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Sample records for extract significantly inhibited

  1. Inhibition of aluminum corrosion using Opuntia extract

    Energy Technology Data Exchange (ETDEWEB)

    El-Etre, A.Y

    2003-11-01

    The inhibitive action of the mucilage extracted from the modified stems of prickly pears, toward acid corrosion of aluminum, is tested using weight loss, thermometry, hydrogen evolution and polarization techniques. It was found that the extract acts as a good corrosion inhibitor for aluminum corrosion in 2.0 M HCl solution. The inhibition action of the extract was discussed in view of Langmuir adsorption isotherm. It was found that the adsorption of the extract on aluminum surface is a spontaneous process. The inhibition efficiency (IE) increases as the extract concentration is increased. The effect of temperature on the IE was studied. It was found that the presence of extract increases the activation energy of the corrosion reaction. Moreover, the thermodynamic parameters of the adsorption process were calculated. It was found also that the Opuntia extract provides a good protection to aluminum against pitting corrosion in chloride ion containing solutions.

  2. Hawthorn extract inhibits human isolated neutrophil functions.

    Science.gov (United States)

    Dalli, Ernesto; Milara, Javier; Cortijo, Julio; Morcillo, Esteban J; Cosín-Sales, Juan; Sotillo, José Francisco

    2008-06-01

    Hawthorn extract is a popular herbal medicine given as adjunctive treatment for chronic heart failure. In contrast to the cardiac properties of hawthorn extract, its anti-inflammatory effect has been scarcely investigated. This study examines the effects of a dry extract of leaves and flowers of Crataegus laevigata on various functional outputs of human neutrophils in vitro. Incubation of human neutrophils obtained from peripheral blood of healthy donors with C. laevigata extract (0.75-250 microg/ml) inhibited N-formyl-Met-Leu-Phe (FMLP)-induced superoxide anion generation, elastase release and chemotactic migration with potency values of 43.6, 21.9, and 31.6 microg/ml, respectively. By contrast, serum-opsonized zymosan-induced phagocytosis was unaltered by plant extract. C. laevigata extract (125 microg/ml) reduced FMLP-induced leukotriene B(4) production and lipopolysaccharide-induced generation of tumour necrosis factor-alpha and interleukin-8. Extract inhibited FMLP-induced intracellular calcium signal with potency of 17.4 microg/ml. Extract also markedly inhibited the extracellular calcium entry into calcium-depleted neutrophils, and the thapsigargin-induced intracellular calcium response. In conclusion, C. laevigata extract inhibited various functional outputs of activated human neutrophils which may be relevant to the pathophysiology of cardiac failure.

  3. Ginger extract inhibits LPS induced macrophage activation and function

    Directory of Open Access Journals (Sweden)

    Bruch David

    2008-01-01

    Full Text Available Abstract Background Macrophages play a dual role in host defence. They act as the first line of defence by mounting an inflammatory response to antigen exposure and also act as antigen presenting cells and initiate the adaptive immune response. They are also the primary infiltrating cells at the site of inflammation. Inhibition of macrophage activation is one of the possible approaches towards modulating inflammation. Both conventional and alternative approaches are being studied in this regard. Ginger, an herbal product with broad anti inflammatory actions, is used as an alternative medicine in a number of inflammatory conditions like rheumatic disorders. In the present study we examined the effect of ginger extract on macrophage activation in the presence of LPS stimulation. Methods Murine peritoneal macrophages were stimulated by LPS in presence or absence of ginger extract and production of proinflammatory cytokines and chemokines were observed. We also studied the effect of ginger extract on the LPS induced expression of MHC II, B7.1, B7.2 and CD40 molecules. We also studied the antigen presenting function of ginger extract treated macrophages by primary mixed lymphocyte reaction. Results We observed that ginger extract inhibited IL-12, TNF-α, IL-1β (pro inflammatory cytokines and RANTES, MCP-1 (pro inflammatory chemokines production in LPS stimulated macrophages. Ginger extract also down regulated the expression of B7.1, B7.2 and MHC class II molecules. In addition ginger extract negatively affected the antigen presenting function of macrophages and we observed a significant reduction in T cell proliferation in response to allostimulation, when ginger extract treated macrophages were used as APCs. A significant decrease in IFN-γ and IL-2 production by T cells in response to allostimulation was also observed. Conclusion In conclusion ginger extract inhibits macrophage activation and APC function and indirectly inhibits T cell activation.

  4. HIV-1 inhibition by extracts of Clusiaceae species from Mexico.

    Science.gov (United States)

    Huerta-Reyes, Maira; Basualdo, Maria del Carmen; Lozada, Lucio; Jimenez-Estrada, Manuel; Soler, Carmen; Reyes-Chilpa, Ricardo

    2004-06-01

    The organic plant extracts of 21 species of Clusiaceae from Mexico were screened for anti HIV-1 reverse transcriptase activity in a non-radioactive immuno colorimetric assay. The extracts of 5 species (23.8%) exhibited significant inhibition (> or =70%) of HIV-1 RT activity; of these, only 4 extracts showed reduced toxicity to human lymphocytic MT2 cells and were further tested as inhibitors of HIV-1 IIIb/LAV replication in a cellular system. The best extracts were Calophyllum brasiliense (hexane) and Clusia quadrangula (CH(2)Cl(2)-MeOH) which inhibited HIV-1 RT (IC(50)=29.6 microg/ml and 42 microg/ml), and showed an EC(50)=92.5 microg/ml and 91 microg/ml, respectively, on MT2 cells. However, only Calophyllum brasiliense hexane extract showed significant inhibition on viral replication (ED(50)=37.1 microg/ml), while Clusia quadrangula was less active (ED(50)=124 microg/ml). These results support the idea that plant extracts represent a valuable source of potential anti HIV compounds.

  5. Olive leaf extract inhibits lead poisoning-induced brain injury**

    Institute of Scientific and Technical Information of China (English)

    Yu Wang; Shengqing Wang; Wenhui Cui; Jiujun He; Zhenfu Wang; Xiaolu Yang

    2013-01-01

    Olive leaves have an antioxidant capacity, and olive leaf extract can protect the blood, spleen and hippocampus in lead-poisoned mice. However, little is known about the effects of olive leaf extract on lead-induced brain injury. This study was designed to determine whether olive leaf extract can inhibit lead-induced brain injury, and whether this effect is associated with antioxidant capacity. First, we established a mouse model of lead poisoning by continuous intragastric administration of lead acetate for 30 days. Two hours after successful model establishment, lead-poisoned mice were given olive leaf extract at doses of 250, 500 or 1 000 mg/kg daily by intragastric administration for 50 days. Under the transmission electron microscope, olive leaf extract attenuated neuronal and capil ary injury and reduced damage to organel es and the matrix around the capil aries in the frontal lobe of the cerebral cortex in the lead-poisoned mice. Olive leaf extract at a dose of 1 000 mg/kg had the greatest protective effect. Spectrophotometry showed that olive leaf extract significantly in-creased the activities of superoxide dismutase, catalase, alkaline phosphatase and acid phospha-tase, while it reduced malondialdehyde content, in a dose-dependent manner. Furthermore, im-munohistochemical staining revealed that olive leaf extract dose-dependently decreased Bax pro-tein expression in the cerebral cortex of lead-poisoned mice. Our findings indicate that olive leaf extract can inhibit lead-induced brain injury by increasing antioxidant capacity and reducing apop-tosis.

  6. Inhibition of Aldose Reductase by Gentiana lutea Extracts

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    Chandrasekhar Akileshwari

    2012-01-01

    Full Text Available Accumulation of intracellular sorbitol due to increased aldose reductase (ALR2 activity has been implicated in the development of various secondary complications of diabetes. Thus, ALR2 inhibition could be an effective strategy in the prevention or delay of certain diabetic complications. Gentiana lutea grows naturally in the central and southern areas of Europe. Its roots are commonly consumed as a beverage in some European countries and are also known to have medicinal properties. The water, ethanol, methanol, and ether extracts of the roots of G. lutea were subjected to in vitro bioassay to evaluate their inhibitory activity on the ALR2. While the ether and methanol extracts showed greater inhibitory activities against both rat lens and human ALR2, the water and ethanol extracts showed moderate inhibitory activities. Moreover, the ether and methanol extracts of G. lutea roots significantly and dose-dependently inhibited sorbitol accumulation in human erythrocytes under high glucose conditions. Molecular docking studies with the constituents commonly present in the roots of G. lutea indicate that a secoiridoid glycoside, amarogentin, may be a potential inhibitor of ALR2. This is the first paper that shows G. lutea extracts exhibit inhibitory activity towards ALR2 and these results suggest that Gentiana or its constituents might be useful to prevent or treat diabetic complications.

  7. Extraction conditions of white rose petals for the inhibition of enzymes related to skin aging.

    Science.gov (United States)

    Choi, Ehn-Kyoung; Guo, Haiyu; Choi, Jae-Kwon; Jang, Su-Kil; Shin, Kyungha; Cha, Ye-Seul; Choi, Youngjin; Seo, Da-Woom; Lee, Yoon-Bok; Joo, Seong-So; Kim, Yun-Bae

    2015-09-01

    In order to assess inhibitory potentials of white rose petal extracts (WRPE) on the activities of enzymes related to dermal aging according to the extraction conditions, three extraction methods were adopted. WRPE was prepared by extracting dried white rose (Rosa hybrida) petals with 50% ethanol (WRPE-EtOH), Pectinex® SMASH XXL enzyme (WRPE-enzyme) or high temperature-high pressure (WRPE-HTHP). In the inhibition of matrix metalloproteinase-1, although the enzyme activity was fully inhibited by all 3 extracts at 100 µg/mL in 60 min, partial inhibition (50-70%) was achieved only by WRPE-EtOH and WRPE-enzyme at 50 µg/mL. High concentrations (≥250 µg/mL) of all 3 extracts markedly inhibited the elastase activity. However, at low concentrations (15.6-125 µg/mL), only WRPE-EtOH inhibited the enzyme activity. Notably, WRPE-EtOH was superior to WRPE-enzyme and WRPE-HTHP in the inhibition of tyrosinase. WRPE-EtOH significantly inhibited the enzyme activity from 31.2 µM, reaching 80% inhibition at 125 µM. In addition to its strong antioxidative activity, the ethanol extract of white rose petals was confirmed to be effective in inhibiting skin aging-related enzymes. Therefore, it is suggested that WRPE-EtOH could be a good candidate for the improvement of skin aging such as wrinkle formation and pigmentation.

  8. Evaluation of antioxidant activity of Ruta graveolens L. extract on inhibition of lipid peroxidation and DPPH radicals and the effects of some external factors on plant extract's potency.

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    S. Mohammadi- Motamed

    2014-01-01

    Full Text Available The antioxidant properties of Ruta graveolens L. were evaluated by two different methods; free radical scavenging using DPPH and inhibition of lipid peroxidation by the ferric thiocyanate method. The IC50 value of the methanol extract in DPPH inhibition was 200.5 μg/mL which was acceptable in comparison with BHT (41.8 μg/mL. In thiocyanate method, the plant extract demonstrated activity as much as BHT in prevention of lipid peroxidation. Increasing the temperature during extraction, significantly decreased the extract power in inhibition of DPPH radicals. The storage time and temperature had no effect on lipid peroxidation inhibition.

  9. Ginger extract inhibits biofilm formation by Pseudomonas aeruginosa PA14.

    Science.gov (United States)

    Kim, Han-Shin; Park, Hee-Deung

    2013-01-01

    Bacterial biofilm formation can cause serious problems in clinical and industrial settings, which drives the development or screening of biofilm inhibitors. Some biofilm inhibitors have been screened from natural products or modified from natural compounds. Ginger has been used as a medicinal herb to treat infectious diseases for thousands of years, which leads to the hypothesis that it may contain chemicals inhibiting biofilm formation. To test this hypothesis, we evaluated ginger's ability to inhibit Pseudomonas aeruginosa PA14 biofilm formation. A static biofilm assay demonstrated that biofilm development was reduced by 39-56% when ginger extract was added to the culture. In addition, various phenotypes were altered after ginger addition of PA14. Ginger extract decreased production of extracellular polymeric substances. This finding was confirmed by chemical analysis and confocal laser scanning microscopy. Furthermore, ginger extract formed noticeably less rugose colonies on agar plates containing Congo red and facilitated swarming motility on soft agar plates. The inhibition of biofilm formation and the altered phenotypes appear to be linked to a reduced level of a second messenger, bis-(3'-5')-cyclic dimeric guanosine monophosphate. Importantly, ginger extract inhibited biofilm formation in both Gram-positive and Gram-negative bacteria. Also, surface biofilm cells formed with ginger extract detached more easily with surfactant than did those without ginger extract. Taken together, these findings provide a foundation for the possible discovery of a broad spectrum biofilm inhibitor.

  10. Extracts from Flammulina velutipes Inhibit the Adhesion of Pathogenic Fungi to Epithelial Cells

    OpenAIRE

    2016-01-01

    Background: Recently, extracts from natural sources have been tested for their antifungal properties. In this aspect, Flammulina velutipes extracts possess a significant amount of branch-chained carbohydrates with mannose moieties that, hypothetically, can reduce the adhesion. Objective: In this study, we assessed the capacity of extracts from F. velutipes (wild-type AQF-1 and ATCC 34574 as the reference strain) to inhibit the adhesion of S. schenkii and C. albicans to epithelial cells. Mater...

  11. Coeliac disease autoantibodies mediate significant inhibition of tissue transglutaminase.

    LENUS (Irish Health Repository)

    Byrne, Greg

    2012-02-01

    The detection of antibodies directed against tissue transglutaminase (tTG) in serum is a sensitive and specific test for suspected coeliac disease. tTG is a ubiquitous, multifunctional enzyme that has been implicated in many important physiological processes as well as the site-specific deamidation of glutamine residues in gluten-derived peptides. This modification of gluten peptides facilitates their binding to HLA-DQ2, which results in amplification of the T-cell response to gluten. The purpose of this study was to investigate the possibility that patient IgA autoantibodies directed against tTG interfere with the crosslinking activity of the enzyme. IgA autoantibodies against tTG were isolated\\/depleted from patient serum and tested for their capacity to interfere with tTG activity in vitro using a sensitive fluorescence-based activity assay. We have demonstrated that autoantibodies cause significant inhibition of tTG-mediated crosslinking at equimolar and 2:1 ratios of antibody to enzyme.

  12. Climate impacts of oil extraction increase significantly with oilfield age

    Science.gov (United States)

    Masnadi, Mohammad S.; Brandt, Adam R.

    2017-08-01

    Record-breaking temperatures have induced governments to implement targets for reducing future greenhouse gas (GHG) emissions. Use of oil products contributes ~35% of global GHG emissions, and the oil industry itself consumes 3-4% of global primary energy. Because oil resources are becoming increasingly heterogeneous, requiring different extraction and processing methods, GHG studies should evaluate oil sources using detailed project-specific data. Unfortunately, prior oil-sector GHG analysis has largely neglected the fact that the energy intensity of producing oil can change significantly over the life of a particular oil project. Here we use decades-long time-series data from twenty-five globally significant oil fields (>1 billion barrels ultimate recovery) to model GHG emissions from oil production as a function of time. We find that volumetric oil production declines with depletion, but this depletion is accompanied by significant growth--in some cases over tenfold--in per-MJ GHG emissions. Depletion requires increased energy expenditures in drilling, oil recovery, and oil processing. Using probabilistic simulation, we derive a relationship for estimating GHG increases over time, showing an expected doubling in average emissions over 25 years. These trends have implications for long-term emissions and climate modelling, as well as for climate policy.

  13. Characterization and Antioxidant Properties of Six Algerian Propolis Extracts: Ethyl Acetate Extracts Inhibit Myeloperoxidase Activity

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    Yasmina Mokhtaria Boufadi

    2014-02-01

    Full Text Available Because propolis contains many types of antioxidant compounds such as polyphenols and flavonoids, it can be useful in preventing oxidative damages. Ethyl acetate extracts of propolis from several Algerian regions show high activity by scavenging free radicals, preventing lipid peroxidation and inhibiting myeloperoxidase (MPO. By fractioning and assaying ethyl acetate extracts, it was observed that both polyphenols and flavonoids contribute to these activities. A correlation was observed between the polyphenol content and the MPO inhibition. However, it seems that kaempferol, a flavonoid, contributes mainly to the MPO inhibition. This molecule is in a high amount in the ethyl acetate extract and demonstrates the best efficiency towards the enzyme with an inhibiting concentration at 50% of 4 ± 2 µM.

  14. Characterization and Antioxidant Properties of Six Algerian Propolis Extracts: Ethyl Acetate Extracts Inhibit Myeloperoxidase Activity

    Science.gov (United States)

    Boufadi, Yasmina Mokhtaria; Soubhye, Jalal; Riazi, Ali; Rousseau, Alexandre; Vanhaeverbeek, Michel; Nève, Jean; Boudjeltia, Karim Zouaoui; Van Antwerpen, Pierre

    2014-01-01

    Because propolis contains many types of antioxidant compounds such as polyphenols and flavonoids, it can be useful in preventing oxidative damages. Ethyl acetate extracts of propolis from several Algerian regions show high activity by scavenging free radicals, preventing lipid peroxidation and inhibiting myeloperoxidase (MPO). By fractioning and assaying ethyl acetate extracts, it was observed that both polyphenols and flavonoids contribute to these activities. A correlation was observed between the polyphenol content and the MPO inhibition. However, it seems that kaempferol, a flavonoid, contributes mainly to the MPO inhibition. This molecule is in a high amount in the ethyl acetate extract and demonstrates the best efficiency towards the enzyme with an inhibiting concentration at 50% of 4 ± 2 μM. PMID:24514562

  15. Inhibition properties of propolis extracts to some clinically important enzymes.

    Science.gov (United States)

    Baltas, Nimet; Yildiz, Oktay; Kolayli, Sevgi

    2016-01-01

    The present study was conducted to envisage inhibition effects of propolis on the crucial enzymes, urease, xanthine oxidase (XO) and acetylcholinesterase (AChE). Some of the antioxidant properties of the propolis samples were determined using the total phenolic content (TPE) and total flavonoids in the eight different ethanolic propolis extracts (EPE) samples. Inhibition values of the enzymes were expressed as inhibition concentration (IC50; mg/mL or μg/mL) causing 50% inhibition of the enzymes with donepezil, acetohydroxamic acid and allopurinol as reference inhibitors. All the propolis extracts exhibited variable inhibition effects on these enzymes, but the higher the phenolic contents the lower the inhibitions values (IC50 = 0.074 to 1.560 mg/mL). IC50 values of the P5 propolis sample having the highest TPE, obtained from Zonguldak, for AChE, urease and XO were 0.081 ± 0.009, 0.080 ± 0.006 and 0.074 ± 0.011 μg/mL, respectively. The EPE proved to be a good source of inhibitor agents that can be used as natural inhibitors to serve human health.

  16. Cinnamon extract inhibits α-glucosidase activity and dampens postprandial glucose excursion in diabetic rats

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    Thirumurugan Kavitha

    2011-06-01

    Full Text Available Abstract Background α-glucosidase inhibitors regulate postprandial hyperglycemia (PPHG by impeding the rate of carbohydrate digestion in the small intestine and thereby hampering the diet associated acute glucose excursion. PPHG is a major risk factor for diabetic vascular complications leading to disabilities and mortality in diabetics. Cinnamomum zeylanicum, a spice, has been used in traditional medicine for treating diabetes. In this study we have evaluated the α-glucosidase inhibitory potential of cinnamon extract to control postprandial blood glucose level in maltose, sucrose loaded STZ induced diabetic rats. Methods The methanol extract of cinnamon bark was prepared by Soxhlet extraction. Phytochemical analysis was performed to find the major class of compounds present in the extract. The inhibitory effect of cinnamon extract on yeast α-glucosidase and rat-intestinal α-glucosidase was determined in vitro and the kinetics of enzyme inhibition was studied. Dialysis experiment was performed to find the nature of the inhibition. Normal male Albino wistar rats and STZ induced diabetic rats were treated with cinnamon extract to find the effect of cinnamon on postprandial hyperglycemia after carbohydrate loading. Results Phytochemical analysis of the methanol extract displayed the presence of tannins, flavonoids, glycosides, terpenoids, coumarins and anthraquinones. In vitro studies had indicated dose-dependent inhibitory activity of cinnamon extract against yeast α-glucosidase with the IC 50 value of 5.83 μg/ml and mammalian α-glucosidase with IC 50 value of 670 μg/ml. Enzyme kinetics data fit to LB plot pointed out competitive mode of inhibition and the membrane dialysis experiment revealed reversible nature of inhibition. In vivo animal experiments are indicative of ameliorated postprandial hyperglycemia as the oral intake of the cinnamon extract (300 mg/kg body wt. significantly dampened the postprandial hyperglycemia by 78.2% and 52

  17. Automatically extracting the significant aspects evaluated in game reviews

    Science.gov (United States)

    Fong, Chiok Hoong; Ng, Yen Kaow

    2017-04-01

    Understanding the criteria (or "aspects") that reviewers use to evaluate games is important to game developers and publishers, since this will give them important input on how to improve their products. Techniques for the extraction of such aspects have been studied by others, albeit not specific to the gaming industry. In this paper we demonstrate an aspect extraction and analysis system specific to computer games. The system extracts game review texts from a list of known websites and automatically extracts candidate aspects from the review text using techniques from natural language processing and sentiment analysis. It then ranks the candidate aspects using the HITS algorithm. To evaluate the correctness of the extracted aspects, we used the system to calculate an overall score for each game by aggregating its highly-rated aspects, weighted by the importance of the respective aspects. The aggregated scores resulted in a ranking of games, which we compared to a known ranking from a popular website - the rankings showed overall consistency, which suggests that the system has extracted valuable aspects from the reviews. Using the extracted aspect, our system also facilitates the analysis of a game, by evaluating how review articles have rated its performance in these extracted aspects.

  18. Corrosion inhibition of carbon steel by extract of Buddleia perfoliata

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    ROY LOPES-SESENES

    2012-06-01

    Full Text Available Buddleia perfoliata leaves extract has been investigated as a carbon steel corrosion inhibitor in 0.5 M sulfuric acid by using polarization curves, electrochemical impedance spectroscopy and weight-loss tests at different concentrations (0, 100, 200, 300, 400 and 500 ppm and temperatures, namely 25, 40 and 60 °C. Results showthat inhibition efficiency increases as the inhibitor concentration increases, decreases with temperature, and reaches a maximum value after 12 h of exposure, decreasing with a further increase in the exposure time. It was found that the inhibitory effect is due to the presence of tannines on this extract.

  19. Cinnamon extract induces tumor cell death through inhibition of NFκB and AP1

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    Lee Sung

    2010-07-01

    Full Text Available Abstract Background Cinnamomum cassia bark is the outer skin of an evergreen tall tree belonging to the family Lauraceae containing several active components such as essential oils (cinnamic aldehyde and cinnamyl aldehyde, tannin, mucus and carbohydrate. They have various biological functions including anti-oxidant, anti-microbial, anti-inflammation, anti-diabetic and anti-tumor activity. Previously, we have reported that anti-cancer effect of cinnamon extracts is associated with modulation of angiogenesis and effector function of CD8+ T cells. In this study, we further identified that anti-tumor effect of cinnamon extracts is also link with enhanced pro-apoptotic activity by inhibiting the activities NFκB and AP1 in mouse melanoma model. Methods Water soluble cinnamon extract was obtained and quality of cinnamon extract was evaluated by HPLC (High Performance Liquid Chromatography analysis. In this study, we tested anti-tumor activity and elucidated action mechanism of cinnamon extract using various types of tumor cell lines including lymphoma, melanoma, cervix cancer and colorectal cancer in vitro and in vivo mouse melanoma model. Results Cinnamon extract strongly inhibited tumor cell proliferation in vitro and induced active cell death of tumor cells by up-regulating pro-apoptotic molecules while inhibiting NFκB and AP1 activity and their target genes such as Bcl-2, BcL-xL and survivin. Oral administration of cinnamon extract in melanoma transplantation model significantly inhibited tumor growth with the same mechanism of action observed in vitro. Conclusion Our study suggests that anti-tumor effect of cinnamon extracts is directly linked with enhanced pro-apoptotic activity and inhibition of NFκB and AP1 activities and their target genes in vitro and in vivo mouse melanoma model. Hence, further elucidation of active components of cinnamon extract could lead to development of potent anti-tumor agent or complementary and alternative

  20. Inhibition of mild steel corrosion using Jatropha Curcas leaf extract

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    OLORUNFEMI MICHAEL AJAYI

    2014-05-01

    Full Text Available Jatropha Curcas leaf was investigated as a green inhibitor on the degradation of mild steel in 4 M HCl and 4 M H2SO4 aqueous solutions using gasometric technique. Mild steel coupons of dimension 2 × 1.5 cm were immersed in test solutions of uninhibited acid and also those with extract concentrations of 4 ml, 6 ml, 8 ml and 10 ml at 30 oC, for up to 30 minutes. The results showed that as the concentration of the extract increases, there was reduction in the corrosion rate. As the extract concentration increased from 4 ml to 10 ml at 30 minutes exposure, the volume of hydrogen gas evolved decreased from 19.1 cm3 to 11.2 cm3 in H2SO4 medium, while it reduced to 5 cm3 from 9 cm3 in HCl medium. Also, the metal surface-phytoconstituent interaction mechanism showed that 6 minutes is the best exposure time for the adsorption of the extract in both acidic media. The Jatropha Curcas leaf extract was adsorbed on the mild steel surface to inhibit corrosion, while the experimental data obtained at 30 minutes exposure in both acidic media were well fitted with the Langmuir adsorption isotherm. Hence, Jatropha Curcas leaf extract is a good and safe inhibitor in both acidic solutions.

  1. Inhibition of Xanthine Oxidase Activity by Gnaphalium Affine Extract

    Institute of Scientific and Technical Information of China (English)

    Wei-qing Lin; Jian-xiang Xie; Xiao-mu Wu; Lin Yang; Hai-dong Wang

    2014-01-01

    Objective To evaluate the inhibitory effect of Gnaphalium affine extracts on xanthine oxidase (XO) activity in vitro and to analyze the mechanism of this effect. Methods In this in vitro study, Kinetic measurements were performed in 4 different inhibitor concentrations and 5 different xanthine concentrations (60, 100, 200, 300, 400 μmol/L). Dixon and Lineweaver-Burk plot analysis were used to determine Ki values and the inhibition mode for the compounds isolated from Gnaphalium affine extract. Results Four potent xanthine oxidase inhibitors were found in 95% ethanolic (v/v) Gnaphalium affine extract. Among them, the flavone Eupatilin exhibited the strongest inhibitory effect on XO with a inhibition constant (Ki) of 0.37μmol/L, lower than the Ki of allopurinol (4.56 mol/L), a known synthetic XO inhibitor. Apigenin (Ki of 0.56μmol/L, a proportion of 0.0053‰in Gnaphalium affine), luteolin (Ki of 2.63 μmol/L, 0.0032‰ in Gnaphalium affine) and 5-hydroxy-6,7,3’,4’-tetramethoxyflavone (Ki of 3.15μmol/L, 0.0043‰ in Gnaphalium affine) also contributed to the inhibitory effect of Gnaphalium affine extract on XO activity. Conclusions These results suggest that the use of Gnaphalium affine in the treatment of gout could be attributed to its inhibitory effect on XO. This study provides a rational basis for the traditional use of Gnaphalium affine against gout.

  2. Gallic acid is the major component of grape seed extract that inhibits amyloid fibril formation.

    Science.gov (United States)

    Liu, Yanqin; Pukala, Tara L; Musgrave, Ian F; Williams, Danielle M; Dehle, Francis C; Carver, John A

    2013-12-01

    Many protein misfolding diseases, for example, Alzheimer's, Parkinson's and Huntington's, are characterised by the accumulation of protein aggregates in an amyloid fibrillar form. Natural products which inhibit fibril formation are a promising avenue to explore as therapeutics for the treatment of these diseases. In this study we have shown, using in vitro thioflavin T assays and transmission electron microscopy, that grape seed extract inhibits fibril formation of kappa-casein (κ-CN), a milk protein which forms amyloid fibrils spontaneously under physiological conditions. Among the components of grape seed extract, gallic acid was the most active component at inhibiting κ-CN fibril formation, by stabilizing κ-CN to prevent its aggregation. Concomitantly, gallic acid significantly reduced the toxicity of κ-CN to pheochromocytoma12 cells. Furthermore, gallic acid effectively inhibited fibril formation by the amyloid-beta peptide, the putative causative agent in Alzheimer's disease. It is concluded that the gallate moiety has the fibril-inhibitory activity.

  3. AQUEOUS EXTRACTS OF PLANTS IN Colletotrichum gloeosporioides INHIBITION IN VITRO AND IN POSTHARVEST GUAVA

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    FERNANDO HENRIQUE ALVES DA SILVA

    2014-01-01

    Full Text Available The effect of plant aqueous extracts in the control of Colletotrichum gloeosporioides (Penz. Penz. & Sacc. the causal agent of guava anthracnose in, was evaluated in vitro with 1, 2 and 3% aqueous ex- tracts of Azadirachta indica, Nerium oleander, Ocimum gratissimum, Syzygium aromaticum. The experiment was installed in a complete randomized desing in a 3x4 factorial scheme (doses x extracts. For the evaluation, it was calculated the percentage of fungal inhibition. The experiment in vivo was conducted by applying Syzy- gium aromaticum and Azadirachta indica aqueous extract at 2 and 3%, respectively, in three different storage conditions: refrigerated with and without plastic film (PVC, and at ambient conditions. The experiment was installed in a completely randomized design, in a 2x3 factorial scheme (extracts x storage conditions. We evaluated the external appearance and severity of disease, loss of weight and Brix degrees. Syzygium aromati- cum extract at 2% provided 100% of fungal mycelial growth inhibition, and Azadirachta indica extract at the highest dosage (3% inhibited 20.22%. In fruits, there was not significant statistical difference between the ef- fect of extracts on the external appearance and severity of disease, loss of weight and Brix degrees. In relation to the storage conditions, the ones with plastic film and refrigerated differed from the other conditions obtain- ing better external appearance and less severity of disease, lower loss of weight and higher Brix degrees.

  4. Matricaria chamomilla extract inhibits both development of morphine dependence and expression of abstinence syndrome in rats.

    Science.gov (United States)

    Gomaa, Adel; Hashem, Tahia; Mohamed, Mahmoud; Ashry, Esraa

    2003-05-01

    The effect of Matricaria chamomilla (M. chamomilla) on the development of morphine dependence and expression of abstinence was investigated in rats. The frequencies of withdrawal behavioral signs (paw tremor, rearing, teeth chattering, body shakes, ptosis, diarrhea, and urination) and weight loss induced by naloxone challenge were demonstrated in morphine-dependent rats receiving M. chamomilla extract or saline. The withdrawal behavioral manifestations and weight loss were inhibited significantly by chronic co-administration of M. chamomilla extract with morphine. Administration of a single dose of M. chamomilla before the naloxone challenge in morphine-dependent animals abolished the withdrawal behavioral manifestations. The dramatic increase of plasma cAMP induced by naloxone-precipitated abstinence was prevented by chronic co-administration of M. chamomilla extract with morphine. These results suggest that M. chamomilla extract inhibits the development of morphine dependence and expression of abstinence syndrome.

  5. α-Amylase and α-Glucosidase Inhibition by Brown Seaweed (Sargassum sp Extracts

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    Muhammad Firdaus

    2014-12-01

    Full Text Available Inhibition of intestinal α-amylase and α-glucosidase is an important strategy to control post-prandial hyperglycemia associated with diabetes mellitus. In vitro inhibitory effects of crude extracts of seaweed against α-amylase and α-glucosidase were studied. Crude ethyl acetate extracts of Sargassum aquifolium were the stronger inhibitor to α-amylase and α-glucosidase than others. Furthermore, Sargassum aquifolium ethyl acetate extract significantly suppressed the rise in postprandial glucose level after oral administration of glucose in normal rats. The results of this study suggest that the crude Sargassum aquifolium extract may suppress the rise in postprandial hyperglycemia in vivo in part, through inhibition of alpha amylase and glucosidase

  6. Postprandial glycaemia and inhibition of α-glucosidase activity by aqueous extract from Coriandrum sativum.

    Science.gov (United States)

    Brindis, F; González-Andrade, M; González-Trujano, M E; Estrada-Soto, S; Villalobos-Molina, R

    2014-01-01

    The antihyperglycaemic properties of the aqueous extract from the leaves and stems of Coriandrum sativum L. were evaluated in normoglycaemic rats, and on α-glucosidase activity from Saccharomyces cerevisiae, in order to validate its use in folk medicine. In in vivo experiments rats were administered with the aqueous extract of the plant at 100, 300 and 500 mg/kg, to observe the effect on oral sucrose tolerance test. The aqueous extract exhibited significant antihyperglycaemic activity at the three tested doses. In vitro experiments with α-glucosidase exhibited a competitive-type inhibition. These results confirm the antidiabetic properties of the extract of C. sativum L., probably by the inhibition of α-glucosidase in the gastrointestinal tract.

  7. Inhibition of lentivirus replication by aqueous extracts of Prunella vulgaris

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    Hauck Cathy

    2009-01-01

    Full Text Available Abstract Background Various members of the mint family have been used historically in Chinese and Native American medicine. Many of these same family members, including Prunella vulgaris, have been reported to have anti-viral activities. To further characterize the anti-lentiviral activities of P. vulgaris, water and ethanol extractions were tested for their ability to inhibit equine infectious anemia virus (EIAV replication. Results Aqueous extracts contained more anti-viral activity than did ethanol extracts, displaying potent anti-lentiviral activity against virus in cell lines as well as in primary cell cultures with little to no cellular cytotoxicity. Time-of-addition studies demonstrated that the extracts were effective when added during the first four h of the viral life cycle, suggesting that the botanical constituents were targeting the virion itself or early entry events. Further analysis revealed that the extracts did not destroy EIAV virion integrity, but prevented viral particles from binding to the surface of permissive cells. Modest levels of anti-EIAV activity were also detected when the cells were treated with the extracts prior to infection, indicating that anti-EIAV botanical constituents could interact with both viral particles and permissive cells to interfere with infectivity. Size fractionation of the extract demonstrated that eight of the nine fractions generated from aqueous extracts displayed anti-viral activity. Separation of ethanol soluble and insoluble compounds in the eight active fractions revealed that ethanol-soluble constituents were responsible for the anti-viral activity in one fraction whereas ethanol-insoluble constituents were important for the anti-viral activity in two of the other fractions. In three of the five fractions that lost activity upon sub-fractionation, anti-viral activity was restored upon reconstitution of the fractions, indicating that synergistic anti-viral activity is present in several

  8. In vitro antibacterial evaluation of Anabaena sp. against several clinically significant microflora and HPTLC analysis of its active crude extracts

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    Chauhan Abhishek

    2010-01-01

    Full Text Available The present study was conducted to evaluate the possible antibacterial activity of Anabaena extracts. Anabaena was isolated from a natural source and cultured in vitro. after suitable growth, cyanobacterial culture was harvested using different solvents. Extracts, thus prepared, were evaluated for their antibacterial potential by agar-well diffusion assay against bacterial species of clinical significance. MIC values were determined further to check the concentration ranges for significant inhibition. HPTLC analysis was done to separate the components of active crude extract in an attempt to identify the bio-active chemical entity. Methanol extract exhibited more potent activity than that of hexane and ethyl acetate extracts. No inhibitory effect was found against Pseudomonas aeruginosa, Salmonella typhi, and Klebsiella pneumoniae. Staphylococcus aureus required about 256 μg/ml of the crude methanol extract for effective inhibition. HPTLC evaluation at λ 254 nm was performed for the separation of a complex mixture of the methanol extract. The results provide evidence that Anabaena sp. extracts might indeed be potential sources of new antibacterial agents.

  9. Growth inhibition to three red tide microalgae by extracts of Ulva pertusa

    Institute of Scientific and Technical Information of China (English)

    2006-01-01

    Growth inhibition effect of different concentration of distilled water extract and four polar organic solvent (methanol, acetone, ether and chloroform) extracts of Ulva pertusa on three typical red tide microalgae (Heterosigma akashiwo, Alexandrium tamarense and Prorocentrum micans) were investigated. Liquid-liquid fractionation and HPLC analysis for methanol extract of U. pertusa were carried out.Growth of the three microalgae was significantly inhibited by the distilled water extract of U. pertusa at relatively higher concentration. However, the cells of the three microalgae did not die completely even at high concentration. Methanol extract of U. pertusa showed the highest growth inhibition on the three microalgae, and all the cells of the three microalgae were killed at relatively high concentration. The other three organic solvent extracts of U. pertusa had no apparent effect on the three microalgae. The results of bioassays and HPLC analysis suggested that the inhibitory substances in U. pertusa to the microalgal growth had relatively high polarities. H. akashiwo was the most sensitive one while A. tamarense was the most tolerant one to the growth inhibitory substances.

  10. Phellinus linteus extract induces autophagy and synergizes with 5-fluorouracil to inhibit breast cancer cell growth.

    Science.gov (United States)

    Lee, Wen-Ying; Hsu, Keng-Fu; Chiang, Tai-An; Chen, Chee-Jen

    2015-01-01

    Phellinus linteus (PL) is a medicinal mushroom due to its several biological properties, including anticancer activity. However, the mechanisms of its anticancer effect remain to be elucidated. We evaluated the inhibitory effects of the ethanolic extract from the PL combined with 5-FU on MDA-MB-231 breast cancer cell line and to determine the mechanism of cell death. Individually, PL extract and 5-FU significantly inhibited the proliferation of MDA-MB-231 cells in a dose-dependent manner. PL extract (30 mg/mL) in combination with 5-FU (10 μg/mL) synergistically inhibited MDA-MB-231 cells by 1.8-fold. PL did not induce apoptosis, as demonstrated by the DNA fragmentation assay, the sub-G1 population, and staining with annexin V-FITC and propidium iodide. The exposure of MDA-MB-231 cells to PL extracts resulted in several confirmed characteristics of autophagy, including the appearance of autophagic vacuoles revealed by monodansylcadaverine staining, the formation of acidic vesicular organelles, autophagosome membrane association of microtubule-associated protein light chain 3 (LC3) characterized by cleavage of LC3 and its punctuate redistribution, and ultrastructural observation of autophagic vacuoles by transmission electron microscopy. We concluded that PL extracts synergized with low doses of 5-FU to inhibit triple-negative breast cancer cell growth and demonstrated that PL extract can induce autophagy-related cell death.

  11. Cranberry and grape seed extracts inhibit the proliferative phenotype of oral squamous cell carcinomas.

    Science.gov (United States)

    Chatelain, Kourt; Phippen, Spencer; McCabe, Jonathan; Teeters, Christopher A; O'Malley, Susan; Kingsley, Karl

    2011-01-01

    Proanthocyanidins, compounds highly concentrated in dietary fruits, such as cranberries and grapes, demonstrate significant cancer prevention potential against many types of cancer. The objective of this study was to evaluate cranberry and grape seed extracts to quantitate and compare their anti-proliferative effects on the most common type of oral cancer, oral squamous cell carcinoma. Using two well-characterized oral squamous cell carcinoma cell lines, CAL27 and SCC25, assays were performed to evaluate the effects of cranberry and grape seed extract on phenotypic behaviors of these oral cancers. The proliferation of both oral cancer cell lines was significantly inhibited by the administration of cranberry and grape seed extracts, in a dose-dependent manner. In addition, key regulators of apoptosis, caspase-2 and caspase-8, were concomitantly up-regulated by these treatments. However, cranberry and grape seed extracts elicited differential effects on cell adhesion, cell morphology, and cell cycle regulatory pathways. This study represents one of the first comparative investigations of cranberry and grape seed extracts and their anti-proliferative effects on oral cancers. Previous findings using purified proanthocyanidin from grape seed extract demonstrated more prominent growth inhibition, as well as apoptosis-inducing, properties on CAL27 cells. These observations provide evidence that cranberry and grape seed extracts not only inhibit oral cancer proliferation but also that the mechanism of this inhibition may function by triggering key apoptotic regulators in these cell lines. This information will be of benefit to researchers interested in elucidating which dietary components are central to mechanisms involved in the mediation of oral carcinogenesis and progression.

  12. Cranberry and Grape Seed Extracts Inhibit the Proliferative Phenotype of Oral Squamous Cell Carcinomas

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    Kourt Chatelain

    2011-01-01

    Full Text Available Proanthocyanidins, compounds highly concentrated in dietary fruits, such as cranberries and grapes, demonstrate significant cancer prevention potential against many types of cancer. The objective of this study was to evaluate cranberry and grape seed extracts to quantitate and compare their anti-proliferative effects on the most common type of oral cancer, oral squamous cell carcinoma. Using two well-characterized oral squamous cell carcinoma cell lines, CAL27 and SCC25, assays were performed to evaluate the effects of cranberry and grape seed extract on phenotypic behaviors of these oral cancers. The proliferation of both oral cancer cell lines was significantly inhibited by the administration of cranberry and grape seed extracts, in a dose-dependent manner. In addition, key regulators of apoptosis, caspase-2 and caspase-8, were concomitantly up-regulated by these treatments. However, cranberry and grape seed extracts elicited differential effects on cell adhesion, cell morphology, and cell cycle regulatory pathways. This study represents one of the first comparative investigations of cranberry and grape seed extracts and their anti-proliferative effects on oral cancers. Previous findings using purified proanthocyanidin from grape seed extract demonstrated more prominent growth inhibition, as well as apoptosis-inducing, properties on CAL27 cells. These observations provide evidence that cranberry and grape seed extracts not only inhibit oral cancer proliferation but also that the mechanism of this inhibition may function by triggering key apoptotic regulators in these cell lines. This information will be of benefit to researchers interested in elucidating which dietary components are central to mechanisms involved in the mediation of oral carcinogenesis and progression.

  13. Inhibition of Pro-inflammatory mediators and cytokines by Chlorella Vulgaris extracts

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    G Sibi

    2016-01-01

    Full Text Available Objective: The aim of this study was to determine the in vitro anti-inflammatory activities of solvent fractions from Chlorella vulgaris by inhibiting the production of pro-inflammatory mediators and cytokines. Methods: Methanolic extracts (80% of C. vulgaris were prepared and partitioned with solvents of increasing polarity viz., n-hexane, chloroform, ethanol, and water. Various concentrations of the fractions were tested for cytotoxicity in RAW 264.7 cells using 3-(4,5-Dimethylthiazol-2-yl-2,5-diphenyl tetrazolium bromide (MTT assay, and the concentrations inducing cell growth inhibition by about 50% (IC50 were chosen for further studies. Lipopolysaccharide (LPS stimulated RAW 264.7 cells were treated with varying concentrations of C. vulgaris fractions and examined for its effects on nitric oxide (NO production by Griess assay. The release of prostaglandin E2 (PGE2, tumor necrosis factor-α (TNF-α, and interleukin 6 (IL-6 were quantified using enzyme-linked immunosorbent assay using Celecoxib and polymyxin B as positive controls. Results: MTT assay revealed all the solvent fractions that inhibited cell growth in a dose-dependent manner. Of all the extracts, 80% methanolic extract exhibited the strongest anti-inflammatory activity by inhibiting NO production (P < 0.01, PGE2 (P < 0.05, TNF-α, and IL-6 (P < 0.001 release in LPS induced RAW 264.7 cells. Both hexane and chloroform fractions recorded a significant (P < 0.05 and dose-dependent inhibition of LPS induced inflammatory mediators and cytokines in vitro. The anti-inflammatory effect of ethanol and aqueous extracts was not significant in the study. Conclusion: The significant inhibition of inflammatory mediators and cytokines by fractions from C. vulgaris suggests that this microalga would be a potential source of developing anti-inflammatory agents and a good alternate for conventional steroidal and nonsteroidal anti-inflammatory drugs.

  14. Growth inhibiting activity of lipophilic extracts from Dipsacus sylvestris Huds. roots against Borrelia burgdorferi s. s. in vitro.

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    Liebold, T; Straubinger, R K; Rauwald, H W

    2011-08-01

    Fresh first year roots from Dipsacus sylvestris HUDS. were extracted with 70% ethanol, ethyl acetate as well as dichloromethane. Extracts were solubilized in water (lipophilic extracts with addition of polysorbate 80) and tested for their activity against Borrelia burgdorferi sensu stricto in vitro during an eight-day period using amoxicillin as standard. The hydroethanolic extract showed no growth inhibition whereas significant growth inhibiting activity could be shown in the two less polar fractions for the first time. Strongest inhibition was found in the ethyl acetate extract. The effect of polysorbate 80 on bacterial growth was examined and found to be negligible. As the nature of bioactive constituents has not been clarified yet, a micellar electrokinetic capillary chromatography fingerprint analysis for a methanolic extract was applied including loganin, chlorogenic acid, cantleyoside and caffeic acid as marker substances.

  15. Antioxidant, antimicrobial and urease inhibiting activities of methanolic extracts from Cyphostemma digitatum stem and roots.

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    Khan, Rasool; Saif, Abdullah Qasem; Quradha, Mohammed Mansour; Ali, Jawad; Rauf, Abdur; Khan, Ajmal

    2016-01-01

    Cyphostemma digitatum stem and roots extracts were investigated for antioxidant, antimicrobial, urease inhibition potential and phytochemical analysis. Phytochemical screening of the roots and stem extract revealed the presence of secondary metabolites including flavonoids, alkaloids, coumarins, saponins, terpenoids, tannins, carbohydrates/reducing sugars and phenolic compounds. The methanolic extracts of the roots displayed highest antioxidant activity (93.518%) against DPPH while the crude methanolic extract of the stem showed highest antioxidant activity (66.163%) at 100 μg/mL concentration. The methanolic extracts of both stem and roots were moderately active or even found to be less active against the selected bacterial and fungal strains (Tables S2 and S3). The roots extract (methanol) showed significant urease enzyme inhibition activity (IC50 = 41.2 ± 0.66; 0.2 mg/mL) while the stem extract was found moderately active (IC50 = 401.1 ± 0.58; 0.2 mg/mL) against thiourea (IC50 = 21.011; 0.2 mg/mL).

  16. Lapacho tea (Tabebuia impetiginosa) extract inhibits pancreatic lipase and delays postprandial triglyceride increase in rats.

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    Kiage-Mokua, Beatrice Nyanchama; Roos, Nils; Schrezenmeir, Jürgen

    2012-12-01

    Earlier work in our laboratory indicated that ethanolic extracts of Tabebuia impetiginosa, Arctium lappa L., Calendula officinalis, Helianthus annuus, Linum usitatissimum and L. propolis, inhibit pancreatic lipase in vitro. In a follow-up study we assessed their effects on plasma triglycerides in rats fed on a fatty meal. Extracts, orlistat or only ethanol were given orally to the rats together with the test meal and the rate of increase of postprandial triglycerides was assessed over 4 h. Clearing of the triglycerides from the blood compartment was abolished by inhibiting lipoprotein lipase with Triton WR-1339. Our results showed that out of all the extracts, the bark of Tabebuia impetiginosa led to a significant delay in the postprandial increase of plasma triglycerides. However, lapachol, which is contained in the bark of Tabebuia impetiginosa and soluble in ethanol, had no lipase inhibitory effect in vitro and hence this substance did not seem to mediate the pertinent effect.

  17. Bioactive Extract from Moringa oleifera Inhibits the Pro-inflammatory Mediators in Lipopolysaccharide Stimulated Macrophages

    Science.gov (United States)

    Fard, Masoumeh Tangestani; Arulselvan, Palanisamy; Karthivashan, Govindarajan; Adam, Siti Khadijah; Fakurazi, Sharida

    2015-01-01

    Introduction: Inflammation is a well-known physiological response to protect the body against infection and restore tissue injury. Nevertheless, the chronic inflammation can trigger various inflammatory associated diseases/disorder. Moringa oleifera is a widely grown plant in most tropical countries and it has been recognized traditionally for several medicinal benefits. Objectives: The objective of this study was to investigate the anti-inflammatory properties of M. oleifera extract on lipopolysaccharide (LPS) - stimulated macrophages. Materials and Methods: The anti-inflammatory effect of M. oleifera hydroethanolic bioactive leaves extracts was evaluated by assessing the inhibition of nitric oxide (NO) production during Griess reaction and the expression of pro-inflammatory mediators in macrophages. Results: Interestingly, we found that M. oleifera hydroethanolic bioactive leaves extract significantly inhibited the secretion of NO production and other inflammatory markers such as prostaglandin E2, tumor necrosis factor alpha, interleukin (IL)-6, and IL-1β. Meanwhile, the bioactive extract has induced the production of IL-10 in a dose-dependent manner. In addition, M. oleifera hydroethanolic bioactive leaves extract effectively suppressed the protein expression of inflammatory markers inducible NO synthase, cyclooxygenase-2, and nuclear factor kappa-light-chain-enhancer of activated B-cells p65 in LPS-induced RAW264.7 macrophages in a dose-dependent manner. Conclusion: These findings support the traditional use of M. oleifera plant as an effective treatment for inflammation associated diseases/disorders. SUMMARY Hydroethanolic extracts of Moringa oleifera effectively inhibit the NO production in LPS induced inflammatory model.M. oleifera crude extracts successfully modulate the production of pro-inflammatory mediators in LPS stimulated macrophages.M. oleifera extracts suppressed the expression of inflammatory mediators in LPS stimulated macrophages. PMID:27013794

  18. Bioactive Extract from Moringa oleifera Inhibits the Pro-inflammatory Mediators in Lipopolysaccharide Stimulated Macrophages.

    Science.gov (United States)

    Fard, Masoumeh Tangestani; Arulselvan, Palanisamy; Karthivashan, Govindarajan; Adam, Siti Khadijah; Fakurazi, Sharida

    2015-10-01

    Inflammation is a well-known physiological response to protect the body against infection and restore tissue injury. Nevertheless, the chronic inflammation can trigger various inflammatory associated diseases/disorder. Moringa oleifera is a widely grown plant in most tropical countries and it has been recognized traditionally for several medicinal benefits. The objective of this study was to investigate the anti-inflammatory properties of M. oleifera extract on lipopolysaccharide (LPS) - stimulated macrophages. The anti-inflammatory effect of M. oleifera hydroethanolic bioactive leaves extracts was evaluated by assessing the inhibition of nitric oxide (NO) production during Griess reaction and the expression of pro-inflammatory mediators in macrophages. Interestingly, we found that M. oleifera hydroethanolic bioactive leaves extract significantly inhibited the secretion of NO production and other inflammatory markers such as prostaglandin E2, tumor necrosis factor alpha, interleukin (IL)-6, and IL-1β. Meanwhile, the bioactive extract has induced the production of IL-10 in a dose-dependent manner. In addition, M. oleifera hydroethanolic bioactive leaves extract effectively suppressed the protein expression of inflammatory markers inducible NO synthase, cyclooxygenase-2, and nuclear factor kappa-light-chain-enhancer of activated B-cells p65 in LPS-induced RAW264.7 macrophages in a dose-dependent manner. These findings support the traditional use of M. oleifera plant as an effective treatment for inflammation associated diseases/disorders. Hydroethanolic extracts of Moringa oleifera effectively inhibit the NO production in LPS induced inflammatory model.M. oleifera crude extracts successfully modulate the production of pro-inflammatory mediators in LPS stimulated macrophages.M. oleifera extracts suppressed the expression of inflammatory mediators in LPS stimulated macrophages.

  19. Extraction of rice bran extract and some factors affecting its inhibition of polyphenol oxidase activity and browning in potato.

    Science.gov (United States)

    Boonsiripiphat, Kunnikar; Theerakulkait, Chockchai

    2009-01-01

    The extraction conditions of rice bran extract (RBE), including extraction ratio, extraction time, and extraction temperature, were studied in relation to enzymatic browning inhibition in potato. The inhibitory effect of RBE on potato polyphenol oxidase (PPO) activity and its total phenolic compound content were highest at an extraction ratio of 1:3 (rice bran:water, w/v), extraction time of 30 min, and extraction temperature of 40 degrees C. RBE showed the most inhibitory effect on PPO activity at pH 6.5. However, the inhibitory effect of RBE on potato PPO activity and its total phenolic compound content were decreased at the higher temperature and longer time.

  20. Inhibition of adhesion of uropathogenic Escherichia coli bacteria to uroepithelial cells by extracts from cranberry.

    Science.gov (United States)

    Ermel, Gwennola; Georgeault, Sylvie; Inisan, Claude; Besnard, Matthieu

    2012-02-01

    Cranberry extract has been reported as a therapeutic agent, mainly in urinary tract infections due to its anti-adhesive capacity. In order to compare the effects of proanthocyanidin (procyanidin) (PAC)-standardized cranberry extracts and commercial PAC A2, we first investigated the presence of genes encoding known adhesins on 13 strains of uropathogenic strains coming from patients with cystisis. After this characterization, the anti-adhesive effects of PAC A2 were assayed on selected uropathogenic Escherichia coli strains before testing cranberry extracts. Before checking inhibitory effect on bacterial adhesion to cells, we showed that neither PAC A2 or three cranberry extracts (A, B, and C) specifically inhibited the growth and did not supply any potential nutrient to E. coli strains, including the unrelated control strain. PAC A2 exhibited an inhibitory effect on the adhesion of two selected uropathogenic strains of E. coli. This work also showed that a preliminary exposure of bacteria to PAC A2 significantly reduced the adhesion. This phenomenon has been also observed with a lesser impact when uroepithelial cells were pretreated with PAC A2. Moreover, the assays were more robust when bacteria were in fast growing conditions (exponential phase): the adhesion to uroepithelial cells was greater. Significant reduction of adhesion to urepithelial cells was observed: around 80% of inhibition of adhesion with the cranberry extracts at equivalent PAC concentration of 50 μg/mL. The effects of the different assayed extracts were not obviously different except for extract B, which inhibited approximately 55% of adhesion at an equivalent PAC concentration of 5 μg/mL.

  1. Inhibition of lipase and inflammatory mediators by Chlorella lipid extracts for antiacne treatment

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    G Sibi

    2015-01-01

    Full Text Available Acne vulgaris is a chronic inflammatory disease, and its treatment is challenging due to the multifactorial etiology and emergence of antibiotic-resistant Propionibacterium acnes strains. This study was focused to reduce antibiotics usage and find an alternate therapeutic source for treating acne. Lipid extracts of six Chlorella species were tested for inhibition of lipase, reactive oxygen species (ROS production, cytokine production using P. acnes (Microbial Type Culture Collection 1951. Lipase inhibitory assay was determined by dimercaprol Tributyrate - 5, 5′- dithiobis 2-nitrobenzoic acid method and ROS production assay was performed using nitro-blue tetrazolium test. The anti-inflammatory activity of algal lipid extracts was determined by in vitro screening method based on inhibition of pro-inflammatory cytokines, tumor necrosis factor-alpha (TNF-α produced by human peripheral blood mononuclear cells. Minimum inhibitory concentration (MIC values of lipid extracts were determined by microdilution method, and the fatty acid methyl esters (FAME were analyzed by gas chromatography-mass spectroscopy. Chlorella ellipsoidea has the highest lipase inhibitory activity with 61.73% inhibition, followed by Chlorella vulgaris (60.31% and Chlorella protothecoides (58.9%. Lipid extracts from C. protothecoides and C. ellipsoidea has significantly reduced the ROS production by 61.27% and 58.34% respectively. Inhibition of pro-inflammatory cytokines TNF-α showed the inhibition ranging from 58.39% to 78.67%. C. vulgaris has exhibited the MICvalue of 10 μg/ml followed by C. ellipsoidea, C. protothecoides and Chlorella pyrenoidosa (20 μg/ml. FAME analysis detected 19 fatty acids of which 5 were saturated fatty acids, and 14 were unsaturated fatty acids ranging from C14 to C24. The results suggest that lipid extracts of Chlorella species has significant inhibitory activity on P. acnes by inhibiting lipase activity. Further, anti-inflammatory reaction caused

  2. White Tea extract induces lipolytic activity and inhibits adipogenesis in human subcutaneous (pre-adipocytes

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    Wenck Horst

    2009-05-01

    Full Text Available Abstract Background The dramatic increase in obesity-related diseases emphasizes the need to elucidate the cellular and molecular mechanisms underlying fat metabolism. To investigate how natural substances influence lipolysis and adipogenesis, we determined the effects of White Tea extract on cultured human subcutaneous preadipocytes and adipocytes. Methods For our in vitro studies we used a White Tea extract solution that contained polyphenols and methylxanthines. Utilizing cultured human preadipocytes we investigated White Tea extract solution-induced inhibition of triglyceride incorporation during adipogenesis and possible effects on cell viability. In vitro studies on human adipocytes were performed aiming to elucidate the efficacy of White Tea extract solution to stimulate lipolytic activity. To characterize White Tea extract solution-mediated effects on a molecular level, we analyzed gene expression of essential adipogenesis-related transcription factors by qRT-PCR and determined the expression of the transcription factor ADD1/SREBP-1c on the protein level utilizing immunofluorescence analysis. Results Our data show that incubation of preadipocytes with White Tea extract solution significantly decreased triglyceride incorporation during adipogenesis in a dose-dependent manner (n = 10 without affecting cell viability (n = 10. These effects were, at least in part, mediated by EGCG (n = 10, 50 μM. In addition, White Tea extract solution also stimulated lipolytic activity in adipocytes (n = 7. Differentiating preadipocytes cultivated in the presence of 0.5% White Tea extract solution showed a decrease in PPARγ, ADD1/SREBP-1c, C/EBPα and C/EBPδ mRNA levels. Moreover, the expression of the transcription factor ADD1/SREBP-1c was not only decreased on the mRNA but also on the protein level. Conclusion White Tea extract is a natural source that effectively inhibits adipogenesis and stimulates lipolysis-activity. Therefore, it can be utilized to

  3. Fermented red ginseng extract inhibits cancer cell proliferation and viability.

    Science.gov (United States)

    Oh, Jisun; Jeon, Seong Bin; Lee, Yuri; Lee, Hyeji; Kim, Ju; Kwon, Bo Ra; Yu, Kang-Yeol; Cha, Jeong-Dan; Hwang, Seung-Mi; Choi, Kyung-Min; Jeong, Yong-Seob

    2015-04-01

    Red ginseng (Panax ginseng C.A. Meyer) is the most widely recognized medicinal herb due to its remedial effects in various disorders, such as cancers, diabetes, and heart problems. In this study, we investigated the anticancer effect of fermented red ginseng extract (f-RGE; provided by Jeonju Biomaterials Institute, Jeonju, South Korea) in a parallel comparison with the effect of nonfermented red ginseng extract (nf-RGE; control) on several cancer cell lines--MCF-7 breast cancer cells, HepG2 hepatocellular carcinoma cells, and reprogrammed MCF-7 cells (mimicking cancer stem cells). Cells were cultured at various concentrations of RGE (from 0.5 up to 5 mg/mL) and their viabilities and proliferative properties were examined. Our data demonstrate the following: (1) nf-RGE inhibited cell viability at ≥1 mg/mL for MCF-7 cells and ≥2 mg/mL for HepG2 cells, (2) in the presence of a carcinogenic agent, 12-O-tetradecanoylphorbol-13-acetate (TPA), nf-RGE treatment in combination with paclitaxel synergistically decreased MCF-7 as well as HepG2 cell viability, (3) f-RGE (which contained a greater level of Rg3 content) more effectively decreased the viability of MCF-7 and HepG2 cells compared to nf-RGE, and (4) f-RGE appeared more potent for inhibiting cancerous differentiation of reprogrammed MCF-7 cells in a synergistic fashion with paclitaxel, especially in the presence of TPA, compared to nf-RGE. These findings suggest that f-RGE treatment may be more effective for decreasing cancer cell survival by inducing apoptotic cell death and also presumably for preventing cancer stem cell differentiation compared to nf-RGE.

  4. Marine Sponge-Derived Streptomyces sp. SBT343 Extract Inhibits Staphylococcal Biofilm Formation

    Science.gov (United States)

    Balasubramanian, Srikkanth; Othman, Eman M.; Kampik, Daniel; Stopper, Helga; Hentschel, Ute; Ziebuhr, Wilma; Oelschlaeger, Tobias A.; Abdelmohsen, Usama R.

    2017-01-01

    Staphylococcus epidermidis and Staphylococcus aureus are opportunistic pathogens that cause nosocomial and chronic biofilm-associated infections. Indwelling medical devices and contact lenses are ideal ecological niches for formation of staphylococcal biofilms. Bacteria within biofilms are known to display reduced susceptibilities to antimicrobials and are protected from the host immune system. High rates of acquired antibiotic resistances in staphylococci and other biofilm-forming bacteria further hamper treatment options and highlight the need for new anti-biofilm strategies. Here, we aimed to evaluate the potential of marine sponge-derived actinomycetes in inhibiting biofilm formation of several strains of S. epidermidis, S. aureus, and Pseudomonas aeruginosa. Results from in vitro biofilm-formation assays, as well as scanning electron and confocal microscopy, revealed that an organic extract derived from the marine sponge-associated bacterium Streptomyces sp. SBT343 significantly inhibited staphylococcal biofilm formation on polystyrene, glass and contact lens surfaces, without affecting bacterial growth. The extract also displayed similar antagonistic effects towards the biofilm formation of other S. epidermidis and S. aureus strains tested but had no inhibitory effects towards Pseudomonas biofilms. Interestingly the extract, at lower effective concentrations, did not exhibit cytotoxic effects on mouse fibroblast, macrophage and human corneal epithelial cell lines. Chemical analysis by High Resolution Fourier Transform Mass Spectrometry (HRMS) of the Streptomyces sp. SBT343 extract proportion revealed its chemical richness and complexity. Preliminary physico-chemical characterization of the extract highlighted the heat-stable and non-proteinaceous nature of the active component(s). The combined data suggest that the Streptomyces sp. SBT343 extract selectively inhibits staphylococcal biofilm formation without interfering with bacterial cell viability. Due to

  5. Inhibiting effect of a hepatoma extract on the mitotic rate of regenerating liver.

    Science.gov (United States)

    Echave Llanos, J M; Badrán, A F; Moreno, F R

    1986-01-01

    Aqueous tumor extracts were prepared by the homogenization of a fast-growing, undifferentiated, transplantable malignant murine hepatoma in distilled water. After centrifugation, an aliquot of 0.01 ml of the supernatant g body weight was injected intraperitoneally into partially hepatectomized mice. Control animals were injected with saline. Groups of mice were killed at various times in relation to the hepatectomy. Four h before killing the animals were given Colcemid (1 microgram/g body weight). The number of Colcemid-arrested mitoses in the hepatocytes and in the littoral cells, respectively, were counted in 140 microscopic fields. The extract significantly inhibited the mitotic rate in hepatocytes when the injection was given between 22 h before, and up to 26 h after hepatectomy. In the littoral cells, a slight initial stimulation was followed by a slight but significant inhibition which occurred when the injection was given at hepatectomy or until 18 h after hepatectomy. The effect was not modified by exposing the extracts to temperatures of 47 degrees C for 30 min or 22 degrees C for 24 h, but 10 min of boiling destroyed their inhibitory effect. Lyophilization and storing at -18 degrees C for up to 4 weeks did not modify the effect. The mitosis-inhibiting effect was also measurable when the extract was injected subcutaneously. There was an almost linear dose-response curve. The results are discussed in relation to circadian rhythms, the pattern of liver cell proliferation after hepatectomy, and recent similar reports from the literature. The conclusion is drawn that extracts of a hepatoma contain one or more growth-inhibitory factors significantly active on regenerating liver cells, and less significantly on littoral cells.

  6. Alcohol and polyphenolic grape extract inhibit platelet adhesion in flowing blood

    NARCIS (Netherlands)

    de Lange, DW; Scholman, WLG; Kraaijenhagen, RJ; Akkerman, JWN; van de Wiel, A

    2004-01-01

    Background Moderate and prolonged alcohol consumption has been associated with decreased cardiovascular morbidity and mortality. Inhibition of platelet function in suspension attributes to these effects. Whether alcohol, red wine, or polyphenolic grape extracts (PGE) inhibit platelet adhesion is not

  7. Curcuminoids extract, hydrolyzed collagen and green tea extract synergically inhibit inflammatory and catabolic mediator's synthesis by normal bovine and osteoarthritic human chondrocytes in monolayer.

    Science.gov (United States)

    Comblain, Fanny; Sanchez, Christelle; Lesponne, Isabelle; Balligand, Marc; Serisier, Samuel; Henrotin, Yves

    2015-01-01

    The main objective of this study was to assess the in vitro effects of curcuminoids extract, hydrolyzed collagen and green tea extract in normal bovine chondrocytes and osteoarthritic human chondrocytes cultured in monolayer. This study also investigated the synergic or additive effects of these compounds. Enzymatically isolated primary bovine or human chondrocytes were cultured in monolayer until confluence and then incubated for 24 hours or 48 hours in the absence or in the presence of interleukin-1β and with or without curcuminoids extract, hydrolyzed collagen or green tea extract, added alone or in combination, at different concentrations. Cell viability was neither affected by these compounds, nor by interleukin 1β. In the absence of interleukin-1β, compounds did not significantly affect bovine chondrocytes metabolism. In human chondrocytes and in the absence of interleukin 1β, curcuminoids extract alone or in combination with hydrolyzed collagen and green tea extract significantly inhibited matrix metalloproteinase-3 production. In interleukin-1β-stimulated bovine chondrocytes, interleukin-6, inducible nitric oxide synthase, cyclooxygenase2, matrix metalloproteinase 3, a disintegrin and metalloproteinase with thrombospondin type I motifs 4 and a disintegrin and metalloproteinase with thrombospondin type I motifs 5 expressions were decreased by curcuminoids extract alone or in combination with hydrolyzed collagen and green tea extract. The combination of the three compounds was significantly more efficient to inhibit interleukin-1β stimulated matrix metalloproteinase-3 expression than curcuminoids extract alone. In interleukin-1β-stimulated human chondrocytes, nitric oxide, interleukin-6 and matrix metalloproteinase 3 productions were significantly reduced by curcuminoids extract alone or in combination with hydrolyzed collagen and green tea extract. These findings indicate that a mixture of curcuminoids extract, hydrolyzed collagen and green tea

  8. Bioactive extract from moringa oleifera inhibits the pro-inflammatory mediators in lipopolysaccharide stimulated macrophages

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    Masoumeh Tangestani Fard

    2015-01-01

    Full Text Available Introduction: Inflammation is a well-known physiological response to protect the body against infection and restore tissue injury. Nevertheless, the chronic inflammation can trigger various inflammatory associated diseases/disorder. Moringa oleifera is a widely grown plant in most tropical countries and it has been recognized traditionally for several medicinal benefits. Objectives: The objective of this study was to investigate the anti-inflammatory properties of M. oleifera extract on lipopolysaccharide (LPS - stimulated macrophages. Materials and Methods: The anti-inflammatory effect of M. oleifera hydroethanolic bioactive leaves extracts was evaluated by assessing the inhibition of nitric oxide (NO production during Griess reaction and the expression of pro-inflammatory mediators in macrophages. Results: Interestingly, we found that M. oleifera hydroethanolic bioactive leaves extract significantly inhibited the secretion of NO production and other inflammatory markers such as prostaglandin E 2 , tumor necrosis factor alpha, interleukin (IL-6, and IL-1b. Meanwhile, the bioactive extract has induced the production of IL-10 in a dose-dependent manner. In addition, M. oleifera hydroethanolic bioactive leaves extract effectively suppressed the protein expression of inflammatory markers inducible NO synthase, cyclooxygenase-2, and nuclear factor kappa-light-chain-enhancer of activated B-cells p65 in LPS-induced RAW264.7 macrophages in a dose-dependent manner. Conclusion: These findings support the traditional use of M. oleifera plant as an effective treatment for inflammation associated diseases/disorders.

  9. Anti-aging and tyrosinase inhibition effects of Cassia fistula flower butanolic extract.

    Science.gov (United States)

    Limtrakul, Pornngarm; Yodkeeree, Supachai; Thippraphan, Pilaiporn; Punfa, Wanisa; Srisomboon, Jatupol

    2016-12-03

    Natural products made from plant sources have been used in a variety of cosmetic applications as a source of nutrition and as a whitening agent. The flowers of Cassia fistula L, family Fabaceae, have been used as a traditional medicine for skin diseases and wound healing and have been reported to possess anti-oxidant properties. The anti-aging effect of C. fistula flower extract on human skin fibroblast was investigated. The butanolic extraction of C. fistula flowers was completed and the active compounds were classified. The cytotoxicity of fibroblasts was evaluated by SRB assay for the purposes of selecting non-toxic doses for further experiments. The collagen and hyaluronic acid (HA) synthesis was then measured using the collagen kit and ELISA, respectively. Moreover, the enzyme activity, including collagenase, matrixmelloproteinase-2 (MMP-2) and tyrosinase, were also evaluated. It was found that the flower extract did not affect skin fibroblast cell growth (IC50 > 200 μg/mL). The results did show that the flower extract significantly increased collagen and HA synthesis in a dose dependent manner. The flower extract (50-200 μg/mL) also significantly inhibited collagenase and MMP-2 activity. Furthermore, this flower extract could inhibit the tyrosinase activity that causes hyperpigmentation, which induces skin aging. The C. fistula flower extract displayed a preventive effect when used for anti-aging purposes in human skin fibroblasts and may be an appropriate choice for cosmetic products that aim to provide whitening effects, and which are designated as anti-aging facial skin care products.

  10. Antibacterial, antioxidant and tyrosinase-inhibition activities of pomegranate fruit peel methanolic extract

    National Research Council Canada - National Science Library

    Fawole, Olaniyi A; Makunga, Nokwanda P; Opara, Umezuruike Linus

    2012-01-01

    This study evaluated, using in vitro assays, the antibacterial, antioxidant, and tyrosinase-inhibition activities of methanolic extracts from peels of seven commercially grown pomegranate cultivars...

  11. Inhibition of viral proteases by Zingiberaceae extracts and flavones isolated from Kaempferia parviflora.

    Science.gov (United States)

    Sookkongwaree, K; Geitmann, M; Roengsumran, S; Petsom, A; Danielson, U H

    2006-08-01

    In order to identify novel lead compounds with antiviral effect, methanol and aqueous extracts of eight medicinal plants in the Zingiberaceae family were screened for inhibition of proteases from human immunodeficiency virus type 1 (HIV-1), hepatitis C virus (HCV) and human cytomegalovirus (HCMV). In general, the methanol extracts inhibited the enzymes more effectively than the aqueous extracts. HIV-1 protease was strongly inhibited by the methanol extract of Alpinia galanga. This extract also inhibited HCV and HCMV proteases, but to a lower degree. HCV protease was most efficiently inhibited by the extracts from Zingiber officinale, with little difference between the aqueous and the methanol extracts. Many of the methanol extracts inhibited HCMV protease, but the aqueous extracts showed weak inhibition. In a first endeavor to identify the active constituents, eight flavones were isolated from the black rhizomes of Kaempferia parviflora. The most effective inhibitors, 5-hydroxy-7-methoxyflavone and 5,7-dimethoxyflavone, inhibited HIV-1 protease with IC50 values of 19 microM. Moreover, 5-hydroxy-3,7-dimethoxyflavone inhibited HCV protease and HCMV protease with IC50 values of 190 and 250 microM, respectively.

  12. Inhibition of Quorum Sensing-Controlled Virulence Factor Production in Pseudomonas aeruginosa PAO1 by Ayurveda Spice Clove (Syzygium Aromaticum Bud Extract

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    Kok-Gan Chan

    2012-03-01

    Full Text Available Quorum sensing controls the virulence determinants in most proteobacteria. In this work, the hexane, chloroform and methanol extracts of an Ayurveda spice, namely clove (Syzygium aromaticum, shown anti-quorum sensing activity. Hexane and methanol extracts of clove inhibited the response of C. violaceum CV026 to exogenously supplied N‑hexanoylhomoserine lactone, in turn preventing violacein production. Chloroform and methanol extracts of clove significantly reduced bioluminescence production by E. coli [pSB1075] grown in the presence of N-(3-oxododecanoyl-L-homoserine lactone. We demonstrated that clove extract inhibited quorum sensing-regulated phenotypes in Pseudomonas aeruginosa PA01, including expression of lecA::lux (by hexane extract, swarming (maximum inhibition by methanol extract, pyocyanin (maximum inhibition by hexane extract. This study shows that the presence of natural compounds that exhibit anti-quorum sensing activity in the clove extracts may be useful as the lead of anti-infective drugs.

  13. Extraction conditions of white rose petals for the inhibition of enzymes related to skin aging

    OpenAIRE

    Choi, Ehn-Kyoung; Guo, Haiyu; Choi, Jae-Kwon; Jang, Su-Kil; Shin, Kyungha; Cha, Ye-Seul; Choi, Youngjin; Seo, Da-Woom; Lee, Yoon-Bok; Joo, Seong-So; Kim, Yun-Bae

    2015-01-01

    In order to assess inhibitory potentials of white rose petal extracts (WRPE) on the activities of enzymes related to dermal aging according to the extraction conditions, three extraction methods were adopted. WRPE was prepared by extracting dried white rose (Rosa hybrida) petals with 50% ethanol (WRPE-EtOH), Pectinex® SMASH XXL enzyme (WRPE-enzyme) or high temperature-high pressure (WRPE-HTHP). In the inhibition of matrix metalloproteinase-1, although the enzyme activity was fully inhibited b...

  14. Loquat (Eriobotrya japonica) leaf extract inhibits the growth of MDA-MB-231 tumors in nude mouse xenografts and invasion of MDA-MB-231 cells.

    Science.gov (United States)

    You, Mi-Kyoung; Kim, Min-Sook; Jeong, Kyu-Shik; Kim, Eun; Kim, Yong-Jae; Kim, Hyeon-A

    2016-04-01

    The present study was conducted to examine the inhibitory effect of loquat leaves on MDA-MB-231 cell proliferation and invasion. Female athymic nude mice were given a subcutaneous (s.c.) inoculation of MDA-MB-231 cells and randomly grouped to receive a s.c. injection of either 500 mg/kg ethanol, water extract or vehicle five times a week. Tumor growth, mitotic rate and necrosis were examined. MDA-MB-231 cells were cultured with DMSO or with various concentrations of loquat water or ethanol extract. Proliferation, adhesion, migration, invasion and matrix metalloproteinase (MMP) activity were examined. Tumor growth of xenograft nude mouse was significantly reduced by loquat extracts. The results of mitotic examination revealed that loquat extracts reduced tumor cell division. Both ethanol and water extracts significantly inhibited MDA-MB-231 cell proliferation. The protein expression of ErbB3 was significantly down-regulated by loquat leaf extracts. Loquat leaf extracts increased apoptosis of MDA-MB-231 cells following 24 hour incubation and the ethanol extract was more potent in inducing apoptosis than the water extract. Furthermore, loquat extracts inhibited adhesion, migration and invasion of MDA-MB-231 cells. MMP activity was significantly inhibited by loquat extracts. Our results show that extracts of loquat inhibit the growth of tumor in MDA-MB-231 xenograft nude mice and the invasion of human breast cancer cells, indicating the inhibition of tumor cell proliferation and invasion.

  15. Inhibition of Fish Nodavirus by Gymnemagenol Extracted from Gymnema sylvestre

    Institute of Scientific and Technical Information of China (English)

    V. Gopiesh Khanna; K. Kannabiran; V. Sarath Babu; A. S. Sahul Hameed

    2011-01-01

    Viral nervous necrosis (VNN) has emerged to become a major problem in the culture of larval and juvenile marine fish worldwide.Bioactive phytochemicals isolated from commonly available medicinal plants are often screened for their efficacy in controlling fish viral diseases.Occurrence of newer viral strains and resistance to existing antiviral drugs are problems currently associated with treatment of VNN,which necessitates looking for alternate sources for effective antiviral drugs.The aim of the present study was to screen antiviral potential of gymnemagenol (C30H50O4) previously extracted from leaves of Gymnema sylvestre.The fish nodavirus,grouper nervous necrosis virus (GNNV) in infected Sahul Indian Grouper Eye (SIGE) cell lines were used to study the antiviral activity of gymnemagenol under in vitro conditions.The susceptibility of the virus to gynmemagenol was confirmed by measuring the viral titre (TCID50 mL-1) in virus-infected SIGE cells every 24 h.Gymnemagenol at 20 μg mL-1 inhibited the proliferation of GNNV to 53% at the end of the 6th d by inhibiting the proliferation of GNNV-infected SIGE cells.The viable SIGE cells were reduced to 47% as determined by 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay.The viral titre (TCID50 mL-1) was also reduced to log 2.8 at the end of the 7th d in gymnemagenol-treated SIGE cells after inoculated with GNNV when compared to untreated control SIGE cell viral titre (log4.1).Based on our results it can be concluded that gymnemagenol could be used as an antiviral agent against GNNV infection.

  16. Corrosion Inhibition of Carbon Steel in HCl Solution by Some Plant Extracts

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    Ambrish Singh

    2012-01-01

    Full Text Available The strict environmental legislations and increasing ecological awareness among scientists have led to the development of “green” alternatives to mitigate corrosion. In the present work, literature on green corrosion inhibitors has been reviewed, and the salient features of our work on green corrosion inhibitors have been highlighted. Among the studied leaves, extract Andrographis paniculata showed better inhibition performance (98% than the other leaves extract. Strychnos nuxvomica showed better inhibition (98% than the other seed extracts. Moringa oleifera is reflected as a good corrosion inhibitor of mild steel in 1 M HCl with 98% inhibition efficiency among the studied fruits extract. Bacopa monnieri showed its maximum inhibition performance to be 95% at 600 ppm among the investigated stem extracts. All the reported plant extracts were found to inhibit the corrosion of mild steel in acid media.

  17. Inhibition of Murine Norovirus and Feline Calicivirus by Edible Herbal Extracts.

    Science.gov (United States)

    Seo, Dong Joo; Choi, Changsun

    2017-03-01

    Human noroviruses (HuNoVs) cause foodborne and waterborne viral gastroenteritis worldwide. Because HuNoV culture systems have not been developed thus far, no available medicines or vaccines preventing infection with HuNoVs exist. Some herbal extracts were considered as phytomedicines because of their bioactive components. In this study, the inhibitory effects of 29 edible herbal extracts against the norovirus surrogates murine norovirus (MNV) and feline calicivirus (FCV) were examined. FCV was significantly inhibited to 86.89 ± 2.01 and 48.71 ± 7.38% by 100 μg/mL of Camellia sinensis and Ficus carica, respectively. Similarly, ribavirin at a concentration of 100 μM significantly reduced the titer of FCV by 77.69 ± 10.40%. Pleuropterus multiflorus (20 μg/mL) showed antiviral activity of 53.33 ± 5.77, and 50.00 ± 16.67% inhibition was observed after treatment with 20 μg/mL of Alnus japonica. MNV was inhibited with ribavirin by 59.22 ± 16.28% at a concentration of 100 μM. Interestingly, MNV was significantly inhibited with 150 µg/mL Inonotus obliquus and 50 μg/mL Crataegus pinnatifida by 91.67 ± 5.05 and 57.66 ± 3.36%, respectively. Treatment with 20 µg/mL Coriandrum sativum slightly reduced MNV by 45.24 ± 4.12%. The seven herbal extracts of C. sinensis, F. carica, P. multiflorus, A. japonica, I. obliquus, C. pinnatifida, and C. sativum may have the potential to control noroviruses without cytotoxicity.

  18. The effect of different concentrations of Neem (Azadiractha indica leaves extract on the inhibition of Streptococcus mutans (In vitro

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    Sri Kavi Subramaniam

    2005-12-01

    Full Text Available The Neem plant has a history for treating gum and teeth problems and this plant is used for oral care in India. The active component (Azadirachta indica has been proven to exhibit antibacterial properties. The objective of this study was to determine the influence of different concentrations of Neem leaves extract on the inhibition of Streptococcus mutans. Neem leaves extract at concentrations of 10%, 20%, 40%, 60%, 80%, and 100% was prepared. Fifty milliliters of each concentration were dropped into holes of 6 millimeters in diameter on a MHA agar that has been inoculated with Streptococcus mutans. Distilled water was used as a control. After 24 hours of incubation, the inhibition diameters were measured and analyzed. The statistical results of the one-way analysis of variance (ANOVA illustrated that the different concentrations of Neem extract had a significant influence on the inhibition of Streptococcus mutans. This was followed with the Least Significant Difference (LSD which implied that there were significant differences between all the concentrations of Neem leaves extract used in this experiment. The conclusion of this study was that Neem leaves extract exhibited antibacterial effect towards Streptococcus mutans and different concentration of Neem leaves extract influenced the inhibition of Streptococcus mutans.

  19. Antioxidant Potential, Lipid Peroxidation Inhibition and Antimicrobial Activities of Satureja montana L. subsp. kitaibelii Extracts

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    Dragoljub D. Cvetković

    2007-09-01

    Full Text Available The antioxidant activity of different Satureja montana L. subsp. kitaibelii extracts was tested by measuring their ability to scavenge reactive hydroxyl radical during the Fenton reaction, using ESR spectroscopy. Also, the influence of these extracts on lipid peroxyl radicals obtained during lipid peroxidation of: (I sunflower oil (37°C, 3h inducedby 4,4'-azobis(4-cyanovaleric acid (ACVA and (II liposomes induced by 2,2'-azobis(2-amidino-propanedihydrochloride (AAPH was studied. n-Butanol extract had the bestantioxidant activity (100% at 0.5 mg/mL in Fenton reaction system; 89.21% at 5 mg/mL in system I; 83.38% at 5 mg/mL in system II. The antioxidant activities of the extracts significantly correlated with total phenolic content. The antimicrobial activity of Satureja montana L. subsp. kitaibelii extracts was investigated. Petroleum ether, chloroform and ethyl acetate extracts expressed a wide range of inhibiting activity against both gram-positive and gram-negative bacteria.

  20. Antioxidant rich grape pomace extract suppresses postprandial hyperglycemia in diabetic mice by specifically inhibiting alpha-glucosidase

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    Hogan Shelly

    2010-08-01

    Full Text Available Abstract Background Postprandial hyperglycemia is an early defect of type 2 diabetes and one of primary anti-diabetic targets. Treatment of postprandial hyperglycemia can be achieved by inhibiting intestinal α-glucosidase, the key enzyme for oligosaccharide digestion and further glucose absorption. Grape pomace is winemaking byproduct rich in bioactive food compounds such as phenolic antioxidants. This study evaluated the anti-diabetic potential of two specific grape pomace extracts by determining their antioxidant and anti-postprandial hyperglycemic activities in vitro and in vivo. Methods The extracts of red wine grape pomace (Cabernet Franc and white wine grape pomace (Chardonnay were prepared in 80% ethanol. An extract of red apple pomace was included as a comparison. The radical scavenging activities and phenolic profiles of the pomace extracts were determined through the measurement of oxygen radical absorbance capacity, DPPH radical scavenging activity, total phenolic content and flavonoids. The inhibitory effects of the pomace extracts on yeast and rat intestinal α-glucosidases were determined. Male 6-week old C57BLKS/6NCr mice were treated with streptozocin to induce diabetes. The diabetic mice were then treated with vehicle or the grape pomace extract to determine whether the oral intake of the extract can suppress postprandial hyperglycemia through the inhibition of intestinal α-glucosidases. Results The red grape pomace extract contained significantly higher amounts of flavonoids and phenolic compounds and exerted stronger oxygen radical absorbance capacity than the red apple pomace extract. Both the grape pomace extracts but not the apple pomace extract exerted significant inhibition on intestinal α-glucosidases and the inhibition appears to be specific. In the animal study, the oral intake of the grape pomace extract (400 mg/kg body weight significantly suppressed the postprandial hyperglycemia by 35% in streptozocin

  1. Ethanol Extract of Alismatis rhizome Inhibits Adipocyte Differentiation of OP9 Cells

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    Yeon-Ju Park

    2014-01-01

    Full Text Available The rhizome of Alisma orientale (Alismatis rhizome has been used in Asia for promoting diuresis to eliminate dampness from the lower-jiao and to expel heat. In this study, an ethanol extract of the rhizome of Alisma orientale (AOE was prepared and its effects on adipocyte differentiation of OP9 cells were investigated. Treatment with AOE in a differentiation medium for 5 days resulted in dose-dependent inhibition of lipid droplet formation in OP9 cells. Furthermore, AOE significantly inhibited adipocyte differentiation by downregulating the expression of the master transcription factor of adipogenesis, peroxisome proliferation-activity receptor γ (PPARγ, and related genes, including CCAAT/enhancer binding protein β (C/EBPβ, fatty acid-binding protein (aP2, and fatty acid synthase (FAS. AOE exerted its inhibitory effects primarily during the early adipogenesis stage (days 1-2, at which time it also exerted dose-dependent inhibition of the expression of C/EBPβ, a protein related to the inhibition of mitotic clonal expansion. Additionally, AOE decreased the expression of autophagy-related proteins, including beclin 1, and the autophagy-related genes, (Atg 7 and Atg12. Our results indicate that AOE’s inhibitory effects on adipocyte differentiation of OP9 cells are mediated by reduced C/EBPβ expression, causing inhibition of mitotic clonal expansion and autophagy.

  2. Adult emergence inhibition and adulticidal activities of medicinal plant extracts againstAnopheles stephensiListon

    Institute of Scientific and Technical Information of China (English)

    AbdulAbduzZahir; AbdulAbdulRahuman; AsokanBa=gavan; GandhiElango; Chinnaperumal Kamaraj

    2010-01-01

    Objective:To determine the adult emergence inhibition (EI) and adulticidal activities of hexane, chloroform, ethyl acetate, and acetone leaves extracts of Anisomeles malabarica (A. malabarica), Euphorbia hirta (E. hirta), Ocimum basilicum (O. basilicum), Ricinus communis (R. communis), Solanum trilobatum (S. trilobatum), Tridax procumbens (T. procumbens)and seeds ofGloriosa superba (G. superba) againstAnopheles stephensi (An. stephensi).Methods: The EI and adulticidal trials were carried out according to World Health Organization (WHO) procedures with slight modifications. The extracts were diluted in dimethyl sulphoxide in order to prepare a serial dilution of test dosages (15.625, 31.25, 62.5, 125, 250, 500 and1 000μg/mL). Five duplicate trials were carried out for every sample concentration, and for each trial a negative control was included and the mortality was determined after24 h of exposure.Results: The highestEI activity was found in ethyl acetate extracts ofA. malabarica, chloroform extracts ofO. basilicum, S.trilobatum, acetone of extract ofR. communis, T. procumbens, and seed extract ofG. superba withEI50 values143.12, 119.82, 157.87, 139.39, 111.19, and134.85 μg/mL, and the effective adulticidal activity was observed in chloroform, acetone extracts ofG. superba, T. procumbens, R. communis, S.trilobatum and ethyl acetate extract ofO. basilicum with LD50 values120.17, 108.77, 127.22, 163.11, 118.27, and93.02μg/mL, respectively. Chi-square value was significant atP<0.05 level.Conclusions: These results should encourage further efforts to investigate the compounds that might possess good EI and adulticidal properties when isolated in pure form.

  3. Preliminary studies of inhibitions in Aspergillus flavus with extracts of ...

    African Journals Online (AJOL)

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    of lichens on the growth of lower Phycomycetes and. Neurospora ... have indicated the possible use of plant as well as lichen extracts in the control of plant diseases. The extraction, ... under light microscope (*400 objective) for the emergence of germ tube. .... artificial fungicide develop, this study has shown that extracts of ...

  4. Inhibition of human low-density lipoprotein oxidation in vitro by ginger extracts.

    Science.gov (United States)

    Gunathilake, K D Prasanna P; Rupasinghe, H P Vasantha

    2014-04-01

    Oxidative modification of low-density lipoprotein (LDL) is thought to play a key role in atherosclerotic plaque formation. Currently, there is a renewed interest in ginger because of its antioxidants and cardioprotective properties. The effects of ethanol, methanol, ethyl acetate, and hexane solvent extracts of ginger and pure major ginger constituents on Cu(2+)-induced oxidation of human LDL in vitro were examined. The LDL oxidation inhibition by ethanol, methanol, ethyl acetate, and hexane extracts of ginger was 71%, 76%, 67%, and 67%, respectively, at their optimum extraction conditions. Inhibition of LDL oxidation by water extracts of ginger, which was prepared by ultrasonic-assisted extraction conditions of 52°C for 15 min, was about 43%. Phenolic bioactives of ginger-6-gingerols, 8-gingerols, 10-gingerols, and 6-shogaol-seem to be strong inhibitors of Cu(+2)-induced LDL oxidation. Overall, ginger extracts, including the water extract possess the antioxidant activities to inhibit human LDL oxidation in vitro.

  5. Phytotoxicity analysis of extracts from compost and their ability to inhibit soil-borne pathogenic fungi and reduce root-knot nematodes.

    Science.gov (United States)

    Xu, Dabing; Raza, Waseem; Yu, Guanghui; Zhao, Qingyun; Shen, Qirong; Huang, Qiwei

    2012-03-01

    Compost extracts are novel organic amendments, typically applied to suppress soil-borne diseases. This research evaluated the phytotoxicity of compost extracts and analyzed their ability to inhibit pathogenic fungal growth and reduce root-knot nematodes. The physical, chemical and biological characteristics of extracts from a pig manure and straw compost were analyzed. Three types of extracts were tested: direct extracts of compost (DEC), aerated fermentation extracts of compost (AFEC) and non-aerated fermentation extracts of compost (NAFEC). All compost extracts showed low phytotoxicity against lettuce and cress, but AFEC and NAFEC were more phytotoxic than DEC. All compost extracts significantly inhibited pathogenic fungal growth except for the fungus Rhizoctonia solania AG4. For two seasons, tomato root biomass of three compost extracts was 1.25-5.67 times greater than CK (water control), and AFEC and NAFEC showed the best tomato root growth promotion. The reduction ratio of root egg mass and density of soil nematodes were 34.51-87.77% and 30.92-51.37%, when applied with three compost extracts. The microbial population in compost extracts was considered to be the most significant factor of inhibition pathogenic fungal growth. No markedly correlations among bacterial community diversity, the inhibition of pathogenic fungal growth and the reduction of root-knot nematodes were observed. This information adds to the understanding of the growth-promoting and suppression effects of compost extracts and will help to enhance crop production.

  6. Taraxacum officinale dandelion extract efficiently inhibited the breast cancer stem cell proliferation

    Directory of Open Access Journals (Sweden)

    Ngu Van Trinh

    2016-07-01

    Full Text Available Background: Breast cancer stem cells (BCSCs play an important role in breast cancer initiation, metastasis, recurrence, and drug resistance. Therefore, targeting BCSCs is an essential strategy to suppress cancer growth. This study aimed to evaluate the effects of dandelion Taraxacum officinale extracts on BCSC proliferation in vitro in 2D and 3D cell culture platforms. Materials and Methods: The BCSCs were maintained under standard conditions, verified for expression of CD44 and CD24 surface markers, and transfected with GFP before use in experiments. In the 2D model, the BCSCs were cultured as adherent cells in standard culture plates; in the 3D model, the BCSCs were cultured on low-adherent plates to form spheroids. The effect of Dandelion extracts on proliferation of BCSC was assessed by evaluating induction of cell death, expression of genes of death receptor signaling pathways, and production of reactive oxygen species (ROS by BCSCs. Results: BCSCs formed spheroids as microtumors in vitro and exhibited some in vivo characteristics of tumors, such as increased expression of N-cadherin and Slug, decreased expression of E-cadherin, capacity to invade into the extracellular matrix (ECM, and presence of a hypoxic environment at the core of tumor spheroids. The dandelion extracts significantly inhibited BCSC proliferation in both two-dimensional (2D and three-dimensional (3D models of BCSCs. However, the IC50 value of dandelion extracts in BCSCs in the 3D model was much higher than that in the 2D model. The results also demonstrated that BCSCs treated with Dandelion extracts showed increased expression of tumor necrosis factor-related apoptosis-inducing ligand (TRAIL and TRAIL receptor 2 (TRAILR2; i.e. death receptor 5; DR5. Moreover, treatment induced expression of DR4. Treatment with methanol dandelion extract enhanced production of ROS in BCSCs. Conclusion: Dandelion extracts are promising extracts for the treatment of breast tumors. The

  7. Inhibition of HIV-1 entry by extracts derived from traditional Chinese medicinal herbal plants

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    Song Xinming

    2009-08-01

    Full Text Available Abstract Background Highly active anti-retroviral therapy (HAART is the current HIV/AIDS treatment modality. Despite the fact that HAART is very effective in suppressing HIV-1 replication and reducing the mortality of HIV/AIDS patients, it has become increasingly clear that HAART does not offer an ultimate cure to HIV/AIDS. The high cost of the HAART regimen has impeded its delivery to over 90% of the HIV/AIDS population in the world. This reality has urgently called for the need to develop inexpensive alternative anti-HIV/AIDS therapy. This need has further manifested by recent clinical trial failures in anti-HIV-1 vaccines and microbicides. In the current study, we characterized a panel of extracts of traditional Chinese medicinal herbal plants for their activities against HIV-1 replication. Methods Crude and fractionated extracts were prepared from various parts of nine traditional Chinese medicinal herbal plants in Hainan Island, China. These extracts were first screened for their anti-HIV activity and cytotoxicity in human CD4+ Jurkat cells. Then, a single-round pseudotyped HIV-luciferase reporter virus system (HIV-Luc was used to identify potential anti-HIV mechanisms of these extracts. Results Two extracts, one from Euphorbiaceae, Trigonostema xyphophylloides (TXE and one from Dipterocarpaceae, Vatica astrotricha (VAD inhibited HIV-1 replication and syncytia formation in CD4+ Jurkat cells, and had little adverse effects on host cell proliferation and survival. TXE and VAD did not show any direct inhibitory effects on the HIV-1 RT enzymatic activity. Treatment of these two extracts during the infection significantly blocked infection of the reporter virus. However, pre-treatment of the reporter virus with the extracts and treatment of the extracts post-infection had little effects on the infectivity or gene expression of the reporter virus. Conclusion These results demonstrate that TXE and VAD inhibit HIV-1 replication likely by blocking

  8. Parsley extract inhibits in vitro and ex vivo platelet aggregation and prolongs bleeding time in rats.

    Science.gov (United States)

    Gadi, Dounia; Bnouham, Mohamed; Aziz, Mohammed; Ziyyat, Abderrahim; Legssyer, Abdelkhaleq; Legrand, Chantal; Lafeve, Françoise Fauvel; Mekhfi, Hassane

    2009-08-17

    Many cardiovascular diseases are associated with an increase in blood platelet activity. In Morocco, parsley (Petroselinum crispum, Apiaceae) is one of the medicinal herbs used to treat cardiovascular diseases such as arterial hypertension. In this study, crude aqueous extract (CAE) of parsley was evaluated for its anti-platelet activity in experimental animals on platelet aggregation in vitro and ex vivo; and on bleeding time in vivo. The in vitro aggregation was monitored after pre-incubation of platelets with CAE. The bleeding time and ex vivo aggregation were performed after oral treatment. CAE inhibited dose dependently platelet aggregation in vitro induced by thrombin, ADP, collagen and epinephrine. The oral administration of CAE (3g/kg) inhibited significantly (p<0.001) platelet aggregation ex vivo and prolonged bleeding time (p<0.001) without changes in the platelet amount. The prolongation of bleeding time by CAE may be attributed to the observed inhibition of platelet aggregation. These effects could be related in part to the polyphenolic compounds present in the extract. These results support the hypothesis that the dietary intake of parsley may be benefit in the normalization of platelet hyperactivation, in the nutritional prevention of cardiovascular diseases and are potentially interesting in the development of new prevention strategies.

  9. Corrosion Inhibition Studies of Mild Steel in Acid Medium Using Musa Acuminata Fruit Peel Extract

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    N. Gunavathy

    2012-01-01

    Full Text Available The inhibition effect of unripe fruit peel extract of Musa acuminata (Cultivar variety – Nendran (MNP on corrosion of mild steel in 1 N HCl has been investigated by weight loss and electrochemical impedance spectroscopy (EIS with various concentrations of the extract. The effect of temperature on the corrosion inhibition of mild steel in the temperature range of 30°C – 80°C was carried out. The results indicate that MNP extract act as an effective inhibitor in the acid environment and is of mixed type inhibitor having efficiency as high as 96% at 2% inhibitor concentration. The inhibition efficiency of MNP extract increases with the increase of concentration but decreases with the increase in temperature. The inhibitor achieves its inhibition by physical adsorption of nutrients of the peel extract on the surface of the mild steel. The experimental data revealed that the adsorption occurred according to the Langmuir and Temkin adsorption isotherm.

  10. INHIBITION OF HUMAN LOW-DENSITY LIPOPROTEINS OXIDATION BY Hibiscus radiatus CUV. CALYCES EXTRACT

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    Hernawan Hernawan

    2010-06-01

    Full Text Available Hibiscus radiatus Cuv calyces extracts rich in polyphenols was screened for their potential to inhibit oxidation of human low-density lipoproteins-cholesterol (LDL-C in vitro. The inhibition of LDL-C oxidation (antioxidant activity was determined by measuring the formation of conjugated dienes and thiobarbituric acid reagent substances (TBARS. LDL-C oxidation was carried out in the presence of H. radiatus Cuv calyces extract (20 and 50 μM. CuSO4 (10 μM was used as the oxidation initiator and  butylated hydroxytoluene (BHT at 50 μM was used as standard antioxidant. The protective effect of H. radiatus Cuv. calyces extract toward human low-density lipoproteins, complex lipid system was  demonstrated by significant increase lag time (> 103 min, diminished of the propagation rate (44 %, and diminution of conjugated dienes formation 59.42 % (50 μM compared to control.   Keywords: antioxidant, conjugated dienes, Hibiscus radiatus Cuv, low-density lipoproteins-cholesterol

  11. Inhibition of Human Cervical Cancer Cell Growth by Ethanolic Extract of Boerhaavia diffusa Linn. (Punarnava Root

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    Rakhi Srivastava

    2011-01-01

    Full Text Available In Indian traditional medicine, Boerhaavia diffusa (punarnava roots have been widely used for the treatment of dyspepsia, jaundice, enlargement of spleen, abdominal pain and as an anti-stress agent. Pharmacological evaluation of the crude ethanolic extract of B. diffusa roots has been shown to possess antiproliferative and immunomodulatory properties. The extract of B. diffusa was studied for anti-proliferative effects on the growth of HeLa cells and for its effect on cell cycle. Bio-assays of extracts from B. diffusa root showed that a methanol : chloroform fraction (BDF 5 had an antiproliferative effect on HeLa cells. After 48 h of exposure, this fraction at a concentration of 200 μg mL−1 significantly reduced cell proliferation with visible morphological changes in HeLa cells. Cell cycle analysis suggests that antiproliferative effect of BDF 5 could be due to inhibition of DNA synthesis in S-phase of cell cycle in HeLa cells, whereas no significant change in cell cycle was detected in control cells. The fraction BDF 5 caused cell death via apoptosis as evident from DNA fragmentation and caspase-9 activation. Thus the extract has potential to be evaluated in detail to assess the molecular mechanism-mediated anticancer activities of this plant.

  12. [Grape seed extract inhibits the growth of prostate cancer PC-3 cells].

    Science.gov (United States)

    Huang, Ting-Ting; Shang, Xue-Jun; Yao, Gen-Hong; Ge, Jing-Ping; Teng, Wen-Hui; Sun, Yi; Huang, Yu-Feng

    2008-04-01

    To investigate the inhibitory effect of grape seed extract (GSE) on the growth of prostate cancer PC-3 cells. PC-3 cells were treated with GSE at the concentration of 100, 200 and 300 microg/ml for 24, 48 and 72 hours, respectively. The the inhibitory effect of GSE on the growth of the PC-3 cells and the kidney cells of SD rats was determined by MTT reduction assay, with primarily cultured kidney cells of 1-3 days old SD rats as the normal control. GSE significantly inhibited the growth of PC-3 cells in a concentration- and time-dependent manner, but had only a mild inhibitory effect on the kidney cells. GSE inhibits the growth of prostate cancer PC-3 cells and can be used as a new drug for the treatment of prostate cancer.

  13. Evaluation of alpha- amylase inhibition by Urtica dioica and Juglans regia extracts

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    Mahsa Rahimzadeh

    2014-06-01

    Full Text Available Objective(s:One strategy for the treatment of diabetes is inhibition of pancreatic α- amylase. Plants contains different chemical constituents with potential for inhibition of α-amylase and hence maybe used as therapeutic. Materials and Methods: Urtica dioica and Juglans regia Linn were tested for α-amylase inhibition. Different concentrations of leaf aqueous extracts were incubated with enzyme substrate solution and the activity of enzyme was measured. For determination of the type of inhibition, Dixon plot was depicted. Acarbose was used as the standard inhibitor. Results: Both plant extracts showed time and concentration dependent inhibition of α-amylase. 60% inhibition was seen with 2 mg/ml of U. dioica and0.4 mg/ml of J. regia aqueous extract. Dixon plots revealed the type of α-amylase inhibition by these two extracts as competitive inhibition. Conclusion: Determination of the type of α-amylase inhibition by these plant extracts could provide by successful use of plant chemicals as drug targets.

  14. The extract of Cordyceps sinensis inhibited airway inflammation by blocking NF-κB activity.

    Science.gov (United States)

    Chiou, Ya-Ling; Lin, Ching-Yuang

    2012-06-01

    Aiming the extract of Cordyceps sinensis significantly inhibits airway inflammation, airway hyperresponsiveness, and the infiltration of eosinophils in the airway of rats and may be related to the modulation of T helper (Th)1 and Th2 cells functions. The mechanisms of C. sinensis involved in modulation of suppression inflammation are not yet determined. In this study, the mechanism involved in the extract of C. sinensis-C.S.3-modulated suppression of inflammation was investigated in vivo and in vitro systems. The results showed that C.S.3 reduced airway inflammation in ovalbumin-induced allergic mice. Furthermore, we found C.S.3 could decrease extracellular signal-regulated kinase 1/2 signaling pathway to suppress activity of nuclear factor-κB in lung cells and cultured airway smooth muscle cells. Conclusion C.S.3 may provide clinical applications for asthma in the future.

  15. Extract of ginkgo biloba EGb761 inhibits cell apoptosis following spinal cord injury

    Institute of Scientific and Technical Information of China (English)

    Jiejun Jiao; Jiannong Jiang; Bin Du; Yuan Mo; Ming Zhou; Hongquan Zhang

    2010-01-01

    The neuroprotective effects of ginkgo biloba extract have been shown in rats following spinal cord injury (SCI). However, the precise protective mechanisms remain unclear. In the present study, low-acid water-soluble extract of ginkgo biloba EGb761 was used to treat rats with SCI. Xanthin oxidase, thiobarbituric acid, terminal deoxyribonucleotidyl transferase-mediated dUTP-digoxigenin nick end labeling assay, and immunohistochemistry were utilized to detect lipid peroxidation, neural cell apoptosis, and inducible nitric oxide synthase activity in rats with SCI. Results revealed significantly increased superoxide dismutase activity, decreased malondialdehyde content, apoptotic index, and inducible nitric oxide synthase expression in SCI rats following EGb761 treatment. Therefore, EGb761 suppressed lipid peroxidation following SCI, relieved neural cell apoptosis, inhibited inducible nitric oxide synthase expression, and ultimately exerted protective effects on SCI.

  16. Fresh garlic extract inhibits Staphylococcus aureus biofilm formation under chemopreventive and chemotherapeutic conditions

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    Panan Ratthawongjirakul

    2016-08-01

    Full Text Available Staphylococcus aureus and methicillin-resistant Staphylococcus aureus (MRSA are the leading aetiological pathogens of nosocomial infections worldwide. These bacteria form biofilms on both biotic and abiotic surfaces causing biofilm-associated infections. Within the biofilm, these bacteria might develop persistent and antimicrobial resistant characteristics resulting in chronic infections and treatment failures. Garlic exhibits broad pharmaceutical properties and inhibitory activities against S. aureus. We investigated the effects of aqueous fresh garlic extract on biofilm formation in S. aureus ATCC25923 and MRSA strains under chemopreventive and chemotherapeutic conditions. The viable bacteria and biofilm levels were quantified through colony count and crystal violet staining, respectively. The use of fresh garlic extract under both conditions significantly inhibited biofilm formation in S. aureus strains ATCC25923 and MRSA. Garlic could be developed as either a prophylactic or therapeutic agent to manage S. aureus biofilm-associated infections.

  17. Melissa officinalis extract inhibits laser-induced choroidal neovascularization in a rat model.

    Science.gov (United States)

    Lee, Eun Kyoung; Kim, Young Joo; Kim, Jin Young; Song, Hyun Beom; Yu, Hyeong Gon

    2014-01-01

    This study investigated the effect of Melissa officinalis extract on laser-induced choroidal neovascularization (CNV) in a rat model. The mechanism by which M. officinalis extract acted was also investigated. Experimental CNV was induced by laser photocoagulation in Brown Norway rats. An active fraction of the Melissa leaf extract was orally administered (50 or 100 mg/kg/day) beginning 3 days before laser photocoagulation and ending 14 days after laser photocoagulation. Optical coherence tomography and fluorescein angiography were performed in vivo to evaluate the thickness and leakage of CNV. Choroidal flat mount and histological analysis were conducted to observe the CNV in vitro. Vascular endothelial growth factor (VEGF), matrix metalloproteinase (MMP)-2, and MMP-9 expression were measured in retinal and choroidal-scleral lysates 7 days after laser injury. Moreover, the effect of M. officinalis extract on tertiary-butylhydroperoxide (t-BH)-induced VEGF secretion and mRNA levels of VEGF, MMP-2, and MMP-9 were evaluated in human retinal epithelial cells (ARPE-19) as well as in human umbilical vein endothelial cells (HUVECs). The CNV thickness in M. officinalis-treated rats was significantly lower than in vehicle-treated rats by histological analysis. The CNV thickness was 33.93±7.64 µm in the high-dose group (Pofficinalis, which was significantly lower than in control rats (53.4%, Pofficinalis extract suppressed t-BH-induced transcription of VEGF and MMP-9 in ARPE-19 cells and HUVECs. Systemic administration of M. officinalis extract suppressed laser-induced CNV formation in rats. Inhibition of VEGF and MMP-9 via anti-oxidative activity may underlie this effect.

  18. Antibacterial, antioxidant and tyrosinase-inhibition activities of pomegranate fruit peel methanolic extract

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    Fawole Olaniyi A

    2012-10-01

    Full Text Available Abstract Background This study evaluated, using in vitro assays, the antibacterial, antioxidant, and tyrosinase-inhibition activities of methanolic extracts from peels of seven commercially grown pomegranate cultivars. Methods Antibacterial activity was tested on Gram-positive (Bacillus subtilis and Staphylococcus aureus and Gram-negative bacteria (Escherichia coli and Klebsiella pneumonia using a microdilution method. Several potential antioxidant activities, including radical-scavenging ability (RSA, ferrous ion chelating (FIC and ferric ion reducing antioxidant power (FRAP, were evaluated. Tyrosinase enzyme inhibition was investigated against monophenolase (tyrosine and diphenolase (DOPA, with arbutin and kojic acid as positive controls. Furthermore, phenolic contents including total flavonoid content (TFC, gallotannin content (GTC and total anthocyanin content (TAC were determined using colourimetric methods. HPLC-ESI/MSn analysis of phenolic composition of methanolic extracts was also performed. Results Methanolic peel extracts showed strong broad-spectrum activity against Gram-positive and Gram-negative bacteria, with the minimum inhibitory concentrations (MIC ranging from 0.2 to 0.78 mg/ml. At the highest concentration tested (1000 μg/ml, radical scavenging activities were significantly higher in Arakta (83.54%, Ganesh (83.56%, and Ruby (83.34% cultivars (P50% against monophenolase and diphenolase activities at the highest screening concentration. The most active peel extract was the Bhagwa cultivar against monophenolase and the Arakta cultivar against diphenolase with IC50 values of 3.66 μg/ml and 15.88 μg/ml, respectively. High amounts of phenolic compounds were found in peel extracts with the highest and lowest total phenolic contents of 295.5 (Ganesh and 179.3 mg/g dry extract (Molla de Elche, respectively. Catechin, epicatechin, ellagic acid and gallic acid were found in all cultivars, of which ellagic acid was the most abundant

  19. Clinically significant CYP2C inhibition by noscapine but not by glucosamine.

    Science.gov (United States)

    Rosenborg, S; Stenberg, M; Otto, S; Ostervall, J; Masquelier, M; Yue, Q-Y; Bertilsson, L; Eliasson, E

    2010-09-01

    Noscapine and glucosamine reportedly interact with warfarin. We investigated the effects of these drugs on various cytochrome P450 (CYP) activity markers. Twelve healthy subjects were phenotyped at baseline and during separate treatments with noscapine and glucosamine. Whereas glucosamine had no significant effect on CYP activity, noscapine caused marked inhibition of CYP2C9 (4.9-fold increase in urinary losartan/E3174 ratio) and CYP2C19 (3.6-fold increase in the plasma omeprazole/5-hydroxyomeprazole ratio). Noscapine-dependent inhibition of CYP2C9 may explain the interaction with warfarin.

  20. Inhibition of human copper trafficking by a small molecule significantly attenuates cancer cell proliferation

    Science.gov (United States)

    Wang, Jing; Luo, Cheng; Shan, Changliang; You, Qiancheng; Lu, Junyan; Elf, Shannon; Zhou, Yu; Wen, Yi; Vinkenborg, Jan L.; Fan, Jun; Kang, Heebum; Lin, Ruiting; Han, Dali; Xie, Yuxin; Karpus, Jason; Chen, Shijie; Ouyang, Shisheng; Luan, Chihao; Zhang, Naixia; Ding, Hong; Merkx, Maarten; Liu, Hong; Chen, Jing; Jiang, Hualiang; He, Chuan

    2015-12-01

    Copper is a transition metal that plays critical roles in many life processes. Controlling the cellular concentration and trafficking of copper offers a route to disrupt these processes. Here we report small molecules that inhibit the human copper-trafficking proteins Atox1 and CCS, and so provide a selective approach to disrupt cellular copper transport. The knockdown of Atox1 and CCS or their inhibition leads to a significantly reduced proliferation of cancer cells, but not of normal cells, as well as to attenuated tumour growth in mouse models. We show that blocking copper trafficking induces cellular oxidative stress and reduces levels of cellular ATP. The reduced level of ATP results in activation of the AMP-activated protein kinase that leads to reduced lipogenesis. Both effects contribute to the inhibition of cancer cell proliferation. Our results establish copper chaperones as new targets for future developments in anticancer therapies.

  1. Inhibition of human copper trafficking by a small molecule significantly attenuates cancer cell proliferation.

    Science.gov (United States)

    Wang, Jing; Luo, Cheng; Shan, Changliang; You, Qiancheng; Lu, Junyan; Elf, Shannon; Zhou, Yu; Wen, Yi; Vinkenborg, Jan L; Fan, Jun; Kang, Heebum; Lin, Ruiting; Han, Dali; Xie, Yuxin; Karpus, Jason; Chen, Shijie; Ouyang, Shisheng; Luan, Chihao; Zhang, Naixia; Ding, Hong; Merkx, Maarten; Liu, Hong; Chen, Jing; Jiang, Hualiang; He, Chuan

    2015-12-01

    Copper is a transition metal that plays critical roles in many life processes. Controlling the cellular concentration and trafficking of copper offers a route to disrupt these processes. Here we report small molecules that inhibit the human copper-trafficking proteins Atox1 and CCS, and so provide a selective approach to disrupt cellular copper transport. The knockdown of Atox1 and CCS or their inhibition leads to a significantly reduced proliferation of cancer cells, but not of normal cells, as well as to attenuated tumour growth in mouse models. We show that blocking copper trafficking induces cellular oxidative stress and reduces levels of cellular ATP. The reduced level of ATP results in activation of the AMP-activated protein kinase that leads to reduced lipogenesis. Both effects contribute to the inhibition of cancer cell proliferation. Our results establish copper chaperones as new targets for future developments in anticancer therapies.

  2. Sida rhombifolia ssp. retusa seed extract inhibits DEN induced murine hepatic preneoplasia and carbon tetrachloride hepatotoxicity.

    Science.gov (United States)

    Poojari, Radhika; Gupta, Sanjay; Maru, Girish; Khade, Bharat; Bhagwat, Sanjay

    2009-01-01

    Sida rhombifolia ssp. retusa is a well established drug in the Ayurvedic system of medicine used for antirheumatism and antiasthmatism. Inhibitory effects of S. rhombifolia ssp. retusa seed extract on DEN induced hepatocellular preneoplastic foci and carbon tetrachloride (CCl4) induced hepatotoxicity was investigated in rats. Rats received DEN, 1ppm/g b.w. in drinking water for 6 weeks or CCl(4), 0.7 ml/kg i.p. once a week for 4 weeks and seed extract 50 mg, 100 mg/kg b.w. orally prior, during and after exposure to DEN/CCl4 for 20 or 5 weeks, respectively. Treatment with seed extract significantly inhibited the increase in DEN/CCl(4) induced activities of pre-cancerous marker enzymes; gamma-glutamyl transpeptidase, glutathione-S-transferase, hepatotoxicity marker enzymes; glutamate pyruvate transaminase, glutamate oxaloacetate transaminase and alkaline phosphatase as well as lipid peroxidase. Depleted glutathione, protein and albumin levels were restored. Also, histopathological and transmission electron microscopic studies showed prevention of cellular degenerative changes. The chemopreventive and hepatoprotective potentials of seed extract are due to free radical scavenging activity and restoration of cellular structural integrity.

  3. Methanolic Extracts of Bitter Melon Inhibit Colon Cancer Stem Cells by Affecting Energy Homeostasis and Autophagy

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    Deep Kwatra

    2013-01-01

    Full Text Available Bitter melon fruit is recommended in ancient Indian and Chinese medicine for prevention/treatment of diabetes. However its effects on cancer progression are not well understood. Here, we have determined the efficacy of methanolic extracts of bitter melon on colon cancer stem and progenitor cells. Both, whole fruit (BMW and skin (BMSk extracts showed significant inhibition of cell proliferation and colony formation, with BMW showing greater efficacy. In addition, the cells were arrested at the S phase of cell cycle. Moreover, BMW induced the cleavage of LC3B but not caspase 3/7, suggesting that the cells were undergoing autophagy and not apoptosis. Further confirmation of autophagy was obtained when western blots showed reduced Bcl-2 and increased Beclin-1, Atg 7 and 12 upon BMW treatment. BMW reduced cellular ATP levels coupled with activation of AMP activated protein kinase; on the other hand, exogenous additions of ATP lead to revival of cell proliferation. Finally, BMW treatment results in a dose-dependent reduction in the number and size of colonospheres. The extracts also decreased the expression of DCLK1 and Lgr5, markers of quiescent, and activated stem cells. Taken together, these results suggest that the extracts of bitter melon can be an effective preventive/therapeutic agent for colon cancer.

  4. Boswellia carterii extract inhibits TH1 cytokines and promotes TH2 cytokines in vitro.

    Science.gov (United States)

    Chevrier, Marc R; Ryan, Abigail E; Lee, David Y-W; Zhongze, Ma; Wu-Yan, Zhang; Via, Charles S

    2005-05-01

    Traditional herbal formulas used to treat inflammatory arthritis in China and India include Boswellia carterii or Boswellia serrata. They both contain boswellic acids (BAs) which have been shown to exhibit anti-inflammatory and antiarthritic properties. This study tests the hypothesis that mixtures of BAs derived from B. carterii have immunomodulatory properties. B. carterii plant resin obtained from China was prepared as an ethanol extract, and the presence of seven BAs was confirmed by column chromatography, high-performance liquid chromatography, and UV laser desorption/ionization tandem mass spectroscopy. The extract was then tested for its ability to alter in vitro production of TH1 cytokines (interleukin-2 [IL-2] and gamma interferon) and TH2 cytokines (IL-4 and IL-10) by murine splenocytes. Delivery of the resin extract using ethanol as a solvent resulted in significant cellular toxicity not seen with the addition of ethanol alone. By contrast, delivery of the resin extract using a sesame oil solvent resulted in a dose-dependent inhibition of TH1 cytokines coupled with a dose-dependent potentiation of TH2 cytokines. These results indicate that a purified mixture of BAs from B. carterii plant resin exhibits carrier-dependent immunomodulatory properties in vitro.

  5. Intracellular coagulation inhibits the extraction of proteins from Prochloron

    Science.gov (United States)

    Fall, R.; Lewin, R. A.; Fall, L. R.

    1983-01-01

    Protein extraction from the prokaryotic alga Prochloron LP (isolated from the ascidian host Lissoclinum patella) was complicated by an irreversible loss of cell fragility in the isolated algae. Accompanying this phenomenon, which is termed intracellular coagulation, was a redistribution of thylakoids around the cell periphery, a loss of photosynthetic O2 production, and a drastic decrease in the extractability of cell proteins. Procedures are described for the successful preparation and transport of cell extracts yielding the enzymes glucose-6-phosphate dehydrogenase and 6-phosphogluconate dehydrogenase as well as other soluble proteins.

  6. Intracellular coagulation inhibits the extraction of proteins from Prochloron

    Science.gov (United States)

    Fall, R.; Lewin, R. A.; Fall, L. R.

    1983-01-01

    Protein extraction from the prokaryotic alga Prochloron LP (isolated from the ascidian host Lissoclinum patella) was complicated by an irreversible loss of cell fragility in the isolated algae. Accompanying this phenomenon, which is termed intracellular coagulation, was a redistribution of thylakoids around the cell periphery, a loss of photosynthetic O2 production, and a drastic decrease in the extractability of cell proteins. Procedures are described for the successful preparation and transport of cell extracts yielding the enzymes glucose-6-phosphate dehydrogenase and 6-phosphogluconate dehydrogenase as well as other soluble proteins.

  7. Inhibition of 304 stainless steel corrosion in acidic solution by Ferula gumosa (galbanum) extract

    Energy Technology Data Exchange (ETDEWEB)

    Behpour, M.; Ghoreishi, S.M.; Soltani, N. [Department of Chemistry, Faculty of Science, University of Kashan (Iran); Kashani, M.K. [Department of Chemistry, Faculty of Science, University of Kashan (Iran); Barij Essence pharmaceutical, Kashan (Iran)

    2009-11-15

    The inhibition effect of the extract of galbanum (Ferula gummosa Boiss.) on the corrosion of 304 stainless steel in 2 M HCl solution was studied by weight loss measurements, Tafel polarization, and electrochemical impedance spectroscopy (EIS) methods. It was found that the inhibition efficiency (IE) increases as the extract concentration is increased. Tafel polarization method revealed the mixed mode inhibition of galbanum extract (GE) with predominant control of anodic reaction. The effect of temperature on the corrosion behavior of steel indicates that inhibition efficiency of the natural substance increases with the rise in temperature. At all temperatures, the adsorption of the extract components onto the steel surface was found to follow the Temkin adsorption isotherm. (Abstract Copyright [2009], Wiley Periodicals, Inc.)

  8. Evaluation of in vitro antioxidant potential anti-inflammatory activity and melanogenesis inhibition of Artocarpus hirsutus Lam. extracts

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    Mahadeva Nayak

    2015-08-01

    Full Text Available Artocarpus hirsutus Lam. belongs to Moraceae family and is endemic to Western Ghats and Kerala in India. This species is found to be effective in traditional medicine for the treatment of ulcer diarrhea and pimples. However extensive biological evaluation on each component of this specific species rarely appears in the literature which restricts its applicability as medicinal herb. The leaf bark and wood of Artocarpus hirsutus Lam. were separately extracted with hot ethanol. The wood extract was further fractionated to isolate major active molecule whose structure was determined from its NMR spectra and LCMS analysis. All the extracts of A. hirsutus Lam. were then studied in vitro to evaluate their potential on tyrosinase inhibition free radical scavenging activity by 11-Diphenyl-2-picrylhydrazyl DPPH method and oxygen radical absorbance capacity ORAC. Furthermore their effects on melanogenesis inhibition were also evaluated by using murine melanoma cells. Activity guided fractionation of wood extract yielded a pure molecule that was characterized as oxyresveratrol. It was observed that antioxidant activity was higher in wood extract compared to the leaf and bark extracts. Isolated pure oxyresveratrol exhibited a significant antioxidant potential with ORAC value of 366532570 mol Trolox equivalentg and having an IC50 of 4.3 gmL for DPPH free radical scavenging activity. This molecule was found to be effective for the tyrosinase inhibition with an IC50 of 0.1 gmL and melanogenesis inhibition in cultured melanoma cells by 44.62 at 0.2 gmL. Oxyresveratrol also exhibited significant inhibition of lipopolysaccharide LPS induced tumour necrosis factor alpha TNF-amp945 secretion from J774A1 murine macrophage cell lines. This study provides substantial evidence for the presence of oxyresveratrol in the wood of A. hirsutus Lam. with promising anti-inflammatory antioxidant and skin lightening property.

  9. Inhibition of Cyclooxygenase Type 1 and 2 Enzyme by Aqueous Extract of Elaeagnus Angustifolia in Mice

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    Shahedeh Farahbakhsh

    2011-09-01

    Full Text Available  Introduction: It has been shown that the extract of Elaeagnus angustifolia can inhibit inflammation and pain induced by formalin in mice and rats. The aim of the present study is to reach evaluations of possible cellular and molecular mechanisms of Elaeagnus angustifolia extract in reducing pain and inflammation through examining the extract ability for inhibition of cyclooxygenase (Cox type 1 and 2 enzymes and corticosterone release from adrenal glands in mice. Methods: Male Swiss Webster mice were evaluated through the injection of 2 μliters to the plantar part of right foot. Elaeagnus angustifolia extract was injected to the animals 30 minutes before formalin. In order to evaluate the mechanism of extract, naloxone and memantine were administered intrapretonealy 30 minutes before the extract administration. In separate groups, after injection of extract, blood samples were taken from animals and corticosterone concentrations were measured. In an in vitro study the effect of extract on the activity of cyclooxygenase type 1 and 2 was assessed. Results: the research data showed the ineffectiveness of the extract on acute phase of pain induced by formalin but it completely inhibits the chronic phase. Naloxone and Memantine administration had no effect on the efficacy of extract in the chronic phase. Also the extract administration did not increase the plasma concentration of corticosterone in mice, but in vitro inhibited Cox1 and Cox 2 enzymes. Discussion: These results indicate that Elaeagnus angustifolia extract probably reducesww pain and inflammation caused by formalin in mice by inhibiting cyclooxygenase type 1 and 2 enzymes.

  10. Flavonoids, Antioxidant Potential, and Acetylcholinesterase Inhibition Activity of the Extracts from the Gametophyte and Archegoniophore of Marchantia polymorpha L.

    Science.gov (United States)

    Wang, Xin; Cao, Jianguo; Wu, Yuhuan; Wang, Quanxi; Xiao, Jianbo

    2016-03-17

    Marchantia polymorpha L. is a representative bryophyte used as a traditional Chinese medicinal herb for scald and pneumonia. The phytochemicals in M. polymorpha L. are terpenoids and flavonoids, among which especially the flavonoids show significant human health benefits. Many researches on the gametophyte of M. polymorpha L. have been reported. However, as the reproductive organ of M. polymorpha L., the bioactivity and flavonoids profile of the archegoniophore have not been reported, so in this work the flavonoid profiles, antioxidant and acetylcholinesterase inhibition activities of the extracts from the archegoniophore and gametophyte of M. polymorpha L. were compared by radical scavenging assay methods (DPPH, ABTS, O(2-)), reducing power assay, acetylcholinesterase inhibition assay and LC-MS analysis. The results showed that the total flavonoids content in the archegoniophore was about 10-time higher than that of the gametophyte. Differences between the archegoniophore and gametophyte of M. polymorpha L. were observed by LC-MS analysis. The archegoniophore extracts showed stronger bio-activities than those of the gametophyte. The archegoniophore extract showed a significant acetylcholinesterase inhibition, while the gametophyte extract hardly inhibited it.

  11. Flavonoids, Antioxidant Potential, and Acetylcholinesterase Inhibition Activity of the Extracts from the Gametophyte and Archegoniophore of Marchantia polymorpha L.

    Directory of Open Access Journals (Sweden)

    Xin Wang

    2016-03-01

    Full Text Available Marchantia polymorpha L. is a representative bryophyte used as a traditional Chinese medicinal herb for scald and pneumonia. The phytochemicals in M. polymorpha L. are terpenoids and flavonoids, among which especially the flavonoids show significant human health benefits. Many researches on the gametophyte of M. polymorpha L. have been reported. However, as the reproductive organ of M. polymorpha L., the bioactivity and flavonoids profile of the archegoniophore have not been reported, so in this work the flavonoid profiles, antioxidant and acetylcholinesterase inhibition activities of the extracts from the archegoniophore and gametophyte of M. polymorpha L. were compared by radical scavenging assay methods (DPPH, ABTS, O2−, reducing power assay, acetylcholinesterase inhibition assay and LC-MS analysis. The results showed that the total flavonoids content in the archegoniophore was about 10-time higher than that of the gametophyte. Differences between the archegoniophore and gametophyte of M. polymorpha L. were observed by LC-MS analysis. The archegoniophore extracts showed stronger bio-activities than those of the gametophyte. The archegoniophore extract showed a significant acetylcholinesterase inhibition, while the gametophyte extract hardly inhibited it.

  12. Inhibition of HIV-1 infection by aqueous extracts of Prunella vulgaris L.

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    McCoy Joe-Ann

    2011-04-01

    Full Text Available Abstract Background The mint family (Lamiaceae produces a wide variety of constituents with medicinal properties. Several family members have been reported to have antiviral activity, including lemon balm (Melissa officinalis L., sage (Salvia spp., peppermint (Mentha × piperita L., hyssop (Hyssopus officinalis L., basil (Ocimum spp. and self-heal (Prunella vulgaris L.. To further characterize the anti-lentiviral activities of Prunella vulgaris, water and ethanol extracts were tested for their ability to inhibit HIV-1 infection. Results Aqueous extracts contained more anti-viral activity than did ethanol extracts, displaying potent antiviral activity against HIV-1 at sub μg/mL concentrations with little to no cellular cytotoxicity at concentrations more than 100-fold higher. Time-of-addition studies demonstrated that aqueous extracts were effective when added during the first five hours following initiation of infection, suggesting that the botanical constituents were targeting entry events. Further analysis revealed that extracts inhibited both virus/cell interactions and post-binding events. While only 40% inhibition was maximally achieved in our virus/cell interaction studies, extract effectively blocked post-binding events at concentrations similar to those that blocked infection, suggesting that it was targeting of these latter steps that was most important for mediating inhibition of virus infectivity. Conclusions We demonstrate that aqueous P. vulgaris extracts inhibited HIV-1 infectivity. Our studies suggest that inhibition occurs primarily by interference of early, post-virion binding events. The ability of aqueous extracts to inhibit early events within the HIV life cycle suggests that these extracts, or purified constituents responsible for the antiviral activity, are promising microbicides and/or antivirals against HIV-1.

  13. Gracilaria edulis extract induces apoptosis and inhibits tumor in Ehrlich ascites tumor cells in vivo.

    Science.gov (United States)

    Patra, Satyajit; Muthuraman, Meenakshi Sundaram

    2013-11-25

    Marine environment is inestimable for their chemical and biological diversity and therefore is an extraordinary resource for the discovery of new anticancer drugs. Recent development in elucidation of the mechanism and therapeutic action of natural products helped to evaluate for their potential activity. We evaluated Gracilaria edulis J. Ag (Brown algae), for its antitumor potential against the Ehrlich ascites tumor (EAT) in vivo and in vitro. Cytotoxicity evaluation of Ethanol Extract of Gracilaria edulis (EEGE) using EAT cells showed significant activity. In vitro studies indicated that EEGE cytotoxicity to EAT cells is mediated through its ability to produce reactive oxygen species (ROS) and therefore decreasing intracellular glutathione (GSH) levels may be attributed to oxidative stress. Apoptotic parameters including Annexin-V positive cells, increased levels of DNA fragmentation and increased caspase-2, caspase-3 and caspase-9 activities indicated the mechanism might be by inducing apoptosis. Intraperitoneally administration of EEGE to EAT-bearing mice helped to increase the lifespan of the animals significantly inhibited tumor growth and increased survival of mice. Extensive hematology, biochemistry and histopathological analysis of liver and kidney indicated that daily doses of EEGE up to 300 mg/kg for 35 days are well tolerated and did not cause hematotoxicity nor renal or hepatotoxicity. Comprehensive antitumor analysis in animal model and in Ehrlich Ascites Tumor cells was done including biochemical, and pathological evaluations indicate antitumor activity of the extract and non toxic in vivo. It was evident that the mechanism explains the apoptotic activity of the algae extract.

  14. Inhibition of bacterial, fungal and plant growth by testa extracts of Citrullus genotypes

    Science.gov (United States)

    Watermelon (Citrullus lanatus var. lanatus (Thunb.) Matsum & Nakai) seed exudates inhibit germination and seedling growth of several plant species and growth of pathogenic fungi and bacteria. This study was conducted to determine if extractable components in testae contribute to the inhibition. T...

  15. Behaviorally inhibited individuals demonstrate significantly enhanced conditioned response acquisition under non-optimal learning conditions.

    Science.gov (United States)

    Holloway, J L; Allen, M T; Myers, C E; Servatius, R J

    2014-03-15

    Behavioral inhibition (BI) is an anxiety vulnerability factor associated with hypervigilance to novel stimuli, threat, and ambiguous cues. The progression from anxiety risk to a clinical disorder is unknown, although the acquisition of defensive learning and avoidance may be a critical feature. As the expression of avoidance is also central to anxiety development, the present study examined avoidance acquisition as a function of inhibited temperament using classical eyeblink conditioning. Individuals were classified as behaviorally inhibited (BI) or non-inhibited (NI) based on combined scores from the Adult and Retrospective Measures of Behavioural Inhibition (AMBI and RMBI, respectively). Acquisition was assessed using delay, omission, or yoked conditioning schedules of reinforcement. Omission training was identical to delay, except that the emission of an eyeblink conditioned response (CR) resulted in omission of the unconditioned airpuff stimulus (US) on that trial. Each subject in the yoked group was matched on total BI score to a subject in the omission group, and received the same schedule of CS and US delivery, resulting in a partial reinforcement training schedule. Delay conditioning elicited significantly more CRs compared to the omission and yoked contingencies, the latter two of which did not differ from each other. Thus, acquisition of an avoidance response was not apparent. BI individuals demonstrated enhanced acquisition overall, while partial reinforcement training significantly distinguished between BI and NI groups. Enhanced learning in BI may be a function of an increased defensive learning capacity, or sensitivity to uncertainty. Further work examining the influence of BI on learning acquisition is important for understanding individual differences in disorder etiology in anxiety vulnerable cohorts.

  16. Effect of crude saponins from Gaultheria trichophylla extract on growth inhibition in human colorectal cancer cells

    Directory of Open Access Journals (Sweden)

    Fiaz Alam

    2015-03-01

    Full Text Available The genus Gaultheria also comprised of species with reported cytotoxic activities. Current research work was carried out to evaluate G. trichophylla crude extract and respective saponins fraction against human colorectal cancer cell line (Caco-2 based on cell viability assays. Caco-2 cells treated with the crude extract showed significant growth inhibition (p< 0.001 in a dose dependent manner with apparent IC50 value of 200 μg/mL and 100 μg/mL in MTT and NRU assays respectively. The fractioned crude saponins showed an enhanced response and inhibited the growth of Caco-2 by 93.6 and 97.4% in MTT and NRU assays respectively, with compared to actinomycin-D (65%. The DAPI staining of cell treated with crude saponins observed under confocal microscope showed shrunken nuclei with apparent nuclear fragmentation and chromatin condensation indicating apoptosis mode of cell death. The study exhibited that the G. Trichophylla saponins induced apoptosis of Caco-2 cell lines. This study provides new evidences to further explore this plant for the novel targets in anticancer drug development.

  17. Comparative spectroscopic analysis of urinary calculi inhibition by Larrea Tridentata infusion and NDGA chemical extract

    Science.gov (United States)

    Manciu, Felicia

    2012-10-01

    In the present comparative spectroscopic study we try to understand calcium oxalate kidney stone formation as well as its inhibition by using a traditional medicine approach with Larrea Tridentata (LT) herbal extracts and nordihydroguaiaretic acid (NDGA), which is a chemical extract of the LT bush. The samples were synthesized without and with LT or NDGA using a simplified single diffusion gel growth technique. While the use of infusion from LT decreases the sizes of calcium oxalate crystals and also changes their structure from monohydrate for pure crystals to dihydrate for crystals grown with different amounts of inhibitor, both Raman and infrared absorption spectroscopic techniques, which are the methods of analysis employed in this work, reveal that NDGA is not responsible for the change in the morphology of calcium oxalate crystals and does not contribute significantly to the inhibition process. The presence of NDGA slightly affects the structure of the crystals by modifying the strength of the C-C bonds as seen in the Raman data. Also, the current infrared absorption results demonstrate the presence of NDGA in the samples through a vibrational line that corresponds to the double bond between carbon atoms of the ester group of NDGA.

  18. Inhibition of Mild Steel Corrosion in Acidic Medium by Aqueous Extract of Tridax procumbens L.

    OpenAIRE

    Ilayaraja, G.; Sasieekhumar, A. R.; Dhanakodi, P.

    2011-01-01

    The inhibition efficiency (IE) of an aqueous extract of Tridax procumbens L. in controlling corrosion of mild steel has been investigated by weight loss method in the absence and presence of corrosion inhibitor at different time interval at room temperature. The result showed that the corrosion inhibition efficiency of these compounds was found to vary with different time interval and different acid concentration. Also, it was found that the corrosion inhibition behavior of Tridax procumbens ...

  19. Cinnamon extract inhibits tau aggregation associated with Alzheimer’s Disease in vitro

    Science.gov (United States)

    An aqueous extract of Ceylon cinnamon (C. zeylanicum) was found to inhibit tau aggregation and filament formation, hallmarks of Alzheimer’s disease (AD) in vitro using brain cells taken from patients who died with AD. The extract also promoted complete disassembly of recombinant tau filaments, and ...

  20. Inhibition of pancreatic lipase and amylase by extracts of different spices and plants.

    Science.gov (United States)

    Sellami, Mohamed; Louati, Hanen; Kamoun, Jannet; Kchaou, Ali; Damak, Mohamed; Gargouri, Youssef

    2017-05-01

    The aim of this study is to search new anti-obesity and anti-diabetic agents from plant and spices crude extracts as alternative to synthetic drugs. The inhibitory effect of 72 extracts was evaluated, in vitro, on lipase and amylase activities. Aqueous extracts of cinnamon and black tea exhibited an appreciable inhibitory effect on pancreatic amylase with IC50 values of 18 and 87 μg, respectively. Aqueous extracts of cinnamon and mint showed strong inhibitory effects against pancreatic lipase with IC50 of 45 and 62 μg, respectively. The presence of bile salts and colipase or an excess of interface failed to restore the lipase activity. Therefore, the inhibition of pancreatic lipase, by extracts of spices and plants, belongs to an irreversible inhibition. Crude extract of cinnamon showed the strongest anti-lipase and anti-amylase activities which offer a prospective therapeutic approach for the management of diabetes and obesity.

  1. Rock Tea extract (Jasonia glutinosa) relaxes rat aortic smooth muscle by inhibition of L-type Ca(2+) channels.

    Science.gov (United States)

    Valero, Marta Sofía; Oliván-Viguera, Aida; Garrido, Irene; Langa, Elisa; Berzosa, César; López, Víctor; Gómez-Rincón, Carlota; Murillo, María Divina; Köhler, Ralf

    2015-12-01

    In traditional herbal medicine, Rock Tea (Jasonia glutinosa) is known for its prophylactic and therapeutic value in various disorders including arterial hypertension. However, the mechanism by which Rock Tea exerts blood pressure-lowering actions has not been elucidated yet. Our aim was to demonstrate vasorelaxing effects of Rock Tea extract and to reveal its possible action mechanism. Isometric myography was conducted on high-K+-precontracted rings from rat thoracic aorta and tested extracts at concentrations of 0.5-5 mg/ml. Whole-cell patch-clamp experiments were performed in rat aortic vascular smooth muscle cells (line A7r5) to determine blocking effects on L-type Ca(2+) channels. Rock Tea extract relaxed the aorta contracted by high [K+] concentration dependently with an EC50 of ≈2.4 mg/ml and produced ≈75 % relaxation at the highest concentration tested. The L-type Ca(2+) channel blocker, verapamil (10(-6) M), had similar effects. Rock Tea extract had no effect in nominally Ca(2+)-free high-K(+) buffer but significantly inhibited contractions to re-addition of Ca(2+). Rock Tea extract inhibited the contractions induced by the L-type Ca(2+) channel activator Bay K 8644 (10(-5) M) and by phenylephrine (10(-6) M). Rock Tea extract and Y-27632 (10(-6) M), Rho-kinase inhibitor, had similar effects and the respective effects were not additive. Patch-clamp experiments demonstrated that Rock Tea extract (2.5 mg/ml) virtually abolished L-type Ca(2+) currents in A7r5. We conclude that Rock Tea extract produced vasorelaxation of rat aorta and that this relaxant effect is mediated by inhibition of L-type Ca(2+) channels. Rock Tea extracts may be of phytomedicinal value for prevention and adjuvant treatment of hypertension and other cardiovascular diseases.

  2. Inhibition of Morganella morganii Histidine Decarboxylase Activity and Histamine Accumulation in Mackerel Muscle Derived from Filipendula ulumaria Extracts.

    Science.gov (United States)

    Nitta, Yoko; Yasukata, Fumiko; Kitamoto, Noritoshi; Ito, Mikiko; Sakaue, Motoyoshi; Kikuzaki, Hiroe; Ueno, Hiroshi

    2016-03-01

    Filipendula ulmaria, also known as meadowsweet, is an herb; its extract was examined for the prevention of histamine production, primarily that caused by contaminated fish. The efficacy of meadowsweet was assessed using two parameters: inhibition of Morganella morganii histidine decarboxylase (HDC) and inhibition of histamine accumulation in mackerel. Ellagitannins from F. ulmaria (rugosin D, rugosin A methyl ester, tellimagrandin II, and rugosin A) were previously shown to be potent inhibitors of human HDC; and in the present work, these compounds inhibited M. morganii HDC, with half maximal inhibitory concentration values of 1.5, 4.4, 6.1, and 6.8 μM, respectively. Application of the extracts (at 2 wt%) to mackerel meat yielded significantly decreased histamine accumulation compared with treatment with phosphate-buffered saline as a control. Hence, F. ulmaria exhibits inhibitory activity against bacterial HDC and might be effective for preventing food poisoning caused by histamine.

  3. Crude fatty acid extracts of Streptomyces sps inhibits the biofilm forming Streptococcus pyogenes ATCC 19615

    Directory of Open Access Journals (Sweden)

    Rajalakshm Manickam

    2014-01-01

    Full Text Available Normal 0 false false false EN-US X-NONE X-NONE MicrosoftInternetExplorer4 Crude fatty acid extract of soil Streptomyces sps on the biofilm formation by Streptococcus pyogenes ATCC 19615 was investigated. Totally, 25 Streptomyces sps were isolated identified from the soil samples collected from Nilgiris hill station. All the isolates were subjected to hydrogen peroxide assay, fatty acid extraction and antibiofilm assay. The fatty acid extracts of S8, S9, and S15 inhibited S. pyogenes at MIC 10 µg/ml. The BIC was observed as 84.6% , 96.41%, 80.5% at 50 µg/ml concentration. Streptolysin S assay showed that the crude lipid extracts have the capability of inhibiting the Streptolysin S activity. There were changes in extracellular protein of the pathogen exposed to the S8, S9 and S15 crude fatty acid extracts (50 µg/ml at the range of 100-120 kDa which elucidates that the fatty acid extracts have a significant role in altering the extracellular protein which might be responsible for virulence of the pathogen. /* Style Definitions */ table.MsoNormalTable {mso-style-name:"Table Normal"; mso-tstyle-rowband-size:0; mso-tstyle-colband-size:0; mso-style-noshow:yes; mso-style-priority:99; mso-style-qformat:yes; mso-style-parent:""; mso-padding-alt:0in 5.4pt 0in 5.4pt; mso-para-margin:0in; mso-para-margin-bottom:.0001pt; mso-pagination:widow-orphan; font-size:11.0pt; font-family:"Calibri","sans-serif"; mso-ascii-font-family:Calibri; mso-ascii-theme-font:minor-latin; mso-fareast-font-family:"Times New Roman"; mso-fareast-theme-font:minor-fareast; mso-hansi-font-family:Calibri; mso-hansi-theme-font:minor-latin; mso-bidi-font-family:"Times New Roman"; mso-bidi-theme-font:minor-bidi;}

  4. Hibiscus sabdariffa extract inhibits in vitro biofilm formation capacity of Candida albicans isolated from recurrent urinary tract infections

    Institute of Scientific and Technical Information of China (English)

    Issam Alshami; Ahmed E Alharbi

    2014-01-01

    Objective: To explore the prevention of recurrent candiduria using natural based approaches and to study the antimicrobial effect of Hibiscus sabdariffa (H. sabdariffa) extract and the biofilm forming capacity of Candida albicans strains in the present of the H. sabdariffa extract.Methods:In this particular study, six strains of fluconazole resistant Candida albicans isolated from recurrent candiduria were used. The susceptibility of fungal isolates, time-kill curves and biofilm forming capacity in the present of the H. sabdariffa extract were determined. Results: Various levels minimum inhibitory concentration of the extract were observed against all the isolates. Minimum inhibitory concentration values ranged from 0.5 to 2.0 mg/mL. Time-kill experiment demonstrated that the effect was fungistatic. The biofilm inhibition assay results showed that H. sabdariffa extract inhibited biofilm production of all the isolates. Conclusions: The results of the study support the potential effect of H. sabdariffa extract for preventing recurrent candiduria and emphasize the significance of the plant extract approach as a potential antifungal agent.

  5. Identification of components of Prunus africana extract that inhibit lipid peroxidation.

    Science.gov (United States)

    Hass, M A; Nowak, D M; Leonova, E; Levin, R M; Longhurst, P A

    1999-11-01

    Extractive and chromatographic separations were performed on V-1326, a chloroform extract from the bark of Prunus africana (also referred to as Pygeum africanum), which is used to treat the symptoms associated with benign prostate hyperplasia (BPH). The relative amounts of eleven identified constituents in crude V-1326 and in separated fractions were determined using gas chromatographic analysis. The ability of V-1326 and its separated fractions to inhibit ferrous ion-induced stimulation of lipid peroxidation in microsomal preparations from rabbit livers was evaluated. The extract, V-1326, and fractions containing high levels of myristic acid potently inhibited lipid peroxidation.

  6. Melissa officinalis extract inhibits laser-induced choroidal neovascularization in a rat model.

    Directory of Open Access Journals (Sweden)

    Eun Kyoung Lee

    Full Text Available PURPOSE: This study investigated the effect of Melissa officinalis extract on laser-induced choroidal neovascularization (CNV in a rat model. The mechanism by which M. officinalis extract acted was also investigated. METHODS: Experimental CNV was induced by laser photocoagulation in Brown Norway rats. An active fraction of the Melissa leaf extract was orally administered (50 or 100 mg/kg/day beginning 3 days before laser photocoagulation and ending 14 days after laser photocoagulation. Optical coherence tomography and fluorescein angiography were performed in vivo to evaluate the thickness and leakage of CNV. Choroidal flat mount and histological analysis were conducted to observe the CNV in vitro. Vascular endothelial growth factor (VEGF, matrix metalloproteinase (MMP-2, and MMP-9 expression were measured in retinal and choroidal-scleral lysates 7 days after laser injury. Moreover, the effect of M. officinalis extract on tertiary-butylhydroperoxide (t-BH-induced VEGF secretion and mRNA levels of VEGF, MMP-2, and MMP-9 were evaluated in human retinal epithelial cells (ARPE-19 as well as in human umbilical vein endothelial cells (HUVECs. RESULTS: The CNV thickness in M. officinalis-treated rats was significantly lower than in vehicle-treated rats by histological analysis. The CNV thickness was 33.93±7.64 µm in the high-dose group (P<0.001, 44.09±12.01 µm in the low-dose group (P = 0.016, and 51.00±12.37 µm in the control group. The proportion of CNV lesions with clinically significant fluorescein leakage was 9.2% in rats treated with high-dose M. officinalis, which was significantly lower than in control rats (53.4%, P<0.001. The levels of VEGF, MMP-2, and MMP-9 were significantly lower in the high-dose group than in the control group. Meanwhile, M. officinalis extract suppressed t-BH-induced transcription of VEGF and MMP-9 in ARPE-19 cells and HUVECs. CONCLUSIONS: Systemic administration of M. officinalis extract suppressed laser

  7. In vitro α-glucosidase inhibition, antioxidant, anticancer, and antimycobacterial properties of ethyl acetate extract of Aegle tamilnadensis Abdul Kader (Rutaceae) leaf.

    Science.gov (United States)

    R, Pratap Chandran; S, Nishanth Kumar; S, Manju; S, Abdul Kader; B S, Dileep Kumar

    2015-01-01

    The present study was aimed to investigate in vitro α-glucosidase inhibition, antioxidant, anticancer, and antimycobacterial activities of the ethyl acetate extract of A. tamilnadensis leaves. The extract recorded strong α-glucosidase inhibition with an IC50 value of 100 μg/ml. The antioxidant potential of the extract was evaluated by nitric oxide radical inhibition, lipid peroxidation inhibition, ferric thiocyanate, and ABTS radical scavenging assay, and the extract recorded significant antioxidant activity. The ferric thiocyanate activity of extract was superior to butylated hydroxyl anisol (BHA), the standard antioxidant agent. The anticancer activity of the extract was evaluated against (1) breast cancer cell lines (MDAM B-231), (2) cervical cancer cell lines (HeLa), and (3) lung cancer cell line (A 549) using MTT assay, and significant activity was recorded against A 549 with an IC50 value of 64 μg/ml. Further studies on the morphology, acridine orange/ethidium bromide staining, and cell cycle analysis by flow cytometry confirm the extract-induced apoptosis in A 549. This extract also recorded significant anti-tuberculosis activity against Mycobacterium smegmatis. The current study suggests that the ethyl acetate extract of A. tamilnadensis is a potential source of natural α-glucosidase inhibitor and antioxidant for protection as well as prevention of life-threatening diseases like cancer.

  8. Inhibition of residual n-hexane in anaerobic digestion of lipid-extracted microalgal wastes and microbial community shift.

    Science.gov (United States)

    Yun, Yeo-Myeong; Shin, Hang-Sik; Lee, Chang-Kyu; Oh, You-Kwan; Kim, Hyun-Woo

    2016-04-01

    Converting lipid-extracted microalgal wastes to methane (CH4) via anaerobic digestion (AD) has the potential to make microalgae-based biodiesel platform more sustainable. However, it is apparent that remaining n-hexane (C6H14) from lipid extraction could inhibit metabolic pathway of methanogens. To test an inhibitory influence of residual n-hexane, this study conducted a series of batch AD by mixing lipid-extracted Chlorella vulgaris with a wide range of n-hexane concentration (∼10 g chemical oxygen demand (COD)/L). Experimental results show that the inhibition of n-hexane on CH4 yield was negligible up to 2 g COD/L and inhibition to methanogenesis became significant when it was higher than 4 g COD/L based on quantitative mass balance. Inhibition threshold was about 4 g COD/L of n-hexane. Analytical result of microbial community profile revealed that dominance of alkane-degrading sulfate-reducing bacteria (SRB) and syntrophic bacteria increased, while that of methanogens sharply dropped as n-hexane concentration increased. These findings offer a useful guideline of threshold n-hexane concentration and microbial community shift for the AD of lipid-extracted microalgal wastes.

  9. Antioxidant and α-amylase inhibition activities of phenolic compounds in the extracts of Indian honey

    Institute of Scientific and Technical Information of China (English)

    Subashini Devarajan; Subhashree Venugopal

    2012-01-01

    AIM:To evaluate the antioxidant and α-amylase inhibition potential of phenolic compounds in the extracts of Indian honey.METHODS:Phenolic compounds were extracted from Indian honey through column chromatography.The antioxidant potential of extracted phenolic compounds was measured by two different biochemical assays:ferric reducing antioxidant power (FRAP)assay and scavenging activity on 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals.Moreover,α-amylase inhibition assay of phenolic compounds of honey was also evaluated.RESULTS:The scavenging inhibition rate varied from 86.8% to 78.6% from the highest (6mg·mL-1) to the lowest (1.5 mg·mL-1) concentration,whereas,reducing power assay varied from 0.89 Abs to 0.19 Abs from the highest to the lowest concentration.Butylated hydroxytoluene (BHT) was used as reference compound for antioxidant assays.α-amylase inhibition assay is reported from the phenolic honey extracts for the first time.The inhibition rate for α-amylase varied from 88.8% to 30.5% from the highest (20 μg·mL-1) to the lowest concentration (4.μg·mL-1).CONCLUSION:Honey phenolic extract possessed antioxidant and α-amylase inhibition activity,thus increasing its potential therapeutic property.

  10. The Lignan-containing Extract of Schisandra chinensis Berries Inhibits the Growth of Chlamydia pneumonia.

    Science.gov (United States)

    Hakala, Elina; Hanski, Leena L; Yrjönen, Teijo; Vuorela, Heikki J; Vuorela, Pia M

    2015-06-01

    The purpose of this study was to investigate the effect and selectivity of an extract of Schisandra chinensis berries against Chlamydia pneumoniae and C. trachomatis. Among the ethnopharmacological uses of the extract from Schisandrae fructus are cough and pneumonia. Therefore we focused on respiratory pathogens. The extract completely inhibited the growth of C. pneumoniae strain CV6 at 250 μg/mL concentration. The inhibition of C. pneumoniae and C. trachomatis growth was dose dependent and established with three different strains. The extract inhibited C. pneumoniae production of infectious progeny in a dose dependent manner. Chlamydia selectivity was elucidated with growth inhibition measurements of three other respiratory bacterial species. A pure compound found in Schisandra chinensis berries, schisandrin B at 20.0 μg/mL concentration inhibited the growth of both C. pneumoniae and C. trachomatis. The extract was found to be non-toxic to the human host cells. These findings highlight the potential of the extract from Schisandra chinensis berries as a source for antichlamydial compounds.

  11. Extracts of Edible Plants Inhibit Pancreatic Lipase, Cholesterol Esterase and Cholesterol Micellization, and Bind Bile Acids

    Directory of Open Access Journals (Sweden)

    Julnaryn Intrawangso

    2012-01-01

    Full Text Available The application of edible plants with more effective ability to inhibit fat digestion and absorption has recently been explored for possible treatment of hyperlipidaemia. The aim of the present study is to investigate the effect of nine edible plants on the inhibition of pancreatic lipase and pancreatic cholesterol esterase activities, as well as the inhibition of cholesterol micelle formation, and bile acid binding. Our findings have shown strong pancreatic lipase inhibitory activity and the inhibition of cholesterol micellization by mulberry leaf extract. Safflower extract was the most potent inhibitor of pancreatic cholesterol esterase. In addition, cat’s whiskers and safflower extracts had a potent bile acid binding activity. It is suggested that a daily intake of these edible plants may delay postprandial hypertriacylglycerolaemia and hypercholesterolaemia, and therefore may be applied for the prevention and treatment of hyperlipidaemia.

  12. Inhibition of Advanced Glycation End-Product Formation and Antioxidant Activity by Extracts and Polyphenols from Scutellaria alpina L. and S. altissima L.

    OpenAIRE

    Izabela Grzegorczyk-Karolak; Krzysztof Gołąb; Jakub Gburek; Halina Wysokińska; Adam Matkowski

    2016-01-01

    Methanolic extracts from the aerial parts and roots of two Scutellaria species, S. alpina and S. altissima, and five polyphenols from these plants demonstrated a significant ability to inhibit the formation of advanced glycation end-products (AGE) in vitro. S. alpina, which is richer in polyphenolic compounds, had strong antiglycation properties. These extracts demonstrated also high activity in the FRAP (ferric-reducing antioxidant power), antiradical (DPPH) and lipid peroxidation inhibition...

  13. Inhibition of thermal induced protein denaturation of extract/fractions of Withania somnifera and isolated withanolides.

    Science.gov (United States)

    Khan, Murad Ali; Khan, Haroon; Rauf, Abdul; Ben Hadda, Taibi

    2015-01-01

    This study describes the in vitro inhibition of protein denaturation of extract/fractions of Withania somnifera and isolated withanolides including 20β hydroxy-1-oxo(22R)-witha-2,5,24 trienolide (1), (20R,22R-14α,20α)-dihydroxy-1-oxowitha-2,5,16,24 tetraenolide (2). The results showed that the extract/fractions of the plant evoked profound inhibitory effect on thermal-induced protein denaturation. The chloroform fraction caused the most dominant attenuation of 68% at 500 μg/mL. The bioactivity-guided isolation from chloroform fraction led to the isolation of compounds 1 and 2 that showed profound protein inhibition with 78.05% and 80.43% effect at 500 μg/mL and thus strongly complimented the activity of extract/fractions. In conclusion, extract/fractions of W. somnifera possessed strong inhibition of protein denaturation that can be attributed to these isolated withanolides.

  14. Significance of bacterial flora in abdominal irradiation-induced inhibition of lung metastases

    Energy Technology Data Exchange (ETDEWEB)

    Matsumoto, T.; Ando, K.; Koike, S.

    1988-06-01

    We have previously reported that abdominal irradiation prior to i.v. injection of syngeneic tumor cells reduced metastases in lung. Our report described an investigation of the significance of intestinal organisms in the radiation effect. We found that eliminating intestinal organisms with antibiotics totally abolished the radiation effect. Monoassociation of germ-free mice revealed that the radiation effect was observable only for Enterobacter cloacae, never for Streptococcus faecium, Bifidobacterium adlesentis, or Escherichia coli. After abdominal irradiation of regular mice, E. cloacae multiplied in cecal contents, adhered to mucous membranes, invaded the cecal wall, and translocated to mesenteric lymph nodes. Intravenous administration of E. cloacae in place of abdominal irradiation inhibited metastases. E. cloacae-monoassociated mice developed fewer metastases than germ-free mice, and the reduction was further enhanced by abdominal irradiation. We concluded that abdominal irradiation caused the invasion of E. cloacae from the mucous membrane of the intestine and inhibited formation of lung metastases.

  15. Grape seed and red wine polyphenol extracts inhibit cellular cholesterol uptake, cell proliferation, and 5-lipoxygenase activity.

    Science.gov (United States)

    Leifert, Wayne R; Abeywardena, Mahinda Y

    2008-12-01

    Accumulating evidence suggests that grape seed and wine polyphenol extracts possess a diverse array of actions and may be beneficial in the prevention of inflammatory-mediated disease such as cardiovascular disease and cancer. This study aimed to determine whether the reported pleiotropic effects of several polyphenolic extracts from grape seed products or red wine would also include inhibition of cholesterol uptake and cell proliferation, and inhibit a known specific target of the inflammatory process, that is, 5-lipoxygenase (5-LOX). Incubation of HT29, Caco2, HepG2, or HuTu80 cells in a medium containing [(3)H]cholesterol in the presence of a grape seed extract (GSE) or red wine polyphenolic compounds (RWPCs) inhibited [(3)H]cholesterol uptake by up to 66% (which appeared maximal). The estimated IC(50) values were 60 and 83 microg/mL for RWPC and GSE, respectively. Similar cholesterol uptake inhibitory effects were observed using the fluorescent cholesterol analogue NBD cholesterol. The inhibition of cholesterol uptake was independent of the sample's (GSE and RWPC) potent antioxidative capacity. Red wine polyphenolic compound and GSE dose dependently inhibited HT29 colon adenocarcinoma cell proliferation, which was accompanied by an increase in apoptosis. In addition, RWPC and GSE inhibited 5-LOX activity with the IC(50) values being 35 and 13 microg/mL, respectively. Two of 3 other GSEs tested also significantly inhibited 5-LOX activity. Inhibition of cholesterol uptake and proinflammatory 5-LOX activity may be beneficial in preventing the development of chronic degenerative diseases such as cardiovascular disease and cancer.

  16. Cigarette Smoke Extract Inhibits the Proliferation of Alveolar Epithelial Cells and Augments the Expression of P21WAF1

    Institute of Scientific and Technical Information of China (English)

    Zongxian JIAO; Qilin AO; Xiaona GE; Mi XIONG

    2008-01-01

    Cigarette smoking is intimately related with the development of chronic obstructive pulmonary diseases, and alveolar epithelium is a major target for the exposure of cigarette smoke ex- tract. In order to investigate the effect of cigarette smoke extract on the proliferation of alveolar epithelial cell type Ⅱand its relationship with P21WAF1, the alveolar epithelial type Ⅱ cell line (A549) cells were chosen as surrogate cells to represent alveolar epithelial type Ⅱ cells. MTT assay was used to detect cell viability after interfered with different concentrations of cigarette smoke ex-tract. It was observed cigarette smoke extract inhibited the growth of A549 cells in a dose- and time-dependent manner. The morphological changes, involving the condensation and margination of nuclear chromatin, even karyorrhexis, were observed by both Hoechst staining and electronic mi-croscopy. Flow cytometry analysis demonstrated the increased cell percentages in G1 and subG1phases after the cells were incubated with cigarette smoke extract. The expression of p21WAF1 protein and mRNA was also significantly increased as detected by the methods of Western blot or reverse transcription-polymerase chain reaction respectively. In conclusion, cigarette smoke extract inhibits the proliferation of alveolar epithelial cell type Ⅱ and blocks them in G1/S phase. The intracellular accumulation of P21WAF1 may be one of the mechanisms which contribute to cigarette smoke ex-tract-induced inhibition of cell proliferation.

  17. A Novel Role of Eruca sativa Mill. (Rocket Extract: Antiplatelet (NF-κB Inhibition and Antithrombotic Activities

    Directory of Open Access Journals (Sweden)

    Eduardo Fuentes

    2014-12-01

    Full Text Available Background: Epidemiological studies have shown the prevention of cardiovascular diseases through the regular consumption of vegetables. Eruca sativa Mill., commonly known as rocket, is a leafy vegetable that has anti-inflammatory activity. However, its antiplatelet and antithrombotic activities have not been described. Methods: Eruca sativa Mill. aqueous extract (0.1 to 1 mg/mL, was evaluated on human platelets: (i P-selectin expression by flow cytometry; (ii platelet aggregation induced by ADP, collagen and arachidonic acid; (iii IL-1β, TGF-β1, CCL5 and thromboxane B2 release; and (iv activation of NF-κB and PKA by western blot. Furthermore, (v antithrombotic activity (200 mg/kg and (vi bleeding time in murine models were evaluated. Results: Eruca sativa Mill. aqueous extract (0.1 to 1 mg/mL inhibited P-selectin expression and platelet aggregation induced by ADP. The release of platelet inflammatory mediators (IL-1β, TGF-β1, CCL5 and thromboxane B2 induced by ADP was inhibited by Eruca sativa Mill. aqueous extract. Furthermore, Eruca sativa Mill. aqueous extract inhibited NF-κB activation. Finally, in murine models, Eruca sativa Mill. aqueous extract showed significant antithrombotic activity and a slight effect on bleeding time. Conclusion: Eruca sativa Mill. presents antiplatelet and antithrombotic activity.

  18. Campomanesia adamantium Peel Extract in Antidiarrheal Activity: The Ability of Inhibition of Heat-Stable Enterotoxin by Polyphenols.

    Science.gov (United States)

    Lescano, Caroline Honaiser; de Oliveira, Ivan Pires; Zaminelli, Tiago; Baldivia, Débora da Silva; da Silva, Luan Ramos; Napolitano, Mauro; Silvério, Camila Bitencourt Mendes; Lincopan, Nilton; Sanjinez-Argandoña, Eliana Janet

    2016-01-01

    Campomanesia adamantium (Myrtaceae) is a medicinal plant distributed in Brazilian Cerrado. Different parts of this plant are used in popular medicine for treatment of several diseases like fever, diarrhea, hypercholesterolemia and rheumatism. The aim of this work was to evaluate the inhibition of heat-stable enterotoxin type A (STa) by gallic acid present in the peel of C. adamantium fruit and assays to assess the antidiarrheal activity, anti-inflammatory and cytotoxic properties of peel extract using the T84 cell line model. The possible inhibition exerted by the gallic acid of the peel extract on the STa peptide was inferred by molecular dynamics simulations. The antidiarrheal effects were investigated measuring cGMP accumulation in cells after stimulation by STa toxin and antibacterial activity was assessed. The anti-inflammatory activity was assessed by inhibition of COX-1 and COX-2. MTT and LDH assays were used to evaluate any possible cytotoxic action while the CyQUANT test was used to investigate the effect on cell proliferation. A representation showing how the possible interactions between STa and the gallic acid of the extract might reduce the action of the enterotoxin is presented. C. adamantium peel extract significantly decreased the levels of cGMP in T84 cells. However, no effect on the species of microorganisms was observed. The extract also inhibited COX-1 (IC50 255.70 ± 0.04 ng/mL) and COX-2 (IC50 569.50 ± 0.11 ng/mL) enzymes. Cytotoxicity assay have shown significant changes in cells treated with the extract, which inhibited the cell proliferation until 72 hours of treatment. Direct interactions of phenolic compounds present in the extract with the STa toxin may limit its activity. Curative effect in the diarrhea treatment and its anti-inflammatory action is based on the pharmacological properties, mechanism of action of the C. adamantium peel extract, and no toxic effects of the peel extract presented on this work.

  19. Campomanesia adamantium Peel Extract in Antidiarrheal Activity: The Ability of Inhibition of Heat-Stable Enterotoxin by Polyphenols

    Science.gov (United States)

    Lescano, Caroline Honaiser; de Oliveira, Ivan Pires; Zaminelli, Tiago; Baldivia, Débora da Silva; da Silva, Luan Ramos; Napolitano, Mauro; Silvério, Camila Bitencourt Mendes; Lincopan, Nilton; Sanjinez-Argandoña, Eliana Janet

    2016-01-01

    Campomanesia adamantium (Myrtaceae) is a medicinal plant distributed in Brazilian Cerrado. Different parts of this plant are used in popular medicine for treatment of several diseases like fever, diarrhea, hypercholesterolemia and rheumatism. The aim of this work was to evaluate the inhibition of heat-stable enterotoxin type A (STa) by gallic acid present in the peel of C. adamantium fruit and assays to assess the antidiarrheal activity, anti-inflammatory and cytotoxic properties of peel extract using the T84 cell line model. The possible inhibition exerted by the gallic acid of the peel extract on the STa peptide was inferred by molecular dynamics simulations. The antidiarrheal effects were investigated measuring cGMP accumulation in cells after stimulation by STa toxin and antibacterial activity was assessed. The anti-inflammatory activity was assessed by inhibition of COX-1 and COX-2. MTT and LDH assays were used to evaluate any possible cytotoxic action while the CyQUANT test was used to investigate the effect on cell proliferation. A representation showing how the possible interactions between STa and the gallic acid of the extract might reduce the action of the enterotoxin is presented. C. adamantium peel extract significantly decreased the levels of cGMP in T84 cells. However, no effect on the species of microorganisms was observed. The extract also inhibited COX-1 (IC50 255.70 ± 0.04 ng/mL) and COX-2 (IC50 569.50 ± 0.11 ng/mL) enzymes. Cytotoxicity assay have shown significant changes in cells treated with the extract, which inhibited the cell proliferation until 72 hours of treatment. Direct interactions of phenolic compounds present in the extract with the STa toxin may limit its activity. Curative effect in the diarrhea treatment and its anti-inflammatory action is based on the pharmacological properties, mechanism of action of the C. adamantium peel extract, and no toxic effects of the peel extract presented on this work. PMID:27764241

  20. DETECTION AND CLINICAL SIGNIFICANCE OF THROMBOMODULIN IN BOTH PLASMA AND TISSUE EXTRACTS OF CANCER PATIENTS

    Institute of Scientific and Technical Information of China (English)

    许晓华; 卢兴国; 徐根波; 朱蕾; 黄连生

    2004-01-01

    Objective: To study the changes of thrombomodulin (TM) in both plasma and tissue extracts of cancer patients for evaluating its clinical significance. Methods: Plasma TM levels were measured by enzyme-linked immunosorbent assay (ELISA) in both plasma of 188 cancer patients and 24 cancer tissue extracts including their adjacent non-cancer tissues. Results: The plasma TM levels both in cancer patients and in metastasis patients were significantly higher than that in controls [(33.47±14.25)μg/L, (41.68±16.96)μg/L, vs(20.40±7.22)μg/L,P0.05). The TM levels in cancer tissue extracts were significantly lower than that in their adjacent non-cancer tissue extracts [(647.71±317.51)μg/L vs (1455.63±772.22)μg/L, P<0.01]. On the contrary, the plasma TM levels in these cancers were significantly higher than that in controls. Conclusion: The rise of plasma TM levels in cancer patients was associated with metastasis and diffusion of cancers. The TM levels can be served as an sensitive index for judging progression and metastasis of cancers.

  1. Alpha-Glucosidase Inhibition and Hypoglycemic Activities of Sweitenia mahagoni Seed Extract

    Directory of Open Access Journals (Sweden)

    Tutik Wresdiyat

    2015-04-01

    Full Text Available Inhibition of α-glucosidase and hypoglycemic activity are two effects commonly used to identify bioactive compounds with potential to treat diabetes. The objectives of this study were to analyse and compare the bioactive compounds and α-glucosidase inhibitory effect of four different types of Swietenia mahagoni seed extract, and to analyse the hypoglycemic activity of the greatest inhibition of α-glucosidase-extract in rats. The extracts were obtained using two different solvents (aqueous and ethanol and two different methods: maceration and reflux methods. This resulted in four types of extract varying by solvent and extraction method. Testing of these extracts for α-glucosidase inhibitory effect was carried out in vitro using spectrophotometer. Testing for hypoglycemic activity was carried out in vivo using rats. A total of 40 male Sprague-Dawley rats were divided into eight groups: (1 the negative control group, received an oral dose of aquadest only, (2 the positive control group, was given 90% sucrose orally without S. mahagoni seed extract, and five treated groups (3-7, were given 90% sucrose followed by the best extract-ethanolic S. mahagoni seed extract in doses of 100, 200, 300, 400, and 500 mg/kgBW, and (8 the acarbose group, was given 90% sucrose orally followed by acarbose. Glucose levels in each animal were measured at 0, 30, 60, 90, and 120 min after treatment. The results showed the greatest inhibition of α-glucosidase in ethanolic extract, using maceration methods. This ethanolic-maceration S. mahagoni seed extract also showed hypoglycemic effects in hyperglycemic rats at dose from 100 to 500 mg/kgBW. Ethanolic extract of S. mahagoni seed, using maceration method, can be proposed as potential antidiabetic agent.

  2. Comparative studies on the effects of a yucca extract and acibenzolar-S-methyl (ASM) on inhibition of Venturia inaequalis in apple leaves

    DEFF Research Database (Denmark)

    Bengtsson, Marianne Vibeke; Wulff, Ednar Gadelha; Jørgensen, Hans Jørgen Lyngs;

    2009-01-01

    The effect of an extract of Yucca schidigera on the control and infection process of the apple scab pathogen, Venturia inaequalis, was examined and compared with the chemical resistance inducer, acibenzolar-S-methyl (ASM). In seedling assays, both materials significantly reduced apple scab symptoms...... and pathogen sporulation on leaves and both showed similar control efficacies as the reference treatment, sulphur. Whereas yucca extract and sulphur gave significant inhibition of conidial germination in vitro, ASM did not inhibit germination. Histopathological studies of the infection process of V. inaequalis...... in apple leaves showed that the yucca extract primarily acted by inhibiting pre-penetration events and penetration itself. In contrast, the ASM treatment significantly inhibited more stages of the infection process (pre-penetration, penetration and post-penetration events). These observations suggest...

  3. Aqueous Leaf Extract of Jatropha gossypiifolia L. (Euphorbiaceae) Inhibits Enzymatic and Biological Actions of Bothrops jararaca Snake Venom

    Science.gov (United States)

    Félix-Silva, Juliana; Souza, Thiago; Menezes, Yamara A. S.; Cabral, Bárbara; Câmara, Rafael B. G.; Silva-Junior, Arnóbio A.; Rocha, Hugo A. O.; Rebecchi, Ivanise M. M.; Zucolotto, Silvana M.; Fernandes-Pedrosa, Matheus F.

    2014-01-01

    Snakebites are a serious public health problem due their high morbi-mortality. The main available specific treatment is the antivenom serum therapy, which has some disadvantages, such as poor neutralization of local effects, risk of immunological reactions, high cost and difficult access in some regions. In this context, the search for alternative therapies is relevant. Therefore, the aim of this study was to evaluate the antiophidic properties of Jatropha gossypiifolia, a medicinal plant used in folk medicine to treat snakebites. The aqueous leaf extract of the plant was prepared by decoction and phytochemical analysis revealed the presence of sugars, alkaloids, flavonoids, tannins, terpenes and/or steroids and proteins. The extract was able to inhibit enzymatic and biologic activities induced by Bothrops jararaca snake venom in vitro and in vivo. The blood incoagulability was efficiently inhibited by the extract by oral route. The hemorrhagic and edematogenic local effects were also inhibited, the former by up to 56% and the latter by 100%, in animals treated with extract by oral and intraperitoneal routes, respectively. The inhibition of myotoxic action of B. jararaca reached almost 100%. According to enzymatic tests performed, it is possible to suggest that the antiophidic activity may be due an inhibitory action upon snake venom metalloproteinases (SVMPs) and/or serine proteinases (SVSPs), including fibrinogenolytic enzymes, clotting factors activators and thrombin like enzymes (SVTLEs), as well upon catalytically inactive phospholipases A2 (Lys49 PLA2). Anti-inflammatory activity, at least partially, could also be related to the inhibition of local effects. Additionally, protein precipitating and antioxidant activities may also be important features contributing to the activity presented. In conclusion, the results demonstrate the potential antiophidic activity of J. gossypiifolia extract, including its significant action upon local effects, suggesting that

  4. Aqueous leaf extract of Jatropha gossypiifolia L. (Euphorbiaceae inhibits enzymatic and biological actions of Bothrops jararaca snake venom.

    Directory of Open Access Journals (Sweden)

    Juliana Félix-Silva

    Full Text Available Snakebites are a serious public health problem due their high morbi-mortality. The main available specific treatment is the antivenom serum therapy, which has some disadvantages, such as poor neutralization of local effects, risk of immunological reactions, high cost and difficult access in some regions. In this context, the search for alternative therapies is relevant. Therefore, the aim of this study was to evaluate the antiophidic properties of Jatropha gossypiifolia, a medicinal plant used in folk medicine to treat snakebites. The aqueous leaf extract of the plant was prepared by decoction and phytochemical analysis revealed the presence of sugars, alkaloids, flavonoids, tannins, terpenes and/or steroids and proteins. The extract was able to inhibit enzymatic and biologic activities induced by Bothrops jararaca snake venom in vitro and in vivo. The blood incoagulability was efficiently inhibited by the extract by oral route. The hemorrhagic and edematogenic local effects were also inhibited, the former by up to 56% and the latter by 100%, in animals treated with extract by oral and intraperitoneal routes, respectively. The inhibition of myotoxic action of B. jararaca reached almost 100%. According to enzymatic tests performed, it is possible to suggest that the antiophidic activity may be due an inhibitory action upon snake venom metalloproteinases (SVMPs and/or serine proteinases (SVSPs, including fibrinogenolytic enzymes, clotting factors activators and thrombin like enzymes (SVTLEs, as well upon catalytically inactive phospholipases A2 (Lys49 PLA2. Anti-inflammatory activity, at least partially, could also be related to the inhibition of local effects. Additionally, protein precipitating and antioxidant activities may also be important features contributing to the activity presented. In conclusion, the results demonstrate the potential antiophidic activity of J. gossypiifolia extract, including its significant action upon local effects

  5. Ethanolic extract of propolis inhibits atherosclerosis in ApoE-knockout mice.

    Science.gov (United States)

    Fang, Yongqi; Sang, Hui; Yuan, Na; Sun, Hongli; Yao, Shutong; Wang, Jiafu; Qin, Shucun

    2013-08-13

    The present study was undertaken to investigate the effects and underlying mechanism of ethanolic extract of propolis (EEP) on the development of atherosclerotic lesions in ApoE-/- mice. Eight-week-old male ApoE-/- mice fed a high-fat diet were treated with EEP (160 mg/kg/d) or vehicle (the same dose) respectively for 14 weeks. The serum levels of total cholesterol (TC), high-density lipoprotein cholesterol (HDL-C) and triglycerides (TG) were determined by enzymatic methods. Non-HDL-C was calculated as TC minus HDL-C. Serum interleukin-6 (IL-6), interleukin-17 (IL-17), endothelin (ET), inducible nitric oxide synthase (iNOS) and vascular endothelial growth factor (VEGF) were determined with enzyme-linked immunosorbent assay methods. Nitric oxide (NO) content was measured with an enzymatic nitrate reductase assay. Analyses of atherosclerotic lesions in whole aorta and aortic root sections were performed with plaque staining using Oil Red O. Compared with the vehicle-treated group, serum contents of total cholesterol (TC), triglycerides (TG) and non-HDL-C reduced significantly by 31.88%, 21.01%, and 27.11% respectively in the EEP-treated group. Administration of EEP decreased the level of IL-6 and increased the level of IL-17 in ApoE-/- mice with a high-fat diet. Compared with the vehicle-treated group,EEP significantly reduced the levels of ET and VEGF,and showed a trend to increase NO and inhibit iNOS. In the ApoE-/- mice fed a high-fat diet, EEP significantly reduced atherosclerotic lesion development in the aortic root and whole aorta. EEP can inhibit atherosclerotic lesion formation in ApoE-/- mice fed a high-fat diet possibly through modulating cholesterol, regulating inflammatory reaction,inhibiting ET and VEGF, and protecting vascular endothelial cells.

  6. Extracts from Traditional Chinese Medicinal Plants Inhibit Acetylcholinesterase, a Known Alzheimer’s Disease Target

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    Dorothea Kaufmann

    2016-08-01

    Full Text Available Inhibition of acetylcholinesterase (AChE is a common treatment for early stages of the most general form of dementia, Alzheimer’s Disease (AD. In this study, methanol, dichloromethane and aqueous crude extracts from 80 Traditional Chinese Medical (TCM plants were tested for their in vitro anti-acetylcholinesterase activity based on Ellman’s colorimetric assay. All three extracts of Berberis bealei (formerly Mahonia bealei, Coptis chinensis and Phellodendron chinense, which contain numerous isoquinoline alkaloids, substantially inhibited AChE. The methanol and aqueous extracts of Coptis chinensis showed IC50 values of 0.031 µg/mL and 2.5 µg/mL, therefore having an up to 100-fold stronger AChE inhibitory activity than the already known AChE inhibitor galantamine (IC50 = 4.33 µg/mL. Combinations of individual alkaloids berberine, coptisine and palmatine resulted in a synergistic enhancement of ACh inhibition. Therefore, the mode of AChE inhibition of crude extracts of Coptis chinensis, Berberis bealei and Phellodendron chinense is probably due to of this synergism of isoquinoline alkaloids. All extracts were also tested for their cytotoxicity in COS7 cells and none of the most active extracts was cytotoxic at the concentrations which inhibit AChE. Based on these results it can be stated that some TCM plants inhibit AChE via synergistic interaction of their secondary metabolites. The possibility to isolate pure lead compounds from the crude extracts or to administer these as nutraceuticals or as cheap alternative to drugs in third world countries make TCM plants a versatile source of natural inhibitors of AChE.

  7. Water extract of the fungi from Fuzhuan brick tea improves the beneficial function on inhibiting fat deposition.

    Science.gov (United States)

    Peng, Yuxuan; Xiong, Zhe; Li, Juan; Huang, Jian-An; Teng, Cuiqin; Gong, Yushun; Liu, Zhonghua

    2014-08-01

    Fuzhuan brick tea (FBT) is traditionally consumed by the ethnic group in the border region of northwest China. The unique yellow fungal (Eurotium cristatum) growth phase is considered to be the key process point in the manufacture of the brick tea. The fungi from FBT are not only strongly correlated to the quality of brick tea, but also have the potential function of preventing obesity. The water extract of fungi (100 μg/mL) can significantly inhibit fat deposition in 3T3-L1 adipocyte and Caenorhabditis elegans. Furthermore, the inhibition of 3T3-L1 adipocyte formation was not due to the suppression on cell viability.

  8. Inhibition of DNA polymerase λ and associated inflammatory activities of extracts from steamed germinated soybeans.

    Science.gov (United States)

    Mizushina, Yoshiyuki; Kuriyama, Isoko; Yoshida, Hiromi

    2014-04-01

    During the screening of selective DNA polymerase (pol) inhibitors from more than 50 plant food materials, we found that the extract from steamed germinated soybeans (Glycine max L.) inhibited human pol λ activity. Among the three processed soybean samples tested (boiled soybeans, steamed soybeans, and steamed germinated soybeans), both the hot water extract and organic solvent extract from the steamed germinated soybeans had the strongest pol λ inhibition. We previously isolated two glucosyl compounds, a cerebroside (glucosyl ceramide, AS-1-4, compound ) and a steroidal glycoside (eleutheroside A, compound ), from dried soybean, and these compounds were prevalent in the extracts of the steamed germinated soybeans as pol inhibitors. The hot water and organic solvent extracts of the steamed germinated soybeans and compounds and selectively inhibited the activity of eukaryotic pol λ in vitro but did not influence the activities of other eukaryotic pols, including those from the A-family (pol γ), B-family (pols α, δ, and ε), and Y-family (pols η, ι, and κ), and also showed no effect on the activity of pol β, which is of the same family (X) as pol λ. The tendency for in vitro pol λ inhibition by these extracts and compounds showed a positive correlation with the in vivo suppression of TPA (12-O-tetradecanoylphorbol-13-acetate)-induced inflammation in mouse ear. These results suggest that steamed germinated soybeans, especially the glucosyl compound components, may be useful for their anti-inflammatory properties.

  9. Saw Palmetto Extract Inhibits Metastasis and Antiangiogenesis through STAT3 Signal Pathway in Glioma Cell

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    Hong Ding

    2015-01-01

    Full Text Available Signal transducer and activator of transcription factor 3 (STAT3 plays an important role in the proliferation and angiogenesis in human glioma. Previous research indicated that saw palmetto extract markedly inhibited the proliferation of human glioma cells through STAT3 signal pathway. But its effect on tumor metastasis and antiangiogenesis is not clear. This study is to further clear the impact of saw palmetto extract on glioma cell metastasis, antiangiogenesis, and its mechanism. TUNEL assay indicated that the apoptotic cells in the saw palmetto treated group are higher than that in the control group (p<0.05. The apoptosis related protein is detected and the results revealed that saw palmetto extract inhibits the proliferation of human glioma. Meanwhile pSTAT3 is lower in the experimental group and CD34 is also inhibited in the saw palmetto treated group. This means that saw palmetto extract could inhibit the angiogenesis in glioma. We found that saw palmetto extract was an important phytotherapeutic drug against the human glioma through STAT3 signal pathway. Saw palmetto extract may be useful as an adjunctive therapeutic agent for treatment of individuals with glioma and other types of cancer in which STAT3 signaling is activated.

  10. Dietary administration of scallion extract effectively inhibits colorectal tumor growth: cellular and molecular mechanisms in mice.

    Directory of Open Access Journals (Sweden)

    Palanisamy Arulselvan

    Full Text Available Colorectal cancer is a common malignancy and a leading cause of cancer death worldwide. Diet is known to play an important role in the etiology of colon cancer and dietary chemoprevention is receiving increasing attention for prevention and/or alternative treatment of colon cancers. Allium fistulosum L., commonly known as scallion, is popularly used as a spice or vegetable worldwide, and as a traditional medicine in Asian cultures for treating a variety of diseases. In this study we evaluated the possible beneficial effects of dietary scallion on chemoprevention of colon cancer using a mouse model of colon carcinoma (CT-26 cells subcutaneously inoculated into BALB/c mice. Tumor lysates were subjected to western blotting for analysis of key inflammatory markers, ELISA for analysis of cytokines, and immunohistochemistry for analysis of inflammatory markers. Metabolite profiles of scallion extracts were analyzed by LC-MS/MS. Scallion extracts, particularly hot-water extract, orally fed to mice at 50 mg (dry weight/kg body weight resulted in significant suppression of tumor growth and enhanced the survival rate of test mice. At the molecular level, scallion extracts inhibited the key inflammatory markers COX-2 and iNOS, and suppressed the expression of various cellular markers known to be involved in tumor apoptosis (apoptosis index, proliferation (cyclin D1 and c-Myc, angiogenesis (VEGF and HIF-1α, and tumor invasion (MMP-9 and ICAM-1 when compared with vehicle control-treated mice. Our findings may warrant further investigation of the use of common scallion as a chemopreventive dietary agent to lower the risk of colon cancer.

  11. Psoralea corylifolia L. Seed Extract Ameliorates Streptozotocin-Induced Diabetes in Mice by Inhibition of Oxidative Stress

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    Eunhui Seo

    2014-01-01

    Full Text Available Pancreatic beta-cell death is known to be the cause of deficient insulin production in diabetes mellitus. Oxidative stress is one of the major causes of beta-cell death. In this study, we investigated the effects of Psoralea corylifolia L. seed (PCS extract on beta-cell death. Oral administration of PCS extract resulted in a significant improvement of hyperglycemia in streptozotocin-induced diabetic mice. PCS extract treatment improved glucose tolerance and increased serum insulin levels. To study the mechanisms involved, we investigated the effects of PCS extract on H2O2-induced apoptosis in INS-1 cells. Treatment with PCS extract inhibited cell death. PCS extract treatment decreased reactive oxygen species level and activated antioxidative enzymes. Among the major components of PCS extract, psoralen and isopsoralen (coumarins, but not bakuchiol, showed preventive effects against H2O2-induced beta-cell death. These findings indicate that PCS extract may be a potential pharmacological agent to protect against pancreatic beta-cell damage caused by oxidative stress associated with diabetes.

  12. Nanoparticles of Selaginella doederleinii leaf extract inhibit human lung cancer cells A549

    Science.gov (United States)

    Syaefudin; Juniarti, A.; Rosiyana, L.; Setyani, A.; Khodijah, S.

    2016-01-01

    The aim of the present study is to evaluate cytotoxicity effect of nanoparticles of Selaginella doederleinii (S. doederleinii) leaves extract. S. doederleinii was extracted by maceration method using 70%(v/v) ethanol as solvent. Phytochemical content was analyzed qualitatively by using Harborne and Thin Layer Chromatography (TLC) methods. Nanoparticle extract was prepared by ionic gelation using chitosan as encapsulant agent. Anticancer activity was performed by using 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. The results showed that S. doederleinii contains of flavonoids. Nanoparticle of S. doederleinii leaves extract greatly inhibited A549 cells growth (cancer cells), with IC50 of 3% or 1020 μg/ml. These nanoparticles extract also inhibited the growth of Chang cells (normal cells), with IC50 of 4% or 1442 μg/ml. The effective concentration of nanoparticles extract which inhibits cancer cells without harming the normal cells is 0.5% or 167 μg/ml. Further studies are needed to obtain the concentration of nanoparticles extract which can selectively suppress cancer cells.

  13. Inhibition of cyclooxygenase activity by standardized hydroalcoholic extracts of four Asteraceae species from the Argentine Puna

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    M.R. Alberto

    2009-09-01

    Full Text Available We determined the anti-inflammatory activity of standardized extracts of four medicinal plant species (Baccharis incarum, B. boliviensis, Chuquiraga atacamensis, Parastrephia lucida that grow in the Argentine Puna (3800 m above sea level and that are used to reduce oxidative stress and alleviate gout and arthritic pain. The extracts of plant aerial parts were standardized in terms of total phenolic compounds and flavone/flavanone content and free radical scavenging activity. All extracts showed high phenolic compound concentration (0.5-1.6 mg/mL, mainly flavones and flavonols (0.1-0.8 mg/mL. The extracts showed hydrogen donating ability (DPPH and ABTS and reactive oxygen species scavenging activity (O2●-, OH-, H2O2. The ability of the extracts to inhibit cyclooxygenase enzymes (COX-1 and COX-2 was determined by calculating percent inhibition of PGE2 production measured by enzyme immunoassay. All extracts inhibited both enzymes with IC50 values of 2.0 to 16.7 µg/mL. The anti-inflammatory activity of B. incarum and C. atacamensis extracts was higher than that of B. boliviensis and P. lucida. The IC50 values obtained for indomethacin were 0.11 and 0.78 µM for COX-1 and COX-2, respectively. The present results are consistent with the anecdotal use of these species in phytotherapic preparations.

  14. Inhibition of cyclooxygenase activity by standardized hydroalcoholic extracts of four Asteraceae species from the Argentine Puna.

    Science.gov (United States)

    Alberto, M R; Zampini, I C; Isla, M I

    2009-09-01

    We determined the anti-inflammatory activity of standardized extracts of four medicinal plant species (Baccharis incarum, B. boliviensis, Chuquiraga atacamensis, Parastrephia lucida) that grow in the Argentine Puna (3800 m above sea level) and that are used to reduce oxidative stress and alleviate gout and arthritic pain. The extracts of plant aerial parts were standardized in terms of total phenolic compounds and flavone/flavanone content and free radical scavenging activity. All extracts showed high phenolic compound concentration (0.5-1.6 mg/mL), mainly flavones and flavonols (0.1-0.8 mg/mL). The extracts showed hydrogen donating ability (DPPH and ABTS) and reactive oxygen species scavenging activity (O2-, OH-, H2O2). The ability of the extracts to inhibit cyclooxygenase enzymes (COX-1 and COX-2) was determined by calculating percent inhibition of PGE2 production measured by enzyme immunoassay. All extracts inhibited both enzymes with IC50 values of 2.0 to 16.7 microg/mL. The anti-inflammatory activity of B. incarum and C. atacamensis extracts was higher than that of B. boliviensis and P. lucida. The IC50 values obtained for indomethacin were 0.11 and 0.78 microM for COX-1 and COX-2, respectively. The present results are consistent with the anecdotal use of these species in phytotherapic preparations.

  15. Pinelliae Rhizoma, a Toxic Chinese Herb, Can Significantly Inhibit CYP3A Activity in Rats

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    Jinjun Wu

    2015-01-01

    Full Text Available Raw Pinelliae Rhizoma (RPR is a representative toxic herb that is widely used for eliminating phlegm or treating cough and vomiting. Given its irritant toxicity, its processed products, including Pinelliae Rhizoma Praeparatum (PRP and Pinelliae Rhizoma Praeparatum cum Zingibere et Alumine (PRPZA, are more commonly applied and administered concomitantly with other chemical drugs, such as cough medications. This study aimed to investigate the effects of RPR, PRP, and PRPZA on CYP3A activity. Testosterone (Tes and buspirone (BP were used as specific probe substrates ex vivo and in vivo, respectively. CYP3A activity was determined by the metabolite formation ratios from the substrates. Ex vivo results show that the metabolite formation ratios from Tes significantly decreased, indicating that RPR, PRP, and PRPZA could inhibit CYP3A activity in rats. CYP3A protein and mRNA levels were determined to explore the underlying mechanism. These levels showed marked and consistent down-regulation with CYP3A activity. A significant decrease in metabolite formation ratios from BP was also found in PRPZA group in vivo, implying that PRPZA could inhibit CYP3A activity. Conclusively, co-administration of PR with other CYP3A-metabolizing drugs may cause drug–drug interactions. Clinical use of PR-related formulae should be monitored carefully to avoid adverse interactions.

  16. Inhibition of class IIb histone deacetylase significantly improves cloning efficiency in mice.

    Science.gov (United States)

    Ono, Tetsuo; Li, Chong; Mizutani, Eiji; Terashita, Yukari; Yamagata, Kazuo; Wakayama, Teruhiko

    2010-12-01

    Since the first mouse clone was produced by somatic cell nuclear transfer, the success rate of cloning in mice has been extremely low. Some histone deacetylase inhibitors, such as trichostatin A and scriptaid, have improved the full-term development of mouse clones significantly, but the mechanisms allowing for this are unclear. Here, we found that two other specific inhibitors, suberoylanilide hydroxamic acid and oxamflatin, could also reduce the rate of apoptosis in blastocysts, improve the full-term development of cloned mice, and increase establishment of nuclear transfer-generated embryonic stem cell lines significantly without leading to obvious abnormalities. However, another inhibitor, valproic acid, could not improve cloning efficiency. Suberoylanilide hydroxamic acid, oxamflatin, trichostatin A, and scriptaid are inhibitors for classes I and IIa/b histone deacetylase, whereas valproic acid is an inhibitor for classes I and IIa, suggesting that inhibiting class IIb histone deacetylase is an important step for reprogramming mouse cloning efficiency.

  17. Malabaricone C-containing mace extract inhibits safrole bioactivation and DNA adduct formation both in vitro and in vivo.

    Science.gov (United States)

    Martati, Erryana; Boonpawa, Rungnapa; van den Berg, Johannes H J; Paini, Alicia; Spenkelink, Albertus; Punt, Ans; Vervoort, Jacques; van Bladeren, Peter J; Rietjens, Ivonne M C M

    2014-04-01

    Safrole, present in mace and its essential oils, causes liver tumors in rodents at high dose levels due to formation of a DNA reactive 1'-sulfooxysafrole. The present study identifies malabaricone C as a mace constituent able to inhibit safrole DNA adduct formation at the level of sulfotransferase mediated bioactivation. This inhibition was incorporated into physiologically based biokinetic rat and human models. Dosing safrole at 50mg/kg body weight and malabaricone C-containing mace extract at a ratio reflecting the relative presence in mace, and assuming 100% or 1% uptake of malabaricone C-containing mace extract, the model predicted inhibition of 1'-sulfooxysafrole formation for rats and humans by 90% and 100% or 61% and 91%, respectively. To validate the model, mace extract and safrole were co-administered orally to Sprague-Dawley rats. LC-ECI-MS/MS based quantification of DNA adduct levels revealed a significant (padduct formation by malabaricone C-containing mace extract in the liver of rats exposed to safrole. The data obtained were used to perform a refined risk assessment of safrole. Overall, the results suggest a lower tumor incidence when safrole would be tested within a relevant food matrix containing sulfotransferase inhibitors compared to dosing pure safrole.

  18. Ligusticum wallichii Extract Inhibited the Expression of IL-1β after AMI in Rats

    Directory of Open Access Journals (Sweden)

    Zhuo Yuan

    2014-01-01

    Full Text Available This study investigated the effects of Ligusticum wallichii on IL-1β expression in myocardium and central nervous system after AMI. AMI rat was administrated with Ligusticum wallichii extract. A series of assays were used to detect the effects of Ligusticum wallichii extract on infarct size, left ventricular ejection fraction, expression of TLR-4, NF-κB, and IL-1β in myocardium, IL-1β expression in serum and hypothalamus, and NPY expression in hypothalamus. We observed that Ligusticum wallichii extract improved the left ventricular ejection fraction and reduced infarct area enlargement after AMI, by inhibiting the expression of IL-1β in myocardium, serum, and hypothalamus. Ligusticum wallichii extract reduced the expression of IL-1β in myocardium by regulating TLR4-NF-κB signaling pathway and inhibited IL-1β in hypothalamus by regulating NPY mRNA expression.

  19. Inhibition of the Cu65/Zn35 brass corrosion by natural extract of Camellia sinensis

    Energy Technology Data Exchange (ETDEWEB)

    Ramde, Tambi, E-mail: t_ramde@univ-ouaga.bf [Equipe Chimie Physique et Electrochimie, Laboratoire de Chimie Moléculaire et des Matériaux, Université de Ouagadougou, 03 BP 7021 Ouagadougou 03 (Burkina Faso); Department of Industrial Engineering, University of Trento, via Sommarive 9, 38123 Trento (Italy); Rossi, Stefano; Zanella, Caterina [Department of Industrial Engineering, University of Trento, via Sommarive 9, 38123 Trento (Italy)

    2014-07-01

    In this work, the corrosion inhibition of brass was studied using natural plant extract, Camellia sinensis, in 0.1 M Na2SO4 solutions with pH 7 and pH 4. Electrochemical techniques (potentiodynamic polarization, electrochemical impedance spectroscopy) and scanning electron microscopy (SEM) were applied to study the brass corrosion behavior in presence and absence of the extract. The results indicated that the extract is a very effective corrosion inhibitor for brass corrosion process in both the acidic and neutral media by virtue of adsorption. The inhibition effect increases by time as demonstrated by the EIS monitoring for 120 h. In the blank solution the corrosion process leads to the formation of a dark oxide patina at pH 7 and induces localized corrosion morphology at pH 4. The extract presence can avoid both the dark patina and the pits formation.

  20. Pharmacological kynurenine 3-monooxygenase enzyme inhibition significantly reduces neuropathic pain in a rat model.

    Science.gov (United States)

    Rojewska, Ewelina; Piotrowska, Anna; Makuch, Wioletta; Przewlocka, Barbara; Mika, Joanna

    2016-03-01

    Recent studies have highlighted the involvement of the kynurenine pathway in the pathology of neurodegenerative diseases, but the role of this system in neuropathic pain requires further extensive research. Therefore, the aim of our study was to examine the role of kynurenine 3-monooxygenase (Kmo), an enzyme that is important in this pathway, in a rat model of neuropathy after chronic constriction injury (CCI) to the sciatic nerve. For the first time, we demonstrated that the injury-induced increase in the Kmo mRNA levels in the spinal cord and the dorsal root ganglia (DRG) was reduced by chronic administration of the microglial inhibitor minocycline and that this effect paralleled a decrease in the intensity of neuropathy. Further, minocycline administration alleviated the lipopolysaccharide (LPS)-induced upregulation of Kmo mRNA expression in microglial cell cultures. Moreover, we demonstrated that not only indirect inhibition of Kmo using minocycline but also direct inhibition using Kmo inhibitors (Ro61-6048 and JM6) decreased neuropathic pain intensity on the third and the seventh days after CCI. Chronic Ro61-6048 administration diminished the protein levels of IBA-1, IL-6, IL-1beta and NOS2 in the spinal cord and/or the DRG. Both Kmo inhibitors potentiated the analgesic properties of morphine. In summary, our data suggest that in neuropathic pain model, inhibiting Kmo function significantly reduces pain symptoms and enhances the effectiveness of morphine. The results of our studies show that the kynurenine pathway is an important mediator of neuropathic pain pathology and indicate that Kmo represents a novel pharmacological target for the treatment of neuropathy.

  1. The CO2 inhibition of terrestrial isoprene emission significantly affects future ozone projections

    Directory of Open Access Journals (Sweden)

    J. A. Pyle

    2008-11-01

    Full Text Available Simulations of future tropospheric composition often include substantial increases in biogenic isoprene emissions arising from the Arrhenius-like leaf emission response and warmer surface temperatures, and from enhanced vegetation productivity in response to temperature and atmospheric CO2 concentration. However, a number of recent laboratory and field data have suggested a direct inhibition of leaf isoprene production by increasing atmospheric CO2 concentration, notwithstanding isoprene being produced from precursor molecules that include some of the primary products of carbon assimilation. The cellular mechanism that underlies the decoupling of leaf photosynthesis and isoprene production still awaits a full explanation but accounting for this observation in a dynamic vegetation model that contains a semi-mechanistic treatment of isoprene emissions has been shown to change future global isoprene emission estimates notably. Here we use these estimates in conjunction with a chemistry-climate model to compare the effects of isoprene simulations without and with a direct CO2-inhibition on late 21st century O3 and OH levels. The impact on surface O3 was significant. Including the CO2-inhibition of isoprene resulted in opposing responses in polluted (O3 decreases of up to 10 ppbv vs. less polluted (O3 increases of up to 10 ppbv source regions, due to isoprene nitrate and peroxy acetyl nitrate (PAN chemistry. OH concentration increased with relatively lower future isoprene emissions, decreasing methane lifetime by ~7 months. Our simulations underline the large uncertainties in future chemistry and climate studies due to biogenic emission patterns and emphasize the problems of using globally averaged climate metrics to quantify the atmospheric impact of reactive, heterogeneously distributed substances.

  2. The CO2 inhibition of terrestrial isoprene emission significantly affects future ozone projections

    Science.gov (United States)

    Young, P. J.; Arneth, A.; Schurgers, G.; Zeng, G.; Pyle, J. A.

    2009-04-01

    Simulations of future tropospheric composition often include substantial increases in biogenic isoprene emissions arising from the Arrhenius-like leaf emission response and warmer surface temperatures, and from enhanced vegetation productivity in response to temperature and atmospheric CO2 concentration. However, a number of recent laboratory and field data have suggested a direct inhibition of leaf isoprene production by increasing atmospheric CO2 concentration, notwithstanding isoprene being produced from precursor molecules that include some of the primary products of carbon assimilation. The cellular mechanism that underlies the decoupling of leaf photosynthesis and isoprene production still awaits a full explanation but accounting for this observation in a dynamic vegetation model that contains a semi-mechanistic treatment of isoprene emissions has been shown to change future global isoprene emission estimates notably. Here we use these estimates in conjunction with a chemistry-climate model to compare the effects of isoprene simulations without and with a direct CO2-inhibition on late 21st century O3 and OH levels. The impact on surface O3 was significant. Including the CO2-inhibition of isoprene resulted in opposing responses in polluted (O3 decreases of up to 10 ppbv) vs. less polluted (O3 increases of up to 10 ppbv) source regions, due to isoprene nitrate and peroxy acetyl nitrate (PAN) chemistry. OH concentration increased with relatively lower future isoprene emissions, decreasing methane lifetime by ~7 months (6.6%). Our simulations underline the large uncertainties in future chemistry and climate studies due to biogenic emission patterns and emphasize the problems of using globally averaged climate metrics (such as global radiative forcing) to quantify the atmospheric impact of reactive, heterogeneously distributed substances.

  3. Ethanolic leaf extract of Langenaria breviflora (bitter gourd) inhibits ...

    African Journals Online (AJOL)

    SARAH

    2015-01-30

    Jan 30, 2015 ... stomach was thereafter opened along greater curvature and gastric content was drained into a centrifuge tube. ... Values with different superscripts along the same column for the parameters are significantly different (p<0.05).

  4. Mentha pulegium extract as a natural product for the inhibition of corrosion. Part I: electrochemical studies.

    Science.gov (United States)

    Khadraoui, Abdelkader; Khelifa, Abdellah; Boutoumi, Hocine; Hammouti, Belkheir

    2014-01-01

    The inhibitory effect of Mentha pulegium extract (MPE) on steel corrosion in 1 M HCl solution was investigated using potentiodynamic polarisation and electrochemical impedance spectroscopy. The inhibition efficiency of MPE was found to increase with the concentration and reached 88% at 33% (v/v). Polarisation measurements show that the natural extract acted as a mixed inhibitor. The remarkable inhibition efficiency of MPE was discussed in terms of blocking of electrode surface by adsorption of inhibitor molecules through active centres. The adsorption of MPE was found to accord with the Temkin isotherm.

  5. Inhibition of Penicillium digitatum by a crude extract from Solanum nigrum leaves

    Directory of Open Access Journals (Sweden)

    Musto, M.

    2014-01-01

    Full Text Available An aqueous crude extract from Solanum nigrum lyophilized leaves was evaluated for its phytochemical composition and antifungal activity against Penicillium digitatum, the causative agent of green mold of citrus fruit. Phytochemical analysis of the extract revealed the presence of some bioactive substances such as alkaloids, tannins, flavonoids, saponins, etc. The extract showed a remarkable inhibition zone against the pathogen in agar well diffusion assays carried out in Petri plates. Storage of the extract at 4 °C for 60 days had no effect on its in vitro antifungal activity. Further, the extract was tested for its in vivo (preventive- and curative treatments antifungal activity on lemons wound-inoculated with P. digitatum. An important preventive antifungal effect was observed after 7 days of storage (100% of inhibition, although this activity decreased after 14 and 21 days (85.71 and 57.14% of inhibition, respectively. A slight curative antifungal activity was observed only after 7 days of storage (14.29% of inhibition. Preliminary findings from this study may contribute to the development of new antifungal agents to protect the lemon fruits from postharvest fungal diseases.

  6. Cytotoxic and Nitric Oxide Inhibition Activities of Propolis Extract along with Microencapsulation by Complex Coacervation.

    Science.gov (United States)

    Onbas, Rabia; Kazan, Aslihan; Nalbantsoy, Ayse; Yesil-Celiktas, Ozlem

    2016-09-01

    In this study, cytotoxicity of ethanol extract of propolis (EEP) originating from Sivas, Turkey was screened against several cancer cell lines, namely PC-3, U87MG, A-549, mPANC96, CaCo-2, MCF-7, HeLa, MDA-MB-231 and a non-tumor cell line HEK293 by MTT assay. The inhibition levels of inducible nitric oxide synthase (iNOS) were also determined by using RAW 264.7 macrophage cells following lipopolysaccharide (LPS) treatment. EEP exhibited significant cytotoxic nitric oxide inhibition activities with an IC50 value of 0.1 ± 0.1 μg/ml indicating a high potential as an anti-inflammatory agent. In spite of these promising results and the fact that propolis is a highly nutritive substance, its low solubility and bitter taste limit the applications as a natural supplement. Encapsulation might serve as a good strategy in order to overcome these problems. Complex coacervation was applied where the main focus was on surfactant type, polymer ratio (alginate:gelatin), stirring rate and concentration of core material. The mean particle size of unloaded microparticles were 22.62 μm obtained with gelatin:alginate ratio of 1:1 at a stirring rate of 1400 rpm with 2 ml of 1 % (w/v) sodium carboxymethyl cellulose (Na-CMC), whereas addition of EEP at a concentration of 100 mg/ml increased the mean particle size to 36.44 μm and yielded an encapsulation efficiency of 98.77 %. The cytotoxicities of EEP loaded microparticles were also assessed both on MCF-7 and MDA-MB-231 where similar results were achieved as free EEP which can enhance the possible use of propolis extract in the industry as a natural supplement.

  7. The α-glucosidase inhibiting isoflavones isolated from Belamcanda chinensis leaf extract

    Directory of Open Access Journals (Sweden)

    Chongming Wu

    2012-01-01

    Full Text Available The dried rhizome of Belamcanda chinensis is an important Chinese traditional medicine used for the treatment of inflammation and many other disorders. Previously, we reported the hypo- and antihyper-glycemic effects of the aqueous leaf extract of B. chinensis (BCL and identified the isoflavones as its principal active fraction. In the present study, the α-glucosidase inhibitory effect of BCL and its rough isoflavone preparation (BIF was tested in vitro and in vivo. Thirteen isoflavones were isolated from BCL and their α-glucosidase inhibitory activity was screened in vitro. The results showed that BCL (500 and 1000 mg/kg and BIF (250 and 500 mg/kg greatly inhibited the increase in blood glucose level after 5 g/kg starch loading in normal mice. Six out of the thirteen isoflavones (swertisin, 2 ” -O-rhamnosylswertisin, genistein, genistin, mangiferin and daidzin exhibited strong α-glucosidase inhibitory activity in vitro. HPLC analysis showed that swertisin was the most abundant isoflavone in BCL accounting for 1.24% of BCL, 7.44% of BIF, and 11.24% of the total isoflavone fraction of BCL, respectively. These results demonstrate that BCL possesses significant α-glucosidase inhibitory activity and swertisin may be the principal active component of BCL in α-glucosidase inhibition.

  8. Ethanol Extract of Capsella bursa-pastoris Improves Hepatic Steatosis Through Inhibition of Histone Acetyltransferase Activity.

    Science.gov (United States)

    Choi, Hyo-Kyoung; Shin, Eun Ju; Park, Su Jin; Hur, Haeng Jeon; Park, Jae Ho; Chung, Min-Yu; Kim, Myung Sunny; Hwang, Jin-Taek

    2017-03-01

    Histone lysine acetylation is thought to play a role in regulating the balance between energy storage and energy expenditure. However, the epigenetic mechanisms by which food phytochemicals influence metabolic processes in the liver have not been thoroughly investigated. In this study, we investigated the effect of an ethanol extract of Capsella bursa-pastoris (ECB) on histone acetyltransferase (HAT) inhibition, and whether it could thereby attenuate lipid accumulation in vitro and in vivo. We observed that ECB inhibits HAT activity as assessed by colorimetric and autoradiography assay systems. ECB also reduced oleic acid (OA)-stimulated histone acetylation at H4K5 and H4K12 and attenuated OA-mediated lipid accumulation in HepG2 cells, in the absence of observable cytotoxicity. We then investigated these effects in vivo. Mice were fed on either a normal diet (ND) or high-fat diet (HFD) in the presence or absence of ECB supplementation. In comparison with the ND controls, the HFD mice exhibited higher body weight, liver fat, adipose tissue size, and total serum cholesterol concentrations, and these effects were significantly attenuated by ECB supplementation. Taken together, these results suggest that ECB protects against the mechanisms responsible for HFD-induced hepatic steatosis, and may involve the targeting of histone H4K acetylation.

  9. Humic-Like Substances from Different Compost Extracts Could Significantly Promote Cucumber Growth

    Institute of Scientific and Technical Information of China (English)

    XU Da-Bing; WANG Qiu-Jun; WU Yun-Cheng; YU Guang-Hui; SHEN Qi-Rong; HUANG Qi-Wei

    2012-01-01

    The effects of direct extracts of compost (DEC),aerated fermentation extracts of compost (AFEC) and non-aerated fermentation extracts of compost (NAFEC) on cucumber growth and the action mechanisms were evaluated based on the structure and activity analysis of humic-like substances.AFEC increased cucumber growth most significantly,followed by DEC and NAFEC,which was insignificant compared to the control treatment.Humic-like substances from compost extracts played an important role in promoting cucumber growth.Application of humic-like substances stimulated auxin-like activity and increased chlorophyll content and nitrogen accumulation in plants.The positive auxin-like activity of humic-like substances could be attributed to the relative distribution of special carbon groups,such as those with a large amount of peptidic and carbohydratic groups or with a low content of phenolic groups.In conclusion,the best growth promotion by application of AFEC was mainly attributed to the humic-like substances in the AFEC.

  10. Repellency, toxicity, and oviposition inhibition of vegetable extracts against greenhouse whitefly Trialeurodes vaporariorum (Westwood (Hemiptera: Aleyrodidae

    Directory of Open Access Journals (Sweden)

    Edgar Eduardo Mendoza-Garcia

    2014-03-01

    Full Text Available In a search for sustainable options of greenhouse whitefly Trialeurodes vaporariorum (Westwood management, the toxic and/or repellent potential of water, ethanolic, and acetonic extracts of Ambrosia artemisiifolia L. (Asteraceae, Comocladia engleriana Loes (Anacardiaceae, Piper auritum Kunth (Piperaceae, Raphanus raphanistrum L. (Brassicaceae, and Taraxacum officinale F.H. Wigg. aggr.* (Asteraceae were evaluated. Repellency was assessed by the cylinder method (olfactometer, while toxicity and oviposition inhibition were assessed by the leaf immersion method. Acetonic extracts did not cause any repellent or insecticidal effect. In contrast, 200 mg mL-1 water and ethanolic extracts of R. raphanistrum and ethanolic extract of A. artemisiifolia had the highest repellent activity (76%, 72%, and 69%, respectively although their activity decreased gradually over time. Ethanolic extracts of P. auritum (66% and R. raphanistrum (56% at 200 mg mL¹ were highlighted as being toxic, while the most effective in inhibiting oviposition were water extracts of R. raphanistrum (76.1% and P. auritum (72.0% and ethanolic extract of P. auritum (69.5%; however, concentrations lower than 60 mg mL-1 caused oviposition stimulation. Our results suggest that water and ethanolic extracts of R. raphanistrum and P. auritum represent a useful tool in integrated whitefly management.

  11. Growth inhibition of fouling bacteria and diatoms by extract of terrestrial plant, Derris scandens (Dicotyledonae:Leguminocae)

    Digital Repository Service at National Institute of Oceanography (India)

    Sawant, S.S.; Sonak, S.; Garg, A.

    Methanol extract of terrestrial plant, Derris scandens Benth, was found to inhibit growth of four diatoms and 7 bacterial species of fouling community. The concentrations required to bring about 100% inhibition of growth of the diatoms ranged...

  12. Growth inhibition of fouling bacteria and diatoms by extract of terrestrial plant, @iDerris scandens@@ (Dicotyledonae:Leguminocae)

    Digital Repository Service at National Institute of Oceanography (India)

    Sawant, S.S.; Sonak, S.; Garg, A.

    Methanol extract of terrestrial plant, @iDerris scandens@@ Benth, was found to inhibit growth of four diatoms and 7 bacterial species of fouling community. The concentrations required to bring about 100% inhibition of growth of the diatoms ranged...

  13. Growth inhibition of fouling bacteria and diatoms by extract of terrestrial plant, Derris scandens (Dicotyledonae:Leguminocae)

    Digital Repository Service at National Institute of Oceanography (India)

    Sawant, S.S.; Sonak, S.; Garg, A.

    Methanol extract of terrestrial plant, Derris scandens Benth, was found to inhibit growth of four diatoms and 7 bacterial species of fouling community. The concentrations required to bring about 100% inhibition of growth of the diatoms ranged...

  14. Extracts of Morus nigra L. Leaves Standardized in Chlorogenic Acid, Rutin and Isoquercitrin: Tyrosinase Inhibition and Cytotoxicity.

    Science.gov (United States)

    de Freitas, Marcela Medeiros; Fontes, Pedro Ribeiro; Souza, Paula Monteiro; William Fagg, Christopher; Neves Silva Guerra, Eliete; de Medeiros Nóbrega, Yanna Karla; Silveira, Damaris; Fonseca-Bazzo, Yris; Simeoni, Luiz Alberto; Homem-de-Mello, Maurício; Oliveira Magalhães, Pérola

    Melanogenesis is a process responsible for melanin production, which is stored in melanocytes containing tyrosinase. Inhibition of this enzyme is a target in the cosmetics industry, since it controls undesirable skin conditions such as hyperpigmentation due to the overproduction of melanin. Species of the Morus genus are known for the beneficial uses offered in different parts of its plants, including tyrosinase inhibition. Thus, this project aimed to study the inhibitory activity of tyrosinase by extracts from Morus nigra leaves as well as the characterization of its chromatographic profile and cytotoxicity in order to become a new therapeutic option from a natural source. M. nigra leaves were collected, pulverized, equally divided into five batches and the standardized extract was obtained by passive maceration. There was no significant difference between batches for total solids content, yield and moisture content, which shows good reproducibility of the extraction process. Tyrosinase enzymatic activity was determined for each batch, providing the percentage of enzyme inhibition and IC50 values obtained by constructing dose-response curves and compared to kojic acid, a well-known tyrosinase inhibitor. High inhibition of tyrosinase activity was observed (above 90% at 15.625 μg/mL). The obtained IC50 values ranged from 5.00 μg/mL ± 0.23 to 8.49 μg/mL ± 0.59 and were compared to kojic acid (3.37 μg/mL ± 0.65). High Performance Liquid Chromatography analysis revealed the presence of chlorogenic acid, rutin and, its major compound, isoquercitrin. The chromatographic method employed was validated according to ICH guidelines and the extract was standardized using these polyphenols as markers. Cytotoxicity, assessed by MTT assay, was not observed on murine melanomas, human keratinocytes and mouse fibroblasts in tyrosinase IC50 values. This study demonstrated the potential of M. nigra leaf extract as a promising whitening agent of natural source against skin

  15. Extracts of Morus nigra L. Leaves Standardized in Chlorogenic Acid, Rutin and Isoquercitrin: Tyrosinase Inhibition and Cytotoxicity

    Science.gov (United States)

    Fontes, Pedro Ribeiro; Souza, Paula Monteiro; William Fagg, Christopher; Neves Silva Guerra, Eliete; de Medeiros Nóbrega, Yanna Karla; Silveira, Damaris; Fonseca-Bazzo, Yris; Simeoni, Luiz Alberto; Homem-de-Mello, Maurício; Oliveira Magalhães, Pérola

    2016-01-01

    Melanogenesis is a process responsible for melanin production, which is stored in melanocytes containing tyrosinase. Inhibition of this enzyme is a target in the cosmetics industry, since it controls undesirable skin conditions such as hyperpigmentation due to the overproduction of melanin. Species of the Morus genus are known for the beneficial uses offered in different parts of its plants, including tyrosinase inhibition. Thus, this project aimed to study the inhibitory activity of tyrosinase by extracts from Morus nigra leaves as well as the characterization of its chromatographic profile and cytotoxicity in order to become a new therapeutic option from a natural source. M. nigra leaves were collected, pulverized, equally divided into five batches and the standardized extract was obtained by passive maceration. There was no significant difference between batches for total solids content, yield and moisture content, which shows good reproducibility of the extraction process. Tyrosinase enzymatic activity was determined for each batch, providing the percentage of enzyme inhibition and IC50 values obtained by constructing dose-response curves and compared to kojic acid, a well-known tyrosinase inhibitor. High inhibition of tyrosinase activity was observed (above 90% at 15.625 μg/mL). The obtained IC50 values ranged from 5.00 μg/mL ± 0.23 to 8.49 μg/mL ± 0.59 and were compared to kojic acid (3.37 μg/mL ± 0.65). High Performance Liquid Chromatography analysis revealed the presence of chlorogenic acid, rutin and, its major compound, isoquercitrin. The chromatographic method employed was validated according to ICH guidelines and the extract was standardized using these polyphenols as markers. Cytotoxicity, assessed by MTT assay, was not observed on murine melanomas, human keratinocytes and mouse fibroblasts in tyrosinase IC50 values. This study demonstrated the potential of M. nigra leaf extract as a promising whitening agent of natural source against skin

  16. Inhibitive action of some plant extracts on the corrosion of steel in acidic media

    Energy Technology Data Exchange (ETDEWEB)

    Abdel-Gaber, A.M. [Department of Chemistry, Faculty of Science, Alexandria University, Ibrahimia, P.O. Box 426, Alexandria 21321 (Egypt)]. E-mail: ashrafmoustafa@yahoo.com; Abd-El-Nabey, B.A. [Department of Chemistry, Faculty of Science, Alexandria University, Ibrahimia, P.O. Box 426, Alexandria 21321 (Egypt); Sidahmed, I.M. [Department of Chemistry, Faculty of Science, Alexandria University, Ibrahimia, P.O. Box 426, Alexandria 21321 (Egypt); El-Zayady, A.M. [Department of Chemistry, Faculty of Science, Alexandria University, Ibrahimia, P.O. Box 426, Alexandria 21321 (Egypt); Saadawy, M. [Department of Chemistry, Faculty of Science, Alexandria University, Ibrahimia, P.O. Box 426, Alexandria 21321 (Egypt)

    2006-09-15

    The effect of extracts of Chamomile (Chamaemelum mixtum L.), Halfabar (Cymbopogon proximus), Black cumin (Nigella sativa L.), and Kidney bean (Phaseolus vulgaris L.) plants on the corrosion of steel in aqueous 1 M sulphuric acid were investigated by electrochemical impedance spectroscopy (EIS) and potentiodynamic polarization techniques. EIS measurements showed that the dissolution process of steel occurs under activation control. Potentiodynamic polarization curves indicated that the plant extracts behave as mixed-type inhibitors. The corrosion rates of steel and the inhibition efficiencies of the extracts were calculated. The results obtained show that the extract solution of the plant could serve as an effective inhibitor for the corrosion of steel in sulphuric acid media. Inhibition was found to increase with increasing concentration of the plant extract up to a critical concentration. The inhibitive actions of plant extracts are discussed on the basis of adsorption of stable complex at the steel surface. Theoretical fitting of different isotherms, Langmuir, Flory-Huggins, and the kinetic-thermodynamic model, were tested to clarify the nature of adsorption.

  17. Effect of Ganoderma applanatum mycelium extract on the inhibition of adipogenesis in 3T3-L1 adipocytes.

    Science.gov (United States)

    Kim, Ji-Eun; Park, Sung-Jin; Yu, Mi-Hee; Lee, Sam-Pin

    2014-10-01

    Ganoderma applanatum (GA) and related fungal species have been used for over 2000 years in China to prevent and treat various human diseases. However, there is no critical research evaluating the functionality of GA grown using submerged culture technology. This study aimed to evaluate the effects of submerged culture GA mycelium (GAM) and its active components (protocatechualdehyde [PCA]) on preadipocyte differentiation of 3T3-L1 cells. Mouse-derived preadipocyte 3T3-L1 cells were treated with differentiation inducers in the presence or absence of GAM extracts. We determined triglyceride accumulations, glycerol-3-phosphate dehydrogenase (GPDH) activities, and differentiation makers. PCA, the active component of GAM extract, was also used to treat 3T3-L1 cells. The MTT assay showed that the GAM extract (0.01-1 mg/mL) was not toxic to 3T3-L1 preadipocyte. Treatment of cells with GAM extracts and its active components significantly decreased the GPDH activity and lipid accumulation, a marker of adipogenesis, in a dose-dependent manner. Western blot analysis results showed that the protein expression levels of peroxisome proliferator-activated receptor γ (PPARγ), CCAAT/enhancer-binding protein α (C/EBPα), and sterol regulatory element-binding protein 1 (SREBP1) were inhibited by the GAM extract. In addition, adipogenic-specific genes such as perilipin, fatty acid synthase (FAS), fatty acid transport protein 1 (FATP1), and fatty acid-binding protein 4 (FABP4) decreased in a dose-dependent manner. Quantitative high-performance liquid chromatography analysis showed that the GAM extract contained 1.14 mg/g PCA. GAM extracts suppressed differentiation of 3T3-L1 preadipocytes, in part, through altered regulation of PPARγ, C/EBPα, and SREBP1. These results suggest that GAM extracts and PCA may suppress adipogenesis by inhibiting differentiation of preadipocytes.

  18. Extract from Aronia melanocarpa fruits potentiates the inhibition of platelet aggregation in the presence of endothelial cells

    Science.gov (United States)

    Luzak, Boguslawa; Golanski, Jacek; Rozalski, Marek; Krajewska, Urszula; Olas, Beata

    2010-01-01

    Introduction Some polyphenolic compounds extracted from Aronia melanocarpa fruits (AM) have been reported to be cardioprotective agents. In this study we evaluated the ability of AM extract to increase the efficacy of human umbilical vein endothelial cells (HUVECs) to inhibit platelet functions in vitro. Material and methods This study encompasses two models of monitoring platelet reactivity: optical aggregation and platelet degranulation (monitored as the surface CD62P expression) in PRP upon the stimulation with ADP. Results We observed that only at low concentrations (5 µg/ml) did AM extract significantly improve antiplatelet action of HUVECs towards ADP-activated platelets in the aggregation test. Conclusions It is concluded that the potentiating effect of AM extract on the endothelial cell-mediated inhibition of platelet aggregation clearly depends on the used concentrations of Aronia-derived active compounds. Therefore, despite these encouraging preliminary outcomes on the beneficial effects of AM extract polyphenols, more profound dose-effect studies should certainly be considered before the implementation of Aronia-originating compounds in antiplatelet therapy and the prevention of cardiovascular diseases. PMID:22371737

  19. Inhibition of Mild Steel Corrosion in Acidic Medium by Aqueous Extract of Tridax procumbens L.

    Directory of Open Access Journals (Sweden)

    G. Ilayaraja

    2011-01-01

    Full Text Available The inhibition efficiency (IE of an aqueous extract of Tridax procumbens L. in controlling corrosion of mild steel has been investigated by weight loss method in the absence and presence of corrosion inhibitor at different time interval at room temperature. The result showed that the corrosion inhibition efficiency of these compounds was found to vary with different time interval and different acid concentration. Also, it was found that the corrosion inhibition behavior of Tridax procumbens L. is greater in sulphuric acid than hydrochloric acid medium. So Tridax procumbens L. can be used as a good inhibitor for preventing mild steel material.

  20. In vitro Inhibition of Acetyl Cholinesterase, Lipoxygenase, Xanthine Oxidase and Antibacterial Activities of Five Indigofera (Fabaceae Aqueous Acetone Extracts from Burkina Faso

    Directory of Open Access Journals (Sweden)

    C.E. Lamien

    2013-05-01

    Full Text Available The aim of this study is to evaluate the inhibition of oxidative stress related enzymes of aqueous acetone extracts, as well as antibacterial activity from five Indigofera species well-known medicinal plant from Burkina. Also are investigated in this study the potential contribution of tannins and of flavonol in these activities Particularly, aqueous acetone extracts were investigated for their Lipoxygenase (LOX, Xanthine Oxidase (XO and Acetylcholinesterase (AChE inhibitions that are implied in inflammation, gout and Alzheimer’s etiology diseases. Interestingly, I. macrocalyx which had the highest flavonol content (of all showed more inhibition against LOX and XO (51.16 and 77.33% respectively. Our study showed a significant correlation between XO inhibition and total flavonol content (R2 = 0.9052. AChE was low sensible to all extracts. In contrast, the extracts were rich in tannin compounds especially in I. tinctoria extract. And results of the in vitro antibacterial activities of these extracts against five bacteria showed that all bacteria were sensible to all extracts particularly S. typhimurium and B. cereus. Our results suggest that the five studied species prove to be good sources of inhibition of the three enzymes involved in oxidative stress and also to have some antibacterial properties. That is what probably explains their uses in folk medicine, singularly, in the treatment of gout, dysentery and anti-inflammatory diseases.

  1. Inhibition of prostate cancer growth by muscadine grape skin extract and resveratrol through distinct mechanisms.

    Science.gov (United States)

    Hudson, Tamaro S; Hartle, Diane K; Hursting, Stephen D; Nunez, Nomeli P; Wang, Thomas T Y; Young, Heather A; Arany, Praveen; Green, Jeffrey E

    2007-09-01

    The phytochemical resveratrol contained in red grapes has been shown to inhibit prostate cancer cell growth, in part, through its antioxidant activity. Muscadine grapes contain unique phytochemical constituents compared with other grapes and are potentially a source for novel compounds with antitumor activities. We compared the antitumor activities of muscadine grape skin extract (MSKE), which we show contains no resveratrol, with that of resveratrol using primary cultures of normal prostate epithelial cells (PrEC) and the prostate cancer cell lines RWPE-1, WPE1-NA22, WPE1-NB14, and WPE1-NB26, representing different stages of prostate cancer progression. MSKE significantly inhibited tumor cell growth in all transformed prostate cancer cell lines but not PrEC cells. Prostate tumor cell lines, but not PrEC cells, exhibited high rates of apoptosis in response to MSKE through targeting of the phosphatidylinositol 3-kinase-Akt and mitogen-activated protein kinase survival pathways. The reduction in Akt activity by MSKE is mediated through a reduction in Akt transcription, enhanced proteosome degradation of Akt, and altered levels of DJ-1, a known regulator of PTEN. In contrast to MSKE, resveratrol did not induce apoptosis in this model but arrested cells at the G(1)-S phase transition of the cell cycle associated with increased expression of p21 and decreased expression of cyclin D1 and cyclin-dependent kinase 4 proteins. These results show that MSKE and resveratrol target distinct pathways to inhibit prostate cancer cell growth in this system and that the unique properties of MSKE suggest that it may be an important source for further development of chemopreventive or therapeutic agents against prostate cancer.

  2. Grape seed extract inhibits in vitro and in vivo growth of human colorectal carcinoma cells.

    Science.gov (United States)

    Kaur, Manjinder; Singh, Rana P; Gu, Mallikarjuna; Agarwal, Rajesh; Agarwal, Chapla

    2006-10-15

    Accumulating evidences suggest the beneficial effects of fruit-and-vegetable consumption in lowering the risk of various cancers, including colorectal cancer. Herein, we investigated the in vitro and in vivo anticancer effects and associated mechanisms of grape seed extract (GSE), a rich source of proanthocyanidins, against colorectal cancer. Effects of GSE were examined on human colorectal cancer HT29 and LoVo cells in culture for proliferation, cell cycle progression, and apoptosis. The in vivo effect of oral GSE was examined on HT29 tumor xenograft growth in athymic nude mice. Xenografts were analyzed by immunohistochemistry for proliferation and apoptosis. The molecular changes associated with the biological effects of GSE were analyzed by Western blot analysis. GSE (25-100 microg/mL) causes a significant dose- and time-dependent inhibition of cell growth with concomitant increase in cell death. GSE induced G1 phase cell cycle arrest along with a marked increase in Cip1/p21 protein level and a decrease in G1 phase-associated cyclins and cyclin-dependent kinases. GSE-induced cell death was apoptotic and accompanied by caspase-3 activation. GSE feeding to mice at 200 mg/kg dose showed time-dependent inhibition of tumor growth without any toxicity and accounted for 44% decrease in tumor volume per mouse after 8 weeks of treatment. GSE inhibited cell proliferation but increased apoptotic cell death in tumors. GSE-treated tumors also showed enhanced Cip1/p21 protein levels and poly(ADP-ribose) polymerase cleavage. GSE may be an effective chemopreventive agent against colorectal cancer, and that growth inhibitory and apoptotic effects of GSE against colorectal cancer could be mediated via an up-regulation of Cip1/p21.

  3. Inhibition Kinetics of Sida rhombifolia L. Extract Toward Xanthine Oxidase by Electrochemical Method

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    Dyah Iswantini

    2014-03-01

    Full Text Available Sida rhombifolia L. is a traditional medicinal plant that has been known with potential as antigout. The previous research suggested that flavonoids crude extract of S. rhombifolia had an inhibitory activity toward xanthine oxidase by 71% and a spectrophotometric measurement showed that the type of flavonoids crude extract inhibition was a competitive inhibition. The purpose of the research was to investigate the type of inhibition kinetic of S. Rhombifolia’s ethanol extract by electrochemical method and to compare the measurements of linearity and sensitivity between spectrophotometric and electrochemical methods. The results showed that the yield of S. Rhombifolia’s ethanol extract was 9.82% with the inhibitory activity ranging from 13.64% to 82.69% (5.00-200 mg L-1 and IC50 value was 91.15±5.74 mg L-1. Allopurinol as a control showed the inhibitory activity of 15.26-70.95% (0.10-4.00 mg L-1 and IC50 value was 2.45±2.21 mg L-1. Inhibition kinetics of the ethanol extract caused a KM increase and unchange of VMAX. Based on the data, the type of inhibition kinetics was a competitive inhibition, with an inhibitor affinity (α value of 3.18. Linearity of xanthine oxidase activity assay by electrochemical and spectrophotometric methods showed the range of 0.01-1.00 mM (R2 = 0.978 and 0.05-0.70 mM (R2 = 0.977 respectively. The sensitivity of electrochemical method was reported higher (0.95 μA mM-1 than the spectrophotometric method (0.007 min-1.

  4. Inhibition of human cytochrome P450 enzymes by Bacopa monnieri standardized extract and constituents.

    Science.gov (United States)

    Ramasamy, Seetha; Kiew, Lik Voon; Chung, Lip Yong

    2014-02-24

    Bacopa monnieri and the constituents of this plant, especially bacosides, possess various neuropharmacological properties. Like drugs, some herbal extracts and the constituents of their extracts alter cytochrome P450 (CYP) enzymes, causing potential herb-drug interactions. The effects of Bacopa monnieri standardized extract and the bacosides from the extract on five major CYP isoforms in vitro were analyzed using a luminescent CYP recombinant human enzyme assay. B. monnieri extract exhibited non-competitive inhibition of CYP2C19 (IC50/Ki = 23.67/9.5 µg/mL), CYP2C9 (36.49/12.5 µg/mL), CYP1A2 (52.20/25.1 µg/mL); competitive inhibition of CYP3A4 (83.95/14.5 µg/mL) and weak inhibition of CYP2D6 (IC50 = 2061.50 µg/mL). However, the bacosides showed negligible inhibition of the same isoforms. B. monnieri, which is orally administered, has a higher concentration in the gut than the liver; therefore, this herb could exhibit stronger inhibition of intestinal CYPs than hepatic CYPs. At an estimated gut concentration of 600 µg/mL (based on a daily dosage of 300 mg/day), B. monnieri reduced the catalytic activities of CYP3A4, CYP2C9 and CYP2C19 to less than 10% compared to the total activity (without inhibitor = 100%). These findings suggest that B. monnieri extract could contribute to herb-drug interactions when orally co-administered with drugs metabolized by CYP1A2, CYP3A4, CYP2C9 and CYP2C19.

  5. Inhibition of Human Cytochrome P450 Enzymes by Bacopa monnieri Standardized Extract and Constituents

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    Seetha Ramasamy

    2014-02-01

    Full Text Available Bacopa monnieri and the constituents of this plant, especially bacosides, possess various neuropharmacological properties. Like drugs, some herbal extracts and the constituents of their extracts alter cytochrome P450 (CYP enzymes, causing potential herb-drug interactions. The effects of Bacopa monnieri standardized extract and the bacosides from the extract on five major CYP isoforms in vitro were analyzed using a luminescent CYP recombinant human enzyme assay. B. monnieri extract exhibited non-competitive inhibition of CYP2C19 (IC50/Ki = 23.67/9.5 µg/mL, CYP2C9 (36.49/12.5 µg/mL, CYP1A2 (52.20/25.1 µg/mL; competitive inhibition of CYP3A4 (83.95/14.5 µg/mL and weak inhibition of CYP2D6 (IC50 = 2061.50 µg/mL. However, the bacosides showed negligible inhibition of the same isoforms. B. monnieri, which is orally administered, has a higher concentration in the gut than the liver; therefore, this herb could exhibit stronger inhibition of intestinal CYPs than hepatic CYPs. At an estimated gut concentration of 600 µg/mL (based on a daily dosage of 300 mg/day, B. monnieri reduced the catalytic activities of CYP3A4, CYP2C9 and CYP2C19 to less than 10% compared to the total activity (without inhibitor = 100%. These findings suggest that B. monnieri extract could contribute to herb-drug interactions when orally co-administered with drugs metabolized by CYP1A2, CYP3A4, CYP2C9 and CYP2C19.

  6. INHIBITION OF CALCIUM OXALATE CRYSTALLIZATION IN-VITRO BY VARIOUS EXTRACTS OF HYPTIS SUAVEOLENS (L. POIT.

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    Agarwal Kumkum

    2012-03-01

    Full Text Available Hyptis suaveolens (L Poit. commonly known as Vilayati tulsi, belongs to the Mint family Lamiaceae. The inhibition of in-vitro calcium-oxalate crystal (a major component of most urinary stones formation by various extracts of Hyptis was investigated by titrimetric method. The inhibitor potency of alcohol extracts of Hyptis suaveolens (L. Poit was found to be comparable to that of cystone (a proprietary drug for dissolving kidney stones. Thus alcohol extract could be further analyzed in vivo and further characterization of its active compound could lead to the discovery of a new candidate drug for the patients with urolithiasis.

  7. Hawberry (Crataegus monogyna Jaqc.) extracts inhibit lipid oxidation and improve consumer liking of ready-to-eat (RTE) pork patties.

    Science.gov (United States)

    Akcan, T; Estévez, M; Rico, S; Ventanas, S; Morcuende, D

    2017-04-01

    The objective of this work was to study the effectiveness of extracts from hawberry (Crataegus monogyna Jacq.) to inhibit lipid oxidation and odor deterioration during processing of ready-to-eat (RTE) pork patties subjected to roasting (180 °C/16 min), chilling (10 days/+3 °C) and reheating in microwave (600 mW/1 min). Acetone extracts of hawberry were chosen based on their total phenolic content (1281.1 ± 84.8 mg gallic acid equivalent (GAE)/100 g fruit) and in vitro antiradical activity (DPPH) (53.33 ± 15.40 g equivalent Trolox per g of fruits). Pork patties treated with increasing concentrations of hawberry extract, 200 and 800 ppm GAE (T2 and T8, respectively) and a control group (T0) of samples, were analyzed for TBARS, volatile carbonyls and odor liking in a consumer test. Hawberry extracts significantly improved the oxidative stability of cooked pork patties keeping TBARS and hexanal counts at basal levels during the whole process. The addition of hawberry phenolic-rich extracts significantly improved the degree of consumer satisfaction regarding the odor of patties. In conclusion, the hawberry extract displayed potential usage as an ingredient with antioxidant properties for the manufacture of high-quality RTE meat products.

  8. Ethyl Acetate Extracts of Semen Impatientis Inhibit Proliferation and Induce Apoptosis of Human Prostate Cancer Cell Lines through AKT/ERK Pathways.

    Science.gov (United States)

    Wang, Tao; Cai, Yang; Song, Wen; Chen, Ruibao; Hu, Dunmei; Ye, Jianhan; Liu, Lu; Peng, Wei; Zhang, Junfeng; Wang, Shaogang; Yang, Weiming; Liu, Jihong; Ding, Yufeng

    2017-01-01

    Objective. To investigate the inhibitory effect of ethyl acetate extracts of Impatiens balsamina L. on prostate cancer cells. Methods. Impatiens balsamina L. was extracted to get water, ethanol, oil ether, ethyl acetate, and butanol extracts. CCK-8 assay was used to detect the inhibitory effect. Apoptosis rates and cell cycle distribution were detected by flow cytometry. Transwell assay was performed to test the ability of migration. The expressions of Bcl-2, Bax, cleaved-caspase-3, p-ERK, ERK, p-AKT, AKT, cyclin D1, cyclin E, and MMP2 were detected by Western blot. Results. Ethyl acetate extracts had the strongest inhibitory effect. After being treated with different concentrations of ethyl acetate extracts, the percentage of G0/G1 phase increased significantly, cyclin D1 and cyclin E expression decreased, apoptosis rate was significantly higher, and the ability of migration of PC-3 and RV1 was inhibited significantly. Western blot showed that the expressions of Bcl-2, p-ERK, and p-AKT were significantly decreased, but the expressions of Bax and caspase-3 cleavage were increased. Conclusions. Impatiens balsamina L. inhibited the proliferation of human prostate cancer cells; ethyl acetate extracts have the strongest effect. It could inhibit cell proliferation and migration, cause G1 phase arrest, and induce apoptosis probably through inhibition of the AKT and ERK pathways.

  9. Determination of the stability of diluted allergen extracts using a concentration step prior to EAST inhibition

    NARCIS (Netherlands)

    Niemeijer, NR; Kauffman, HF; DeMonchy, JGR; Meijer, G.

    1996-01-01

    Background Generally the stability of diluted allergen extracts, as used for skin testing, provocation testing and immunotherapy can not be measured using a normal enzyme allergosorbent test (EAST) inhibition method. Objective The aim of this study was to determine the stability of diluted allergen

  10. Pumpkin seed extract: Cell growth inhibition of hyperplastic and cancer cells, independent of steroid hormone receptors.

    Science.gov (United States)

    Medjakovic, Svjetlana; Hobiger, Stefanie; Ardjomand-Woelkart, Karin; Bucar, Franz; Jungbauer, Alois

    2016-04-01

    Pumpkin seeds have been known in folk medicine as remedy for kidney, bladder and prostate disorders since centuries. Nevertheless, pumpkin research provides insufficient data to back up traditional beliefs of ethnomedical practice. The bioactivity of a hydro-ethanolic extract of pumpkin seeds from the Styrian pumpkin, Cucurbita pepo L. subsp. pepo var. styriaca, was investigated. As pumpkin seed extracts are standardized to cucurbitin, this compound was also tested. Transactivational activity was evaluated for human androgen receptor, estrogen receptor and progesterone receptor with in vitro yeast assays. Cell viability tests with prostate cancer cells, breast cancer cells, colorectal adenocarcinoma cells and a hyperplastic cell line from benign prostate hyperplasia tissue were performed. As model for non-hyperplastic cells, effects on cell viability were tested with a human dermal fibroblast cell line (HDF-5). No transactivational activity was found for human androgen receptor, estrogen receptor and progesterone receptor, for both, extract and cucurbitin. A cell growth inhibition of ~40-50% was observed for all cell lines, with the exception of HDF-5, which showed with ~20% much lower cell growth inhibition. Given the receptor status of some cell lines, a steroid-hormone receptor independent growth inhibiting effect can be assumed. The cell growth inhibition for fast growing cells together with the cell growth inhibition of prostate-, breast- and colon cancer cells corroborates the ethnomedical use of pumpkin seeds for a treatment of benign prostate hyperplasia. Moreover, due to the lack of androgenic activity, pumpkin seed applications can be regarded as safe for the prostate.

  11. Risperidone significantly inhibits interferon-gamma-induced microglial activation in vitro.

    Science.gov (United States)

    Kato, Takahiro; Monji, Akira; Hashioka, Sadayuki; Kanba, Shigenobu

    2007-05-01

    Microglia has recently been regarded to be a mediator of neuroinflammation via the release of proinflammatory cytokines, nitric oxide (NO) and reactive oxygen species (ROS) in the central nervous system (CNS). Microglia has thus been reported to play an important role in the pathology of neurodegenerative disease, such as Alzheimer's disease (AD) and Parkinson's disease (PD). The pathological mechanisms of schizophrenia remain unclear while some recent neuroimaging studies suggest even schizophrenia may be a kind of neurodegenerative disease. Risperidone has been reported to decrease the reduction of MRI volume during the clinical course of schizophrenia. Many recent studies have demonstrated that immunological mechanisms via such as interferon (IFN)-gamma and cytokines might be relevant to the pathophysiology of schizophrenia. In the present study, we thus investigated the effects of risperidone on the generation of nitric oxide, inducible NO synthase (iNOS) expression and inflammatory cytokines: interleukin (IL)-1beta, IL-6 and tumor necrosis factor (TNF)-alpha by IFN-gamma-activated microglia by using Griess assay, Western blotting and ELISA, respectively. In comparison with haloperidol, risperidone significantly inhibited the production of NO and proinflammatory cytokines by activated microglia. The iNOS levels of risperidone-treated cells were much lower than those of the haloperidol-treated cells. Antipsychotics, especially risperidone may have an anti-inflammatory effect via the inhibition of microglial activation, which is not only directly toxic to neurons but also has an inhibitory effect on neurogenesis and oligodendrogenesis, both of which have been reported to play a crucial role in the pathology of schizophrenia.

  12. Corrosion inhibition performance of different bark extracts on aluminium in alkaline solution

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    Namrata Chaubey

    2017-02-01

    Full Text Available The present work shows the effect of stem bark extracts of three trees namely Moringa oleifera (MO, Terminalia arjuna (TA and Mangifera indica (MI on the corrosion behaviour of Aluminium Alloy (AA in 1 M NaOH. The inhibition performance was studied by using gravimetric, potentiodynamic polarization and electrochemical impedance spectroscopy (EIS measurements. Among these extracts, MO exhibited the maximum inhibition efficiency η (% of 85.3% at 0.6 g/L at 303 K. Polarization measurement showed that all the examined extracts are of mixed-type inhibitors. Langmuir’s adsorption isotherm was found to be best fit. Morphology of the surface was examined by scanning electron microscopy (SEM and atomic force microscopy (AFM which confirmed the existence of a protective film of inhibitor molecule on AA surface.

  13. Saffron Aqueous Extract Inhibits the Chemically-induced Gastric Cancer Progression in the Wistar Albino Rat

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    S. Zahra Bathaie

    2013-01-01

    Full Text Available Objective(s: Gastric cancer is the first and second leading cause of cancer related death in Iranian men and women, respectively. Gastric cancer management is based on the surgery, radiotherapy and chemotherapy. In the present study, for the first time, the beneficial effect of saffron (Crocus sativus L. aqueous extract (SAE on the 1-Methyl-3-nitro-1-nitrosoguanidine (MNNG-induced gastric cancer in rat was investigated. Materials and Methods: MNNG was used to induce gastric cancer and then, different concentrations of SAE were administered to rats. After sacrificing, the stomach tissue was investigated by both pathologist and flow cytometry, and several biochemical parameters was determined in the plasma (or serum and stomach of rats. Results: Pathologic data indicated the induction of cancer at different stages from hyperplasia to adenoma in rats; and the inhibition of cancer progression in the gastric tissue by SAE administration; so that, 20% of cancerous rats treated with higher doses of SAE was completely normal at the end of experiment and there was no rat with adenoma in the SAE treated groups. In addition, the results of the flow cytometry/ propidium iodide staining showed that the apoptosis/proliferation ratio was increased due to the SAE treatment of cancerous rats. Moreover, the significantly increased serum LDH and decreased plasma antioxidant activity due to cancer induction fell backwards after treatment of rats with SAE. But changes in the other parameters (Ca2+, tyrosine kinase activity and carcino-embryonic antigen were not significant. Conclusion: SAE inhibits the progression of gastric cancer in rats, in a dose dependent manner.

  14. In Vitro Inhibition of Cholera Toxin Production in Vibrio cholerae by Methanol Extract of Sweet Fennel Seeds and Its Components.

    Science.gov (United States)

    Chatterjee, Shruti; Zahid, M Shamim Hasan; Awasthi, Sharda Prasad; Chowdhury, Nityananda; Asakura, Masahiro; Hinenoya, Atsushi; Ramamurthy, T; Iwaoka, Emiko; Aoki, Shunji; Yamasaki, Shinji

    2016-09-21

    A newly emerged Vibrio cholerae O1 El Tor variant strain with multidrug resistance is considered a threat to public health. Recent strategies to suppress virulence factors production instead of bacterial growth may lead to less selective pressure for the emergence of resistant strains. The use of spices and their active constituents as the inhibitory agents against cholera toxin (CT) production in V. cholerae may be an alternative approach to treat cholera. In this study, we examined the potential of sweet fennel seed (Foeniculum vulgare Miller var. dulce) methanol extract to inhibit CT production in V. cholerae without affecting viability. The methanol extract of sweet fennel seeds significantly inhibited CT production in various V. cholerae strains, regardless of serogroup or biotype. Interestingly, trans-anethole and 4-allylanisole, essential oil components of sweet fennel seeds, also demonstrated similar effects. Here, we report that sub-bactericidal concentrations of sweet fennel seed methanol extract and its major components can drastically inhibit CT production in various V. cholerae strains.

  15. Compounds from Terminalia mantaly L. (Combretaceae Stem Bark Exhibit Potent Inhibition against Some Pathogenic Yeasts and Enzymes of Metabolic Significance

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    Marthe Aimée Tchuente Tchuenmogne

    2017-01-01

    Full Text Available Background: Pathogenic yeasts resistance to current drugs emphasizes the need for new, safe, and cost-effective drugs. Also, new inhibitors are needed to control the effects of enzymes that are implicated in metabolic dysfunctions such as cancer, obesity, and epilepsy. Methods: The anti-yeast extract from Terminalia mantaly (Combretaceae was fractionated and the structures of the isolated compounds established by means of spectroscopic analysis and comparison with literature data. Activity was assessed against Candida albicans, C. parapsilosis and C. krusei using the microdilution method, and against four enzymes of metabolic significance: glucose-6-phosphate dehydrogenase, human erythrocyte carbonic anhydrase I and II, and glutathione S-transferase. Results: Seven compounds, 3,3′-di-O-methylellagic acid 4′-O-α-rhamnopyranoside; 3-O-methylellagic acid; arjungenin or 2,3,19,23-tetrahydroxyolean-12-en-28-oïc acid; arjunglucoside or 2,3,19,23-tetrahydroxyolean-12-en-28-oïc acid glucopyranoside; 2α,3α,24-trihydroxyolean-11,13(18-dien-28-oïc acid; stigmasterol; and stigmasterol 3-O-β-d-glucopyranoside were isolated from the extract. Among those, 3,3′-di-O-methylellagic acid 4′-O-α-rhamnopyranoside, 3-O-methylellagic acid, and arjunglucoside showed anti-yeast activity comparable to that of reference fluconazole with minimal inhibitory concentrations (MIC below 32 µg/mL. Besides, Arjunglucoside potently inhibited the tested enzymes with 50% inhibitory concentrations (IC50 below 4 µM and inhibitory constant (Ki <3 µM. Conclusions: The results achieved indicate that further SAR studies will likely identify potent hit derivatives that should subsequently enter the drug development pipeline.

  16. Inhibition of collagen production in scleroderma fibroblast cultures by a connective tissue glycoprotein extracted from normal dermis

    Energy Technology Data Exchange (ETDEWEB)

    Maquart, F.X.; Bellon, G.; Cornillet-Stoupy, J.; Randoux, A.; Triller, R.; Kalis, B.; Borel, J.P.

    1985-08-01

    It was shown in a previous paper that a connective tissue glycoprotein (CTGP) extracted from normal rabbit dermis was able to inhibit total protein and collagen syntheses by normal dermis fibroblast cultures. In the present study, the effects of CTGP on scleroderma fibroblasts were investigated. (/sup 14/C)Proline incorporation into total proteins of the supernatant was not significantly different from that found in controls. By contrast, the amount of collagen, expressed as percentage of total secreted protein, was far higher in scleroderma cultures than in normal ones (14.4% +/- 6.0% vs 4.6% +/- 0.9%). Addition of CTGP to the medium induced a concentration-dependent inhibition of (/sup 14/C)proline incorporation into proteins from both control and scleroderma cells. In control cultures, no significant decrease of the percentage of collagen was observed, but over 60 micrograms/ml, both cytotoxic effects and inhibition of protein synthesis occurred. In scleroderma cultures, the inhibition was twice as effective on collagen as on noncollagen protein synthesis. The inhibition of collagen secretion was not related either to changes in collagen hydroxylation or to the intracellular catabolism of newly synthesized procollagen.

  17. Attachment and penetration of acyclovir-resistant herpes simplex virus are inhibited by Melissa officinalis extract.

    Science.gov (United States)

    Astani, Akram; Navid, Mojdeh Heidary; Schnitzler, Paul

    2014-10-01

    Medicinal plants are increasingly of interest as novel source of drugs for antiherpetic agents, because herpes simplex virus (HSV) might develop resistance to commonly used antiviral drugs. An aqueous extract of Melissa officinalis and the phenolic compounds caffeic acid, p-coumaric acid and rosmarinic acid were examined for their antiviral activity against herpes simplex virus type 1 (HSV-1) acyclovir-sensitive and clinical isolates of acyclovir-resistant strains in vitro. When drugs were added during the intracellular replication of HSV-1 infected cells, no antiviral effect was observed by plaque reduction assay. However, Melissa extract interacted directly with free viral particles of two acyclovir-resistant HSV strains at low IC50 values of 0.13 and 0.23 µg/mL and high selectivity indices of 2692 and 1522, respectively. The Melissa extract and rosmarinic acid inhibited HSV-1 attachment to host cells in a dose-dependent manner for acyclovir-sensitive and acyclovir-resistant strains. These results indicate that mainly rosmarinic acid contributed to the antiviral activity of Melissa extract. Penetration of herpes viruses into cells was inhibited by Melissa extract at 80% and 96% for drug-sensitive and drug-resistant viruses, respectively. Melissa extract exhibits low toxicity and affects attachment and penetration of acyclovir-sensitive and acyclovir-resistant HSVs in vitro. Copyright © 2014 John Wiley & Sons, Ltd.

  18. Efficacy of antimicrobials extracted from organic pecan shell for inhibiting the growth of Listeria spp.

    Science.gov (United States)

    Babu, Dinesh; Crandall, Philip G; Johnson, Casey L; O'Bryan, Corliss A; Ricke, Steven C

    2013-12-01

    Growers and processors of USDA certified organic foods are in need of suitable organic antimicrobials. The purpose of the research reported here was to develop and test natural antimicrobials derived from an all-natural by-product, organic pecan shells. Unroasted and roasted organic pecan shells were subjected to solvent free extraction to produce antimicrobials that were tested against Listeria spp. and L. monocytogenes serotypes to determine the minimum inhibitory concentrations (MIC) of antimicrobials. The effectiveness of pecan shell extracts were further tested using a poultry skin model system and the growth inhibition of the Listeria cells adhered onto the skin model were quantified. The solvent free extracts of pecan shells inhibited Listeria strains at MICs as low as 0.38%. The antimicrobial effectiveness tests on a poultry skin model exhibited nearly a 2 log reduction of the inoculated cocktail mix of Listeria strains when extracts of pecan shell powder were used. The extracts also produced greater than a 4 log reduction of the indigenous spoilage bacteria on the chicken skin. Thus, the pecan shell extracts may prove to be very effective alternative antimicrobials against food pathogens and supplement the demand for effective natural antimicrobials for use in organic meat processing.

  19. Well-tolerated Spirulina extract inhibits influenza virus replication and reduces virus-induced mortality.

    Science.gov (United States)

    Chen, Yi-Hsiang; Chang, Gi-Kung; Kuo, Shu-Ming; Huang, Sheng-Yu; Hu, I-Chen; Lo, Yu-Lun; Shih, Shin-Ru

    2016-04-12

    Influenza is one of the most common human respiratory diseases, and represents a serious public health concern. However, the high mutability of influenza viruses has hampered vaccine development, and resistant strains to existing anti-viral drugs have also emerged. Novel anti-influenza therapies are urgently needed, and in this study, we describe the anti-viral properties of a Spirulina (Arthrospira platensis) cold water extract. Anti-viral effects have previously been reported for extracts and specific substances derived from Spirulina, and here we show that this Spirulina cold water extract has low cellular toxicity, and is well-tolerated in animal models at one dose as high as 5,000 mg/kg, or 3,000 mg/kg/day for 14 successive days. Anti-flu efficacy studies revealed that the Spirulina extract inhibited viral plaque formation in a broad range of influenza viruses, including oseltamivir-resistant strains. Spirulina extract was found to act at an early stage of infection to reduce virus yields in cells and improve survival in influenza-infected mice, with inhibition of influenza hemagglutination identified as one of the mechanisms involved. Together, these results suggest that the cold water extract of Spirulina might serve as a safe and effective therapeutic agent to manage influenza outbreaks, and further clinical investigation may be warranted.

  20. Tinospora crispa extract inhibits MMP-13 and migration of head and neck squamous cell carcinoma cell lines

    Institute of Scientific and Technical Information of China (English)

    Hataipan Phienwej; Ih-si Swasdichira; Surattana Amnuoypol; Prasit Pavasant; Piyamas Sumrejkanchanakij

    2015-01-01

    To investigate the effect of Tinospora crispa (T. crispa) extract on matrix metalloproteinase 13 (MMP-13) expression and cell migration. Methods: The cytotoxicity of T. crispa extract was examined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay on head and neck squamous cell carcinoma (HNSCC) cell lines. The effect on expression of MMP-13 was analysed by RT-PCR and ELISA. The migration was assessed by wound healing assay. Results: MMP-13 mRNA was highly expressed in the metastatic human HNSCC cell lines, HN22 and HSC-3. T. crispa extract at a concentration of 100.0 µg/mL caused about 50% reduction of cell survival. T. crispa extract at a non-toxic concentration of 12.5, 25.0 and 50.0 µg/mL significantly suppressed MMP-13 mRNA expression and secreted MMP-13 in both HN22 and HSC-3. The expression of tissue inhibitors of metalloprotease by HSC-3 cells was attenuated by 25.0 and 50.0 µg/mL of T. crispa extract. Addition of the extract to cells in a wound healing assay showed inhibition of cell migration by HN22 cells. Conclusions: These data suggest that T. crispa could be considered as a potential therapeutic drug to prevent metastasis of HNSCC.

  1. In vitro study of the PLA2 inhibition and antioxidant activities of Aloe vera leaf skin extracts

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    Gargouri Youssef

    2011-02-01

    Full Text Available Abstract Background In the present work we determined the total phenolic content of Aloe vera leaf skin (AVLS extracts by using various solvents (hexane, chloroform-ethanol (1/1, ethyl acetate, butanol and water. We have also evaluated the antioxidant and the anti-PLA2 properties of these extracts by measuring their inhibition potency on the human pro-inflammatory phospholipase A2 (group IIA. Results The water extract exhibits the highest inhibitory effect with an IC50 = 0.22 mg/ml and interestingly no effect was observed on the digestive phospholipase A2 (group IB even at a concentration of 5 mg/ml. Antioxidant activities were also analyzed and the most active extracts were observed when using chloroform ethanol (1/1 and ethyl acetate (IC50 = 0.274 and 0.326 mg/ml, respectively. Analysis of the total phenolic content reveals that the water extract, with the best anti-PLA2 effect, was poor in phenolic molecules (2 mg GAE/g. This latter value has to be compared with the chloroform-ethanol and the ethyl acetate extracts (40 and 23.8 mg GAE/g, respectively, mostly responsible for the antioxidant activity. Conclusion A significant correlation was established between the total phenolic content and the antioxidant capacity but not with the anti PLA2 activity. Results from phytochemical screening suggest that the anti PLA2 molecules were probably catechin tannins compounds.

  2. Bioactive compounds extracted from Indian wild legume seeds: antioxidant and type II diabetes-related enzyme inhibition properties.

    Science.gov (United States)

    Gautam, Basanta; Vadivel, Vellingiri; Stuetz, Wolfgang; Biesalski, Hans K

    2012-03-01

    Seven different wild legume seeds (Acacia leucophloea, Bauhinia variegata, Canavalia gladiata, Entada scandens, Mucuna pruriens, Sesbania bispinosa and Tamarindus indica) from various parts of India were analyzed for total free phenolics, l-Dopa (l-3,4 dihydroxyphenylalanine), phytic acid and their antioxidant capacity (ferric-reducing antioxidant power [FRAP] and 2,2-diphenyl-1-picrylhydrazyl [DPPH] assay) and type II diabetes-related enzyme inhibition activitiy (α-amylase). S. bispinosa had the highest content in both total free phenolics and l-Dopa, and relatively low phytic acid when compared with other seeds. Phytic acid content, being highest in E. scandens, M. pruriens and T. indica, was highly predictive for FRAP (r = 0.47, p < 0.05) and DPPH (r = 0.66, p < 0.001) assays. The phenolic extract from T. indica and l-Dopa extract from E. scandens showed significantly higher FRAP values among others. All seed extracts demonstrated a remarkable reducing power (7-145 mM FeSO4 per mg extract), DPPH radical scavenging activity (16-95%) and α-amylase enzyme inhibition activity (28-40%).

  3. Selected Tea and Tea Pomace Extracts Inhibit Intestinal α-Glucosidase Activity in Vitro and Postprandial Hyperglycemia in Vivo

    Directory of Open Access Journals (Sweden)

    Jungbae Oh

    2015-04-01

    Full Text Available Type 2 diabetes mellitus (T2DM is a metabolic disorder characterized by postprandial hyperglycemia, which is an early defect of T2DM and thus a primary target for anti-diabetic drugs. A therapeutic approach is to inhibit intestinal α-glucosidase, the key enzyme for dietary carbohydrate digestion, resulting in delayed rate of glucose absorption. Although tea extracts have been reported to have anti-diabetic effects, the potential bioactivity of tea pomace, the main bio waste of tea beverage processing, is largely unknown. We evaluated the anti-diabetic effects of three selected tea water extracts (TWE and tea pomace extracts (TPE by determining the relative potency of extracts on rat intestinal α-glucosidase activity in vitro as well as hypoglycemic effects in vivo. Green, oolong, and black tea bags were extracted in hot water and the remaining tea pomace were dried and further extracted in 70% ethanol. The extracts were determined for intestinal rat α-glucosidases activity, radical scavenging activity, and total phenolic content. The postprandial glucose-lowering effects of TWE and TPE of green and black tea were assessed in male Sprague-Dawley (SD rats and compared to acarbose, a known pharmacological α-glucosidase inhibitor. The IC50 values of all three tea extracts against mammalian α-glucosidase were lower or similar in TPE groups than those of TWE groups. TWE and TPE of green tea exhibited the highest inhibitory effects against α-glucosidase activity with the IC50 of 2.04 ± 0.31 and 1.95 ± 0.37 mg/mL respectively. Among the specific enzymes tested, the IC50 values for TWE (0.16 ± 0.01 mg/mL and TPE (0.13 ± 0.01 mg/mL of green tea against sucrase activity were the lowest compared to those on maltase and glucoamylase activities. In the animal study, the blood glucose level at 30 min after oral intake (0.5 g/kg body wt of TPE and TWE of both green and black tea was significantly reduced compared to the control in sucrose-loaded SD

  4. Selected tea and tea pomace extracts inhibit intestinal α-glucosidase activity in vitro and postprandial hyperglycemia in vivo.

    Science.gov (United States)

    Oh, Jungbae; Jo, Sung-Hoon; Kim, Justin S; Ha, Kyoung-Soo; Lee, Jung-Yun; Choi, Hwang-Yong; Yu, Seok-Yeong; Kwon, Young-In; Kim, Young-Cheul

    2015-01-01

    Type 2 diabetes mellitus (T2DM) is a metabolic disorder characterized by postprandial hyperglycemia, which is an early defect of T2DM and thus a primary target for anti-diabetic drugs. A therapeutic approach is to inhibit intestinal α-glucosidase, the key enzyme for dietary carbohydrate digestion, resulting in delayed rate of glucose absorption. Although tea extracts have been reported to have anti-diabetic effects, the potential bioactivity of tea pomace, the main bio waste of tea beverage processing, is largely unknown. We evaluated the anti-diabetic effects of three selected tea water extracts (TWE) and tea pomace extracts (TPE) by determining the relative potency of extracts on rat intestinal α-glucosidase activity in vitro as well as hypoglycemic effects in vivo. Green, oolong, and black tea bags were extracted in hot water and the remaining tea pomace were dried and further extracted in 70% ethanol. The extracts were determined for intestinal rat α-glucosidases activity, radical scavenging activity, and total phenolic content. The postprandial glucose-lowering effects of TWE and TPE of green and black tea were assessed in male Sprague-Dawley (SD) rats and compared to acarbose, a known pharmacological α-glucosidase inhibitor. The IC50 values of all three tea extracts against mammalian α-glucosidase were lower or similar in TPE groups than those of TWE groups. TWE and TPE of green tea exhibited the highest inhibitory effects against α-glucosidase activity with the IC50 of 2.04 ± 0.31 and 1.95 ± 0.37 mg/mL respectively. Among the specific enzymes tested, the IC50 values for TWE (0.16 ± 0.01 mg/mL) and TPE (0.13 ± 0.01 mg/mL) of green tea against sucrase activity were the lowest compared to those on maltase and glucoamylase activities. In the animal study, the blood glucose level at 30 min after oral intake (0.5 g/kg body wt) of TPE and TWE of both green and black tea was significantly reduced compared to the control in sucrose-loaded SD rats. The TPE

  5. Determination of trace mercury in compost extract by inhibition based glucose oxidase biosensor

    Institute of Scientific and Technical Information of China (English)

    LIU Jian-xiao; XU Xiang-min; TANG Lin; ZENG Guang-ming

    2009-01-01

    A novel inhibition based biosensor of glucose oxidase(GOx) for environmental mercury detection was developed. An electropolymerized aniline membrane was prepared on a platinum electrode containing ferrocene as electron transfer mediator, on which GOx was cross-linked by glutaraldehyde. The response of the sensor was based on the current reduction in the electrochemical system by inhibition of mercury against GOx electrode. The detection limit of the inhibition-based sensor for mercury is 0.49 μg/L, and the linear response ranges are 0.49-783.21 μg/L and 783.21 μg/L-25.55 mg/L. The GOx membrane can be completely reactivated after inhibition, and remains 70% of the activity in more than one month. The sensor was used for mercury determination in compost extract with good results.

  6. Melissa officinalis extract inhibits attachment of herpes simplex virus in vitro.

    Science.gov (United States)

    Astani, Akram; Reichling, Jürgen; Schnitzler, Paul

    2012-01-01

    Extracts and essential oils of medicinal plants are increasingly of interest as novel drugs for antiherpetic agents, since the herpes simplex virus (HSV) might develop resistance to commonly used antiviral drugs. An aqueous extract of Melissa officinalis as well as phenolic extract compounds, i.e. caffeic acid, p-coumaric acid and rosmarinic acid were examined for their antiviral activity against herpes simplex virus type 1 (HSV-1) in vitro. When drugs were added to HSV-1-infected cells, no antiviral effect was observed as determined by plaque reduction assay and analysis of expression of viral protein ICP0. However, the Melissa extract demonstrated a high virucidal activity against HSV-1, even at very low concentrations of 1.5 μg/ml, whereas similar results for phenolic compounds were only achieved at 100 times higher concentrations. Besides the virucidal activity, the Melissa extract and rosmarinic acid inhibited HSV-1 attachment to host cells in a dose-dependent manner. These results indicate that rosmarinic acid was the main contributor to the antiviral activity of Melissa extract. However, the selectivity index of Melissa extract of 875 against HSV is superior to the selectivity indices of single constituents. Melissa extract exhibits low toxicity, is virucidal and affects HSV-1 attachment to host cells in vitro. Copyright © 2012 S. Karger AG, Basel.

  7. Inhibition of glucose- and fructose-mediated protein glycation by infusions and ethanolic extracts of ten culinary herbs and spices

    Institute of Scientific and Technical Information of China (English)

    Jugjeet Singh Ramkissoon; Mohamad Fawzi Mahomoodally; Anwar Hussein Subratty; Nessar Ahmed

    2016-01-01

    Objective: To investigate the inhibitory activity of ten culinary herbs and spices namely on glucose-mediated glycation (GMG) and fructose-mediated glycation (FMG) of bovine serum albumin. Methods: Fluorescence was used as an index of albumin glycation using glucose and fructose as substrates in the presence of infusions and ethanolic extracts of ten culinary herbs and spices. Antioxidant activity of the extracts was evaluated using reducing power, metal ion chelating and superoxide radical scavenging assays. Phytochemicals profile was analysed using 13 standard methods. Results: FMG was found to be significantly higher than GMG (95 and 84 AU, respectively; P 0.05) was found in the percentage glycation inhibitory activity of infusions compared to ethanolic extracts. The mean percentage inhibitory activity of the extracts for GMG (45.9%) and for FMG (45.1%) was not significantly different (P > 0.05). Qualitative phytochemical analysis showed the presence of alkaloids, fla-vonoids, tannins, terpenoids, anthraquinones, steroids, reducing sugars, proteins, phenols, saponins, phlobatannins, and cardiac glycosides. Conclusions: The higher rate of fluorescence generation by fructation suggests that glycation by fructose deserves much attention as a glycating agent. Data herein showed that the extracts inhibited GMG and FMG. Thus, these edible plants could be a natural source of antioxidants and anti-glycation agent for preventing advanced glycation end-products-mediated complications.

  8. Inhibition Effect of Mace Extract Microemulsion on Vitamin C Photooxidation in Aqueous Systems

    Directory of Open Access Journals (Sweden)

    Hasbullah Hasbullah

    2014-01-01

    Full Text Available Photooxidation in food systems cause nutritional losses and produces undesirable flavor, toxic and color compounds, which make foods less acceptable or unacceptable to consumers. The objective of this research was to know the effectiveness of mace extract microemulsion to inhibit vitamin C photooxidation in aqueous systems. Aqueous food systems used are both beverage model system and apple juice beverage, where in each system enriched by 100 ppm vitamin C as substrate and 20 ppm erytrosin as photosensitiser. It is about one percent and two percent of microemulsion that contain mace extract of 0, 500 and 750 ppm were added into each of aqueous food system. Inhibition effect of mace extract microemulsion toward vitamin C photooxidation based on the rate of vitamin C degradation in aqueous food systems that illuminated by fluorescent light with 2000 lux intensity within eight hours. The result indicated the mace extract microemulsion has anti-photooxidation activity and ability to inhibit vitamin C photooxidation in aqueous systems.

  9. Corrosion Inhibition by Tithonia diversifolia (Hemsl) A. Gray leaves extract for 304 SS in hydrochloric acid solution

    Science.gov (United States)

    Firdausi, S.; Kurniawan, F.

    2016-04-01

    The inhibition effect of Tithonia diversifolia (Hemsl) A. Gray leaves extract on the corrosion phenomena of 304 SS in 1 M HCl has been studied by polarization potentiodynamic. The powder of T. diversifolia was extracted by demineralized water which was cultivated in East Java, Indonesia. The extract was characterized by FTIR spectrophotometer. The presence of T. diversifolia can inhibit the corrosion rate of 304 SS. The efficiency inhibition value of 2 g/L T. diversifolia leaves extract reached up to 77.27% at room temperature.

  10. Adsorption and corrosion-inhibiting effect of Dacryodis edulis extract on low-carbon-steel corrosion in acidic media.

    Science.gov (United States)

    Oguzie, E E; Enenebeaku, C K; Akalezi, C O; Okoro, S C; Ayuk, A A; Ejike, E N

    2010-09-01

    The inhibition of low-carbon-steel corrosion in 1M HCl and 0.5M H(2)SO(4) by extracts of Dacryodis edulis (DE) was investigated using gravimetric and electrochemical techniques. DE extract was found to inhibit the uniform and localized corrosion of carbon steel in the acidic media, affecting both the cathodic and anodic partial reactions. The corrosion process was inhibited by adsorption of the extracted organic matter onto the steel surface in a concentration-dependent manner and involved both protonated and molecular species. Molecular dynamics simulations were performed to illustrate the process of adsorption of some specific components of the extract.

  11. Extracts of medicinal herb Sanguisorba officinalis inhibit the entry of human immunodeficiency virus type one.

    Science.gov (United States)

    Liang, Jianguo; Chen, Jianping; Tan, Zhiwu; Peng, Jie; Zheng, Xiao; Nishiura, Kenji; Ng, Jenny; Wang, Zhiyu; Wang, Dongmei; Chen, Zhiwei; Liu, Li

    2013-12-01

    Highly active antiretroviral therapy (HAART) has been successful in reducing HIV-1-associated morbidity and mortality since its introduction in 1996. It, however, fails to eradicate HIV-1 infection thoroughly. The high cost of life-long HAART and the emergence of drug resistance among HIV-1-infected individuals have brought renewed pressure for the discovery of novel antivirals and alternative medicines. Traditional Chinese medicine (TCM) is one of the mainstreams of complementary and alternative medicine, and serves as rich resources for new drug development. Despite almost 100 plant-derived compounds are in clinical trials, few target HIV-1 infection. In this study, we discovered that extract of Sanguisorba officinalis (SOE) has anti-HIV-1 activities. Using a cell-based assay and single-cycle luciferase reporter viruses pseudotyped with envelopes from HIV-1 or control viruses, we found that SOE exhibited significant inhibitory ability against both CCR5 and CXCR4 tropic HIV-1 (ADA and HXB2) with respective IC50 values of 1.91±0.16 μg/ml and 3.70±0.53 μg/ml. Interestingly, SOE also inhibited SIV infection but failed to block vesicular stomatitis virus (VSV), SARS-CoV and influeunza H5N1 pseudoviruses. Furthermore, we showed that SOE had no effects on post-entry events of HIV-1 replication. It blocked entry by acting on viral envelope directly because SOE pre-treatment with the virus but not with cell lines expressing viral receptors showed the maximal inhibitory activity. In addition, SOE was able to inhibit reverse-transcription-inhibitor-resistant viruses (K103N, Y188L, and K103N/Y188L/G190A) and a protease-inhibitor-resistant strain (PI-2840). Our findings demonstrated SOE as a novel and specific entry inhibitor, which shed lights on the discovery of anti-HIV-1 drugs from traditional herbal medicines.

  12. Oral infusion of pomegranate fruit extract inhibits prostate carcinogenesis in the TRAMP model.

    Science.gov (United States)

    Adhami, Vaqar Mustafa; Siddiqui, Imtiaz Ahmad; Syed, Deeba N; Lall, Rahul Kumar; Mukhtar, Hasan

    2012-03-01

    We earlier provided evidence that oral consumption of pomegranate fruit extract (PFE) inhibits prostate cancer (PCa) cell growth in nude mice. To ascertain convincing evidence of chemopreventive effects of PFE against PCa, its efficacy requires to be evaluated in animal models that closely emulate human disease. Here, we provide evidence of remarkable tumor growth inhibitory effects of PFE using the TRAMP model. Mice received 0.1 and 0.2% PFE, equivalent to 250 and 500 ml of pomegranate juice, in drinking water, starting at 6 weeks and examined at 12, 20 and 34 weeks of age. In water-fed group, 100% mice developed palpable tumors by 20 weeks compared with only 30 and 20% in the 0.1 and 0.2% PFE-supplemented groups, respectively. At 34 weeks, palpable tumors were observed in 70 of 0.1% and only 50 of 0.2% PFE-supplemented mice. Compared with median survival of 43 weeks in water-fed mice, 0.1 and 0.2% PFE-supplemented mice exhibited median life expectancy of 73 and 92 weeks, respectively. Compared with respective water-fed groups, none of the mice in PFE-supplemented groups exhibited metastases to any of the distant organs at 20 weeks and only 20% mice exhibited metastasis at 34 weeks of age. Many of the PFE-supplemented animals had multiple foci of well-differentiated carcinoma but no evidence of poorly differentiated carcinoma. PFE supplementation resulted in simultaneous and significant inhibition of IGF-I/Akt/mTOR pathways in the prostate tissues and tumors. We suggest that pomegranate juice be evaluated in clinical trials in patients at high risk for developing PCa.

  13. Aqueous extract of Rabdosia rubescens leaves: forming nanoparticles, targeting P-selectin, and inhibiting thrombosis.

    Science.gov (United States)

    Wang, Yuji; Tang, Jingcheng; Zhu, Haimei; Jiang, Xueyun; Liu, Jiawang; Xu, Wenyun; Ma, Haiping; Feng, Qiqi; Wu, Jianhui; Zhao, Ming; Peng, Shiqi

    2015-01-01

    The hot water extract of Rabdosia rubescens was traditionally used as an antithrombotic medicine. To explore its antithrombotic utility and mechanism, we carried out a series of in vitro and in vivo assays in this study. In vitro platelet aggregation assay showed that the half maximal inhibitory concentration values of aqueous extract of R. rubescens leaves (AERL) inhibiting platelet aggregation induced by thrombin, arachidonic acid, adenosine diphosphate, and platelet-activating factor ranged from 0.12 mg/mL to 1.43 mg/mL. The minimal effective oral dose of AERL inhibiting the rats from forming thrombus was 25 mg/kg. Both in vitro and in vivo actions were correlated with AERL concentration-dependently inhibiting sP-selectin release. In water, AERL formed nanoparticles, and their size depended on the concentration. Docking the five nucleotides, 21 phenolic acids, and four diterpenoids identified by high-performance liquid chromatography-photodiode array detector/(-)electrospray ionization-tandem mass spectrometry analysis into the active site of P-selectin, rosmarinic acid was predicted to be the antithrombotic ingredient of AERL. In flow cytometry analysis, 1 μM of rosmarinic acid effectively inhibited sP-selectin release in arachidonic acid-activated platelets. In a rat model, 5 mg/kg of oral rosmarinic acid effectively inhibited thrombosis.

  14. Pentacyclic triterpenes in birch bark extract inhibit early step of herpes simplex virus type 1 replication.

    Science.gov (United States)

    Heidary Navid, M; Laszczyk-Lauer, M N; Reichling, J; Schnitzler, P

    2014-09-25

    Antiviral agents frequently applied for treatment of herpesvirus infections include acyclovir and its derivatives. The antiviral effect of a triterpene extract of birch bark and its major pentacyclic triterpenes, i.e. betulin, lupeol and betulinic acid against acyclovir-sensitive and acyclovir-resistant HSV type 1 strains was examined. The cytotoxic effect of a phytochemically defined birch bark triterpene extract (TE) as well as different pentacyclic triterpenes was analyzed in cell culture, and revealed a moderate cytotoxicity on RC-37 cells. TE, betulin, lupeol and betulinic acid exhibited high levels of antiviral activity against HSV-1 in viral suspension tests with IC50 values ranging between 0.2 and 0.5 μg/ml. Infectivity of acyclovir-sensitive and clinical isolates of acyclovir-resistant HSV-1 strains was significantly reduced by all tested compounds and a direct concentration- and time-dependent antiherpetic activity could be demonstrated. In order to determine the mode of antiviral action, TE and the compounds were added at different times during the viral infection cycle. Addition of these drugs to uninfected cells prior to infection or to herpesvirus-infected cells during intracellular replication had low effect on virus multiplication. Minor virucidal activity of triterpenes was observed, however both TE and tested compounds exhibited high anti-herpetic activity when viruses were pretreated with these drugs prior to infection. Pentacyclic triterpenes inhibit acyclovir-sensitive and acyclovir-resistant clinical isolates of HSV-1 in the early phase of infection. Copyright © 2014 Elsevier GmbH. All rights reserved.

  15. A Methanol Extract of Adansonia digitata L. Leaves Inhibits Pro-Inflammatory iNOS Possibly via the Inhibition of NF-κB Activation.

    Science.gov (United States)

    Ayele, Yihunie; Kim, Jung-Ah; Park, Eunhee; Kim, Ye-Jung; Retta, Negussie; Dessie, Gulelat; Rhee, Sang-Ki; Koh, Kwangoh; Nam, Kung-Woo; Kim, Hee Seon

    2013-03-01

    This study examined the total polyphenol content of eight wild edible plants from Ethiopia and their effect on NO production in Raw264.7 cells. Owing to its relatively high polyphenol concentration and inhibition of NO production, the methanol extract of Adansonia digitata L. leaf (MEAD) was subjected to detailed evaluation of its antioxidant and anti-inflammatory effects. Antioxidant effects were assessed by measuring free-radical-scavenging activity using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and oxygen-radical-absorbance capacity (ORAC) assays, while anti-inflammatory effects were assessed by measuring inducible nitric oxide synthase (iNOS) expression in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. In the ORAC assay, MEAD was 10.2 times more potent than vitamin C at eliminating peroxyl radicals. In DPPH assay, MEAD also showed a strong ROS scavenging effect. MEAD significantly inhibited iNOS activity (IC50=28.6 μg/ml) of LPS-stimulated Raw264.7 cells. We also investigated the relationship between iNOS expression and nuclear factor kappa B (NF-κB) activation. MEAD inhibited IκBα degradation and NF-κB translocation from the cytosol to the nucleus in LPS-induced RAW264.7 cells without significant cytotoxic effects, as confirmed by MTT assay. These results suggest that MEAD inhibits anti-inflammatory iNOS expression, which might be related to the elimination of peroxyl radicals and thus the inhibition of IκBα-mediated NF-κB signal transduction.

  16. Autophagy Inhibition Enhances the Mitochondrial-Mediated Apoptosis Induced by Mangrove (Avicennia marina) Extract in Human Breast Cancer Cells

    KAUST Repository

    Esau, Luke

    2015-01-10

    Aims: Avicennia marina (AM) is a widely distributed mangrove plant that has been used in traditional medicine for centuries for the treatment of a number of diseases. The objective of the present study was to evaluate the leaf ethyl acetate extract of AM for its cytotoxic and apoptotic potential along with in-depth investigations of its mechanism of action in breast cancer MCF-7 cells. Study Design: The ethyl acetate extract of leaves and stems of AM was tested against estrogen positive breast cancer cell line MCF-7 using various assays. Place and Duration of Study: The study was carried out at King Abdullah University of Science and Technology, Thuwal, Saudi Arabia, from July 2013-June 2014. Methodology: Dose- and time-dependent growth inhibition of cancer cells was measured using MTT assay. The mechanisms of apoptosis induction were determined using various assays: phosphatidylserine exposure, caspase-3/7 activation, mitochondrial membrane potential disruption, reactive oxygen species (ROS) production, cell cycle analysis, autophagy, and protein expression using western blotting. The modulation of apoptotic genes (p53, Mdm2, NF-kB, Bad, Bax, Bcl-2 and Casp7) was also determined using real time PCR. Results: The AM extract inhibited breast cancer cell growth and induced apoptosis in a concentration dependent manner. We demonstrated a non-classical mode of apoptosis induction in MCF-7 cells by AM extract, where ROS production altered the mitochondrial membrane potential to induce apoptosis. Breast cancer cells treated with 200 µg/ml concentration of AM extract showed increased ROS production and disrupted MMP but no PARP-1 cleavage and a marked decrease in Caspase-7 protein levels (24 and 48 h) were detected. A significant amount of autophagy was also observed at the same concentration. However, treatment of MCF-7 cells with 200 µg/ml of AM extract along with the inhibition of autophagy by chloroquine, significantly increased the apoptosis from 20% to 45

  17. Oligomeric procyanidins of French maritime pine bark extract (Pycnogenol) effectively inhibit alpha-glucosidase.

    Science.gov (United States)

    Schäfer, Angelika; Högger, Petra

    2007-07-01

    The standardized maritime pine bark extract (Pycnogenol) was reported to exert clinical anti-diabetic effects after peroral intake. However, an increased insulin secretion was not observed after administration of the extract to patients. Our aim was to elucidate whether the described clinical effects of Pycnogenol are related to inhibition of alpha-glucosidase. Therefore, we analyzed the inhibitory activity of Pycnogenol, green tea extract and acarbose towards alpha-glucosidase. Furthermore, we explored different fractions of Pycnogenol containing compounds of diverse molecular masses from polyphenolic monomers, dimers and higher oligomers to uncover which components exhibited the most pronounced inhibitory activity. We found that Pycnogenol exhibited the most potent inhibition (IC(50) about 5 microg/mL) on alpha-glucosidase compared to green tea extract (IC(50) about 20 microg/mL) and acarbose (IC(50) about 1mg/mL). The inhibitory action of Pycnogenol was stronger in extract fractions containing higher procyanidin oligomers. The results obtained assign a novel, local effect to oligomeric procyanidins and contribute to the explanation of glucose-lowering effects of Pycnogenol observed in clinical trials with diabetic patients.

  18. Ginkgo biloba leaf extract induces DNA damage by inhibiting topoisomerase II activity in human hepatic cells.

    Science.gov (United States)

    Zhang, Zhuhong; Chen, Si; Mei, Hu; Xuan, Jiekun; Guo, Xiaoqing; Couch, Letha; Dobrovolsky, Vasily N; Guo, Lei; Mei, Nan

    2015-09-30

    Ginkgo biloba leaf extract has been shown to increase the incidence in liver tumors in mice in a 2-year bioassay conducted by the National Toxicology Program. In this study, the DNA damaging effects of Ginkgo biloba leaf extract and many of its constituents were evaluated in human hepatic HepG2 cells and the underlying mechanism was determined. A molecular docking study revealed that quercetin, a flavonoid constituent of Ginkgo biloba, showed a higher potential to interact with topoisomerase II (Topo II) than did the other Ginkgo biloba constituents; this in silico prediction was confirmed by using a biochemical assay to study Topo II enzyme inhibition. Moreover, as measured by the Comet assay and the induction of γ-H2A.X, quercetin, followed by keampferol and isorhamnetin, appeared to be the most potent DNA damage inducer in HepG2 cells. In Topo II knockdown cells, DNA damage triggered by Ginkgo biloba leaf extract or quercetin was dramatically decreased, indicating that DNA damage is directly associated with Topo II. DNA damage was also observed when cells were treated with commercially available Ginkgo biloba extract product. Our findings suggest that Ginkgo biloba leaf extract- and quercetin-induced in vitro genotoxicity may be the result of Topo II inhibition.

  19. Inhibition of growth and sporulation of Penicillium expansum by extracts of selected Basidiomycetes

    Directory of Open Access Journals (Sweden)

    Teresa Florianowicz

    2014-01-01

    Full Text Available A screening of antifungal activity of 33 Basidiomycetes strains was realized with their extracts. The influence of aqueous extracts of fruit-bodies of the testeded fungi after addition of spores or hyphae of Penicillium expansum on growth and sporulation of the fitopathogen in vitro was estimated. The species: Hydnum repandum L.: Fr., Pleurotus ostreatus (Jacq.: Fr. Kummer, Coprinus comatus (Műll Fr. S.F. Gray, Coprinus atramentarius (Bull: Fr. Fr. and Lactarius turpis (Weinm. Fr. reduced the mycelial growth and inhibited sporulation of this pathogen.

  20. Inhibition of calcium carbonate deposition on stainless steel using olive leaf extract as a green inhibitor.

    Science.gov (United States)

    Aidoud, Roumaissa; Kahoul, Abdelkrim; Naamoune, Farid

    2017-01-01

    The antiscale properties of the aqueous extract of olive (Olea europaea L.) leaves as a natural scale inhibitor for stainless steel surface in Hammam raw water were investigated using chronoamperometry (CA) and electrochemical impedance spectroscopy techniques in conjunction with a microscopic examination. The X-ray diffraction analysis reveals that the scale deposited over the pipe walls consists of pure CaCO3 calcite. The CA, in accordance with electrochemical impedance spectra and scanning electron microscopy, shows that the inhibition efficiency increases with increasing extract concentration. This efficiency is considerably reduced as the temperature is increased.

  1. Human placental extract mediated inhibition of proteinase K: implications of heparin and glycoproteins in wound physiology.

    Science.gov (United States)

    Sharma, Kanika; Mukherjee, Chaitali; Roy, Siddhartha; De, Debashree; Bhattacharyya, Debasish

    2014-09-01

    Efficient debridement of the wound bed following the removal of microbial load prevents its progression into a chronic wound. Bacterial infection and excessive proteolysis characterize impaired healing and therefore, their inhibition might restore the disturbed equilibrium in the healing process. Human placental extract exhibits reversible, non-competitive inhibition towards Proteinase K, a microbial protease, by stabilizing it against auto-digestion. Scattering and fluorescence studies followed by biochemical analysis indicated the involvement of a glycan moiety. Surface plasmon resonance demonstrated specific interaction of heparin with Proteinase K having Kd in μM range. Further, Proteinase K contains sequence motifs similar to other heparin-binding proteins. Molecular docking revealed presence of clefts suitable for binding of heparin-derived oligosaccharides. Comprehensive analysis of this inhibitory property of placental extract partly explains its efficacy in curing wounds with common bacterial infections.

  2. Inhibition of microbial growth by spice extracts and their effect of irradiation

    Energy Technology Data Exchange (ETDEWEB)

    Ito, Hitoshi; Meixu, G. [Japan Atomic Energy Research Inst., Takasaki, Gunma (Japan). Takasaki Radiation Chemistry Research Establishment

    1994-08-01

    The antimicrobial activity of black pepper, rosemary and red pepper has been tested against 12 microorganisms. Alcoholic extracts of these spices were not exhibited strong activity against gram-negative bacteria in laboratory media. The growth of Bacillus subtilis and Clostridium botulinum type A was inhibited by 1% of black pepper, 0.5% rosemary and 0.03% red pepper. A little reduction of antimicrobial activity to B. subtilis was observed on extracts of gamma-irradiated black pepper or rosemary at 10 and 50 kGy. In the case of red pepper, irradiation of 10 or 50 kGy enhanced a little of antimicrobial activity to B. subtilis. Similar effect of irradiation was also observed on the inhibition of aflatoxin production by Aspergillus parasiticus in SL broth. (author).

  3. Ocimum basilicum extract exhibits antidiabetic effects via inhibition of hepatic glucose mobilization and carbohydrate metabolizing enzymes

    Science.gov (United States)

    Ezeani, Chinelo; Ezenyi, Ifeoma; Okoye, Theophine; Okoli, Charles

    2017-01-01

    Aim: Ocimum basilicum L (Lamiaceae) is used as a traditional remedy for different ailments, including diabetes mellitus. This study investigated the antidiabetic effects of an extract of aerial parts of O. basilicum. Methods: Antihyperglycemic effect of the extract was determined by its effects on α-amylase and α-glucosidase in vitro, while antidiabetic properties were studied in alloxan induced diabetic rats treated for 28 days with extract and compared to those treated with oral metformin (150 mg/kg). The study and analysis was conducted between 2014 and 2015. Results: The treatment with 100 and 200 mg/kg extract significantly (P glycogenolysis and/or stimulate glycogenesis. PMID:28163956

  4. Aqueous and organic extracts of Trigonellafoenum-graecum L. Inhibit the mycelia growth of fungi

    Institute of Scientific and Technical Information of China (English)

    R. HAOUALA; S. HAWALA; A. EL-AYEB; R. KHANFIR; N. BOUGHANMI

    2008-01-01

    Aqueous extracts from various plant parts of fenugreek (3%) (aerial parts: leaves and stems (LS), roots (R), ground seeds (GS) and not ground seeds (NGS)) and petroleum ether, ethyl acetate and methanolic fractions of the aerial parts were assayed to determine their antifungal potential against Botrytis cinema, Fusarium graminearum, Alternaria sp., Pythium aphanidermatum, and Rhizoctinia solani. All fenugreek plant parts showed antifungal potential and the magnitude of their inhibitory effects was species and plant parts dependent. R extract was shown less toxic (30.38%), whereas NGS extract expressed the strongest inhibition, with an average of 71.44%, followed by GS (58.56%) and LS (57.1%). Screening indicated that P. aphanidermatum was the most resistant species, with an average inhibition of 34.5%. E graminearum, Alternaria sp. and R. solani were the most sensitive species, and were similarly inhibited (63.5%). The stability test indicated that the aqueous extracts of all plant parts lost approximately 50% of their relative activity after one month of storage at 4℃, whilst they lost 60%-90% of their activity when stored at ambient temperature for one month. The antifungal activity resided mainly in the methanol fraction and the minimum inhibitory concentration (MIC) of methanol fraction witch caused total inhibition of R. solani and Alternaria sp. was 60 μg/ml. Results of current study suggested that the constituents of Trigonella foenum-graecum have potential against harmful pathogenic fungi. Therefore, fenugreek could be an important source of biologically active compounds useful for developing better new antifungal drugs.

  5. Oral infusion of pomegranate fruit extract inhibits prostate carcinogenesis in the TRAMP model

    OpenAIRE

    Adhami, Vaqar Mustafa; Siddiqui, Imtiaz Ahmad; Syed, Deeba N.; Lall, Rahul Kumar; Mukhtar, Hasan

    2011-01-01

    We earlier provided evidence that oral consumption of pomegranate fruit extract (PFE) inhibits prostate cancer (PCa) cell growth in nude mice. To ascertain convincing evidence of chemopreventive effects of PFE against PCa, its efficacy requires to be evaluated in animal models that closely emulate human disease. Here, we provide evidence of remarkable tumor growth inhibitory effects of PFE using the TRAMP model. Mice received 0.1 and 0.2% PFE, equivalent to 250 and 500 ml of pomegranate juice...

  6. Oral infusion of pomegranate fruit extract inhibits prostate carcinogenesis in the TRAMP model

    OpenAIRE

    Adhami, Vaqar Mustafa; Siddiqui, Imtiaz Ahmad; Syed, Deeba N.; Lall, Rahul Kumar; Mukhtar, Hasan

    2011-01-01

    We earlier provided evidence that oral consumption of pomegranate fruit extract (PFE) inhibits prostate cancer (PCa) cell growth in nude mice. To ascertain convincing evidence of chemopreventive effects of PFE against PCa, its efficacy requires to be evaluated in animal models that closely emulate human disease. Here, we provide evidence of remarkable tumor growth inhibitory effects of PFE using the TRAMP model. Mice received 0.1 and 0.2% PFE, equivalent to 250 and 500 ml of pomegranate juice...

  7. Effect of black raspberry extract in inhibiting NFkappa B dependent radioprotection in human breast cancer cells.

    Science.gov (United States)

    Madhusoodhanan, Rakhesh; Natarajan, Mohan; Singh, Jamunarani Veeraraghavan Nisha; Jamgade, Ambarish; Awasthi, Vibhudutta; Anant, Shrikant; Herman, Terence S; Aravindan, Natarajan

    2010-01-01

    Black raspberry extracts (RSE) have been shown to inhibit cancer cell growth and stimulate apoptosis. Also, studies have demonstrated that RSE inhibits transcriptional regulators including NFkappa B. Accordingly, we investigated the effect of RSE in inhibiting radiation (IR) induced NFkappa B mediated radioprotection in breast adenocarcinoma cells. MCF-7 cells were exposed to IR (2Gy), treated with RSE (0.5, 1.0, 2.0 micro g/ml) or treated with RSE (1.0 micro g/ml) followed by IR exposure, and harvested after 1, 3, 6, 24, 48, and 72 h. NFkappa B DNA-binding activity was measured by EMSA and phosphorylated Ikappa Balpha by immunoblotting. Expression of IAP1, IAP2, XIAP and survivin were measured by QPCR and immunoblotting. Cell survival was measured using MTT assay and cell death using Caspase-3/7 activity. Effect of RSE on IR induced MnSOD, TNFalpha, IL-1alpha and MnSOD activity was also determined. RSE inhibited NFkappa B activity in a dose-dependent manner. Also, RSE inhibited IR-induced sustained activation of NFkappa B, and NFkappa B regulated IAP1, IAP2, XIAP, and survivin. In addition, RSE inhibited IR-induced TNFalpha, IL-1alpha, and MnSOD levels and MnSOD activity. RSE suppressed cell survival and enhanced cell death. These results suggest that RSE may act as a potent radiosensitizer by overcoming the effects of NFkappa B mediated radioprotection in human breast cancer cells.

  8. [Diagnostic significance of the spinal-brain stem polysynaptic reflex and the period of inhibition].

    Science.gov (United States)

    Ivanichev, G A

    1985-01-01

    Electrical stimulation of the radial nerve associated with voluntary contraction of the shoulder girdle inhibited bioelectrical activity not only in the muscles of the hypothenar but also in the proximal muscles. In resting muscles, such stimulation elicited a reflex response with a large latent period. With weak voluntary tension stimulation elicited a reflex response while in the presence of considerable contraction the reflex response merged with bioelectrical activity, with a clearly demonstrable subsequent period of inhibition. The current viewpoint about the antidromal blockade of the segmental motoneurons is debated. It is suggested that the polysynaptic reflex and the inhibition period are connected with the same level of realization -- the oral portions of the brain stem.

  9. Immobilization of Tyrosinase from Avocado Crude Extract in Polypyrrole Films for Inhibitive Detection of Benzoic Acid

    Directory of Open Access Journals (Sweden)

    André Brisolari

    2014-07-01

    Full Text Available Inhibition-based biosensors were developed by immobilizing tyrosinase (Tyr, polyphenol oxidase from the crude extract of avocado fruit on electrochemically prepared polypyrrole (PPy films. The biosensors were prepared during the electropolymerization of pyrrole in a solution containing a fixed volume of the crude extract of avocado. The dependence of the biosensor responses on the volume used from the crude extract, values of pH and temperature was studied, and a substrate, catechol, at different concentrations, was amperometrically detected by these biosensors. Benzoic acid, a competitive inhibitor of Try, was added to the catechol solutions at specific concentrations aimed at obtaining the inhibition constant, K’m, which ranged from 1.7 to 4.6 mmol∙L−1 for 0.0 and 60 µmol∙L−1 of benzoic acid, respectively. Studies on the inhibition caused by benzoic acid by using PPy/Try films, and catechol as a substrate, allowed us propose how to develop, under optimized conditions, simple and low-cost biosensors based on the use of avocado fruit.

  10. Extract of feverfew inhibits interactions of human platelets with collagen substrates

    Energy Technology Data Exchange (ETDEWEB)

    Loesche, W.M.; Mazurov, A.V.; Heptinstall, S.; Groenewegen, W.A.; Repin, V.S.; Till, U.

    1987-12-01

    The interaction of platelets with surfaces coated with collagens of type III (C III) or IV (C IV) has been studied by measuring the deposition of /sup 51/Cr-labeled platelets and by scanning electron microscopy (SEM). Experiments were performed using platelet-rich plasma (PRP) and suspensions of gel-filtered platelets (GFP). Platelets were deposited on C III mainly as surface-bound aggregates. In contrast they were deposited on C IV mainly as spread forms of individual cells. Formation of aggregates on C III was more extensive for PRP than for GFP; in contrast platelet spreading on C IV was more extensive for GFP than for PRP. The effects of an extract of the plant feverfew on platelet-collagen interactions were determined. Feverfew extract inhibited the deposition of /sup 51/Cr-labeled platelets on both C III and C IV in a dose-dependent way. Similar concentrations of extract were needed to inhibit the formation of surface-bound aggregates and to inhibit platelet spreading in both PRP and GFP.

  11. Grape extracts inhibit multiple events in the cell biology of cholera intoxication.

    Directory of Open Access Journals (Sweden)

    Srikar Reddy

    Full Text Available Vibrio cholerae produces cholera toxin (CT, an AB5 protein toxin that is primarily responsible for the profuse watery diarrhea of cholera. CT is secreted into the extracellular milieu, but the toxin attacks its Gsα target within the cytosol of a host cell. Thus, CT must cross a cellular membrane barrier in order to function. This event only occurs after the toxin travels by retrograde vesicular transport from the cell surface to the endoplasmic reticulum (ER. The catalytic A1 polypeptide then dissociates from the rest of the toxin and assumes an unfolded conformation that facilitates its transfer to the cytosol by a process involving the quality control system of ER-associated degradation. Productive intoxication is blocked by alterations to the vesicular transport of CT and/or the ER-to-cytosol translocation of CTA1. Various plant compounds have been reported to inhibit the cytopathic activity of CT, so in this work we evaluated the potential anti-CT properties of grape extract. Two grape extracts currently sold as nutritional supplements inhibited CT and Escherichia coli heat-labile toxin activity against cultured cells and intestinal loops. CT intoxication was blocked even when the extracts were added an hour after the initial toxin exposure. A specific subset of host-toxin interactions involving both the catalytic CTA1 subunit and the cell-binding CTB pentamer were affected. The extracts blocked toxin binding to the cell surface, prevented unfolding of the isolated CTA1 subunit, inhibited CTA1 translocation to the cytosol, and disrupted the catalytic activity of CTA1. Grape extract could thus potentially serve as a novel therapeutic to prevent or possibly treat cholera.

  12. Effect of Morinda Tinctoria Leaves Extract on the Corrosion Inhibition of Mild Steel in Acid Medium

    Institute of Scientific and Technical Information of China (English)

    K.Krishnaveni; J.Ravichandran; A.Selvaraj

    2013-01-01

    The Morinda tinctoria (MT) plant leaves extract was prepared in aqueous and hydrochloric acid media and was used as corrosion inhibitor for mild steel in hydrochloric acid medium.MT is found to be an efficient inhibitor at room temperature and the efficiency decreases with increase in temperature.Results from colorimetric studies predict the amount of iron present in the test solution and the percentage inhibition efficiency values calculated from this data fit well with the weight loss experiments.The AC impedance studies reveal that the mild steel surface is positively charged and the process of inhibition is through charge transfer.Polarisation studies indicate the mixed nature of the inhibitor.Thermodynamic parameters obtained predict that the process of inhibition is a spontaneous one.

  13. Corrosion Inhibition of Mild Steel in Citric Acid by Aqueous Extract of Piper Nigrum L.

    Directory of Open Access Journals (Sweden)

    P. Matheswaran

    2012-01-01

    Full Text Available The inhibition efficiency (IE of an aqueous extract of Piper Nigrum L. in controlling corrosion of mild steel at pH 12 has been evaluated by weight loss method in the absence and presence of inhibitor in citric acid medium at different concentration. The result showed that the corrosion inhibition efficiency of these compounds was found to vary with the different concentration at two hour time interval at room temperature. Also, it was found that the corrosion inhibition behaviour of Piper Nigrum L. is greater in 2 N Citric acid than 1 N Citric acid medium. So Piper Nigrum L. can be used has a good inhibitor for preventing mild steel material which is used in many construction purpose.

  14. Kinetics of acetylcholinesterase inhibition by an aqueous extract of Cuminum cyminum seeds

    Directory of Open Access Journals (Sweden)

    Suresh Kumar

    2014-03-01

    Full Text Available The cholinergic hypothesis of Alzheimer’s disease (AD has provided the rationale for the current pharmacotherapy of this disease. Acetylcholinesterase (AChE inhibitors are currently the only approved therapy for the symptomatic treatment of AD. The current drugs available in the market has shown various side effect which prompted scientist to search for new and potent AChE inhibitors which exerts minimal side effect in AD patient. In present study, an aqueous extract of Cumin cyminum was tested for in vitro acetylcholinesterase inhibitory activity based on Ellman’s method. C. cyminum showed maximum inhibition of 76.90±0.003% in an aqueous extract at 50μg/ml final concentration. Further studies were conducted to elucidate the mode of AChE inhibition by kinetic studies. Competitive inhibition was observed at lower concentrations (12.5μg/ml & 25μg/ml and mixed inhibition was observed at higher concentrations (50μg/ml & 100μg/ml.

  15. Akt- and CREB-Mediated Prostate Cancer Cell Proliferation Inhibition by Nexrutine, a Phellodendron amurense Extract

    Directory of Open Access Journals (Sweden)

    Gretchen E. Garcia

    2006-06-01

    Full Text Available Evidence from epidemiological studies suggests that plant-based diets can reduce the risk of prostate cancer. However, very little information is available concerning the use of botanicals in preventing prostate cancer. As a first step toward developing botanicals as prostate cancer preventives, we examined the effect of Nexrutine on human prostate cancer cells. Nexrutine is a herbal extract developed from Phellodendron amurense. Phellodendron extracts have been used traditionally in Chinese medicine for hundreds of years as an antidiarrheal, astringent, and anti-inflammatory agent. The present study investigated its potential antitumor effect on human prostate cancer cells. Our results suggest that it inhibits tumor cell proliferation through apoptosis induction and inhibition of cell survival signaling. The results of the present study indicate that Nexrutine treatment 1 inhibits the proliferation of both androgenresponsive and androgen-independent human prostate cancer cells through induction of apoptosis; 2 reduces levels of pAkt, phosphorylated cAMP response-binding protein (pCREB, and CREB DNA-binding activity; and 3 induces apoptosis in prostate cancer cells stably overexpressing Bcl-2. Further Akt kinase activity was reduced in cells treated with Nexrutine, and ectopic expression of myristoylated Akt protected from Nexrutine induced inhibition of proliferation, implicating a role for Akt signaling.

  16. Corrosion Inhibition and Adsorption Properties of Ethanolic Extract of Calotropis for Corrosion of Aluminium in Acidic Media

    OpenAIRE

    Sudesh Kumar; Suraj Prakash Mathur

    2013-01-01

    The corrosion inhibition of aluminium in sulfuric acid solution in the presence of different plant parts, namely, leaves, latex, and fruit was studied using weight loss method and thermometric method. The ethanolic extracts of Calotropis procera and Calotropis gigantea act as an inhibitor in the acid environment. The inhibition efficiency increases with increase in inhibitor concentration. The plant parts inhibit aluminium, and inhibition is attributed, due to the adsorption of the plant part...

  17. Prepulse inhibition (PPI) disrupting effects of Glycyrrhiza glabra extract in mice: a possible role of monoamines.

    Science.gov (United States)

    Michel, Haidy E; Tadros, Mariane G; Abdel-Naim, Ashraf B; Khalifa, Amani E

    2013-06-07

    Liquorice extract was reported to have nootropic and/or antiamnestic effects. Prepulse inhibition (PPI) of startle response is a multimodal, cross-species phenomenon used as a measure of sensorimotor gating. Previous studies indicated that liquorice/its constituents augmented mouse brain monoamine levels. Increased brain monoamines' transmission was suggested to underlie PPI disruption. However, the effect of antiamnestic dose(s) of the extract on PPI has not been investigated despite the coexistence of impaired memory and PPI deficit in some neurological disorders. The effect of administration of the antiamnestic dose of the extract (150 mg/kg for 7 days) was tested on PPI of acoustic startle response in mice. It resulted in PPI disruption and therefore its effect on monoamines' levels was investigated in a number of mouse brain areas involved in PPI response mediation. Results demonstrated that the extract antiamnestic dose augmented cortical, hippocampal and striatal monoamine levels. It was therefore concluded that liquorice extract (150 mg/kg)-induced PPI deficit was mediated through augmenting monoaminergic transmission in the cortex, hippocampus and striatum. These findings can be further investigated in experimental models for autism, psychosis and Huntington's disease to decide the safety of using liquorice extract in ameliorating memory disturbance in disorders manifesting PPI deficit.

  18. Corrosion inhibition of steel in sulfuric acidic solution by the Chenopodium Ambrosioides Extracts

    Directory of Open Access Journals (Sweden)

    L. Bammou

    2014-10-01

    Full Text Available The influence of natural occurring extract of Chenopodium Ambrosioides (CAE on the corrosion inhibition of carbon steel in sulfuric acid solution is studied by the weight loss method, potentiodynamic polarization and impedance spectroscopy (EIS measurements. The experimental results reveal that extract has a good inhibiting effect on the metal tested in 0.5 M H2SO4 solution. The protection efficiency increases with increasing inhibitor concentration to attain 94% at 4 g/l. Potentiodynamic polarization studies clearly reveal that it acts essentially as a cathodic inhibitor. EIS results show that the change in the impedance parameters (Rt and Cdl with concentration of extract of Chenopodium Ambrosioides is indicative of the adsorption of molecules leading to the formation of a protective layer on the surface of carbon steel. The efficiency decreases with temperature. The adsorption of Chenopodium Ambrosioides extract is found to obey the Langmuir adsorption isotherm. The activation energies and enthalpies of the corrosion process of carbon steel in acidic medium were determined.

  19. Inhibition of human P450 enzymes by natural extracts used in traditional medicine.

    Science.gov (United States)

    Rodeiro, Idania; Donato, María T; Jimenez, Nuria; Garrido, Gabino; Molina-Torres, Jorge; Menendez, Roberto; Castell, José V; Gómez-Lechón, María J

    2009-02-01

    Different medicinal plants are widely used in Cuba and Mexico to treat several disorders. This paper reports in vitro inhibitory effects on the P450 system of herbal products commonly used by people in Cuba and Mexico in traditional medicine for decades. Experiments were conducted in human liver microsomes. The catalytic activities of CYP1A1/2, 2D6, and 3A4 were measured using specific probe substrates. The Heliopsis longipes extract exhibited a concentration-dependent inhibition of the three enzymes, and similar effects were produced by affinin (an alkamide isolated from the H. longipes extract) and two catalytically reduced alkamides. Mangifera indica L. and Thalassia testudinum extracts, two natural polyphenol-rich extracts, diminished CYP1A1/2 and 3A4 activities, but not the CYP2D6 activity. These results suggest that these herbs inhibit the major human P450 enzymes involved in drug metabolism and could induce potential herbal-drug interactions.

  20. Acetylcholinesterase inhibition, antioxidant activity and toxicity of Peumus boldus water extracts on HeLa and Caco-2 cell lines.

    Science.gov (United States)

    Falé, P L; Amaral, F; Amorim Madeira, P J; Sousa Silva, M; Florêncio, M H; Frazão, F N; Serralheiro, M L M

    2012-08-01

    This work aimed to study the inhibition on acetylcholinesterase activity (AChE), the antioxidant activity and the toxicity towards Caco-2 and HeLa cells of aqueous extracts of Peumus Boldus. An IC(50) value of 0.93 mg/mL, for AChE inhibition, and EC(50) of 18.7 μg/mL, for the antioxidant activity, was determined. This activity can be attributed to glycosylated flavonoid derivatives detected, which were the main compounds, although boldine and other aporphine derivatives were also present. No changes in the chemical composition or the biochemical activities were found after gastrointestinal digestion. Toxicity of P. boldus decoction gave an IC(50) value 0.66 mg/mL for HeLa cells, which caused significant changes in the cell proteome profile. Copyright © 2012 Elsevier Ltd. All rights reserved.

  1. In vitro antibacterial, alpha-amylase inhibition potential of three nudibranchs extracts from South East coast of India

    Institute of Scientific and Technical Information of China (English)

    Giji Sadhasivam; Arumugam Muthuvel; Wanjale Mrunal Vitthal; Abirami Pachaiyappan; Mohan Kumar; Balasubramanian Thangavel

    2013-01-01

    Objective: To study the antibacterial and antiamylase properties of methanol and acetone extracts of nudibranchs including Bursatella leachii (B. leachii), Kalinga ornata (K. ornata),Aplysia sp. Methods: Crude methanol and acetone extracts of sea slugs were tested for inhibition of fish bacterial pathogens' growth through disc diffusion method. The activity was measured based on the formation of inhibition zone around the disc impregnated with crude extracts. The α-amylase inhibitory effect was also measured calorimetrically. The chemical fingerprinting of the extract was recorded with HPTLC and GC-MS. Results: The solvent extracts of all the three sea slugs showed antibacterial property. The maximum zone of inhibition (>15-20 mm) was recorded for methanol and acetone extracts of K.ornata. The methanol extract of Aplysia sp. exhibited 93% inhibition against α-amylase, following by B. leachii (methanol) 70.6% and K. ornata (methanol) 49.03% inhibition respectively. The acetone extracts didn' t show any notable inhibition. The presence of free amino acids like lysine, aspartic acid, glutamic acid, arginine etc., terpenoids and pigents were confirmed through HPTLC analysis. The presence of siloxanes and propanoic acid were also revealed through GC-MS. Conclusions: This study suggests that further scrutinisation of the B. leachii, K. ornata and Aplysia sp. will pave the way for development of antibacterial and α-amylase inhibitory agent for therapeutic application.

  2. In vitro antibacterial, alpha-amylase inhibition potential of three nudibranchs extracts from South East coast of India

    Directory of Open Access Journals (Sweden)

    Giji Sadhasivam

    2013-10-01

    Full Text Available Objective: To study the antibacterial and antiamylase properties of methanol and acetone extracts of nudibranchs including Bursatella leachii (B. leachii, Kalinga ornata (K. ornata, Aplysia sp. Methods: Crude methanol and acetone extracts of sea slugs were tested for inhibition of fish bacterial pathogens' growth through disc diffusion method. The activity was measured based on the formation of inhibition zone around the disc impregnated with crude extracts. The α-amylase inhibitory effect was also measured calorimetrically. The chemical fingerprinting of the extract was recorded with HPTLC and GC-MS. Results: The solvent extracts of all the three sea slugs showed antibacterial property. The maximum zone of inhibition (>15-20 mm was recorded for methanol and acetone extracts of K. ornata. The methanol extract of Aplysia sp. exhibited 93% inhibition against α-amylase, following by B. leachii (methanol 70.6% and K. ornata (methanol 49.03% inhibition respectively. The acetone extracts didn' t show any notable inhibition. The presence of free amino acids like lysine, aspartic acid, glutamic acid, arginine etc., terpenoids and pigents were confirmed through HPTLC analysis. The presence of siloxanes and propanoic acid were also revealed through GC-MS. Conclusions: This study suggests that further scrutinisation of the B. leachii, K. ornata and Aplysia sp. will pave the way for development of antibacterial and α-amylase inhibitory agent for therapeutic application.

  3. Standardized Kaempferia parviflora Extract Inhibits Intrinsic Aging Process in Human Dermal Fibroblasts and Hairless Mice by Inhibiting Cellular Senescence and Mitochondrial Dysfunction

    Directory of Open Access Journals (Sweden)

    Ji-Eun Park

    2017-01-01

    Full Text Available Intrinsic skin aging is a complex biological phenomenon mainly caused by cellular senescence and mitochondrial dysfunction. This study evaluated the inhibitory effect of Kaempferia parviflora Wall ex. Baker ethanol extract (KPE on H2O2-stimulated cellular senescence and mitochondrial dysfunction both in vitro and in vivo. KPE significantly increased cell growth and suppressed senescence-associated β-galactosidase activation. KPE inhibited the expression of cell-cycle inhibitors (p53, p21, p16, and pRb and stimulated the expression of cell-cycle activators (E2F1 and E2F2. H2O2-induced hyperactivation of the phosphatidylinositol 3-kinase/protein kinase B (AKT signaling pathway was suppressed by KPE through regulated expression of forkhead box O3a (FoxO3a and mammalian target of rapamycin (mTOR. KPE attenuated inflammatory mediators (interleukin-6 (IL-6, IL-8, nuclear factor kappa B (NF-κB, and cyclooxygenase-2 (COX-2 and increased the mRNA expression of PGC-1α, ERRα, NRF1, and Tfam, which modulate mitochondrial biogenesis and function. Consequently, reduced ATP levels and increased ROS level were also reversed by KPE treatment. In hairless mice, KPE inhibited wrinkle formation, skin atrophy, and loss of elasticity by increasing the collagen and elastic fibers. The results indicate that KPE prevents intrinsic aging process in hairless mice by inhibiting cellular senescence and mitochondrial dysfunction, suggesting its potential as a natural antiaging agent.

  4. Standardized Kaempferia parviflora Extract Inhibits Intrinsic Aging Process in Human Dermal Fibroblasts and Hairless Mice by Inhibiting Cellular Senescence and Mitochondrial Dysfunction.

    Science.gov (United States)

    Park, Ji-Eun; Woo, Seon Wook; Kim, Mi-Bo; Kim, Changhee; Hwang, Jae-Kwan

    2017-01-01

    Intrinsic skin aging is a complex biological phenomenon mainly caused by cellular senescence and mitochondrial dysfunction. This study evaluated the inhibitory effect of Kaempferia parviflora Wall ex. Baker ethanol extract (KPE) on H2O2-stimulated cellular senescence and mitochondrial dysfunction both in vitro and in vivo. KPE significantly increased cell growth and suppressed senescence-associated β-galactosidase activation. KPE inhibited the expression of cell-cycle inhibitors (p53, p21, p16, and pRb) and stimulated the expression of cell-cycle activators (E2F1 and E2F2). H2O2-induced hyperactivation of the phosphatidylinositol 3-kinase/protein kinase B (AKT) signaling pathway was suppressed by KPE through regulated expression of forkhead box O3a (FoxO3a) and mammalian target of rapamycin (mTOR). KPE attenuated inflammatory mediators (interleukin-6 (IL-6), IL-8, nuclear factor kappa B (NF-κB), and cyclooxygenase-2 (COX-2)) and increased the mRNA expression of PGC-1α, ERRα, NRF1, and Tfam, which modulate mitochondrial biogenesis and function. Consequently, reduced ATP levels and increased ROS level were also reversed by KPE treatment. In hairless mice, KPE inhibited wrinkle formation, skin atrophy, and loss of elasticity by increasing the collagen and elastic fibers. The results indicate that KPE prevents intrinsic aging process in hairless mice by inhibiting cellular senescence and mitochondrial dysfunction, suggesting its potential as a natural antiaging agent.

  5. Red Pepper (Capsicum baccatum) Extracts Present Anti-Inflammatory Effects In Vivo and Inhibit the Production of TNF-α and NO In Vitro.

    Science.gov (United States)

    Allemand, Alexandra; Leonardi, Bianca Franco; Zimmer, Aline Rigon; Moreno, Susana; Romão, Pedro Roosevelt Torres; Gosmann, Grace

    2016-08-01

    Capsicum baccatum is the most consumed red pepper species in Brazil. Our previous studies demonstrated the anti-inflammatory properties of its crude extract, whose activity is yet to be fully characterized. Herein, we examined the anti-inflammatory in vivo effects of enriched extracts obtained through bioguided fractionation as dichloromethane (DCM), butanol (BUT), and residual aqueous (RAq) extracts and its influence on inflammatory mediators produced by macrophages in vitro. We demonstrated that all C. baccatum extracts presented anti-inflammatory activity in vivo. In addition, we showed that BUT and RAq were more effective in inhibiting the neutrophil migration induced by carrageenan (Cg) to peritoneal cavity and both extracts inhibited paw edema induced by Cg, prostaglandin E2, and histamine in mice. Furthermore, the pretreatment with C. baccatum extracts significantly reduced the levels of myeloperoxidase (MPO) in the paw tissues of mice compared with the carrageenan group. Once again, RAq and BUT caused the greatest reduction in MPO levels. Moreover, it was demonstrated for the first time that C. baccatum inhibited the nitric oxide and tumor necrosis factor-alpha production by lipopolysaccharide/interferon gamma (IFN-γ)-stimulated macrophages. These anti-inflammatory effects seem to be at least, in part, independent of capsaicin. Hence, red pepper has bioactive compounds and might be used to develop food-derived extracts to treat related inflammatory diseases.

  6. Crocus sativus stigma extract and its major constituent crocin possess significant antiproliferative properties against human prostate cancer.

    Science.gov (United States)

    D'Alessandro, Anna M; Mancini, Andrea; Lizzi, Anna Rita; De Simone, Angela; Marroccella, Carmine Esposito; Gravina, Giovanni Luca; Tatone, Carla; Festuccia, Claudio

    2013-01-01

    In this study, we investigated the antiproliferative effects of saffron extract (SE) and its major constituent crocin on 5 different malignant and 2 nonmalignant prostate cancer cell lines. Using high performance liquid chromatography (HPLC), the purity and content of crocin were determined. All cells were incubated with different concentrations of SE or crocin for 48 h. Cell cycle and apoptosis were also evaluated. In a time- and concentration-dependent manner, both SE and crocin reduced cell proliferation in all malignant cell lines with IC50 values ranging between 0.4 and 4 mg/ml for SE and between 0.26 and 0.95 mM/ml for crocin. Nonmalignant cells were not affected. Flow cytometry profiles revealed that most cells were arrested at G0/G1 phase with a significant presence of apoptotic cells. Western blot analysis revealed that the expression of Bcl-2 was strikingly downregulated, whereas Bax was upregulated. Analysis of caspase activity indicated a caspase-dependent pathway with involvement of caspase-9 activation, suggesting an intrinsic pathway. Based on these findings, it can be concluded that both SE and crocin can inhibit cell proliferation, arrest cell cycle progression, inducing apoptosis in prostate cancer. Consequently, these agents could potentially be used as a chemopreventive as well as a chemotherapeutic agent for prostate cancer management.

  7. Helichrysum and grapefruit extracts inhibit carbohydrate digestion and absorption, improving postprandial glucose levels and hyperinsulinemia in rats.

    Science.gov (United States)

    de la Garza, Ana Laura; Etxeberria, Usune; Lostao, María Pilar; San Román, Belén; Barrenetxe, Jaione; Martínez, J Alfredo; Milagro, Fermín I

    2013-12-11

    Several plant extracts rich in flavonoids have been reported to improve hyperglycemia by inhibiting digestive enzyme activities and SGLT1-mediated glucose uptake. In this study, helichrysum ( Helichrysum italicum ) and grapefruit ( Citrus × paradisi ) extracts inhibited in vitro enzyme activities. The helichrysum extract showed higher inhibitory activity of α-glucosidase (IC50 = 0.19 mg/mL) than α-amylase (IC50 = 0.83 mg/mL), whereas the grapefruit extract presented similar α-amylase and α-glucosidase inhibitory activities (IC50 = 0.42 mg/mL and IC50 = 0.41 mg/mL, respectively). Both extracts reduced maltose digestion in noneverted intestinal sacs (57% with helichrysum and 46% with grapefruit). Likewise, both extracts inhibited SGLT1-mediated methylglucoside uptake in Caco-2 cells in the presence of Na(+) (56% of inhibition with helichrysum and 54% with grapefruit). In vivo studies demonstrated that helichrysum decreased blood glucose levels after an oral maltose tolerance test (OMTT), and both extracts reduced postprandial glucose levels after the oral starch tolerance test (OSTT). Finally, both extracts improved hyperinsulinemia (31% with helichrysum and 50% with grapefruit) and HOMA index (47% with helichrysum and 54% with grapefruit) in a dietary model of insulin resistance in rats. In summary, helichrysum and grapefruit extracts improve postprandial glycemic control in rats, possibly by inhibiting α-glucosidase and α-amylase enzyme activities and decreasing SGLT1-mediated glucose uptake.

  8. Vellozia flavicans Mart. ex Schult. hydroalcoholic extract inhibits the neuromuscular blockade induced by Bothrops jararacussu venom

    Science.gov (United States)

    2014-01-01

    Background Snakebite is a significant public health issue in tropical countries. In Brazil, some of the most common snake envenomations are from Bothrops. Bothrops bites trigger local and systemic effects including edema, pain, erythema, cyanosis, infections, and necrosis. Vellozia flavicans is a plant from the Brazilian “cerrado” (savanna) that is popularly used as an anti-inflammatory medicine. Since inflammation develops quickly after Bothrops bites, which can lead to infection, the aim of the present study was to observe possible anti-snake venom and antimicrobial activities of V. flavicans (Vf). Methods The chromatographic profile of the main constituents from the Vf leaf hydroalcoholic extract was obtained by thin-layer chromatography (TLC). The anti-snake venom activity was measured by Vf’s ability to neutralize the in vitro neuromuscular blockade caused by Bothrops jararacussu venom (Bjssu) in a mouse phrenic nerve-diaphragm model (PND). After a 20 min incubation, preparations of PND were added to Tyrode’s solution (control); Vf (0.2, 0.5, 1, and 2 mg/mL); 40 μg/mL Bjssu; pre-incubation for 30 min with Bjssu and 1 mg/mL Vf; and a Bjssu pretreated preparation (for 10 min) followed by 1 mg/mL Vf. Myographic recording was performed, and the contractile responses were recorded. The antimicrobial activity (minimum inhibitory concentration [MIC] and minimum bactericidal concentration [MBC]) was obtained for Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, and Enterococcus faecalis, using gentamicin and vancomycin as positive controls. Results TLC analysis yielded several compounds from Vf, such as flavonoids (quercetin) and phenolic acids (chlorogenic acid). Bjssu completely blocked the contractile responses of PND preparations, while Vf preserved 97% (±10%) of the contractile responses when incubated with Bjssu. In the PND pretreated with Bjssu, Vf was able to inhibit the neuromuscular blockade progress. MIC and MBC of Vf ranged

  9. Corrosion Inhibition of Aluminum in 0.5 M HCl by Garlic aqueous extract

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    Saedah R. Al-Mhyawi

    2014-06-01

    Full Text Available The inhibition efficiency of extract of Garlic on aluminium in hydrochloric acid solutions has been evaluated by weight loss techniques. Values of inhibition efficiency obtained are dependent upon the concentration of inhibitor and temperature. Generally, inhibition was found to increase with inhibitor concentration, half-life, activation energy but decrease with temperature and first-order rate constant at the temperatures studied. Physical adsorption mechanism has been proposed for the inhibition and Langmuir , Temkin adsorption isotherm was obeyed. Garlic is an inhibitor of aluminium corrosion in 0.5 M hydrochloric acid solution.The values of standard free energy of adsorption suggest that the adsorption of inhibitor on aluminium surface occurred by physisorption mechanism. the negative sign of the Free Energy of adsorption indicates that the adsorption of the inhibitors on the aluminum surface was a spontaneous process.the negative values of enthalpy of adsorption (ΔH suggest that the chemical reaction involved in the adsorption of the inhibitors on the metal surface is an exothermic process, hence increase in the reaction temperature of the medium will decrease the inhibition efficiency.

  10. Growth Inhibition of Struvite Crystals in the Presence of Herbal Extract Boerhaavia diffusa Linn

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    C. K. Chauhan

    2009-01-01

    Full Text Available Problem statement: The formation of a urinary stone, known as nephrolithiasis, urolithiasis, renal calculi or kidney stone is a serious, debilitating problem in all societies throughout the world. Struvite or Ammonium Magnesium Phosphate Hexahydrate (AMPH is one of the components of urinary stone (calculi. Struvite stones are commonly found in women. Struvites form in humans as a result of urinary tract infection with ureolithic urea splitting micro organisms. These stones can grow rapidly forming "staghorn-calculi", which is more painful urological disorder. Therefore, it is of prime importance to study the growth and inhibition of Struvite crystals. Approach: This in vitro study had been carried out in the presence of herbal extract of Boerhaavia diffusa Linn. by using single diffusion gel growth technique. Sodium metasilicate solution of specific gravity 1.05 and an aqueous solution of ammonium dihydrogen phosphate of 0.5 M concentration were mixed so that the pH value 7.0 could be set. After the gelation, equal amount of supernatant solution of 1.0 M magnesium acetate prepared with 0.5 and 1% concentrations of the herbal extract of B. diffusa Linn. were gently poured on the set gels in the respective test tubes in the aseptic medium. Results: The growth of crystals without and with herbal extracts was monitored at regular time intervals. As the concentration of B. diffusa Linn. increased, the inhibition of crystals also increased in the gel media as well as the dissolution of crystals at the gel-liquid interface increases. The de-fragmentation of some grown crystals was also noticed. Conclusion: The herbal extract of B. diffusa Linn. inhibited the growth of struvite crystals in vitro. This study incorporated multidisciplinary interests and may be used for formulating the strategy for prevention or dissolution of urinary stones.

  11. Bothrops jararacussu venom-induced neuromuscular blockade inhibited by Casearia gossypiosperma Briquet hydroalcoholic extract

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    TM Camargo

    2010-01-01

    Full Text Available The hydroalcoholic extract of Casearia gossypiosperma Briquet (Flacourtiaceae was standardized for the first time through quality control procedures including pharmacognostic methods, fingerprint chromatograms, defined amounts of marker substances and physicochemical characteristics. The pharmacological activity of C. gossypiosperma (Cg hydroalcoholic extract was assayed by a traditional in vitro test, which involved irreversible neuromuscular blockade induced by Bothrops jararacussu (Bjssu venom (60 µg/mL in mouse phrenic nerve-diaphragm preparations. Bjssu venom blocked muscle activity for 26 (± 2.0 minutes (n = 6. Cg extract (0.1 mg/mL induced changes on the baseline muscle activity without impairing the muscle function and inhibited 87.6% (± 1.8 (n = 6 of the Bjssu venom-induced blockade. Both flavonoids (0.624 g% and polyphenols (4.63 g% from the extract were spectrophotometrically quantified. Therefore, the present study confirms the antibothropic activity of Cg extract, supporting the ethnomedical use of Casearia sp. in the treatment of snakebite victims.

  12. Inhibition of Serratia marcescens Smj-11 biofilm formation by Alcaligenes faecalis STN17 crude extract

    Energy Technology Data Exchange (ETDEWEB)

    Lutfi, Zainal; Ahmad, Asmat [School of Biosciences and Biotechnology, Faculty of Science and Technology, Universiti Kebangsaan Malaysia (UKM), 43600 Bangi, Selangor (Malaysia); Usup, Gires [School of Environmental and Natural Resources Sciences, Faculty of Science and Technology, Universiti Kebangsaan Malaysia (UKM), 43600 Bangi, Selangor (Malaysia)

    2014-09-03

    Serratia marcescens biofilms are formed when they are bound to surfaces in aqueous environments. S. marcescens utilizes N-acylhomoserine lactone (AHL) as its quorum sensing signal molecule. The accumulation of AHL indicates the bacteria to produce matrices to form biofilms. Prodigiosin (2-methyl-3-pentyl-6-methoxyprodigiosin), which causes red pigmentation in the colonies, are also produced when the AHL reaches a certain threshold. The Alcaligenes faecalis STN17 crude extract is believed to inhibit quorum sensing in the S. marcescens Smj-11 and, thus, impedes its biofilm formation ability. A. faecalis STN17 was grown in marine broth, and ethyl acetate extraction was carried out. The crude compound of A. faecalis STN17 was diluted at high concentration (0.2-6.4 mg/mL) and was taken to confirm anti-biofilm activity through the crystal violet method in 96-wells plate. Then, the crude extract underwent purification using simple solvents partitioning test to discern the respective compounds that had the anti-biofilm activity under the crystal violet method. The crystal violet test showed that the crude did have anti-biofilm activity on S. marcescens Smj-11, but did not kill the cells. This finding signifies that the suppression of biofilm formation in S. marcescens by A. faecalis STN17 has a strong correlation. The partitioning test showed that A. faecalis STN17 crude extract has several compounds and only the compound(s) in chloroform showed activities. In conclusion, the crude extract of A. faecalis STN17 has the ability to inhibit S. marcescens Smj-11 biofilm formation.

  13. Corrosion inhibition of C38 steel in 1 M hydrochloric acid medium by alkaloids extract from Oxandra asbeckii plant

    Energy Technology Data Exchange (ETDEWEB)

    Lebrini, M. [Laboratoire Materiaux et Molecules en Milieu Amazonien, CNRS 8172-UMR ECOFOG, Campus Trou Biran, Cayenne 97337, French Guiana (France); Robert, F.; Lecante, A. [Laboratoire Materiaux et Molecules en Milieu Amazonien, UAG-UMR ECOFOG, Campus Trou Biran, Cayenne 97337, French Guiana (France); Roos, C., E-mail: christophe.roos@guyane.univ-ag.f [Laboratoire Materiaux et Molecules en Milieu Amazonien, UAG-UMR ECOFOG, Campus Trou Biran, Cayenne 97337, French Guiana (France)

    2011-02-15

    Research highlights: The inhibition effect of alkaloid extract of Oxandra asbeckii plant on the corrosion of C38 steel in 1 M hydrochloric acid solution has been investigated by potentiodynamic polarization and electrochemical impedance spectroscopy (EIS). Oxandra asbeckii extract examined acted as an efficient corrosion inhibitor in 1 M HCl. Polarization studies showed that Oxandra asbeckii extract was a mixed-type inhibitor and its inhibition efficiency increased with the inhibitor concentration. - Abstract: The inhibition effect of alkaloids extract from Oxandra asbeckii plant (OAPE) on the corrosion of C38 steel in 1 M hydrochloric acid solution has been investigated by potentiodynamic polarization and electrochemical impedance spectroscopy (EIS). The corrosion inhibition efficiency increases on increasing plant extracts concentration. Cathodic and anodic polarization curves show that OAPE is a mixed-type inhibitor. The effect of temperature on the corrosion behavior of C38 steel in 1 M HCl with and without addition of plant extract was studied in the temperature range 25-55 {sup o}C. The thermodynamic functions of dissolution and adsorption processes were calculated from experimental polarization data and the interpretation of the results are given. The adsorption of this plant extract on the C38 steel surface obeys the Langmuir adsorption isotherm. Surface analysis (Raman) was also carried out to establish the corrosion inhibitive property of this plant extract in HCl solution.

  14. Sappan Lignum Extract Inhibits Restenosis in the Injured Artery through the Deactivation of Nuclear Factor-κB

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    Guang Long

    2014-08-01

    Full Text Available The aim of the study was to explore whether Sappan Lignum Extract (SLE would inhibit vascular restenosis in injured artery and its inhibitory mechanism by using a balloon-injured rat carotid artery restenosis model. Different doses of SLE were administered to the rats by tube feeding, starting from four days before surgery and continuing twice per day for two weeks after carotid injury. Injured carotid arteries isolated from rats were embedded in paraffin block and tissue sections were stained with H&E to assess restenosis. The Effects of SLE on vascular restenosis, which are involved in smooth muscle cell cycle, NF-κB p65 expression, and Superoxide (O2- production, was assessed by RT-PCR, western blot assay, and immunohistochemistry. The results showed that in a rat carotid model of balloon dilatation injury, SLE significantly reduced the intimal-to-medial area ratio and vascular restenosis after 14 days of the injury. Immunohistochemistry study revealed no inhibited PCNA expression caused by SLE. Rat serum containing Sappan Lignum (RSC was found neither anti-proliferative effect in cultured vascular smooth muscle cells (VSMCs and nor arrest cell cycle progress detected by flow cytometry. RSC remarkably decreased the expression of TNF-α mRNA and protein in cultured VSMCs. Electrophoretic mobility shift assay proved that RSC inhibited the binding of NF-κB to specific DNA sequences in TNF-α treated VSMCs. Western blot pronounced that RSC and N-acetyl-L-cysteine (NAC reduced expression of NF-κB p65 in nuclear extracts in TNF-α treated VSMCs. RSC and NAC also attenuated superoxide anion generation in TNF-α treated VSMCs. In summary, the inhibitory effects of SLE on vascular restenosis may not be mediated through inhibiting vascular cell proliferation, but through inhibiting vascular inflammation instead, which may be attributed to the inhibition of TNF-α and subsequent deactivation of NF-κB, which was in part mediated through inhibiting

  15. Growth inhibition of struvite crystals in the presence of herbal extract Commiphora wightii.

    Science.gov (United States)

    Chauhan, C K; Joshi, M J; Vaidya, A D B

    2009-12-01

    Struvite is one of the components of urinary stone. Large number of people is suffering from urinary stones (calculi) problem all over the globe. These stones can grow rapidly forming "staghorn-calculi", which is more painful urological disorder. Therefore, it is of prime importance to study the growth and inhibition of Struvite crystals. This in vitro study has been carried out in the presence of herbal extract of Commiphora wightii by using single diffusion gel growth technique. Sodium metasilicate solution of specific gravity 1.05 and an aqueous solution of ammonium dihydrogen phosphate of 0.5 M concentration were mixed so that the pH value 7.0 could be set. After the gelation, equal amount of supernatant solutions comprising of pure 1.0 M magnesium acetate as well as the mixtures of magnesium acetate and the herbal extract solutions of 0.5 and 1% concentrations of C. wightii were gently poured on the set gels. From the study of growth and inhibition behavior of Struvite crystals, it was found that C. wightii inhibits the growth of the Struvite. This study incorporates multidisciplinary interests and may be used for formulating the strategy for prevention or dissolution of urinary stones.

  16. Inhibition of human dendritic cell activation by hydroethanolic but not lipophilic extracts of turmeric (Curcuma longa).

    Science.gov (United States)

    Krasovsky, Joseph; Chang, David H; Deng, Gary; Yeung, Simon; Lee, Mavis; Leung, Ping Chung; Cunningham-Rundles, Susanna; Cassileth, Barrie; Dhodapkar, Madhav V

    2009-03-01

    Turmeric has been extensively utilized in Indian and Chinese medicine for its immune-modulatory properties. Dendritic cells (DCs) are antigen-presenting cells specialized to initiate and regulate immunity. The ability of DCs to initiate immunity is linked to their activation status. The effects of turmeric on human DCs have not been studied. Here we show that hydroethanolic (HEE) but not lipophilic "supercritical" extraction (SCE) of turmeric inhibits the activation of human DCs in response to inflammatory cytokines. Treatment of DCs with HEE also inhibits the ability of DCs to stimulate the mixed lymphocyte reaction (MLR). Importantly, the lipophilic fraction does not synergize with the hydroethanolic fraction for the ability of inhibiting DC maturation. Rather, culturing of DCs with the combination of HEE and SCE leads to partial abrogation of the effects of HEE on the MLR initiated by DCs. These data provide a mechanism for the anti-inflammatory properties of turmeric. However, they suggest that these extracts are not synergistic and may contain components with mutually antagonistic effects on human DCs. Harnessing the immune effects of turmeric may benefit from specifically targeting the active fractions.

  17. Interleukin-1beta inhibits paw oedema induced by local administration of latex of Calotropis procera extracts.

    Science.gov (United States)

    Arya, Soneera; Kumar, Vijay L

    2004-01-01

    Interleukin-1beta (IL-1beta), a pro-inflammatory cytokine, has been reported to exhibit anti-inflammatory properties in the carrageenan-induced paw oedema model. In the present study, we have evaluated the anti-inflammatory activity of IL-1beta against inflammation induced by local administration of the methanol extract of dried latex of Calotropis procera (MeDL) and compared it with that against carrageenan. The anti-inflammatory activity of standard anti-inflammatory drugs, phenylbutazone (PBZ) and dexamethasone (DEX), was also evaluated against both inflammagens. Injection of an aqueous solution of dried latex and MeDL into the sub-plantar surface of the rat paw produced intense inflammation with a peak response occurring within 2 h, while the peak inflammatory response with carrageenan was obtained at 3 h. Subcutaneous injection of IL-1beta was found to be more effective against the inflammatory response elicited by carrageenan (70% inhibition) as compared to MeDL (50% inhibition) at 20microg/kg dose. On the other hand, PBZ effectively inhibited the inflammatory response elicited by both MeDL and carrageenan, while DEX was more effective against carrageenan. Thus, our study indicates that the difference in the anti-inflammatory effect of IL-1beta against latex of C. procera extract and carrageenan is due to the release of different mediators released by these inflammagens.

  18. Effects of tanshinone nanoemulsion and extract on inhibition of lung cancer cells A549

    Science.gov (United States)

    Lee, W. D.; Liang, Y. J.; Chen, B. H.

    2016-12-01

    Danshen (Salvia miltiorrhiza), a Chinese medicinal herb, consists of several functional components including tanshinones responsible for prevention of several chronic diseases. This study intends to prepare tanshinone extract and nanoemulsion from danshen and determine their inhibition effect on lung cancer cells A549. A highly stable tanshinone nanoemulsion composed of Capryol 90, Tween 80, ethanol and deionized water with the mean particle size of 14.2 nm was successfully prepared. Tanshinone nanoemulsion was found to be more effective in inhibiting A549 proliferation than tanshinone extract. Both nanoemulsion and extract could penetrate into cytoplasm through endocytosis, with the former being more susceptible than the latter. A dose-dependent response in up-regulation of p-JNK, p53 and p21 and down-regulation of CDK2, cyclin D1 and cyclin E1 expressions was observed with the cell cycle arrested at G0/G1 phase. The cellular microcompartment change of A549 was also investigated. The study demonstrated that tanshinone nanoemulsion may be used as a botanic drug for treatment of lung cancer.

  19. Corrosion inhibition and adsorption characteristics of Tridax Procumbens L leaves extract on mild steel immersed in 1M HCl solution

    Directory of Open Access Journals (Sweden)

    Kenneth Kanayo ALANEME

    2016-12-01

    Full Text Available The corrosion inhibition and adsorption mechanism of Tridax procumbens Linn leaves extract on mild steel immersed in 1M HCl solution was investigated. Mass loss, corrosion rate and inhibition efficiency from gravimetric and potentiodynamic polarization measurements, atomic adsorption spectroscopy (AAS, Fourier transform infra red spectroscopy (FTIR, and scanning electron microscopy; were used for the analysis. The results show that within the selected range of concentration of the extract and corrosion test temperatures, the inhibition efficiency obtained was within the range of 81 and 96 %. The efficiency values were observed to increase with increase in the extract concentration but decreased slightly with increase in temperature. The inhibitor molecules were noted to be physically adsorbed on the mild steel surface with OH, NH, and CO groups confirmed as the active phytochemical constituents in the extract responsible for the adsorption. The adsorption process fitted perfectly with the Langmuir adsorption isotherm indicating that the extract was strongly adsorbed on the mild steel surface.

  20. Edema induced by Bothrops asper (Squamata: Viperidae) snake venom and its inhibition by Costa Rican plant extracts.

    Science.gov (United States)

    Badilla, Beatriz; Chaves, Fernando; Mora, Gerardo; Poveda, Luis J

    2006-06-01

    We tested the capacity of leaf (Urera baccifera, Loasa speciosa, Urtica leptuphylla, Chaptalia nutans, and Satureja viminea) and root (Uncaria tomentosa) extracts to inhibit edema induced by Bothrops asper snake venom. Edema-forming activity was studied plethysmographically in the rat hind paw model. Groups of rats were injected intraperitoneally with various doses of each extract and, one hour later, venom was injected subcutaneously in the right hind paw. Edema was assessed at various time intervals. The edematogenic activity was inhibited in those animals that received an injection U. tomentosa, C. nutans or L. speciosa extract. The extract of U. baccifera showed a slight inhibition of the venom effect. Extract from S. viminea and, to a lesser extent that of U. leptuphylla, induced a pro-inflammatory effect, increasing the edema at doses of 250 mg/kg at one and two hours.

  1. Inhibition of human platelet aggregation in vitro by standardized extract of Wendtia calycina

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    Milagros Garcia Mesa

    2011-10-01

    Full Text Available Wendtia calycina (Griseb. Griseb., Vivianiaceae, is a Paraguayan herbaceous plant commonly known as burrito. Our previous study indicated that burrito leaves are a very good source of phenylpropanoid glycosides, principally verbascoside. From W. calycina leaves, a standardized, water-soluble extract rich in phenylpropanoid glycosides (WSE has been developed on an industrial scale to be used as a food supplement, cosmetic, phytomedicine, and ingredient of different formulations. In this study, we investigated the effect of the WSE on human platelet aggregation in vitro induced by adenosine diphosphate (ADP, epinephrine (EPN, collagen (COL or arachidonic acid (AA. WSE, concentration-dependently, inhibited ADP and EP-induced human platelet aggregation (IC50 were 0.82±0.15 mg/mL and 0.41±0.02 mg/mL, respectively. It did not inhibit collagen-induced platelet aggregation, thus suggesting a selectivity for the ADP-induced platelet activation pathways.

  2. Study of the inhibition effect of ethanolic extract of mangosteen pericarp on atherogenesis in hypercholesterolemic rat

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    Titin Andri Wihastuti

    2015-10-01

    Full Text Available Objective: To investigate the effect of ethanolic extract of mangosteen pericarp (EEMP through lipid profile, H2O2, nuclear factor-kappa B (NF-κB, inducible nitric oxide synthase (iNOS and endothelial nitric oxide synthase (eNOS measurement in hypercholesterolemic rat. Methods: A total of 20 rats were used in true laboratory experiment which were divided into 5 groups (n = 4 using posttest-only design. There were a normal diet group, a hypercholesterol diet (HCD group, a group that was given HCD with EEMP 200 mg/kg body weight, a group that was given HCD with 400 mg/kg body weight and a group that was given HCD with 800 mg/kg body weight. The lipid profile was measured using Cobas Mira. On the other hand, H2O2 was analysed using colorimetric hydrogen peroxide kit. Double staining immunofluorescence was given to observe NF-κB, iNOS and eNOS by using confocal laser scanning microscopy. The result was analyzed quantitatively using Olymphus Fluoview software (version 1.7a. Results: Lipid profile was significantly worsened in HCD and H2O2 level and expressions of NF-κB, iNOS and eNOS were also increased in HCD. EEMP 200 mg/kg body weight generally did not show significant results. However, high density lipoprotein level was affected by EEMP 400 mg/kg body weight, but not for other lipid profiles which reduced H2O2 level and NF-κB, iNOS and eNOS expressions significantly. EEMP 800 mg/kg body weight had been shown to be the most effective dose to improve lipid profile, decrease level of H2O2 and the expression of NF-κB and iNOS and maintain expression of eNOS. Conclusions: EEMP is an anti-inflammatory and antioxidant agent to inhibit atherogenesis in hypercholesterolemic rat.

  3. In vitro antioxidant and DNA damage inhibition activity of aqueous extract of Lantana camara L. (Verbenaceae) leaves

    Institute of Scientific and Technical Information of China (English)

    Kokati Venkata Bhaskara Rao

    2012-01-01

    Objective: To investigate the in vitro antioxidant and DNA damage inhibition potential of aqueous extract of Lantana camara leaves. Methods: Antioxidant activity of the aqueous extract of L. camara was estimated by 2, 2-diphenyl-1-picrylhydrazyl radical scavenging assay, metal chelating activity and reducing power assay. DNA damage inhibition was performed by photolysing H2O2 by UV radiation in the presence of pBR322 and extract. Estimation of phenolic content was carried out by Folin-Ciocalteau assay. Results: Extract exhibited high antioxidant activity in DPPH radical scavenng assay (IC50= 42.66 μg/ml), metal chelating activity (IC50= 1036.4μg/ml) and reducing power assay. Extract also exhibited the complete protection of pBR322 plasmid DNA during DNA damage inhibition assay. Extract showed high phenolic content which justified the antioxidant and DNA damage inhibition properties of the plant. Conclusions:These observations emphasize that aqueous extract of L. camara possess high antioxidant and DNA damage inhibition potential, thus, the plant can be used to develop natural antioxidant compounds for therapeutic use.

  4. Antioxidant activity and growth inhibition of human colon cancer cells by crude and purified fucoidan preparations extracted from Sargassum cristaefolium

    Directory of Open Access Journals (Sweden)

    Cheng-Yuan Wang

    2015-12-01

    Full Text Available Fucose-containing sulfated polysaccharides, also termed “fucoidans”, which are known to possess antioxidant, anticoagulant, anticancer, antiviral, and immunomodulating properties, are normally isolated from brown algae via various extraction techniques. In the present study, two methods (SC1 and SC2 for isolation of fucoidan from Sargassum cristaefolium were compared, with regard to the extraction yields, antioxidant activity, and inhibition of growth of human colon cancer cells exhibited by the respective extracts. SC1 and SC2 differ in the number of extraction steps and concentration of ethanol used, as well as the obtained sulfated polysaccharide extracts, namely, crude fucoidan preparation (CFP and purified fucoidan preparation (PFP, respectively. Thin layer chromatography, Fourier transform infrared analysis, and measurements of fucose and sulfate contents revealed that the extracts were fucoidan. There was a higher extraction yield for CFP, which contained less fucose and sulfate but more uronic acid, and had weaker antioxidant activity and inhibition of growth in human colon cancer cells. In contrast, there was a lower extraction yield for PFP, which contained more fucose and sulfate but less uronic acid, and had stronger antioxidant activity and inhibition of growth in human colon cancer cells. Thus, since the difference in bioactive activities between CFP and PFP was not remarkable, the high extraction yield of SC1 might be favored as a method in industrial usage for extracting fucoidan.

  5. Achyrocline satureioides (Lam. D.C. Hydroalcoholic Extract Inhibits Neutrophil Functions Related to Innate Host Defense

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    Eric Diego Barioni

    2013-01-01

    Full Text Available Achyrocline satureioides (Lam. D.C. is a herb native to South America, and its inflorescences are popularly employed to treat inflammatory diseases. Here, the effects of the in vivo actions of the hydroalcoholic extract obtained from inflorescences of A. satureioides on neutrophil trafficking into inflamed tissue were investigated. Male Wistar rats were orally treated with A. satureioides extract, and inflammation was induced one hour later by lipopolysaccharide injection into the subcutaneous tissue. The number of leukocytes and the amount of chemotactic mediators were quantified in the inflammatory exudate, and adhesion molecule and toll-like receptor 4 (TLR-4 expressions and phorbol-myristate-acetate- (PMA- stimulated oxidative burst were quantified in circulating neutrophils. Leukocyte-endothelial interactions were quantified in the mesentery tissue. Enzymes and tissue morphology of the liver and kidney were evaluated. Treatment with A. satureioides extract reduced neutrophil influx and secretion of leukotriene B4 and CINC-1 in the exudates, the number of rolling and adhered leukocytes in the mesentery postcapillary venules, neutrophil L-selectin, β2-integrin and TLR-4 expression, and oxidative burst, but did not cause an alteration in the morphology and activities of liver and kidney. Together, the data show that A. satureioides extract inhibits neutrophil functions related to the innate response and does not cause systemic toxicity.

  6. Inhibition of oxidative DNA damage in vitro by extracts of brussels sprouts.

    Science.gov (United States)

    Zhu, C; Poulsen, H E; Loft, S

    2000-08-01

    Cruciferous vegetables have cancer preventive effects which may be due to reduction of oxidative DNA damage. We investigated the effect of an aqueous extract of cooked Brussels sprouts on formation of 7-hydro-8-oxo-2'-deoxyguanosine (8-oxodG) in calf thymus DNA in vitro. Damage was induced by a Fenton reaction, UVC (254 nm), UVA (365 nm), sunlamp light, and methylene blue with visible light. The extract inhibited 8-oxodG formation in all systems except visible light with methylene blue. The IC50 values were 6-20 microg/ml corresponding to the extract of 5-20 g of Brussels sprouts distributed in a volume of 50 L. The protective effect in the Fenton reaction was unaffected by addition of EDTA. After HPLC separation fractions were identified with similar DNA protective effects. Sinigrin, a glucosinolate abundant in Brussels sprouts, co-eluted with the most effective fraction and had DNA protective effects. In comparison with other antioxidants the patterns of effect of the extract in the five damage systems were more similar to that of sodium azide than to those of dimethylsulfoxide and vitamin C. Constituents of Brussels sprouts can protect DNA by direct scavenging, e.g. hydroxyl radical and other oxidants, without prooxidant effects at concentrations potentially achievable by modest intake of the vegetable.

  7. Inhibition of crystallization of calcium oxalate by the extraction of Tamarix gallica L.

    Science.gov (United States)

    Bensatal, Ahmed; Ouahrani, M R

    2008-12-01

    The main objective is to study the inhibitor effect of acid fraction of the extract of Tamarix gallica L on the crystallization of calcium oxalate. The extract of Tamarix gallica L is very rich by acid compounds that are used as an inhibitor of nephrolithiasis (calcium oxalate). Our study of the calcium oxalate crystallization is based on the model of turbidimetry by means of a spectrophotometer. The calcium oxalate formation is induced by the addition of oxalate solutions of sodium and of calcium chloride. The addition of inhibitor with various concentrations enabled us to give information on the percentage of inhibition. The comparison between the turbidimetric slopes with and without inhibitor gives the effectiveness of inhibitor for the acid fraction. By comparing the photographs of with and without inhibitor, we concluded that the extract of Tamarix gallica L acts at the stage of growth. The acid fraction of the extract of Tamarix gallica L gives an activity remarkable in the formation of urinary lithiasis (calcium oxalate); this effectiveness is due to the presence of functions of acid.

  8. Growth inhibition of struvite crystals by the aqueous root extract of Rotula aquatica.

    Science.gov (United States)

    Chauhan, C K; Joshi, M J; Vaidya, A D B

    2011-06-01

    Formation of urinary stone is a serious and debilitating problem throughout the world. In the present study, the inhibitory effect of aqueous extract of root of Rotula aquatica was investigated against struvite crystals (one of the components of urinary stone) grown in vitro using single diffusion gel growth technique. For setting the gel, sodium metasilicate solution (specific gravity 1.05) and 0.5 M aqueous solution of ammonium dihydrogen phosphate were mixed, so that the pH of the mixture could be set at 7.0. Equal amounts of supernatant solution of magnesium acetate (1.0 M) prepared with 0.0%, 0.5% and 1% concentrations of the extract were gently poured on the set gels. It was observed that the number, dimension, total mass, total volume, growth rate and depth of growth of struvite crystals decreased with the increasing extract concentrations in the supernatant solutions. The enhancement of dissolution rate and fragmentation of struvite crystals suggested potential application of the extract for inhibition of struvite type urinary stone.

  9. [Grape seed proanthocyanidins extract inhibits pancreatic cancer cell growth through down-regulation of miR-27a expression].

    Science.gov (United States)

    Ma, Jia; Fang, Binbin; Zeng, Fanpeng; Pang, Haijie; Ma, Cong; Xia, Jun

    2015-01-01

    To explore the eff ect of grape seed proanthocyanidins extract (GSPE) on the growth of pancreatic cancer cells and the underlying mechanisms. The pancreatic cancer AsPC-1 cells were cultured in vitro. The effects of GSPE on cell proliferation, apoptosis and migration were analyzed by MTT, Annexin V-FITC/PI and Transwell migration assay, respectively. The expression of miR-27a and FOXO1 in AsPC-1 cells was determined by real-time RT-PCR and Western blot, respectively. The miR-27a inhibitors were applied to verify the role of miR-27a in mediation of GSPE effects. GSPE inhibited cell growth in a dose-dependent manner. This inhibitory effect was significant when the dosage of GSPE was more than 50 μg/mL (P<0.05 vs control). GSPE also could induce apoptosis and inhibit cell migration. MiR-27a expression was notably down-regulated when the dosage of GSPE was 75 μg/mL (P<0.01 vs control). Compared with the control group, cell proliferation inhibition was significantly increased in the miR-27a inhibitor group, the GSPE group and the miR-27a inhibitor plus GSPE group (P<0.01), while cell migration was significantly decreased (P<0.01). Compared with the GSPE or the miR-27a inhibitor group, the growth and migration inhibitory effects in the miR-27a inhibitor plus GSPE group were more obviously (P<0.01). Both GSPE and miR-27a inhibitor alone could up-regulate FOXO1 expression. But these effects were more apparent when they are applied in combination. GSPE inhibites AsPC-1 cells' growth and migration partly through down-regulation of miR-27a expression.

  10. Investigation between Alcoholic Extract and Essential Oil Melissa Officinalis L. New in Growth Inhibition of E. coli

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    Nooshin Naghsh

    2013-08-01

    Full Text Available Background: Therapy of plant is not any side effects and drug resustant for inhibition of disease in world. In this study, antimicrobial effects of Melissa officinalis L. ethanol exteract and essential oil on E. coli have been investigated. Materials and Methods: In this investigation, diameter of inhibitory zone of these materials was measured in disk agar diffusion method. Therefore, Melissa officinalisL. ethanolic exteract (80% and essential oil have been supplied. Then, antimicrobial activity these substances next for 24 hour for ethanol extraction 80% concentration 50 to 1000 mg/mL and essential oil concentration with 3% to 100% has been considered. Also, comparison of mean diameter of inhibitory zone between treatment and control groups of ANOVA has been used.Results: Results of these investigations were shown that extract ethanol Melissa officinalis L. was any inhibitory effect on E. coli growth 24 hour after of treatment. Also, diameter of inhibitory zone for 100% essential oil have been 33.2±0.13mm in E. coli that has been increased in comparison control groups significantly (p=0.001. This inhibitory effects was more than cefixime and cefteriaxone (p=0.00, p=0.01.Conclusion: These found were shown that this plant prevents growth of E. coli In vitro condition. This essential oil could be suggested as antimicrobial agents for inhibition of bacterial diseases in human.

  11. The role of acid anion on the inhibition of the acidic corrosion of steel by lupine extract

    Energy Technology Data Exchange (ETDEWEB)

    Abdel-Gaber, A.M. [Chemistry Department, Faculty of Science, Alexandria University, Ibrahimia, P.O. Box 426, Alexandria 21321 (Egypt)], E-mail: ashrafmoustafa@yahoo.com; Abd-El-Nabey, B.A.; Saadawy, M. [Chemistry Department, Faculty of Science, Alexandria University, Ibrahimia, P.O. Box 426, Alexandria 21321 (Egypt)

    2009-05-15

    The inhibitive effect of lupine (Lupinous albus L.) extract on the corrosion of steel in aqueous solution of 1 M sulphuric and 2 M hydrochloric acids was investigated by potentiodynamic polarization and electrochemical impedance spectroscopy (EIS) techniques. Potentiodynamic polarization curves indicated that the lupine extract acts as a mixed-type inhibitor. EIS measurements showed that the dissolution process is under activation control. The inhibition efficiency of the extract obtained from impedance and polarization measurements was in a good agreement and was found to increase with increasing concentration of the extract. The obtained results showed that, the lupine extract could serve as an effective inhibitor for the corrosion of steel in acid media and the extract was more effective in case of hydrochloric acid. Theoretical fitting of the corrosion data to the kinetic-thermodynamic model was tested to show the nature of adsorption.

  12. Inhibition of NF-κB activation and MMP-9 secretion by plasma of human volunteers after ingestion of maritime pine bark extract (Pycnogenol

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    Ďuračková Zdeňka

    2006-01-01

    Full Text Available Abstract French maritime pine bark extract (Pycnogenol® displays a variety of anti-inflammatory effects in vivo. Aim of this study was to determine whether human plasma after oral intake of Pycnogenol contains sufficient concentrations of active principles to inhibit key mediators of inflammation. Blood samples from seven healthy volunteers were obtained before and after five days administration of 200 mg Pycnogenol per day. Plasma samples statistically significantly inhibited matrix metalloproteinase 9 (MMP-9 release from human monocytes and NF-κB activation. Thus, we provide evidence that bioavailable active principles of Pycnogenol exert anti-inflammatory effects by inhibition of proinflammatory gene expression which is consistent with documented clinical observations. We suggest that our ex vivo method is suitable to substantiate molecular pharmacological mechanisms of complex plant extracts in a more focussed and rational way compared to in vitro studies by taking into account the processes of absorption and metabolism.

  13. ANTIOXIDANT, ANTI-INFLAMMATORY AND DIABETES RELATED ENZYME INHIBITION PROPERTIES OF LEAVES EXTRACT FROM SELECTED VARIETIES OF PHOENYX DACTYLIFERA L.

    OpenAIRE

    Laouini Salah Eddine

    2013-01-01

    Objective: to investigate the antioxidant, anti-inflammatory, and antidiabetic activities of ethanolic leaves extracts of three selected varieties of Phoenyx dactylifera L. namely: “Ghars”, “Deglet Nour” and “Hamraya”. Methods: The assessment of the antioxidant potential of crude leaves extracts, using superoxide anions inhibition, DPPH and total antioxidant activity essays, was carried out. Furthermore, the anti-inflammatory properties of the extracts were determined by measuring the inhibi...

  14. In vitro and in vivo α-amylase and α-glucosidase inhibiting activities of the protein extracts from two varieties of bitter gourd (Momordica charantia L.).

    Science.gov (United States)

    Poovitha, Sundar; Parani, Madasamy

    2016-07-18

    α-amylase and α-glucosidase digest the carbohydrates and increase the postprandial glucose level in diabetic patients. Inhibiting the activity of these two enzymes can control postprandial hyperglycemia, and reduce the risk of developing diabetes. Bitter gourd or balsam pear is one of the important medicinal plants used for controlling postprandial hyperglycemia in diabetes patients. However, there is limited information available on the presence of α-amylase and α-glucosidase inhibiting compounds. In the current study, the protein extracts from the fruits of M. charantia var. charantia (MCC) and M. charantia var. muricata (MCM) were tested for α-amylase and α-glucosidase inhibiting activities in vitro, and glucose lowering activity after oral administration in vivo. The protein extract from both MCC and MCM inhibited the activity of α-amylase and α-glucosidase through competitive inhibition, which was on par with Acarbose as indicated by in vitro percentage of inhibition (66 to 69 %) and IC50 (0.26 to 0.29 mg/ml). Both the protein extracts significantly reduced peak blood glucose and area under the curve in Streptozotocin-induced diabetic rats, which were orally challenged with starch and sucrose. Protein extracts from the fruits of the two varieties of bitter gourd inhibited α-amylase and α-glucosidase in vitro and lowered the blood glucose level in vivo on par with Acarbose when orally administrated to Streptozotocin-induced diabetic rats. Further studies on mechanism of action and methods of safe and biologically active delivery will help to develop an anti-diabetic oral protein drug from these plants.

  15. Grape seed extract inhibits VEGF expression via reducing HIF-1alpha protein expression.

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    Lu, Jianming; Zhang, Keqiang; Chen, Shiuan; Wen, Wei

    2009-04-01

    Grape seed extract (GSE) is a widely consumed dietary supplement that has antitumor activity. Here, we have investigated the inhibitory effect of GSE on the expression of vascular endothelial growth factor (VEGF) and the mechanism underlying this action. We found that GSE inhibited VEGF messenger RNA (mRNA) and protein expression in U251 human glioma cells and MDA-MB-231 human breast cancer cells. GSE inhibited transcriptional activation of the VEGF gene through reducing protein but not mRNA expression of hypoxia-inducible factor (HIF) 1alpha. The inhibitory effect of GSE on HIF-1alpha expression was mainly through inhibiting HIF-1alpha protein synthesis rather than promoting protein degradation. Consistent with this result, GSE-suppressed phosphorylation of several important components involved in HIF-1alpha protein synthesis, such as Akt, S6 kinase and S6 protein. Furthermore, in the MDA-MB-231 tumor, we found that GSE treatment inhibited the expression of VEGF and HIF-1alpha and the phosphorylation of S6 kinase without altering the subcellular localization of HIF-1alpha, correlating with reduced vessel density and tumor size. Depletion of polyphenol with polyvinylpyrrolidone abolished the inhibitory activity of GSE, suggesting a water-soluble fraction of polyphenol in GSE is responsible for the inhibitory activity. Taken together, our results indicate that GSE inhibits VEGF expression by reducing HIF-1alpha protein synthesis through blocking Akt activation. This finding provides new insight into the mechanisms of anticancer activity of GSE and reveals a novel molecular mechanism underlying the antiangiogenic action of GSE.

  16. Selective COX-2 inhibition by a Pterocarpus marsupium extract characterized by pterostilbene, and its activity in healthy human volunteers.

    Science.gov (United States)

    Hougee, Sander; Faber, Joyce; Sanders, Annemarie; de Jong, Romy B; van den Berg, Wim B; Garssen, Johan; Hoijer, Maarten A; Smit, H Friso

    2005-05-01

    In this study, an extract of Pterocarpus marsupium Roxb. containing pterostilbene has been evaluated for its PGE2-inhibitory activity in LPS-stimulated PBMC. In addition, the COX-1/2 selective inhibitory activity of P. marsupium (PM) extract was investigated. Biological activity, as well as safety of PM extract was evaluated in healthy human volunteers. PM extract, pterostilbene and resveratrol inhibited PGE2 production from LPS-stimulated human peripheral blood mononuclear cells (PBMC) with IC50 values of 3.2 +/- 1.3 microg/mL, 1.0 +/- 0.6 microM and 3.2 +/- 1.4 microM, respectively. When pterostilbene content of PM extract is calculated, PGE2 production inhibition of PM extract is comparable to PGE2 production inhibition of purified pterostilbene. Furthermore, in a COX-1 whole blood assay (WBA) PM extract was not effective while in a COX-2 WBA, PM extract decreased PGE2 production indicating COX-2 specific inhibition. In healthy human volunteers, the oral use of 450 mg PM extract did not decrease PGE2 production ex vivo in a WBA. Pterostilbene levels in serum were increased, but were 5-fold lower than the observed IC50 for PGE2 inhibition in LPS-stimulated PBMC. No changes from base-line of the safety parameters were observed and no extract-related adverse events occurred during the study. In conclusion, this is the first study to describe the selective COX-2 inhibitory activity of a Pterocarpus marsupium extract. Moreover, the PGE2 inhibitory activity of PM extract was related to its pterostilbene content. In humans, 450 mg PM extract resulted in elevated pterostilbene levels in serum, which were below the active concentration observed in vitro. In addition, short-term supplementation of 450 mg PM extract is considered to be a safe dose based on the long history of use, the absence of abnormal blood cell counts and blood chemistry values and the absence of extract-related adverse events. This strongly argues for a dose-finding study of PM extract in humans to

  17. Synergistic Effect on Corrosion Inhibition Efficiency of Ginger Affinale Extract in Controlling Corrosion of Mild Steel in Acid Medium

    Energy Technology Data Exchange (ETDEWEB)

    Subramanian, Ananth Kumar; Arumugam, Sankar [Kandaswami Kandar' s College, Namakkal (India); Mallaiya, Kumaravel; Subramaniam, Rameshkumar [PSG College of Technology Peelamedu, Coimbatore (India)

    2013-12-15

    The corrosion inhibition nature of Ginger affinale extract for the corrosion of mild steel in 0.5N H{sub 2}SO{sub 4} was investigated using weight loss, electrochemical impedance and potentiodynamic polarization methods. The results revealed that Ginger affinale extract acts as a good corrosion inhibitor in 0.5N H{sub 2}SO{sub 4} medium. The inhibition efficiency increased with an increase in inhibitor concentration. The inhibition could be attributed to the adsorption of the inhibitor on the steel surface.

  18. Tapirira guianensis Aubl. Extracts Inhibit Proliferation and Migration of Oral Cancer Cells Lines

    Science.gov (United States)

    Silva-Oliveira, Renato José; Lopes, Gabriela Francine; Camargos, Luiz Fernando; Ribeiro, Ana Maciel; dos Santos, Fábio Vieira; Severino, Richele Priscila; Severino, Vanessa Gisele Pasqualotto; Terezan, Ana Paula; Thomé, Ralph Gruppi; dos Santos, Hélio Batista; Reis, Rui Manuel; Ribeiro, Rosy Iara Maciel de Azambuja

    2016-01-01

    Cancer of the head and neck is a group of upper aerodigestive tract neoplasms in which aggressive treatments may cause harmful side effects to the patient. In the last decade, investigations on natural compounds have been particularly successful in the field of anticancer drug research. Our aim is to evaluate the antitumor effect of Tapirira guianensis Aubl. extracts on a panel of head and neck squamous cell carcinoma (HNSCC) cell lines. Analysis of secondary metabolites classes in fractions of T. guianensis was performed using Nuclear Magnetic Resonance (NMR). Mutagenicity effect was evaluated by Ames mutagenicity assay. The cytotoxic effect, and migration and invasion inhibition were measured. Additionally, the expression level of apoptosis-related molecules (PARP, Caspases 3, and Fas) and MMP-2 was detected using Western blot. Heterogeneous cytotoxicity response was observed for all fractions, which showed migration inhibition, reduced matrix degradation, and decreased cell invasion ability. Expression levels of MMP-2 decreased in all fractions, and particularly in the hexane fraction. Furthermore, overexpression of FAS and caspase-3, and increase of cleaved PARP indicates possible apoptosis extrinsic pathway activation. Antiproliferative activity of T. guianensis extract in HNSCC cells lines suggests the possibility of developing an anticancer agent or an additive with synergic activities associated with conventional anticancer therapy. PMID:27834805

  19. Extract from Eugenia punicifolia is an antioxidant and inhibits enzymes related to metabolic syndrome.

    Science.gov (United States)

    Lopes Galeno, Denise Morais; Carvalho, Rosany Piccolotto; Boleti, Ana Paula de Araújo; Lima, Arleilson Sousa; Oliveira de Almeida, Patricia Danielle; Pacheco, Carolina Carvalho; Pereira de Souza, Tatiane; Lima, Emerson Silva

    2014-01-01

    The present study aimed to investigate in vitro biological activities of extract of Eugenia punicifolia leaves (EEP), emphasizing the inhibitory activity of enzymes related to metabolic syndrome and its antioxidant effects. The antioxidant activity was analyzed by free radicals scavengers in vitro assays: DPPH·, ABTS(·+), O2(·−), and NO· and a cell-based assay. EEP were tested in inhibitory colorimetric assays using α-amylase, α-glucosidase, xanthine oxidase, and pancreatic lipase enzymes. The EEP exhibited activity in ABTS(·+), DPPH·, and O2(·−) scavenger (IC50 = 10.5 ± 1.2, 28.84 ± 0.54, and 38.12 ± 2.6 μg/mL), respectively. EEP did not show cytotoxic effects, and it showed antioxidant activity in cells in a concentration-dependent manner. EEP exhibited inhibition of α-amylase, α-glucosidase, and xanthine oxidase activities in vitro assays (IC50 = 122.8 ± 6.3; 2.9 ± 0.1; 23.5 ± 2.6), respectively; however, EEP did not inhibit the lipase activity. The findings supported that extract of E. punicifolia leaves is a natural antioxidant and inhibitor of enzymes, such as α-amylase, α-glucosidase, and xanthine oxidase, which can result in a reduction in the carbohydrate absorption rate and decrease of risks factors of cardiovascular disease, thereby providing a novel dietary opportunity for the prevention of metabolic syndrome.

  20. Inhibition of anaphylaxis-like reaction and mast cell activation by water extract from the fruiting body of Phellinus linteus.

    Science.gov (United States)

    Choi, Yun Ho; Yan, Guang Hai; Chai, Ok Hee; Lim, Jung Min; Sung, So Young; Zhang, Xin; Kim, Ji-Hyun; Choi, Su Hwan; Lee, Moo Sam; Han, Eui-Hyeog; Kim, Hyoung Tae; Song, Chang Ho

    2006-07-01

    Mast cell-mediated anaphylactic reaction is involved in many allergic diseases such as asthma and allergic rhinitis. Phellinus linteus has been used as a traditional herb medicine in oriental countries and is known to have anti-tumor, immunomodulatory, anti-inflammatory, and anti-allergic activities. However, roles of Phellinus linteus in the mast cell-mediated anaphylactic reactions have not fully been examined. In the present study, we have investigated the effects of water extract from the fruiting body of Phellinus linteus (WEPL) on mast cell-mediated anaphylaxis-like reactions. Oral administration of WEPL inhibited the compound 48/80-induced systemic anaphylaxis-like reaction and ear swelling response. WEPL also inhibited the anti-dinitrophenyl (DNP) IgE-mediated passive systemic and cutaneous anaphylaxis. WEPL had no cytotoxicity on rat peritoneal mast cells (RPMC). WEPL dose-dependently reduced histamine release from RPMC activated by compound 48/80 or anti-DNP IgE. Moreover, WEPL decreased the compound 48/80-induced calcium uptake into RPMC. Furthermore, WEPL increased the level of intracellular cAMP and significantly inhibited the compound 48/80-induced cAMP reduction in RPMC. These results suggest that WEPL may serve as an effective therapeutic agent for allergic diseases.

  1. Anti-inflammatory activities of Physalis alkekengi var. franchetii extract through the inhibition of MMP-9 and AP-1 activation.

    Science.gov (United States)

    Hong, Ju-Mi; Kwon, Ok-Kyoung; Shin, In-Sik; Song, Hyuck-Hwan; Shin, Na-Rae; Jeon, Chan-Mi; Oh, Sei-Ryang; Han, Sang-Bae; Ahn, Kyung-Seop

    2015-01-01

    Physalis alkekengi has been traditionally used for the treatment of coughs, middle ear infections, and sore throats in Korea, Europe, and China. It exhibits a variety of pharmacological activities such as anti-inflammatory, anti-oxidant, and anti-cancer effects. The anti-inflammatory effects of the P. alkekengi methanol extract (PA) and its molecular mechanisms have not yet been fully investigated. In the present study, the chromatogram of PA was established by UPLC analysis. The anti-inflammatory effects of PA were also investigated using murine microphage cell lines, RAW 264.7 cells, and a murine model of OVA induced asthma. In LPS-stimulated RAW264.7 cells, PA reduced the MMP-9 expression with decreases in the production of nitric oxide, inteleukin-6, and tumor necrosis factor-α. Furthermore, PA suppressed the phosphorylation of MAPKs, which resulted in the inhibition of AP-1 activation. These effects of PA were consistent with the results of the in vivo experiment. PA-treated mice significantly inhibited inflammatory cell counts and cytokine production in bronchoalveolar lavage fluids and airway-hyperresponsiveness in OVA-induced asthmatic mice. PA treated mice also showed a marked inhibition of inducible nitric oxide synthase and MMP-9 expression. In conclusion, our results suggest that PA may be a valuable therapeutic material in treating various inflammatory diseases, including allergic asthma.

  2. Coffee extract inhibits adipogenesis in 3T3-L1 preadipocyes by interrupting insulin signaling through the downregulation of IRS1.

    Science.gov (United States)

    Maki, Chihiro; Funakoshi-Tago, Megumi; Aoyagi, Ryohei; Ueda, Fumihito; Kimura, Masaki; Kobata, Kenji; Tago, Kenji; Tamura, Hiroomi

    2017-01-01

    Although epidemiological data have indicated that a strong negative association exists between coffee consumption and the prevalence of obesity-associated diseases, the molecular mechanisms by which coffee intake prevents obesity-associated diseases has not yet been elucidated. In this study, we found that coffee intake significantly suppressed high-fat diet (HFD)-induced metabolic alternations such as increases in body weight and the accumulation of adipose tissue, and up-regulation of glucose, free fatty acid, total cholesterol and insulin levels in the blood. We also found that coffee extract significantly inhibited adipogenesis in 3T3-L1 preadipocytes. In the early phase of adipogenesis, 3T3-L1 cells treated with coffee extract displayed the retardation of cell cycle entry into the G2/M phase called as mitotic clonal expansion (MCE). Coffee extract also inhibited the activation of CCAAT/enhancer-binding protein β (C/EBPβ) by preventing its phosphorylation by ERK. Furthermore, the coffee extract suppressed the adipogenesis-related events such as MCE and C/EBPβ activation through the down-regulation of insulin receptor substrate 1 (IRS1). The stability of the IRS1 protein was markedly decreased by the treatment with coffee extract due to proteasomal degradation. These results have revealed an anti-adipogenic function for coffee intake and identified IRS1 as a novel target for coffee extract in adipogenesis.

  3. An extract of Uncaria tomentosa inhibiting cell division and NF-kappa B activity without inducing cell death.

    Science.gov (United States)

    Akesson, Christina; Lindgren, Hanna; Pero, Ronald W; Leanderson, Tomas; Ivars, Fredrik

    2003-12-01

    Previous reports have demonstrated that extracts of the plant Uncaria tomentosa inhibit tumor cell proliferation and inflammatory responses. We have confirmed that C-Med 100, a hot water extract of this plant, inhibits tumor cell proliferation albeit with variable efficiency. We extend these findings by showing that this extract also inhibits proliferation of normal mouse T and B lymphocytes and that the inhibition is not caused by toxicity or by induction of apoptosis. Further, the extract did not interfere with IL-2 production nor IL-2 receptor signaling. Since there was no discrete cell cycle block in C-Med 100-treated cells, we propose that retarded cell cycle progression caused the inhibition of proliferation. Collectively, these data suggested interference with a common pathway controlling cell growth and cell cycle progression. Indeed, we provide direct evidence that C-Med 100 inhibits nuclear factor kappa B (NF-kappa B) activity and propose that this at least partially causes the inhibition of proliferation.

  4. Study on Corrosion Inhibition Efficiency of Stem Alkaloid Extract of Different Varieties of Holy Basil on Aluminium in HCl Solution

    Energy Technology Data Exchange (ETDEWEB)

    Kumpawat, Nutan; Chaturvedi, Alok; Upadhyay, R. K. [Synthetic and Surface Science Laboratory, Ajmer (India)

    2012-08-15

    Corrosion inhibition efficiencies of holy basil on Al in HCl solution were studied by weight loss and thermometric methods in presence and in absence of stem extract of three different varieties of holy basil viz. ocimum basilicum (E{sub B}), ocimum canum (E{sub C}) and ocimum sanctum (E{sub S}). Inhibition efficiency increases with the increasing concentration of stem extract and decreases with increases in acid strength. Results show that all varieties under study are good corrosion inhibitors, among which, E{sub B} is most effective. Maximum inhibition efficiency was found 97.09% in 0.5N HCl solution with 0.6% stem extract. The Langmuir adsorption isotherm indicates that surface coverage also increases with increasing in the concentration of extract of stem in HCl solution.

  5. Methanolic extract of Ruta graveolens L. inhibits inflammation and oxidative stress in adjuvant induced model of arthritis in rats.

    Science.gov (United States)

    Ratheesh, M; Shyni, G L; Helen, A

    2009-04-01

    Ruta graveolens L. (Rutaceae) are traditionally used for the treatment of rheumatism, arthritis and other inflammatory conditions in the traditional medicine of India. The purpose of this study was to investigate anti-inflammatory and anti-oxidant effects of methanolic extract of Ruta graveolens L. in adjuvant induced arthritis in rats. Methanolic extract of Ruta graveolens (MER) exhibited maximum percentage of oedema inhibition at a dose of 20 mg/kg on 21st day of adjuvant arthritis. The effect was higher than that of standard drug indomethacin. The activities of cycloxygenase-2 and myeloperoxidase and concentration of thiobarbituric acid reactive substance (TBARS) were decreased and the activities of antioxidant enzymes, vitamins C & E and reduced glutathione level were increased on treatment with MER. The increment in ESR and total WBC, reduction in RBC count and haemoglobin and aberrant changes to the C-reactive protein (CRP) and ceruloplasmin levels observed in the arthritic animals were also found to be significantly restored in MER treated rats. Histopathology of paw tissue showed decreased oedema formation and cellular infiltration on supplementation with MER. Thus the results demonstrated the potential beneficiary effect of methanolic extract of Ruta graveolens on adjuvant induced arthritis in rats.

  6. Aqueous extract of Rabdosia rubescens leaves: forming nanoparticles, targeting P-selectin, and inhibiting thrombosis

    Directory of Open Access Journals (Sweden)

    Wang Y

    2015-11-01

    Full Text Available Yuji Wang,1 Jingcheng Tang,1 Haimei Zhu,1 Xueyun Jiang,1 Jiawang Liu,1 Wenyun Xu,1 Haiping Ma,1 Qiqi Feng,1 Jianhui Wu,1 Ming Zhao,1,2 Shiqi Peng1 1Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Engineering Research Center of Endogenous Prophylactic of Ministry of Education of China, Beijing Laboratory of Biomedical Materials, College of Pharmaceutical Sciences, Capital Medical University, Beijing, People’s Republic of China; 2Faculty of Biomedical Science and Environmental Biology, Kaohsiung Medical University, Kaohsiung, Taiwan Abstract: The hot water extract of Rabdosia rubescens was traditionally used as an antithrombotic medicine. To explore its antithrombotic utility and mechanism, we carried out a series of in vitro and in vivo assays in this study. In vitro platelet aggregation assay showed that the half maximal inhibitory concentration values of aqueous extract of R. rubescens leaves (AERL inhibiting platelet aggregation induced by thrombin, arachidonic acid, adenosine diphosphate, and platelet-activating factor ranged from 0.12 mg/mL to 1.43 mg/mL. The minimal effective oral dose of AERL inhibiting the rats from forming thrombus was 25 mg/kg. Both in vitro and in vivo actions were correlated with AERL concentration-dependently inhibiting sP-selectin release. In water, AERL formed nanoparticles, and their size depended on the concentration. Docking the five nucleotides, 21 phenolic acids, and four diterpenoids identified by high-performance liquid chromatography–photodiode array detector/(-electrospray ionization-tandem mass spectrometry analysis into the active site of P-selectin, rosmarinic acid was predicted to be the antithrombotic ingredient of AERL. In flow cytometry analysis, 1 µM of rosmarinic acid effectively inhibited sP-selectin release in arachidonic acid-activated platelets. In a rat model, 5 mg/kg of oral rosmarinic acid effectively inhibited thrombosis. Keywords: R. rubescens, s

  7. Ethanol Extract of Atractylodes macrocephala Protects Bone Loss by Inhibiting Osteoclast Differentiation

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    Youn-Hwan Hwang

    2013-06-01

    Full Text Available The rhizome of Atractylodes macrocephala has been used mainly in Traditional Chinese Medicine for invigorating the functions of the stomach and spleen. In the present study, we investigated the inhibitory effect of the 70% ethanol extract of the rhizome of Atractylodes macrocephala (AMEE on osteoclast differentiation. We found that AMEE inhibits osteoclast differentiation from its precursors induced by receptor activator of nuclear factor-κB ligand (RANKL, an essential cytokine required for osteoclast differentiation. AMEE attenuated RANKL-induced activation of NF-κB signaling pathway, subsequently inhibiting the induction of osteoclastogenic transcription factors, c-Fos and nuclear factor of activated T cells cytoplasmic 1. Consistent with the in vitro results, administration of AMEE protected RANKL-induced bone loss in mice. We also identified atractylenolide I and II as active constituents contributing to the anti-osteoclastogenic effect of AMEE. Taken together, our results demonstrate that AMEE has a protective effect on bone loss via inhibiting osteoclast differentiation and suggest that AMEE may be useful in preventing and treating various bone diseases associated with excessive bone resorption.

  8. Aqueous extract of Pinus caribaea inhibits the damage induced by ultraviolet radiations, in plasmid DNA

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    Marioly Vernhes Tamayo

    2017-08-01

    Full Text Available Context: The incidence of solar ultraviolet radiation (UV on Earth has increased due to diminish of the ozone layer. This enviromental agent is highly genotoxic causing numerous damage in DNA molecule. Nowadays there is a growing interest in the search of compounds capable to minimize these effects. In particular, phytocompounds have been tested as excelent candidates for their antigenotoxic properties. Aims: To evaluate the protective effect of the aqueous extract of Pinus caribaea (EPC against the damage induced by the UVB and UVC radiation. Methods: The cell-free plasmid DNA assay was employed. The forms of plasmid were separated electrophoretically in agarose gel. For genotoxic and photoprotective evaluation of P. caribaea, different concentrations of the extract (0.1 – 2.0 mg/mL and exposure times were evaluated. The CPD lesions were detected enzymatically. Additionally, the transmittance of the aqueous extract against 254 nm and 312 nm was measured. Results: None of the concentrations were genotoxic in 30 min of treatment, for superior times a clastogenic effect was observed. The EPC despite inhibiting the activity of the enzyme T4 endo V, impedes photolesions formation in DNA at concentrations ≥ 0.1 mg/mL. Conclusions: The EPC has photoprotective properties, this effect could be related with its antioxidants and absorptives capacities.

  9. Fresh raspberry phytochemical extract inhibits hepatic lesion in a Wistar rat model

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    Wang Lei

    2010-11-01

    Full Text Available Abstract Background Red raspberry possesses potent antioxidant capacity and antiproliferative activity against cancer in vitro. Methods The objective of this study was to determine the protective effects of raspberry 80% acetone extract in a rat hepatic lesions model induced by diethylnitrosamine (DEN. Rats were treated with the red raspberry extract (0.75, 1.5 or 3.0 g/kg of body weight by gavage starting 2 h after DEN administration and continuing for 20 weeks. Results A dose-dependent inhibition by red raspberry extract of DEN-induced hepatic nodule formation which stands for hepatic lesions was observed. Corresponding hepatic nodule incidence rates were 45.0, 40.0, 25.0 and 5.0% in positive control, low, middle and high groups, respectively (P Conclusions These findings demonstrate that the potent capacity of red raspberry diet could not only suppress DEN-induced hepatic lesions in rats, but also reduce the definite diagnostic features of neoplasm.

  10. The Study of Synergistic Effects of n.butanolic Cyclamen coum Extract and Ciprofloxacin on inhibition of Pseudomonas aeruginosa biofilm formation

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    ahya abdi ali

    2015-02-01

    Full Text Available   Introduction : Infections caused by Pseudomonas aeruginosa biofilm are the major causes of death in patients with cystic fibrosis (CF. Some studies revealed that biofilms are resistant to several antibiotics because of their impermeable structures. In order to re-sensitize bacteria to different antibiotics, biofilm formation should be inhibited. In this research, evaluation of antibiofilm activity of n-butanolic Cyclamen coum extract as a medici­nal plant from Myrsinaceae family, in combination with ciprofloxacin was carried out.   Materials and method s: The biofilm formation ability by P. aeruginosa PAO1 and one clinically isolated P. aeruginosa (PA214 was confirmed by microtiter plate method. Extraction of the tubers of Cyclamen coum was done by fractionation method . The antibiofilm and antibacterial properties of n-butanolic C. coum extract (which includes saponin compounds alone and in combination with ciprofloxacin by using microdilution and crystal violet methods were examined. The cytotoxicity effect of the n-butanolic extract on HT-29 cells was assayed by MTT (3- (4,5-dimethylthiazol-2-yl -2,5-diphenyl-tetrazolium bromide test.   Results : The biofilm formation ability by P. aeruginosa strains was quantitatively confirmed. Saponin content of the n-butanolic C.coum extract was 156 µg/mL. The extract revealed antibacterial activity against the growth of planktonic P. aeruginosa strains. The combination of n-butanolic C.coum extract and ciprofloxacin significantly inhibited P.aeruginosa biofilm formation (ΣFBIC = 0.5. The n-butanolic C.coum extract showed insignificant cytotoxic effect against HT-29 human cancer cell line after 48 hours and 72 hours incubation .   Discussion and conclusion : It can be concluded that n-butanolic C.coum extract in combination with ciprofloxacin significantly revealed antibiofilm activity against P. aeruginosa biofilm however, further clinical investigations are required.

  11. Rhodiola rosea extracts and salidroside decrease the growth of bladder cancer cell lines via inhibition of the mTOR pathway and induction of autophagy.

    Science.gov (United States)

    Liu, Zhongbo; Li, Xuesen; Simoneau, Anne R; Jafari, Mahtab; Zi, Xiaolin

    2012-03-01

    The incidence of human urinary bladder cancer increases markedly with age, suggesting a mechanistic connection between aging and bladder carcinogenesis and a potential use of anti-aging agents in bladder cancer chemoprevention. Rhodiola rosea, growing in high altitude or cold regions of the world, has been reported to have anti-aging effects in Drosophila. We demonstrated that a R. rosea extract and one of its bioactive components, salidroside, inhibited the growth of bladder cancer cell lines with a minimal effect on nonmalignant bladder epithelial cells TEU-2. Interestingly, the R. rosea extract and salidroside component exhibited a selective ability to inhibit the growth of p53 knockout primary mouse embryo fibroblasts (p53-/- MEFs) compared to their wild-type counterparts. The growth inhibitory effects of the R. rosea extract and salidroside were, however, attenuated in TSC2 and p53 double knock MEFs (TSC2-/-, p53-/- MEFs), suggesting that TSC2 protein is, at least in part, required for the growth inhibitory effects of the R. rosea extract and salidroside. The R. rosea extract and salidroside treatment of UMUC3 cells resulted in an increase of AMP-activated protein kinase (AMPK)-α phosphorylation and a decrease of 4E-BP1 phosphorylation, leading to increased binding of 4E-BP1 to m7 GTP. These results indicate that the R. rosea extract and salidroside inhibit translation initiation. Furthermore, both the R. rosea extract and salidroside treatment of UMUC3 cells caused a significant percentage of cells undergoing autophagy. Therefore, the R. rosea extract and salidroside deserve further study as novel agents for chemoprevention of bladder carcinogenesis. Copyright © 2011 Wiley Periodicals, Inc.

  12. Salacia campestris root bark extract: peroxidase inhibition, antioxidant and antiradical profile

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    José Carlos Rebuglio Vellosa

    2009-03-01

    Full Text Available Reactive oxygen species (ROS and free radical species have been implicated in initiating or accompanying many diseases in living organisms; there is thus, a continual need for antioxidants molecules to inactivate ROS/free radicals. Many studies of plants crude extracts have demonstrated free-radical scavenging and antioxidant action. Salacia species have long been used, in several countries, as traditional medicines against certain diseases and for their anti-inflammatory properties. In this study, Salacia campestris Walp (Hippocrateaceae root bark ethanol extract (ScEtOH was assessed for its ability to scavenge free radicals and reactive oxygen species; the results were expressed as percentage inhibition of the active species. ScEtOH was efficient against studied species: DPPH radical (obtained inhibition = 30%, ABTS•+ (IC50 = 1.8±0.8 μg/mL, HOCl (IC50 = 1.7 ± 0.1 μg/mL, O2•- (obtained inhibition = 32%, and NO• (obtained inhibition = 18 %. Peroxidase activity inhibition was evaluated through the guaiacol oxidation reaction catalyzed by hemin, HRP and myeloperoxidase (MPO; data showed that ScEtOH at 10 μg/mL led to 54 and 51% of inhibition, respectively, for the hemin and HRP systems. In the MPO system, ScEtOH promoted a 50% inhibition at 8.9 μg/mL, whereas quercetin, a powerful MPO inhibitor, inhibited this system at 1.35 μg/mL.Espécies reativas do oxigênio (ERO e radicais livres estão relacionados ao início ou à exacerbação de muitas doenças em organismos vivos; existindo portanto uma necessidade contínua por moléculas antioxidantes que inativem as ERO e radicais livres. Muitos estudos com extratos brutos de plantas têm demonstrado propriedades antioxidantes e seqüestradoras de radicais livres. Espécies de Salacia são utilizadas, em muitos países, como remédio tradicional contra certas doenças e por suas propriedades antiinflamatórias. Neste estudo, o extrato bruto etanólico da casca da raiz da Salacia

  13. Grape seed extract inhibits angiogenesis via suppression of the vascular endothelial growth factor receptor signaling pathway.

    Science.gov (United States)

    Wen, Wei; Lu, Jianming; Zhang, Keqiang; Chen, Shiuan

    2008-12-01

    Blockade of angiogenesis is an important approach for cancer treatment and prevention. Vascular endothelial growth factor (VEGF) is one of the most critical factors that induce angiogenesis and has thus become an attractive target for antiangiogenesis treatment. However, most current anti-VEGF agents often cause some side effects when given chronically. Identification of naturally occurring VEGF inhibitors derived from diet would be one alternative approach with an advantage of known safety. Grape seed extract (GSE), a widely used dietary supplement, is known to have antitumor activity. In this study, we have explored the activity of GSE on VEGF receptor and angiogenesis. We found that GSE could directly inhibit the kinase activity of purified VEGF receptor 2, a novel activity of GSE that has not been characterized. GSE could also inhibit the VEGF receptor/mitogen-activated protein kinase-mediated signaling pathway in endothelial cells. As a result, GSE could inhibit VEGF-induced endothelial cell proliferation and migration as well as sprout formation from aorta ring. In vivo assay further showed that GSE could inhibit tumor growth and tumor angiogenesis of MDA-MB-231 breast cancer cells in mice. Consistent with the in vitro data, GSE treatment of tumor-bearing mice led to concomitant reduction of blood vessel density and phosphorylation of mitogen-activated protein kinase. Depletion of polyphenol with polyvinylpyrrolidone abolished the antiangiogenic activity of GSE, suggesting a water-soluble fraction of polyphenol in GSE is responsible for the antiangiogenic activity. Taken together, this study indicates that GSE is a well-tolerated and inexpensive natural VEGF inhibitor and could potentially be useful in cancer prevention or treatment.

  14. Prevention of secretory diarrhea by ethanol extract of Bistortae rhizoma through inhibition of chloride channel

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    Bo Yu

    2015-08-01

    Full Text Available Inhibition of cystic fibrosis transmembrane conductance regulator (CFTR and Ca2+-activated Cl- channel (CaCC represents an attractive approach for the treatment of secretory diarrhea. The aim of the study is to investigate the molecular basis of the anti-diarrheal effect of traditional Chinese herbal anti-diarrheal medicine Bistortae rhizoma. Fluorescence quenching assay indicated that the 40% methanol /water fraction (D5 dose-dependently inhibited both CFTR and CaCC function in transfected Fischer rat thyroid (FRT cells. Ex vivo studies indicated that D5 inhibited both forskolin (FSK-activated CFTR current and CCh-induced CaCC current in rat colonic mucosa. In the mouse closed-loop model, intraluminal application of D5 (200 µg/mL significantly reduced cholera toxin-stimulated fluid secretion. In the intestinal motility model, D5 significantly delayed intestinal peristalsis in mice. Our research suggests that CFTR and CaCC-mediated intestinal epithelial Cl- secretion inhibiting and gastrointestinal motility delaying may account for the anti-diarrheal activity of B. rhizoma.

  15. Investigating migration inhibition and apoptotic effects of Fomitopsis pinicola chloroform extract on human colorectal cancer SW-480 cells.

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    Yaqin Wang

    Full Text Available BACKGROUND: Fomitopsis pinicola (Sw. Ex Fr.m Karst (FPK which belongs to the Basidiomycota fungal class is one of the most popular medical fungi in China. It has been used for many diseases: cancer, heart diseases, diabetes and so on. However, little study on the pro-apoptotic effect and migration inhibition of FPK chloroform extract (FPKc has been reported and the possible involved mechanism has not been illuminated. METHODOLOGY/PRINCIPAL FINDINGS: Chemical analysis was performed by HPLC which showed ergosterol (ES concentration was 105 µg/mg. MTT assay revealed that FPKc could selectively inhibit SW-480 cells viability with the IC50 of 190.28 µg/ml. Wound healing and transwell assay indicated that FPKc could inhibit the migration of SW-480 cells obviously, FPKc could also dramatically decreased the matrix metalloproteinases-2, 9 (MMP-2 and MMP-9 expression. Annexin V-FITC/PI staining, nuclear Hoechst 33342 staining and DNA fragmentation analysis revealed that FPKc and ES could induce SW-480 cells apoptosis. The apoptosis process closely involved in ROS accumulation and depletion of GSH, activation of caspase 3, poly (ADP-ribose polymerase (PARP degradation. FPKc could also up-regulate P53 expression and thus lead to G1 phase arrest. When SW-480 cells were pretreated with N-acetylcysteine (NAC, the ROS generation, cell viability and apoptotic ratio were partially declined, which indicated that ROS was vertical in the pro-apoptosis process induced by FPKc. Moreover, in the whole process, ES which has been previously found in FPKc had the similar effect to FPKc. Thus we could conclude that ES, as one of the highest abundant components in FPKc, might also be one of the active constituents. CONCLUSION/SIGNIFICANCE: FPKc could inhibit the migration of SW-480 cells, induce SW-480 cells G1 phase arrest and cause ROS-mediated apoptosis effect. And ES might be one of the effective constituents in the whole process.

  16. Inhibition of proliferation of osteosarcoma by nano calcium phosphates:potential hard tissue repair after tumor extraction

    Institute of Scientific and Technical Information of China (English)

    HU Qinghong; CAI Yurong; SHI Zbongli; YAN Weiqi; TANG Ruikang

    2007-01-01

    Spherical- or cylindrical-shaped nanosized cal-cium phosphate particles are considered as an integral part of biological hard tissues such as bone and tooth enamel.Thes ize effects of these nanoparticles were evaluated by cocultur-ing osteosarcoma (U2OS) cells on their films or in their aque-ous suspensions.Experimental results demonstrated that these nanophase minerals could inhibit the proliferations of U2OS significantly.The effects were increased with decreas-ing particle sizes,and the 20-nm sized calcium phosphate,the basic building blocks during bone/enamel formations,was the most effective inhibitor.The particle size is believed to play an important role on cellular behaviors and this in vitro study suggested the potential of calcium phosphate nanopar-ticles for use in therapeutic replacement and reconstruction of bone merits after tumor extractions.

  17. INHIBITION OF COXACKIE VIRUS B3 IN MICE USING METHANOLIC EXTRACT OF CALLIANDRA HAEMATOCEPHALA

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    Mohamed Shaheen

    2014-12-01

    Full Text Available Coxsackie virus B3 (CVB3 represents current major threats to public health and considers as an important viral pathogen related to viral myocarditis. We determined the safety of methanolic extract of Calliandra haematocephala in non-infected mice then two safe doses were selected to be evaluated in infected mice with CVB3 by determining the morbidity, mortality, heart to body weight ratio (HW/BW, virus titers in heart tissue. The effect of the extract on the heart tissues and the activities LDH, AST, and CK enzymes in the mice infected with CVB3 were also determined. Our results recorded that the methanolic extract at 100 mg/kg body was safe dose in mice and didn’t shown significant changes in funtions or histological structures of liver and kindey in non-infected mice and therefore we used 100 mg/kg and 50 mg/kg to be evaluated in infected mice with CVB3. We observed that the methaolic extract of Calliandra haematocephala leaves at the two doses decreased the morbidity, mortality, HW/BW, virus titers, necrosis and mononuclear cell infiltration. The levels of LDH, AST, and CK enzymes were also reduced in the treated infected mice compared with those untreated infected mice. This result suggested that the methaolic extract of Calliandra haematocephala may represent a potential antiviral drug to treatment viral myocarditis

  18. Ethanol Extracts of Fresh Davallia formosana (WL1101 Inhibit Osteoclast Differentiation by Suppressing RANKL-Induced Nuclear Factor-κB Activation

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    Tzu-Hung Lin

    2013-01-01

    Full Text Available The rhizome of Davallia formosana is commonly used to treat bone disease including bone fracture, arthritis, and osteoporosis in Chinese herbal medicine. Here, we report the effects of WL1101, the ethanol extracts of fresh rhizomes of Davallia formosana on ovariectomy-induced osteoporosis. In addition, excess activated bone-resorbing osteoclasts play crucial roles in inflammation-induced bone loss diseases, including rheumatoid arthritis and osteoporosis. In this study, we examined the effects of WL1101 on receptor activator of nuclear factor-κB ligand (RANKL-induced osteoclastogenesis. Treatment with WL1101 significantly inhibited RANKL-stimulated osteoclastogenesis. Two isolated active compounds, ((−-epicatechin or WL14 (4-hydroxy-3-aminobenzoic acid could also inhibit RANKL-induced osteoclastogenesis. WL1101 suppressed the RANKL-induced nuclear factor-κB (NF-κB activation and nuclear translocation, which is the key process during osteoclastogenesis, by inhibiting the activation of IκB kinase (IKK and IκBα. In animal model, oral administration of WL1101 (50 or 200 mg/kg/day effectively decreased the excess bone resorption and significantly antagonized the trabecular bone loss in ovariectomized rats. Our results demonstrate that the ethanol extracts of fresh rhizomes of Davallia formosana inhibit osteoclast differentiation via the inhibition of NF-κB activation and effectively ameliorate ovariectomy-induced osteoporosis. WL1101 may thus have therapeutic potential for the treatment of diseases associated with excessive osteoclastic activity.

  19. Inhibition of prostate cancer cell growth by an avocado extract: role of lipid-soluble bioactive substances.

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    Lu, Qing-Yi; Arteaga, James R; Zhang, Qifeng; Huerta, Sergio; Go, Vay Liang W; Heber, David

    2005-01-01

    Although the avocado is known as a rich source of monounsaturated fatty acids, there has been far less attention given to its content of other bioactive substances including carotenoids, which might contribute to cancer preventive properties similar to those attributed to other fruits and vegetables. The yellow-green color of the avocado prompted us to study the carotenoid content of this fruit using established methods in our laboratory. The California Hass avocado (Persea americana Mill.) was selected for study, because it is the most commonly consumed variety in the southwest United States. These avocados were found to contain the highest content of lutein among commonly eaten fruits as well as measurable amounts of related carotenoids (zeaxanthin, alpha-carotene, and beta-carotene). Lutein accounted for 70% of the measured carotenoids, and the avocado also contained significant quantities of vitamin E. An acetone extract of avocado containing these carotenoids and tocopherols was shown to inhibit the growth of both androgen-dependent (LNCaP) and androgen-independent (PC-3) prostate cancer cell lines in vitro. Incubation of PC-3 cells with the avocado extract led to G(2)/M cell cycle arrest accompanied by an increase in p27 protein expression. Lutein alone did not reproduce the effects of the avocado extract on cancer cell proliferation. In common with other colorful fruits and vegetables, the avocado contains numerous bioactive carotenoids. Because the avocado also contains a significant amount of monounsaturated fat, these bioactive carotenoids are likely to be absorbed into the bloodstream, where in combination with other diet-derived phytochemicals they may contribute to the significant cancer risk reduction associated with a diet of fruits and vegetables.

  20. Emblica officinalis extract induces autophagy and inhibits human ovarian cancer cell proliferation, angiogenesis, growth of mouse xenograft tumors.

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    Alok De

    Full Text Available Patients with ovarian cancer (OC may be treated with surgery, chemotherapy and/or radiation therapy, although none of these strategies are very effective. Several plant-based natural products/dietary supplements, including extracts from Emblicaofficinalis (Amla, have demonstrated potent anti-neoplastic properties. In this study we determined that Amla extract (AE has anti-proliferative effects on OC cells under both in vitro and in vivo conditions. We also determined the anti-proliferative effects one of the components of AE, quercetin, on OC cells under in vitro conditions. AE did not induce apoptotic cell death, but did significantly increase the expression of the autophagic proteins beclin1 and LC3B-II under in vitro conditions. Quercetin also increased the expression of the autophagic proteins beclin1 and LC3B-II under in vitro conditions. AE also significantly reduced the expression of several angiogenic genes, including hypoxia-inducible factor 1α (HIF-1α in OVCAR3 cells. AE acted synergistically with cisplatin to reduce cell proliferation and increase expression of the autophagic proteins beclin1 and LC3B-II under in vitro conditions. AE also had anti-proliferative effects and induced the expression of the autophagic proteins beclin1 and LC3B-II in mouse xenograft tumors. Additionally, AE reduced endothelial cell antigen - CD31 positive blood vessels and HIF-1α expression in mouse xenograft tumors. Together, these studies indicate that AE inhibits OC cell growth both in vitro and in vivo possibly via inhibition of angiogenesis and activation of autophagy in OC. Thus AE may prove useful as an alternative or adjunct therapeutic approach in helping to fight OC.

  1. Inhibition of cholesterol oxidation products (COPs) formation in emulsified porcine patties by phenolic-rich avocado (Persea americana Mill.) extracts.

    Science.gov (United States)

    Rodríguez-Carpena, Javier-Germán; Morcuende, David; Petrón, María Jesus; Estévez, Mario

    2012-03-07

    The effect of phenolic-rich extracts from avocado peel on the formation of cholesterol oxidation products (COPs) in porcine patties subjected to cooking and chill storage was studied. Eight COPs (7α-hydroxycholesterol, 7β-hydroxycholesterol, 7-ketocholesterol, 20α-hydroxycholesterol, 25-hydroxycholesterol, cholestanetriol, 5,6β-epoxycholesterol, and 5,6α-epoxycholesterol) were identified and quantified by GC-MS. The addition of avocado extracts (∼600 GAE/kg patty) to patties significantly inhibited the formation of COPs during cooking. Cooked control (C) patties contained a larger variety and greater amounts of COPs than the avocado-treated (T) counterparts. COPs sharply increased in cooked patties during the subsequent chilled storage. This increase was significantly higher in C patties than in the T patties. Interestingly, the amount of COPs in cooked and chilled T patties was similar to those found in cooked C patties. The mechanisms implicated in cholesterol oxidation in a processed meat product, the protective effect of avocado phenolics, and the potential implication of lipid and protein oxidation are thoroughly described in the present paper.

  2. Rhubarb tannins extract inhibits the expression of aquaporins 2 and 3 in magnesium sulphate-induced diarrhoea model.

    Science.gov (United States)

    Liu, Chunfang; Zheng, Yanfang; Xu, Wen; Wang, Hui; Lin, Na

    2014-01-01

    Tannins, a group of major active components of Chinese rhubarb and widely distributed in nature, have a significant antidiarrhoeal activity. Aquaporins (AQPs) 2 and 3 play important roles in regulating water transfer during diarrhoea. The present study aims to determine the effect of the total tannins extract of rhubarb on aquaporins (AQPs) 2 and 3 in diarrhoea mice and HT-29 cells both induced by magnesium sulphate (MgSO4). Our results showed that rhubarb tannins extract (RTE) significantly decreased the faecal water content in colon and evaluation index of defecation of diarrhoea mice. Interestingly, RTE could markedly reduce the mRNA and protein expression levels of AQPs 2 and 3 in apical and lateral mucosal epithelial cells in the colons of diarrhoea mice and HT-29 cells both induced by MgSO4 in a dose-dependent manner. Furthermore, RTE suppressed the production of cyclic monophosphate- (cAMP-) dependent protein kinase A catalytic subunits α (PKA C-α) and phosphorylated cAMP response element-binding protein (p-CREB, Ser133) in MgSO4-induced HT-29 cells. Our data showed for the first time that RTE inhibit AQPs 2 and 3 expression in vivo and in vitro via downregulating PKA/p-CREB signal pathway, which accounts for the antidiarrhoeal effect of RTE.

  3. Traditional Preparations and Methanol Extracts of Medicinal Plants from Papua New Guinea Exhibit Similar Cytochrome P450 Inhibition

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    Erica C. Larson

    2016-01-01

    Full Text Available The hypothesis underlying this current work is that fresh juice expressed from Papua New Guinea (PNG medicinal plants (succus will inhibit human Cytochrome P450s (CYPs. The CYP inhibitory activity identified in fresh material was compared with inhibition in methanol extracts of dried material. Succus is the most common method of traditional medicine (TM preparation for consumption in PNG. There is increasing concern that TMs might antagonize or complicate drug therapy. We have previously shown that methanol extracts of commonly consumed PNG medicinal plants are able to induce and/or inhibit human CYPs in vitro. In this current work plant succus was prepared from fresh plant leaves. Inhibition of three major CYPs was determined using human liver microsomes and enzyme-selective model substrates. Of 15 species tested, succus from 6/15 was found to inhibit CYP1A2, 7/15 inhibited CYP3A4, and 4/15 inhibited CYP2D6. Chi-squared tests determined differences in inhibitory activity between succus and methanol preparations. Over 80% agreement was found. Thus, fresh juice from PNG medicinal plants does exhibit the potential to complicate drug therapy in at risk populations. Further, the general reproducibility of these findings suggests that methanol extraction of dried material is a reasonable surrogate preparation method for fresh plant samples.

  4. Mechanisms underlying the anti-inflammatory effects of Clinacanthus nutans Lindau extracts: inhibition of cytokine production and Toll-like receptor-4 activation

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    Chun Wai eMai

    2016-02-01

    Full Text Available Clinacanthus nutans has had a long history of use in folk medicine in Malaysia and Southeast Asia; mostly in the relief of inflammatory conditions. In this study, we investigated the effects of different extracts of C. nutans upon lipopolysaccharide (LPS induced inflammation in order to identify its mechanism of action. Extracts of leaves and stem bark of C. nutans were prepared using polar and non-polar solvents to produce four extracts, namely polar leaf extract (LP, non-polar leaf extract (LN, polar stem extract (SP and non-polar stem extracts (SN. The extracts were standardized by determining its total phenolic and total flavonoid contents. Its anti-inflammatory effects were assessed on LPS induced nitrite release in RAW264.7 macrophages and Toll-like receptor (TLR-4 activation in TLR-4 transfected human embryonic kidney cells (HEK-BlueTM-hTLR4 cells. The levels of inflammatory cytokines (TNF-α, IFN-γ, IL-1β, IL-6, IL-12p40 and IL-17 in treated RAW264.7 macrophages were quantified to verify its anti-inflammatory effects. Western blotting was used to investigate the effect of the most potent extract (LP on TLR-4 related inflammatory proteins (p65, p38, ERK, JNK, IRF3 in RAW264.7 macrophages. All four extracts produced a significant, concentration-dependent reduction in LPS-stimulated nitric oxide, LPS-induced TLR-4 activation in HEK-BlueTM-hTLR4 cells and LPS-stimulated cytokines production in RAW264.7 macrophages. The most potent extract, LP, also inhibited all LPS-induced TLR-4 inflammatory proteins. These results provide a basis for understanding the mechanisms underlying the previously demonstrated anti-inflammatory activity of C. nutans extracts.

  5. Mechanisms Underlying the Anti-Inflammatory Effects of Clinacanthus nutans Lindau Extracts: Inhibition of Cytokine Production and Toll-Like Receptor-4 Activation.

    Science.gov (United States)

    Mai, Chun W; Yap, Kok S I; Kho, Mee T; Ismail, Nor H; Yusoff, Khatijah; Shaari, Khozirah; Chin, Swee Y; Lim, Erin S H

    2016-01-01

    Clinacanthus nutans has had a long history of use in folk medicine in Malaysia and Southeast Asia; mostly in the relief of inflammatory conditions. In this study, we investigated the effects of different extracts of C. nutans upon lipopolysaccharide (LPS) induced inflammation in order to identify its mechanism of action. Extracts of leaves and stem bark of C. nutans were prepared using polar and non-polar solvents to produce four extracts, namely polar leaf extract (LP), non-polar leaf extract (LN), polar stem extract (SP), and non-polar stem extracts (SN). The extracts were standardized by determining its total phenolic and total flavonoid contents. Its anti-inflammatory effects were assessed on LPS induced nitrite release in RAW264.7 macrophages and Toll-like receptor (TLR-4) activation in TLR-4 transfected human embryonic kidney cells (HEK-Blue(TM)-hTLR4 cells). The levels of inflammatory cytokines (TNF-α, IFN-γ, IL-1β, IL-6, IL-12p40, and IL-17) in treated RAW264.7 macrophages were quantified to verify its anti-inflammatory effects. Western blotting was used to investigate the effect of the most potent extract (LP) on TLR-4 related inflammatory proteins (p65, p38, ERK, JNK, IRF3) in RAW264.7 macrophages. All four extracts produced a significant, concentration-dependent reduction in LPS-stimulated nitric oxide, LPS-induced TLR-4 activation in HEK-Blue(TM)-hTLR4 cells and LPS-stimulated cytokines production in RAW264.7 macrophages. The most potent extract, LP, also inhibited all LPS-induced TLR-4 inflammatory proteins. These results provide a basis for understanding the mechanisms underlying the previously demonstrated anti-inflammatory activity of C. nutans extracts.

  6. Inhibition of lipid peroxidation by extracts/subfractions of Chickrassy ( Chukrasia tabularis A. Juss.)

    Science.gov (United States)

    Kaur, Rajbir; Thind, Tarunpreet Singh; Singh, Bikram; Arora, Saroj

    2009-01-01

    Polyphenols and polyphenol-rich fractions of plants have been reported to have protective effects against lipid peroxidation, most probably by serving as scavengers of free radicals and/or by chelating metal ions. In the present study, the effect of different extracts/subfractions of Chickrassy ( Chukrasia tabularis) on peroxyl radical mediated damage to the polyunsaturated fatty acids was investigated. Liver homogenate was used as experimental material. The production of malondialdehyde served as a marker of lipid peroxidation and oxidative stress. It was observed that polyphenol-rich fractions, particularly the ethyl acetate fractions of bark and leaves, showed the highest protective activity of 83.02% and 88.62% inhibition, respectively. This study will help in knowing the scientific validation of this plant, for its use in ayurvedic formulations.

  7. Bergamot juice extract inhibits proliferation by inducing apoptosis in human colon cancer cells.

    Science.gov (United States)

    Visalli, Giuseppa; Ferlazzo, Nadia; Cirmi, Santa; Campiglia, Pietro; Gangemi, Sebastiano; Di Pietro, Angela; Calapai, Gioacchino; Navarra, Michele

    2014-01-01

    Colorectal cancer (CRC) is a leading cause of cancer mortality in the industrialized world, second to lung cancer. A lot of evidences highlight that a diet rich in fruits and vegetables may reduce the risk of some types of cancer including CRC. In this study we demonstrate that Citrus bergamia juice extracts (BJe) reduces CRC cell growth by multiple mechanisms. Low BJe concentrations inhibit MAPKs pathway and alter apoptosis-related proteins, that in turn induce cell cycle arrest and apoptosis in HT-29 cells. Instead, high concentrations of BJe induce oxidative stress causing DNA damage. Our study highlights the role of BJe as modulator of cell apoptosis in CRC cells and strengthens our previous hypothesis that the flavonoid fraction of bergamot juice may play a role as anti-cancer drug.

  8. Inhibition of quorum sensing in the opportunistic pathogenic bacterium Chromobacterium violaceum by an extract from fruiting bodies of Lingzhi or Reishi medicinal mushroom, Ganoderma lucidum (W.Curt.:Fr.) P. Karst. (higher Basidiomycetes).

    Science.gov (United States)

    Zhu, Hu; Liu, Wei; Tian, Baozhen; Liu, Huijun; Ning, Shoujiao

    2011-01-01

    Extracts of Lingzhi or Reishi medicinal mushroom, Ganoderma lucidum, inhibited quorum sensing in Chromobacterium violaceum CV026. G. lucidum fruiting bodies were milled and extracted with ethyl acetate. The crude extract was dissolved in an appropriate concentration of methanol, sterilized by filtration through a 0.22-μm membrane filter, and added to Ch. Violaceum CV026 cultures, which were used as an indicator to monitor quorum sensing inhibition. Inhibitory activity was measured by quantifying violacein production using a microplate reader. Methanol-soluble compounds extracted from G. lucidum significantly inhibited quorum sensing-controlled behavior in Ch. Violaceum in a concentration-dependent manner. The results suggest that compounds in G. lucidum might be useful to control and handle detrimental infections caused by human, animal, and plant pathogens. Further studies are in progress in our lab to isolate the specific compounds from G. lucidum extract, evaluate them as quorum sensing inhibitors, and analyze their mechanism of action.

  9. Bioguided Fractionation Shows Cassia alata Extract to Inhibit Staphylococcus epidermidis and Pseudomonas aeruginosa Growth and Biofilm Formation

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    Samuel Takashi Saito

    2012-01-01

    Full Text Available Plant extracts have a long history to be used in folk medicine. Cassia alata extracts are known to exert antibacterial activity but details on compounds and mechanism of action remain poorly explored. We purified and concentrated the aqueous leaf extract of C. alata by reverse phase-solid phase extraction and screened the resulting CaRP extract for antimicrobial activity. CaRP extract exhibited antimicrobial activity for Pseudomonas aeruginosa, Staphylococcus epidermidis, S. aureus, and Bacillus subtilis. CaRP also inhibited biofilm formation of S. epidermidis and P. aeruginosa. Several bacterial growth-inhibiting compounds were detected when CaRP extract was fractionated by TLC chromatography coupled to bioautography agar overlay technique. HPLC chromatography of CaRP extract yielded 20 subfractions that were tested by bioautography for antimicrobial activity against S. aureus and S. epidermidis. Five bioactive fractions were detected and chemically characterized, using high-resolution mass spectrometry (qTOF-MS/MS. Six compounds from four fractions could be characterized as kaempferol, kaempferol-O-diglucoside, kaempferol-O-glucoside, quercetin-O-glucoside, rhein, and danthron. In the Salmonella/microsome assay CaRP showed weak mutagenicity (MI<3 only in strain TA98, pointing to a frameshift mutation activity. These results indicate that C. alata leaf extract contains a minimum of 7 compounds with antimicrobial activity and that these together or as single substance are active in preventing formation of bacterial biofilm, indicating potential for therapeutic applications.

  10. Surface functionalization of bioactive glasses with natural molecules of biological significance, part II: Grafting of polyphenols extracted from grape skin

    Science.gov (United States)

    Zhang, Xin; Ferraris, Sara; Prenesti, Enrico; Verné, Enrica

    2013-12-01

    Polyphenols, as one of the most important family of phytochemicals protective substances from grape fruit, possess various biological activities and health-promoting benefits, for example: inhibition of some degenerative diseases, cardiovascular diseases and certain types of cancers, reduction of plasma oxidative stress and slowing aging. The combination of polyphenols and biomaterials may have good potential to reach good bioavailability and controlled release, as well as to give biological signaling properties to the biomaterial surfaces. In this research, conventional solvent extraction was developed for obtaining polyphenols from dry grape skins. The Folin&Ciocalteu method was used to determine the amount of total polyphenols in the extracts. Surface functionalization of two bioactive glasses (SCNA and CEL2) was performed by grafting the extracted polyphenols on their surfaces. The effectiveness of the functionalization was tested by UV spectroscopy, which analyzes the amount of polyphenols in the uptake solution (before and after functionalization) and on solid samples, and XPS, which analyzes the presence of phenols on the material surface.

  11. Inhibitory effects of brown algae extracts on histamine production in mackerel muscle via inhibition of growth and histidine decarboxylase activity of Morganella morganii.

    Science.gov (United States)

    Kim, Dong Hyun; Kim, Koth Bong Woo Ri; Cho, Ji Young; Ahn, Dong Hyun

    2014-04-01

    This study was performed to investigate the inhibitory effects of brown algae extracts on histamine production in mackerel muscle. First, antimicrobial activities of brown algae extracts against Morganella morganii were investigated using a disk diffusion method. An ethanol extract of Ecklonia cava (ECEE) exhibited strong antimicrobial activity. The minimum inhibitory concentration (MIC) of ECEE was 2 mg/ml. Furthermore, the brown algae extracts were examined for their ability to inhibit crude histidine decarboxylase (HDC) of M. morganii. The ethanol extract of Eisenia bicyclis (EBEE) and ECEE exhibited significant inhibitory activities (19.82% and 33.79%, respectively) at a concentration of 1 mg/ml. To obtain the phlorotannin dieckol, ECEE and EBEE were subjected to liquid-liquid extraction, silica gel column chromatography, and HPLC. Dieckol exhibited substantial inhibitory activity with an IC50 value of 0.61 mg/ml, and exhibited competitive inhibition. These extracts were also tested on mackerel muscle. The viable cell counts and histamine production in mackerel muscle inoculated with M. morganii treated with ≥2.5 MIC of ECEE (weight basis) were highly inhibited compared with the untreated sample. Furthermore, treatment of crude HDC-inoculated mackerel muscle with 0.5% ECEE and 0.5% EBEE (weight basis), which exhibited excellent inhibitory activities against crude HDC, reduced the overall histamine production by 46.29% and 56.89%, respectively, compared with the untreated sample. Thus, these inhibitory effects of ECEE and EBEE should be helpful in enhancing the safety of mackerel by suppressing histamine production in this fish species.

  12. Siegesbeckia orientalis Extract Inhibits TGFβ1-Induced Migration and Invasion of Endometrial Cancer Cells

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    Chi-Chang Chang

    2016-08-01

    Full Text Available Type II endometrial carcinoma typically exhibits aggressive metastasis and results in a poor prognosis. Siegesbeckia orientalis Linne is a traditional Chinese medicinal herb with several medicinal benefits, including the cytotoxicity against various cancers. This study investigates the inhibitory effects of S. orientalis ethanol extract (SOE on the migration and invasion of endometrial cancer cells, which were stimulated by transforming growth factor β (TGFβ. The inhibitory effects were evaluated by determining wound healing and performing the Boyden chamber assay. This study reveals that SOE can inhibit TGFβ1-induced cell wound healing, cell migration, and cell invasion in a dose-dependent manner in RL95-2 and HEC-1A endometrial cancer cells. SOE also reversed the TGFβ1-induced epithelial-mesenchymal transition, including the loss of the cell-cell junction and the lamellipodia-like structures. Western blot analysis revealed that SOE inhibited the phosphorylation of ERK1/2, JNK1/2, and Akt, as well as the expression of MMP-9, MMP-2, and u-PA in RL95-2 cells dose-dependently. The results of this investigation suggest that SOE is a potential anti-metastatic agent against human endometrial tumors.

  13. Curcumin and Boswellia serrata gum resin extract inhibit chikungunya and vesicular stomatitis virus infections in vitro.

    Science.gov (United States)

    von Rhein, Christine; Weidner, Tatjana; Henß, Lisa; Martin, Judith; Weber, Christopher; Sliva, Katja; Schnierle, Barbara S

    2016-01-01

    Chikungunya virus (CHIKV) is a mosquito-transmitted alphavirus that causes chikungunya fever and has infected millions of people mainly in developing countries. The associated disease is characterized by rash, high fever, and severe arthritis that can persist for years. CHIKV has adapted to Aedes albopictus, which also inhabits temperate regions including Europe and the United States of America. CHIKV has recently caused large outbreaks in Latin America. No treatment or licensed CHIKV vaccine exists. Traditional medicines are known to have anti-viral effects; therefore, we examined whether curcumin or Boswellia serrata gum resin extract have antiviral activity against CHIKV. Both compounds blocked entry of CHIKV Env-pseudotyped lentiviral vectors and inhibited CHIKV infection in vitro. In addition, vesicular stomatitis virus vector particles and viral infections were also inhibited to the same extent, indicating a broad antiviral activity. Although the bioavailability of these compounds is rather poor, they might be used as a lead structure to develop more effective antiviral drugs or might be used topically to prevent CHIKV spread in the skin after mosquito bites.

  14. Ethanol extract of Elaeocarpus petiolatus inhibits lipopolysaccharide-induced inflammation in macrophage cells.

    Science.gov (United States)

    Kwon, Ok-Kyoung; Ahn, Kyung-Seop; Park, Ji-Won; Jang, Ha-Young; Joung, Hyouk; Lee, Hyeong-Kyu; Oh, Sei-Ryang

    2012-04-01

    Elaeocarpus petiolatus is known to exert active oxygen scavenging, anti-aging, and whitening actions. However, the biological effects of E. petiolatus on inflammation and the underlying mechanisms are yet to be established. In the present study, we investigated the anti-inflammatory effects of the ethanol extract from E. petiolatus (EPE) bark in murine Raw264.7 macrophages stimulated with lipopolysaccharide (LPS). EPE inhibited the production of PGE(2), TNF-α, and IL-1β in a dose-dependent manner in Raw264.7 cells stimulated with LPS. The decrease in PGE(2) production was correlated with reduced COX-2 expression. Furthermore, EPE suppressed the phosphorylation of extracellular signal-related kinases (ERK), c-Jun N-terminal kinase (JNK), and p38 as well as translocation of the NF-κB p65 subunit from the cytosol to nucleus. Our results suggest that EPE exerts anti-inflammatory activity through inhibition of inflammatory mediators, such as PGE(2), TNF-α, and IL-1β, and downregulation of COX-2 via suppression of NF-κB translocation and phosphorylation of ERK, JNK, and p38 in LPS-stimulated Raw264.7 cells.

  15. The Extract of Rhodobacter sphaeroides Inhibits Melanogenesis through the MEK/ERK Signaling Pathway

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    Chen-Hsun Liu

    2013-06-01

    Full Text Available Reducing hyperpigmentation has been a big issue for years. Even though pigmentation is a normal mechanism protecting skin from UV-causing DNA damage and oxidative stress, it is still an aesthetic problem for many people. Bacteria can produce some compounds in response to their environment. These compounds are widely used in cosmetic and pharmaceutical applications. Some probiotics have immunomodulatory activities and modulate the symptoms of several diseases. Previously, we found that the extracts of Rhodobacter sphaeroides (Lycogen™ inhibited nitric oxide production and inducible nitric-oxide synthase expression in activated macrophages. In this study, we sought to investigate an anti-melanogenic signaling pathway in α-melanocyte stimulating hormone (α-MSH-treated B16F10 melanoma cells and zebrafish. Treatment with Lycogen™ inhibited the cellular melanin contents and expression of melanogenesis-related protein, including microphthalmia-associated transcription factor (MITF and tyrosinase in B16F10 cells. Moreover, Lycogen™ reduced phosphorylation of MEK/ERK without affecting phosphorylation of p38. Meanwhile, Lycogen™ decreased zebrafish melanin expression in a dose-dependent manner. These findings establish Lycogen™ as a new target in melanogenesis and suggest a mechanism of action through the ERK signaling pathway. Our results suggested that Lycogen™ may have potential cosmetic usage in the future.

  16. Results of a screening programme to identify plants or plant extracts that inhibit ruminal protein degradation.

    Science.gov (United States)

    Selje, N; Hoffmann, E M; Muetzel, S; Ningrat, R; Wallace, R J; Becker, K

    2007-07-01

    One aim of the EC Framework V project, 'Rumen-up' (QLK5-CT-2001-00 992), was to find plants or plant extracts that would inhibit the nutritionally wasteful degradation of protein in the rumen. A total of 500 samples were screened in vitro using 14C-labelled casein in a 30-min incubation with ruminal digesta. Eight were selected for further investigation using a batch fermentation system and soya protein and bovine serum albumin as proteolysis substrates; proteolysis was monitored over 12 h by the disappearance of soluble protein and the production of branched SCFA and NH3. Freeze-dried, ground foliage of Peltiphyllum peltatum, Helianthemum canum, Arbutus unedo, Arctostaphylos uva-ursi and Knautia arvensis inhibited proteolysis (P fermentation. The effects showed some resemblance to those obtained in parallel incubations containing 3 mum-monensin, suggesting that K. arvensis may be a plant-derived feed additive that can suppress growth and activity of key proteolytic ruminal micro-organisms in a manner similar to that already well known for monensin.

  17. Ampelopsis brevipedunculata Extract Prevents Bone Loss by Inhibiting Osteoclastogenesis in Vitro and in Vivo

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    Ju-Young Kim

    2014-11-01

    Full Text Available Osteoclasts play a critical role in bone resorbing disorders such as osteoporosis, periodontitis, and rheumatoid arthritis. Therefore, discovery of agents capable of suppressing osteoclast differentiation may aid the development of a therapeutic access for the treatment of pathological bone loss. Ampelopsis brevipedunculata has been used as herbal folk medicine to treat liver diseases and inflammation in Asia. However, its effects on osteoclast differentiation are unknown. We were aimed to investigate the anti-osteoclastogenic activity in vitro and in vivo and to elucidate the underlying mechanism of Ampelopsis brevipedunculata extract (ABE. In this study, ABE inhibited receptor activator of NF-κB ligand (RANKL-induced osteoclast differentiation, the formation of filamentous actin rings and the bone resorbing activity of mature osteoclasts. ABE inhibited RANKL-induced p38 and IκB phosphorylation and IκB degradation. Also, ABE suppressed the mRNA and protein expression of nuclear factor of activated T cells c1 (NFATc1 and c-Fos, and the mRNA expression of genes required for cell fusion and bone resorption, such as osteoclast-associated receptor (OSCAR, tartrate resistant acid phosphatase (TRAP, cathepsin K, dendritic cell-specific transmembrane protein (DC-STAMP, β3-integrin and osteoclast stimulatory transmembrane protein (OC-STAMP. Furthermore, results of micro-CT and histologic analysis indicated that ABE remarkably prevented lipopolysaccharide (LPS-induced bone erosion. These results demonstrate that ABE prevents LPS-induced bone erosion through inhibition of osteoclast differentiation and function, suggesting the promise of ABE as a potential cure for various osteoclast-associated bone diseases.

  18. Corrosion inhibition of Eleusine aegyptiaca and Croton rottleri leaf extracts on cast iron surface in 1 M HCl medium

    Science.gov (United States)

    Rajeswari, Velayutham; Kesavan, Devarayan; Gopiraman, Mayakrishnan; Viswanathamurthi, Periasamy; Poonkuzhali, Kaliyaperumal; Palvannan, Thayumanavan

    2014-09-01

    The adsorption and corrosion inhibition activities of Eleusine aegyptiaca (E. aegyptiaca) and Croton rottleri (C. rottleri) leaf extracts on cast iron corrosion in 1 M hydrochloric acid solution were studied first time by weight loss and electrochemical techniques viz., Tafel polarization and electrochemical impedance spectroscopy. The results obtained from the weight loss and electrochemical methods showed that the inhibition efficiency increased with inhibitor concentrations. It was found that the extracts acted as mixed-type inhibitors. The addition of halide additives (KCl, KBr, and KI) on the inhibition efficiency has also been investigated. The adsorption of the inhibitors on cast iron surface both in the presence and absence of halides follows the Langmuir adsorption isotherm model. The inhibiting nature of the inhibitors was supported by FT-IR, UV-vis, Wide-angle X-ray diffraction and SEM methods.

  19. Allelopathic inhibition on red tide microalgae Skeletonema costatum by five macroalgal extracts

    Institute of Scientific and Technical Information of China (English)

    Zhen AN; Zhenyu WANG; Fengmin LI; Zhijia TIAN; Hongying HU

    2008-01-01

    This study aims to identify effective antialgal allelochemicals from marine macroalgae that inhibit the growth of red tide-,microalgae. Practically, new algicidal agents were developed to control red tide. The growth inhibitory effects of 5 marinemacroalgae Porphyra tenera, Laminaria japonica, Ulva pertusa, Enteromorpha cla- thrata, and Undaria pinnatifida on Skeletonema costatum were evaluated by adding crude seawater extracts of macroalgal dry tissue into the culture medium containing S. costatum. The half-effective concentrations at 120 h (EC50, 120h) of the seawater extracts were 0.6, 0.9, 1.0, 1.0, and 4.7 g/L for the five macroalgae above, respect-ively. E. clathrata, L. japonica and U. pertusa showed strong allelopathic effect on the growth of S. costatum. There have been no previous reports with regard to the allelopathic effects of the former two macroalgae so far. The possible allelochemicals of 21 compounds of the E. clathrata were detected using Gas chromatography-mass spectrometry (GC-MS) analysis. Unsaturated fatty acids, acrylic acid (C3H4O2), and linolenic acid (C18H30O2) were the most likely allelochemicals in E. clathrata.

  20. Inhibition of 12/15 lipoxygenase by curcumin and an extract from Curcuma longa L.

    Science.gov (United States)

    Bezáková, Lýdia; Košťálová, Daniela; Obložinský, Marek; Hoffman, Peter; Pekárová, Mária; Kollárová, Renáta; Holková, Ivana; Mošovská, Silvia; Sturdík, Ernest

    2014-02-01

    Curcumin (diferuloylmethane) is an orange-yellow secondary metabolic compound from the rhizome of turmeric (Curcuma longa L.), a spice often found in curry powder. It is one of the major curcuminoids of turmeric. For centuries, curcumin has been used in some medicinal preparations or as a food colouring agent. A variety of enzymes that are closely associated with inflammation and cancer were found to be modulated by curcumin. This paper summarized the results of the inhibitory effect of curcumin and a Curcuma longa L. ethanolic extract on lipoxygenase from the rat lung cytosolic fraction. The positional specificity determination of arachidonic acid dioxygenation by RP- and SP-HPLC methods showed that in a purified enzyme preparation from the rat lung cytosol the specific form of lipoxygenase (LOX) is present exhibiting 12/15-LOX dual specificity (with predominant 15-LOX activity). The inhibitory activity of curcumin and Curcuma longa extract on LOX from cytosolic fraction of rat lung was expressed in the percentage of inhibition and as IC50. Lineweaver-Burk plot analysis has indicated that curcumin is the competitive inhibitor of 12/15 LOX from the rat lung cytosolic fraction.

  1. Moringa oleifera aqueous leaf extract inhibits reducing monosaccharide-induced protein glycation and oxidation of bovine serum albumin.

    Science.gov (United States)

    Nunthanawanich, Pornpimon; Sompong, Weerachat; Sirikwanpong, Sukrit; Mäkynen, Kittana; Adisakwattana, Sirichai; Dahlan, Winai; Ngamukote, Sathaporn

    2016-01-01

    Advanced glycation end products (AGEs) play an important factor for pathophysiology of diabetes and its complications. Moringa oleifera is one of the medicinal plants that have anti-hyperglycemic activity. However, anti-glycation property of Moringa oleifera leaf extract on the different types of reducing monosaccharides-induced protein glycation has not been investigated. Therefore, the aim of this study was to examine the protective effect of Moringa oleifera aqueous leaf extract (MOE) on reducing sugars-induced protein glycation and protein oxidation. Total phenolic content of MOE was measured using the Folin-Ciocalteu method. Bovine serum albumin was incubated with 0.5 M of reducing sugars (glucose or fructose) with or without MOE (0.5-2.0 mg/mL) for 1, 2, 3 and 4 weeks. The results found that total phenolic content was 38.56 ± 1.50 mg gallic acid equivalents/g dry extract. The formation of fluorescent and non-fluorescent AGEs [N (ε)-(carboxymethyl) lysine (CML)] and the level of fructosamine were determined to indicate protein glycation, whereas the level of protein carbonyl content and thiol group were examined for protein oxidation. MOE (0.5-2.0 mg/mL) significantly inhibited the formation of fluorescent, N (ε)-CML and markedly decreased fructosamine level (P < 0.05). Moreover, MOE significantly prevented protein oxidation manifested by reducing protein carbonyl and the depletion of protein thiol in a dose-dependent manner (P < 0.05). Thus, the findings indicated that polyphenols containing in MOE have high potential for decreasing protein glycation and protein oxidation that may delay or prevent AGE-related diabetic complications.

  2. Extracting biologically significant patterns from short time series gene expression data

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    McGinnis Thomas

    2009-08-01

    Full Text Available Abstract Background Time series gene expression data analysis is used widely to study the dynamics of various cell processes. Most of the time series data available today consist of few time points only, thus making the application of standard clustering techniques difficult. Results We developed two new algorithms that are capable of extracting biological patterns from short time point series gene expression data. The two algorithms, ASTRO and MiMeSR, are inspired by the rank order preserving framework and the minimum mean squared residue approach, respectively. However, ASTRO and MiMeSR differ from previous approaches in that they take advantage of the relatively few number of time points in order to reduce the problem from NP-hard to linear. Tested on well-defined short time expression data, we found that our approaches are robust to noise, as well as to random patterns, and that they can correctly detect the temporal expression profile of relevant functional categories. Evaluation of our methods was performed using Gene Ontology (GO annotations and chromatin immunoprecipitation (ChIP-chip data. Conclusion Our approaches generally outperform both standard clustering algorithms and algorithms designed specifically for clustering of short time series gene expression data. Both algorithms are available at http://www.benoslab.pitt.edu/astro/.

  3. Buddleja officinalis Maximowicz Extract Inhibits Lipid Accumulation on Adipocyte Differentiation in 3T3-L1 Cells and High-Fat Mice

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    Jin-Kyu Kim

    2012-07-01

    Full Text Available Obesity is a global health problem. It is also known to be a risk factor for the development of metabolic disorders, type 2 diabetes, systemic hypertension, cardiovascular disease, dyslipidemia, and atherosclerosis. In this study, we elucidated that Buddleja officinalis Maximowicz extract significantly inhibited lipid accumulation during 3T3-L1 adipocyte differentiation. Furthermore, Buddleja officinalis Maximowicz extract reduced the body weight gain induced through feeding a high-fat diet to C57BL/6 mice. The treatment of Buddleja officinalis Maximowicz extract significantly reduced the adipose tissue weight to 2.7/100 g of body weight in high-fat mice. When their adipose tissue morphology was investigated for histochemical staining, the distribution of cell size in the high-fat diet groups was hypertrophied compared with those from Buddleja officinalis Maximowicz extract-treated mice. In addition, in Buddleja officinalis Maximowicz extract-treated mice, a significant reduction of serum triglyceride and T-cholesterol was observed at to 21% and 17%, respectively. The discovery of bioactive compounds from diet or dietary supplementation is one of possible ways to control obesity and to prevent or reduce the risks of various obesity-related diseases. These results support that Buddleja officinalis Maximowicz extract is expected to create the therapeutic interest with respect to the treatment of obesity.

  4. Corrosion inhibition of mild steel in 1 M HCl solution by henna extract: A comparative study of the inhibition by henna and its constituents (Lawsone, Gallic acid, {alpha}-D-Glucose and Tannic acid)

    Energy Technology Data Exchange (ETDEWEB)

    Ostovari, A. [Technical Inspection Engineering Department, Petroleum University of Technology, Abadan (Iran, Islamic Republic of)], E-mail: A.Ostovari@gmail.com; Hoseinieh, S.M.; Peikari, M. [Technical Inspection Engineering Department, Petroleum University of Technology, Abadan (Iran, Islamic Republic of); Shadizadeh, S.R. [Petroleum Engineering Department, Petroleum University of Technology, Abadan (Iran, Islamic Republic of); Hashemi, S.J. [Technical Inspection Engineering Department, Petroleum University of Technology, Abadan (Iran, Islamic Republic of)

    2009-09-15

    The inhibitive action of henna extract (Lawsonia inermis) and its main constituents (lawsone, gallic acid, {alpha}-D-Glucose and tannic acid) on corrosion of mild steel in 1 M HCl solution was investigated through electrochemical techniques and surface analysis (SEM/EDS). Polarization measurements indicate that all the examined compounds act as a mixed inhibitor and inhibition efficiency increases with inhibitor concentration. Maximum inhibition efficiency (92.06%) is obtained at 1.2 g/l henna extract. Inhibition efficiency increases in the order: lawsone > henna extract > gallic acid > {alpha}-D-Glucose > tannic acid. Also, inhibition mechanism and thermodynamic parameters are discussed.

  5. Inhibition of AKT signaling by supercritical CO2 extract of mango ginger (Curcuma amada Roxb.) in human glioblastoma cells.

    Science.gov (United States)

    Ramachandran, Cheppail; Portalatin, Gilda; Quirin, Karl-W; Escalon, Enrique; Khatib, Ziad; Melnick, Steven J

    2015-12-01

    Mango ginger (Curcuma amada Roxb.) is a less-investigated herb for anticancer properties than other related Curcuma species. AKT (a serine/threonine protein kinase B, originally identified as an oncogene in the transforming retrovirus AKT8) plays a central role in the development and promotion of cancer. In this investigation, we have analyzed the effect of supercritical CO2 extract of mango ginger (CA) on the genetic pathways associated with AKT signaling in human glioblastoma cells. The inhibitory effect of supercritical CO2 extract of mango ginger (Curcuma amada) on AKT signaling was investigated in U-87MG glioblastoma cells. CA was highly cytotoxic to glioblastoma cell line (IC50=4.92±0.81 µg/mL) compared to mHypoE-N1 normal mouse hypothalamus cell line (IC50=40.57±0.06 µg/mL). CA inhibits AKT (protein Kinase B) and adenosine monophophate -activated protein kinase α (AMPKα) phosphorylation significantly in a dose-dependent manner. The cell migration which is necessary for invasion and metastasis was also inhibited by CA treatment, with about 43% reduction at 20 µg/mL concentration. Analysis of mRNA and protein expression of genes associated with apoptosis, cell proliferation and angiogenesis showed that CA modulates expression of genes associated with apoptosis (Bax, Bcl-2, Bcl-X, BNIP3, caspase-3, mutant p53 and p21), cell proliferation (Ki67) and angiogenesis vascular endothelial growth factor (VEGF). Additionally, heat shock protein 90 (HSP90) and AMPKα genes interacting with the AKT signaling pathway were also downregulated by CA treatment. These results indicate the molecular targets and mechanisms underlying the anticancer effect of CA in human glioblastoma cells.

  6. Cortex cinnamomi extract prevents streptozotocin- and cytokine-induced β-cell damage by inhibiting NF-κB

    Institute of Scientific and Technical Information of China (English)

    Kang-Beom Kwon; Eun-Kyung Kim; Eun-Sil Jeong; Young-Hoon Lee; Young-Rae Lee; Jin-Woo Park; Do-Gon Ryu; Byung-Hyun Park

    2006-01-01

    AIM: To clarify the mechanism underlying the antidiabetic activities of cortex cinnamomi extract (CCE).METHODS: To induce in vivo diabetes, mice were injected with streptozotocin (STZ) via a tail vein (100 mg STZ/kg body weight). To determine the effects of CCE,mice were administered CCE twice daily for 7 d by oral gavage starting 1 wk before the STZ injection. Blood glucose and plasma insulin concentration were measured as an index of diabetes. Also, to induce cytotoxicity of RINm5F cells, we treated with cytokines (IL-1β (2.0 ng/mL) and IFN-γ (100 U/mL)). Cell viability and nitric oxide production were measured colorimetrically.Inducible nitric oxide synthase (iNOS) mRNA and protein expression were determined by RT-PCR and Western blotting, respectively. The activation of NF-KB was assayed by using gel mobility shift assays of nuclear extracts.RESULTS: Treatment of mice with STZ resulted in hyperglycemia and hypoinsulinemia, which was further evidenced by immunohistochemical staining of islets. However, the diabetogenic effects of STZ were completely prevented when mice were pretreated with CCE. The inhibitory effect of CCE on STZ-induced hyperglycemia was mediated through the suppression of iNOS expression. In rat insulinoma RINm5F cells,CCE completely protected against interleukin-1β and interferon-y-mediated cytotoxicity. Moreover, RINm5F cells incubated with CCE showed significant reductions in interleukin-1β and interferon-y-induced nitric oxide production and in iNOS mRNA and protein expression,and these findings correlated well with in vivo observations.CONCLUSION: The molecular mechanism by which CCE inhibits iNOS gene expression appears to involve the inhibition of NF-κB activation. These results reveal the possible therapeutic value of CCE for the prevention of diabetes mellitus progression.

  7. In Vitro Antioxidant, Anticoagulant and Antimicrobial Activity and in Inhibition of Cancer Cell Proliferation by Xylan Extracted from Corn Cobs

    Directory of Open Access Journals (Sweden)

    Hugo Alexandre Oliveira Rocha

    2011-12-01

    Full Text Available Xylan is one of most abundant polymer after cellulose. However, its potential has yet to be completely recognized. Corn cobs contain a considerable reservoir of xylan. The aim of this work was to study some of the biological activities of xylan obtained from corn cobs after alkaline extraction enhanced by ultrasonication. Physical chemistry and infrared analyses showed 130 kDa heteroxylan containing mainly xylose:arabinose: galactose:glucose (5.0:1.5:2.0:1.2. Xylan obtained exhibited total antioxidant activity corresponding to 48.5 mg of ascorbic acid equivalent/g of xylan. Furthermore, xylan displayed high ferric chelating activity (70% at 2 mg/mL. Xylan also showed anticoagulant activity in aPTT test. In antimicrobial assay, the polysaccharide significantly inhibited bacterial growth of Klebsiella pneumoniae. In a test with normal and tumor human cells, after 72 h, only HeLa tumor cell proliferation was inhibited (p < 0.05 in a dose-dependent manner by xylan, reaching saturation at around 2 mg/mL, whereas 3T3 normal cell proliferation was not affected. The results suggest that it has potential clinical applications as antioxidant, anticoagulant, antimicrobial and antiproliferative compounds.

  8. Ameliorative Effect of Grape Seed Proanthocyanidin Extract on Cadmium-Induced Meiosis Inhibition During Oogenesis in Chicken Embryos.

    Science.gov (United States)

    Hou, Fuyin; Xiao, Min; Li, Jian; Cook, Devin W; Zeng, Weidong; Zhang, Caiqiao; Mi, Yuling

    2016-04-01

    Cadmium (Cd) is an environmental endocrine disruptor that has toxic effects on the female reproductive system. Here the ameliorative effect of grape seed proanthocyanidin extract (GSPE) on Cd-induced meiosis inhibition during oogenesis was explored. As compared with controls, chicken embryos exposed to Cd (3 µg/egg) displayed a changed oocyte morphology, decreased number of meiotic germ cells, and decreased expression of the meiotic marker protein γH2AX. Real time RT-PCR also revealed a significant down-regulation in the mRNA expressions of various meiosis-specific markers (Stra8, Spo11, Scp3, and Dmc1) together with those of Raldh2, a retinoic acid (RA) synthetase, and of the receptors (RARα and RARβ). In addition, exposure to Cd increased the production of H2 O2 and malondialdehyde in the ovaries and caused a corresponding reduction in glutathione and superoxide dismutase. Simultaneous supplementation of GSPE (150 µg/egg) markedly alleviated the aforementioned Cd-induced embryotoxic effects by upregulating meiosis-related proteins and gene expressions and restoring the antioxidative level. Collectively, the findings provided novel insights into the underlying mechanism of Cd-induced meiosis inhibition and indicated that GSPE might potentially ameliorate related reproductive disorders. © 2016 Wiley Periodicals, Inc.

  9. Protein Synthesis Inhibition Activity by Strawberry Tissue Protein Extracts during Plant Life Cycle and under Biotic and Abiotic Stresses

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    Walther Faedi

    2013-07-01

    Full Text Available Ribosome-inactivating proteins (RIPs, enzymes that are widely distributed in the plant kingdom, inhibit protein synthesis by depurinating rRNA and many other polynucleotidic substrates. Although RIPs show antiviral, antifungal, and insecticidal activities, their biological and physiological roles are not completely understood. Additionally, it has been described that RIP expression is augmented under stressful conditions. In this study, we evaluated protein synthesis inhibition activity in partially purified basic proteins (hereafter referred to as RIP activity from tissue extracts of Fragaria × ananassa (strawberry cultivars with low (Dora and high (Record tolerance to root pathogens and fructification stress. Association between the presence of RIP activity and the crop management (organic or integrated soil, growth stage (quiescence, flowering, and fructification, and exogenous stress (drought were investigated. RIP activity was found in every tissue tested (roots, rhizomes, leaves, buds, flowers, and fruits and under each tested condition. However, significant differences in RIP distribution were observed depending on the soil and growth stage, and an increase in RIP activity was found in the leaves of drought-stressed plants. These results suggest that RIP expression and activity could represent a response mechanism against biotic and abiotic stresses and could be a useful tool in selecting stress-resistant strawberry genotypes.

  10. Corrosion inhibition of Eleusine aegyptiaca and Croton rottleri leaf extracts on cast iron surface in 1 M HCl medium

    Energy Technology Data Exchange (ETDEWEB)

    Rajeswari, Velayutham [Department of Chemistry, Periyar University, Salem 636011 (India); Kesavan, Devarayan [Department of Chemistry, Dhirajlal Gandhi College of Technology, Salem 636309 (India); Gopiraman, Mayakrishnan [Department of Chemistry, National Institute of Technology, Tiruchirappalli 620015 (India); Viswanathamurthi, Periasamy, E-mail: viswanathamurthi72@gmail.com [Department of Chemistry, Periyar University, Salem 636011 (India); Poonkuzhali, Kaliyaperumal; Palvannan, Thayumanavan [Department of Bio-Chemistry, Periyar University, Salem 636011 (India)

    2014-09-30

    Graphical abstract: - Highlights: • Eleusine aegyptiaca and Croton rottleri are commonly available, less-toxic and eco-friendly inhibitors for cast iron corrosion. • The active constituents present in extracts adsorbed on the iron surface to inhibit the acidic corrosion. • The higher values of E{sub a} and ΔH{sup *} point out the higher inhibition efficiency noticed for the inhibitors. • Weight loss methods at various temperature and spectral data provides evidence for adsorption mechanism of inhibitors. - Abstract: The adsorption and corrosion inhibition activities of Eleusine aegyptiaca (E. aegyptiaca) and Croton rottleri (C. rottleri) leaf extracts on cast iron corrosion in 1 M hydrochloric acid solution were studied first time by weight loss and electrochemical techniques viz., Tafel polarization and electrochemical impedance spectroscopy. The results obtained from the weight loss and electrochemical methods showed that the inhibition efficiency increased with inhibitor concentrations. It was found that the extracts acted as mixed-type inhibitors. The addition of halide additives (KCl, KBr, and KI) on the inhibition efficiency has also been investigated. The adsorption of the inhibitors on cast iron surface both in the presence and absence of halides follows the Langmuir adsorption isotherm model. The inhibiting nature of the inhibitors was supported by FT-IR, UV–vis, Wide-angle X-ray diffraction and SEM methods.

  11. Nitration of Tyrosine Residue Y10 of Aβ1-42 Significantly Inhibits Its Aggregation and Cytotoxicity.

    Science.gov (United States)

    Zhao, Jie; Wu, Jinming; Yang, Zhen; Li, Hailing; Gao, Zhonghong

    2017-04-17

    Amyloid-β plaques and oxidative stress are the major hallmarks of Alzheimer's disease. Our previous study found that the heme-Aβ complex enhanced the catalytic effect of free heme on protein tyrosine nitration in the presence of hydrogen peroxide (H2O2) and nitrite (NO2(-)). Y10 in Aβ could be the first target to be nitrated. We also found that nitration of Aβ1-40 significantly decreased its aggregation. However, a contrary report showed that nitration of Aβ1-42 by peroxynitrite enhanced its aggregation. To rule out the interference of peroxynitrite caused Aβ oxidation, we used synthetic Y10 nitrated Aβ1-42 to study the influence of Y10 nitration on Aβ1-42's aggregation and cytotoxicity in this study. We confirmed that Aβ1-42 could be nitrated in the presence of H2O2, NO2(-), and heme by dot blotting. CD spectroscopy showed an increase of β-sheet structure of Aβ1-42 and its mutants. The thioflavin T (ThT) flourescence assay revealed that both nitration and chlorination significantly inhibited Aβ1-42 fibril formation. TEM and AFM observations of Aβ peptide aggregates further confirmed that Y10 modification inhibited Aβ1-42 fibril formation. The cytotoxicity study of native and modified Aβ peptides on SH-SY5Y cells revealed that nitration of Aβ1-42 remarkably decreased the neurotoxicity of Aβ1-42. On the basis of these results, we hypothesized that nitration of Y10 may block the π-π stacking interactions of Aβ1-42 so that it inhibit its aggregation and neurotoxicity. More importantly, considerable evidence suggested that the levels of nitrite plus nitrate significantly decreased in the brain of AD patients. Thus, we believe that these findings would be helpful for further understanding the function of Aβ in AD.

  12. Topical Application of Herbal Mixture Extract Inhibits Ovalbumin- or 2,4-Dinitrochlorobenzene-Induced Atopic Dermatitis

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    Soon Re Kim

    2012-01-01

    Full Text Available KM110329 is four traditional herbal medicine mixtures with anti-inflammatory properties. Atopic dermatitis (AD is an inflammatory skin disease associated with enhanced T-helper2 (Th2 lymphocyte response to allergens that results in elevated serum eosinophil and Immunoglobulin E (IgE levels and leukocyte infiltration in atopic skin sites. In this study, we investigated the effect of topical application of KM110329 ethanol extract on the ovalbumin (OVA or 2,4-dinitrochlorobenzene- (DNCB- induced AD mouse models. For that purpose, we observed the effects of KM110329 on blood eosinophils, skin mast cells, production of serum IgE, and expression of cytokine mRNA in the atopic dermatitis skin lesions of OVA allergen- or DNCB-treated BALB/c mice. KM110329 significantly reduced blood eosinophils cell numbers in OVA or DNCB-treated BALB/c mice. Histological analyses demonstrated decreased mast cell count as well as dermal infiltration by inflammatory cells. In the skin lesions, mRNA expression of interleukine (IL-4, IL-13, and IL-17 was inhibited by KM110329. KM110329 also suppressed the production of serum IgE level in both the OVA- and DNCB-induced atopic dermatitis model. Taken together, our results showed that topical application of KM110329 extracts exerts beneficial effects in AD symptoms, suggesting that KM110329 might be a useful candidate for the treatment of AD.

  13. Ethanol extract of Justicia gendarussa inhibits lipopolysaccharide stimulated nitric oxide and matrix metalloproteinase-9 expression in murine macrophage.

    Science.gov (United States)

    Varma, R Sandeep; Ashok, G; Vidyashankar, S; Patki, P; Nandakumar, Krishna S

    2011-06-01

    Justicia gendarussa Burm (Acanthaceae) is a plant used to treat inflammatory diseases such as rheumatoid arthritis. However, the mechanism involved in the anti-inflammatory properties of this plant has not been studied well. The in vitro anti-inflammatory activities of ethanol extract of Justicia gendarussa leaves (J-01) are studied here for the first time. The ethanol extract, J-01 was prepared from the leaves of Justicia gendarussa. The inhibitory effect of J-01 in nitric oxide (NO) production, inducible nitric oxide synthase (iNOS) and matrix metalloproteinase-9 (MMP-9) gene expressions were studied in lipopolysaccharide (LPS) stimulated macrophage cell line RAW 264.7. J-01 in a concentration dependent manner (200-50 μg/mL) attenuated NO production from macrophage stimulated with LPS (1 μg/mL). Further, J-01 significantly suppressed iNOS mRNA expression in these cells. J-01 has also downregulated the MMP-9 gene expression in LPS stimulated macrophage. The modulatory function of J-01 in inhibiting NO, iNOS, and MMP-9 as obtained from the present in vitro studies provide first scientific evidence to support the anti-inflammatory properties of Justicia gendarussa. This plant may have potential use in the management of inflammatory conditions such as arthritis.

  14. Phenolic Extract from Moringa oleifera Leaves Inhibits Key Enzymes Linked to Erectile Dysfunction and Oxidative Stress in Rats’ Penile Tissues

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    Ganiyu Oboh

    2015-01-01

    Full Text Available This study was designed to determine the antioxidant properties and inhibitory effects of extract from Moringa oleifera leaves on angiotensin-I-converting enzyme (ACE and arginase activities in vitro. The extract was prepared and phenolic (total phenols and flavonoid contents, radical (nitric oxide (NO, hydroxyl (OH scavenging abilities, and Fe2+-chelating ability were assessed. Characterization of the phenolic constituents was done via high performance liquid chromatography-diode array detection (HPLC-DAD analysis. Furthermore, the effects of the extract on Fe2+-induced MDA production in rats’ penile tissue homogenate as well as its action on ACE and arginase activities were also determined. The extract scavenged NO∗, OH∗, chelated Fe2+, and inhibited MDA production in a dose-dependent pattern with IC50 values of 1.36, 0.52, and 0.38 mg/mL and 194.23 µg/mL, respectively. Gallic acid, chlorogenic acid, quercetin, and kaempferol were the most abundant phenolic compounds identified in the leaf extract. The extract also inhibited ACE and arginase activities in a dose-dependent pattern and their IC50 values were 303.03 and 159.59 µg/mL, respectively. The phenolic contents, inhibition of ACE, arginase, and Fe2+-induced MDA production, and radical (OH∗, NO∗ scavenging and Fe2+-chelating abilities could be some of the possible mechanisms by which M. oleifera leaves could be used in the treatment and/or management of erectile dysfunction.

  15. Hydrophilic extract from Posidonia oceanica inhibits activity and expression of gelatinases and prevents HT1080 human fibrosarcoma cell line invasion.

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    Barletta, Emanuela; Ramazzotti, Matteo; Fratianni, Florinda; Pessani, Daniela; Degl'Innocenti, Donatella

    2015-01-01

    Posidonia oceanica (L.) Delile is an endemic Mediterranean sea-grass distributed in the infralittoral zones, where it forms meadows playing a recognized ecological role in the coastal marine habitat. Although its use as a traditional herbal remedy is poorly documented, recent literature reports interesting pharmacological activities as antidiabetic, antioxidant and vasoprotective. Differently from previous literature, this study presents a hydrophilic extraction method that recovers metabolites that may be tested in biological buffers. We showed for the first time in the highly invasive HT1080 human fibrosarcoma cell line that our hydrophilic extract from P. oceanica was able to strongly decrease gene and protein expression of gelatinases MMP-2 and MMP-9 and to directly inhibit in a dose-dependent manner gelatinolytic activity in vitro. Moreover, we have revealed that our extract strongly inhibited HT1080 cell migration and invasion. Biochemical analysis of the hydrophilic extract showed that catechins were the major constituents with minor contribution of gallic acid, ferulic acid and chlorogenic plus a fraction of uncharacterized phenols. However, if each individual compound was tested independently, none by itself was able to induce a direct inhibition of gelatinases as strong as that observed in total extract, opening up new routes to the identification of novel compounds. These results indicate that our hydrophilic extract from P. oceanica might be a source of new pharmacological natural products for treatment or prevention of several diseases related to an altered MMP-2 and MMP-9 expression.

  16. Hydroalcoholic extract of Rosemary (Rosmarinus officinalis L.) and its constituent carnosol inhibit formalin-induced pain and inflammation in mice.

    Science.gov (United States)

    Emami, F; Ali-Beig, H; Farahbakhsh, S; Mojabi, N; Rastegar-Moghadam, B; Arbabian, S; Kazemi, M; Tekieh, E; Golmanesh, L; Ranjbaran, M; Jalili, C; Noroozzadeh, A; Sahraei, H

    2013-04-01

    The anti-inflammatory and anti-nociceptive properties of Rosmarinus officinalis L. (ROL) extract and its major constituent, carnosol in male NMRI mice (W:25-30 g) have been evaluated in the present study. Formalin (2%, 20 microL) was injected into the plantar portion of the hind paw and resulting pain and inflammation was studied for 60 min. The plant extract, carnosol and other drugs were administered intraperitoneally or subcutaneously 30 min before formalin injection. In a separate experiment, the effects of the extract and carnosol on plasma corticosterone levels and activity of the enzymes cyclooxygenase type 1 and 2 (COX1 and COX2) were investigated. Injection of different doses of ROL and carnosol reduced pain in the phase 2 of the formalin test, which was not inhibited by naloxone and/or memantine. In addition, pretreatment of the animals with ROL and/or carnosol reduces the formalin-induced inflammation. Furthermore, the extract and carnosol did not affect plasma corticosterone levels compared with the control group. Interestingly, both the extract and carnosol inhibited COX1 and COX2 activity. It could be concluded that ROL extract and carnosol suppressed pain and inflammation induced by formalin injection, which may be due to inhibition of COX1 and COX2 enzymes activity.

  17. Differential activities of fungi-derived tannases on biotransformation and substrate inhibition in green tea extract.

    Science.gov (United States)

    Baik, Joo Hyun; Suh, Hyung Joo; Cho, So Young; Park, Yooheon; Choi, Hyeon-Son

    2014-11-01

    Tannases are important enzymes in the antioxidant potential of tea leaves. In this study, we evaluated the effect of two tannases (T1 and T2) on biotransformation of tea polyphenols and antioxidative activities from catechins in green tea extract (GTE). The T1 tannase-catalyzed reaction was inhibited by the addition of >2.0% GTE substrate, whereas the T2-catalyzed reaction was not inhibited, even by addition of 5.0% GTE. Furthermore, the T1 tannase-catalyzed reaction was inhibited by addition of 10 mg mL(-1) EGCG, whereas the T2 tannase-catalyzed reaction did not display any inhibitory effect. These results indicate that T2 tannase was more tolerant than T1 tannase to substrate inhibition in degallation reactions. Specifically, the substrate EGCG (90,687.1 μg mL(-1)) was transformed into gallic acid (50,242.9 μg mL(-1)) and EGC (92,598.3 μg mL(-1)) after 1-h treatment with T2 tannase (500 U g(-1)). The tannase-mediated product displayed higher in vitro radical-scavenging activity than the control. IC50 value of GTE on ABTS and DPPH radicals (46.1 μg mL(-1) and 18.4 μg mL(-1), respectively) decreased markedly after T2 tannase treatment (to 35.8 μg mL(-1) and 15.1 μg mL(-1), respectively). These results indicate that T2 tannase treatment of GTE enhanced its radical-scavenging activity, an increase that was also observed in the reaction using EGCG substrate. Taken together, our results revealed that T2 tannase is more suitable for biotransformation of catechins in GTE than T1 tannase, and T2 treatment provides an enhanced radical-scavenging effect.

  18. Berberine and a Berberis lycium extract inactivate Cdc25A and induce {alpha}-tubulin acetylation that correlate with HL-60 cell cycle inhibition and apoptosis

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    Khan, Musa [Department of Plant Sciences, Quaid-i-Azam University Islamabad (Pakistan); Institute of Clinical Pathology, Medical University of Vienna, Waehringer Guertel 18-20, A-1090 Vienna (Austria); Department of Pharmacognosy, Faculty of Life Sciences, University of Vienna, Althanstrasse 14 (Austria); Giessrigl, Benedikt; Vonach, Caroline; Madlener, Sibylle [Institute of Clinical Pathology, Medical University of Vienna, Waehringer Guertel 18-20, A-1090 Vienna (Austria); Prinz, Sonja [Department of Pharmacognosy, Faculty of Life Sciences, University of Vienna, Althanstrasse 14 (Austria); Herbaceck, Irene; Hoelzl, Christine [Department of Medicine I, Institute of Cancer Research, Medical University of Vienna, Borschkegasse 8a (Austria); Bauer, Sabine; Viola, Katharina [Institute of Clinical Pathology, Medical University of Vienna, Waehringer Guertel 18-20, A-1090 Vienna (Austria); Mikulits, Wolfgang [Department of Medicine I, Institute of Cancer Research, Medical University of Vienna, Borschkegasse 8a (Austria); Quereshi, Rizwana Aleem [Department of Plant Sciences, Quaid-i-Azam University Islamabad (Pakistan); Knasmueller, Siegfried; Grusch, Michael [Department of Medicine I, Institute of Cancer Research, Medical University of Vienna, Borschkegasse 8a (Austria); Kopp, Brigitte [Department of Pharmacognosy, Faculty of Life Sciences, University of Vienna, Althanstrasse 14 (Austria); Krupitza, Georg, E-mail: georg.krupitza@meduniwien.ac.at [Institute of Clinical Pathology, Medical University of Vienna, Waehringer Guertel 18-20, A-1090 Vienna (Austria)

    2010-01-05

    Berberis lycium Royle (Berberidacea) from Pakistan and its alkaloids berberine and palmatine have been reported to possess beneficial pharmacological properties. In the present study, the anti-neoplastic activities of different B. lycium root extracts and the major constituting alkaloids, berberine and palmatine were investigated in p53-deficient HL-60 cells. The strongest growth inhibitory and pro-apoptotic effects were found in the n-butanol (BuOH) extract followed by the ethyl acetate (EtOAc)-, and the water (H{sub 2}O) extract. The chemical composition of the BuOH extract was analyzed by TLC and quantified by HPLC. 11.1 {mu}g BuOH extract (that was gained from 1 mg dried root) contained 2.0 {mu}g berberine and 0.3 {mu}g/ml palmatine. 1.2 {mu}g/ml berberine inhibited cell proliferation significantly, while 0.5 {mu}g/ml palmatine had no effect. Berberine and the BuOH extract caused accumulation of HL-60 cells in S-phase. This was preceded by a strong activation of Chk2, phosphorylation and degradation of Cdc25A, and the subsequent inactivation of Cdc2 (CDK1). Furthermore, berberine and the extract inhibited the expression of the proto-oncogene cyclin D1. Berberine and the BuOH extract induced the acetylation of {alpha}-tubulin and this correlated with the induction of apoptosis. The data demonstrate that berberine is a potent anti-neoplastic compound that acts via anti-proliferative and pro-apoptotic mechanisms independent of genotoxicity.

  19. Antioxidant activity and inhibition of aflatoxin B1-, nifuroxazide-, and sodium azide-induced mutagenicity by extracts from Rhamnus alaternus L.

    Science.gov (United States)

    Ammar, Rebai Ben; Sghaier, Mohamed Ben; Boubaker, Jihed; Bhouri, Wissem; Naffeti, Aicha; Skandrani, Ines; Bouhlel, Ines; Kilani, Soumaya; Ghedira, Kamel; Chekir-Ghedira, Leila

    2008-07-10

    The effect of extracts obtained from Rhamnus alaternus L. leaves on genotoxicity and SOS response induced by aflatoxin B(1) (10 microg/assay) as well as nifuroxazide (20 microg/assay) was investigated in a bacterial assay system, i.e., the SOS chromotest with Escherichia coli PQ37. The evaluation of the mutagenic and antimutagenic actions of the same extracts against the sodium azide (1.5 microg/plate)-induced mutagenicity was assayed using the Salmonella typhimurium assay system. The R. alaternus tested extracts exhibited no genotoxicity either with or without the external S9 activation mixture. However, all the extracts, particularly aqueous extract (A) and its chloroformic fraction (A(2)) significantly decreased the genotoxicity induced by aflatoxin B(1) and nifuroxazide. Moreover, the different extracts showed no mutagenicity when tested with Salmonella typhimurium strains TA1535 and TA1538 either with or without the S9 mix. Aqueous extract as well as its A(2) fraction exhibited the highest level of protection towards the direct mutagen, sodium azide-induced response in TA1535 strain with mutagenicity inhibition percentages of 83.6% and 91.4%, respectively, at a dose of 250 microg/plate. The results obtained by the Ames test assay confirm those of SOS chromotest. These same active extracts exhibited high xanthine oxidase (XOD) inhibiting with respective IC(50) values of 208 and 137 microg/ml, and superoxide anion-scavenging effects (IC(50) values of 132 and 117 microg/ml) when tested in the XOD enzymatic assay system. Our findings emphasize the potential of R. alaternus to prevent mutations and also its antioxidant effect.

  20. Exploration of larvicidal and adult emergence inhibition activities of Ricinus communis seed extract against three potential mosquito vectors in Kolkata, India

    Institute of Scientific and Technical Information of China (English)

    Shyamapada Mandal

    2010-01-01

    Objective:To determine the larvicidal and adult emergence inhibition activities of castor (Ricinus communis) seed extract against three potential mosquito vectorsAnopheles stephensi (An. stephensi), Culex quinquefasciatus (Cx. quinquefasciatus) andAedes albopictus (Ae. albopictus) in India.Methods: TheR. communis seed extract was tested, employingWHO procedure, against fourth larval instars of the three mosquito species for 24 h and larval mortalities were recorded at various concentrations (2-64 μg/mL); the 24 hLC50 values of theR. communis seed extract were determined following Probit analysis. The larval killing, antipupation and adult emergence inhibition rates of the test extract, using a single concentration of2μLC50, were studied at different time periods (24-72 h); the extract toxicity was tested against a fish,Oreochromis niloticus (O. niloticus).Results: TheR. communis seed extract exhibited larvicidal effects with 100 % killing activities at concentrations32-64 μg/mL, and withLC50values 7.10, 11.64 and 16.84μg/mL forCx. quinquefasciatus, An. stephensiand Ae. albopictuslarvae, respectively. When the larvae were treated with the extract at a single concentration of2×LC50, significant differences were observed, compared to control groups, in rate of pupation (P<0.001) as well as in adult formation (P<0.001).Conclusions: The present findings suggest that theR. communis seed extract provided an excellent potential for controllingAn. stephensi, Cx. quinquefasciatus andAe. albopictus mosquito vectors.

  1. Carbohydrase inhibition and anti-cancerous and free radical scavenging properties along with DNA and protein protection ability of methanolic root extracts of Rumex crispus.

    Science.gov (United States)

    Shiwani, Supriya; Singh, Naresh Kumar; Wang, Myeong Hyeon

    2012-10-01

    The study elucidated carbohydrase inhibition, anti-cancerous, free radical scavenging properties and also investigated the DNA and protein protection abilities of methanolic root extract of Rumex crispus (RERC). For this purpose, pulverized roots of Rumex crispus was extracted in methanol (80% and absolute conc.) for 3 hrs for 60℃ and filtered and evaporated with vacuum rotary evaporator. RERC showed high phenolic content (211 µg/GAE equivalent) and strong 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging (IC(50) = 42.86 (absolute methanol) and 36.91 µg/mL (80% methanolic extract)) and reduced power ability. Furthermore, RERC exhibited significant protective ability in H(2)O(2)/Fe(3+)/ascorbic acid-induced protein or DNA damage and percentage inhibition of the HT-29 cell growth rate following 80% methanolic RERC exposure at 400 µg/mL was observed to be highest (10.2% ± 1.03). Moreover, methanolic RERC inhibited α-glucosidase and amylase effectively and significantly (P < 0.05). Conclusively, RERC could be considered as potent carbohydrase inhibitor, anti-cancerous and anti-oxidant.

  2. Green tea (Camellia sinensis) extract inhibits both the metastasis and osteolytic components of mammary cancer 4T1 lesions in mice.

    Science.gov (United States)

    Luo, Ke-Wang; Ko, Chun-Hay; Yue, Grace Gar-Lee; Lee, Julia Kin-Ming; Li, Kai-Kai; Lee, Michelle; Li, Gang; Fung, Kwok-Pui; Leung, Ping-Chung; Lau, Clara Bik-San

    2014-04-01

    Green tea (Camellia sinensis, CS), a kind of Chinese tea commonly consumed as a healthy beverage, has been demonstrated to have various biological activities, including antioxidation, antiobesity and anticancer. Our study aims to investigate the antitumor, antimetastasis and antiosteolytic effects of CS aqueous extract both in vitro and in vivo using metastasis-specific mouse mammary carcinoma 4T1 cells. Our results showed that treatment of 4T1 cells with CS aqueous extract resulted in significant inhibition of 4T1 cell proliferation. CS extract induced 4T1 apoptosis in a dose-dependent manner as assessed by annexin-V and propidium iodide staining and caspase-3 activity. Western blot analysis showed that CS increased the expression of Bax-to-Bcl-2 ratio and activated caspase-8 and caspase-3 to induce apoptosis. CS also inhibited 4T1 cell migration and invasion at 0.06-0.125 mg/ml. In addition, CS extract (0.6 g/kg, orally fed daily for 4 weeks) was effective in decreasing the tumor weight by 34.8% in female BALB/c mice against water treatment control (100%). Apart from the antitumor effect, CS extract significantly decreased lung and liver metastasis in BALB/c mice bearing 4T1 tumors by 54.5% and 72.6%, respectively. Furthermore, micro-computed tomography and in vitro osteoclast staining analysis suggested that CS extract was effective in bone protection against breast cancer-induced bone destruction. In conclusion, the present study demonstrated that the CS aqueous extract, which closely mimics green tea beverage, has potent antitumor and antimetastasis effects in breast cancer and could protect the bone from breast cancer-induced bone destruction.

  3. Water Extractable Phytochemicals from Peppers (Capsicum spp. Inhibit Acetylcholinesterase and Butyrylcholinesterase Activities and Prooxidants Induced Lipid Peroxidation in Rat Brain In Vitro

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    Omodesola O. Ogunruku

    2014-01-01

    Full Text Available Background. This study sought to investigate antioxidant capacity of aqueous extracts of two pepper varieties (Capsicum annuum var. accuminatum (SM and Capsicum chinense (RO and their inhibitory effect on acetylcholinesterase and butyrylcholinesterase activities. Methods. The antioxidant capacity of the peppers was evaluated by the 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid (ABTS radical scavenging ability and ferric reducing antioxidant property. The inhibition of prooxidant induced lipid peroxidation and cholinesterase activities in rat brain homogenates was also evaluated. Results. There was no significant difference (P>0.05 in the total phenol contents of the unripe and ripe Capsicum spp. extracts. Ripe and unripe SM samples had significantly higher (P<0.05 ABTS* scavenging ability than RO samples, while the ripe fruits had significantly higher (P<0.05 ferric reducing properties in the varieties. Furthermore, the extracts inhibited Fe2+ and quinolinic acid induced lipid peroxidation in rats brain homogenates in a dose-dependent manner. Ripe and unripe samples from SM had significantly higher AChE inhibitory abilities than RO samples, while there was no significant difference in the BuChE inhibitory abilities of the pepper samples. Conclusion. The antioxidant and anticholinesterase properties of Capsicum spp. may be a possible dietary means by which oxidative stress and symptomatic cognitive decline associated with neurodegenerative conditions could be alleviated.

  4. Extract from Nandina domestica inhibits lipopolysaccharide-induced cyclooxygenase-2 expression in human pulmonary epithelial A549 cells.

    Science.gov (United States)

    Ueki, Takuro; Akaishi, Tatsuhiro; Okumura, Hidenobu; Abe, Kazuho

    2012-01-01

    Extract from fruits of Nandina domestica THUNBERG (NDE) has been used to improve cough and breathing difficulty in Japan for many years. To explore whether NDE may alleviate respiratory inflammation, we investigated its effect on expression of cyclooxygenase-2 (COX-2) and production of prostaglandin E₂ (PGE₂) in human pulmonary epithelial A549 cells in culture. Treatment with lipopolysaccharide (LPS; 6 µg/mL) resulted in an increase of COX-2 expression and PGE₂ production in A549 cells. Both the LPS-induced COX-2 expression and PGE₂ production were significantly inhibited by NDE (1-10 µg/mL) in a concentration-dependent manner. NDE did not affect COX-1 expression nor COX activity. These results suggest that NDE downregulates LPS-induced COX-2 expression and inhibits PGE₂ production in pulmonary epithelial cells. Furthermore, higenamine and nantenine, two major constituents responsible for tracheal relaxing effect of NDE, did not mimic the inhibitory effect of NDE on LPS-induced COX-2 expression in A549 cells. To identify active constituent(s) of NDE responsible for the anti-inflammatory effect, NDE was introduced in a polyaromatic absorbent resin column and stepwise eluted to yield water fraction, 20% methanol fraction, 40% methanol fraction, 99.8% methanol fraction, and 99.5% acetone fraction. However, none of these five fractions alone inhibited LPS-induced COX-2 expression. On the other hand, exclusion of water fraction from NDE abolished the inhibitory effect of NDE on LPS-induced COX-2 expression. These results suggest that constituent(s) present in water fraction is required but not sufficient for the anti-inflammatory activity of NDE, which may result from interactions among multiple constituents.

  5. Inhibition of Advanced Glycation End-Product Formation and Antioxidant Activity by Extracts and Polyphenols from Scutellaria alpina L. and S. altissima L.

    Science.gov (United States)

    Grzegorczyk-Karolak, Izabela; Gołąb, Krzysztof; Gburek, Jakub; Wysokińska, Halina; Matkowski, Adam

    2016-06-14

    Methanolic extracts from the aerial parts and roots of two Scutellaria species, S. alpina and S. altissima, and five polyphenols from these plants demonstrated a significant ability to inhibit the formation of advanced glycation end-products (AGE) in vitro. S. alpina, which is richer in polyphenolic compounds, had strong antiglycation properties. These extracts demonstrated also high activity in the FRAP (ferric-reducing antioxidant power), antiradical (DPPH) and lipid peroxidation inhibition assays. Among the pure compounds, baicalin was the strongest glycation inhibitor (90.4% inhibition at 100 μg/mL), followed by luteolin (85.4%). Two other flavone glycosides had about half of this activity. Verbascoside was similar to the reference drug aminoguanidine (71.2% and 75.9%, respectively). The strong correlation observed between AGE inhibition and total flavonoid content indicated that flavonoids contribute significantly to antiglycation properties. A positive correlation was also observed between antiglycative and antioxidant activities. The studied skullcap species can be considered as a potential source of therapeutic agents for hyperglycemia-related disorders.

  6. Inhibition of Advanced Glycation End-Product Formation and Antioxidant Activity by Extracts and Polyphenols from Scutellaria alpina L. and S. altissima L.

    Directory of Open Access Journals (Sweden)

    Izabela Grzegorczyk-Karolak

    2016-06-01

    Full Text Available Methanolic extracts from the aerial parts and roots of two Scutellaria species, S. alpina and S. altissima, and five polyphenols from these plants demonstrated a significant ability to inhibit the formation of advanced glycation end-products (AGE in vitro. S. alpina, which is richer in polyphenolic compounds, had strong antiglycation properties. These extracts demonstrated also high activity in the FRAP (ferric-reducing antioxidant power, antiradical (DPPH and lipid peroxidation inhibition assays. Among the pure compounds, baicalin was the strongest glycation inhibitor (90.4% inhibition at 100 μg/mL, followed by luteolin (85.4%. Two other flavone glycosides had about half of this activity. Verbascoside was similar to the reference drug aminoguanidine (71.2% and 75.9%, respectively. The strong correlation observed between AGE inhibition and total flavonoid content indicated that flavonoids contribute significantly to antiglycation properties. A positive correlation was also observed between antiglycative and antioxidant activities. The studied skullcap species can be considered as a potential source of therapeutic agents for hyperglycemia-related disorders.

  7. Green tea extract inhibits paraquat-induced pulmonary fibrosis by suppression of oxidative stress and endothelin-l expression.

    Science.gov (United States)

    Kim, Hak-Ryul; Park, Byung-Kyu; Oh, Yeon-Mok; Lee, Yun-Song; Lee, Dong-Soon; Kim, Hyun-Kuk; Kim, Joo-Young; Shim, Tae-Sun; Lee, Sang-Do

    2006-01-01

    Paraquat-induced pulmonary fibrosis involves two factors, direct injury by oxygen free radicals and indirect injury by inflammatory cells and fibroblasts. Endothelin-1 (ET-1) has been shown to act as a mediator of pulmonary fibrosis, and its formation increases during oxidative stress. We investigated whether green tea extract (GTE), which has antioxidant properties, inhibits paraquat-induced pulmonary fibrosis and whether ET-1 is involved in this process. Paraquat (0.3 mg/kg) was instilled into the right lungs of rats, following which the rats were either not further treated (Group P, n = 7), or they were administered 1% GTE mixed with feed (Group PG; n = 7) or the ET(A) receptor antagonist ZD2574 (10 mg/kg through gavage; Group PZ; n = 7) for two weeks. As control, we used rats instilled with saline (Group N; n = 6). Two weeks after paraquat instillation, we assayed the degree of pulmonary fibrosis by light microscopic morphometry and hydroxyproline content; lipid peroxidation as a marker of oxidative stresses by measurement of malondialdehyde (MDA); ET-1 by immunohistochemistry; and prepro-ET-1 mRNA expression by reverse transcription-polymerase chain reaction. Compared with Group N, significant pulmonary fibrosis was observed in Group P, accompanied by increases in MDA, ET-1, and prepro-ET-1 mRNA expression. Compared with Group P, Group PG showed significant decreases in pulmonary fibrosis, along with decreases in MDA, ET-1, and prepro-ET-1 mRNA expression. We also observed significant decreases in pulmonary fibrosis in Group PZ compared with Group P. These findings suggest that GTE inhibits paraquat-induced pulmonary fibrosis by suppression of oxidative stress and ET-1 expression.

  8. Modes of Inhibition of α-Amylase and α-Glucosidase by Aqueous Extract of Morinda lucida Benth Leaf

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    M. I. Kazeem

    2013-01-01

    Full Text Available Diabetes mellitus is a metabolic disorder of glucose metabolism. The management of blood glucose level is the hallmark in the treatment of this disease. This may be achieved through the use of oral hypoglycemic drugs such as biguanides, insulin secretagogues, and α-glucosidase inhibitors. The purpose of the present study was to investigate the inhibitory effect of Morinda lucida leaf extracts on the activities of α-amylase and α-glucosidase. This was performed using α-amylase from Aspergillus oryzae and α-glucosidase from Saccharomyces cerevisiae. Aqueous extract of Morinda lucida gave the highest percentage yield (9.99% of the plant out of the three extracts (compared to acetone and ethanolic extracts and possesses the highest inhibitory activity against α-amylase (IC50 value of 2.30 mg/mL and α-glucosidase (IC50 value of 2.00 mg/mL. Kinetic analysis revealed that the aqueous extract of this plant leaf inhibited the α-amylase competitively but displayed mixed noncompetitive mode of inhibition towards α-glucosidase. It can be concluded that aqueous extract of Morinda lucida exhibited the best inhibitory activity on the two enzymes studied and the presence of phytochemicals like flavonoids, saponins, and tannins may have contributed greatly to the inhibitory activity of the plant extract.

  9. Inhibition of glucose- and fructose-mediated protein glycation by infusions and ethanolic extracts of ten culinary herbs and spices

    Directory of Open Access Journals (Sweden)

    Jugjeet Singh Ramkissoon

    2016-06-01

    Conclusions: The higher rate of fluorescence generation by fructation suggests that glycation by fructose deserves much attention as a glycating agent. Data herein showed that the extracts inhibited GMG and FMG. Thus, these edible plants could be a natural source of antioxidants and anti-glycation agent for preventing advanced glycation end-products-mediated complications.

  10. Rhus javanica Gall Extract Inhibits the Differentiation of Bone Marrow-Derived Osteoclasts and Ovariectomy-Induced Bone Loss

    Directory of Open Access Journals (Sweden)

    Tae-Ho Kim

    2016-01-01

    Full Text Available Inhibition of osteoclast differentiation and bone resorption is a therapeutic strategy for the management of postmenopausal bone loss. This study investigated the effects of Rhus javanica (R. javanica extracts on bone marrow cultures to develop agents from natural sources that may prevent osteoclastogenesis. Extracts of R. javanica (eGr cocoons spun by Rhus javanica (Bell. Baker inhibited the osteoclast differentiation and bone resorption. The effects of aqueous extract (aeGr or 100% ethanolic extract (eeGr on ovariectomy- (OVX- induced bone loss were investigated by various biochemical assays. Furthermore, microcomputed tomography (µCT was performed to study bone remodeling. Oral administration of eGr (30 mg or 100 mg/kg/day for 6 weeks augmented the inhibition of femoral bone mineral density (BMD, bone mineral content (BMC, and other factors involved in bone remodeling when compared to OVX controls. Additionally, eGr slightly decreased bone turnover markers that were increased by OVX. Therefore, it may be suggested that the protective effects of eGr could have originated from the suppression of OVX-induced increase in bone turnover. Collectively, the findings of this study indicate that eGr has potential to activate bone remodeling by inhibiting osteoclast differentiation and bone loss.

  11. Sweet potato leaf extract inhibits the simulated in vitro gastrointestinal digestion of native starch

    Directory of Open Access Journals (Sweden)

    Toong Long Jeng

    2015-09-01

    Full Text Available Several studies have reported the therapeutic use of caffeoylquinic acid (CQA derivatives in the management of hyperglycemia. This study used a simulated in vitro gastrointestinal digestion model to assess the inhibitory effects of CQA derivatives-rich sweet potato leaf extract (SPLE and a commercially produced green coffee bean extract (GCBE, each with total polyphenols contents of 452 mg g−1 and 278 mg g−1, respectively, against starch digestion. The changes in the amounts of total polyphenols and total CQA derivatives during in vitro gastrointestinal digestion were also examined. The results indicated that both extracts contained substantial levels of CQA derivatives (136 mg g−1 and 83.5 mg g−1 of extract for SPLE and GCBE, respectively. The amounts of total polyphenols and total CQA derivatives in 20 mg of SPLE and GCBE samples decreased from 9.04 mg to 0.58 mg and from 5.56 mg to 0.58 mg, and from 2.72 mg to 0.16 mg and from 1.67 mg to 0.10 mg, respectively, following in vitro gastrointestinal digestion and subsequent dialysis. When SPLE and GCBE were accompanied with starch for in vitro digestion test, they both exhibited inhibitory effect against starch digestion during simulated intestinal digestion, with estimated half maximal inhibitory concentration (IC50 values of 4.91 mg and 6.06 mg polyphenols, respectively. The amount of glucose permeated through dialysis membrane also decreased significantly in comparison with the extract-negative control. Thus, both SPLE and GCBE were capable of modulating the release of glucose from starch digestion in simulated intestinal tract. The observed inhibitory effects against glucose release were presumably due in part to the presence of CQA derivatives in the tested extracts. The SPLE had higher inhibitory effect against in vitro starch digestion than the commercially prepared reference GCBE. Therefore, the SPLE might be used to manage hyperglycemia over the long term.

  12. Acetylcholinesterase inhibition starting from extracts of Bauhinia variegata L., Bauhinia var. candida (Aiton Buch.-Ham., and Bauhinia ungulata L

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    Kamilla Monteiro dos Santos

    2011-12-01

    Full Text Available INTRODUCTION: A treatment to the Alzheimer's disease consists inhibition of the acetylcholinesterase, which is responsible for the acetylcholine control in the synapses. METHODS: We have investigated the potential of inhibition of the acetylcholinesterase produced by hexane extracts of leaves, branches, and flowers from three Bauhinia specimens, which is based on the technique of thin layer chromatography and on identifying the organ of the plant that possesses larger concentration of inhibitors. RESULTS: Retention factor analysis shows values of 0.31aA, 0.31aA, and 0.46aB for flowers B. variegata, B. var. candida, and B. ungulata, respectively. CONCLUSIONS: The flower extract of B. ungulata is the most suitable for further studies on this inhibition.

  13. The inhibition of Typhonium flagelliforme Lodd. Blume leaf extract on COX-2 expression of Wi Dr colon cancer cells

    Institute of Scientific and Technical Information of China (English)

    Agustina Setiawati; Handika Immanuel; Mery Tri Utami

    2016-01-01

    Objective: To determine the inhibition activity of Typhonium flagelliforme Lodd. Blume(T. flagelliforme) leaf extract on cyclooxygenase 2(COX-2) expression of colon cancer cells.Methods: T. flagelliforme leaf extract was prepared to macerate in ethyl acetate. In vitro anticancer activity was assayed by MTT method on Wi Dr colon cancer cells. This study applied apoptosis induction assay to investigate the mechanism of cell death using double staining method. COX-2 expression was stained by immunocytochemistry.Results: T. flagelliforme showed anticancer activity and induced apoptosis on Wi Dr cells through inhibition of COX-2 expression with IC5070 mg/m L.Conclusions: This study showed that T. flagelliforme is a promising chemopreventive agent for colon cancer through COX-2 inhibition.

  14. Inhibition of P2X7 Receptor by Extracts of Chinese Medicine

    Institute of Scientific and Technical Information of China (English)

    Andreas Spielmann; 顾全保; 马春辉; 黄成钢; 宣利江; Wolfgang Schwarz

    2008-01-01

    目的:探讨中草药石菖蒲粗提物SCP01及其纯化物SCP02(α-细辛脑)和迷迭香抽提物X0728对人肥大细胞的作用.方法:用膜片钳技术全细胞记录人肥大细胞膜ATP激活的P2X7受体的电流.结果:40μg/mL SCP01抑制P2X7电流(27.6±2.0)%,而同样浓度的SCP02抑制(29.5±2.2)%(-100 mV电位下),笔者还比较了商业用α-细辛脑的效厘,42 μg/mL可抑制P2X7电流(52.2±2.0)%.相反,40 μg/mL X0728激活P2X7电流(28.6±2.8)%,所有这些作用都是电压依赖性的.结论:α-细辛脑对P2X7的抑制将阻滞胞内钙的增加,从而可以解释抑制神经元死亡的原因.而X0728刺激P2X7的药理学效应尚需进一步研究.%Objective: To investigate the influence of Acorus gramineus (Soland), a crude extract, SCP01, and a purified component, SCP02, and of Rosmarinus officinalis L., X0728 on human mast cells (HMC-1 Cell Line). Methods: Current-voltage of P2X7 receptors on human mast cell membrane activated by ATP was recorded by the whole-cell patch clamp technique. Results: The current at-100 mV mediated by P2X7was inhibited by (27.6±2.0) % in the presence of 40 μg/mL SCP01 and by (29.5±2.2) % in the presence of 40 μg/mL SCP02, which was identified as α-asarone. 42 μg/mL of the commercially available α-asarone inhibited the P2X7-mediated current by (52.2±2.0) %. In contrast to SCP01 and SCP02, 40μg/mL X0728 provoked stimulation of the current by (28.6±2.8) %. All effects were voltage-independent. Conclusion: The inhibition of P2X7by α-asarone will inhibit intracellular calcium increase and this may account for the inhibition of reported excitotoxic cell death. The pharmacological function of P2X7stimulation by X0728 needs further investigation.

  15. Oral grape seed extract inhibits prostate tumor growth and progression in TRAMP mice.

    Science.gov (United States)

    Raina, Komal; Singh, Rana P; Agarwal, Rajesh; Agarwal, Chapla

    2007-06-15

    Prostate cancer chemoprevention is an alternative and potential strategy to control this malignancy. Herein, we evaluated the chemopreventive efficacy of grape seed extract (GSE) against prostate cancer in transgenic adenocarcinoma of the mouse prostate (TRAMP) mice where animals were fed with GSE by oral gavage at 200 mg/kg body weight dose during 4 to 28 weeks of age. Our results showed a significant reduction (46%, P cancer growth and progression in TRAMP mice, which could be mediated via a strong suppression of cell cycle progression and cell proliferation and an increase in apoptosis.

  16. Marine organism sulfated polysaccharides exhibiting significant antimalarial activity and inhibition of red blood cell invasion by Plasmodium.

    Science.gov (United States)

    Marques, Joana; Vilanova, Eduardo; Mourão, Paulo A S; Fernàndez-Busquets, Xavier

    2016-04-13

    The antimalarial activity of heparin, against which there are no resistances known, has not been therapeutically exploited due to its potent anticoagulating activity. Here, we have explored the antiplasmodial capacity of heparin-like sulfated polysaccharides from the sea cucumbers Ludwigothurea grisea and Isostichopus badionotus, from the red alga Botryocladia occidentalis, and from the marine sponge Desmapsamma anchorata. In vitro experiments demonstrated for most compounds significant inhibition of Plasmodium falciparum growth at low-anticoagulant concentrations. This activity was found to operate through inhibition of erythrocyte invasion by Plasmodium, likely mediated by a coating of the parasite similar to that observed for heparin. In vivo four-day suppressive tests showed that several of the sulfated polysaccharides improved the survival of Plasmodium yoelii-infected mice. In one animal treated with I. badionotus fucan parasitemia was reduced from 10.4% to undetectable levels, and Western blot analysis revealed the presence of antibodies against P. yoelii antigens in its plasma. The retarded invasion mediated by sulfated polysaccharides, and the ensuing prolonged exposure of Plasmodium to the immune system, can be explored for the design of new therapeutic approaches against malaria where heparin-related polysaccharides of low anticoagulating activity could play a dual role as drugs and as potentiators of immune responses.

  17. Marine organism sulfated polysaccharides exhibiting significant antimalarial activity and inhibition of red blood cell invasion by Plasmodium

    Science.gov (United States)

    Marques, Joana; Vilanova, Eduardo; Mourão, Paulo A. S.; Fernàndez-Busquets, Xavier

    2016-01-01

    The antimalarial activity of heparin, against which there are no resistances known, has not been therapeutically exploited due to its potent anticoagulating activity. Here, we have explored the antiplasmodial capacity of heparin-like sulfated polysaccharides from the sea cucumbers Ludwigothurea grisea and Isostichopus badionotus, from the red alga Botryocladia occidentalis, and from the marine sponge Desmapsamma anchorata. In vitro experiments demonstrated for most compounds significant inhibition of Plasmodium falciparum growth at low-anticoagulant concentrations. This activity was found to operate through inhibition of erythrocyte invasion by Plasmodium, likely mediated by a coating of the parasite similar to that observed for heparin. In vivo four-day suppressive tests showed that several of the sulfated polysaccharides improved the survival of Plasmodium yoelii-infected mice. In one animal treated with I. badionotus fucan parasitemia was reduced from 10.4% to undetectable levels, and Western blot analysis revealed the presence of antibodies against P. yoelii antigens in its plasma. The retarded invasion mediated by sulfated polysaccharides, and the ensuing prolonged exposure of Plasmodium to the immune system, can be explored for the design of new therapeutic approaches against malaria where heparin-related polysaccharides of low anticoagulating activity could play a dual role as drugs and as potentiators of immune responses. PMID:27071342

  18. Arrabidaea chica Hexanic Extract Induces Mitochondrion Damage and Peptidase Inhibition on Leishmania spp.

    Directory of Open Access Journals (Sweden)

    Igor A. Rodrigues

    2014-01-01

    Full Text Available Currently available leishmaniasis treatments are limited due to severe side effects. Arrabidaea chica is a medicinal plant used in Brazil against several diseases. In this study, we investigated the effects of 5 fractions obtained from the crude hexanic extract of A. chica against Leishmania amazonensis and L. infantum, as well as on the interaction of these parasites with host cells. Promastigotes were treated with several concentrations of the fractions obtained from A. chica for determination of their minimum inhibitory concentration (MIC. In addition, the effect of the most active fraction (B2 on parasite’s ultrastructure was analyzed by transmission electron microscopy. To evaluate the inhibitory activity of B2 fraction on Leishmania peptidases, parasites lysates were treated with the inhibitory and subinhibitory concentrations of the B2 fraction. The minimum inhibitory concentration of B2 fraction was 37.2 and 18.6 μg/mL for L. amazonensis and L. infantum, respectively. Important ultrastructural alterations as mitochondrial swelling with loss of matrix content and the presence of vesicles inside this organelle were observed in treated parasites. Moreover, B2 fraction was able to completely inhibit the peptidase activity of promastigotes at pH 5.5. The results presented here further support the use of A. chica as an interesting source of antileishmanial agents.

  19. Arrabidaea chica Hexanic Extract Induces Mitochondrion Damage and Peptidase Inhibition on Leishmania spp.

    Science.gov (United States)

    Rodrigues, Igor A.; Azevedo, Mariana M. B.; Chaves, Francisco C. M.; Alviano, Celuta S.; Alviano, Daniela S.; Vermelho, Alane B.

    2014-01-01

    Currently available leishmaniasis treatments are limited due to severe side effects. Arrabidaea chica is a medicinal plant used in Brazil against several diseases. In this study, we investigated the effects of 5 fractions obtained from the crude hexanic extract of A. chica against Leishmania amazonensis and L. infantum, as well as on the interaction of these parasites with host cells. Promastigotes were treated with several concentrations of the fractions obtained from A. chica for determination of their minimum inhibitory concentration (MIC). In addition, the effect of the most active fraction (B2) on parasite's ultrastructure was analyzed by transmission electron microscopy. To evaluate the inhibitory activity of B2 fraction on Leishmania peptidases, parasites lysates were treated with the inhibitory and subinhibitory concentrations of the B2 fraction. The minimum inhibitory concentration of B2 fraction was 37.2 and 18.6 μg/mL for L. amazonensis and L. infantum, respectively. Important ultrastructural alterations as mitochondrial swelling with loss of matrix content and the presence of vesicles inside this organelle were observed in treated parasites. Moreover, B2 fraction was able to completely inhibit the peptidase activity of promastigotes at pH 5.5. The results presented here further support the use of A. chica as an interesting source of antileishmanial agents. PMID:24818162

  20. Marrubium vulgare extract inhibits human-LDL oxidation and enhances HDL-mediated cholesterol efflux in THP-1 macrophage.

    Science.gov (United States)

    Berrougui, Hicham; Isabelle, Maxim; Cherki, Mounia; Khalil, Abdelouahed

    2006-12-14

    The objective of the present study was to elucidate the beneficial properties of aqueous extracts of Marrubium vulgare (AEM) towards cardiovascular disease by protecting human-LDL against lipid peroxidation and promoting HDL-mediated cholesterol efflux. Human-LDL were oxidised by incubation with CuSO(4) in the presence of increased concentrations of AEM (0-100 microg/ml). LDL lipid peroxidation was evaluated by conjugated diene formation, vitamin E disappearance as well as LDL-electrophoretic mobility. HDL-mediated cholesterol efflux assay was carried out in human THP-1 macrophages. Incubation of LDL with AEM significantly prolonged the lag phase (P=0.014), lowered the progression rate of lipid peroxidation (P=0.004), reduced the disappearance of vitamin E and the electrophoretic mobility in a dose-dependent manner. Also, incubation of HDL with AEM significantly increased HDL-mediated cholesterol efflux from THP-1 macrophages implicating an independent ATP binding cassette A1 (ABCA1) pathways. Our findings suggest that M. vulgare provides a source of natural antioxidants, which inhibit LDL oxidation and enhance reverse cholesterol transport and thus can prevent cardiovascular diseases development. These antioxidant properties increase the anti-atherogenic potential of HDL.

  1. Rosehip Extract Inhibits Lipid Accumulation in White Adipose Tissue by Suppressing the Expression of Peroxisome Proliferator-activated Receptor Gamma.

    Science.gov (United States)

    Nagatomo, Akifumi; Nishida, Norihisa; Matsuura, Yoichi; Shibata, Nobuhito

    2013-06-01

    Recent studies have shown that Rosa canina L. and tiliroside, the principal constituent of its seeds, exhibit anti-obesity and anti-diabetic activities via enhancement of fatty acid oxidation in the liver and skeletal muscle. However, the effects of rosehip, the fruit of this plant, extract (RHE), or tiliroside on lipid accumulation in adipocytes have not been analyzed. We investigated the effects of RHE and tiliroside on lipid accumulation and protein expression of key transcription factors in both in vitro and in vivo models. RHE and tiliroside inhibited lipid accumulation in a dose-dependent manner in 3T3-L1 cells. We also analyzed the inhibitory effect of RHE on white adipose tissue (WAT) in high-fat diet (HFD)-induced obesity mice model. Male C57BL/6J mice were fed HFD or HFD supplemented with 1% RHE (HFDRH) for 8 weeks. The HFDRH-fed group gained less body weight and had less visceral fat than the HFD-fed group. Liver weight was significantly lower in the HFDRH-fed group and total hepatic lipid and triglyceride (TG) content was also reduced. A significant reduction in the expression of peroxisome proliferator-activated receptor gamma (PPARγ) was observed in epididymal fat in the HFDRH-fed group, in comparison with controls, through Western blotting. These results suggest that downregulation of PPARγ expression is involved, at least in part, in the suppressive effect of RHE on lipid accumulation in WAT.

  2. Blackberry extract inhibits UVB-induced oxidative damage and inflammation through MAP kinases and NF-κB signaling pathways in SKH-1 mice skin

    Energy Technology Data Exchange (ETDEWEB)

    Divya, Sasidharan Padmaja; Wang, Xin; Pratheeshkumar, Poyil; Son, Young-Ok; Roy, Ram Vinod [Center for Research on Environmental Disease, University of Kentucky, 1095 VA Drive, Lexington, KY 40536 (United States); Department of Toxicology and Cancer Biology, University of Kentucky, 1095 VA Drive, Lexington, KY 40536 (United States); Kim, Donghern; Dai, Jin [Department of Toxicology and Cancer Biology, University of Kentucky, 1095 VA Drive, Lexington, KY 40536 (United States); Hitron, John Andrew; Wang, Lei [Center for Research on Environmental Disease, University of Kentucky, 1095 VA Drive, Lexington, KY 40536 (United States); Department of Toxicology and Cancer Biology, University of Kentucky, 1095 VA Drive, Lexington, KY 40536 (United States); Asha, Padmaja [National Centre for Aquatic Animal Health, Cochin University of Science and Technology, Cochin (India); Shi, Xianglin [Center for Research on Environmental Disease, University of Kentucky, 1095 VA Drive, Lexington, KY 40536 (United States); Department of Toxicology and Cancer Biology, University of Kentucky, 1095 VA Drive, Lexington, KY 40536 (United States); Zhang, Zhuo, E-mail: zhuo.zhang@uky.edu [Department of Toxicology and Cancer Biology, University of Kentucky, 1095 VA Drive, Lexington, KY 40536 (United States)

    2015-04-01

    Extensive exposure of solar ultraviolet-B (UVB) radiation to skin induces oxidative stress and inflammation that play a crucial role in the induction of skin cancer. Photochemoprevention with natural products represents a simple but very effective strategy for the management of cutaneous neoplasia. In this study, we investigated whether blackberry extract (BBE) reduces chronic inflammatory responses induced by UVB irradiation in SKH-1 hairless mice skin. Mice were exposed to UVB radiation (100 mJ/cm{sup 2}) on alternate days for 10 weeks, and BBE (10% and 20%) was applied topically a day before UVB exposure. Our results show that BBE suppressed UVB-induced hyperplasia and reduced infiltration of inflammatory cells in the SKH-1 hairless mice skin. BBE treatment reduced glutathione (GSH) depletion, lipid peroxidation (LPO), and myeloperoxidase (MPO) in mouse skin by chronic UVB exposure. BBE significantly decreased the level of pro-inflammatory cytokines IL-6 and TNF-α in UVB-exposed skin. Likewise, UVB-induced inflammatory responses were diminished by BBE as observed by a remarkable reduction in the levels of phosphorylated MAP Kinases, Erk1/2, p38, JNK1/2 and MKK4. Furthermore, BBE also reduced inflammatory mediators such as cyclooxygenase-2 (COX-2), prostaglandin E{sub 2} (PGE{sub 2}), and inducible nitric oxide synthase (iNOS) levels in UVB-exposed skin. Treatment with BBE inhibited UVB-induced nuclear translocation of NF-κB and degradation of IκBα in mouse skin. Immunohistochemistry analysis revealed that topical application of BBE inhibited the expression of 8-oxo-7, 8-dihydro-2′-deoxyguanosine (8-oxodG), cyclobutane pyrimidine dimers (CPD), proliferating cell nuclear antigen (PCNA), and cyclin D1 in UVB-exposed skin. Collectively, these data indicate that BBE protects from UVB-induced oxidative damage and inflammation by modulating MAP kinase and NF-κB signaling pathways. - Highlights: • Blackberry extract inhibits UVB-induced glutathione depletion.

  3. Selective growth inhibition of human breast cancer cells by graviola fruit extract in vitro and in vivo involving downregulation of EGFR expression.

    Science.gov (United States)

    Dai, Yumin; Hogan, Shelly; Schmelz, Eva M; Ju, Young H; Canning, Corene; Zhou, Kequan

    2011-01-01

    The epidermal growth factor receptor (EGFR) is an oncogene frequently overexpressed in breast cancer (BC), and its overexpression has been associated with poor prognosis and drug resistance. EGFR is therefore a rational target for BC therapy development. This study demonstrated that a graviola fruit extract (GFE) significantly downregulated EGFR gene expression and inhibited the growth of BC cells and xenografts. GFE selectively inhibited the growth of EGFR-overexpressing human BC (MDA-MB-468) cells (IC(50) = 4.8 μg/ml) but had no effect on nontumorigenic human breast epithelial cells (MCF-10A). GFE significantly downregulated EGFR mRNA expression, arrested cell cycle in the G0/G1 phase, and induced apoptosis in MDA-MB-468 cells. In the mouse xenograft model, a 5-wk dietary treatment of GFE (200 mg/kg diet) significantly reduced the protein expression of EGFR, p-EGFR, and p-ERK in MDA-MB-468 tumors by 56%, 54%, and 32.5%, respectively. Overall, dietary GFE inhibited tumor growth, as measured by wet weight, by 32% (P < 0.01). These data showed that dietary GFE induced significant growth inhibition of MDA-MB-468 cells in vitro and in vivo through a mechanism involving the EGFR/ERK signaling pathway, suggesting that GFE may have a protective effect for women against EGFR-overexpressing BC.

  4. Comparison of different cover crop mulches and extracts on inhibition of crop and weed growth

    Directory of Open Access Journals (Sweden)

    Sturm, Domonic Johannes

    2016-02-01

    Full Text Available Weed suppression of cover crops is a result of competition for light, space, water and nutrients and the release of allelochemicals in the soil. Two laboratory and greenhouse experiments were conducted to analyse biochemical effects of extracts and mulches of Fagopyrum tataricum (L. Gaertn., Raphanus sativus var. oleiformis Pers. and a cover crop mixture on germination and plant growth of the crop plants maize (Zea mays L. and sugar beet (Beta vulgaris ssp. vulgaris var. altissima Döll. and the weeds Chenopodium album L., Matricaria chamomilla L. and Stellaria media (L. Vill.. In the first experiment, aqueous cover crop extracts were applied on crop and weed seeds in germination assays. Germination rate, mean germination time and root length of crops and weeds were measured. In experiment 2, the influence of cover crop mulch on germination rate and dry weight of the test plants was determined after a period of 21 days. Significant reductions of the root length for all test plants were observed in experiment 1. Additionally, mean germination time was extended for crops and weeds by all cover crops. Germination rate and dry matter of crops and weeds were decreased significantly in experiment 2 compared to the untreated control. Root length, germination rate and mean germination time in germination tests in experiment 1 were found to be correlated with biomass of crops and weeds in experiment 2. This work reveals the important role of biochemical effects on weed suppression by cover crops.

  5. Repression of proinflammatory gene expression by lipid extract of Nostoc commune var sphaeroides Kützing, a blue-green alga, via inhibition of nuclear factor-kappaB in RAW 264.7 macrophages.

    Science.gov (United States)

    Park, Young-Ki; Rasmussen, Heather E; Ehlers, Sarah J; Blobaum, Kara R; Lu, Fan; Schlegal, Vicki L; Carr, Timothy P; Lee, Ji-Young

    2008-02-01

    We investigated whether lipid extract from a blue-green alga, N commune, modulates proinflammatory gene expression in RAW 264.7 macrophages. The cells were incubated with N commune lipid extract (0-100 microg/mL) and subsequently activated by LPS (100 ng/mL). Quantitative real-time PCR analysis showed that mRNA abundance of proinflammatory mediators, including TNF-alpha, COX-2, IL-1beta, IL-6, and iNOS, was significantly reduced by N commune lipid extract in a dose-dependent manner. Secretion of TNF-alpha and IL-1beta into cell culture medium was also significantly decreased by N commune lipid extract. Thin-layer chromatography-densitometry analysis showed that N commune lipid extract contained approximately 15% of fatty acids. To determine whether the inhibition of proinflammatory mediator production by N commune lipid extract is primarily conferred by fatty acids in the lipid extract, macrophages were incubated with 100 microg/mL of N commune lipid extract or 15 microg/mL of a fatty acid mixture, which was formulated to reflect the fatty acid composition of N commune lipid extract. The fatty acid mixture significantly reduced RNA abundance of TNF-alpha and COX-2, but to a lesser extent than did the N commune lipid extract, suggesting the presence of additional bioactive compounds with an antiinflammatory property in the lipid extract. As NF-kappaB is a major regulator for the proinflammatory gene expression, we measured its DNA-binding activity. DNA-binding activity of NF-kappaB was significantly reduced by N commune lipid extract. In conclusion, our study suggests that N commune lipid extract represses the expression of proinflammatory genes in RAW 264.7 macrophages, at least in part, by inhibiting the activation of NF-kappaB pathway.

  6. Inhibition of glucose-and fructose-mediated protein glycation by infusions and ethanolic extracts of ten culinary herbs and spices

    Institute of Scientific and Technical Information of China (English)

    Jugjeet Singh Ramkissoon; Mohamad Fawzi Mahomoodally; Anwar Hussein Subratty; Nessar Ahmed

    2016-01-01

    Objective: To investigate the inhibitory activity of ten culinary herbs and spices namely on glucose-mediated glycation(GMG) and fructose-mediated glycation(FMG) of bovine serum albumin.Methods: Fluorescence was used as an index of albumin glycation using glucose and fructose as substrates in the presence of infusions and ethanolic extracts of ten culinary herbs and spices. Antioxidant activity of the extracts was evaluated using reducing power,metal ion chelating and superoxide radical scavenging assays. Phytochemicals profile was analysed using 13 standard methods.Results: FMG was found to be significantly higher than GMG(95 and 84 AU,respectively; P 0.05) was found in the percentage glycation inhibitory activity of infusions compared to ethanolic extracts. The mean percentage inhibitory activity of the extracts for GMG(45.9%) and for FMG(45.1%) was not significantly different(P > 0.05). Qualitative phytochemical analysis showed the presence of alkaloids, flavonoids, tannins, terpenoids, anthraquinones, steroids, reducing sugars, proteins, phenols,saponins, phlobatannins, and cardiac glycosides.Conclusions: The higher rate of fluorescence generation by fructation suggests that glycation by fructose deserves much attention as a glycating agent. Data herein showed that the extracts inhibited GMG and FMG. Thus, these edible plants could be a natural source of antioxidants and anti-glycation agent for preventing advanced glycation endproducts-mediated complications.

  7. Green corrosion inhibition of mild steel to aqueous sulfuric acid by the extract of Corchorus olitorius stems

    Science.gov (United States)

    Gobara, Mohamed; Zaghloul, Basem; Baraka, Ahmad; Elsayed, Mohamed; Zorainy, Mahmoud; Mokhtar Kotb, Mohamed; Elnabarawy, Hany

    2017-04-01

    Extract of Corchorus olitorius stems (ECS) was used as a green inhibitor for the inhibition of mild steel corrosion in 0.5 M H2SO4 solution. GC/MS was used for both qualitative and quantitative analysis of the extract. The corrosion performance of the extract was evaluated using electrochemical impedance spectroscopy, potentiodynamic polarization and weight loss. The results showed that ECS is a mixed-type inhibitor which reduces both anodic and cathodic reactions and the inhibition efficiency was reached up to 93%. Adsorption isotherm data was recorded at different temperatures and analyzed by selected adsorption isotherm models to reveal characteristics of inhibition. Thermodynamic calculations showed that the inhibition efficiency increases with increasing inhibitor concentration, and decreases with increasing temperature. Adsorption of ECS on the mild steel surface was found to be spontaneous and exothermic. Adsorption is suggested to be physisorption according to El-Awady isotherm model. Also, the scanning electron microscopy (SEM) was used to investigate the surface morphology to confirm the corrosion results.

  8. Herbal extracts of Tribulus terrestris and Bergenia ligulata inhibit growth of calcium oxalate monohydrate crystals in vitro

    Science.gov (United States)

    Joshi, V. S.; Parekh, B. B.; Joshi, M. J.; Vaidya, A. B.

    2005-02-01

    A large number of people in this world are suffering from urinary stone problem. Calcium oxalate monohydrate (COM) and calcium oxalate dihydrate (COD) containing stones (calculi) are commonly found. In the present study, COM crystals were grown by a double diffusion gel growth technique using U-tubes. The gel was prepared from hydrated sodium metasilicate solution. The gel framework acts like a three-dimensional crucible in which the crystal nuclei are delicately held in the position of their formation, and nutrients are supplied for the growth. This technique can be utilized as a simplified screening static model to study the growth, inhibition and dissolution of urinary stones in vitro. The action of putative litholytic medicinal plants, Tribulus terrestris Linn. ( T.t) and Bergenia ligulata Linn. ( B.l.), has been studied in the growth of COM crystals. Tribulus terrestris and Bergenia ligulata are commonly used as herbal medicines for urinary calculi in India. To verify the inhibitive effect, aqueous extracts of Tribulus terrestris and Bergenia ligulata were added along with the supernatant solutions. The growth was measured and compared, with and without the aqueous extracts. Inhibition of COM crystal growth was observed in the herbal extracts. Maximum inhibition was observed in Bergenia ligulata followed by Tribulus terrestris. The results are discussed.

  9. Inhibition of human calcineurin and yeast calcineurin-dependent gene expression by Jasminum humile leaf and root extracts.

    Science.gov (United States)

    Prescott, Thomas A K; Ariño, Joaquín; Kite, Geoffrey C; Simmonds, Monique S J

    2012-03-27

    The leaves of Jasminum humile are used to treat skin disorders in a way which resembles the use of modern topical anti-inflammatory drugs. Ethanolic extracts of the roots and leaves were shown to inhibit calcineurin which is a regulator of inflammatory gene expression. A novel yeast calcineurin reporter gene assay suitable for a 96 well plate format was developed to test for inhibition of calcineurin-dependent gene expression. Calmodulin/calcineurin phosphatase assays were then used to further elucidate the mode of action of the extracts. Jasminum humile root and leaf extract exhibited calcineurin inhibition activity that was shown to be mediated through a direct interaction with calcineurin enzyme. The activity is sufficient to block calcineurin-dependent gene expression in a yeast model. The activity of the plant supports its traditional use in the treatment of inflammatory skin disorders. The specially adapted yeast reporter assay was found to be a highly effective way of detecting calcineurin inhibitors in plant extracts. Crown Copyright © 2012. Published by Elsevier Ireland Ltd. All rights reserved.

  10. SCAVENGING ACTIVITY, ANTI-INFLAMMATORY AND DIABETES RELATED ENZYME INHIBITION PROPERTIES OF ETHANOL LEAVES EXTRACT OF PHOENYX DACTYLIFERA

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    S. E. Laouini

    2015-07-01

    Full Text Available In this study we investigate the antioxidant, anti-inflammatory, and antidiabetic activities of ethanolic leaf extracts of three selected varieties of Phoenyx dactylifera L. namely: “Ghars”, “Deglet Nour” and “Hamraya”. The assessment of the antioxidant potential of crude leaf extracts, using superoxide anions inhibition, radical scavenging activity "DPPH" and total antioxidant activity essays, was carried out. Furthermore, the anti-inflammatory properties of the extracts were determined by measuring the inhibition of nitric oxide (NO production. Moreover, the antidiabetic effect was evaluated by inhibition of α-amylase and α-glucosidase enzymes. The total phenolic content measured by Folin-ciocalteu method. The raw leaf extracts of the selected varieties were found to contain a high content of total phenolic content (342.45 mg GAE/ gDW for GE and therefore exhibited a higher antioxidant activity and inhibitory effect of radicals scavenging activity against DPPH and superoxide anion (IC50=7.44 μg/mL and 39.11 μg/mL respectively.

  11. SCAVENGING ACTIVITY, ANTI-INFLAMMATORY AND DIABETES RELATED ENZYME INHIBITION PROPERTIES OF ETHANOL LEAVES EXTRACT OF PHOENYX DACTYLIFERA

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    S. E. Laouini

    2013-12-01

    Full Text Available In this study we investigate the antioxidant, anti-inflammatory, and antidiabetic activities of ethanolic leaf extracts of three selected varieties of Phoenyx dactylifera L. namely: “Ghars”, “Deglet Nour” and “Hamraya”. The assessment of the antioxidant potential of crude leaf extracts, using superoxide anions inhibition, radical scavenging activity "DPPH" and total antioxidant activity essays, was carried out. Furthermore, the anti-inflammatory properties of the extracts were determined by measuring the inhibition of nitric oxide (NO production. Moreover, the antidiabetic effect was evaluated by inhibition of α-amylase and α-glucosidase enzymes. The total phenolic content measured by Folin-ciocalteu method. The raw leaf extracts of the selected varieties were found to contain a high content of total phenolic content (342.45 mg GAE/ gDW for GE and therefore exhibited a higher antioxidant activity and inhibitory effect of radicals scavenging activity against DPPH and superoxide anion (IC50=7.44 μg/mL and 39.11 μg/mL respectively.

  12. Evaluation of the Inhibition of Carbohydrate Hydrolyzing Enzymes, the Antioxidant Activity, and the Polyphenolic Content of Citrus limetta Peel Extract

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    Eduardo Padilla-Camberos

    2014-01-01

    Full Text Available Type 2 diabetes mellitus is one of the most frequent causes of death in Mexico, characterized by chronic hyperglycemia. One alternative strategy for this metabolic abnormality is inhibiting the enzymes responsible for the metabolism of carbohydrates. We evaluated whether the aqueous Citrus limetta peel extract could inhibit the metabolism of carbohydrates. We found that this extract inhibited primarily the enzyme α-amylase by 49.6% at a concentration of 20 mg/mL and to a lesser extent the enzyme α-glucosidase with an inhibition of 28.2% at the same concentration. This inhibition is likely due to the high polyphenol content in the Citrus limetta peel (19.1 mg GAE/g. Antioxidant activity of the Citrus limetta peel demonstrated dose-dependent antioxidant activity, varying from 6.5% at 1.125 mg/mL to 42.5% at 20 mg/mL. The study of these polyphenolic compounds having both antihyperglycemic and antioxidant activities may provide a new approach to the management of type 2 diabetes mellitus.

  13. Inhibition of lipid oxidation and rancidity in precooked pork patties by radical-scavenging licorice (Glycyrrhiza glabra) extract.

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    Jiang, Jiang; Zhang, Xin; True, Alma D; Zhou, Lirong; Xiong, Youling L

    2013-11-01

    This study investigated the efficacy of licorice extract (LE) to curtail lipid oxidation and protect sensory attributes of ground pork during refrigerated and frozen storage. Pork patties (20% fat) were formulated with 0%, 0.02%, 0.05%, and 0.1% (meat basis) LE or rosemary extract (RE) as comparison or 0.01% (fat basis) BHA with 0 or 1.5% NaCl. Raw and precooked (75 °C) patties were packaged in polyvinylchloride overwrapped trays and stored at 2 °C up to 7 and 14 d, respectively, or at -20 °C up to 6 mo. Lipid oxidation (thiobarbituric acid-reactive substances [TBARS]) and sensory attributes of stored patty samples were evaluated, radical scavenging activity of the LE was measured, and the active phenolic compounds were identified. Cooking yield (<85%) was similar among antioxidant treatments, and lipid oxidation was minimal in refrigerated or frozen raw samples. However, TBARS values in refrigerated precooked control patties (0.22 mg/kg) rose to 9.3 to 9.4 mg/kg after 14 d, compared to 3.4 to 4.4 and 4.4 to 6.9 mg/kg in patties treated with 0.1% LE and RE, respectively. In frozen precooked samples, TBARS (0.22 mg/kg) increased to 1.3 mg/kg (P < 0.05) in control patties after 6 mo and had no significant change in patties treated with 0.1% LE or 0.01% butylated hydroxyanisol. Sensory panel evaluation confirmed strong inhibition of rancidity production by LE, corroborating its remarkable antiradical activity due to the presence of multiple phenolics. The results indicate that licorice has great potential as a natural antioxidative additive to extend the shelf-life of precooked pork.

  14. An extract of Phellinus linteus grown on germinated brown rice inhibits inflammation markers in RAW264.7 macrophages by suppressing inflammatory cytokines, chemokines, and mediators and up-regulating antioxidant activity.

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    Park, Hye-Jin; Han, Eun Su; Park, Dong Ki; Lee, Chan; Lee, Ki Won

    2010-12-01

    The immunomodulatory activity of an organic extract of Phellinus linteus grown on slightly germinated brown rice (PBR) was previously demonstrated. Here, we investigated the possible anti-inflammatory activity of the PBR extract by analyzing its effect on the expression of macrophage-derived cytokines, chemokines, and mediator genes that participate in immune and inflammatory responses and diseases. The extract profoundly inhibited the induction of cytokines and chemokines, including tumor necrosis factor-α, chemokine (C-X-C motif) ligand-10, granulocyte-macrophage colony-stimulating factor, and interleukin-6, in lipopolysaccharide (LPS)-stimulated RAW264.7 mouse macrophage cells. It also greatly inhibited LPS-stimulated production of nitric oxide (NO) and prostaglandin E(2) in RAW264.7 cells by suppressing the expression of inducible NO synthase and cyclooxygenase-2. PBR extract inhibited NO production with a twofold lower half-maximal inhibitory concentration value than P. linteus extract. To elucidate the underlying mechanism of action, we examined the effect of the PBR extract on the LPS-induced phosphorylation of mitogen-activated protein kinases (MAPKs) in RAW264.7 cells. PBR extract greatly inhibited extracellular signal-regulated kinase and c-Jun N-terminal kinase phosphorylation and slightly inhibited p38 MAPK phosphorylation. It also significantly increased intracellular glutathione peroxidase activity and heme oxygenase-1 protein expression. Thus, the PBR extract has anti-inflammatory activity in LPS-stimulated RAW264.7 cells by virtue of its ability to suppress the production of inflammatory cytokines and chemokines via inhibition of MAPK activation and up-regulation of antioxidant activities.

  15. Direct contact between dendritic cells and bronchial epithelial cells inhibits T cell recall responses towards mite and pollen allergen extracts in vitro.

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    Papazian, D; Wagtmann, V R; Hansen, S; Würtzen, P A

    2015-08-01

    Airway epithelial cells (AECs) form a polarized barrier along the respiratory tract. They are the first point of contact with airborne antigens and are able to instruct resident immune cells to mount appropriate immune responses by either soluble or contact-dependent mechanisms. We hypothesize that a healthy, polarized epithelial cell layer inhibits inflammatory responses towards allergens to uphold homeostasis. Using an in-vitro co-culture model of the airway epithelium, where a polarized cell layer of bronchial epithelial cells can interact with dendritic cells (DCs), we have investigated recall T cell responses in allergic patients sensitized to house dust mite, grass and birch pollen. Using allergen extract-loaded DCs to stimulate autologous allergen-specific T cell lines, we show that AEC-imprinted DCs inhibit T cell proliferation significantly of Bet v 1-specific T cell lines as well as decrease interleukin (IL)-5 and IL-13 production, whereas inhibition of Phl p 5-specific T cells varied between different donors. Stimulating autologous CD4(+) T cells from allergic patients with AEC-imprinted DCs also inhibited proliferation significantly and decreased production of both T helper type 1 (Th1) and Th2 cytokines upon rechallenge. The inhibitory effects of AECs' contact with DCs were absent when allergen extract-loaded DCs had been exposed only to AECs supernatants, but present after direct contact with AECs. We conclude that direct contact between DCs and AECs inhibits T cell recall responses towards birch, grass and house dust mite allergens in vitro, suggesting that AECs-DC contact in vivo constitute a key element in mucosal homeostasis in relation to allergic sensitisation.

  16. Phenolic Extract from Moringa oleifera Leaves Inhibits Key Enzymes Linked to Erectile Dysfunction and Oxidative Stress in Rats' Penile Tissues.

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    Oboh, Ganiyu; Ademiluyi, Adedayo O; Ademosun, Ayokunle O; Olasehinde, Tosin A; Oyeleye, Sunday I; Boligon, Aline A; Athayde, Margareth L

    2015-01-01

    This study was designed to determine the antioxidant properties and inhibitory effects of extract from Moringa oleifera leaves on angiotensin-I-converting enzyme (ACE) and arginase activities in vitro. The extract was prepared and phenolic (total phenols and flavonoid) contents, radical (nitric oxide (NO), hydroxyl (OH)) scavenging abilities, and Fe(2+)-chelating ability were assessed. Characterization of the phenolic constituents was done via high performance liquid chromatography-diode array detection (HPLC-DAD) analysis. Furthermore, the effects of the extract on Fe(2+)-induced MDA production in rats' penile tissue homogenate as well as its action on ACE and arginase activities were also determined. The extract scavenged NO (∗) , OH (∗) , chelated Fe(2+), and inhibited MDA production in a dose-dependent pattern with IC50 values of 1.36, 0.52, and 0.38 mg/mL and 194.23 µg/mL, respectively. Gallic acid, chlorogenic acid, quercetin, and kaempferol were the most abundant phenolic compounds identified in the leaf extract. The extract also inhibited ACE and arginase activities in a dose-dependent pattern and their IC50 values were 303.03 and 159.59 µg/mL, respectively. The phenolic contents, inhibition of ACE, arginase, and Fe(2+)-induced MDA production, and radical (OH (∗) , NO (∗) ) scavenging and Fe(2+)-chelating abilities could be some of the possible mechanisms by which M. oleifera leaves could be used in the treatment and/or management of erectile dysfunction.

  17. Anthocyanin-rich purple corn extract inhibit diabetes-associated glomerular angiogenesis.

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    Min-Kyung Kang

    Full Text Available Diabetic nephropathy (DN is one of the major diabetic complications and the leading cause of end-stage renal disease. Abnormal angiogenesis results in new vessels that are often immature and play a pathological role in DN, contributing to renal fibrosis and disrupting glomerular failure. Purple corn has been utilized as a daily food and exerts disease-preventive activities. This study was designed to investigate whether anthocyanin-rich purple corn extract (PCE prevented glomerular angiogenesis under hyperglycemic conditions. Human endothelial cells were cultured in conditioned media of mesangial cells exposed to 33 mM high glucose (HG-HRMC-CM. PCE decreased endothelial expression of vascular endothelial growth factor (VEGF and hypoxia inducible factor (HIF-1α induced by HG-HRMC-CM. Additionally, PCE attenuated the induction of the endothelial marker of platelet endothelial cell adhesion molecule (PECAM-1 and integrin β3 enhanced in HG-HRMC-CM. Endothelial tube formation promoted by HG-HRMC-CM was disrupted in the presence of PCE. In the in vivo study employing db/db mice treated with 10 mg/kg PCE for 8 weeks, PCE alleviated glomerular angiogenesis of diabetic kidneys by attenuating the induction of VEGF and HIF-1α. Oral administration of PCE retarded the endothelial proliferation in db/db mouse kidneys, evidenced by its inhibition of the induction of vascular endothelium-cadherin, PECAM-1 and Ki-67. PCE diminished the mesangial and endothelial induction of angiopoietin (Angpt proteins under hypeglycemic conditions. The induction and activation of VEGF receptor 2 (VEGFR2 were dampened by treating PCE to db/db mice. These results demonstrate that PCE antagonized glomerular angiogenesis due to chronic hyperglycemia and diabetes through disturbing the Angpt-Tie-2 ligand-receptor system linked to renal VEGFR2 signaling pathway. Therefore, PCE may be a potent therapeutic agent targeting abnormal angiogenesis in DN leading to kidney failure.

  18. Inhibition of Saccharomyces cerevisiae Pdr5p by a natural compound extracted from Brazilian Red Propolis

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    Cinzia Lotti

    2011-10-01

    Full Text Available Multidrug resistance of cancer cells and pathogenic microorganisms leading to the treatment failure of some forms of cancer or life-threatening bacterial or fungal infections is often caused by the overexpression of multidrug efflux pumps belonging to the ATP-binding cassette transporters superfamily. The multidrug resistance of fungal cells often involves the overexpression of efflux pumps belonging to the pleiotropic drug resistance (PDR family of ABC transporters. Possibly the best-studied fungal PDR transporter is the multidrug resistance transporter Pdr5p of Saccharomyces cerevisiae. Some research groups have been searching for new inhibitors of these efflux pumps in order to alleviate resistance. Natural products are a great source for the discovery of new compounds with biological activity. Propolis is a complex resinous material collected by honeybees from exudates and buds of certain plant sources and this material is thought to serve as a defense substance for bee hives. Propolis is widely used in traditional medicine and is reported to have a broad spectrum of pharmacological properties. Literature reported some biological functionalities of propolis, such as antibacterial, antiviral, fungicidal, anti-inflammatory and anti-carcinogenic activities. The chemical composition of propolis is qualitatively and quantitatively variable. Components isolated from methanolic extract of red Brazilian propolis (Alagoas, Northeast of Brazil are isoflavonoids (including pterocarpans, isoflavans, isoflavones, flavanones and polyprenylated benzophenones. In this work we demonstrated the effects of five different isolated compounds on the ATPase activity of Pdr5p. Out of all five substances tested, only BRP-1 was able to completely abolish the enzymatic activity while others worked as positive modulators of the enzyme activity. BRP-1also inhibited the efflux of Rhodamine 6G from yeast cells overexpressing Pdr5p. Taken together, these results

  19. Milk Thistle Extract and Silymarin Inhibit Lipopolysaccharide Induced Lamellar Separation of Hoof Explants in Vitro

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    Nicole Reisinger

    2014-10-01

    Full Text Available The pathogenesis of laminitis is not completely identified and the role of endotoxins (lipopolysaccharides, LPS in this process remains unclear. Phytogenic substances, like milk thistle (MT and silymarin, are known for their anti-inflammatory and antioxidant properties and might therefore have the potential to counteract endotoxin induced effects on the hoof lamellar tissue. The aim of our study was to investigate the influence of endotoxins on lamellar tissue integrity and to test if MT and silymarin are capable of inhibiting LPS-induced effects in an in vitro/ex vivo model. In preliminary tests, LPS neutralization efficiency of these phytogenics was determined in an in vitro neutralization assay. Furthermore, tissue explants gained from hooves of slaughter horses were tested for lamellar separation after incubation with different concentrations of LPS. By combined incubation of explants with LPS and either Polymyxin B (PMB; positive control, MT or silymarin, the influence of these substances on LPS-induced effects was assessed. In the in vitro neutralization assay, MT and silymarin reduced LPS concentrations by 64% and 75%, respectively, in comparison PMB reduced 98% of the LPS concentration. In hoof explants, LPS led to a concentration dependent separation. Accordantly, separation force was significantly decreased by 10 µg/mL LPS. PMB, MT and silymarin could significantly improve tissue integrity of explants incubated with 10 µg/mL LPS. This study showed that LPS had a negative influence on the structure of hoof explants in vitro. MT and silymarin reduced endotoxin activity and inhibited LPS-induced effects on the lamellar tissue. Hence, MT and silymarin might be used to support the prevention of laminitis and should be further evaluated for this application.

  20. Attenuation of cysteamine-induced duodenal ulcer with Cochinchina momordica seed extract through inhibiting cytoplasmic phospholipase A2/5-lipoxygenase and activating γ-glutamylcysteine synthetase.

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    Choi, Ki-Seok; Kim, Eun-Hee; Hong, Hua; Ock, Chan Young; Lee, Jeong Sang; Kim, Joo-Hyun; Hahm, Ki-Baik

    2012-04-01

    Cysteamine is a reducing aminothiol used for inducing duodenal ulcer through mechanisms of oxidative stress related to thiol-derived H(2)O(2) reaction. Cochinchina momordica saponins have been suggested to be protective against various gastric diseases based on their cytoprotective and anti-inflammatory mechanisms. This study was aimed to document the preventive effects of Cochinchina momordica seed extract against cysteamine-induced duodenal ulcer as well as the elucidation of its pharmacological mechanisms. Cochinchina momordica seed extract (50, 100, 200 mg/kg) was administrated intragastrically before cysteamine administration, after which the incidence of the duodenal ulcer, ulcer size, serum gastrin level, and the ratio of reduced glutathione (GSH)/oxidized glutathione disulfide (GSSG) as well as biochemical and molecular measurements of cytoplasmic phospholipase A(2) (cPLA(2)), cyclooxygenase-2 (COX-2), 5-lipoxygenase and the expression of proinflammatory genes including IL-1β, IL-6, COX-2 were measured in rat model. Additional experiments of electron spin resonance measurement and the changes of glutathione were performed. Cochinchina momordica seed extract effectively prevented cysteamine-induced duodenal ulcer in a dose-dependent manner as reflected with significant decreases in either duodenal ulcerogenesis or perforation accompanied with significantly decreased in serum gastrin in addition to inflammatory mediators including cPLA(2), COX-2, and 5-lipoxygenase. Cochinchina momordica seed extract induced the expression of γ-glutamylcysteine synthetase (γ-GCS)-related glutathione synthesis as well as significantly reduced the expression of cPLA(2). Cochinchina momordica seed extract preserved reduced glutathione through increased expressions of γ-GCS. Cochinchina momordica seed extracts exerted significantly protective effect against cysteamine-induced duodenal ulcer by either cPLA2 inhibition or glutathione preservation. © 2012 Journal of

  1. Inhibitive effect of Xylopia ferruginea extract on the corrosion of mild steel in 1M HCl medium

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    Raja, Pandian Bothi; Rahim, Afidah Abdul; Osman, Hasnah; Awang, Khalijah

    2011-08-01

    The alkaloid content of the leaves and stem bark of Xylopia ferruginea plant was isolated and tested for its anticorrosion potential on mild steel corrosion in a hydrochloric acid medium by using electrochemical impedance spectroscopy, potentiodynamic polarization measurement, scanning electron microscopy (SEM), and Fourier transform infra red (FTIR) analysis. The experimental results reveal the effective anticorrosion potential of the plant extract. The mixed mode of action exhibited by the plant extract is evidenced from the polarization study. SEM images proof the formation of a protective layer over the mild steel surface, and this is supported by the FTIR study. The possible mode of the corrosion inhibition mechanism has also been discussed.

  2. Lysimachia foenum-graecum Herba Extract, a Novel Biopesticide, Inhibits ABC Transporter Genes and Mycelial Growth of Magnaporthe oryzae

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    Youngjin Lee

    2016-02-01

    Full Text Available To identify a novel biopesticide controlling rice blast disease caused by Magnaporthe oryzae, 700 plant extracts were evaluated for their inhibitory effects on mycelial growth of M. oryzae. The L. foenum-graecum Herba extract showed the lowest inhibition concentration (IC₅₀ of 39.28 μg/ml, which is lower than the IC₅₀ of blasticidin S (63.06 μg/ml, a conventional fungicide for rice blast disease. When treatments were combined, the IC₅₀ of blasticidin S was dramatically reduced to 10.67 μg/ml. Since ABC transporter genes are involved in fungicide resistance of many organisms, we performed RT-PCR to investigate the transcriptional changes of 40 ABC transporter family genes of M. oryzae treated with the plant extract, blasticidin S, and tetrandrine, a recognized ABC transporter inhibitor. Four ABC transporter genes were prominently activated by blasticidin S treatment, but were suppressed by combinational treatment of blasticidin S with the plant extract, or with tetrandrine that didn’t show cellular toxicity by itself in this study. Mycelial death was detected via confocal microscopy at 24 h after plant extract treatment. Finally, subsequent rice field study revealed that the plant extract had high control efficacy of 63.3% and should be considered a biopesticide for rice blast disease. These results showed that extract of L. foenum graecum Herba suppresses M. oryzae ABC transporter genes inducing mycelial death and therefore may be a potent novel biopesticide.

  3. Antinociception produced by Thalassia testudinum extract BM-21 is mediated by the inhibition of acid sensing ionic channels by the phenolic compound thalassiolin B

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    Thomas Olivier P

    2011-01-01

    Full Text Available Abstract Background Acid-sensing ion channels (ASICs have a significant role in the sensation of pain and constitute an important target for the search of new antinociceptive drugs. In this work we studied the antinociceptive properties of the BM-21 extract, obtained from the sea grass Thalassia testudinum, in chemical and thermal models of nociception in mice. The action of the BM-21 extract and the major phenolic component isolated from this extract, a sulphated flavone glycoside named thalassiolin B, was studied in the chemical nociception test and in the ASIC currents of the dorsal root ganglion (DRG neurons obtained from Wistar rats. Results Behavioral antinociceptive experiments were made on male OF-1 mice. Single oral administration of BM-21 produced a significant inhibition of chemical nociception caused by acetic acid and formalin (specifically during its second phase, and increased the reaction time in the hot plate test. Thalassiolin B reduced the licking behavior during both the phasic and tonic phases in the formalin test. It was also found that BM-21 and thalassiolin B selectively inhibited the fast desensitizing (τ Conclusions To our knowledge, this is the first report of an ASIC-current inhibitor derived of a marine-plant extract, and in a phenolic compound. The antinociceptive effects of BM-21 and thalassiolin B may be partially because of this action on the ASICs. That the active components of the extract are able to cross the blood-brain barrier gives them an additional advantage for future uses as tools to study pain mechanisms with a potential therapeutic application.

  4. Extracts of Azadirachta indica and Melia azedarach seeds inhibit folliculogenesis in albino rats

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    Roop J.K.

    2005-01-01

    Full Text Available The seed oil of Azadirachta indica A. Juss (neem is used in traditional medicine for its antidiabetic, spermicidal, antifertility, antibacterial, and wound healing properties. The present study was undertaken to investigate the quantitative aspects of follicular development in cyclic female albino rats (135 ± 10 g; 8 groups with 6 animals in each group after oral administration of polar (PF and non-polar (NPF fractions of A. indica seed extract at 3 and 6 mg kg body weight-1 day-1 and Melia azedarach Linn. (dharek seed extract at 24 mg kg body weight-1 day-1 for 18 days. The extracts were prepared using a flash evaporator at 35°C and then dissolved in olive oil to prepare doses on a per kg body weight basis. There was a significant reduction (P = 0.05 in the number of normal single layered follicles (A. indica: 0.67 ± 0.33 and 4.67 ± 2.03 after 3 and 6 mg/kg NPF, and 3.33 ± 1.67 and 1.00 ± 1.00 after 3 and 6 mg/kg PF vs control: 72.67 ± 9.14 and M. azedarach: 0.60 ± 0.40 and 1.80 ± 1.2 after 24 mg/kg PF and NPF, respectively, vs control: 73.40 ± 7.02 and follicles in various stages (I-VII of follicular development in all treatment groups. These extracts also significantly reduced (P = 0.05 the total number of normal follicles in the neem (14.67 ± 5.93 and 1.00 ± 1.00 after 3 and 6 mg/kg PF and 3.67 ± 0.88 and 5.33 ± 2.03 after 3 and 6 mg/kg NPF and dharek (13.00 ± 3.58 and 14.60 ± 2.25 after 24 mg/kg NPF and PF treatments compared to control (216.00 ± 15.72 and 222.20 ± 19.52, respectively. Currently, indiscriminate use of persistent and toxic rodenticides to control rodent populations has created serious problems such as resistance and environmental contamination. Therefore, it becomes necessary to use ecologically safe and biologically active botanical substances that are metabolized and are not passed on to the next trophic level, and that interfere with the reproductive potential particularly growth and differentiation of

  5. Fucans, sulfated polysaccharides extracted from brown seaweeds, inhibit vascular smooth muscle cell proliferation. II. Degradation and molecular weight effect.

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    Logeart, D; Prigent-Richard, S; Boisson-Vidal, C; Chaubet, F; Durand, P; Jozefonvicz, J; Letourneur, D

    1997-12-01

    Fucan, a sulfated polysaccharide extracted from brown seaweeds, inhibits smooth muscle cell (SMC) proliferation with a higher antiproliferative activity than heparin (Logeart et al., Eur. J. Cell Biol. 74, 1997, this issue). In order to investigate the structure-activity relationship of fucan on SMC growth, we have prepared by size exclusion chromatography fucan fractions of various molecular masses ranging from 5.5 to 556 kDa. Our experiments showed that the antiproliferative activity is dependent on the molecular weight of the polysaccharide. The molecular weight threshold indicated that about 30 saccharidic units on fucan were necessary to give the antiproliferative activity on SMCs. A kinetics study of DNA synthesis using tritiated thymidine uptake was also performed with different molecular weight fucan fractions. Although all tested fractions acted as soon as the cells enter the first cell cycle, the duration and potency of action varied. Moreover, displacement experiments of iodinated fucan revealed that the low molecular fucan fraction interacted weakly with the binding sites. Finally, gel permeation chromatography of internalized radiolabeled heparin and fucans was performed with SMCs. A rapid degradation of internalized heparin was observed, whereas only low molecular weight fucan fractions were partially degraded by SMCs. Together, these results indicate the significance of molecular weight on the antiproliferative activity of fucans on SMCs, and might help to understand their mechanism of action. In addition, the degradation experiments with internalized heparin and fucans ruled out a direct link between polysaccharide degradation and the antiproliferative effect on SMCs.

  6. Fenugreek Seed Extract Inhibit Fat Accumulation and Ameliorates Dyslipidemia in High Fat Diet-Induced Obese Rats

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    Parveen Kumar

    2014-01-01

    Full Text Available This study investigated the inhibitory effect of aqueous extract of Trigonella foenum-graecum seeds (AqE-TFG on fat accumulation and dyslipidemia in high fat diet- (HFD- induced obese rats. Female Wistar rats were fed with HFD ad libitum, and the rats on HFD were treated orally with AqE-TFG or orlistat ((HFD for 28 days + AqE-TFG (0.5 and 1.0 g/kg or orlistat (10 mg/kg from day 8 to 28, respectively. Treatment with AqE-TFG produced significant reduction in body weight gain, body mass index (BMI, white adipose tissue (WAT weights, blood glucose, serum insulin, lipids, leptin, lipase, and apolipoprotein-B levels and elevation in adiponectin levels. AqE-TFG improved serum aspartate amino transferase (AST, alanine amino transferase (ALT, and lactate dehydrogenase (LDH levels. AqE-TFG treatment reduced the hepatic and cardiac thiobarbituric acid reactive substances (TBARS and elevated the antioxidant enzyme (glutathione (GSH, superoxide dismutase (SOD, and catalase (CAT levels. In addition, liver and uterine WAT lipogenic enzyme (fatty acid synthetase (FAS and glucose-6-phosphate dehydrogenase (G6PD activities were restored towards normal levels. These findings demonstrated the preventive effect of AqE-TFG on fat accumulation and dyslipidemia, due to inhibition of impaired lipid digestion and absorption, in addition to improvement in glucose and lipid metabolism, enhancement of insulin sensitivity, increased antioxidant defense, and downregulation of lipogenic enzymes.

  7. Study on Effects of Extracts from Salvia Miltiorrhiza and Curcuma Longa in Inhibiting Phosphorylated Extracellular Signal Regulated Kinase Expression in Rat's Hepatic Stellate Cells

    Institute of Scientific and Technical Information of China (English)

    CHENG Yang; PING Jian; LIU Cheng; TAN Ying-zi; CHEN Gao-feng

    2006-01-01

    Objective: To study the effect of salvianolic acid B (SAB) and curcumin, the extracts of Salvia Miltiorrhiza and Curcuma Longa, on the proliferation and activation of hepatic stellate cell (HSC), and the extracellular signal regulated kinase (ERK) expression in it. Methods: Rat's HSC-T6 were cultured and treated by SAB or curcumin. The inhibitory effect on cell proliferation was determined by 3-(4,5-dimthyl-2-2thiazoly)-2,5-diphenyl-2H-tetrazolium bromide (MTT) colorimetry, and the expression levels of α smooth actin (α-SMA), collagen type Ⅰ , and ERK were determined by Western blot. Results: SAB and curcumin inhibited the proliferation and activation of rat's HSC-T6 in dose-dependent fashion and significantly reduced the expression level of α-SMA ( P<0.01 ). Curcumin significantly reduced the expression of collagen type Ⅰ( P<0.05). Both SAB and curcumin showed insignificant effect on the ERK expression level, but they could significantly reduce the level of phosphorylated-ERK expression, showing significant difference as compared with that in the control group ( P<0.01 and P<0.05 respectively). Conclusion: SAB and curcumin could significantly inhibit the proliferation, activation of HSC, and the production of type Ⅰ collagen in HSC, the mechanism may be associated with their inhibition on ERK phosphorylation.

  8. Antimicrobial Activity, Growth Inhibition of Human Tumour Cell Lines, and Phytochemical Characterization of the Hydromethanolic Extract Obtained from Sapindus saponaria L. Aerial Parts

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    Khaled N. Rashed

    2013-01-01

    Full Text Available The hydromethanolic extract of Sapindus saponaria L. aerial parts was investigated for antimicrobial activity (against several Gram-positive and Gram-negative bacteria and fungi and capacity to inhibit the growth of different human tumor cell lines as also nontumor liver cells. The evaluated extract was further characterized in terms of phytochemicals using UV, 1H-NMR, 13C-NMR, and MS spectroscopic tools. The extract has shown a significant antimicrobial activity on all tested bacterial and fungal species. The best activity was achieved against Bacillus cereus and Staphylococcus aureus among bacteria and against all three Penicillium species tested. It also revealed cytotoxicity against human colon (HCT-15, cervical (HeLa, breast (MCF-7, and lung (NCI-H460 carcinoma cell lines, with HeLa being the most susceptible tumor cell line. The extract was not toxic for nontumor liver cells. Chromatographic separation of the extract resulted in the isolation and identification of stigmasterol, oleanolic acid, luteolin, luteolin 8-C-β-glucoside (orientin, luteolin 6-C-β-glucoside (isoorientin, luteolin 7-O-β-glucuronide, and rutin. The results of the present findings may be useful for the discovery of novel antitumor and antimicrobial agents from plant origin.

  9. Excess Cdt1 inhibits nascent strand elongation by repressing the progression of replication forks in Xenopus egg extracts.

    Science.gov (United States)

    Nakazaki, Yuta; Tsuyama, Takashi; Seki, Masayuki; Takahashi, Mikiko; Enomoto, Takemi; Tada, Shusuke

    2016-02-01

    Cdt1 is a protein essential for initiation of DNA replication; it recruits MCM helicase, a core component of the replicative DNA helicase, onto replication origins. In our previous study, we showed that addition of excess Cdt1 inhibits nascent strand elongation during DNA replication in Xenopus egg extracts. In the present study, we investigated the mechanism behind the inhibitory effect of Cdt1. We found that addition of recombinant Cdt1 inhibited nascent DNA synthesis in a reinitiation-independent manner. To identify the mechanism by which Cdt1 inhibits nascent strand elongation, the effect of Cdt1 on loading of Mcm4 and Rpa70 onto chromatin was examined. The results showed that Cdt1 suppressed the excessive Rpa70 binding caused by extensive, aphidicolin-induced DNA unwinding; this unwinding occurs between stalled DNA polymerases and advancing replication forks. These findings suggested that excess Cdt1 suppressed the progression of replication forks.

  10. Glycyrrhiza glabra L. Extract Inhibits LPS-Induced Inflammation in RAW Macrophages.

    Science.gov (United States)

    Li, Chunmei; Eom, Taekil; Jeong, Yoonhwa

    2015-01-01

    Glycyrrhiza glabra has been used in medicine for thousands of years. Our previous study revealed that the methanolic extract of Glycyrrhiza glabra L. (EGGR) exhibits significant nitric oxide (NO) inhibitory effect on lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages among 100 other extracts. Accordingly, the aim of the present study was to investigate the potential anti-inflammatory effect of EGGR. The anti-inflammatory effect of EGGR on LPS-stimulated RAW 264.7 macrophages was measured by MTT assay, NO content analysis, reactive oxygen species (ROS) level analysis, RT-PCR, Western blot analysis, and ELISA assay. Low doses of EGGR were non-toxic to macrophages and imparted protective effect against LPS induced cell death. Incubation of LPS-treated macrophages with 100 μg/mL EGGR led to an increase in cell viability from 66.6 to 99%. Moreover, EGGR led to down regulation of NO (NO2+NO3) and ROS productions in a dose-dependent manner. In particular, 100 μg/mL EGGR led to a reduction in NO2+NO3 level from 336.2 to 24.1 pM/mL, and ROS level from 483.5 to 128.4%. Consistent with the result related to NO production, EGGR suppressed the ability of LPS to induce mRNA and protein expressions of nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) cytokines, tumor necrosis factor-α (TNF-α), interleukin 1β (IL-1β), and IL-6 productions which were analyzed by an ELISA assay. These results provide a comprehensive approach into the anti-inflammatory effect of EGGR on LPS-stimulated macrophages; however, efforts are underway on gaining detailed insight into anti-inflammatory signaling pathways.

  11. Tinospora crispa extract inhibits MMP-13 and migration of head and neck squamous cell carcinoma cell lines

    Institute of Scientific and Technical Information of China (English)

    Hataipan; Phienwej; Ih-si; Swasdichira; Surattana; Amnuoypol; Prasit; Pavasant; Piyamas; Sumrejkanchanakij

    2015-01-01

    Objective: To investigate the effect of Tinospora crispa(T. crispa) extract on matrix metalloproteinase 13(MMP-13) expression and cell migration. Methods: The cytotoxicity of T. crispa extract was examined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay on head and neck squamous cell carcinoma(HNSCC) cell lines. The effect on expression of MMP-13 was analysed by RT-PCR and ELISA. The migration was assessed by wound healing assay. Results: MMP-13 m RNA was highly expressed in the metastatic human HNSCC cell lines, HN22 and HSC-3. T. crispa extract at a concentration of 100.0 μg/m L caused about 50% reduction of cell survival. T. crispa extract at a non-toxic concentration of 12.5, 25.0 and 50.0 μg/m L signii cantly suppressed MMP-13 m RNA expression and secreted MMP-13 in both HN22 and HSC-3. The expression of tissue inhibitors of metalloprotease by HSC-3 cells was attenuated by 25.0 and 50.0 μg/m L of T. crispa extract. Addition of the extract to cells in a wound healing assay showed inhibition of cell migration by HN22 cells. Conclusions: These data suggest that T. crispa could be considered as a potential therapeutic drug to prevent metastasis of HNSCC.

  12. Saffron (Crocus sativus) ethanolic extract and its constituent, safranal, inhibits morphine-induced place preference in mice.

    Science.gov (United States)

    Ghoshooni, H; Daryaafzoon, M; Sadeghi-Gharjehdagi, S; Zardooz, H; Sahraei, H; Tehrani, S P; Noroozzadeh, A; Bahrami-Shenasfandi, F; Kaka, G H; Sadraei, S H

    2011-10-15

    The effects of saffron ethanolic extract and its constituent, safranal, on the acquisition and expression of morphine-induced place preference (CPP) in male Swiss Webster mice (20-25 g) were investigated in the present study. An unbiased place conditioning method was applied for assessment of morphine reward properties. The saffron extract and safranal were administered intraperitoneally (i.p.) during (acquisition) or after induction (expression) of morphine CPP. In a pilot study, the extract and safranal were alone administered to the animals to assess if they have any reward properties. Subcutaneous (s.c.) of morphine (4 and 8 mg kg(-1)) and extract (50 mg kg(-1); i.p.) induced CPP. Extract (10, 50 and 100 mg kg(-1); i.p.) reduced the acquisition and expression of morphine CPP. The same results were obtained when safranal (1, 5 and 10 mg kg(-1), i.p.) was used. It may be concluded that both ethanolic saffron extract and safranal can inhibit the acquisition and expression of morphine-induced CPP in the mice.

  13. Catechin-based procyanidins from Peumus boldus Mol. aqueous extract inhibit Helicobacter pylori urease and adherence to adenocarcinoma gastric cells.

    Science.gov (United States)

    Pastene, Edgar; Parada, Víctor; Avello, Marcia; Ruiz, Antonieta; García, Apolinaria

    2014-11-01

    In this work, the anti-Helicobacter pylori effect of an aqueous extract from dried leaves of Peumus boldus Mol. (Monimiaceae) was evaluated. This extract displayed high inhibitory activity against H. pylori urease. Therefore, in order to clarify the type of substances responsible for such effect, a bioassay-guided fractionation strategy was carried out. The active compounds in the fractions were characterized through different chromatographic methods (RP-HPLC; HILIC-HPLC). The fraction named F5 (mDP = 7.8) from aqueous extract was the most active against H. pylori urease with an IC50  = 15.9 µg gallic acid equivalents (GAE)/mL. HPLC analysis evidenced that F5 was composed mainly by catechin-derived proanthocyanidins (LC-MS and phloroglucinolysis). The anti-adherent effect of boldo was assessed by co-culture of H. pylori and AGS cells. Both the aqueous extract and F5 showed an anti-adherent effect in a concentration-dependent manner. An 89.3% of inhibition was reached at 2.0 mg GAE/mL of boldo extract. In conjunction, our results suggest that boldo extract has a potent anti-urease activity and anti-adherent effect against H. pylori, properties directly linked with the presence of catechin-derived proanthocyanidins. Copyright © 2014 John Wiley & Sons, Ltd.

  14. Flax Fiber Hydrophobic Extract Inhibits Human Skin Cells Inflammation and Causes Remodeling of Extracellular Matrix and Wound Closure Activation

    Directory of Open Access Journals (Sweden)

    Monika Styrczewska

    2015-01-01

    Full Text Available Inflammation is the basis of many diseases, with chronic wounds amongst them, limiting cell proliferation and tissue regeneration. Our previous preclinical study of flax fiber applied as a wound dressing and analysis of its components impact on the fibroblast transcriptome suggested flax fiber hydrophobic extract use as an anti-inflammatory and wound healing preparation. The extract contains cannabidiol (CBD, phytosterols, and unsaturated fatty acids, showing great promise in wound healing. In in vitro proliferation and wound closure tests the extract activated cell migration and proliferation. The activity of matrix metalloproteinases in skin cells was increased, suggesting activation of extracellular components remodeling. The expression of cytokines was diminished by the extract in a cannabidiol-dependent manner, but β-sitosterol can act synergistically with CBD in inflammation inhibition. Extracellular matrix related genes were also analyzed, considering their importance in further stages of wound healing. The extract activated skin cell matrix remodeling, but the changes were only partially cannabidiol- and β-sitosterol-dependent. The possible role of fatty acids also present in the extract is suggested. The study shows the hydrophobic flax fiber components as wound healing activators, with anti-inflammatory cannabidiol acting in synergy with sterols, and migration and proliferation promoting agents, some of which still require experimental identification.

  15. Inhibition of chemiluminescence and chemotactic activity of phagocytes in vitro by the extracts of selected medicinal plants.

    Science.gov (United States)

    Jantan, Ibrahim; Harun, Nurul Hikmah; Septama, Abdi Wira; Murad, Shahnaz; Mesaik, M A

    2011-04-01

    The methanol extracts of 20 selected medicinal plants were investigated for their effects on the respiratory burst of human whole blood, isolated human polymorphonuclear leukocytes (PMNs) and isolated mice macrophages using a luminol/lucigenin-based chemiluminescence assay. We also tested the effect of the extracts on chemotactic migration of PMNs using the Boyden chamber technique. The extracts of Curcuma domestica L., Phyllanthus amarus Schum & Thonn and C. xanthorrhiza Roxb. were the samples producing the strongest oxidative burst of PMNs with luminol-based chemiluminescence, with IC(50) values ranging from 0.5 to 0.7 μg/ml. For macrophage cells, the extracts which showed strong suppressive activity for luminol-based chemiluminescence were C. xanthorrhiza and Garcinia mangostana L. Among the extracts studied, C. mangga Valton & Vazsjip, Piper nigrum L. and Labisia pumila var. alata showed strong inhibitory activity on lucigenin-amplified oxidative burst of PMNs, with IC(50) values ranging from 0.9 to 1.5 μg/ml. The extracts of Zingiber officinale Rosc., Alpinia galangal (L.) Willd and Averrhoa bilimbi Linn showed strong inhibition on the chemotaxic migration of cells, with IC(50) values comparable to that of ibuprofen (1.5 μg/ml). The results suggest that some of these plants were able to modulate the innate immune response of phagocytes at different steps, emphasizing their potential as a source of new immunomodulatory agents.

  16. Flax Fiber Hydrophobic Extract Inhibits Human Skin Cells Inflammation and Causes Remodeling of Extracellular Matrix and Wound Closure Activation.

    Science.gov (United States)

    Styrczewska, Monika; Kostyn, Anna; Kulma, Anna; Majkowska-Skrobek, Grazyna; Augustyniak, Daria; Prescha, Anna; Czuj, Tadeusz; Szopa, Jan

    2015-01-01

    Inflammation is the basis of many diseases, with chronic wounds amongst them, limiting cell proliferation and tissue regeneration. Our previous preclinical study of flax fiber applied as a wound dressing and analysis of its components impact on the fibroblast transcriptome suggested flax fiber hydrophobic extract use as an anti-inflammatory and wound healing preparation. The extract contains cannabidiol (CBD), phytosterols, and unsaturated fatty acids, showing great promise in wound healing. In in vitro proliferation and wound closure tests the extract activated cell migration and proliferation. The activity of matrix metalloproteinases in skin cells was increased, suggesting activation of extracellular components remodeling. The expression of cytokines was diminished by the extract in a cannabidiol-dependent manner, but β-sitosterol can act synergistically with CBD in inflammation inhibition. Extracellular matrix related genes were also analyzed, considering their importance in further stages of wound healing. The extract activated skin cell matrix remodeling, but the changes were only partially cannabidiol- and β-sitosterol-dependent. The possible role of fatty acids also present in the extract is suggested. The study shows the hydrophobic flax fiber components as wound healing activators, with anti-inflammatory cannabidiol acting in synergy with sterols, and migration and proliferation promoting agents, some of which still require experimental identification.

  17. A Novel Approach to Extract Significant Patterns of Travel Time Intervals of Vehicles from Freeway Gantry Timestamp Sequences

    Directory of Open Access Journals (Sweden)

    Jing-Doo Wang

    2017-08-01

    Full Text Available It is attractive to extract and determine the key features of traffic patterns for mitigating road congestion and predicting travel time of vehicles in traffic analysis. Based on the previous work that is a scalable approach via a Hadoop MapReduce programming model, this paper aims to extract significant patterns of travel time intervals of vehicles from freeway traffic in Taiwan, and meanwhile to compute the statistics of these patterns from the point of view one may concern. Experimental resources are the records of timestamp gantry sequences of vehicles passed in five months from 2016/11 to 2017/3 that were downloaded from the Traffic Data Collection System, one of Taiwan government open data platforms. To select one specific gantry sequence for demonstration, the longest sequence on the trip within the Taiwan National Freeway No. 5 is selected. Experimental results show that some statistics of vehicle travel time intervals according to 24 h per day are computed for illustration. These statistics can not only provide clues to experts to analyze traffic congestions, but also help drivers how to avoid rush hours. Furthermore, this work is able to handle a larger amount of real data and be promising for further traffic and transportation research in the future.

  18. Induction of apoptosis and inhibition of proliferation in human tumor cells treated with extracts of Uncaria tomentosa.

    Science.gov (United States)

    Sheng, Y; Pero, R W; Amiri, A; Bryngelsson, C

    1998-01-01

    Growth inhibitory activities of novel water extracts of Uncaria tomentosa (C-Med-100) were examined in vitro using two human leukemic cell lines (K562 and HL60) and one human EBV-transformed B lymphoma cell line (Raji). The proliferative capacities of HL60 and Raji cells were strongly suppressed in the presence of the C-Med-100 while K562 was more resistant to the inhibition. Furthermore, the antiproliferative effect was confirmed using the clonogenic assay, which showed a very close correlation between C-Med-100 concentration and the surviving fraction. The suppressive effect of Uncaria tomentosa extracts on tumor cell growth appears to be mediated through induction of apoptosis which was demonstrated by characteristic morphological changes, internucleosomal DNA fragmentation after agarose gel electrophoresis and DNA fragmentation quantification. C-Med-100 induced a delayed type of apoptosis becoming most dose-dependently prominent after 48 hours of exposure. Both DNA single and double strand breaks were increased 24 hours after C-Med-100 treatment, which suggested a well-established linkage between the DNA damage and apoptosis. The induction of DNA strand breaks coupled to apoptosis may explain the growth inhibition of the tumor cells by Uncaria tomentosa extracts. These results provide the first direct evidence for the antitumor properties of Uncaria tomentosa extracts to be via a mechanism of selective induction of apoptosis.

  19. Inhibitive Effect by Acid Extract of Ficus Exasperata Leaves on the Sulphuric Acid Corrosion of Mild Steel

    Directory of Open Access Journals (Sweden)

    N. S. Patel

    2009-01-01

    Full Text Available Extract of Ficus exasperata leaves was investigated as corrosion inhibitor of mild steel in 1 N H2SO4 using conventional weight loss, electrochemical polarizations, electrochemical impedance spectroscopy and scanning electron microscopic studies. The weight loss results showed that the extract of Ficus exasperata is excellent corrosion inhibitor. Electrochemical polarizations data revealed the mixed mode of inhibition. The results of electrochemical impedance spectroscopy shows that the change in the impedance parameters, charge transfer resistance and double layer capacitance, with the change in concentration of the extract is due to the adsorption of active molecules leading to the formation of a protective layer on the surface of mild steel. Scanning electron microscopic studies provided the confirmatory evidence of improved surface condition, due to the adsorption, for the corrosion protection.

  20. Storage Effect on Phenols and on the Antioxidant Activity of Extracts from Anemopsis californica and Inhibition of Elastase Enzyme

    Directory of Open Access Journals (Sweden)

    Carmen Lizette Del-Toro-Sánchez

    2015-01-01

    Full Text Available The amount of total phenols and flavonoids and the antioxidant activity of leaf, stem, and rhizome methanolic extracts from a commonly consumed Anemopsis californica under different storage conditions were investigated. Storage conditions were at 50, 25, 4, and −20°C, protected or not from light, during 180 days. The inhibition of the elastase enzyme was also evaluated. The results demonstrated that leaf, stem, and rhizome methanolic extracts of Anemopsis californica maintain approximately up to 97 and 95% stability in phenolic content and antioxidant activity, respectively, when stored during 60 days at −20°C in the dark. Additionally, these extracts, principally from leaf and rhizome, showed an elastase inhibitory effect by 75 and 71.8%, respectively. Therefore, this study provides the basis for further research on the anti-inflammatory activity. On the other hand, Anemopsis californica could comprise a good alternative of use as antioxidant in foods.

  1. Ginkgo biloba extracts attenuate lipopolysaccharide-induced inflammatory responses in acute lung injury by inhibiting the COX-2 and NF-κB pathways.

    Science.gov (United States)

    Yao, Xin; Chen, Nan; Ma, Chun-Hua; Tao, Jing; Bao, Jian-An; Zong-Qi, Cheng; Chen, Zu-Tao; Miao, Li-Yan

    2015-01-01

    In the present study, we analyzed the role of Ginkgo biloba extract in lipopolysaccharide(LPS)-induced acute lung injury (ALI). ALI was induced in mice by intratracheal instillation of LPS. G. biloba extract (12 and 24 mg·kg(-1)) and dexamethasone (2 mg·kg(-1)), as a positive control, were given by i.p. injection. The cells in the bronchoalveolar lavage fluid (BALF) were counted. The degree of animal lung edema was evaluated by measuring the wet/dry weight ratio. The superoxidase dismutase (SOD) and myeloperoxidase (MPO) activities were assayed by SOD and MPO kits, respectively. The levels of inflammatory mediators, tumor necrosis factor-a, interleukin-1b, and interleukin-6, were assayed by enzyme-linked immunosorbent assay. Pathological changes of lung tissues were observed by H&E staining. The levels of NF-κB p65 and COX-2 expression were detected by Western blotting. Compared to the LPS group, the treatment with the G. biloba extract at 12 and 24 mg·kg(-1) markedly attenuated the inflammatory cell numbers in the BALF, decreased NF-κB p65 and COX-2 expression, and improved SOD activity, and inhibited MPO activity. The histological changes of the lungs were also significantly improved. The results indicated that G. biloba extract has a protective effect on LPS-induced acute lung injury in mice. The protective mechanism of G. biloba extract may be partly attributed to the inhibition of NF-κB p65 and COX-2 activation.

  2. Antimicrobial effect by extracts of rhizome of Alpinia officinarum Hance may relate to its inhibition of beta-ketoacyl-ACP reductase.

    Science.gov (United States)

    Huang, Hui; Wu, Dan; Tian, Wei-Xi; Ma, Xiao-Feng; Wu, Xiao-Dong

    2008-06-01

    Inhibitory effects on bacterial growth showed that 40% ethanol extract of galangal (rhizome of Alpinia officinarum Hance) can inhibit Staphylococcus aureus, alpha-Hemolytic streptococcus, beta-Hemolytic streptococcus and Streptococcus pneumoniae. beta-ketoacyl-ACP reductase (FabG, EC.1.1.1.100) is a key enzyme in type II fatty acid synthase system in bacteria and catalyzes beta-ketoacyl-ACP reduction. The galangal extracts inhibited FabG with an IC(50) value of only 4.47 +/- 0.10 microg/mL and is more potent than other previously published inhibitors. Kinetics studies showed that the inhibition consisted of both reversible and irreversible inhibition. The extracts of galangal inhibit FabG in a competitive pattern against NADPH. So far, no inhibitor has been reported to exhibit irreversible inhibition of FabG, whereas the galangal ethanol extract can inhibit FabG irreversibly. The irreversible inhibition presented two phases. It is probable that the galangal extract inhibit FabG, thereby displaying antibacterial ability.

  3. In vitro inhibition activity of polyphenol-rich extracts from Syzygium aromaticum (L.) Merr. & Perry (Clove) buds against carbohydrate hydrolyzing enzymes linked to type 2 diabetes and Fe2+-induced lipid peroxidation in rat pancreas

    Institute of Scientific and Technical Information of China (English)

    Stephen Adeniyi Adefegha; Ganiyu Oboh

    2012-01-01

    To investigate and compare the inhibitory properties of free and bound phenolic extracts of clove bud against carbohydrate hydrolyzing enzymes (alpha-amylase & alpha-glucosidase) and Fe2+-induced lipid peroxidation in rat pancreas in vitro. Methods: The free phenolics were extracted with 80% (v/v) acetone, while bound phenolics were extracted from the alkaline and acid hydrolyzed residue with ethyl acetate. Then, the interaction of the extracts with alpha-amylase and alpha-glucosidase was subsequently assessed. Thereafter, the total phenolic contents and antioxidant activities of the extracts were determined. Results: The result revealed that both extracts inhibited alpha-amylase and alpha-glucosidase in a dose-dependent manner. However, the alpha-glucosidase inhibitory activity of the extracts were significantly (P<0.05) higher than their alpha-amylase inhibitory activity. The free phenolics (31.67 mg/g) and flavonoid (17.28 mg/g) contents were significantly (P<0.05) higher than bound phenolic (23.52 mg/g) and flavonoid (13.70 mg/g) contents. Both extracts also exhibited high antioxidant activities as typified by their high reducing power, 1,1 diphenyl-2- picrylhydrazyl (DPPH) and 2, 2-azinobis-3-ethylbenzo-thiazoline-6-sulfonate (ABTS) radical scavenging abilities, as well as inhibition of Fe2+-induced lipid peroxidation in rat pancreas in vitro. Conclusions: This study provides a biochemical rationale by which clove elicits therapeutic effect on type 2 diabetes.

  4. Inhibition of cyclooxygenase activity by standardized hydroalcoholic extracts of four Asteraceae species from the Argentine Puna

    OpenAIRE

    Alberto,M.R.; Zampini,I.C.; Isla, M. I.

    2009-01-01

    We determined the anti-inflammatory activity of standardized extracts of four medicinal plant species (Baccharis incarum, B. boliviensis, Chuquiraga atacamensis, Parastrephia lucida) that grow in the Argentine Puna (3800 m above sea level) and that are used to reduce oxidative stress and alleviate gout and arthritic pain. The extracts of plant aerial parts were standardized in terms of total phenolic compounds and flavone/flavanone content and free radical scavenging activity. All extracts sh...

  5. Inhibition of lung cancer cells A549 and H460 by curcuminoid extracts and nanoemulsions prepared from Curcuma longa Linnaeus

    Science.gov (United States)

    Chang, Hong-Bin; Chen, Bing-Huei

    2015-01-01

    The objectives of this study were to explore the inhibition mechanism of lung cancer cells A549 and H460 by curcuminoid extracts and nanoemulsions prepared from Curcuma longa Linnaeus. In addition, human bronchus epithelial cell line BEAS-2B (normal cell) was selected for comparison. A high-performance liquid chromatography (HPLC) method was developed to separate and quantify the various curcuminoids in C. longa extract, including curcumin (1,714.5 μg/mL), demethoxycurcumin (1,147.4 μg/mL), and bisdemethoxycurcumin (190.2 μg/mL). A high-stability nanoemulsion composed of Tween 80, water, and curcuminoid extract was prepared, with mean particle size being 12.6 nm. The cell cycle was retarded at G2/M for both the curcuminoid extract and nanoemulsion treatments; however, the inhibition pathway may be different. H460 cells were more susceptible to apoptosis than A549 cells for both curcuminoid extract and nanoemulsion treatments. Growth of BEAS-2B remained unaffected for both the curcuminoid extract and nanoemulsion treatments, with a concentration range from 1 to 4 μg/mL. Also, the activities of caspase-3, caspase-8, and caspase-9 followed a dose-dependent increase for both A549 and H460 cells for both the treatments, accompanied by a dose-dependent increase in cytochrome C expression and a dose-dependent decrease in CDK1 expression. Interestingly, a dose-dependent increase in cyclin B expression was shown for A549 cells for both the treatments, while a reversed trend was found for H460 cells. Both mitochondria and death receptor pathways may be responsible for apoptosis of both A549 and H460 cells. PMID:26345201

  6. Inhibition of lung cancer cells A549 and H460 by curcuminoid extracts and nanoemulsions prepared from Curcuma longa Linnaeus.

    Science.gov (United States)

    Chang, Hong-Bin; Chen, Bing-Huei

    2015-01-01

    The objectives of this study were to explore the inhibition mechanism of lung cancer cells A549 and H460 by curcuminoid extracts and nanoemulsions prepared from Curcuma longa Linnaeus. In addition, human bronchus epithelial cell line BEAS-2B (normal cell) was selected for comparison. A high-performance liquid chromatography (HPLC) method was developed to separate and quantify the various curcuminoids in C. longa extract, including curcumin (1,714.5 μg/mL), demethoxycurcumin (1,147.4 μg/mL), and bisdemethoxycurcumin (190.2 μg/mL). A high-stability nanoemulsion composed of Tween 80, water, and curcuminoid extract was prepared, with mean particle size being 12.6 nm. The cell cycle was retarded at G2/M for both the curcuminoid extract and nanoemulsion treatments; however, the inhibition pathway may be different. H460 cells were more susceptible to apoptosis than A549 cells for both curcuminoid extract and nanoemulsion treatments. Growth of BEAS-2B remained unaffected for both the curcuminoid extract and nanoemulsion treatments, with a concentration range from 1 to 4 μg/mL. Also, the activities of caspase-3, caspase-8, and caspase-9 followed a dose-dependent increase for both A549 and H460 cells for both the treatments, accompanied by a dose-dependent increase in cytochrome C expression and a dose-dependent decrease in CDK1 expression. Interestingly, a dose-dependent increase in cyclin B expression was shown for A549 cells for both the treatments, while a reversed trend was found for H460 cells. Both mitochondria and death receptor pathways may be responsible for apoptosis of both A549 and H460 cells.

  7. Inhibition of secretary PLA₂--VRV-PL-VIIIa of Russell's viper venom by standard aqueous stem bark extract of Mangifera indica L.

    Science.gov (United States)

    Dhananjaya, B L; Sudarshan, S

    2015-03-01

    The aqueous extract of Mangifera indica is known to possess anti-snake venom activities. However, its inhibitory potency and mechanism of action on multi-toxic phospholipases A2s, which are the most toxic and lethal component of snake venom is still unknown. Therefore, this study was carried out to evaluate the modulatory effect of standard aqueous bark extract of M. indica on VRV-PL-VIIIa of Indian Russells viper venom. Mangifera indica extract dose dependently inhibited the GIIB sPLA2 (VRV-PL-VIIIa) activity with an IC50 value of 6.8±0.3 μg/ml. M. indica extract effectively inhibited the indirect hemolytic activity up to 96% at ~40 μg/ml concentration. Further, M. indica extract at different concentrations (0-50 μg/ml) inhibited the edema formed in a dose dependent manner. It was found that there was no relieve of inhibitory effect of the extract when examined as a function of increased substrate and calcium concentration. The inhibition was irreversible as evident from binding studies. The in vitro inhibition is well correlated with in situ and in vivo edema inducing activities. As the inhibition is independent of substrate, calcium concentration and was irreversible, it can be concluded that M. indica extracts mode of inhibition could be due to direct interaction of components present in the extract with PLA2 enzyme. In conclusion, the aqueous extract of M. indica effectively inhibits svPLA2 (Snake venom phospholipase A2) enzymatic and its associated toxic activities, which substantiate its anti-snake venom properties. Further in-depth studies are interesting to known on the role and mechanism of the principal inhibitory constituents present in the extract, so as to develop them into potent anti-snake venom and as an anti-inflammatory agent.

  8. The potential of aqueous extracts of Bellucia dichotoma Cogn. (Melastomataceae) to inhibit the biological activities of Bothrops atrox venom: A comparison of specimens collected in the states of Pará and Amazonas, Brazil.

    Science.gov (United States)

    de Moura, Valéria Mourão; de Souza, Luana Yamille Andrade; da Costa Guimarães, Noranathan; Dos Santos, Ilia Gilmara Carvalho; de Almeida, Patrícia Danielle Oliveira; de Oliveira, Ricardo Bezerra; Mourão, Rosa Helena Veras; Dos-Santos, Maria Cristina

    2017-01-20

    The effectiveness of aqueous extract of Bellucia dichotoma Cogn. (Melastomataceae) specimems collected in Santarém, PA, against some biological activities of Bothrops atrox venom (BaV) has been scientifically proven. Here, we analyzed the components and assessed the anti-snakebite potential of aqueous extracts of bark of B. dichotoma collected in Manaus, AM, (AEBd-MAO) and Santarém, PA, (AEBd-STM), both in Brazil. The phytochemical profiles of the aqueous extracts were identified using thin layer chromatography (TLC), and the concentrations of phenolics were determined by colorimetric assay. The inhibitory potential of the extracts was tested against the phospholipase A2, coagulant and gelatinolytic activities of BaV in vitro and its defibrinating and edema-inducing activities in vivo. Interaction between BaV and the extracts was investigated using SDS-Page electrophoresis and Western blotting. Extract cytotoxicity and antioxidant potential were assessed using the human fibroblast cell line MRC-5 and the DPPH assay in cell culture, respectively. While there was no difference between the phytochemical profiles of the extracts, AEBd-MAO had higher concentrations of total phenolics, total tannins and hydrolysable tannins. The extracts inhibited 100% of the phospholipase and coagulant activity of BaV when pre-incubated. Without pre-incubation, however, there was no reduction in phospholipase activity, although significant inhibition of coagulant activity was observed. In the doses used in folk medicine, without pre-incubation, both extracts inhibited 100% of the coagulant activity of BaV. In vivo, the extracts were unable to inhibit the defibrinating activity of the venom but were effective in inhibiting its edema-inducing activity. In the profiles of the extracts pre-incubated with BaV, not all the protein bands revealed by SDS-PAGE and Western blot were observed. Both extracts had a high antioxidant potential and neither had a cytotoxic effect. Although the

  9. A Fucus vesiculosus extract inhibits estrogen receptor activation and induces cell death in female cancer cell lines.

    Science.gov (United States)

    Zhang, Jianqing; Riby, Jacques E; Conde, Lucia; Grizzle, William E; Cui, Xiangqin; Skibola, Christine F

    2016-05-28

    We previously reported the anti-estrogenic activity of the brown seaweed, Fucus vesiculosus. The present study aimed to further investigate its anti-estrogenic modes of action and to assess other potentially biologically relevant anti-tumorigenic effects in estrogen receptor (ER)-dependent and -independent female cancer cell lines. The CALUX® assay was used to determine the effect of a F. vesiculosus extract (FVE) on activation of the ER. Aromatase enzymatic activity was measured to determine the potential effect of FVE on estradiol (E2) biosynthesis. Transcriptional activity profiling of 248 genes involved in cancer, immunity, hormonal regulation, protein phosphorylation, transcription, metabolism, and cellular structure was conducted using the NanoString nCounter® analysis system in FVE-treated breast, ovarian and endometrial cancer cell lines. The effects of FVE on cell viability, morphology, membrane integrity, mitochondrial toxicity, induction of apoptotic and autophagic markers, and cell signaling were also analyzed. In co-treatments with 12.5 pM (EC50) E2, FVE (2 %) reduced ER activation by 50 %, exhibiting potent ER antagonistic effects. FVE inhibited aromatase activity in an in vitro assay (IC50 2.0 %). ER-dependent and -independent cancer cell lines showed significantly decreased viability that correlated with increasing FVE concentrations and altered morphological features suggestive of apoptosis and autophagy. Expression of genes that were significantly altered by FVE (p vesiculosus. Moreover, the induction of autophagy and apoptosis on breast, endometrial and ovarian cancer cell lines suggests additional anti-tumorigenic actions of FVE that are independent of ER status in female cancers.

  10. Polyyne-Enriched Extract from Oplopanax elatus Significantly Ameliorates the Progression of Colon Carcinogenesis in ApcMin/+ Mice

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    Xin Qiao

    2017-09-01

    Full Text Available Colorectal cancer (CRC is the third most common cancer in the world. Oplopanax elatus is widely used in traditional medicine. However, little is known about its pharmacological effects and bioactive compounds. We evaluated the effects of the polyyne-enriched extract from O. elatus (PEO on the progression of colon carcinogenesis in ApcMin/+ mice. In addition, these effects were also investigated in HCT116 and SW480 cells. After PEO oral administration (0.2% diet for 12 weeks, PEO significantly improved body weight changes and reduced the tumor burden and tumor multiplicity compared with the untreated mice. Meanwhile, western blot and immunohistochemistry results showed PEO significantly reduced the expression of β-catenin and cyclinD1 in both small intestine and the colon tissues compared with the untreated mice. In addition, PEO treatment significant decreased the cell viability in both HCT116 and SW480 cell lines. It also decreased the levels of β-catenin, cyclinD1, c-myc and p-GSK-3β in HCT116 and SW480 cells at 25 μM. These results indicate that PEO may have potential value in prevention of colon cancer by down-regulating Wnt-related protein.

  11. Inhibition of Human Cytochrome P450 Enzymes by Allergen Removed Rhus verniciflua Stoke Standardized Extract and Constituents

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    Hyunsik Jung

    2014-01-01

    Full Text Available Objective. Potential interactions between herbal extracts and the cytochrome P450 (CYP system lead to serious adverse events or decreased drug efficacy. Rhus verniciflua stoke (RVS and its constituents have been reported to have various pharmacological properties. We evaluated the inhibitory potential of RVS and its constituents on the major CYP isoforms. Methods. The effects of allergen removed RVS (aRVS standardized extract and major components, fustin and fisetin isolated from aRVS, were evaluated on CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 isoenzyme activity by a luminescent CYP recombinant human enzyme assay. Results. The aRVS extract showed relative potent inhibitory effects on the CYP2C9 (IC50, <0.001 μg/mL, CYP2C19 (IC50, 9.68 μg/mL, and CYP1A2 (IC50, 10.0 μg/mL. However, it showed weak inhibition on CYP3A4 and CYP2D6. Fustin showed moderate inhibitory effects on the CYP2C19 (IC50, 64.3 μg/mL and weak inhibition of the other CYP isoforms similar to aRVS. Fisetin showed potent inhibitory effects on CYP2C9, CYP2C19, and CYP1A2. Fisetin showed moderate inhibition of CYP2D6 and weak inhibition of CYP3A4. Conclusions. These results indicate that aRVS, a clinically available herbal medicine, could contribute to herb-drug interactions when orally coadministered with drugs metabolized by CYP2C9, CYP2C19, and CYP1A2.

  12. Evaluation of four different systems for extraction of RNA from stool suspensions using MS-2 coliphage as an exogenous control for RT-PCR inhibition.

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    Lester M Shulman

    Full Text Available Knowing when, and to what extent co-extracted inhibitors interfere with molecular RNA diagnostic assays is of utmost importance. The QIAamp Viral RNA Mini Kit (A; MagNA Pure LC2.0 Automatic extractor (B; KingFisher (C; and NucliSENS EasyMag (D RNA extraction systems were evaluated for extraction efficiency and co-purification of inhibitors from stool suspensions. Real-Time Reverse Transcriptase Polymerase Chain Reaction (rRT-PCR of MS-2 coliphage spiked into each system's lysis buffer served as an external control for both. Cycle thresholds (Cts of the MS2 were determined for RNA extracted from stool suspensions containing unknown (n = 93 or varying amounts of inhibitors (n = 92. Stool suspensions from the latter group were also used to determine whether MS-2 and enterovirus rRT-PCR inhibitions were correlated. Specifically 23 RNA extracts from stool suspensions were spiked with enterovirus RNA after extraction and 13 of these stool suspension were spiked with intact enterovirus before extraction. MS2 rRT-PCR inhibition varied for RNAs extracted by the different systems. Inhibition was noted in 12 (13.0%, 26 (28.3%, 7 (7.6%, and 7 (7.6% of the first 93 RNA extracts, and 58 (63.0%, 55 (59.8%, 37 (40.2% and 30 (32.6% of the second 92 extracts for A, B, C, and D, respectively. Furthermore, enterovirus rRT-PCR inhibition correlated with MS2 rRT-PCR inhibition for added enterovirus RNA or virus particles. In conclusion, rRT-PCR for MS-2 RNA is a good predictor of inhibition of enterovirus RNA extracted from stool suspensions. EasyMag performed the best, however all four extraction methods were suitable provided that external controls identified problematic samples.

  13. Diesel exhaust particulate extracts inhibit transcription of nuclear respiratory factor-1 and cell viability in human umbilical vein endothelial cells

    Energy Technology Data Exchange (ETDEWEB)

    Mattingly, Kathleen A.; Klinge, Carolyn M. [University of Louisville School of Medicine, Department of Biochemistry and Molecular Biology, Center for Genetics and Molecular Medicine, Louisville, KY (United States)

    2012-04-15

    Endothelial dysfunction precedes cardiovascular disease and is accompanied by mitochondrial dysfunction. Here we tested the hypothesis that diesel exhaust particulate extracts (DEPEs), prepared from a truck run at different speeds and engine loads, would inhibit genomic estrogen receptor activation of nuclear respiratory factor-1 (NRF-1) transcription in human umbilical vein endothelial cells (HUVECs). Additionally, we examined how DEPEs affect NRF-1-regulated TFAM expression and, in turn, Tfam-regulated mtDNA-encoded cytochrome c oxidase subunit I (COI, MTCO1) and NADH dehydrogenase subunit I (NDI) expression as well as cell proliferation and viability. We report that 17{beta}-estradiol (E{sub 2}), 4-hydroxytamoxifen (4-OHT), and raloxifene increased NRF-1 transcription in HUVECs in an ER-dependent manner. DEPEs inhibited NRF-1 transcription, and this suppression was not ablated by concomitant treatment with E{sub 2}, 4-OHT, or raloxifene, indicating that the effect was not due to inhibition of ER activity. While E{sub 2} increased HUVEC proliferation and viability, DEPEs inhibited viability but not proliferation. Resveratrol increased NRF-1 transcription in an ER-dependent manner in HUVECs, and ablated DEPE inhibition of basal NRF-1 expression. Given that NRF-1 is a key nuclear transcription factor regulating genes involved in mitochondrial activity and biogenesis, these data suggest that DEPEs may adversely affect mitochondrial function leading to endothelial dysfunction and resveratrol may block these effects. (orig.)

  14. Inhibition of the emergence of multi drug resistant Staphylococcus aureus by Withania somnifera root extracts

    Institute of Scientific and Technical Information of China (English)

    Shuvo Datta; Nishith Kumar Pal; Ashoke Kumar Nandy

    2011-01-01

    Objective:To search systematically for an alternative therapy with compounds particularly from plant origin.Methods: Efficacy test of different root extracts ofWithania somnifera (W. somnifera) (L) Dunalagainst multi drug resistant(MDR)Staphylococcus aureus(S. aureus)variants was performed following the agar well diffusion method. Evaluation of susceptibility pattern of the isolates was carried out by employing disk diffusion method using standard antibiotic disks. Results:In vitro study withW. somniferaroot extracts was found to be effective against all the MDRS. aureusstrains isolated from local and patient sources. Different root extracts of WS showed different degree of effectiveness against the isolates.Conclusions: The major active principles responsible for the antibacterial efficacy were mainly present in methanol(MeOH) extract and ethanol (EtOH)extracts as well as in butanol (BuOH) extract fraction. Amongst all the extracts the BuOH fraction was found to be most active against all the isolates but aqueous extract was the least active one. Finally it may be concluded that the antimicrobials fromW. somnifera may raise an alternative therapy forMDR staphylococcal infections in near future.

  15. Inhibition effects on fermentation of hardwood extracted hemicelluloses by acetic acid and sodium.

    Science.gov (United States)

    Walton, Sara; van Heiningen, Adriaan; van Walsum, Peter

    2010-03-01

    Extraction of hemicellulose from hardwood chips prior to pulping is a possible method for producing ethanol and acetic acid in an integrated forest bio-refinery, adding value to wood components normally relegated to boiler fuel. Hemicellulose was extracted from hardwood chips using green liquor, a pulping liquor intermediate consisting of aqueous NaOH, Na(2)CO(3), and Na(2)S, at 160 degrees C, held for 110 min in a 20 L rocking digester. The extracted liquor contained 3.7% solids and had a pH of 5.6. The organic content of the extracts was mainly xylo-oligosaccharides and acetic acid. Because it was dilute, the hemicellulose extract was concentrated by evaporation in a thin film evaporator. Concentrates from the evaporator reached levels of up to 10% solids. Inhibitors such as acetic acid and sodium were also concentrated by this method, presenting a challenge for the fermentation organisms. Fermentation experiments were conducted with Escherichia coli K011. The un-concentrated extract supported approximately 70% conversion of the initial sugars in 14 h. An extract evaporated down to 6% solids was also fermentable while a 10% solids extract was not initially fermentable. Strain conditioning was later found to enable fermentation at this level of concentration. Alternative processing schemes or inhibitor removal prior to fermentation are necessary to produce ethanol economically.

  16. Use of raw Euphorbia tirucalli extract for inhibition of ascitic Ehrlich tumor.

    Science.gov (United States)

    Santos, Orlando José Dos; Sauaia Filho, Euler Nicolau; Nascimento, Flávia Raquel Fernandes do; Júnior, Francisco Cardoso Silva; Fialho, Eder Magalhães Silva; Santos, Rayan Haquim Pinheiro; Santos, Rennan Abud Pinheiro; Serra, Izabel Cristina Portela Bogéa

    2016-02-01

    to evaluate the effect of the Euphorbia tirucalli hydroalcoholic extract (ETHE) on the development of Ehrlich Tumor, in its ascitic form. we intraperitoneally inoculated 15 Swiss mice with 10.44 x 107 cells of Ehrlich Tumor and divided them in two groups one day after: ETHE Group (eight mice), treated with a dosage of 125 mg/kg/day of EHTE for five days; and Control Group (seven mice), treated only with 0.9% isotonic saline solution over the same period. The treatment was done by gavage. Ten days after inoculation, four mice from each group were sacrificed for quantification of tumor cell number, ascitic fluid volume and bone marrow cell number. The remaining animals were maintained to evaluate survival. The ascitic fluid volume and the tumor cell number were decreased in the ETHE group when compared with the control group, but with no statistical significance. On the other hand, survival was higher in the ETHE group, as well as the number of bone marrow cells. Treatment with ETHE after inoculation of Ehrlich Tumor decreases its development and increases survival and the bone marrow cellularity, thus reducing the myelosuppression present in the Ehrlich Tumor bearing mice.

  17. Methanolic extract of Cuminum cyminum inhibits ovariectomy-induced bone loss in rats.

    Science.gov (United States)

    Shirke, Sarika S; Jadhav, Sanket R; Jagtap, Aarti G

    2008-11-01

    Several animal and clinical studies have shown that phytoestrogens, plant-derived estrogenic compounds, can be useful in treating postmenopausal osteoporosis. Phytoestrogens and phytoestrogen-containing plants are currently under active investigation for their role in estrogen-related disorders. The present study deals with anti-osteoporotic evaluation of phytoestrogen-rich plant Cuminum cyminum, commonly known as cumin. Adult Sprague-Dawley rats were bilaterally ovariectomized (OVX) and randomly assigned to 3 groups (10 rats/group). Additional 10 animals were sham operated. OVX and sham control groups were orally administered with vehicle while the other two OVX groups were administered 0.15 mg/kg estradiol and 1 g/kg of methanolic extract of Cuminum cyminum fruits (MCC) in two divided doses for 10 weeks. At the end of the study blood, bones and uteri of the animals were collected. Serum was evaluated for calcium, phosphorus, alkaline phosphatase and tartarate resistant acid phosphatase. Bone density, ash density, mineral content and mechanical strength of bones were evaluated. Scanning electron microscopic (SEM) analysis of bones (tibia) was performed. Results were analyzed using ANOVA and Tukeys multiple comparison test. MCC (1 g/kg, p.o.) significantly reduced urinary calcium excretion and significantly increased calcium content and mechanical strength of bones in comparison to OVX control. It showed greater bone and ash densities and improved microarchitecture of bones in SEM analysis. Unlike estradiol it did not affect body weight gain and weight of atrophic uterus in OVX animals. MCC prevented ovariectomy-induced bone loss in rats with no anabolic effect on atrophic uterus. The osteoprotective effect was comparable with estradiol.

  18. Extract from Periostracum cicadae Inhibits Oxidative Stress and Inflammation Induced by Ultraviolet B Irradiation on HaCaT Keratinocytes

    Directory of Open Access Journals (Sweden)

    Tsong-Min Chang

    2017-01-01

    Full Text Available Periostracum cicadae is widely used for the treatment of skin diseases such as eczema, pruritus, and itching. The current study sought to evaluate the effect of P. cicadae extract on ultraviolet B (UVB irradiation and identify the mechanisms involved. Photodamage-protective activity of P. cicadae extracts against oxidative challenge was screened using HaCaT keratinocytes. P. cicadae extracts did not affect cell viability but decreased reactive oxygen species (ROS production. The extract attenuates the expression of interleukin-6 (IL-6, matrix metalloproteinase-2 (MMP-2, and MMP-9 in UVB-treated HaCaT cells. Also, P. cicadae abrogated UVB-induced activation of NF-κB, p53, and activator protein-1 (AP-1. The downmodulation of IL-6 by P. cicadae was inhibited by the p38 inhibitor (SB203580 or JNK inhibitor (SP600125. Moreover, the extract attenuated the expression of NF-κB and induced thrombomodulin in keratinocytes and thereby effectively downregulated inflammatory responses in the skin. The nuclear accumulation and expression of NF-E2-related factor (Nrf2 were increased by P. cicadae treatment. Furthermore, treatment with P. cicadae remarkably ameliorated the skin’s structural damage induced by irradiation. This study demonstrates that P. cicadae may protect skin cells against oxidative insult by modulating ROS concentration, IL-6, MMPs generation, antioxidant enzymes activity, and cell signaling pathways.

  19. The Eschericia coli Growth Inhibition Activity of Some Fermented Medicinal Plant Leaf Extract from the Karo Highland, North Sumatra

    Directory of Open Access Journals (Sweden)

    NOVIK NURHIDAYAT

    2009-10-01

    Full Text Available A lot of traditional medicinal plant has antibacterial acitivities. Most of these plants are freshly chewed or grounded and used directly to treat infectious bacterial deseases. However, some practices employ a traditionally spontaneous fermentation on boiled extracted leaf, root or other parts of the plant. This work reports a laboratory stimulated spontaneous fermentation of leaf extracts from selected medicinal plants collected from the Karo Higland. The spontaenous fermentation was stimulated to be carried out by the Acetobacter xylinum and Saccharomyces cerevisiae. The anti-infectious agent activity was assayed on the Eschericia coli growth inhibition. A complementary non fermented leaf extract was also made and assayed as a comparative measure. Indeed, the fermented leaf extract of bitter bush (Eupatorium pallescens, cacao (Theobroma cacao, avocado (Persia gratissima, passion fruit (Passiflora edulis, cassava (Cassava utillissima, diamond flower (Hedyotis corymbosa, periwinkle (Catharanthus roseus, and gandarusa (Justicia gendarussa have relatively higher anti-E.coli acitivity than those of non fermented ones. However, there were no anti-E.coli activity was detected in both fermented and non fermented leaf extract of the guava (Psidium guajava and common betel (Piper nigrum.

  20. Inhibition of cholinesterase activity by extracts, fractions and compounds from Calceolaria talcana and C. integrifolia (Calceolariaceae: Scrophulariaceae).

    Science.gov (United States)

    Cespedes, Carlos L; Muñoz, Evelyn; Salazar, Juan R; Yamaguchi, Lydia; Werner, Enrique; Alarcon, Julio; Kubo, Isao

    2013-10-25

    Extracts, fractions and compounds from Calceolaria talcana and C. integrifolia exhibited strong inhibitory effects of the activity of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes using the in vitro Ellmańs method. The most active samples were from the ethyl acetate extract, which caused a mixed-type inhibition against AChE (69.8% and 79.5% at 100 and 200 μg/ml, respectively) and against BChE (98.5% and 99.8% at 100 and 200 μg/ml, respectively) and its major components verbascoside 8 (50.9 and 70.0% at 200 μg/ml, against AChE and BChE, respectively), martynoside 9, and fraction F-7 (which corresponds to a mixture of 8, 9, and other phenylethanoids and phenolics that remain unidentified) (80.2 and 85.3% at 100 and 200 μg/ml, against AChE, respectively and 99.1 and 99.7% at 100 and 200 μg/ml, against BChE, respectively) inhibited the acetylcholinesterase enzyme competitively. The most polar fraction F-5 from n-hexane extract (a mixture of naphthoquinones: 2-hydroxy-3-(1,1-dimethylallyl-1,4-naphthoquinone) 6, α-dunnione 7 and other polar compounds that remain unidentified) showed a mixed-type inhibition (71.5 and 72.1% against AChE and BChE at 200 μg/ml, respectively). Finally, the methanol-soluble residue presented a complex, mixed-type inhibition (39.9 and 67.9% against AChE and BChE at 200 μg/ml, respectively). The mixture F-3 with diterpenes was obtained from the n-hexane extract: (1,10-cyclopropyl-9-epi-ent-isopimarol) 1, 19-α-hydroxy-abietatriene 2, and F-4 a mixture of triterpenes α-lupeol 3, β-sitosterol 4, ursolic acid 5 together with a complex mixture of terpenes that did not show activity. In summary, extracts and natural compounds from C. talcana and C. integrifolia were isolated, identified and characterized as cholinesterase inhibitors. Copyright © 2013 Elsevier Ltd. All rights reserved.

  1. Inhibition of α-glucosidase activity by ethanolic extract of Melia azedarach L. leaves

    Science.gov (United States)

    Sulistiyani; Safithri, Mega; Puspita Sari, Yoana

    2016-01-01

    Development of α-glucosidase inhibitor derived from natural products is an opportunity for a more economic management of diabetes prevention. The objective of this study was to test the activity of α-glucosidase with or without potential inhibitor compounds. By in vitro method, α-glucosidase hydrolizes p-nitrophenyl-α-D-glucopiranoside to glucose and the yellow of p-nitrophenol which can be determined with spectrophotometry at 400 nm. The ability of ethanolic leaf extract of Melia azedarach L. as a-glucosidase inhibitor was compared with that of commercial acarbose (Glucobay®). Acarbose showed strong inhibitory activity against a-glucosidase with IC50 values of 2.154 µg/mL. The crude ethanolic leaf extract of M. azedarach, however, showed less inhibitory activity with IC50 value of 3, 444.114 µg/mL. Total phenolics of M. azedarach leaves EtOH extract showed 17.94 µg GAE/mg extract and flavonoids total compound of 9.55 µg QE/mg extract. Based on the published wide range of IC50 values of extracts reported as a-glucosidase inhibitor which were between 10, 000 ppm-0.66 ppm, our result suggests that extract of M.azedarach leaves is potential candidate for development of anti-hyperglycemic formulation.

  2. Acellular bone marrow extracts significantly enhance engraftment levels of human hematopoietic stem cells in mouse xeno-transplantation models.

    Directory of Open Access Journals (Sweden)

    Kazem Zibara

    Full Text Available Hematopoietic stem cells (HSC derived from cord blood (CB, bone marrow (BM, or mobilized peripheral blood (PBSC can differentiate into multiple lineages such as lymphoid, myeloid, erythroid cells and platelets. The local microenvironment is critical to the differentiation of HSCs and to the preservation of their phenotype in vivo. This microenvironment comprises a physical support supplied by the organ matrix as well as tissue specific cytokines, chemokines and growth factors. We investigated the effects of acellular bovine bone marrow extracts (BME on HSC in vitro and in vivo. We observed a significant increase in the number of myeloid and erythroid colonies in CB mononuclear cells (MNC or CB CD34+ cells cultured in methylcellulose media supplemented with BME. Similarly, in xeno-transplantation experiments, pretreatment with BME during ex-vivo culture of HSCs induced a significant increase in HSC engraftment in vivo. Indeed, we observed both an increase in the number of differentiated myeloid, lymphoid and erythroid cells and an acceleration of engraftment. These results were obtained using CB MNCs, BM MNCs or CD34(+ cells, transplanted in immuno-compromised mice (NOD/SCID or NSG. These findings establish the basis for exploring the use of BME in the expansion of CB HSC prior to HSC Transplantation. This study stresses the importance of the mechanical structure and soluble mediators present in the surrounding niche for the proper activity and differentiation of stem cells.

  3. Hambatan Ekspresi Vascular Endothelial Growth Factor oleh Ekstrak Daun Sambung Nyawa pada Endotel Membran Korioalantois (EFFECTIVITY OF SAMBUNG NYAWA LEAF EXTRACT TO INHIBIT VASCULAR ENDOTHELIAL GROWTH FACTOR EXPRESSION ON ENDOTHELIALS OF CHORIOALLANTOIC

    Directory of Open Access Journals (Sweden)

    Iwan Sahrial Hamid

    2013-08-01

    Full Text Available Angiogenesis is the new blood vessels formation normality and important on growth and developmentof individu. Angiogenesis also have contribution to carcinogenesis or uncontrolled and malignant cancercell development, become pathologic condition like inflammatory and infection. The purpose of this researchfor knew the effectivities of Gynura procumbens extract on various dose for inhibition Vascular EndothelialGrowth Factor (VEGF expression. This research was done to effort cancer progress inhibition. However,angiogenesis is part of carcinogenesis causes. The Chorio Allantoic Membrane (CAM methods was usedfor this aim. Eggs at the age of nine days were divided into 6 groups. Group I were negative control ofvehicle, group II were zero treatment: 60 ng bFGF which aplicated into paper dish. The next four groupswere extract of Gynura procumbens that divided in four dose: 60, 75, 90 and 110 µg + bFGF 60 ng whichapplicated into  paper dish.  At the twelve days old, VEGF expression analysis was done whichimunohystochemical method with anti VEGF’s antibody. The result of this research showed that therewas significant different (p<0.05 on give of Gynura procumbens extract to VEGF expression. The mostsignificant VEGF inhibition by Gynura procumbens extract with dose 110 µg. The conclusion on this studywas Gynura procumbens extract effective to inhibit the VEGF expression on CAM embrio chick.

  4. A Mushroom Extract Piwep from Phellinus igniarius Ameliorates Experimental Autoimmune Encephalomyelitis by Inhibiting Immune Cell Infiltration in the Spinal Cord

    Directory of Open Access Journals (Sweden)

    Lan Li

    2014-01-01

    Full Text Available The present study aimed to evaluate the therapeutic potential of a mushroom extract from Phellinus igniarius in an animal model of multiple sclerosis. The medicinal mushroom, Phellinus igniarius, contains biologically active compounds that modulate the human immune system. Experimental autoimmune encephalomyelitis (EAE was induced by immunization with myelin oligodendrocyte glycoprotein (MOG 35–55 in C57BL/6 female mice. A water-ethanol extract of Phellinus igniarius (Piwep was delivered intraperitoneally every other day for the entire experimental course. Three weeks after the initial immunization, demyelination and immune cell infiltration in the spinal cord were examined. Piwep injection profoundly decreased the daily incidence rate and clinical score of EAE. The Piwep-mediated inhibition of the clinical course of EAE was accompanied by suppression of demyelination and infiltration of encephalitogenic immune cells including CD4+ T cells, CD8+ T cells, macrophages, and B cells in the spinal cord. Piwep reduced expression of vascular cell adhesion molecule-1 (VCAM-1 in the spinal cord and integrin-α4 in the lymph node of EAE mice. Piwep also inhibited proliferation of lymphocytes and secretion of interferon-γ in the lymph node of EAE mice. The results suggest that a mushroom extract, Piwep, may have a high therapeutic potential for ameliorating multiple sclerosis progression.

  5. Hexane Extracts of Calophyllum brasiliense Inhibit the Development of Gastric Preneoplasia in Helicobacter felis Infected INS-Gas Mice

    Science.gov (United States)

    Lemos, Larissa M. S.; Miyajima, Fabio; Castilho, Geovane R. C.; Martins, Domingos Tabajara O.; Pritchard, D. Mark; Burkitt, Michael D.

    2017-01-01

    Objectives: Indigenous Latin American populations have used extracts from Calophyllum brasiliense, a native hardwood, to treat gastrointestinal symptoms for generations. The hexane extract of Calophyllum brasiliense stem bark (HECb) protects against ethanol-mediated gastric ulceration in Swiss–Webster mice. We investigated whether HECb inhibits the development of gastric epithelial pathology following Helicobacter felis infection of INS-Gas mice. Materials and Methods: Groups of five male, 6-week-old INS-Gas mice were colonized with H. felis by gavage. From 2 weeks after colonization their drinking water was supplemented with 2% Tween20 (vehicle), low dose HECb (33 mg/L, lHECb) or high dose HECb (133 mg/L, hHECb). Equivalent uninfected groups were studied. Animals were culled 6 weeks after H. felis colonization. Preneoplastic pathology was quantified using established histological criteria. Gastric epithelial cell turnover was quantified by immunohistochemistry for Ki67 and active-caspase 3. Cytokines were quantified using an electrochemiluminescence assay. Results: Vehicle-treated H. felis infected mice exhibited higher gastric atrophy scores than similarly treated uninfected mice (mean atrophy score 5.6 ± 0.87 SEM vs. 2.2 ± 0.58, p < 0.01). The same pattern was observed following lHECb. Following hHECb treatment, H. felis status did not significantly alter atrophy scores. Gastric epithelial apoptosis was not altered by H. felis or HECb administration. Amongst vehicle-treated mice, gastric epithelial cell proliferation was increased 2.8-fold in infected compared to uninfected animals (p < 0.01). Administration of either lHECb or hHECb reduced proliferation in infected mice to levels similar to uninfected mice. A Th17 polarized response to H. felis infection was observed in all infected groups. hHECb attenuated IFN-γ, IL-6, and TNF production following H. felis infection [70% (p < 0.01), 67% (p < 0.01), and 41% (p < 0.05) reduction vs. vehicle, respectively

  6. Spatholobus suberectus Column Extract Inhibits Estrogen Receptor Positive Breast Cancer via Suppressing ER MAPK PI3K/AKT Pathway

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    Jia-Qi Sun

    2016-01-01

    Full Text Available Although Chinese herbal compounds have long been alternatively applied for cancer treatment in China, their treatment effects have not been sufficiently investigated. The Chinese herb Spatholobus suberectus is commonly prescribed to cancer patients. HPLC analysis has shown that the main components of Spatholobus suberectus are flavonoids that can be classified as phytoestrogens, having a structure similar to estrogen. This study was designed to investigate the effects of Spatholobus suberectus column extract (SSCE on the estrogen receptor-positive (ER+ breast cancer cell line MCF-7 and its possible molecular mechanism. In our study, MTT assay was performed to evaluate cell viability. The results show that SSCE (80, 160, and 320 μg/ml significantly decreased the viability of MCF-7 cells. SSCE also triggered apoptosis, arrested the cell cycle at the G0/G1 phase, and inhibited cell migration. A dual-luciferase reporter system showed that SSCE suppressed intranuclear p-ER activity; Western blot analysis confirmed the repressed expression of phosphorylated-ER alpha (p-ERα, ERK1/2, p-ERK1/2, AKT, p-AKT, p-mTOR, PI3K, and p-PI3K, indicating that SSCE suppressed the MAPK PI3K/AKT signaling pathway. Collectively, our results suggest that SSCE causes apoptosis, an arrest in the G0/G1 phase, and a decrease in migration in ER+ MCF-7 cells via hypoactivity of the ER and suppression of the MAPK PI3K/AKT pathway.

  7. Carbohydrase inhibition and anti-cancerous and free radical scavenging properties along with DNA and protein protection ability of methanolic root extracts of Rumex crispus

    National Research Council Canada - National Science Library

    Supriya Shiwani; Naresh Kumar Singh; Myeong Hyeon Wang

    2012-01-01

    The study elucidated carbohydrase inhibition, anti-cancerous, free radical scavenging properties and also investigated the DNA and protein protection abilities of methanolic root extract of Rumex crispus (RERC...

  8. Pyrolysates of raw vitrinites and their residues after CS2-NMP solvent extraction and its significance for petroleum geology

    Institute of Scientific and Technical Information of China (English)

    LIU Dayong; PENG Ping'an

    2006-01-01

    Binary solvent (CS2-NMP) has extreme high extraction ability to coals, and it can extract most bitumens out of coals and vitrinites. And large amount of messages on side chains and their distribution character in vitrinites should be acquired through flash pyrolysis before and after binary solvent (CS2-NMP) extraction. A few low maturated coals have been selected and vitrinites are handpicked from coals. Then vitrinites have been extracted using different solvents in the order of polarity. Flash pyrolysis-Gas Chromatography/Mass spectrum has been applied to samples. The result shows that CS2-NMP is efficient for the extraction of vitirnites, giving much higher extraction yield than common solvents. Production ratio of liquid hydrocarbons in pyrolysates of vitrinites extracted with CS2-NMP is lower than that of raw vitrinites. And relative ratio of each component in pyrolysates has changed apparently. Production ratio of aliphatic hydrocarbons, especially those long chain aliphatics have decreased much after mixed solvent extraction. It shows that bitumens extracted with CS2-NMP have largely contributed to pyrolysates, especially those aliphatics in pyrolysates.

  9. Ampelopsis brevipedunculata extract prevents bone loss by inhibiting osteoclastogenesis in vitro and in vivo

    National Research Council Canada - National Science Library

    Kim, Ju-Young; Park, Sun-Hyang; Oh, Hyun Mee; Kwak, Sung Chul; Baek, Jong Min; Lee, Myeung Su; Rho, Mun Chual; Oh, Jaemin

    2014-01-01

    .... However, its effects on osteoclast differentiation are unknown. We were aimed to investigate the anti-osteoclastogenic activity in vitro and in vivo and to elucidate the underlying mechanism of Ampelopsis brevipedunculata extract (ABE...

  10. Growth inhibition of periphytic diatoms by methanol extracts of sponges and holothurians

    Digital Repository Service at National Institute of Oceanography (India)

    Mokashe, S.S.; Garg, A; Anil, A; Wagh, A

    Crude methanol extracts of a holothurian Holothuria leucospilota, and two sponges Craniella sp. and Ircinia ramosa were tested for their inhibitory effects on the growth of two marine diatoms, Navicula subinflata and N. crucicula, by diatom plating...

  11. Ethanol extract and chromatographic fractions of Tamarindus indica stem bark inhibits Newcastle disease virus replication.

    Science.gov (United States)

    Okoh, Omobola O; Obiiyeke, Grace E; Nwodo, Uchechukwu U; Okoh, Anthony I

    2017-12-01

    The plethora of ethnomedicinal applications of Tamarindus indica Linn. (Leguminosae), tamarind, includes treatment of human and livestock ailments; preparations are recognized antipyretics in fevers, laxatives and carminatives. African folklore has various applications of tamarind. However, in Nyasaland, domestic fowl are fed with preparations for prophylactic properties. The objective of this study is to evaluate the antiviral properties of T. indica extract. Tamarindus indica stem bark was extracted through ethanol maceration over 24 h, and the crude extract was fractionated by gravity-propelled column chromatography. Newcastle disease virus (NDV) inhibitory activity of extract and fractions were evaluated in vivo using 10-d-old embryonated chicken egg (ECE) as the medium for virus cultivation and antivirus assay. About 240 ECE were grouped into eight (three controls and five experimental) and, 200 μL of the extract and fractions respectively inoculated into NDV pre-infected eggs and incubated at 37 °C. Allantoic fluid was harvested 5 d post-virus infection and assayed for haemagglutination (HA). Anti-NDV assessment showed 62.5 mg/mL of crude extract and fractions: TiA, TiC and TiD to yield a HA titre of 1:128 each, while TiB showed 1:64 HA titre. At 125 mg/mL, a titre of 1:16 was recorded against TiB and TiD and, 1:8 against TiA. Similarly, crude extract and TiC, each recorded 1:4 HA titre. However, the minimum concentrations of extract and fraction for virus inactivation were 0.24 mg/mL and 0.49 mg/mL, respectively. The antiviral activity shown by T. indica portends novel antiviral drugs and, perhaps, as scaffold for new drugs.

  12. Clinacanthus nutans (Burm. f.) Lindau Ethanol Extract Inhibits Hepatoma in Mice through Upregulation of the Immune Response

    OpenAIRE

    Danmin Huang; Wenjie Guo; Jing Gao; Jun Chen; Joshua Opeyemi Olatunji

    2015-01-01

    Clinacanthans nutans (Burm. f.) Lindau is a popular medicinal vegetable in Southern Asia, and its extracts have displayed significant anti-proliferative effects on cancer cells in vitro. However, the underlying mechanism for this effect has yet to be established. This study investigated the antitumor and immunomodulatory activity of C. nutans (Burm. f.) Lindau 30% ethanol extract (CN30) in vivo. CN30 was prepared and its main components were identified using high-performance liquid chromatogr...

  13. Extraction and inhibition of enzymatic activity of botulinum neurotoxins/A1, /A2, and /A3 by a panel of monoclonal anti-BoNT/A antibodies.

    Directory of Open Access Journals (Sweden)

    Suzanne R Kalb

    Full Text Available Botulinum neurotoxins (BoNTs are extremely potent toxins that are capable of causing death or respiratory failure leading to long-term intensive care. Treatment includes serotype-specific antitoxins, which must be administered early in the course of the intoxication. Rapidly determining human exposure to BoNT is an important public health goal. In previous work, our laboratory focused on developing Endopep-MS, a mass spectrometry-based endopeptidase method for detecting and differentiating BoNT/A-G serotypes in buffer and BoNT/A, /B, /E, and /F in clinical samples. We have previously reported the effectiveness of antibody-capture to purify and concentrate BoNTs from complex matrices, such as clinical samples. Because some antibodies inhibit or neutralize the activity of BoNT, the choice of antibody with which to extract the toxin is critical. In this work, we evaluated a panel of 16 anti-BoNT/A monoclonal antibodies (mAbs for their ability to inhibit the in vitro activity of BoNT/A1, /A2, and /A3 complex as well as the recombinant LC of A1. We also evaluated the same antibody panel for the ability to extract BoNT/A1, /A2, and /A3. Among the mAbs, there were significant differences in extraction efficiency, ability to extract BoNT/A subtypes, and inhibitory effect on BoNT catalytic activity. The mAbs binding the C-terminal portion of the BoNT/A heavy chain had optimal properties for use in the Endopep-MS assay.

  14. Fagraea racemosa leaf extract inhibits oxidative stress-induced liver damage in Wistar rats

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    Eva Rachmi

    2012-07-01

    (six Wistar rats each, respectively, once per day for 30 days. CCl4 injected intraperitoneally to those three groups, twice a week (1,5 ml/kg bw.  Two control groups were provided that were one normal control group and one CCl4 control group.  On the 30th day, the rats were killed and its liver examined with Haematoxyllin eosin staining. Histopathological changes were graded based on the degree of steatosis, hydropic degeneration, and inflammation. Data were analyzed with ANOVA and LSD post hoc (p≤0.05 using SPSS version 13.0 Results: The results showed improvement between the three treatment groups and the CCl4 control group about the degree of hydropic degeneration and inflammation (P ≤ 0.05. However, there were significant increased of steatosis 50 and 100 mg/kg bw treatment groups, before its significantly decrease at 200 mg/kg bw treatment group (2.5 g/kg. Conclusions: Fagraea racemosa leaves methanolic extract could protect liver from free radicals generated by CCl4. The result indicated that Fagraea racemosa has promising quality to be explored as antioxidant supplement. (Health Science Indones 2011;2:46-51

  15. Apoptosis-mediated inhibition of human breast cancer cell proliferation by lemon citrus extract.

    Science.gov (United States)

    Alshatwi, Ali A; Shafi, Gowhar; Hasan, Tarique N; Al-Hazzani, Amal A; Alsaif, Mohammed A; Alfawaz, Mohammed A; Lei, K Y; Munshi, Anjana

    2011-01-01

    Dietary phytochemicals have a variety of antitumor properties. In the present study, the antitumor activity of methanolic extract of lemon fruit (lemon extract; LE) (LE) on the MCF-7 breast cancer cell line was investigated in vitro. Apoptotic cell death was analyzed using the TUNEL assay. In addition, the apoptosis mediated by LE extract in the MCF-7 cells was associated with the increased expression of the tumor suppressor p53 and caspase-3. Additionally, the expression of a pro-apoptotic gene, bax, was increased, and the expression of an anti-apoptotic gene, bcl-2, was decreased by LE extract treatment, resulting in a shift in the Bax:Bcl-2 ratio to one that favored apoptosis. The expression of a major apoptotic gene, caspase-3, was increased by LE extract treatment. In light of the above results, we concluded that LE extract can induce the apoptosis of MCF-7 breast cancer cells via Bax-related caspase-3 activation. This study provides experimental data that are relevant to the possible future clinical use of LE to treat breast cancer.

  16. In vitro cancer cell growth inhibition and antioxidant activity of Bombax ceiba (Bombacaceae) flower extracts.

    Science.gov (United States)

    Tundis, Rosa; Rashed, Khaled; Said, Ataa; Menichini, Francesco; Loizzo, Monica R

    2014-05-01

    The flowers of Bombax ceiba were investigated for their chemical composition, antioxidant effects and antiproliferative activity against seven human cancer cell lines. The antiproliferative responses of diethyl ether (DE) and light petroleum (PE) extracts were evaluated by sulforhodamine B (SRB) assay against MCF-7, HeLa, COR-L23, C32, A375, ACHN, and LNCaP cells in comparison with a human normal cell line, 142BR. Moreover, extracts were characterized by GC-MS analysis and tested for their antioxidant properties by different in vitro systems, namely DPPH, Fe-chelating activity and beta-carotene bleaching test. Both PE and DE extracts showed the highest antiproliferative activity against human renal adenocarcinoma (ACHN) in a concentration-dependent manner. PE extract showed the highest radical scavenging activity against the DPPH radical, while DE extract was more active in the beta-carotene bleaching test. The presence of beta-sitosterol and some fatty acids may contribute to the bioactivity of B. ceiba flower extracts.

  17. Evaluation of a Brain Acetylcholinesterase Extraction Method and Kinetic Constants after Methyl-Paraoxon Inhibition in Three Brazilian Fish Species

    Science.gov (United States)

    Freitas, A. P.; Santos, C. R.; Sarcinelli, P. N.; Hauser-Davis, R. A.; Lopes, R. M.

    2016-01-01

    Acetylcholinesterase (AChE) is an important enzyme in the control of the neuronal action potential and sensitive to organophosphate inhibition. Brain fish AChE is less sensitive to organophosphate inhibition than AChE from terrestrial animals, although this sensitivity is variable among species and has not yet been fully evaluated in fish species. In this setting, inhibition kinetic constants for progressive irreversible inhibition of brain acetylcholinesterase due to methyl-paraoxon exposure were determined in three fish species (Mugil liza, Genidens genidens and Lagocephalus laevigatus) and hen (Gallus domesticus). Enzyme extraction using a detergent was shown to be adequate, and samples presented activity inhibition in high substrate concentrations and suppression of inhibition by methyl-paraoxon in the presence of the substrate, similar to kinetic patterns from purified enzyme preparations. Catfish (G. genidens) AChE presented the highest sensitivity among the evaluated fish species (IC50 = 1031.20 nM ± 63.17) in comparison to M. liza and L. laevigatus (IC50: 2878.83 ± 421.94 and 2842.5 ± 144.63 nM respectively). The lower dissociation constant (Kd = 20.3 ± 2.95 μM) of catfish AChE showed greater enzyme affinity for methyl-paraoxon, explaining this species higher sensitivity to organophosphates. Hen AChE presented higher ki (900.57 ± 65.3 mM-1min-1) and, consequently, greater sensitivity to methyl-paraoxon, explained by a lower Kd (0.6 ± 0.13 μM). Furthermore, hen AChE did not differentiate between the propionylthiocholine and acetylthiocholine substrates, indicating easier access of methyl-paraoxon to the hen enzyme activity site. The results obtained herein indicate a suitable extraction of AChE and, despite different inhibition kinetic constants, demonstrate that fish AChE is less sensitive to methyl-paraoxon, probably due to reduced access to the catalytic center which provides greater enzyme substrate selectivity. PMID:27655611

  18. Daphne Genkwa Sieb. et Zucc. Water-Soluble Extracts Act on Enterovirus 71 by Inhibiting Viral Entry

    Directory of Open Access Journals (Sweden)

    Chia-Wen Chang

    2012-04-01

    Full Text Available Dried flowers of Daphne genkwa Sieb. et Zucc. (Thymelaeaceae are a Chinese herbal medicine used as an abortifacient with purgative, diuretic and anti-inflammatory activities. However, the activity of this medicine against enteroviral infections has not been investigated. The water-extract of dried buds of D. genkwa Sieb. et Zucc. (DGFW was examined against various strains of enterovirus 71 (EV71 by neutralization assay, and its initial mode of action was characterized by time-of-addition assay followed by attachment and penetration assays. Pretreatment of DGFW with virus abolished viral replication, indicating that DGFW inhibits EV71 by targeting the virus. GFW exerts its anti-EV71 effects by inhibiting viral entry without producing cytotoxic side effects and thus provides a potential agent for antiviral chemotherapeutics.

  19. Aqueous extracts of two varieties of ginger (Zingiber officinale) inhibit angiotensin I-converting enzyme, iron(II), and sodium nitroprusside-induced lipid peroxidation in the rat heart in vitro.

    Science.gov (United States)

    Akinyemi, Ayodele J; Ademiluyi, Adedayo O; Oboh, Ganiyu

    2013-07-01

    Ginger has reportedly been used in folk medicine for the management and prevention of hypertension and other cardiovascular diseases. Therefore, this study sought to investigate the inhibitory effect of aqueous extracts of two varieties of ginger on a key enzyme linked to hypertension (angiotensin I-converting enzyme [ACE]), and on pro-oxidants [Fe(2+) and sodium nitroprusside (SNP)] which have been shown to induce lipid peroxidation in the rat's isolated heart in vitro. Aqueous extracts (0.05 mg/mL) of red ginger (Zingiber officinale var. Rubra) and white ginger (Zingiber officinale Roscoe) were prepared and the ability of the extracts to inhibit ACE along with Fe(2+)- and SNP-induced lipid peroxidation was determined in rat's heart in vitro. Results revealed that both extracts inhibited ACE in a dose-dependent manner (25-125 μg/mL). However, red ginger extract (EC50=27.5 μg/mL) had a significantly (Pginger extract (EC50=87.0 μg/mL). Furthermore, incubation of the rat's heart in the presence of Fe(2+) and SNP caused a significant increase (Pginger extracts (78-313 μg/mL) caused a dose-dependent decrease in the MDA content of the stressed heart homogenates. This suggests that the possible mechanism through which ginger exerts its antihypertensive properties may be through inhibition of ACE activity and prevention of lipid peroxidation in the heart. Furthermore, red ginger showed stronger inhibition of ACE than white ginger. Additionally, it should be noted that these protective properties of the ginger varieties could be attributed to their polyphenol contents.

  20. Sedum sarmentosum Bunge extract induces apoptosis and inhibits proliferation in pancreatic cancer cells via the hedgehog signaling pathway.

    Science.gov (United States)

    Bai, Yongheng; Chen, Bicheng; Hong, Weilong; Liang, Yong; Zhou, Mengtao; Zhou, Lan

    2016-05-01

    Sedum sarmentosum Bunge, a traditional Chinese herbal medicine, has a wide range of clinical applications including antibiosis, anti-inflammation and anti-oxidation. In the present study, we identified that its extract (SSBE) exerts pancreatic anticancer activity in vitro and in vivo. In the cultured pancreatic cancer PANC-1 cell line, SSBE inhibited cell growth in a concentration-dependent manner, and it was accompanied by the downregulated expression of proliferating cell nuclear antigen (PCNA). In addition, SSBE treatment also increased cellular apoptosis in a mitochondrial-dependent manner. Moreover, SSBE induced p53 expression, reduced c-Myc expression, and inhibited epithelial-mesenchymal transition (EMT). The antiproliferative activity of SSBE in the pancreatic cancer cells was found to be closely related to cell cycle arrest at the G2/M phase by upregulating p21(Waf1/CIP1) expression. Further study showed that this inhibitory effect of SSBE was through downregulation of the activity of the proliferation-related Hedgehog signaling pathway. Exogenous recombinant protein Shh was used to activate Hedgehog signaling, thereby resulting in the abolishment of the SSBE-mediated inhibition of pancreatic cancer cell growth. In animal xenograft models of pancreatic cancer, activated Hedgehog signaling was also observed compared with the vehicle controls, but was reduced by SSBE administration. As a result, SSBE suppressed the growth of pancreatic tumors. Thus, these findings demonstrate that SSBE has therapeutic potential for pancreatic cancer, and this anticancer effect in pancreatic cancer cells is associated with inhibition of the Hedgehog signaling pathway.

  1. Inhibition of lung cancer cells A549 and H460 by curcuminoid extracts and nanoemulsions prepared from Curcuma longa Linnaeus

    Directory of Open Access Journals (Sweden)

    Chang HB

    2015-08-01

    Full Text Available Hong-Bin Chang,1 Bing-Huei Chen1,21Department of Food Science, 2Graduate Institute of Medicine, Fu Jen Catholic University, Taipei, TaiwanAbstract: The objectives of this study were to explore the inhibition mechanism of lung cancer cells A549 and H460 by curcuminoid extracts and nanoemulsions prepared from Curcuma longa Linnaeus. In addition, human bronchus epithelial cell line BEAS-2B (normal cell was selected for comparison. A high-performance liquid chromatography (HPLC method was developed to separate and quantify the various curcuminoids in C. longa extract, including curcumin (1,714.5 µg/mL, demethoxycurcumin (1,147.4 µg/mL, and bisdemethoxycurcumin (190.2 µg/mL. A high-stability nanoemulsion composed of Tween 80, water, and curcuminoid extract was prepared, with mean particle size being 12.6 nm. The cell cycle was retarded at G2/M for both the curcuminoid extract and nanoemulsion treatments; however, the inhibition pathway may be different. H460 cells were more susceptible to apoptosis than A549 cells for both curcuminoid extract and nanoemulsion treatments. Growth of BEAS-2B remained unaffected for both the curcuminoid extract and nanoemulsion treatments, with a concentration range from 1 to 4 µg/mL. Also, the activities of caspase-3, caspase-8, and caspase-9 followed a dose-dependent increase for both A549 and H460 cells for both the treatments, accompanied by a dose-dependent increase in cytochrome C expression and a dose-dependent decrease in CDK1 expression. Interestingly, a dose-dependent increase in cyclin B expression was shown for A549 cells for both the treatments, while a reversed trend was found for H460 cells. Both mitochondria and death receptor pathways may be responsible for apoptosis of both A549 and H460 cells.Keywords: curcuminoid extract, curcuminoid nanoemulsion, Curcuma longa Linnaeus, lung cancer cell, cell cycle, apoptosis mechanism

  2. The anti-inflammatory activity of standard aqueous stem bark extract of Mangifera indica L. as evident in inhibition of Group IA sPLA2.

    Science.gov (United States)

    Dhananjaya, Bhadrapura Lakkappa; Shivalingaiah, Sudharshan

    2016-03-01

    The standard aqueous stem bark extract is consumed as herbal drink and used in the pharmaceutical formulations to treat patients suffering from various disease conditions in Cuba. This study was carried out to evaluate the modulatory effect of standard aqueous bark extract of M. indica on Group IA sPLA2. M. indica extract, dose dependently inhibited the GIA sPLA2 (NN-XIa-PLA2) activity with an IC50 value 8.1 µg/ml. M. indica extract effectively inhibited the indirect hemolytic activity up to 98% at ~40 µg/ml concentration and at various concentrations (0-50 µg/ml), it dose dependently inhibited the edema formation. When examined as a function of increased substrate and calcium concentration, there was no relieve of inhibitory effect on the GIA sPLA2. Furthermore, the inhibition was irreversible as evidenced from binding studies. It is observed that the aqueous extract ofM. indica effectively inhibits sPLA2 and it is associated inflammatory activities, which substantiate their anti-inflammatory properties. The mode of inhibition could be due to direct interaction of components present in the extract, with sPLA2 enzyme. Further studies on understanding the principal constituents, responsible for the anti-inflammatory activity would be interesting to develop this into potent anti-inflammatory agent.

  3. The anti-inflammatory activity of standard aqueous stem bark extract of Mangifera indica L. as evident in inhibition of Group IA sPLA2

    Directory of Open Access Journals (Sweden)

    BHADRAPURA LAKKAPPA DHANANJAYA

    2016-03-01

    Full Text Available ABSTRACT The standard aqueous stem bark extract is consumed as herbal drink and used in the pharmaceutical formulations to treat patients suffering from various disease conditions in Cuba. This study was carried out to evaluate the modulatory effect of standard aqueous bark extract of M. indica on Group IA sPLA2. M. indica extract, dose dependently inhibited the GIA sPLA2 (NN-XIa-PLA2 activity with an IC50 value 8.1 µg/ml. M. indica extract effectively inhibited the indirect hemolytic activity up to 98% at ~40 µg/ml concentration and at various concentrations (0-50 µg/ml, it dose dependently inhibited the edema formation. When examined as a function of increased substrate and calcium concentration, there was no relieve of inhibitory effect on the GIA sPLA2. Furthermore, the inhibition was irreversible as evidenced from binding studies. It is observed that the aqueous extract ofM. indica effectively inhibits sPLA2 and it is associated inflammatory activities, which substantiate their anti-inflammatory properties. The mode of inhibition could be due to direct interaction of components present in the extract, with sPLA2 enzyme. Further studies on understanding the principal constituents, responsible for the anti-inflammatory activity would be interesting to develop this into potent anti-inflammatory agent.

  4. Inhibition of IRAK-4 activity for rescuing endotoxin LPS-induced septic mortality in mice by lonicerae flos extract

    Energy Technology Data Exchange (ETDEWEB)

    Park, Sun Hong; Roh, Eunmiri [College of Pharmacy, Chungbuk National University, Cheongju 361-763 (Korea, Republic of); Kim, Hyun Soo [Pharmaceutical R and D Center, Huons Co., Ltd., Anyang (Korea, Republic of); Baek, Seung-Il [College of Pharmacy, Chungbuk National University, Cheongju 361-763 (Korea, Republic of); Choi, Nam Song [Pharmaceutical R and D Center, Huons Co., Ltd., Anyang (Korea, Republic of); Kim, Narae; Hwang, Bang Yeon; Han, Sang-Bae [College of Pharmacy, Chungbuk National University, Cheongju 361-763 (Korea, Republic of); Kim, Youngsoo, E-mail: youngsoo@chungbuk.ac.kr [College of Pharmacy, Chungbuk National University, Cheongju 361-763 (Korea, Republic of)

    2013-12-13

    Highlights: •Lonicerae flos extract (HS-23) is a clinical candidate, Phase I for sepsis treatment. •Here, HS-23 or its major constituents rescued LPS-induced septic mortality in mice. •As a mechanism, they directly inhibited IRAK-4-catalyzed kinase activity. •Thus, they suppressed LPS-induced expression of NF-κB/AP-1-target inflammatory genes. -- Abstract: Lonicerae flos extract (HS-23) is a clinical candidate currently undergoing Phase I trial in lipopolysaccharide (LPS)-injected healthy human volunteers, but its molecular basis remains to be defined. Here, we investigated protective effects of HS-23 or its major constituents on Escherichia coli LPS-induced septic mortality in mice. Intravenous treatment with HS-23 rescued LPS-intoxicated C57BL/6J mice under septic conditions, and decreased the levels of cytokines such as tumor necrosis factor α (TNF-α), interleukin (IL)-1β and high-mobility group box-1 (HMGB-1) in the blood. Chlorogenic acid (CGA) and its isomers were assigned as major constituents of HS-23 in the protection against endotoxemia. As a molecular mechanism, HS-23 or CGA isomers inhibited endotoxin LPS-induced autophosphorylation of the IL-1 receptor-associated kinase 4 (IRAK-4) in mouse peritoneal macrophages as well as the kinase activity of IRAK-4 in cell-free reactions. HS-23 consequently suppressed downstream pathways critical for LPS-induced activation of nuclear factor (NF)-κB or activating protein 1 (AP-1) in the peritoneal macrophages. HS-23 also inhibited various toll-like receptor agonists-induced nitric oxide (NO) production, and down-regulated LPS-induced expression of NF-κB/AP-1-target inflammatory genes in the cells. Taken together, HS-23 or CGA isomers exhibited anti-inflammatory therapy against LPS-induced septic mortality in mice, at least in part, mediated through the inhibition of IRAK-4.

  5. Water extracts of cabbage and kale inhibit ex vivo H(2)O(2)-induced DNA damage but not rat hepatocarcinogenesis.

    Science.gov (United States)

    Horst, M A; Ong, T P; Jordão, A A; Vannucchi, H; Moreno, F S; Lajolo, F M

    2010-03-01

    The chemopreventive potential of water extracts of the Brassica vegetables cabbage and kale was evaluated by administering their aqueous extracts in drinking water ad libitum to Wistar rats submitted to Ito's hepatocarcinogenesis model (CB group and K group, respectively - 14 rats per group). Animals submitted to this same model and treated with water were used as controls (W group - 15 rats). Treatment with the vegetable extracts did not inhibit (P > 0.05) placental glutathione S-transferase-positive preneoplastic lesions (PNL). The number of apoptotic bodies did not differ (P > 0.05) among the experimental groups. Ex vivo hydrogen peroxide treatment of rat livers resulted in lower (P kale- (110.8 +/- 10.0 microm) treated animals compared with control (120.9 +/- 12.7 microm), as evaluated by the single cell gel (comet) assay. Treatment with cabbage (2 +/- 0.3 microg/g) or kale (4 +/- 0.2 microg/g) resulted in increased (P kale aqueous extracts on PNL, these Brassica vegetables presented protection against DNA damage, an effect possibly related to increased hepatic lutein concentrations. However, it must be pointed out that the cause-effect relationship between lutein levels and protection is hypothetical and remains to be demonstrated.

  6. Significant Enrichment of Polyunsaturated Fatty Acids (PUFAs) in the Lipids Extracted by Supercritical CO2 from the Livers of Australian Rock Lobsters (Jasus edwardsii).

    Science.gov (United States)

    Nguyen, Trung T; Zhang, Wei; Barber, Andrew R; Su, Peng; He, Shan

    2015-05-13

    Australian rock lobster (Jasus edwardsii) liver contains approximately 24.3% (w/w) lipids, which can contain a high amount of polyunsaturated fatty acids (PUFAs). However, this material has been found to be contaminated with arsenic (240 mg/kg) and cadmium (8 mg/kg). The high level of contaminants in the raw material and the large amount of PUFAs in the lipids prove a significant challenge in the extraction of high-quality lipids from this byproduct by conventional methods. Supercritical carbon dioxide (SC-CO2) extraction is a highly promising technology for lipid extraction with advantages including low contamination and low oxidation. The technique was optimized to achieve nearly 94% extraction of lipids relative to conventional Soxhlet extraction in Australian rock lobster liver at conditions of 35 MPa and 50 °C for 4 h. The extracted lipids are significantly enriched in PUFAs at 31.3% of total lipids, 4 times higher than those in the lipids recovered by Soxhlet extraction (7.8%). Specifically, the concentrations of docosahexaenoic acid (DHA) and eicosapentaenoic acid (EPA) in SC-CO2 extraction are 7 times higher than those obtained by Soxhlet extraction. Moreover, very small amounts of toxic heavy metals such as lead (Pb), arsenic (As), mercury (Hg), and cadmium (Cd) were detected in the SC-CO2-extracted lipids, 0.5-27 times lower than those in the Soxhlet-extracted lipids, which are 40-200 times lower than the regulatory limit maximum values. The low levels of contaminants and the high proportion of PUFAs (dominated by DHA and EPA) found in the SC-CO2-extracted lipids from Australian rock lobster liver suggest that the material could potentially be used as a valuable source of essential fatty acids for human consumption.

  7. Anti-TB activity of Evodia elleryana bark extract

    Science.gov (United States)

    Barrows, Louis R.; Powan, Emma; Pond, Christopher D.; Matainaho, Teatulohi

    2009-01-01

    An ethyl acetate extract of bark from Evodia elleryana produced significant growth inhibition of Mycobacterium tuberculosis at concentrations only minimally inhibitory to human T cells. The crude extract yielded 95% inhibition of TB at 50 μg/ml. The crude extract yielded 29 % growth inhibition of human T-cells in culture at that concentration. PMID:17350179

  8. Hericium erinaceus (Lion’s Mane) mushroom extracts inhibit metastasis of cancer cells to the lung in CT-26 colon cancer-transplanted mice

    Science.gov (United States)

    We investigated the anti-metastatic activity of four Hericium erinaceus edible mushroom extracts using CT-26 murine colon carcinoma cells as an indicator of inhibition of cell migration to the lung. Hot water (HWE) and microwaved 50% ethanol (MWE) extracts of Hericium erinaceus strongly elicited ca...

  9. INHIBITION OF COXACKIE VIRUS B3 IN MICE USING METHANOLIC EXTRACT OF CALLIANDRA HAEMATOCEPHALA

    OpenAIRE

    Mohamed Shaheen; Mamdouh El-Gamal; Adel Mousa; Samy Mostafa; Nagwa El-Esnawy

    2014-01-01

    Coxsackie virus B3 (CVB3) represents current major threats to public health and considers as an important viral pathogen related to viral myocarditis. We determined the safety of methanolic extract of Calliandra haematocephala in non-infected mice then two safe doses were selected to be evaluated in infected mice with CVB3 by determining the morbidity, mortality, heart to body weight ratio (HW/BW), virus titers in heart tissue. The effect of the extract on the heart tissues and the activities...

  10. Inhibition of Raf/MAPK signaling in Xenopus oocyte extracts by Raf-1-specific peptides.

    Science.gov (United States)

    Radziwill, G; Steinhusen, U; Aitken, A; Moelling, K

    1996-10-01

    Raf-1 is an upstream element of the mitogen-activated protein kinase (MAPK) pathway which leads to cell proliferation and differentiation. In this study Raf-1 derived peptides comprising the conserved amino acid residues Arg89 and Ser259, involved in binding of activated Ras and 14-3-3 proteins, respectively, were shown to interfere with MAPK activation in extracts from immature Xenopus oocytes. Lipids prepared from oocyte extracts can stimulate MAPK in a Ras- and protein kinase C-independent manner. This lipid-induced MAPK activation is blocked by a Raf-1 derived peptide comprising Ser259.

  11. Corrosion Inhibition Performance of Lignin Extract of Sun Flower (Tithonia Diversifolia on Medium Carbon Low Alloy Steel Immersed in H2SO4 Solution

    Directory of Open Access Journals (Sweden)

    Kenneth K. ALANEME

    2012-08-01

    Full Text Available The inhibition potentials of lignin extract of sun flower was investigated by evaluating the corrosion behaviour of medium carbon low alloy steel immersed in 1M H2SO4 solution containing varied concentration of the extract. Mass loss, corrosion rate, and adsorption characterization were utilized to evaluate the corrosion inhibition and adsorption properties of the extract. The results revealed that the lignin extract is an efficient inhibitor of corrosion in mild steel immersed in 1M H2SO4. The corrosion rates were observed to decrease with increase in concentration of lignin extract but increase with temperature. The activation energies and the negative free energy of adsorption obtained from the adsorption studies indicate that the lignin extract is physically adsorbed on the surface of the steel and that the adsorption is strong, spontaneous and fit excellently with the assumptions of the Langmuir adsorption isotherm.

  12. Evaluation of RAST inhibition as a method for the standardization of house-dust extracts

    NARCIS (Netherlands)

    Bruynzeel, P.L.B.; Kersten, W.; Berrens, L.

    1980-01-01

    RAST-inhibition was evaluated as a method for the in vitro standardization of house dust allergens, using four lyophilized house-dust preparations of different degree of purification (R1, R2, R3 and R4). When a serum pool of highly house-dust sensitive patients was used, a qualitatively similar pote

  13. Extract of the seed coat of Tamarindus indica inhibits nitric oxide production by murine macrophages in vitro and in vivo.

    Science.gov (United States)

    Komutarin, T; Azadi, S; Butterworth, L; Keil, D; Chitsomboon, B; Suttajit, M; Meade, B J

    2004-04-01

    The seed coat extract of Tamarindus indica, a polyphenolic flavonoid, has been shown to have antioxidant properties. The present studies investigated the inhibitory effect of the seed coat extract of T. indica on nitric oxide production in vitro using a murine macrophage-like cell line, RAW 264.7, and in vitro and in vivo using freshly isolated B6C3F1 mouse peritoneal macrophages. In vitro exposure of RAW 264.7 cells or peritoneal macrophages to 0.2-200 microg/mL of T. indica extract significantly attenuated (as much as 68%) nitric oxide production induced by lipopolysaccharide (LPS) and interferon gamma (IFN-gamma) in a concentration-dependent manner. In vivo administration of T. indica extract (100-500 mg/kg) to B6C3F1 mice dose-dependently suppressed TPA, LPS and/or IFN-gamma induced production of nitric oxide in isolated mouse peritoneal macrophages in the absence of any effect on body weight. Exposure to T. indica extract had no effect on cell viability as assessed by the MTT assay. In B6C3F1 mice, preliminary safety studies demonstrated a decrease in body weight at only the highest dose tested (1000 mg/kg) without alterations in hematology, serum chemistry or selected organ weights or effects on NK cell activity. A significant decrease in body weight was observed in BALB/c mice exposed to concentrations of extract of 250 mg/kg or higher. Oral exposure of BALB/c mice to T. indica extract did not modulate the development of T cell-mediated sensitization to DNFB or HCA as measured by the local lymph node assay, or dermal irritation to nonanoic acid or DNFB. These studies suggest that in mice, T. indica extract at concentrations up to 500 mg/kg may modulate nitric oxide production in the absence of overt acute toxicity.

  14. Traditional Chinese medicine herbal extracts of Cibotium barometz, Gentiana scabra, Dioscorea batatas, Cassia tora, and Taxillus chinensis inhibit SARS-CoV replication.

    Science.gov (United States)

    Wen, Chih-Chun; Shyur, Lie-Fen; Jan, Jia-Tsrong; Liang, Po-Huang; Kuo, Chih-Jung; Arulselvan, Palanisamy; Wu, Jin-Bin; Kuo, Sheng-Chu; Yang, Ning-Sun

    2011-10-01

    Development of anti-severe acute respiratory syndrome associated coronavirus (SARS-CoV) agents is pivotal to prevent the reemergence of the life-threatening disease, SARS. In this study, more than 200 extracts from Chinese medicinal herbs were evaluated for anti-SARS-CoV activities using a cell-based assay that measured SARS-CoV-induced cytopathogenic effect (CPE) in vitro on Vero E6 cells. Six herbal extracts, one each from Gentianae Radix ( lóng dǎn; the dried rhizome of Gentiana scabra), Dioscoreae Rhizoma ( shān yào; the tuber of Dioscorea batatas), Cassiae Semen ( jué míng zǐ; the dried seed of Cassia tora) and Loranthi Ramus ( sāng jì shēng; the dried stem, with leaf of Taxillus chinensis) (designated as GSH, DBM, CTH and TCH, respectively), and two from Rhizoma Cibotii ( gǒu jǐ; the dried rhizome of Cibotium barometz) (designated as CBE and CBM), were found to be potent inhibitors of SARS-CoV at concentrations between 25 and 200 μg/ml. The concentrations of the six extracts needed to inhibit 50% of Vero E6 cell proliferation (CC50) and 50% of viral replication (EC50) were determined. The resulting selective index values (SI = CC50/EC50) of the most effective extracts CBE, GSH, DBM, CTH and TCH were > 59.4, > 57.5, > 62.1, > 59.4, and > 92.9, respectively. Among these extracts, CBM and DBM also showed significant inhibition of SARS-CoV 3CL protease activity with IC50 values of 39 μg/ml and 44 μg/ml, respectively. Our findings suggest that these six herbal extracts may have potential as candidates for future development of anti-SARS therapeutics.AbbreviationsSARS,severe acute respiratory syndromeCoV,coronavirusCPE,cytopathogenic effectTCM,traditional Chinese medicine.

  15. The standard aqueous stem bark extract of Mangifera indica L. inhibits toxic PLA2 - NN-XIb-PLA2 of Indian cobra venom.

    Science.gov (United States)

    Dhananjaya, Bhadrapura Lakkappa; Sudarshan, Shivalingaiah; Dongol, Yashad; More, Sunil S

    2016-05-01

    The aqueous extract of Mangifera indica is known to possess diverse medicinal properties, which also includes anti-snake venom activities. However, its inhibitory potency and mechanism of action on multi-toxic snake venom phospholipases A2s are still unknown. Therefore, the objective of this study was to evaluate the modulatory effect of standard aqueous bark extract of M. indica on NN-XIb-PLA2 of Indian cobra venom. The in vitro sPLA2, in situ hemolytic and in vivo edema inhibition effect were carried out as described. Also the effect of substrate and calcium concentration was carried out. M. indica extract dose dependently inhibited the GIA sPLA2 (NN-XIb-PLA2) activity with an IC50 value of 7.6 μg/ml. M. indica extract effectively inhibited the indirect hemolytic activity up to 98% at ∼40 μg/ml concentration. Further, M. indica extract (0-50 μg/ml) inhibited the edema formed in a dose dependent manner. When examined as a function of increased substrate and calcium concentration, there was no relieve of inhibitory effect of M. indica extract on the NN-XIb-PLA2. Further, the inhibition was irreversible as evident from binding studies. The in vitro inhibition is well correlated with in situ and in vivo edema inhibiting activities of M. indica. As the inhibition is independent of substrate and calcium and was irreversible, it can be concluded that M. indica extract mode of inhibition could be due to direct interaction of components present in the extract with the PLA2 enzyme. The aqueous extract of M. indica effectively inhibits svPLA2 enzymatic and its associated toxic activities, which substantiate their anti-snake venom properties. Further in-depth studies on the role and mechanism of the principal constituents present in the extract, responsible for the anti-PLA2 activity will be interesting to develop them into potent antisnake component and also as an anti-inflammatory agent.

  16. The standard aqueous stem bark extract of Mangifera indica L. inhibits toxic PLA2 – NN-XIb-PLA2 of Indian cobra venom

    Directory of Open Access Journals (Sweden)

    Bhadrapura Lakkappa Dhananjaya

    2016-05-01

    Full Text Available The aqueous extract of Mangifera indica is known to possess diverse medicinal properties, which also includes anti-snake venom activities. However, its inhibitory potency and mechanism of action on multi-toxic snake venom phospholipases A2s are still unknown. Therefore, the objective of this study was to evaluate the modulatory effect of standard aqueous bark extract of M. indica on NN-XIb-PLA2 of Indian cobra venom. The in vitro sPLA2, in situ hemolytic and in vivo edema inhibition effect were carried out as described. Also the effect of substrate and calcium concentration was carried out. M. indica extract dose dependently inhibited the GIA sPLA2 (NN-XIb-PLA2 activity with an IC50 value of 7.6 μg/ml. M. indica extract effectively inhibited the indirect hemolytic activity up to 98% at ∼40 μg/ml concentration. Further, M. indica extract (0–50 μg/ml inhibited the edema formed in a dose dependent manner. When examined as a function of increased substrate and calcium concentration, there was no relieve of inhibitory effect of M. indica extract on the NN-XIb-PLA2. Further, the inhibition was irreversible as evident from binding studies. The in vitro inhibition is well correlated with in situ and in vivo edema inhibiting activities of M. indica. As the inhibition is independent of substrate and calcium and was irreversible, it can be concluded that M. indica extract mode of inhibition could be due to direct interaction of components present in the extract with the PLA2 enzyme. The aqueous extract of M. indica effectively inhibits svPLA2 enzymatic and its associated toxic activities, which substantiate their anti-snake venom properties. Further in-depth studies on the role and mechanism of the principal constituents present in the extract, responsible for the anti-PLA2 activity will be interesting to develop them into potent antisnake component and also as an anti-inflammatory agent.

  17. The capacity of Java turmeric extract as anti Sreptococcus mutans in inhibiting enamel demineralization (In vitro

    Directory of Open Access Journals (Sweden)

    Handoko Tirta

    2016-06-01

    Full Text Available Xanthorrhizol isolated from Java turmeric is able to maintain the pH of biofilm model in vitro for 4 hours. It was known that MBC of Java turmeric extract was 25%. The purpose of this study is to analyse the effect of 25% Java turmeric extract on email demineralization exposed to Streptococcus mutans (S. mutans biofilm. Biofilm model was obtained by culturizing S. mutans which was cultured on TYS Broth during 24 hours on 6 well-plates which was layered by pellicle. Java turmeric extract was added to biofilm model at various duration between 1-48 hours. The degree of acidity (pH measurement using pH universal indicator. Biofilm model was also cultured at tooth sample surface. Java turmeric extract was added at 16-20 hours. Microhardness test was conducted using Knoop indenter before and after the intervention. After 4 hours, the pH of biofilm model which was exposed to Java turmeric 25% was not decreasing. No difference was found on the enamel microhardness between experiment and control groups. Java turmeric 25% is able to prevent reduction of biofilm pH, but does not have effect on enamel demineralization.

  18. Inhibition of melanosis formation in Pacific white shrimp by the extract of lead (Leucaena leucocephala) seed.

    Science.gov (United States)

    Nirmal, Nilesh Prakash; Benjakul, Soottawat

    2011-09-15

    Lead (Leucaena leucocephala) seed extract was prepared using distilled water as a medium. An extraction yield of 26.16g/100g of seed was obtained after extraction at room temperature for 12h. Total phenolic and mimosine contents in the lead seed extract powder (LSEP) were 17.4g GAE/100g and 8.8g/100g, respectively. LSEP at different concentrations (0.05%, 0.1%, 0.25%, 0.5%, and 1%, w/v) showed inhibitory activity towards polyphenoloxidase (PPO) of Pacific white shrimp in a dose dependent manner. When the whole Pacific white shrimp were treated with 0.25% and 0.5% (w/v) LSEP, the shrimp treated with 0.5% LSEP had the lower melanosis score throughout the storage of 12days and showed a higher score for colour and odour, as well as overall likeness, compared with the control (without treatment) and 1.25% sodium metabisulphite treated samples at day 12 (P<0.05). Meat of shrimps treated with LSEP at both levels had the increase in mimosine content up to 8days, suggesting the migration of mimosine into shrimp muscle during extended storage. Therefore, 0.5% LSEP can be used as a novel melanosis inhibitor for Pacific white shrimp.

  19. Estimates of Soil Bacterial Ribosome Content and Diversity Are Significantly Affected by the Nucleic Acid Extraction Method Employed.

    Science.gov (United States)

    Wüst, Pia K; Nacke, Heiko; Kaiser, Kristin; Marhan, Sven; Sikorski, Johannes; Kandeler, Ellen; Daniel, Rolf; Overmann, Jörg

    2016-05-01

    Modern sequencing technologies allow high-resolution analyses of total and potentially active soil microbial communities based on their DNA and RNA, respectively. In the present study, quantitative PCR and 454 pyrosequencing were used to evaluate the effects of different extraction methods on the abundance and diversity of 16S rRNA genes and transcripts recovered from three different types of soils (leptosol, stagnosol, and gleysol). The quality and yield of nucleic acids varied considerably with respect to both the applied extraction method and the analyzed type of soil. The bacterial ribosome content (calculated as the ratio of 16S rRNA transcripts to 16S rRNA genes) can serve as an indicator of the potential activity of bacterial cells and differed by 2 orders of magnitude between nucleic acid extracts obtained by the various extraction methods. Depending on the extraction method, the relative abundances of dominant soil taxa, in particular Actino bacteria and Proteobacteria, varied by a factor of up to 10. Through this systematic approach, the present study allows guidelines to be deduced for the selection of the appropriate extraction protocol according to the specific soil properties, the nucleic acid of interest, and the target organisms. Copyright © 2016, American Society for Microbiology. All Rights Reserved.

  20. Estimates of Soil Bacterial Ribosome Content and Diversity Are Significantly Affected by the Nucleic Acid Extraction Method Employed

    Science.gov (United States)

    Wüst, Pia K.; Nacke, Heiko; Kaiser, Kristin; Marhan, Sven; Sikorski, Johannes; Kandeler, Ellen; Daniel, Rolf

    2016-01-01

    Modern sequencing technologies allow high-resolution analyses of total and potentially active soil microbial communities based on their DNA and RNA, respectively. In the present study, quantitative PCR and 454 pyrosequencing were used to evaluate the effects of different extraction methods on the abundance and diversity of 16S rRNA genes and transcripts recovered from three different types of soils (leptosol, stagnosol, and gleysol). The quality and yield of nucleic acids varied considerably with respect to both the applied extraction method and the analyzed type of soil. The bacterial ribosome content (calculated as the ratio of 16S rRNA transcripts to 16S rRNA genes) can serve as an indicator of the potential activity of bacterial cells and differed by 2 orders of magnitude between nucleic acid extracts obtained by the various extraction methods. Depending on the extraction method, the relative abundances of dominant soil taxa, in particular Actinobacteria and Proteobacteria, varied by a factor of up to 10. Through this systematic approach, the present study allows guidelines to be deduced for the selection of the appropriate extraction protocol according to the specific soil properties, the nucleic acid of interest, and the target organisms. PMID:26896137

  1. Aqueous extract of Rosmarinus officinalis L. inhibits neutrophil influx and cytokine secretion.

    Science.gov (United States)

    Silva, Ana Mara de Oliveira E; Machado, Isabel Daufenback; Santin, José Roberto; de Melo, Illana Louise Pereira; Pedrosa, Gabriela Vieira; Genovese, Maria Ines; Farsky, Sandra Helena Poliselli; Mancini-Filho, Jorge

    2015-01-01

    Rosmarinus officinalis L. phenolic compounds have attracted considerable attention because of their antioxidant and antimicrobial properties, including its ability to treat inflammatory disorders. In this work, we investigated the in vivo and in vitro effects of R. officinalis aqueous extract on neutrophil trafficking from the blood into an inflamed tissue, on cell-derived secretion of chemical mediators, and on oxidative stress. Anti-inflammatory activity was investigated using carrageenan-induced inflammation in the subcutaneous tissue of male Wistar rats orally treated with the R. officinalis extract (100, 200, or 400 mg/kg). The leukocyte influx (optical microscopy), secretion of chemical mediators (prostaglandin E2 (PGE2), TNF-α, interleukin 6 (IL-6), leukotriene B4 (LTB4), and cytokine-induced neutrophil chemoattractant 1 by enzyme-linked immunosorbent assay), and the anti-oxidative profile (super oxide dismutase (SOD), glutathione peroxidase, and thiobarbituric acid reactive substance (TBARS) spectrophotometry) were quantified in the inflamed exudate. N-Formyl-methionine-leucine-phenylalanine-induced chemotaxis, lipopolysaccharide-induced NO2 (-) production (Greiss reaction), and adhesion molecule expression (flow cytometry) were in vitro quantified using oyster glycogen recruited peritoneal neutrophils previous treated with the extract (1, 10, or 100 µg/mL). Animals orally treated with phosphate-buffered saline and neutrophils incubated with Hank's balanced salt solution were used as control. R. officinalis extract oral treatment caused a dose-dependent reduction in the neutrophil migration as well as decreased SOD, TBARS, LTB4, PGE2, IL-6, and TNF-α levels in the inflamed exudate. In vitro treatment with R. officinalis decreased neutrophil chemotaxis, NO2 (-) production, and shedding of L-selectin and β2 integrin expressions. Results here presented show that R. officinalis aqueous extract displays important in vivo and in vitro anti

  2. In Vitro and In Vivo Antimalarial Activity Assays of Seeds from Balanites aegyptiaca: Compounds of the Extract Show Growth Inhibition and Activity against Plasmodial Aminopeptidase

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    Peter Kusch

    2011-01-01

    Full Text Available Balanites aegyptiaca (Balanitaceae is a widely grown desert plant with multiuse potential. In the present paper, a crude extract from B. aegyptiaca seeds equivalent to a ratio of 1 : 2000 seeds to the extract was screened for antiplasmodial activity. The determined IC50 value for the chloroquine-susceptible Plasmodium falciparum NF54 strain was 68.26 g/L±3.5. Analysis of the extract by gas chromatography-mass spectrometry detected 6-phenyl-2(H-1,2,4-triazin-5-one oxime, an inhibitor of the parasitic M18 Aspartyl Aminopeptidase as one of the compounds which is responsible for the in vitro antiplasmodial activity. The crude plant extract had a of 2.35 g/L and showed a dose-dependent response. After depletion of the compound, a significantly lower inhibition was determined with a of 4.8 g/L. Moreover, two phenolic compounds, that is, 2,6-di-tert-butyl-phenol and 2,4-di-tert-butyl-phenol, with determined IC50 values of 50.29 M±3 and 47.82 M±2.5, respectively, were detected. These compounds may contribute to the in vitro antimalarial activity due to their antioxidative properties. In an in vivo experiment, treatment of BALB/c mice with the aqueous Balanite extract did not lead to eradication of the parasites, although a reduced parasitemia at day 12 p.i. was observed.

  3. Artocarpus altilis (Parkinson) Fosberg Extracts and Geranyl Dihydrochalcone Inhibit STAT3 Activity in Prostate Cancer DU145 Cells.

    Science.gov (United States)

    Jeon, Yoon Jung; Jung, Seung-Nam; Chang, Hyeyoun; Yun, Jieun; Lee, Chang Woo; Lee, Joonku; Choi, Sangho; Nash, Oyekanmi; Han, Dong Cho; Kwon, Byoung-Mog

    2015-05-01

    Artocarpus altilis (Parkinson) Fosberg has traditionally been used in Indonesia for the treatment of liver cirrhosis, hyperte