Choi, Inho

    2016-02-02

    Advanced glycation end-products (AGEs) resulting from non-enzymatic glycation are one of the major factors implicated in secondary complications of diabetes. Scientists are focusing on discovering new compounds that may be used as potential AGEs inhibitors without affecting the normal structure and function of biomolecules. A number of natural and synthetic compounds have been proposed as AGE inhibitors. In this study, we investigated the inhibitory effects of AgNPs (silver nanoparticles) in AGEs formation. AgNPs (~30.5 nm) synthesized from Aloe Vera leaf extract were characterized using UV-Vis spectroscopy, energy-dispersive X-ray spectroscopy (EDX), high resolution-transmission electron microscopy, X-ray diffraction and dynamic light scattering (DLS) techniques. The inhibitory effects of AgNPs on AGEs formation were evaluated by investigating the degree of reactivity of free amino groups (lysine and arginine residues), protein-bound carbonyl and carboxymethyl lysine (CML) content, and the effects on protein structure using various physicochemical techniques. The results showed that AgNPs significantly inhibit AGEs formation in a concentration dependent manner and that AgNPs have a positive effect on protein structure. These findings strongly suggest that AgNPs may play a therapeutic role in diabetes-related complications.

  8. Zingiber cassumunar, Guazuma ulmifolia, and Murraya paniculata Extracts as Antiobesity: In Vitro Inhibitory Effect on Pancreatic Lipase Activity

    Directory of Open Access Journals (Sweden)

    DYAH ISWANTINI

    2011-03-01

    Full Text Available Zingiber cassumunar Roxb. (Bangle, Guazuma ulmifolia Lamk. (Jati belanda, and Murraya paniculata (Kemuning have been used as slimming agents in jamu. A few researches have performed studies on their potency as antiobesity. The aim of this research was to investigate the potency of Z. cassumunar rhizome, G. ulmifolia, and M. paniculata leaf extracts as antiobesity agent based on in vitro inhibition activity of the extracts on pancreatic lipase activity. In this research, water content determination, phytochemical assay, toxicity assay and in vitro assay of inhibition activity on pancreatic lipase were performed toward single and mixture extracts of Z. cassumunar, G. ulmifolia, and M. paniculata resulted by water, ethanol, and saponin extractions. The results indicated that 100 ppm of ethanol extraction of Z. cassumunar had highest inhibition effect on the activity of pancreatic lipase (29.17%, followed by 100 ppm of water extraction of M. paniculata (25.66%, 60 ppm of ethanol extraction of G. ulmifolia leaves (25.13% and ethanol extraction mixture of Z. cassumunar, G. ulmifolia, and M. paniculata leaves with ratio of 25:25:25 (21.58%. These inhibition effects were higher than inhibitory effect of 100 ppm of Xenical®/orlistat as the positive control, with the inhibition value of 17.53%. Saponin crude extracts had lower inhibitory effect than the other extractions. It was suggested that ethanol extraction of Z. cassumunar, and G. ulmifolia and water extraction of M. paniculata had potency as antiobesity agent.

  9. Inhibitory effect of three C-glycosylflavonoids from Cymbopogon citratus (Lemongrass) on human low density lipoprotein oxidation.

    Science.gov (United States)

    Orrego, Roxana; Leiva, Elba; Cheel, José

    2009-09-30

    This study assessed the inhibitory effect of three C-glycosylflavonoids from Cymbopogon citratus leaves--isoorientin (1), swertiajaponin (2) and isoorientin 2"-Orhamnoside (3)--on human LDL oxidation. Isolated LDL was incubated with compounds 1-3 and the kinetics of lipid peroxidation were assessed by conjugated diene and malondialdehyde-thiobarbituric acid reactive substances (MDA-TBARS) formation after addition of copper ions. Significant differences (p < 0.05) between the lag time phase of the control and the lag time phase in the presence of the compounds 1 (0.25 microM) and 2 (0.50 microM) were observed. After five hours of incubation all three compounds showed a significant inhibitory effect on MDA-TBARS formation with respect to the control. After six hours of incubation only compound 1 kept a remarkable antioxidant effect. This study demonstrates that isoorientin (1) is an effective inhibitor of in vitro LDL oxidation. As oxidative damage to LDL is a key event in the formation of atherosclerotic lesions, the use of this natural antioxidant may be beneficial to prevent or attenuate atherosclerosis.

  10. Kinetic spectrophotometric determination of rutin by its inhibitory effect on the oxidation of amaranth by potassium periodate.

    Science.gov (United States)

    Wang, Shuhao; Du, Lingyun; Yao, Xingjun; Niu, Xueli; Zhuang, Huisheng

    2005-01-01

    A novel kinetic spectrophotometric method is described for the determination of rutin. The method is based on the inhibitory effect of rutin on the oxidation reaction of amaranth by potassium periodate in acidic media at 100 degrees C. The linear range for the determination of rutin is 0.02 - 0.50 microg/ml, and the detection limit is 0.014 microg/ml. The method has been successfully applied to the determination of rutin in medicine of rutin tablet and traditional Chinese medicine.

  11. The inhibitory effect of some new synthesized xanthates on mushroom tyrosinase activities.

    Science.gov (United States)

    Alijanianzadeh, M; Saboury, A A; Mansuri-Torshizi, H; Haghbeen, K; Moosavi-Movahedi, A A

    2007-04-01

    Three iso-alkyldithiocarbonates (xanthates), as sodium salts, C3H7OCS2Na (I), C4H9OCS2Na (II) and C5H11OCS2Na (III), were synthesized, by the reaction between CS2 with the corresponding iso-alcohol in the presence of NaOH, and examined for inhibition of both cresolase and catecholase activities of mushroom tyrosinase (MT) from a commercial source of Agricus bisporus. 4-[(4-methylbenzo)azo]-1,2-benzendiol (MeBACat) and 4-[(4-methylphenyl)azo]-phenol (MePAPh) were used as synthetic substrates for the enzyme for the catecholase and cresolase reactions, respectively. Lineweaver-Burk plots showed different patterns of mixed and competitive inhibition for the three xanthates and also for cresolase and catecholase activities of MT. For cresolase activity, I and II showed a mixed inhibition pattern but III showed a competitive inhibition pattern. For catecholase activity, I showed mixed inhibition but II and III showed competitive inhibition. These new synthesized compounds are potent inhibitors of MT with K(i) values of 9.8, 7.2 and 6.1 microM for cresolase inhibitory activity, and also 12.9, 21.8 and 42.2 microM for catecholase inhibitory activity for I, II and III, respectively. They showed a greater inhibitory potency towards the cresolase activity of MT. Both substrate and inhibitor can be bound to the enzyme with negative cooperativity between the binding sites (alpha > 1) and this negative cooperativity increases with increasing length of the aliphatic tail in these compounds in both cresolase and catecholase activities. The cresolase inhibition is related to the chelating of the copper ions at the active site by a negative head group (S-) of the anion xanthate, which leads to similar values of K(i) for all three xanthates. Different K(i) values for catecholase inhibition are related to different interactions of the aliphatic chains of I, II and III with hydrophobic pockets in the active site of the enzyme.

  12. Selective Growth Inhibitory Effect of Biochanin A Against Intestinal Tract Colonizing Bacteria

    Directory of Open Access Journals (Sweden)

    Olga Sklenickova

    2010-03-01

    Full Text Available Both bifidobacteria and clostridia are part of the natural gut microflora and while clostridia may be responsible for severe intestinal infections, bifidobacteria are probiotic microorganisms belonging to the most important prospective bacteria in the bowel. The antimicrobial activity of biochanin A was tested in vitro against six Bifidobacterium spp., and eight Clostridium spp. using the broth microdilution method. Biochanin A showed an inhibition against all clostridia in the range of minimum inhibitory concentrations (MIC from 64 μg/mL (for Cl. clostridioforme, strains DSM 933 and I3 to 1,024 μg/mL (for Cl. perfringens, DSM 11778. No bifidobacteria were suppressed at four-fold higher concentration (MICs > 4,096 than MIC of Cl. perfringens. These results indicate selective growth inhibition of biochanin A and its potential use in antimicrobial prevention and/or protection.

  13. Effects of Subminimum Inhibitory Concentrations of Antibiotics on the Pasteurella multocida Proteome: A Systems Approach

    Directory of Open Access Journals (Sweden)

    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.

  14. 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.

  15. 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.

  16. Inhibitory effect of sodium hypochlorite and chlorhexidine digluconate in clinical isolates of Sporothrix schenckii.

    Science.gov (United States)

    Madrid, Isabel Martins; Mattei, Antonella Souza; Santin, Rosema; dos Reis Gomes, Angelita; Cleff, Marlete Brum; Meireles, Mário Carlos Araújo

    2012-05-01

    The susceptibility of Sporothrix schenckii isolates from clinical cases of canine, feline and human sporotrichosis, and from the environment, was evaluated with 4% sodium hypochlorite and 6.6% chlorhexidine digluconate using the broth microdilution, agar diffusion and direct exposure techniques. The minimal inhibitory concentration was smaller than 0.8% for chlorhexidine digluconate and between 8% and 4% for sodium hypochlorite. Inhibition zones were not found in agar diffusion for sodium hypochlorite, and zones averaging 1.9 mm were found for chlorhexidine digluconate. In the direct exposure test, sodium hypochlorite demonstrated best performance at 20 min of contact, as chlorhexidine digluconate presented little antimicrobial activity. © 2011 Blackwell Verlag GmbH.

  17. Understanding the inhibitory effect of highly potent and selective archazolides binding to the vacuolar ATPase.

    Science.gov (United States)

    Dreisigacker, Sandra; Latek, Dorota; Bockelmann, Svenja; Huss, Markus; Wieczorek, Helmut; Filipek, Slawomir; Gohlke, Holger; Menche, Dirk; Carlomagno, Teresa

    2012-08-27

    Vacuolar ATPases are a potential therapeutic target because of their involvement in a variety of severe diseases such as osteoporosis or cancer. Archazolide A (1) and related analogs have been previously identified as selective inhibitors of V-ATPases with potency down to the subnanomolar range. Herein we report on the determination of the ligand binding mode by a combination of molecular docking, molecular dynamics simulations, and biochemical experiments, resulting in a sound model for the inhibitory mechanism of this class of putative anticancer agents. The binding site of archazolides was confirmed to be located in the equatorial region of the membrane-embedded V(O)-rotor, as recently proposed on the basis of site-directed mutagenesis. Quantification of the bioactivity of a series of archazolide derivatives, together with the docking-derived binding mode of archazolides to the V-ATPase, revealed favorable ligand profiles, which can guide the development of a simplified archazolide analog with potential therapeutic relevance.

  18. 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.

  19. 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.

  20. Inhibitory effect of gels loaded with a low concentration of antibiotics against biofilm formation by Enterococcus faecalis and Porphyromonas gingivalis.

    Science.gov (United States)

    A Algarni, Amnah; H Yassen, Ghaeth; L Gregory, Richard

    2015-09-01

    We explored longitudinally the inhibitory effect of gels loaded with 1 mg/mL modified triple antibiotic paste (MTAP) or double antibiotic paste (DAP) against biofilm formation by Enterococcus faecalis and Porphyromonas gingivalis. Methylcellulose-based antibiotic gels of MTAP (ciprofloxacin, metronidazole and clindamycin) and DAP (ciprofloxacin and metronidazole) were prepared at a concentration of 1 mg/mL. Individually cultured E. faecalis and P. gingivalis bacterial suspensions were treated with MTAP, DAP, or placebo (vehicle only) gels at different dilutions and allowed to grow in 96-well microtiter plates. Untreated bacterial suspensions served as a negative control. Crystal violet assays were used to evaluate biofilm formation after 48 h. The ability of the gels to inhibit biofilm formation was determined immediately, and at 1 month and 3 months after the gels had been prepared. Data were analyzed using a mixed-model ANOVA. The MTAP and DAP gels significantly reduced biofilm formation by both bacterial species at all time points, regardless of the tested dilution. No-significant differences in biofilm-inhibitory effects between MTAP and DAP gels were observed at the majority of the tested dilutions through various time points. Gels loaded with 1 mg/mL MTAP and DAP demonstrated a significant antibiofilm effect against E.faecalis and P. gingivalis.

  1. The inhibitory effect of Mycoplasma fermentans on tumour necrosis factor (TNF)-alpha-induced apoptosis resides in the membrane lipoproteins.

    Science.gov (United States)

    Gerlic, Motti; Horowitz, Jacob; Farkash, Shai; Horowitz, Shulamith

    2007-01-01

    Mycoplasma have been shown to be involved in the alteration of several eukaryotic cell functions, such as cytokine production, gene expression and more. We have previously reported that infection of human myelomonocytic U937 cell line with live Mycoplasma fermentans (M. fermentans) inhibited tumour necrosis factor (TNF-alpha)-induced apoptosis. Mycoplasmal membrane lipoproteins are considered to be the most potent initiators of inflammatory reactions in mycoplasmal infections. The aim of this study was to clarify whether the inhibitory effect on TNFalpha-induced apoptosis is exerted by M. fermentans lipoproteins (LPMf). A significant reduction in TNFalpha-induced apoptosis was demonstrated by stimulation of U937 cells with M. fermentans total proteins, LPMf or MALP-2 (M. fermentans synthetic lipopeptide), but not with M. fermentans hydrophilic protein preparation (AqMf). To investigate the mechanism of M. fermentans antiapoptotic effect, the reduction of mitochondrial transmembrane potential (delta psi m) was measured. M. fermentans total proteins LPMf and MALP-2, but not AqMf, inhibited the reduction of delta psi m. In addition, M. fermentans total proteins LPMf and MALP-2, but not AqMf, downregulated the formation of active caspase-8. NF-kappaB was transactivated in cells treated with M. fermentans lipoproteins, and was essential for host cell survival, but not for the inhibition of TNFalpha-induced apoptosis by LPMf. Our results suggest that the inhibitory effect exerted by M. fermentans on TNFalpha-induced apoptosis in U937 cells is due to the membrane lipoproteins of these bacteria.

  2. An investigation into the inhibitory effect of ultraviolet radiation on Trichophyton rubrum.

    Science.gov (United States)

    Cronin, Leah J; Mildren, Richard P; Moffitt, Michelle; Lauto, Antonio; Morton, C Oliver; Stack, Colin M

    2014-01-01

    Fungal infection of nails, onychomycosis, is predominantly caused by Trichophyton rubrum. This infection is an important public health concern due to its persistent nature and high recurrence rates. Alternative treatments are urgently required. One such alternative is phototherapy involving the action of photothermal or photochemical processes. The aim of this novel study was to assess which wavelengths within the ultraviolet (UV) spectrum were inhibitory and equally important nail transmissible. Initial irradiations of T. rubrum spore suspensions were carried out using a tunable wavelength lamp system (fluence ≤3.1 J/cm(2)) at wavelengths between 280 and 400 nm (UVC to UVA) to evaluate which wavelengths prevented fungal growth. Light-emitting diodes (LEDs) of defined wavelengths were subsequently chosen with a view to evaluate and potentially implement this technology as a low-cost "in-home" treatment. Our experiments demonstrated that exposure at 280 nm using an LED with a fluence as low as 0.5 J/cm(2) was inhibitory, i.e., no growth following a 2-week incubation (p < 0.05; one-way ANOVA), while exposure to longer wavelengths was not. A key requirement for the use of phototherapy in the treatment of onychomycosis is that it must be nail transmissible. Our results indicate that the treatment with UVC is not feasible given that there is no overlap between the antifungal activity observed at 280 nm and transmission through the nail plate. However, a potential indirect application of this technology could be the decontamination of reservoirs of infection such as the shoes of infected individuals, thus preventing reinfection.

  3. In vitro inhibitory effect of tetrahydrocurcuminoids on Fusarium proliferatum growth and fumonisin B₁ biosynthesis.

    Science.gov (United States)

    Coma, Véronique; Portes, Elise; Gardrat, Christian; Richard-Forget, Florence; Castellan, Alain

    2011-02-01

    Many plant pathogens produce toxic metabolites when growing on food and feed. Some antioxidative components seem to prevent fungal growth and mycotoxin formation. Recently, we synthesized a new class of powerful antioxidative compounds, i.e. tetrahydrocurcuminoids, and its structure/antioxidant activity relationships have been established. The South West of France produces large amounts of corn, which can be infected by Fusarium species, particularly F. proliferatum. In this context, the efficiency of tetrahydrocurcuminoids, which can be obtained from natural curcuminoids, was investigated to control in vitro the growth of F. proliferatum and the production of its associated mycotoxin, fumonisin B₁. The relation between structure and antifungal activity was studied. Tetrahydrocurcumin (THC1), with two guaiacyl phenolic subunits, showed the highest inhibitory activity (measured as radial growth on agar medium) against the F. proliferatum development (67% inhibition at a concentration of 13.6 µmol ml⁻¹). The efficiencies of THC2 (36% at a concentration of 11.5 µmol ml⁻¹), which contains syringyl phenolic units, and THC3 (30% at a concentration of 13.6 µmol ml⁻¹), which does not have any substituent on the aromatic rings, were relatively close. These results indicate that the simultaneous presence of guaiacyl phenols and the enolic function of the β-diketone moiety play an important role in the inhibition mechanisms. The importance of this combination was confirmed using n-propylguaiacol and acetylacetone as molecular models. Under the same conditions, ferulic acid and eugenol, other natural phenolic antioxidants, were less efficient in inhibiting fungal growth. THC1 also reduced fumonisin B₁ production in liquid medium by approximately 35, 50 and 75% at concentrations of 0.8, 1.3, and 1.9 µmol ml⁻¹, respectively. These very low inhibitory concentrations show that tetrahydrocurcuminoids could be one of the most promising biobased molecules for the

  4. Antifungal Effects of Zataria multiflora Essential Oil on the Inhibitory Growth of some Postharvest Pathogenic Fungi

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    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.

  5. Inhibitory effects of oral prednisolone and fexofenadine on skin responses by prick tests with histamine and compound 48/80.

    Science.gov (United States)

    Inoue, Tomoko; Katoh, Norito; Kishimoto, Saburo; Matsunaga, Kayoko

    2002-12-01

    The prick test is a useful skin test for diagnosing immediate hypersensitivity response. Sometimes it is necessary to perform prick tests on patients who have already received antihistamines or corticosteroids. It is, however, occasionally uncertain whether the results of prick tests are reliable. In this study, the inhibitory effects of prednisolone (10 mg/day) and fexofenadine (120 mg/day) on the response to prick tests induced with histamine and compound 48/80 were examined. During a 7-day-continual drug administration, prick tests were performed 8 h after drug administration. The inhibitory effects of fexofenadine on both the histamine- and compound 48/80-induced skin responses were exhibited on the 1st day and persisted from 24 to 36 h after the final administration. The histamine-induced wheal responses were not inhibited by prednisolone, while the compound 48/80-induced flare and wheal responses were significantly inhibited on the 5th day of drug administration. These responses returned to the baseline level 24 h after the last drug administration. Thus, the results of skin tests performed during administration of antihistamines and corticosteroids should be carefully interpreted.

  6. Inhibitory effects of Cnidium monnieri fruit extract on pulmonary inflammation in mice induced by cigarette smoke condensate and lipopolysaccharide.

    Science.gov (United States)

    Kwak, Ho-Geun; Lim, Heung-Bin

    2014-09-01

    The aim of this study was to investigate the inhibitory effect of Cnidium monnieri fruit (CM) extracts on pulmonary inflammation induced in mice by cigarette smoke condensate (CSC) and lipopolysaccharide (LPS). Pulmonary inflammation was induced by intratracheal instillation of LPS and CSC five times within 12 days. CM extract was administered orally at a dose of 50 or 200 mg·kg(-1). The number of inflammatory cells in the bronchoalveolar lavage fluid was counted using a fluorescence activated cell sorter. Inflammatory mediator levels were determined by enzyme-linked immunosorbent assay. The administration of LPS and CSC exacerbated airway hyper-responsiveness (AHR) and induced an accumulation of inflammatory cells and mediators, and led to histological changes. However, these responses are modulated by treatment with CM, and the treatment with CM extract produces similar or more extensive results than the treatment with cyclosporin A (CSA). CM extract may have an inhibitory effect on pulmonary inflammation related with chronic obstructive pulmonary disease. Copyright © 2014 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.

  7. Isolation and identification of sea buckthorn (Hippophae rhamnoides) phenolics with antioxidant activity and α-glucosidase inhibitory effect.

    Science.gov (United States)

    Kim, Ju-Sung; Kwon, Yong-Soo; Sa, Yeo-Jin; Kim, Myong-Jo

    2011-01-12

    This study was performed to evaluate the antioxidant and α-glucosidase inhibitory effects from the extract, fractions, and isolated compounds of sea buckthorn leaves. Six compounds, kaempferol-3-O-β-D-(6''-O-coumaryl) glycoside, 1-feruloyl-β-D-glucopyranoside, isorhamnetin-3-O-glucoside, quercetin 3-O-β-D-glucopyranoside, quercetin 3-O-β-D-glucopyranosyl-7-O-α-L-rhamnopyranoside, and isorhamnetin-3-O-rutinoside, were isolated from sea buckthorn leaf extracts. The butanol fraction (EC(50) = 1.81 μg/mL) along with quercetin 3-O-β-D-glucopyranoside (EC(50) = 1.86 μg/mL) had a higher DPPH radical-scavenging activity and showed stronger reducing power (OD(700) = 1.83 and 1.78, respectively). The butanol fraction (477 mg GAE/g) contained the highest amount of phenolic compounds and also the most powerful α-glucosidase inhibitory effect (86%) at 5 μg/mL. The results indicate that sea buckthorn leaf extracts could potentially be used for food additives and the development of useful natural compounds.

  8. [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.

  9. Inhibitory effect of antioxidant-rich marinades on the formation of heterocyclic aromatic amines in pan-fried beef.

    Science.gov (United States)

    Viegas, Olga; Amaro, L Filipe; Ferreira, Isabel M P L V O; Pinho, Olívia

    2012-06-20

    The inhibitory effect of antioxidant-rich marinades containing beer and white wine (with/without alcohol) alone or mixed with herbs commonly used as meat flavoring (garlic, ginger, thyme, rosemary, and red chili pepper) on the formation of heterocyclic aromatic amines (HAs) in pan-fried beef was studied. Radical-scavenging activity was evaluated by DPPH assay, before the addition of meat to the marinade (T0) and after 4 h of meat marinating (T4). At T0, wine with herbs possessed the highest scavenging activity (73.5%), followed by wine (72.5%), dealcoholized wine with herbs (53.4%), beer and herbs (41.7%), dealcoholized wine (39.6%), and beer (25.9%). At T4, a decrease in the radical-scavenging activity of all marinades was observed, although with a similar radical-scavenging profile. All of the six marinades under the study reduced the total amount of HAs, keeping meat with good overall sensory quality. Beer marinades were more efficient than white wine marinades, and the addition of herbs provided a superior inhibitory effect, reducing around 90% of HAs. No correlation was observed between radical-scavenging activity of marinades and total or individual HAs formation. Herbs explained around 30% of inhibition of PhIP formation, whereas alcohol increased PhIP formation.

  10. 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.

  11. 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.

  12. In Vitro Antioxidant Properties, HIV-1 Reverse Transcriptase and Acetylcholinesterase Inhibitory Effects of Traditional Herbal Preparations Sold in South Africa

    Directory of Open Access Journals (Sweden)

    Johannes Van Staden

    2010-10-01

    Full Text Available The antioxidant potentials for fourteen multipurpose traditional herbal preparations sold in South Africa were determined using the DPPH radical scavenging, ferric reducing power and β-carotene-linoleic acid model system, the anti-HIV-1 reverse transcriptase (RT enzyme inhibitory effects using an ELISA kit and acetylcholinesterase (AChE enzyme inhibition using the microtitre plate assay. Nine of the herbal mixtures (Umzimba omubi, Umuthi wekukhwehlela ne zilonda, Mvusa ukunzi, Umpatisa inkosi, Imbiza ephuzwato, Vusa umzimba, Supreme one hundred, Sejeso herbal mixture Ingwe® and Ingwe® special muti exhibited higher antioxidant potentials, while only four (Imbiza ephuzwato, Ingwe® muthi mixture, Sejeso herbal mixture Ingwe® and African potato extractTM showed potent activity against the RT enzyme. Nine mixtures (Imbiza ephuzwato, Umpatisa inkosi, African potato extractTM, Sejeso herbal mixture Ingwe®, Vusa umzimba; Ingwe® muthi mixture, Ibhubezi™, Lion izifozonke Ingwe® and Ingwe® special muti showed AChE enzyme inhibitory activity greater than 50%. The observed activity exhibited by some of the herbal mixtures gives some credence to the manufacturers’ claims and goes part of the way towards validating their use against certain conditions such as oxidative stress, HIV/AIDS proliferation and some mental conditions. It is however, desirable to carry out further studies to determine the effects of mixing plant species/parts in one mixture on the antioxidant potency as well as isolating active constituents from the herbal mixtures.

  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. Profound thrombocytopenia after primary exposure to eptifibatide

    OpenAIRE

    Norgard, Nicholas; Badgley,Brian

    2010-01-01

    Nicholas B Norgard, Brian T BadgleyUniversity at Buffalo, School of Pharmacy and Pharmaceutical Sciences, Buffalo, NY, USAAbstract: Eptifibatide is a glycoprotein IIb/IIIa receptor antagonist used to reduce the incidence of ischemic events in patients with acute coronary syndromes and those undergoing percutaneous coronary intervention. A minority of patients given eptifibatide develop acute, profound thrombocytopenia (<20,000 cells/mm3) within a few hours of receiving the drug. This c...

  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. 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 IC50 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.

  17. 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.

  18. 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.

  19. Selective binding modes and allosteric inhibitory effects of lupane triterpenes on protein tyrosine phosphatase 1B.

    Science.gov (United States)

    Jin, Tiantian; Yu, Haibo; Huang, Xu-Feng

    2016-02-11

    Protein Tyrosine Phosphatase 1B (PTP1B) has been recognized as a promising therapeutic target for treating obesity, diabetes, and certain cancers for over a decade. Previous drug design has focused on inhibitors targeting the active site of PTP1B. However, this has not been successful because the active site is positively charged and conserved among the protein tyrosine phosphatases. Therefore, it is important to develop PTP1B inhibitors with alternative inhibitory strategies. Using computational studies including molecular docking, molecular dynamics simulations, and binding free energy calculations, we found that lupane triterpenes selectively inhibited PTP1B by targeting its more hydrophobic and less conserved allosteric site. These findings were verified using two enzymatic assays. Furthermore, the cell culture studies showed that lupeol and betulinic acid inhibited the PTP1B activity stimulated by TNFα in neurons. Our study indicates that lupane triterpenes are selective PTP1B allosteric inhibitors with significant potential for treating those diseases with elevated PTP1B activity.

  20. Inhibitory effect of cyanide on nitrification process and its eliminating method in a suspended activated sludge process.

    Science.gov (United States)

    Han, Yuanyuan; Jin, Xibiao; Wang, Yuan; Liu, Yongdi; Chen, Xiurong

    2014-02-01

    Inhibition of nitrification by four typical pollutants (acrylonitrile, acrylic acid, acetonitrile and cyanide) in acrylonitrile wastewater was investigated. The inhibitory effect of cyanide on nitrification was strongest, with a 50% inhibitory concentration of 0.218 mg·gVSS-1 being observed in a municipal activated sludge system. However, the performance of nitrification was recovered when cyanide was completely degraded. The nitrification, which had been inhibited by 4.17 mg·gVSS-1 of free cyanide for 24 h, was recovered to greater than 95% of that without cyanide after 10 days of recovery. To overcome cyanide inhibition, cyanide-degrading bacteria were cultivated in a batch reactor by increasing the influent cyanide concentration in a stepwise manner, which resulted in an increase in the average cyanide degradation rate from 0.14 to 1.01 mg CN-·gVSS-1·h-1 over 20 days. The cultured cyanide-degrading bacteria were shaped like short rods, and the dominant cyanide-degrading bacteria strain was identified as Pseudomonas fluorescens NCIMB by PCR.

  1. Inhibitory effect of organic acids on arcobacters in culture and their use for control of Arcobacter butzleri on chicken skin.

    Science.gov (United States)

    Skřivanová, Eva; Molatová, Zuzana; Matěnová, Michaela; Houf, Kurt; Marounek, Milan

    2011-01-05

    The inhibitory effects of 17 organic acids (C₂-C₁₆ fatty acids, sorbic, benzoic, phenylacetic, fumaric, succinic, lactic, malic and citric) on Arcobacter butzleri, Arcobacter cryaerophilus and Arcobacter skirrowii were investigated by determining their IC₅₀ values, defined as the concentration of acid at which the target DNA sequence was expressed at 50% of the positive control level in cultures incubated at 30°C for 24 h. DNA was analysed by real-time PCR. The Arcobacter strains tested were inhibited by all the organic acids, with the sensitivities in the order A. skirrowii > A. cryaerophilus > A. butzleri. Eight acids with IC₅₀ values of acids at 5 mg/mL for 1 min. Samples of skin were collected from carcass halves after storage at 4°C for 0, 1, 2 or 3 days for enumeration of arcobacters on Muller-Hinton agar. All eight tested acids suppressed bacterial proliferation. The highest inhibitory activities were observed for benzoic, citric, malic and sorbic acids. Subsequent sensory analysis revealed benzoic acid to be the most suitable organic acid for chicken skin treatment. Copyright © 2010 Elsevier B.V. All rights reserved.

  2. Lactobacillus fermentation enhances the inhibitory effect of Hwangryun-haedok-tang in an ovariectomy-induced bone loss.

    Science.gov (United States)

    Shim, Ki-Shuk; Kim, Taesoo; Ha, Hyunil; Lee, Kwang Jin; Cho, Chang-Won; Kim, Han Sung; Seo, Dong-Hyun; Ma, Jin Yeul

    2013-05-16

    Hwangryun-haedok-tang (HRT) is traditional herbal medicine used to treat inflammatory-related diseases in Asia. However, its effect on osteoclastogenesis and bone loss is still unknown. In this study, we evaluated the effect of HRT and its fermented product (fHRT) on the receptor activator for the nuclear factor-κB ligand-induced osteoclastogenesis using murine bone marrow-derived macrophages and postmenopausal bone loss using an ovariectomy (OVX) rat model. Tartrate resistant acid phosphatase (TRAP) staining was employed to evaluate osteoclast formation. mRNA level of transcription factor and protein levels of signaling molecules were determined by real-time quantitative polymerase chain reaction and Western blot analysis, respectively. Effect of HRT or fHRT on OVX-induced bone loss was evaluated using OVX rats orally administered HRT, or fHRT with 300 mg/kg for 12 weeks. Micro-CT analysis of femora was performed to analyze bone parameter. HRT or fHRT treatment significantly decreased TRAP activity and the number of TRAP positive multinuclear cells on osteoclastogenesis. Interestingly, these inhibitory effects of HRT were enhanced by fermentation. Furthermore, fHRT significantly inhibited mRNA and protein expression of nuclear factor of activated T cells cytoplasmic 1, which leads to down-regulation of NFATc1-regulated mRNA expressions such as TRAP, the d2 isoform of vacuolar ATPase V(0) domain, and cathepsin K. Administration of fHRT significantly inhibited the decrease of bone mineral density, and improved bone parameter of femora more than that of HRT and vehicle in OVX rats. This study demonstrated that lactic bacterial fermentation fortifies the inhibitory effect of HRT on osteoclastogenesis and bone loss. These results suggest that fermented HRT might have the beneficial potential on osteoporosis by inhibiting osteoclastogenesis.

  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. [The inhibitory effects of siRNA expression vector on the expression of human papillomavirus E6 gene].

    Science.gov (United States)

    Li, Da-ke; Peng, Zhi-lan; Niu, Xiao-yu; Wang, Dan-qing

    2005-05-01

    To investigate the inhibitory effects of RNAi(RNA interference)expression vector on the expression of human papilomavirus E6 gene. siRNA expression vectors were constructed to be aimed directly at HPV16 E6 gene. The recombinants were transfected into cervical cancer cell line, caski, with liposomes. Expression of E6 was detected with fluorescence quantitative PCR (FQ-PCR) and flow cytometry. Three kinds of expression vectors could reduce the expression of E6 mRNA and protein all in caski-B cell. The expression of E6 mRNA reduced to 21.7% of control group, and the protein inhibition ratio reached 98.1%. The RNAi expression vector can effectively inhibit the expression of HPVE6 gene.

  5. Inhibitory effect of aqueous extract from the gall of Rhus chinensis on alpha-glucosidase activity and postprandial blood glucose.

    Science.gov (United States)

    Shim, Young-Jun; Doo, Ho-Kyung; Ahn, Se-Young; Kim, Yong-Suk; Seong, Je-Kyung; Park, In-Sun; Min, Bon-Hong

    2003-04-01

    The present study examined the inhibitory effect of aqueous extract from the gall of Rhus chinensis (AEGRC) on alpha-glucosidase activity, an enzyme responsible for digestion of carbohydrate to monosaccharides in the process of intestinal absorption. AEGRC inhibited Bacillus alpha-glucosidase acitvity with an IC(50) of 0.9 micro g/ml. Its inhibition on alpha-glucosidase was determined to be noncompetitive and reversible when the enzyme-substrate mixture was simultaneously treated with AEGRC as an inhibitor. In addition, when it was orally administered to rats with sucrose (2g/kg), AEGRC (250-1000mg/kg) significantly suppressed the increase of blood glucose levels after sucrose loading in a dose dependent manner. These results suggest that AEGRC might exert anti-diabetic effect by suppressing carbohydrate absorption from intestine, and thereby reducing the postprandial increase of blood glucose.

  6. Inhibitory Effect of Algal Extracts on Mycelial Growth of the Tomato-Wilt Pathogen, Fusarium oxysporum f. sp. lycopersici

    Science.gov (United States)

    Kim, Jiyoung

    2008-01-01

    The present study was undertaken to explore the inhibitory effect of cyanobacterial extracts of Nostoc commune FA-103 against the tomato-wilt pathogen, Fusarium oxysporum f. sp. lycopersici. In an optimal medium, cell growth, antifungal activity, and antifungal compound production could be increased 2.7-fold, 4.1-fold, and 13.4-fold, respectively. A crude algal extract had a similar effect as mancozeb at the recommended dose, both in laboratory and pot tests. In vitro and in vivo fungal growth, spore sporulation and fungal infection of wilt pathogen in tomato seeds were significantly inhibited by cyanobacterial extracts. Nostoc commune FA-103 extracts have potential for the suppression of Fusarium oxysporum f. sp. lycopersici. PMID:23997634

  7. Inhibitory effects of carbon nanotubes on the degradation of 14C-2,4-dichlorophenol in soil.

    Science.gov (United States)

    Zhou, Wenqiang; Shan, Jun; Jiang, Bingqi; Wang, Lianhong; Feng, Jianfang; Guo, Hongyan; Ji, Rong

    2013-01-01

    Concerns on the potential risks of engineered nanoparticles to the environment are increasing; however, little is known about the effects of carbon nanotubes (CNTs) on the environmental fate of hydrophobic organic pollutants in soil. We incubated radioactive labeled 2,4-dichlorophenol ((14)C-2,4-DCP) in a soil in the presence of various concentrations (0, 2, 20, and 2000 mg kg(-1) dry soil) of single-walled (SWCNTs) and multi-walled (MWCNTs) carbon nanotubes, and determined the mineralization, degradation, and residue distribution of 2,4-DCP in the soil. CNTs were added to the soil either after the spiking of (14)C-2,4-DCP or together with (14)C-2,4-DCP as a mixture. CNTs at the concentration of 2000 mg kg(-1) significantly (Psoil after 90 d of incubation. Pre-adsorption of (14)C-2,4-DCP on CNTs showed stronger inhibitory effects on the degradation of (14)C-2,4-DCP, already significant with CNTs at 20 mg kg(-1). In general, SWCNTs had a higher effect on the degradation and residue distribution of 2,4-DCP in the soil than MWCNTs. The inhibitory effects are supposed to be owing to limited activities of soil endogenous microorganisms, potential toxicities of CNTs to the microorganisms, and reduced bioavailability of 2,4-DCP in the presence of CNTs, even though a desorption hysteresis of 2,4-DCP on CNTs was not observed. Our results indicate that CNTs have more significant impacts on the environmental fate of the hydrophobic pollutants entering soil together with CNTs via strong sorption than the pollutants already present in soil. Copyright © 2012 Elsevier Ltd. All rights reserved.

  8. Re-expression of ARHI (DIRAS3 induces autophagy in breast cancer cells and enhances the inhibitory effect of paclitaxel

    Directory of Open Access Journals (Sweden)

    Bast Robert C

    2011-01-01

    Full Text Available Abstract Background ARHI is a Ras-related imprinted gene that inhibits cancer cell growth and motility. ARHI is downregulated in the majority of breast cancers, and loss of its expression is associated with its progression from ductal carcinoma in situ (DCIS to invasive disease. In ovarian cancer, re-expression of ARHI induces autophagy and leads to autophagic death in cell culture; however, ARHI re-expression enables ovarian cancer cells to remain dormant when they are grown in mice as xenografts. The purpose of this study is to examine whether ARHI induces autophagy in breast cancer cells and to evaluate the effects of ARHI gene re-expression in combination with paclitaxel. Methods Re-expression of ARHI was achieved by transfection, by treatment with trichostatin A (TSA or by a combination of TSA and 5-aza-2'-deoxycytidine (DAC in breast cancer cell cultures and by liposomal delivery of ARHI in breast tumor xenografts. Results ARHI re-expression induces autophagy in breast cancer cells, and ARHI is essential for the induction of autophagy. When ARHI was re-expressed in breast cancer cells treated with paclitaxel, the growth inhibitory effect of paclitaxel was enhanced in both the cell culture and the xenografts. Although paclitaxel alone did not induce autophagy in breast cancer cells, it enhanced ARHI-induced autophagy. Conversely, ARHI re-expression promoted paclitaxel-induced apoptosis and G2/M cell cycle arrest. Conclusions ARHI re-expression induces autophagic cell death in breast cancer cells and enhances the inhibitory effects of paclitaxel by promoting autophagy, apoptosis, and G2/M cell cycle arrest.

  9. Experimental study on inhibitory effects of histone deacetylase inhibitor MS-275 and TSA on bladder cancer cells.

    Science.gov (United States)

    Qu, Wei; Kang, Yin-Dong; Zhou, Mei-Sheng; Fu, Li-Li; Hua, Zhen-Hao; Wang, Li-Ming

    2010-01-01

    To investigate the inhibitory effect of histone deacetylase (HDAC) inhibitors (MS-275 and TSA) on T24 human bladder cancer cells in vitro, and explore the possible mechanism. The MTT assay was employed to evaluate the inhibitory effect of MS-275 and TSA on T24 cell growth. FCM was used to analyze the variation of T24 cell cycle distribution and the apoptotic ratio after T24 cells were treated with MS-275 and TSA. Histone acetylation level was detected by Western blot. mRNA expression of p21 WAF1/CIP1, cyclin A, and cyclin E was measured by FQ-PCR. Dynamic changes of Bcl-2 and bax expression were detected by FCM. MS-275 and TSA inhibited T24 cell growth in a concentration and time-dependent manner. Treatment with 4 μmol/l MS-275 or 0.4 μmol/l TSA blocked cell cycling in the G0/G1 phase and induced a significant increase in cell apoptosis. MS-275 and TSA significantly increased the level of histone acetylation, induced p21CIP1WAF1 mRNA expression, and inhibited cyclin A mRNA expression, though no significant effect was observed on cyclin E. Bcl-2 expression was down-regulated, while bax expression was up-regulated. HDAC inhibitors can block bladder cancer cell cycle in vitro and induce apoptosis. The molecular mechanism may be associated with increased level of histone acetylation, down-regulation of p21WAF1/CIP1 expression, up-regulation of cyclin A expression, and dynamic change of bcl-2 and bax expression. Copyright © 2010 Elsevier Inc. All rights reserved.

  10. The Inhibitory Effects of Eucalyptus Extract on Herpes Simplex Virus-1 Replication in Baby Hamster Kidney Cells

    Directory of Open Access Journals (Sweden)

    Karimi A

    2012-04-01

    Full Text Available Background and Objectives: In recent years, following the increasing of drug resistant strain of viruses, there has been an increasing interest in the use of natural substances with antiviral activity and low side effects. One of these herbal medicines, Eucaliptus, has shown some therapeutic effects including antibacterial and antiviral activities. Therefore, this study aimed to determine the minimum inhibitory concentration of hydroalchoholic extract of Eucaliptus on Herpes simplex virus-1 (HSV-1 in vitro. Methods: In this experimental study, the hydroalchoholic extract of Eucalyptus leaves was prepared using 70% ethanol through maceration method. Baby Hamster Kidney (BHK cells were grown in monolayer culture with Dulbecco's modified Eagle's medium (DMEM supplemented with 5% fetal calf serum and plated onto 48-well culture plates. 50% cytotoxic concentration (CC50% of the extract on BHK cells was determined, and subsequently 50% inhibitory concentration (IC50% of the herbal extract on replication of HSV-1 both in extracellular and intracellular cases was assessed. Results: Based on Probit analysis, CC50% of the extract was 0.650mg/ml. Significant relationships between the concentration of the extract and cell death in the cell studied were shown using the Probit model (p<0.01. IC50s of the extract on the virus before cellular attachment and after entering the cells were 456.82µg/ml and 180.75µg/ml, respectively. Based on the model, with increasing the extract concentration, the percentage of inhibition of cytopathic effect (CPE in both stages was increased (p<0.05. Conclusion: Based on the findings of this study, hydroalchoholic extract of Eucaliptus could be probably an appropriate anti herpetic herbal medicine.

  11. 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.

  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

    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

  13. Asystole Following Profound Vagal Stimulation During Hepatectomy

    Directory of Open Access Journals (Sweden)

    Preeta John

    2008-01-01

    Full Text Available Asystole in a non laparoscopic upper abdominal surgery following intense vagal stimulation is a rare event. This case report highlights the need for awareness of such a complication when a thoracic epidural anaesthetic has been given in addition to a general anaesthetic for an upper abdominal procedure. A combined thoracic epidural and general anaesthetic was given. The anterior abdominal wall was retracted forty minutes after administration of the epidural bolus. This maneuver resulted in a profound vagal response with bradycardia and asystole. The patient was resuscitated successfully with a cardiac massage, atropine and adrenaline and the surgery was resumed. Surgery lasted eleven hours and was uneventful.

  14. Temperature influence on silver nanoparticles inhibitory effect on photosystem II photochemistry in two green algae, Chlorella vulgaris and Dunaliella tertiolecta.

    Science.gov (United States)

    Oukarroum, Abdallah; Polchtchikov, Stephanie; Perreault, François; Popovic, Radovan

    2012-06-01

    In this study, the effect of silver nanoparticles (AgNPs) on the photosynthetic performance of two green algae, Chlorella vulgaris and Dunaliella tertiolecta, was investigated at 25°C and 31°C. To induce AgNPs effect, algal cells were exposed for 24 h to concentrations varying from 0 to 10 mg/L. The polyphasic OJIP fluorescence transient was used to evaluate photosystem II (PSII). We show that growth media and temperature had different effects in AgNPs agglomerates formation and Zeta potential. When temperature conditions change, inhibitory effect of AgNPs also undergoes changes. Increase of temperature induced higher altering effects to PSII quantum yield, primary photosynthetic electron transport, and consequently higher decrease of total photosynthetic performance if compared to AgNPs effect alone. AgNPs has a negative effect on D. tertiolecta compared to C. vulgaris. We conclude that temperature tends to enhance the toxic effects on aquatic alga and these alterations might have serious consequences on ecosystem equilibrium and aquatic plant communities.

  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 and mechanisms of high molecular-weight phlorotannins from Sargassum thunbergii on ADP-induced platelet aggregation

    Science.gov (United States)

    Wei, Yuxi; Wang, Changyun; Li, Jing; Guo, Qi; Qi, Hongtao

    2009-09-01

    We evaluated the effects of high molecular-weight phlorotannins from Sargassum thunbergii (STP) on ADP-induced platelet aggregation and arachidonic acid (AA) metabolism in New Zealand white rabbits and Wistar rats. The inhibition of STP on platelet aggregation was investigated using a turbidimetric method, and the levels of the terminal products of AA metabolism were measured using the corresponding kits for maleic dialdehyde (MDA), thromboxane B2 (TXB2) and 6-keto-prostaglandin F1α (6-keto-PGF1α) by colorimetry and radioimmunoassay, as appropriate. We found that STP could inhibit ADP-induced platelet aggregation, and the inhibitory ratio was 91.50% at the STP concentration of 4.0 mg/mL. Furthermore, STP markedly affected AA metabolism by decreasing the synthesis of MDA ( Pplatelets were activated ( Pmetabolism and these findings partly revealed the molecular mechanism by which STP inhibits ADP-induced platelet aggregation.

  17. Effect of stimulus parameters and contraction level on inhibitory responses in human jaw-closing muscles: Implications for contingent stimulation

    DEFF Research Database (Denmark)

    Jadidi, F; Wang, K; Arendt-Nielsen, Lars

    2009-01-01

    % of the maximal voluntary contraction (MVC). Results: The stimulus intensities required to reach the perceived intensity levels were inversely related to stimulus duration (P stimuli was dependent on stimulus intensity (P ....001, respectively) but not contraction level. There were significant decreases evoked by the 450 ms stimuli in RMS-EMG values in the 400-500 ms compared with the pre-stimulus interval (P ... results suggest that the ES2 reflex response is associated with the duration of the electrical stimuli, the intensity level but not the contraction level. In contrast, the inhibitory effects of ultra-long stimuli (450 ms) are not specifically related to the intensity level suggesting that this is a non...

  18. Tyrosinase Inhibitory Effect and Antioxidative Activities of Fermented and Ethanol Extracts of Rhodiola rosea and Lonicera japonica

    Directory of Open Access Journals (Sweden)

    Yuh-Shuen Chen

    2013-01-01

    Full Text Available This is the first study to investigate the biological activities of fermented extracts of Rhodiola rosea L. (Crassulaceae and Lonicera japonica Thunb. (Caprifoliaceae. Alcaligenes piechaudii CC-ESB2 fermented and ethanol extracts of Rhodiola rosea and Lonicera japonica were prepared and the antioxidative activities of different concentrations of samples were evaluated using in vitro antioxidative assays. Tyrosinase inhibition was determined by using the dopachrome method with L-DOPA as substrate. The results demonstrated that inhibitory effects (ED50 values on mushroom tyrosinase of fermented Rhodiola rosea, fermented Lonicera japonica, ethanol extract of Lonicera japonica, and ethanol extract of Rhodiola rosea were 0.78, 4.07, 6.93, and >10 mg/ml, respectively. The DPPH scavenging effects of fermented Rhodiola rosea (ED50 = 0.073 mg/ml and fermented Lonicera japonica (ED50 = 0.207 mg/ml were stronger than effects of their respective ethanol extracts. Furthermore, the scavenging effect increases with the presence of high content of total phenol. However, the superoxide scavenging effects of fermented Rhodiola rosea was less than effects of fermented Lonicera japonica. The results indicated that fermentation of Rhodiola rosea and Lonicera japonica can be considered as an effective biochemical process for application in food, drug, and cosmetics.

  19. Tyrosinase inhibitory effect and antioxidative activities of fermented and ethanol extracts of Rhodiola rosea and Lonicera japonica.

    Science.gov (United States)

    Chen, Yuh-Shuen; Liou, Hua-Chian; Chan, Chin-Feng

    2013-01-01

    This is the first study to investigate the biological activities of fermented extracts of Rhodiola rosea L. (Crassulaceae) and Lonicera japonica Thunb. (Caprifoliaceae). Alcaligenes piechaudii CC-ESB2 fermented and ethanol extracts of Rhodiola rosea and Lonicera japonica were prepared and the antioxidative activities of different concentrations of samples were evaluated using in vitro antioxidative assays. Tyrosinase inhibition was determined by using the dopachrome method with L-DOPA as substrate. The results demonstrated that inhibitory effects (ED50 values) on mushroom tyrosinase of fermented Rhodiola rosea, fermented Lonicera japonica, ethanol extract of Lonicera japonica, and ethanol extract of Rhodiola rosea were 0.78, 4.07, 6.93, and >10 mg/ml, respectively. The DPPH scavenging effects of fermented Rhodiola rosea (ED50 = 0.073 mg/ml) and fermented Lonicera japonica (ED50 = 0.207 mg/ml) were stronger than effects of their respective ethanol extracts. Furthermore, the scavenging effect increases with the presence of high content of total phenol. However, the superoxide scavenging effects of fermented Rhodiola rosea was less than effects of fermented Lonicera japonica. The results indicated that fermentation of Rhodiola rosea and Lonicera japonica can be considered as an effective biochemical process for application in food, drug, and cosmetics.

  20. Inhibitory effects of ascorbic acid, vitamin E, and vitamin B-complex on the biological activities induced by Bothrops venom.

    Science.gov (United States)

    Oliveira, Carlos Henrique de Moura; Assaid Simão, Anderson; Marcussi, Silvana

    2016-01-01

    Natural compounds have been widely studied with the aim of complementing antiophidic serum therapy. The present study evaluated the inhibitory potential of ascorbic acid and a vitamin complex, composed of ascorbic acid, vitamin E, and all the B-complex vitamins, on the biological activities induced by snake venoms. The effect of vitamins was evaluated on the phospholipase, proteolytic, coagulant, and fibrinogenolytic activities induced by Bothrops moojeni (Viperidae), B. jararacussu, and B. alternatus snake venoms, and the hemagglutinating activity induced by B. jararacussu venom. The vitamin complex (1:5 and 1:10 ratios) totally inhibited the fibrinogenolytic activity and partially the phospholipase activity and proteolytic activity on azocasein induced by the evaluated venoms. Significant inhibition was observed in the coagulation of human plasma induced by venoms from B. alternatus (1:2.5 and 1:5, to vitamin complex and ascorbic acid) and B. moojeni (1:2.5 and 1:5, to vitamin complex and ascorbic acid). Ascorbic acid inhibited 100% of the proteolytic activities of B. moojeni and B. alternatus on azocasein, at 1:10 ratio, the effects of all the venoms on fibrinogen, the hemagglutinating activity of B. jararacussu venom, and also extended the plasma coagulation time induced by all venoms analyzed. The vitamins analyzed showed relevant in vitro inhibitory potential over the activities induced by Bothrops venoms, suggesting their interaction with toxins belonging to the phospholipase A2, protease, and lectin classes. The results can aid further research in clarifying the possible mechanisms of interaction between vitamins and snake enzymes.

  1. Inhibitory effects of rosmarinic acid on pterygium epithelial cells through redox imbalance and induction of extrinsic and intrinsic apoptosis.

    Science.gov (United States)

    Chen, Ya-Yu; Tsai, Chia-Fang; Tsai, Ming-Chu; Hsu, Yu-Wen; Lu, Fung-Jou

    2017-07-01

    Pterygium is a common tumor-like ocular disease, which may be related to exposure to chronic ultraviolet (UV) radiation. Although the standard treatment for pterygium is surgical intervention, the recurrence rate of pterygium is high when no effective inhibitory drug is used after surgery. Rosmarinic acid (RA) is a polyphenol antioxidant with many biological activities, including anti-UV and anti-tumor properties. This study aimed to examine the inhibitory effects of RA on pterygium epithelial cells (PECs). Methylthiazolyldiphenyl-tetrazolium bromide (MTT) assay was used to examine the cell cytotoxicity of PECs after RA treatment. A fluorescent probe, DCFH-DA (2',7'-dichlorofluorescin diacetate), was stained with PECs to measure intracellular reactive oxygen species (ROS) levels. Antioxidant activity assays were used to measure the levels of superoxide dismutase (SOD) and catalase (CAT) in PECs. Western blot analysis was used to determine the protein expression of nuclear factor E2-related factor 2 (Nrf2), heme oxygenase 1 (HO-1), quinone acceptor oxidoreductase 1 (NQO1), and apoptosis-associated proteins. RA significantly reduced the cell viability of the PECs. Treatment with RA remarkably increased the Nrf2 protein expression levels in the nucleus, HO-1 and NQO1 protein expression levels, and the activities of SOD and CAT. As a result, intracellular ROS levels in PECs were decreased. Additionally, the induction of extrinsic apoptosis on PECs by RA was associated with increasing expressions levels of Fas, Fas-associated protein with death domain (FADD), tumor necrosis factor-alpha (TNF-α), and caspase 8 protein. Moreover, the induction of intrinsic apoptotic cell death in PECs was confirmed through upregulation of cytochrome c, Bax, caspase 9, and caspase 3 and downregulation of Bcl-2 and pro-caspase 3. Our study demonstrated that RA could inhibit the viability of PECs through regulation of extrinsic and intrinsic apoptosis pathways. Therefore, RA may have

  2. Inhibitory effect of iron withdrawal by chelation on the growth of human and murine mammary carcinoma and fibrosarcoma cells.

    Science.gov (United States)

    Power Coombs, Melanie R; Grant, Taryn; Greenshields, Anna L; Arsenault, Daniel J; Holbein, Bruce E; Hoskin, David W

    2015-10-01

    Since iron uptake is essential for cell growth, rapidly dividing cancer cells are sensitive to iron depletion. To explore the effect of iron withdrawal on cancer cell growth, mouse and human mammary carcinoma cells (4T1 and MDA-MB-468, respectively) and mouse and human fibrosarcoma cells (L929 and HT1080, respectively) were cultured in the absence or presence of DIBI, a novel iron-chelating polymer containing hydroxypyridinone iron-ligand functionality. Cell growth was measured by a colorimetric assay for cell metabolic activity. DIBI-treated 4T1, MDA-MB-468, L929 and HT1080 cells, as well as their normal counterparts, showed a dose- and time-dependent reduction in growth that was selective for human cancer cells and mouse fibrosarcoma cells. The inhibitory effect of DIBI on fibrosarcoma and mammary carcinoma cell growth was reversed by addition of exogenous iron in the form of iron (III) citrate, confirming the iron selectivity of DIBI and that its inhibitory activity was iron-related. Fibrosarcoma and mammary carcinoma cell growth inhibition by DIBI was associated with S-phase cell cycle arrest and low to moderate levels of cell death by apoptosis. Consistent with apoptosis induction following DIBI-mediated iron withdrawal, fibrosarcoma and mammary carcinoma cells exhibited mitochondrial membrane permeabilization. A comparison of DIBI to other iron chelators showed that DIBI was superior to deferiprone and similar to or better than deferoxamine for inhibition of fibrosarcoma and mammary carcinoma cell growth. These findings suggest that iron withdrawal from the tumor microenvironment with a selective and potent iron chelator such as DIBI may prevent or inhibit tumor progression. Copyright © 2015 Elsevier Inc. All rights reserved.

  3. 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.

  4. Profound Impacts of AN Arctic Face Lift

    Science.gov (United States)

    Nghiem, Son

    Son Nghiem, son.v.nghiem@jpl.nasa.gov Jet Propulsion Laboratory, California Institute of Technology, Pasadena, California, United States The ice cover on the Arctic Ocean has undergone a face lift that removes much of the older and thicker perennial ice and replaces it with the younger and thinner seasonal ice. Although the sea ice cover is a thin skin compared to the depth of the Arctic Ocean, this face lift exerts profound change in the Arctic environment. Here, we present scatterometer remote sensing of Arctic sea ice change and its implication on chemical processes from the ice surface to the troposphere extending into the internal continental land. In the context of a half century change, the extent of perennial ice declines at rate of 0.5 million km2 per decade in the 1970s-1990s while there is no discernable trend in the 1950s-1960s. Abruptly, the rate of decrease has tripled to 1.5 million km2 per decade in the 2000s. A record was set in the reduction of Arctic perennial ice extent in winter 2008. By 1 March 2008, perennial ice extent was reduced by one million km2 compared to that at the same time in 2007. On 1 May 2009, perennial ice extent was reduced to 2.1 million km2 , which is a virtual tie to 2.2 million km2 of perennial ice extent on 1 May 2008 given the uncertainty of ±0.2 million km2 . Although the extent of perennial ice extent is similar, its distribution is quite different, with a significant perennial ice pack in the Beaufort Sea in 2008, and in contrast a large expanse of perennial ice along the Transpolar Drift Stream in 2009. The continuing drastic reduction of perennial ice significantly decreases the overall surface albedo, resulting in enhanced solar heat absorption in spring and summer, which further decreases the Arctic ice pack through the ice-albedo feedback mechanism and ice melt from the underside due to oceanic thermodynamic interactions. Satellite maps of sea ice class distribution show the closely conformation with patterns of

  5. Observations on Working Psychoanalytically with a Profoundly Amnesic Patient.

    Science.gov (United States)

    Moore, Paul A; Salas, Christian E; Dockree, Suvi; Turnbull, Oliver H

    2017-01-01

    Individuals with profound amnesia are markedly impaired in explicitly recalling new episodic events, but appear to preserve the capacity to use information from other sources. Amongst these preserved capacities is the ability to form new memories of an emotional nature - a skill at the heart of developing and sustaining interpersonal relationships. The psychoanalytic study of individuals with profound amnesia might contribute to the understanding the importance of each memory system, including effects on key analytic processes such as transference and countertransference. However, psychoanalytic work in the presence of profound amnesia might also require important technical modifications. In the first report of its kind, we describe observations from a long term psychoanalytic process (72 sessions) with an individual (JL) who has profound amnesia after an anoxic episode. The nature of therapy was shaped by JL's impairment in connecting elements that belong to distant (and even relatively close) moments in the therapeutic process. However, we were also able to document areas of preservation, in what appears to be a functioning therapeutic alliance. As regards transference, the relationship between JL and his analyst can be viewed as the evolution of a narcissistic transference, and case material is provided that maps this into three phases: (i) rejecting; (ii) starting to take in; and (iii) full use of the analytic space - where each phase exhibits differing degrees of permeability between JL and the analyst. This investigation appears to have important theoretical implications for psychoanalytic practice, and for psychotherapy in general - and not only with regard to brain injured populations. We especially note that it raises questions concerning the mechanism of therapeutic action in psychoanalysis and psychotherapy, and the apparent unimportance of episodic memory for many elements of therapeutic change.

  6. Observations on Working Psychoanalytically with a Profoundly Amnesic Patient

    Science.gov (United States)

    Moore, Paul A.; Salas, Christian E.; Dockree, Suvi; Turnbull, Oliver H.

    2017-01-01

    Individuals with profound amnesia are markedly impaired in explicitly recalling new episodic events, but appear to preserve the capacity to use information from other sources. Amongst these preserved capacities is the ability to form new memories of an emotional nature – a skill at the heart of developing and sustaining interpersonal relationships. The psychoanalytic study of individuals with profound amnesia might contribute to the understanding the importance of each memory system, including effects on key analytic processes such as transference and countertransference. However, psychoanalytic work in the presence of profound amnesia might also require important technical modifications. In the first report of its kind, we describe observations from a long term psychoanalytic process (72 sessions) with an individual (JL) who has profound amnesia after an anoxic episode. The nature of therapy was shaped by JL’s impairment in connecting elements that belong to distant (and even relatively close) moments in the therapeutic process. However, we were also able to document areas of preservation, in what appears to be a functioning therapeutic alliance. As regards transference, the relationship between JL and his analyst can be viewed as the evolution of a narcissistic transference, and case material is provided that maps this into three phases: (i) rejecting; (ii) starting to take in; and (iii) full use of the analytic space – where each phase exhibits differing degrees of permeability between JL and the analyst. This investigation appears to have important theoretical implications for psychoanalytic practice, and for psychotherapy in general – and not only with regard to brain injured populations. We especially note that it raises questions concerning the mechanism of therapeutic action in psychoanalysis and psychotherapy, and the apparent unimportance of episodic memory for many elements of therapeutic change. PMID:28890703

  7. Observations on Working Psychoanalytically with a Profoundly Amnesic Patient

    Directory of Open Access Journals (Sweden)

    Paul A. Moore

    2017-08-01

    Full Text Available Individuals with profound amnesia are markedly impaired in explicitly recalling new episodic events, but appear to preserve the capacity to use information from other sources. Amongst these preserved capacities is the ability to form new memories of an emotional nature – a skill at the heart of developing and sustaining interpersonal relationships. The psychoanalytic study of individuals with profound amnesia might contribute to the understanding the importance of each memory system, including effects on key analytic processes such as transference and countertransference. However, psychoanalytic work in the presence of profound amnesia might also require important technical modifications. In the first report of its kind, we describe observations from a long term psychoanalytic process (72 sessions with an individual (JL who has profound amnesia after an anoxic episode. The nature of therapy was shaped by JL’s impairment in connecting elements that belong to distant (and even relatively close moments in the therapeutic process. However, we were also able to document areas of preservation, in what appears to be a functioning therapeutic alliance. As regards transference, the relationship between JL and his analyst can be viewed as the evolution of a narcissistic transference, and case material is provided that maps this into three phases: (i rejecting; (ii starting to take in; and (iii full use of the analytic space – where each phase exhibits differing degrees of permeability between JL and the analyst. This investigation appears to have important theoretical implications for psychoanalytic practice, and for psychotherapy in general – and not only with regard to brain injured populations. We especially note that it raises questions concerning the mechanism of therapeutic action in psychoanalysis and psychotherapy, and the apparent unimportance of episodic memory for many elements of therapeutic change.

  8. Revealing the brain's adaptability and the transcranial direct current stimulation facilitating effect in inhibitory control by multiscale entropy.

    Science.gov (United States)

    Liang, Wei-Kuang; Lo, Men-Tzung; Yang, Albert C; Peng, Chung-Kang; Cheng, Shih-Kuen; Tseng, Philip; Juan, Chi-Hung

    2014-04-15

    The abilities to inhibit impulses and withdraw certain responses are critical for human's survival in a fast-changing environment. These processes happen fast, in a complex manner, and sometimes are difficult to capture with fMRI or mean electrophysiological brain signal alone. Therefore, an alternative measure that can reveal the efficiency of the neural mechanism across multiple timescales is needed for the investigation of these brain functions. The present study employs a new approach to analyzing electroencephalography (EEG) signal: the multiscale entropy (MSE), which groups data points with different timescales to reveal any occurrence of repeated patterns, in order to theoretically quantify the complexity (indicating adaptability and efficiency) of neural systems during the process of inhibitory control. From this MSE perspective, EEG signals of successful stop trials are more complex and information rich than that of unsuccessful stop trials. We further applied transcranial direct current stimulation (tDCS), with anodal electrode over presupplementary motor area (preSMA), to test the relationship between behavioral modification with the complexity of EEG signals. We found that tDCS can further increase the EEG complexity of the frontal lobe. Furthermore, the MSE pattern was found to be different between high and low performers (divided by their stop-signal reaction time), where the high-performing group had higher complexity in smaller scales and less complexity in larger scales in comparison to the low-performing group. In addition, this between-group MSE difference was found to interact with the anodal tDCS, where the increase of MSE in low performers benefitted more from the anodal tDCS. Together, the current study demonstrates that participants who suffer from poor inhibitory control can efficiently improve their performance with 10min of electrical stimulation, and such cognitive improvement can be effectively traced back to the complexity within the

  9. 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.

  10. 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 ...

  11. Cytotoxic effects of peanut phenolics possessing histone deacetylase inhibitory activity in breast and cervical cancer cell lines.

    Science.gov (United States)

    Saenglee, Somprasong; Jogloy, Sanun; Patanothai, Aran; Leid, Mark; Senawong, Thanaset

    2016-12-01

    Epigenetic histone modifications are considered as a promising avenue for cancer preventive and therapeutic strategies. The purpose of this study was to evaluate the antiproliferative and histone deacetylase (HDAC) inhibitory activity of selected peanut phenolics, including p-coumaric acid, ferulic acid, sinapinic acid and resveratrol, in MCF-7 and HeLa cells. The cytotoxic and HDAC inhibitory activities were assessed by MTT assays, flow cytometric analyses of cell cycle arrest and apoptosis induction, and western blotting. The results showed that all four phenolics inhibited proliferation of both MCF-7 and HeLa cells in a dose-dependent manner. Among the phenolics tested, resveratrol was the most effective in inhibiting growth of cancer cells. Treatment with all phenolics resulted in histone H3 hyperacetylation in both cell lines, indicating potential for HDAC inhibition. These phenolics induced apoptosis in both MCF-7 and HeLa cells in a concentration-dependent manner. Moreover, all phenolics induced G0/G1-phase arrest of the cell cycle in MCF-7 cells while p-coumaric and ferulic acids caused S-phase arrest in HeLa cells. Exposure to p-coumaric acid increased p53 and p21 expression but decreased CDK4 levels in both cell types, which could result in the observed G0/G1 arrest. Moreover, inhibition of ERK1/2 phosphorylation by ferulic acid and resveratrol contributed to cell growth inhibition. Peanut phenolics appear to influence the extent of histone acetylation in MCF-7 and HeLa cells, and this activity modulates multiple pathways that are implicated in cancer prevention. Copyright © 2016 Institute of Pharmacology, Polish Academy of Sciences. All rights reserved.

  12. Inhibitory effect of magnesium L-ascorbyl-2-phosphate (VC-PMG) on melanogenesis in vitro and in vivo.

    Science.gov (United States)

    Kameyama, K; Sakai, C; Kondoh, S; Yonemoto, K; Nishiyama, S; Tagawa, M; Murata, T; Ohnuma, T; Quigley, J; Dorsky, A; Bucks, D; Blanock, K

    1996-01-01

    An inhibitory effect of ascorbic acid (AsA) on melanogenesis has been described. However, AsA is quickly oxidized and decomposed in aqueous solution and thus is not generally useful as a depigmenting agent. Our purpose was to examine the effect on pigmentation of magnesium-L-ascorbyl-2-phosphate (VC-PMG), a stable derivative of AsA. Percutaneous absorption of VC-PMG was examined in dermatomed human skin, and its effect on melanin production by mammalian tyrosinase and human melanoma cells in culture was also measured. A 10% VC-PMG cream was applied to the patients. VC-PMG suppressed melanin formation by tyrosinase and melanoma cells. In situ experiments demonstrated that VC-PMG cream was absorbed into the epidermis and that 1.6% remained 48 hours after application. The lightening effect was significant in 19 of 34 patients with chloasma or senile freckles and in 3 of 25 patients with normal skin. VC-PMG is effective in reducing skin hyperpigmentation in some patients.

  13. Diterpenoids and phenylethanoid glycosides from the roots of Clerodendrum bungei and their inhibitory effects against angiotensin converting enzyme and α-glucosidase.

    Science.gov (United States)

    Liu, Qing; Hu, Hai-Jun; Li, Peng-Fei; Yang, Ying-Bo; Wu, Li-Hong; Chou, Gui-Xin; Wang, Zheng-Tao

    2014-07-01

    Abietane derivatives, bungnates A, B, 15-dehydrocyrtophyllone A and 15-dehydro-17-hydroxycyrtophyllone A, and two phenylethanoid glycosides, bunginoside A and 3″,4″-di-O-acetylmartynoside, together with nine known abietane derivatives and fourteen known phenylethanoid glycosides, were isolated from dried roots of Clerodendrum bungei. Their structures were determined on the basis of detailed spectroscopic analyses and acidic hydrolysis. The absolute configuration of bunginoside A was established from analysis of CD data. Selected compounds were evaluated for inhibitory effects against angiotensin converting enzyme (ACE) and α-glucosidase. 15-Dehydrocyrtophyllone A showed an ACE inhibitory effect, and verbascoside, leucosceptoside A and isoacteoside exhibited strong inhibitory capacity against α-glucosidase. Copyright © 2014 Elsevier Ltd. All rights reserved.

  14. Comparative evaluation of inhibitory effect of curcumin and doxycycline on matrix metalloproteinase-9 activity in chronic periodontitis

    Directory of Open Access Journals (Sweden)

    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.

  15. inhibitory effects of citral, cinnamaldehyde, and tea polyphenols on mixed biofilm formation by foodborne Staphylococcus aureus and Salmonella enteritidis.

    Science.gov (United States)

    Zhang, Hongmei; Zhou, Wenyuan; Zhang, Wenyan; Yang, Anlin; Liu, Yanlan; Jiang, Yan; Huang, Shaosong; Su, Jianyu

    2014-06-01

    Biofilms are significant hazards in the food industry. In this study, we investigated the effects of food additive such as citral, cinnamaldehyde, and tea polyphenols on mixed biofilm formation by foodborne Staphylococcus aureus and Salmonella serotype Enteritidis. The adhesion rates of mixed strains in sub-MIC of additives were determined by a microtiter plate assay and bacterial communication signal autoinducer 2 (AI-2) production via a bioluminescence reporter Vibrio harveyi BB170. The structure of mixed biofilm was analyzed using scanning electron microscopy. The effect of the disinfectants hydrogen peroxide, sodium hypochlorite, and peracetic acid was tested on the mixed biofilm. Our results demonstrated that citral, cinnamaldehyde, and tea polyphenols were able to significantly inhibit mixed biofilm formation, while citral could reduce the synthesis of AI-2. Conversely, we observed a significant increase in AI-2 mediated by cinnamaldehyde. Tea polyphenols at lower concentrations induced AI-2 synthesis; however, AI-2 synthesis was significantly inhibited at higher concentrations (300 m g/ml). Food additives inhibited the adhesion of mixed bacteria on stainless steel chips and increased the sensitivity of the mixed biofilm to disinfectants. In conclusion, citral, cinnamaldehyde, and tea polyphenols had strong inhibitory effects on mixed biofilm formation and also enhanced the effect of disinfectant on mixed biofilm formation. This study provides a scientific basis for the application of natural food additives to control biofilm formation of foodborne bacteria.

  16. 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.

  17. Comparative evaluation of inhibitory effect of curcumin and doxycycline on matrix metalloproteinase-9 activity in chronic periodontitis.

    Science.gov (United States)

    Guru, Sanjeela Rakshith; Kothiwale, Shaila V; Saroch, Nitin; Guru, Rakshith Chander

    2017-01-01

    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. 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 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. 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.

  18. Pomegranate juice protects macrophages from triglyceride accumulation: inhibitory effect on DGAT1 activity and on triglyceride biosynthesis.

    Science.gov (United States)

    Rosenblat, Mira; Aviram, Michael

    2011-01-01

    To analyze the effects of pomegranate juice (PJ) and punicalagin on macrophage triglyceride metabolism. Triglyceride metabolism was analyzed in PJ- or punicalagin-treated J774A.1 macrophages or in mouse peritoneal macrophages (MPM) harvested from C57BL/6 mice or from paraoxonase 2 (PON2)-deficient mice. PJ (0-50 μM) significantly and dose-dependently decreased the triglyceride content and triglyceride biosynthesis rate in J774A.1 macrophages or in C57BL/6 MPM by about 30%. Similarly, punicalagin, the major PJ polyphenol, inhibited the MPM triglyceride biosynthesis rate by 40%. The triglyceride hydrolytic rate, however, was not significantly affected by PJ or punicalagin. The activity of diacylglycerol acyltransferase 1 (DGAT1; the rate-limiting enzyme in triglyceride biosynthesis) was significantly inhibited, by 54%, in C57BL/6 MPM that were treated with 50 μM PJ or punicalagin, with no significant effect on DGAT1 mRNA or protein expression. Both PJ and punicalagin increased (1.7-fold) MPM PON2 mRNA expression, and PON2 was previously shown to inhibit DGAT1 activity. However, the addition of PJ or punicalagin (50 μM) to microsomes from PON2-deficient MPM still resulted in a significant reduction (50-58%) in DGAT1 activity. We conclude that the inhibitory effect of PJ on triglyceride biosynthesis could be attributed to a direct effect of PJ on DGAT1 activity. Copyright © 2011 S. Karger AG, Basel.

  19. 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.

  20. 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.