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.

Corrosion Inhibition of Aluminium in Acid Media By Citrullus Colocynthis Extract

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Rajkiran Chauhan

2011-01-01

Full Text Available Inhibition of corrosion of aluminium in acid solution by methanol extract of Citrullus colocynthis plant has been studied using mass loss and thermometric measurements. It has been found that the plant extract act as a good corrosion inhibitor for aluminium in all concentrations of sulphuric and hydrochloric acid solution. The inhibition action depends on the concentration of acid and inhibitor. Results for mass loss and thermometric measurement indicate that inhibition efficiency increase with increasing inhibitor concentration. The inhibition action of the plant extract is discussed in view of Langmuir adsorption isotherm. It has been observed that the adsorption of the extract on aluminium surface is a spontaneous process. The plant extract provides a good protection to aluminium against corrosion.

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.

Inhibition of MAO by fractions and constituents of hypericum extract.

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Bladt, S; Wagner, H

1994-10-01

The inhibition of monoamine oxidase (MAO) by six fractions from hypericum extract and three characteristic constituents (as pure substances) were analyzed in vitro and ex vivo to study the antidepressive mechanism of action. Rat brain homogenates were used as the in vitro model, while the ex vivo analysis was performed after intraperitoneal application of the test substances to albino rats. Massive inhibition of MAO-A could be shown with the total extract and all fractions only at the concentration of 10(-3) mol/L. At 10(-4) mol/L, one fraction rich in flavonoides showed an inhibition of 39%, and all other fractions demonstrated less than 25% inhibition. Using pure hypericin as well as in all ex vivo experiments, no relevant inhibiting effects could be shown. From the results it can be concluded that the clinically proven antidepressive effect of hypericum extract cannot be explained in terms of MAO inhibition.

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.

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.

Peptide Extracts from Cultures of Certain Lactobacilli Inhibit Helicobacter pylori.

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De Vuyst, Luc; Vincent, Pascal; Makras, Eleftherios; Leroy, Frédéric; Pot, Bruno

2010-03-01

Helicobacter pylori inhibition by probiotic lactobacilli has been observed in vitro and in vivo. Carefully selected probiotic Lactobacillus strains could therefore play an important role in the treatment of H. pylori infection and eradication. However, the underlying mechanism for this inhibition is not clear. The aim of this study was to examine if peptide extracts, containing bacteriocins or other antibacterial peptides, from six Lactobacillus cultures (Lactobacillus acidophilus La1, Lactobacillus amylovorus DCE 471, Lactobacillus casei YIT 9029, Lactobacillus gasseri K7, Lactobacillus johnsonii La1, and Lactobacillus rhamnosus GG) contribute to the inhibition of H. pylori. Peptide extracts from cultures of Lact. amylovorus DCE 471 and Lact. johnsonii La1 were most active, reducing the viability of H. pylori ATCC 43504 with more than 2 log units within 4 h of incubation (P < 0.001). The four other extracts were less or not active. When six clinical isolates of H. pylori were tested for their susceptibility towards five inhibitory peptide extracts, similar observations were made. Again, the peptide extracts from Lact. amylovorus DCE 471 and Lact. johnsonii La1 were the most inhibitory, while the three other extracts resulted in a much lower inhibition of H. pylori. Protease-treated extracts were inactive towards H. pylori, confirming the proteinaceous nature of the inhibitory substance.

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

International Nuclear Information System (INIS)

Kwon, Ho-Keun; Lee, Sung Haeng; Park, Zee Yong; Im, Sin-Hyeog; Hwang, Ji-Sun; So, Jae-Seon; Lee, Choong-Gu; Sahoo, Anupama; Ryu, Jae-Ha; Jeon, Won Kyung; Ko, Byoung Seob; Im, Chang-Rok

2010-01-01

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. 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. 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. 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 medicine for the treatment of diverse cancers

Fern extracts potentiate fluconazole activity and inhibit morphological changes in Candida species

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Maria A. Freitas

2017-11-01

Conclusions: The extracts obtained from the fern species L. venustum and P. calomelanos dose not present significant antifungal activity. However, P. calomelanos potentiates the activity of fluconazole and both extracts inhibits the morphological changes in Candida species, indicating that they have potential pharmacological activity as modulators of fungal biology. Therefore, novel studies are required to characterize the interference of these extracts in the virulence and pathogenicity of Candida species as well as the potential of fern species to treat fungal infections.

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

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

Science.gov (United States)

2011-01-01

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 52.0% in maltose and sucrose

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.

Inhibition of urease by extracts derived from 15 Chinese medicinal herbs.

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Shi, Da-Hua; Liu, Yu-Wei; Liu, Wei-Wei; Gu, Zhi-Feng

2011-07-01

Helicobacter pylori is a major causative factor in gastritis-like disorders, and urease plays a key role in Helicobacter pylori colonizing and persisting in the mucous layer of the human stomach. In China, a variety of Chinese medicinal herbs have been prescribed to attenuate or eradicate gastritis-like disorders. However, little is known about the urease inhibition of Chinese medicinal herbs. The present study was conducted to investigate the urease inhibition activities of the ethanol and water extracts of 15 Chinese medicinal herbs. The ethanol and water extracts derived from 15 medicinal herbs, traditionally used for the treatment of gastritis-like disorders in China, were tested for urease-inhibition activity using the phenol red method. Screened at 10 µg/mL, 14 ethanol extracts and 10 water extracts showed urease inhibition. The ethanol extracts of Magnolia officinalis Rehd. et Wils. (Magnoliaceae) and Cassia obtusifolia L. (Leguminosae) possessed inhibition rates higher than 50% with IC₅₀ values of 6.5 and 12.3 µg/mL, respectively. After fractionating successively, the petroleum ether fraction of the ethanol extracts of Magnolia officinalis showed the best activity with 90.8% urease inhibition at a concentration of 10 µg/mL. The bioautography of the petroleum ether fraction indicated the existence of the urease inhibitors in the herb. The present results indicated that some Chinese medicinal herbs might treat gastritis-like disorders via the inhibition of Helicobacter pylori urease and the further possibility for discovering useful novel urease inhibitors from the Chinese medicinal herbs.

Methanol Extract of Hydroclathrus clathratus Inhibits Production of ...

African Journals Online (AJOL)

Methanol Extract of Hydroclathrus clathratus Inhibits Production of Nitric Oxide, Prostaglandin E2 and Tumor Necrosis Factor-α in Lipopolysaccharidestimulated BV2 Microglial Cells via Inhibition of NF-κB Activity. RGPT Jayasooriya, D-O Moon, YH Chol, C-H Yoon, G-Y Kim ...

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.

Inhibition and Adsorption impact of Leave Extracts of Cnidoscolus ...

African Journals Online (AJOL)

Corrosion inhibition in the presence of alokaloid and non alkaloid extracts of Cnidoscolus aconitifolius in 1M HCl was studied using the weight loss and hydrogen evolution techniques at 303, 313 and 333 K. The results obtained revealed that the inhibition efficiency decreased with increase in temperature. Inhibition ...

Inhibition of seed germination by extracts of bitter Hawkesbury watermelon containing cucurbitacin, a feeding stimulant for corn rootworm (Coleoptera: Chrysomelidae).

Science.gov (United States)

Martin, Phyllis A W; Blackburn, Michael

2003-04-01

Cucurbitacins are feeding stimulants for corn rootworm used in baits to control the adults of this insect pest. Corn rootworm larvae also feed compulsively on cucurbitacins. Cucurbitacins are reported to be gibberellin antagonists that may preclude their use as seed treatments for these soil-dwelling insects. The crude extract of a bitter Hawkesbury watermelon containing cucurbitacin E-glycoside significantly inhibited germination of watermelon, squash, and tomato seeds. Although the germination of corn seed was not significantly inhibited, root elongation was inhibited by crude extracts, but not by high-performance liquid chromatography-purified cucurbitacin E-glycoside. Therefore, the effects of the major components in the bitter watermelon extract (e.g., sugars) on seed germination and root elongation were determined. Pure sugars (glucose and fructose), at concentrations found in watermelon extract, mimicked the inhibition of seed germination and root elongation seen with the crude bitter Hawkesbury watermelon extract. Removal of these sugars may be necessary to use this extract as a bait for corn rootworm larvae as a seed or root treatment.

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

Science.gov (United States)

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).

Saw palmetto ethanol extract inhibits adipocyte differentiation.

Science.gov (United States)

Villaverde, Nicole; Galvis, Adriana; Marcano, Adriana; Priestap, Horacio A; Bennett, Bradley C; Barbieri, M Alejandro

2013-07-01

The fruits of saw palmetto have been used for the treatment of a variety of urinary and reproductive system problems. In this study we investigated whether the fruit extracts affect in vitro adipogenesis. Saw palmetto ethanol extract inhibited the lipid droplet accumulation by induction media in a dose-dependent manner, and it also attenuated the protein expressions of C-EBPα and PPARγ. Phosphorylation of Erk1/2 and Akt1 were also decreased by saw palmetto ethanol extract. This report suggests that saw palmetto extracts selectively affect the adipocyte differentiation through the modulation of several key factors that play a critical role during adipogenesis.

Ginger Extract Inhibits Biofilm Formation by Pseudomonas aeruginosa PA14

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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. PMID:24086697

Hypoglycemic effect of basil (Ocimum basilicum) aqueous extract is mediated through inhibition of α-glucosidase and α-amylase activities: an in vitro study.

Science.gov (United States)

El-Beshbishy, Ha; Bahashwan, Sa

2012-02-01

The present study investigated the in vitro hypoglycemic activity of basil (Ocimum basilicum) aqueous extract. Preliminary phytochemical screening of the extract revealed the presence of reducing sugars, cardiac glycosides, tannins, saponins, glycosides, flavonoids and steroids. The total polyphenols content (TPC), flavonoids content (FC), percentage diphenylpicrylhydrazyl (DPPH( · )) radical inhibition and total antioxidant status (TAS) were estimated. The FC was 41 ± 2.2 rutin/g dry extract, the TPC was 146 ± 5.26 mg catechin/g dry extract and the TAS was 5.12 ± 0.7 mmol/L. The %DPPH( · ) free radical inhibition was 60%, 54%, 49% and 43%, respectively, for different extract concentrations; 20, 18.2, 16.3 and 14.5 mg/ml, respectively. The extract elicited significant dose-dependent pattern against rat intestinal sucrase (RIS; IC(50) = 36.72 mg/ml), rat intestinal maltase (RIM; IC(50) = 21.31 mg/ml) and porcine pancreatic α-amylase (PPA; IC(50) = 42.50 mg/ml) inhibitory activities. The inhibition was greater against maltase compared with sucrase. These effects may be attributed to the high TPC and FC levels. The linear regression analysis revealed strong significant positive correlations between %DPPH( · ) radical inhibition and each of %RIS, %RIM and %PPA inhibiting activity. Also, strong significant positive correlations between %RIS and either %RIM or %PPA inhibition activity were observed. We concluded therefore that basil aqueous extract via antioxidant and possibly α-glucosidase and α-amylase inhibiting activities, offered positive benefits to control diabetes.

Corrosion Inhibition of Aluminium in Acid Media By Citrullus Colocynthis Extract

OpenAIRE

Chauhan, Rajkiran; Garg, Urvija; Tak, R. K.

2011-01-01

Inhibition of corrosion of aluminium in acid solution by methanol extract of Citrullus colocynthis plant has been studied using mass loss and thermometric measurements. It has been found that the plant extract act as a good corrosion inhibitor for aluminium in all concentrations of sulphuric and hydrochloric acid solution. The inhibition action depends on the concentration of acid and inhibitor. Results for mass loss and thermometric measurement indicate that inhibition efficiency increase wi...

Inhibition effect on lipid oxidation of irradiated pork by adding hawthorn flavonoid extract

International Nuclear Information System (INIS)

Wang Xiaoming; Liu Chao; Cao Lei; Li Kexi

2011-01-01

The antioxidant activity of hawthorn flavonoid extract and its inhibition effect on irradiated pork lipid oxidant were investigated. The results showed that hawthorn flavonoids had efficient scavenging effect on DPPH free radicals (DPPH ·), and the scavenging rate reached 56% while 2 ml of 0.035 mg/ml hawthorn flavonoid extract was added. Hawthorn flavonoid extract can inhibition the lipid oxidation of irradiated pork effectively and it showed a stronger inhibition ability while the hawthorn flavonoid extract were used together with Vc. It is concluded that can decrease the lipid oxidation of pork, hawthorn flavonoid extract is a remarkable natural antioxidant. (authors)

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.

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...

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.

Antimicrobial activity and acetylcholinesterase inhibition by extracts from chromatin modulated fungi

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Matheus Thomaz Nogueira Silva Lima

Full Text Available ABSTRACT Major health challenges as the increasing number of cases of infections by antibiotic multiresistant microorganisms and cases of Alzheimer's disease have led to searching new control drugs. The present study aims to verify a new way of obtaining bioactive extracts from filamentous fungi with potential antimicrobial and acetylcholinesterase inhibitory activities, using epigenetic modulation to promote the expression of genes commonly silenced. For such finality, five filamentous fungal species (Talaromyces funiculosus, Talaromyces islandicus, Talaromyces minioluteus, Talaromyces pinophilus, Penicillium janthinellum were grown or not with DNA methyltransferases inhibitors (procainamide or hydralazine and/or a histone deacetylase inhibitor (suberohydroxamic acid. Extracts from T. islandicus cultured or not with hydralazine inhibited Listeria monocytogenes growth in 57.66 ± 5.98% and 15.38 ± 1.99%, respectively. Increment in inhibition of acetylcholinesterase activity was observed for the extract from P. janthinellum grown with procainamide (100%, when compared to the control extract (39.62 ± 3.76%. Similarly, inhibition of acetylcholinesterase activity increased from 20.91 ± 3.90% (control to 92.20 ± 3.72% when the tested extract was obtained from T. pinophilus under a combination of suberohydroxamic acid and procainamide. Concluding, increases in antimicrobial activity and acetylcholinesterase inhibition were observed when fungal extracts in the presence of DNA methyltransferases and/or histone deacetylase modulators were tested.

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

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Mahadeva Nayak

2017-01-01

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.

Kaffir lime leaves extract inhibits biofilm formation by Streptococcus mutans.

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Kooltheat, Nateelak; Kamuthachad, Ludthawun; Anthapanya, Methinee; Samakchan, Natthapon; Sranujit, Rungnapa Pankla; Potup, Pachuen; Ferrante, Antonio; Usuwanthim, Kanchana

2016-04-01

Although kaffir lime has been reported to exhibit antioxidant and antileukemic activity, little is known about the antimicrobial effect of kaffir lime extract. Because Streptococcus mutans has been known to cause biofilm formation, it has been considered the most important causative pathogen of dental caries. Thus, the effective control of its effects on the oral biofilm is the key to the prevention of dental caries. The aims of the present study were to investigate the effect of kaffir lime leaves extract on biofilm formation and its antibacterial activity on S. mutans. We examined the effect of kaffir lime leaves extract on growth and biofilm formation of S. mutans. For the investigation we used a kaffir lime extract with high phenolic content. The minimum inhibitory concentration of the extract was determined by broth microdilution assay. The inhibitory effect of the test substances on biofilm formation was also investigated by biofilm formation assay and qRT-PCR of biofilm formation-associated genes. Kaffir lime leaves extract inhibits the growth of S. mutans, corresponding to the activity of an antibiotic, ampicillin. Formation of biofilm by S. mutans was also inhibited by the extract. These results were confirmed by the down-regulation of genes associated with the biofilm formation. The findings highlight the ability of kaffir lime leaves extract to inhibit S. mutans activity, which may be beneficial in the prevention of biofilm formation on dental surface, reducing dental plaque and decreasing the chance of dental carries. Copyright © 2016 Elsevier Inc. All rights reserved.

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

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

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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.

Prostaglandin E 2 (PgE 2 ) Inhibition By Crude Extracts Of Selected ...

African Journals Online (AJOL)

This study was undertaken to assess anti-inflammatory activity of crude extracts of Cassine transvaalensis Burtt-Davy, Clerodendrum uncinatum Schinz and Commiphora glandulosa Schinz using COX inhibition assay. Water extract of C. transvaalensis root bark (125mg/ml) exhibited a (90%) PGE2 inhibition in ...

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

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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

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

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2012-01-01

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 comprising

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

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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.

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

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Alshami, Issam; Alharbi, Ahmed E

2014-02-01

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. 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. 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. 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.

Phytochemical Screening, Alpha-Glucosidase Inhibition, Antibacterial and Antioxidant Potential of Ajuga bracteosa Extracts.

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Hafeez, Kokab; Andleeb, Saiqa; Ghousa, Tahseen; Mustafa, Rozina G; Naseer, Anum; Shafique, Irsa; Akhter, Kalsoom

2017-01-01

Ajuga bracteosa, a medicinal herb, is used by local community to cure a number of diseases such as inflammation, jaundice bronchial asthma, cancer and diabetes. The aim of present work was to evaluate the antioxidant potential, in vitro antidiabetic and antimicrobial effects of A. bracteosa. n-hexane, ethyl acetate, chloroform, acetone, methanol and aqueous extracts of Ajuga bracteosa roots, were prepared via maceration. Antibacterial activity was carried out by agar well diffusion method. Quantitative and qualitative phytochemical screening was done. The antioxidant activity was determined by iron (II) chelating activity, iron reducing power, DPPH, and ABTS free radical scavenging methods, Antidiabetic activity was evaluated through inhibition of α-glucosidase assay. Phytochemical analysis showed the presence of phenols, flavonoids, tannins, saponins, quinines, terpenoids, xanthoproteins, glycosides, carbohydrates, steroids, phytosterols and amino acids. DPPH and ABTS potential values were recorded as 61.92% to 88.84% and 0.11% to 38.82%, respectively. Total phenolic and total flavonoid contents were expressed as gallic acid and rutin equivalents. Total iron content was expressed as FeSO4 equivalents. Chloroform and n-hexane extracts showed significant enzyme inhibition potential with IC50 values of 29.92 μg/ml and 131.7 μg/ml respectively. Aqueous extract showed maximum inhibition of E. coli, S. typhimurium, E. amnigenus, S. pyogenes, and S. aureus, (18.0±1.0 mm, 12.5±0.7 mm, 17.0±0.0 mm, 11.0±0.0 mm and 15.3±2.0 mm mm), respectively. Similarly, n-hexane extract showed maximum inhibition of E. coli, E. amnigenus, S. aureus (11.6±1.5 mm; 11.3±1.5 mm; 13.3±0.5 mm). This study also shows that n-hexane, chloroform, ethyl acetate and aqueous extracts of A. bracteosa root possess α-glucosidase inhibitory activities and therefore it may be used as hypoglycemic agents in the management of postprandial hyperglycemia. Ajuga bracteosa root extracts may provide a

Evaluation of the inhibitive effect of some plant extracts on the acid corrosion of mild steel

International Nuclear Information System (INIS)

Oguzie, Emeka E.

2008-01-01

Corrosion inhibition of mild steel in 2 M HCl and 1 M H 2 SO 4 by extracts of selected plants was investigated using a gasometric technique at temperatures of 30 and 60 deg. C. The studied plants materials include leaf extracts Occimum viridis (OV), Telferia occidentalis (TO), Azadirachta indica (AI) and Hibiscus sabdariffa (HS) as well as extracts from the seeds of Garcinia kola (GK). The results indicate that all the extracts inhibited the corrosion process in both acid media by virtue of adsorption and inhibition efficiency improved with concentration. Synergistic effects increased the inhibition efficiency in the presence of halide additives. Inhibition mechanisms were deduced from the temperature dependence of the inhibition efficiency as well as from assessment of kinetic and activation parameters that govern the processes. Comparative analysis of the inhibitor adsorption behaviour in 2 M HCl and 1 M H 2 SO 4 as well as the effects of temperature and halide additives suggest that both protonated and molecular species could be responsible for the inhibiting action of the extracts

Evaluation of the inhibitive effect of some plant extracts on the acid corrosion of mild steel

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Oguzie, Emeka E. [Electrochemistry and Materials Science Research Laboratory, Department of Chemistry, Federal University of Technology, PMB 1526, Owerri (Nigeria)], E-mail: oguziemeka@yahoo.com

2008-11-15

Corrosion inhibition of mild steel in 2 M HCl and 1 M H{sub 2}SO{sub 4} by extracts of selected plants was investigated using a gasometric technique at temperatures of 30 and 60 deg. C. The studied plants materials include leaf extracts Occimum viridis (OV), Telferia occidentalis (TO), Azadirachta indica (AI) and Hibiscus sabdariffa (HS) as well as extracts from the seeds of Garcinia kola (GK). The results indicate that all the extracts inhibited the corrosion process in both acid media by virtue of adsorption and inhibition efficiency improved with concentration. Synergistic effects increased the inhibition efficiency in the presence of halide additives. Inhibition mechanisms were deduced from the temperature dependence of the inhibition efficiency as well as from assessment of kinetic and activation parameters that govern the processes. Comparative analysis of the inhibitor adsorption behaviour in 2 M HCl and 1 M H{sub 2}SO{sub 4} as well as the effects of temperature and halide additives suggest that both protonated and molecular species could be responsible for the inhibiting action of the extracts.

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

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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.

Luteolin-7-O-Glucoside Present in Lettuce Extracts Inhibits Hepatitis B Surface Antigen Production and Viral Replication by Human Hepatoma Cells in Vitro

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Xiao-Xian Cui

2017-12-01

Full Text Available Hepatitis B virus (HBV infection is endemic in Asia and chronic hepatitis B (CHB is a major public health issue worldwide. Current treatment strategies for CHB are not satisfactory as they induce a low rate of hepatitis B surface antigen (HBsAg loss. Extracts were prepared from lettuce hydroponically cultivated in solutions containing glycine or nitrate as nitrogen sources. The lettuce extracts exerted potent anti-HBV effects in HepG2 cell lines in vitro, including significant HBsAg inhibition, HBV replication and transcription inhibition, without exerting cytotoxic effects. When used in combination interferon-alpha 2b (IFNα-2b or lamivudine (3TC, the lettuce extracts synergistically inhibited HBsAg expression and HBV replication. By using differential metabolomics analysis, Luteolin-7-O-glucoside was identified and confirmed as a functional component of the lettuce extracts and exhibited similar anti-HBV activity as the lettuce extracts in vitro. The inhibition rate on HBsAg was up to 77.4%. Moreover, both the lettuce extracts and luteolin-7-O-glucoside functioned as organic antioxidants and, significantly attenuated HBV-induced intracellular reactive oxygen species (ROS accumulation. Luteolin-7-O-glucoside also normalized ROS-induced mitochondrial membrane potential damage, which suggests luteolin-7-O-glucoside inhibits HBsAg and HBV replication via a mechanism involving the mitochondria. Our findings suggest luteolin-7-O-glucoside may have potential value for clinical application in CHB and may enhance HBsAg and HBV clearance when used as a combination therapy.

Selected Phytochemicals and Culinary Plant Extracts Inhibit Fructose Uptake in Caco-2 Cells.

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Lee, Yurim; Lim, Yeni; Kwon, Oran

2015-09-18

This study compared the ability of nine culinary plant extracts containing a wide array of phytochemicals to inhibit fructose uptake and then explored the involvement of intestinal fructose transporters and phytochemicals for selected samples. The chemical signature was characterized by high performance liquid chromatography with mass spectrometry. Inhibition of [(14)C]-fructose uptake was tested by using human intestinal Caco-2 cells. Then, the relative contribution of the two apical-facing intestinal fructose transporters, GLUT2 and GLUT5, and the signature components for fructose uptake inhibition was confirmed in naive, phloretin-treated and forskolin-treated Caco-2 cells. HPLC/MS analysis of the chemical signature revealed that guava leaf contained quercetin and catechin, and turmeric contained curcumin, bisdemethoxycurcumin and dimethoxycurcumin. Similar inhibition of fructose uptake (by ~50%) was observed with guava leaf and turmeric in Caco-2 cells, but with a higher contribution of GLUT2 for turmeric and that of GLUT5 for guava leaf. The data suggested that, in turmeric, demethoxycurcumin specifically contributed to GLUT2-mediated fructose uptake inhibition, and curcumin did the same to GLUT5-mediated fructose uptake inhibition, but GLUT2 inhibition was more potent. By contrast, in guava leaf, catechin specifically contributed to GLUT5-mediated fructose uptake inhibition, and quercetin affected both GLUT5- and GLUT2-mediated fructose uptake inhibition, resulting in the higher contribution of GLUT5. These results suggest that demethoxycurcumin is an important contributor to GLUT2-mediated fructose uptake inhibition for turmeric extract, and catechin is the same to GLUT5-mediated fructose uptake inhibition for guava leaf extract. Quercetin, curcumin and bisdemethoxycurcumin contributed to both GLUT5- and GLUT2-mediated fructose uptake inhibition, but the contribution to GLUT5 inhibition was higher than the contribution to GLUT2 inhibition.

Diospyros kaki Extract Inhibits Alkali Burn-Induced Corneal Neovascularization.

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Yang, Sung Jae; Jo, Hyoung; Kim, Kyung-A; Ahn, Hong Ryul; Kang, Suk Woo; Jung, Sang Hoon

2016-01-01

The purpose of this study was to evaluate the effect of ethanol extract of Diospyros kaki (EEDK) leaves on corneal neovascularization (CoNV) in rats. One week after the alkali burns in the corneas, the CoNV area coverage in the CoNV-positive control group, 100 mg/kg EEDK group, and 200 mg/kg EEDK group was 43.3% ± 5.5%, 337.7% ± 2.5%, and 27.2% ± 4.3%, respectively. The areas of CoNV in the EEDK-treated groups were significantly different from those of the CoNV group. EEDK significantly attenuated the upregulation of vascular endothelial growth factor, fibroblast growth factor, interleukin-6, and matrix metalloproteinase-2 (MMP-2) protein levels. Orally administrated D. kaki inhibited CoNV development in rats.

Pouteria ramiflora extract inhibits salivary amylolytic activity and decreases glycemic level in mice

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NEIRE M. DE GOUVEIA

2013-09-01

Full Text Available In this study, extracts of plant species from the Cerrado biome were assessed in order to find potential inhibitors of human salivary alpha-amylase. The plants were collected and extracts were obtained from leaves, bark, and roots. We performed a preliminary phytochemical analysis and a screening for salivar alpha-amylase inhibitory activity. Only three botanical families (Sapotaceae, Sapindaceae and Flacourtiaceae and 16 extracts showed a substantial inhibition (>75% of alpha-amylase. The ethanolic extracts of Pouteria ramiflora obtained from stem barks and root barks decreased amylolytic activity above 95% at a final concentration of 20 µg/mL. Thus, adult male Swiss mice were treated orally with P. ramiflora in acute toxicity and glycemic control studies. Daily administration with 25, 50 and 100 mg/kg of aqueous extract of P. ramiflora for eight days can reduce significantly body weight and blood glucose level in mice. These data suggest that the crude polar extract of P. ramiflora decreases salivary amylolytic activity while lowering the blood levels of glucose.

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.

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

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Ding, Hong; Shen, Jinglian; Yang, Yang; Che, Yuqin

2015-01-01

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 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.

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

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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.

Tyrosinase inhibition and antioxidant properties of Asphodelus microcarpus extracts.

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Di Petrillo, Amalia; González-Paramás, Ana Maria; Era, Benedetta; Medda, Rosaria; Pintus, Francesca; Santos-Buelga, Celestino; Fais, Antonella

2016-11-09

Asphodelus microcarpus belongs to the family Liliaceae that include several medicinal plants. In the traditional medicine plants of the genus Asphodelus are used to treat skin disorders such as ectodermal parasites, psoriasis, microbial infection and for lightening freckles. In order to find novel skin depigmenting agents, the present work was carry out to evaluate antioxidant activity and tyrosinase inhibitory potential of leaves, flowers and tubers extracts of A. microcarpus. The phytochemical composition of the active extract was also evaluated. Three different extracts (water, methanol and ethanol) from leaves, flowers and tubers of A. microcarpus were evaluated for their inhibitory effect on tyrosinase activity using L-3,4-dihydroxyphenylalanine (L-DOPA) as substrate. Inhibition of cellular tyrosinase activity and melanin production was also investigated in melanoma B16F10 cells. Antioxidant activity, total phenolic and flavonoids contents were determined using standard in vitro methods. HPLC-DAD-MS was used to identify phenolic profile of the active extract. The results showed that all extracts have a direct inhibitory anti-tyrosinase activity, with ethanolic extract from flowers (FEE) exhibiting the stronger effect. Kinetic analysis revealed that FEE acts as an uncompetitive inhibitor with a Ki value of 0.19 mg/mL. The same effect was observed in murine melanoma B16F10 cells. Cellular tyrosinase activity as well as melanin content were reduced in FEE-treated cells. The results were comparable to that of the standard tyrosinase inhibitor (kojic acid). Furthermore, the same extract showed the highest antioxidant activity and an elevated levels of total phenolics and flavonoid content. Eleven phenolic components were identified as chlorogenic acid, luteolin derivates, naringenin and apigenin. Our findings showed that FEE from A. microcarpus inhibits tyrosinase and exerted antimelanogenesis effect in B16F10 cells. This extract also showed the highest scavenging

The plant extract Isatis tinctoria L. extract (ITE) inhibits allergen-induced airway inflammation and hyperreactivity in mice.

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Brattström, A; Schapowal, A; Kamal, M A; Maillet, I; Ryffel, B; Moser, R

2010-07-01

The herbal Isatis tinctoria extract (ITE) inhibits the inducible isoform of cyclooxygenase (COX-2) as well as lipoxygenase (5-LOX) and therefore possesses anti-inflammatory properties. The extract might also be useful in allergic airway diseases which are characterized by chronic inflammation. ITE obtained from leaves by supercritical carbon dioxide extraction was investigated in ovalbumin (OVA) immunised BALB/c mice given intranasally together with antigen challenge in the murine model of allergic airway disease (asthma) with the analysis of the inflammatory and immune parameters in the lung. ITE given with the antigen challenge inhibited in a dose related manner the allergic response. ITE diminished airway hyperresponsiveness (AHR) and eosinophil recruitment into the bronchoalveolar lavage (BAL) fluid upon allergen challenge, but had no effect in the saline control mice. Eosinophil recruitment was further assessed in the lung by eosinophil peroxidase (EPO) activity at a dose of 30 microg ITE per mouse. Microscopic investigations revealed less inflammation, eosinophil recruitment and mucus hyperproduction in the lung in a dose related manner. Diminution of AHR and inflammation was associated with reduced IL-4, IL-5, and RANTES production in the BAL fluid at the 30 microg ITE dose, while OVA specific IgE and eotaxin serum levels remained unchanged. ITE, which has been reported inhibiting COX-2 and 5-LOX, reduced allergic airway inflammation and AHR by inhibiting the production of the Th2 cytokines IL-4 and IL-5, and RANTES. (c) 2009 Elsevier GmbH. All rights reserved.

Phytochemical analysis of Binahong (Anredera Cordifolia) leaves extract to inhibit In Vitro growth of Aeromonas Hydrophila

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Basyuni, Mohammad; Ginting, Prita Yulianti Anasta Br; Lesmana, Indra

2017-11-01

Binahong (Anredera cordifolia) is one of the medicinal plants commonly used to treat the disease of living organisms. The secondary metabolite of A. cordifolia leaves has been shown antibacterial activity. This study aimed to investigate the secondary metabolite of A. cordifolia leaves showing antibacterial and analysis the effectiveness of antibacterial to inhibit the growth of bacteria Aeromonas hydrophila. A paper disc soaked in a solution of A. cordifolia leaves extract was used to test in vitro at a concentration of 0% (w/v), 0.2%, 0.4%, 0.6%, 0.8%, and positive control of antibiotic (oxytetracycline), respectively. The extracts then placed on a tryptone soy agar (TSA) medium containing bacteria A. hydrophila and incubated at 37 °C for 24 hours. In vitro test showed that A. cordifolia leaves extract inhibited the growth of bacteria A. hydrophila with an inhibition area around the paper disc. The inhibition growth of A. hydrophila increased with the increasing of extract concentration. Bacterial growth was inhibited in the diameter zone of A. hydrophila under different levels of the extracts were 0 mm (0 % negative control), 8.4 mm (0.2 %), 9.4 mm (0.4 %), 10.5 mm (0.6 %), 11.9 mm (0.8 %), 27.5 mm (positive control), respectively. Phytochemical screening of A. cordifolia leaves extract indicated that the extracts contained flavonoid, phenol, saponin, alkaloid, triterpenoid, and β-sitosterol. Our in vitro study demonstrated the inhibition growth of A. hydrophila that caused the disease of motile Aeromonas septicemia (MAS).

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

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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.

Synergistic Effect of Azadirachta Indica Extract and Iodide Ions on the Corrosion Inhibition of Aluminium in Acid Media

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Arab, S. T.; Al- Turkustani, A. M.; Al- Dhahiri, R. H. [King Abd El- Aziz University, Jeddah (Saudi Arabia)

2008-06-15

The synergistic action caused by iodide ions on the corrosion inhibition of aluminium (Al) in 0.5 M HCl in the presence of Azadirachta Indica (AZI) plant extract has been investigated using potintiodynamic polarization and impedance techniques. It is found that AZI extract inhibits the corrosion of aluminium in 0.5 M HCl. The inhibition efficiency increases with the increase in AZI extract concentration, until 24% v/v of AZI extract, then Inh.% is decreased with father increase in AZI extract concentration. The adsorption of this extract in the studied concentration is found to obey Frewendlish adsorption isotherm. The addition of iodide ions enhances the inhibition efficiency to a considerable extent. The increase in Inh.% values in presence of fixed concentration of iodide ions indicates that AZI extract forms an insoluble complex at lower AZI extract concentrations by undergoing a joint adsorption. But at higher concentrations of AZI extract, competitive adsorption is found between iodide ions and the formed complex leading to less Inh.%. The Inh.% decreased in presence of iodide ions with AZI extract than in presence of AZI extract alone at all studied iodide concentrations. The synergism parameter S {sub θ} is defined and calculated from surface coverage values. This parameter in the case of AZI extract is found to be more than unity, indicating that the enhanced inhibition efficiency caused by the addition of iodide ions.

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

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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 IC 50 values of 18 and 87 μg, respectively. Aqueous extracts of cinnamon and mint showed strong inhibitory effects against pancreatic lipase with IC 50 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.

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.

Antibacterial activity of cinnamon ethanol extract (cinnamomum burmannii) and its application as a mouthwash to inhibit streptococcus growth

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Waty, Syahdiana; Suryanto, Dwi; Yurnaliza

2018-03-01

Cinnamon bark has been commonly used as spicy and traditional medicine. It contains several antibacterial compounds such as flavonoids, saponins, and cinnamaldehyde. Several studies have been done to know the antibacterial effect on bacteria such as Streptococcus in vitro. This study aimed to examine the antibacterial activity of cinnamon ethanol extract against Streptococcus and its application as mouthwash to inhibit the bacteria. The cinnamon bark was macerated followed by extracted in 80% ethanol. Bacterial samples were isolated from dental plaque of patients visiting dental clinic drg. Syahdiana Waty in Medan, North Sumatra. The isolates were identified using Vitek 2 compact. Secondary metabolites were detected using previously described method. Antibacterial assay was done at extract concentration of 6.25%, 12.5%, and 25%. The result showed that alkaloids, flavonoids, saponins, and glycoside were detected in the extract. Nine bacterial species were identified as Streptococcus mitis, S. sanguinis, S. salivarius, S. pluranimalium, S. pneumoniae, S. alactolyticus, Kocuria rosea, Kocuria kristinae, and Spingomonas paucimolis. It showed that the extract of Cinnamon bark significantly inhibited Streptococcus growth, and it was effective as mouthwash.

Potential of Piper betle extracts on inhibition of oral pathogens.

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Phumat, Pimpak; Khongkhunthian, Sakornrat; Wanachantararak, Phenphichar; Okonogi, Siriporn

2017-01-01

In the present study, antimicrobial activity of Piper betle crude ethanol extract against 4 strains of oral pathogens; Candida albicans DMST 8684, C. albicans DMST 5815, Streptococcus gordonii DMST 38731 and Streptococcus mutans DMST 18777 was compared with other medicinal plants. P. betle showed the strongest antimicrobial activity against all tested strains. Fractionated extracts of P. betle using hexane, ethyl acetate, and ethanol, respectively, were subjected to antimicrobial assay. The result revealed that the fractionated extract from ethyl acetate (F-EtOAc) possessed the strongest antimicrobial activity against all tested strains. Its inhibition zones against those pathogens were 23.00 ± 0.00, 24.33 ± 0.58, 12.50 ± 0.70 and 11.00 ± 0.00 mm, respectively and its minimum inhibitory concentrations were 0.50, 1.00, 0.50 and 1.00 mg/mL, respectively. Interestingly, the minimum concentration to completely kill those pathogens was the same for all strains and found to be 2.00 mg/mL. Killing kinetic study revealed that the activity of F-EtOAc was dose dependent. HPLC chromatograms of P. betle extracts were compared with its antimicrobial activity. An obvious peak at a retention time of 4.11 min was found to be a major component of F-EtOAc whereas it was a minor compound in the other extracts. This peak was considered to be an active compound of P. betle as it was consistent with the antimicrobial activity of F-EtOAc, the most potential extract against the tested pathogens. It is suggested that F-EtOAc is a promising extract of P. betle for inhibition of oral pathogens. Separation and structure elucidation of the active compound of this extract will be further investigated.

Assessment of Anti-Influenza Activity and Hemagglutination Inhibition of Plumbago indica and Allium sativum Extracts.

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Chavan, Rahul Dilip; Shinde, Pramod; Girkar, Kaustubh; Madage, Rajendra; Chowdhary, Abhay

2016-01-01

Human influenza is a seasonal disease associated with significant morbidity and mortality. Anti-flu ayurvedic/herbal medicines have played a significant role in fighting the virus pandemic. Plumbagin and allicin are commonly used ingredients in many therapeutic remedies, either alone or in conjunction with other natural substances. Evidence suggests that these extracts are associated with a variety of pharmacological activities. To evaluate anti-influenza activity from Plumbago indica and Allium sativum extract against Influenza A (H1N1)pdm09. Different extraction procedures were used to isolate the active ingredient in the solvent system, and quantitative HPLTC confirms the presence of plumbagin and allicin. The cytotoxicity was carried out on Madin-Darby Canine kidney cells, and the 50% cytotoxic concentration (CC50) values were below 20 mg/mL for both plant extracts. To assess the anti-influenza activity, two assays were employed, simultaneous and posttreatment assay. A. sativum methanolic and ethanolic extracts showed only 14% reduction in hemagglutination in contrast to P. indica which exhibited 100% reduction in both simultaneous and posttreatment assay at concentrations of 10 mg/mL, 5 mg/mL, and 1 mg/mL. Our results suggest that P. indica extracts are good candidates for anti-influenza therapy and should be used in medical treatment after further research. The search for natural antiviral compounds from plants is a promising approach in the development of new therapeutic agents. In the past century, several scientific efforts have been directed toward identifying phytochemicals capable of inhibiting virus. Knowledge of ethnopharmacology can lead to new bioactive plant compounds suitable for drug discovery and development. Macromolecular docking studies provides most detailed possible view of drug-receptor interaction where the structure of drug is designed based on its fit to three dimensional structures of receptor site rather than by analogy to other

Effect of Bawang Dayak (Eleutherine palmifolia (L) Merr) crude extract towards bacteria inhibition zone and carp (Cyprinus carpio) hematology

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Maftuch

2017-05-01

Negative impacts of antibiotics and chemical substance usage in aquaculture demand the researchers discover more efficient alternative yet environmentally friendly to overcome fish diseases. One alternative is by using Bawang Dayak (Eleutherine palmifolia (L.) Merr). This research aimed to reveal the effect of Bawang Dayak crude extract towards the inhibition zone of A. hydrophilia, V. harveyi, and P. fluorescens bacteria. Furthermore, it was also conducted to investigate the carp (C. carpio) hematology which was infected with A. hydrophila bacteria, and find the most appropriate dose of Bawang Dayak crude extract to inhibit the bacteria. This experimental research was performed by using Completely Randomized Design with 4 treatments and 3 replications. The best result of the zone of inhibition test in A. hydrophila bacteria was at the dose of 70 ppm while V. harveyi and P. Fluorescens bacteria were at the dose of 85 ppm. Then, fish hematology was found best at the dose of 80 ppm. Bawang Dayak crude extract was significant towards the inhibition zone of A. hydrophila, V. harveyi and P. Fluorescens bacteria, and carp hematology which was infected with A. hydrophila bacteria.

CORROSION INHIBITIVE PROPERTIES OF EXTRACT OF JATROPHA CURCAS LEAVES ON MILD STEEL IN HYDROCHLORIC ACID ENVIRONMENT

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J. Odusote

2016-09-01

Full Text Available Jatropha curcas leaves extract was tested as a green corrosion inhibitor for mild steel in aqueous hydrochloric acid solution using gravimetric and thermometric techniques. The results reveal that the inhibition efficiency vary with concentration of the leaf extract and the time of immersion. Maximum inhibition efficiency was found to be 95.92% in 2M HCl with 0.5 g/l concentration of the extract in gravimetric method, while 87.04% was obtained in thermometric method. The inhibiting effect was attributed to the presence of alkaloids, flavonoids, saponins, tannins and phenol in the extract. The adsorption processes of the Jatropha curcas leaves extract onto the mild steel is consistent with the assumptions of Langmuir isotherm model and also found to be spontaneous. From the results, a physical adsorption mechanism is proposed for the adsorption of Jatropha curcas leaves extract onto mild steel surface.

Inhibition of melanogenesis and antioxidant properties of Magnolia grandiflora L. flower extract

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Huang Huey-Chun

2012-06-01

Full Text Available Abstract Background Magnolia grandiflora L. flower is wildly used in Asian as a traditional herbal medication. The purpose of the study was to investigate the antimelanogenic and antioxidant properties of Magnolia grandiflora L. flower extract. In the study, the inhibitory effects of M. grandiflora L. flower extract on mushroom tyrosinase, B16F10 intracellular tyrosinase activity and melanin content were determined spectrophotometrically. Meanwhile, the antioxidative capacity of the flower extract was also investigated. Results Our results revealed that M. grandiflora L. flower extract inhibit mushroom tyrosinase activity (IC50 =11.1%; v/v, the flower extract also effectively suppressed intracellular tyrosinase activity (IC50 = 13.6%; v/v and decreased the amount of melanin (IC50 = 25.6%; v/v in a dose-dependent manner in B16F10 cells. Protein expression level of tyrosinase and tyrosinase-related protein 1 (TRP-1 were also decreased by the flower extract. Additionally, antioxidant capacities such as ABTS+ free radical scavenging activity, reducing capacity and total phenolic content of the flower extract were increased in a dose-dependent pattern. Conclusions Our results concluded that M. grandiflora L. flower extract decreased the expression of tyrosinase and TRP-1, and then inhibited melanogenesis in B16F10 cells. The flower extract also show antioxidant capacities and depleted cellular reactive oxygen species (ROS. Hence, M. grandiflora L. flower extract could be applied as a type of dermatological whitening agent in skin care products.

Murraya koenigii leaf extract inhibits proteasome activity and induces cell death in breast cancer cells.

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Noolu, Bindu; Ajumeera, Rajanna; Chauhan, Anitha; Nagalla, Balakrishna; Manchala, Raghunath; Ismail, Ayesha

2013-01-09

Inhibition of the proteolytic activity of 26S proteasome, the protein-degrading machine, is now considered a novel and promising approach for cancer therapy. Interestingly, proteasome inhibitors have been demonstrated to selectively kill cancer cells and also enhance the sensitivity of tumor cells to chemotherapeutic agents. Recently, polyphenols/flavonoids have been reported to inhibit proteasome activity. Murraya koenigii Spreng, a medicinally important herb of Indian origin, has been used for centuries in the Ayurvedic system of medicine. Here we show that Murraya koenigii leaves (curry leaves), a rich source of polyphenols, inhibit the proteolytic activity of the cancer cell proteasome, and cause cell death. Hydro-methanolic extract of curry leaves (CLE) was prepared and its total phenolic content [TPC] determined by, the Folin-Ciocalteau's method. Two human breast carcinoma cell lines: MCF-7 and MDA-MB-231 and a normal human lung fibroblast cell line, WI-38 were used for the studies. Cytotoxicity of the CLE was assessed by the MTT assay. We studied the effect of CLE on growth kinetics using colony formation assay. Growth arrest was assessed by cell cycle analysis and apoptosis by Annexin-V binding using flow cytometry. Inhibition of the endogenous 26S proteasome was studied in intact cells and cell extracts using substrates specific to 20S proteasomal enzymes. CLE decreased cell viability and altered the growth kinetics in both the breast cancer cell lines in a dose-dependent manner. It showed a significant arrest of cells in the S phase albeit in cancer cells only. Annexin V binding data suggests that cell death was via the apoptotic pathway in both the cancer cell lines. CLE treatment significantly decreased the activity of the 26S proteasome in the cancer but not normal cells. Our study suggests M. koenigii leaves to be a potent source of proteasome inhibitors that lead to cancer cell death. Therefore, identification of active component(s) from the leaf

Inhibition effect of cashew stem bark extract (Anacardium Occidentale L. on biofilm formation of Streptococcus sanguinis

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Rizni Amaliah

2012-12-01

Full Text Available Background: Biofilm is communities of microorganisms attached to solid surface and enclosed in extracellular matrix that protected microorganisms from antibacterial agents and host defense. One of bacteria might have a role in initial colonization of biofilm formation is Streptococcus sanguinis (S. sanguinis. Previous studies showed that cashew stem bark extract (Anacardium occidentale L. can inhibit the growth of Streptococcus strains. Purpose: The purpose of this study was to determine the inhibition effect of cashew (Anacardium occidentale L. stem bark ethanol extract on biofilm formation of S. sanguinis. Methods: Streptococcus sanguinis grown in Brain Heart Infusion (BHI + 2% sucrose medium by using microplate polystyrene 96 wells. The samples were divided into 3 groups, 5% polyethyleneglycol (PEG as negative control, cashew stem bark extract (concentration 3.125 mg/ml, 6.25 mg/ml, 9.375 mg/ml, and 12.5 mg/ml, and 0.12% chlorhexidine (as positive control. Biofilm was stained by 1% crystal violet. Afterwards, optical density (OD of samples were measured by microplate reader λ 595 nm. The data of biofilm formation inhibition percentage were analyzed by one way ANOVA and then continued by Least Significant Difference (LSD test. Results: The result of one way ANOVA showed that there were significant differences in inhibition of S. sanguinis biofilm formation (p<0.05. LSD test showed that concentration extract 3.125 mg/ml had significant difference with concentration 9.375 mg/ml and 12.5 mg/ml. Reciprocally, concentration 6.25 mg/ml had significant difference with concentration 9.375 mg/ml and 12.5 mg/ml. Conclusion: Cashew stem bark extract was able to inhibit biofilm formation of S. sanguinis.Latar belakang: Biofilm merupakan sekumpulan mikroorganisme yang melekat pada permukaan solid dan diselubungi oleh matriks ekstraseluler yang melindungi mikroorganisme dari bahan-bahan antibakteri dan sel-sel pertahanan tubuh. Salah satu bakteri yang

Hibiscus sabdariffa (Roselle) Extracts and Wine: Phytochemical Profile, Physicochemical Properties, and Carbohydrase Inhibition.

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Ifie, Idolo; Marshall, Lisa J; Ho, Peter; Williamson, Gary

2016-06-22

Three varieties of Hibiscus sabdariffa were analyzed for their phytochemical content and inhibitory potential on carbohydrate-digesting enzymes as a basis for selecting a variety for wine production. The dark red variety was chosen as it was highest in phenolic content and an aqueous extract partially inhibited α-glucosidase (maltase), with delphinidin 3-O-sambubioside, cyanidin 3-O-sambubioside, and 3-O-caffeoylquinic acid accounting for 65% of this activity. None of the varieties significantly inhibited α-amylase. Regarding Hibiscus sabdariffa wine, the effect of fermentation temperature (20 and 30 °C) on the physicochemical, phytochemical, and aroma composition was monitored over 40 days. The main change in phytochemical composition observed was the hydrolysis of 3-O-caffeolquinic acid and the concomitant increase of caffeic acid irrespective of fermentation temperature. Wine fermented at 20 °C was slightly more active for α-glucosidase inhibition with more fruity aromas (ethyl octanoate), but there were more flowery notes (2-phenylethanol) at 30 °C.

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

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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.

Saw palmetto extracts potently and noncompetitively inhibit human alpha1-adrenoceptors in vitro.

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Goepel, M; Hecker, U; Krege, S; Rübben, H; Michel, M C

1999-02-15

We wanted to test whether phytotherapeutic agents used in the treatment of lower urinary tract symptoms have alpha1-adrenoceptor antagonistic properties in vitro. Preparations of beta-sitosterol and extracts of stinging nettle, medicinal pumpkin, and saw palmetto were obtained from several pharmaceutical companies. They were tested for their ability to inhibit [3H]tamsulosin binding to human prostatic alpha1-adrenoceptors and [3H]prazosin binding to cloned human alpha1A- and alpha1B-adrenoceptors. Inhibition of phenylephrine-stimulated [3H]inositol phosphate formation by cloned receptors was also investigated. Up to the highest concentration which could be tested, preparations of beta-sitosterol, stinging nettle, and medicinal pumpkin were without consistent inhibitory effect in all assays. In contrast, all tested saw palmetto extracts inhibited radioligand binding to human alpha1-adrenoceptors and agonist-induced [3H]inositol phosphate formation. Saturation binding experiments in the presence of a single saw palmetto extract concentration indicated a noncompetitive antagonism. The relationship between active concentrations in vitro and recommended therapeutic doses for the saw palmetto extracts was slightly lower than that for several chemically defined alpha1-adrenoceptor antagonists. Saw palmetto extracts have alpha1-adrenoceptor-inhibitory properties. If bioavailability and other pharmacokinetic properties of these ingredients are similar to those of the chemically defined alpha1-adrenoceptor antagonists, alpha1-adrenoceptor antagonism might be involved in the therapeutic effects of these extracts in patients with lower urinary tract symptoms suggestive of benign prostatic obstruction.

[Inhibition effects of black rice pericarp extracts on cell proliferation of PC-3 cells].

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Jiang, Weiwei; Yu, Xudong; Ren, Guofeng

2013-05-01

To observe the inhibitive effects of black rice pericarp extracts on cell proliferation of human prostate cancer cell PC-3 and to explore its effecting mechanism. The black rice pericarp extract was used to treat the PC-3 cells. The inhibitory effect of black rice pericarp extract on cells proliferation of PC-3 was tested by MTT method. Cell apoptosis rates and cell cycle were measured by flow cytometric assay (FCM). Western blot was used to study the protein expression levels of p38, p-p38, JNK, p-JNK. A dose-dependent and time-dependent proliferation inhibition of black rice pericarp extract was demonstrated in PC-3. The most prominent experiment condition was inhibitory concentration with 300microg/ml and treated for 72 h. The experiment result of flow cytometry analysis demonstrates that the apoptosis rate of PC-3 cells increased along with the increasing of black rice pericarp extract concentration, and a G1-S cell cycle arrest was induced in a dose-dependent manner. After PC-3 cell was treated with black rice pericarp extract for 72 h, the expressions of p-p38, p-JNK protein increased. Black rice pericarp extract could inhibit proliferation, change the cell cycle distributions and induce apoptosis in human prostatic cancer cell PC-3. Its inhibitory effect may be through promoting activation of the JNK, p38 signaling pathway. These results suggest that black rice pericarp extract maybe has an inhibitory effect on prostatic cancer.

Components in aqueous Hibiscus rosa-sinensis flower extract inhibit in vitro melanoma cell growth

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Karina H. Goldberg

2017-01-01

Full Text Available Skin cancer is extremely common, and melanoma causes about 80% of skin cancer deaths. In fact, melanoma kills over 50 thousand people around the world each year, and these numbers are rising. Clearly, standard treatments are not effectively treating melanoma, and alternative therapies are needed to address this problem. Hibiscus tea has been noted to have medicinal properties, including anticancer effects. Extracts from Hibiscus have been shown to inhibit the growth of a variety of cancer cells. In particular, recent studies found that polyphenols extracted from Hibiscus sabdariffa by organic solvents can inhibit melanoma cell growth. However, effects of aqueous extracts from Hibiscus rosa-sinesis flowers, which are commonly used to make traditional medicinal beverages, have not been examined on melanoma cells. Here, we report that aqueous H. rosa-sinesis flower extract contains compounds that inhibit melanoma cell growth in a dose dependent manner at concentrations that did not affect the growth of nontransformed cells. In addition, these extracts contain low molecular weight growth inhibitory compounds below 3 kD in size that combine with larger compounds to more effectively inhibit melanoma cell growth. Future work should identify these compounds, and evaluate their potential to prevent and treat melanoma and other cancers.

Water extractable phytochemicals from Capsicum pubescens (tree pepper) inhibit lipid peroxidation induced by different pro-oxidant agents in brain

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Oboh, G [Biochemistry Department, Federal University of Technology, Akure, Ondo State (Nigeria); [Departamento de Quimica, Universidade Federal de Santa Maria (UFSM), Campus Universitario - Camobi, Santa Maria RS (Brazil); [Abdus Salam International Centre for Theoretical Physics, Trieste (Italy)]. E-mail: goboh2001@yahoo.com; Rocha, J B.T. [Campus Universitario - Camobi, Santa Maria RS (Brazil)

2006-03-15

Reactive oxygen species (ROS) is the cause of neurodegenerative disorders such as Lou Gehrig's disease, Parkinson's disease and Huntington's disease; one practical way to prevent and manage neurodegenerative diseases is through the eating of food rich in antioxidants (dietary means). In this study, the antioxidant and neuroprotective properties of aqueous extract of ripe and unripe Capsicum pubescens (popularly known as tree pepper) on different pro-oxidant induced lipid peroxidation in Rat's brain (in vitro) is been investigated. Aqueous extract of freshly harvested pepper was prepared, and the total phenol content, vitamin C, ferric reducing antioxidant property (FRAP) and Fe (II) chelating ability was determined. In addition, the ability of the extracts to protect the Rat's brain against some pro-oxidant FeSO{sub 4}, Sodium nitroprusside and Quinolinic acid - induced oxidative stress was also determined. The results of the study revealed that ripe Capsicum pubescens had a significantly higher (P<0.05) total phenol [ripe (113.7mg/100g), unripe (70.5mg/100g)] content and ferric reducing antioxidant property than the unripe pepper. However, there was no significant difference in the vitamin C [ripe (231.5{mu}g/g), unripe (224.4{mu}g/g)] content and Fe (II) chelating ability. Furthermore, the pepper extracts caused a significant decrease (P<0.05) in 25{mu}M Fe(II), 7{mu}M Sodium Nitroprusside and 1mM Quinolinic acid induced lipid peroxidation in the Rat's brain in a dose-dependent manner. However, the ripe pepper inhibited MDA (Malondialdehyhide) production in the Rat's brain than the unripe pepper. Conversely, both extract did not significantly inhibit Fe (II)/H{sub 2}O{sub 2} induced decomposition of deoxyribose. Therefore, ripe and unripe Capsicum pubescens would inhibit lipid peroxidation in vitro. However, the ripe potent was a more potent inhibitor of lipid peroxidation, which is probably due to its higher vitamin C and phenol content, reducing power and Fe

Effect of Rice Straw Extract and Alkali Lignin on the Corrosion Inhibition of Carbon Steel

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Rabiahtul Zulkafli; Norinsan Kamil Othman; Irman Abdul Rahman; Azman Jalar

2014-01-01

A paddy residue based corrosion inhibitor was prepared by treating finely powdered rice straw with aqueous ethanol under acid catalyst (0.01 M H 2 SO 4 ). Commercial alkali lignin was obtained from Sigma-Aldrich. Prior to the corrosion test, the extraction yield and alkali lignin was characterized via FTIR to determine the functional group. The effect of paddy residue extract and commercial alkali lignin on the corrosion inhibition of carbon steel in 1 M HCl was investigated through the weight loss method, potentiodynamic polarization technique and scanning electron microscopy (SEM). The corrosion inhibition efficiency of the extract and alkali lignin at different immersion times (3 h, 24 h and 42 h) was evaluated. The results show that the paddy waste extract exhibited lesser weight loss of carbon steel in the acidic medium in comparison to the commercial alkali lignin, suggesting that the paddy residue extract is more effective than the commercial alkali lignin in terms of its corrosion inhibition properties. The results obtained proves that the extract from paddy residue could serve as an effective inhibitor for carbon steel in acidic mediums. (author)

Extract from the fermented soybean product Natto inhibits Vibrio biofilm formation and reduces shrimp mortality from Vibrio harveyi infection.

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Yatip, Pattanan; Nitin Chandra Teja, D; Flegel, Timothy W; Soowannayan, Chumporn

2018-01-01

Many bacteria, including Vibrio pathogens of shrimp, need to colonize and/or form biofilms in hosts or the environment to cause disease. Thus, one possible control strategy for shrimp Vibriosis is biofilm inhibition. With this objective, an extract from the Japanese fermented soybean product, Natto was tested with the luminescent shrimp pathogen Vibrio harveyi (VH) for its ability to inhibit or degrade biofilm and to interfere with cell growth in broth. Natto is a traditional fermentation product of Bacillus subtilis var Natto (BSN1). Using 96 well microtiter plates coated with 0.4% chitosan, we found that biofilm formation by VH was inhibited, while growth in parallel broth cultures was not. When an extract from Natto prepared using BSN1 was mixed with feed for the whiteleg shrimp Penaeus vannamei before immersion challenge with V. harveyi at 10 6  cfu/ml, survival was significantly higher (p≤0.05) than for control shrimp given feed without these additives. Further work done to test whether d-amino acids were involved in biofilm formation as previously reported for B. subtilis, Staphylococus aureus and Pseudomonas aeruginosa gave negative results. In conclusion, we discovered that Natto extract can inhibit Vibrio biofilm formation and that it or BSN1 alone added to shrimp feed can significantly reduce shrimp mortality in immersion challenges with pathogenic VH. This shows some promise for possible application against Vibriosis in shrimp since Natto is generally regarded as safe (GRAS) for human consumption. Copyright © 2017 Elsevier Ltd. All rights reserved.

Phytochemicals Content, Antioxidant and α-Glucosidase Inhibition Activity of Bouea Macrophylla Griff Seed Extract

International Nuclear Information System (INIS)

Zainah Adam; Hazlina Ahmad Hassali; Rosniza Razali

2016-01-01

Bouea macrophylla Griff or locally known as kundang is one of the common fruit plant available in Malaysia. This plant from Anacardiaceae family is native to Southeast Asia particularly in Malaysia, Thailand and Indonesia. Medicinal values of this plant is not yet been explored. The present study was done to evaluate phytochemicals constituents in B. macrophylla seed extract qualitatively and quantitatively. Biological evaluations focusing on antioxidant and α-glucosidase inhibition were also performed. Qualitative phytochemicals screening revealed the presence of anthraquinones, terpenoids, flavanoids, tannins, alkaloids, glycosides, reducing sugar, steroids, triterpenes, phenolic, coumarine and proteins in B. macrophylla seed extract. Quantitative determination showed that B. macrophylla seed extract contains high amount of phenolic compounds (689.17±37.50 mg GAE/ g extract), but low amount of flavonoids (2.78±0.01 mg QE/ g extract), suggesting that most of the phenolics in B. macrophylla seed extract were non-flavonoids. Antioxidant assays showed that the extract possesses strong reducing power and DPPH radical scavenging activity (IC_5_0: 4.73±0.51 μg/ ml). These activities were almost comparable to that of vitamin C. α-Glucosidase inhibition study showed that the extract inhibited alpha-glucosidase activity potently with the IC_5_0 value of 0.55±0.04 mg/ ml, suggesting the ability of the plant to delay glucose absorption in small intestine, hence reduces hyperglycemia in diabetic condition. Potent antioxidant and α-glucosidase inhibitory activity of the extract might be attributed to the presence of high amount of phenolic compounds. In conclusion, this study showed that B. macrophylla seed extract contains various phytochemicals, possess strong antioxidant property and showed promising antidiabetic activity. These results indicate that B. macrophylla might have the potential to be developed as new pharmacological agent targeting on oxidative stress

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.

Inhibition of myeloperoxidase and antioxidative activity of Gentiana lutea extracts.

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Nastasijević, Branislav; Lazarević-Pašti, Tamara; Dimitrijević-Branković, Suzana; Pašti, Igor; Vujačić, Ana; Joksić, Gordana; Vasić, Vesna

2012-07-01

The aim of this study was to investigate the inhibitory activity of Gentiana lutea extracts on the enzyme myeloperoxidase (MPO), as well as the antioxidant activity of these extracts and their correlation with the total polyphenol content. Extracts were prepared using methanol (100%), water and ethanol aqueous solutions (96, 75, 50 and 25%v/v) as solvents for extraction. Also, isovitexin, amarogentin and gentiopicroside, pharmacologically active constituents of G. lutea were tested as potential inhibitors of MPO. Antioxidant activity of extracts was determined using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging test and also using cyclic voltammetry (CV). Among all extracts, the antioxidant capacity of 50% ethanol aqueous extract was the highest, both when measured using the DPPH test, with IC(50)=20.6 μg/ml, and when using CV. Also, 50% ethanol extract, showed the best inhibition of MPO activity in comparison with other extracts. In the group of the selected G. lutea constituents, gentiopicroside has proved to be the strongest inhibitor of MPO, with IC(50)=0.8 μg/ml. Also, the concentration of G. lutea constituents were determined in all extracts, using Ultra Performance Liquid Chromatography (UPLC). Copyright © 2012 Elsevier B.V. All rights reserved.

Potency of a novel saw palmetto ethanol extract, SPET-085, for inhibition of 5alpha-reductase II.

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Pais, Pilar

2010-08-01

The nicotinamide adenine dinucleotide phosphate (NADPH)-dependent membrane protein 5alpha-reductase irreversibly catalyses the conversion of testosterone to the most potent androgen, 5alpha-dihydrotestosterone (DHT). In humans, two 5alpha-reductase isoenyzmes are expressed: type I and type II. Type II is found primarily in prostate tissue. Saw palmetto extract (SPE) has been widely used for the treatment of lower urinary tract symptoms secondary to benign prostatic hyperplasia (BPH). The mechanisms of the pharmacological effects of SPE include the inhibition of 5alpha-reductase, among other actions. Clinical studies of SPE have been equivocal, with some showing significant results and others not. These inconsistent results may be due, in part, to varying bioactivities of the SPE used in the studies. The aim of the present study was to determine the in vitro potency of a novel saw palmetto ethanol extract (SPET-085), an inhibitor of the 5alpha-reductase isoenzyme type II, in a cell-free test system. On the basis of the enzymatic conversion of the substrate androstenedione to the 5alpha-reduced product 5alpha-androstanedione, the inhibitory potency was measured and compared to those of finasteride, an approved 5alpha-reductase inhibitor. SPET-085 concentration-dependently inhibited 5alpha-reductase type II in vitro (IC(50)=2.88+/-0.45 microg/mL). The approved 5alpha-reductase inhibitor, finasteride, tested as positive control, led to 61% inhibition of 5alpha-reductase type II. SPET-085 effectively inhibits the enzyme that has been linked to BPH, and the amount of extract required for activity is very low compared to data reported for other extracts. It can be concluded from data in the literature that SPET-085 is as effective as a hexane extract of saw palmetto that exhibited the highest levels of bioactivity, and is more effective than other SPEs tested. This study confirmed that SPET-085 has prostate health-promoting bioactivity that also corresponds favorably to

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

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Marcela Medeiros de Freitas

Full Text Available 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

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

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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

Murraya koenigii leaf extract inhibits proteasome activity and induces cell death in breast cancer cells

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Noolu Bindu

2013-01-01

Full Text Available Abstract Background Inhibition of the proteolytic activity of 26S proteasome, the protein-degrading machine, is now considered a novel and promising approach for cancer therapy. Interestingly, proteasome inhibitors have been demonstrated to selectively kill cancer cells and also enhance the sensitivity of tumor cells to chemotherapeutic agents. Recently, polyphenols/flavonoids have been reported to inhibit proteasome activity. Murraya koenigii Spreng, a medicinally important herb of Indian origin, has been used for centuries in the Ayurvedic system of medicine. Here we show that Murraya koenigii leaves (curry leaves, a rich source of polyphenols, inhibit the proteolytic activity of the cancer cell proteasome, and cause cell death. Methods Hydro-methanolic extract of curry leaves (CLE was prepared and its total phenolic content [TPC] determined by, the Folin-Ciocalteau’s method. Two human breast carcinoma cell lines: MCF-7 and MDA-MB-231 and a normal human lung fibroblast cell line, WI-38 were used for the studies. Cytotoxicity of the CLE was assessed by the MTT assay. We studied the effect of CLE on growth kinetics using colony formation assay. Growth arrest was assessed by cell cycle analysis and apoptosis by Annexin-V binding using flow cytometry. Inhibition of the endogenous 26S proteasome was studied in intact cells and cell extracts using substrates specific to 20S proteasomal enzymes. Results CLE decreased cell viability and altered the growth kinetics in both the breast cancer cell lines in a dose-dependent manner. It showed a significant arrest of cells in the S phase albeit in cancer cells only. Annexin V binding data suggests that cell death was via the apoptotic pathway in both the cancer cell lines. CLE treatment significantly decreased the activity of the 26S proteasome in the cancer but not normal cells. Conclusions Our study suggests M. koenigii leaves to be a potent source of proteasome inhibitors that lead to cancer cell death

Inhibition of hematopoietic prostaglandin D2 synthase (H-PGDS) by an alkaloid extract from Combretum molle.

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Moyo, Rejoice; Chimponda, Theresa; Mukanganyama, Stanley

2014-07-05

Hematopoietic prostaglandin D2 synthase (H-PGDS, GST Sigma) is a member of the glutathione S-transferase super family of enzymes that catalyses the conjugation of electrophilic substances with reduced glutathione. The enzyme catalyses the conversion of PGH2 to PGD2 which mediates inflammatory responses. The inhibition of H-PGDS is of importance in alleviating damage to tissues due to unwarranted synthesis of PGD2. Combretum molle has been used in African ethno medicinal practices and has been shown to reduce fever and pain. The effect of C. molle alkaloid extract on H-PGDS was thus, investigated. H-PGDS was expressed in Escherichia coli XL1-Blue cells and purified using nickel immobilized metal affinity chromatography. The effect of C. molle alkaloid extract on H-PGDS activity was determined with 1-chloro-2, 4-dinitrobenzene (CDNB) as substrate. The effect of C. molle alkaloid extract with time on H-PGDS was determined. The mechanism of inhibition was then investigated using CDNB and glutathione (GSH) as substrates. A specific activity of 24 μmol/mg/min was obtained after H-PGDS had been purified. The alkaloid extract exhibited a 70% inhibition on H-PGDS with an IC50 of 13.7 μg/ml. C. molle alkaloid extract showed an uncompetitive inhibition of H-PGDS with Ki = 41 μg/ml towards GSH, and non-competitive inhibition towards CDNB with Ki = 7.7 μg/ml and Ki' = 9.2 μg/ml. The data shows that C. molle alkaloid extract is a potent inhibitor of H-PGDS. This study thus supports the traditional use of the plant for inflammation.

Supercritical fluid extraction of grape seeds: extract chemical composition, antioxidant activity and inhibition of nitrite production in LPS-stimulated Raw 264.7 cells.

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Pérez, Concepción; Ruiz del Castillo, María Luisa; Gil, Carmen; Blanch, Gracia Patricia; Flores, Gema

2015-08-01

Grape by-products are a rich source of bioactive compounds having broad medicinal properties, but are usually wasted from juice/wine processing industries. The present study investigates the use of supercritical fluid extraction (SFE) for obtaining an extract rich in bioactive compounds. First, some variables involved in the extraction were applied. SFE conditions were selected based on the oil mass yield, fatty acid profile and total phenolic composition. As a result, 40 °C and 300 bar were selected as operational conditions. The phenolic composition of the grape seed oil was determined using LC-DAD. The antioxidant activity was determined by ABTS and DPPH assays. For the anti-inflammatory activity the inhibition of nitrite production was assessed. The grape seed oil extracted was rich in phenolic compounds and fatty acids with significant antioxidant and anti-inflammatory activities. From these results, added economic value to this agroindustrial residue is proposed using environmentally friendly techniques.

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

International Nuclear Information System (INIS)

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

1985-01-01

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. [ 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 [ 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

Inhibition by Seeds of Phalaris canariensis Extracts of Key Enzymes Linked to Obesity.

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Perez Gutierrez, Rosa Martha; Madrigales Ahuatzi, Diana; Cruz Victoria, Teresa

2016-01-01

�-glucosidase, respectively, and produced inhibition in rat intestinal sucrose. Further, the ALM extract showed significantly inhibitory effects against PL, LPL, and lipolysis of 3T3-LI adipocytes. The results provide evidence for the effects of the seeds of P canariensis for a retarded absorption of carbohydrates and lipids through the inhibition of enzymes that are related to obesity and diabetes mellitus type 2.

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

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

International Nuclear Information System (INIS)

Ito, Hitoshi; Meixu, G.

1994-01-01

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)

Combined effects of plant extracts in inhibiting the growth of Bacillus cereus in reconstituted infant rice cereal.

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Jun, Hyejung; Kim, Jinsol; Bang, Jihyun; Kim, Hoikyung; Beuchat, Larry R; Ryu, Jee-Hoon

2013-01-01

A study was done to determine the potential use of plant extracts to inhibit the growth of Bacillus cereus in reconstituted infant rice cereal. A total of 2116 extracts were screened for inhibitory activity against B. cereus using an agar well diffusion assay. The minimal inhibitory concentrations (MIC) and minimal lethal concentrations (MLC) of 14 promising extracts in tryptic soy broth (TSB) were determined. Dryopteris erythrosora (autumn fern) root extract showed the lowest MIC (0.0156 mg/ml), followed by Siegesbeckia glabrescens (Siegesbeckia herb) leaf (0.0313 mg/ml), Morus alba (white mulberry) cortex (0.0313 mg/ml), Carex pumila (sand sedge) root (0.0625 mg/ml), and Citrus paradisi (grapefruit) seed (0.0625 mg/ml) extracts. The order of MLCs of extracts was D. erythrosora root (0.0156 mg/ml)extracts against B. cereus in TSB were determined using a checkerboard assay. A combination of D. erythrosora and C. pumila extracts showed a partial synergistic inhibition, with a fractional inhibitory concentration index (FICI) of 0.75. Single and combined inhibitory activities of selected plant extracts against B. cereus in reconstituted infant rice cereal were investigated. The MICs of S. glabrescens, M. alba, D. erythrosora, and C. pumila extracts against B. cereus were 1.0, 2.0, 2.0, and 8.0mg/ml, respectively. A combination of D. erythrosora (1.00 mg/ml) and C. pumila (1.00 mg/ml) extracts showed a partial synergistic effect (FICI 0.63) in inhibiting the growth of B. cereus. Results indicate that by combining extracts, the amounts of D. erythrosora and C. pumila extracts can be reduced by 50% and 87.5%, respectively, compared with individual extracts, and give similar inhibitory activity in reconstituted infant rice cereal. Sensory evaluation showed that supplementing reconstituted infant rice cereal with plant extracts reduces sensorial quality. These observations will be useful when developing and applying interventions using natural plant extracts to inhibit B

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

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Chihiro Maki

Full Text Available 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.

Ginkgo Biloba Extract Kaempferol Inhibits Cell Proliferation and Induces Apoptosis in Pancreatic Cancer Cells

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Zhang, Yuqing; Chen, Aaron Y.; Li, Min; Chen, Changyi; Yao, Qizhi

2010-01-01

Background Kaempferol is one of the most important constituents in ginkgo flavonoids. Recent studies indicate kaempferol may have anti-tumor activities. The objective in this study was to determine the effect and mechanisms of kaempferol on pancreatic cancer cell proliferation and apoptosis. Materials and Methods Pancreatic cancer cell lines MIA PaCa-2 and Panc-1 were treated with Kampferol, and the inhibitory effects of kaempferol on pancreatic cancer cell proliferation were examined by direct cell counting, 3H-thymidine incorporation and MTS assay. Lactate dehydrogenase (LDH) release from cells was determined as an index of cytotoxicity. Apoptosis was analyzed by TUNEL assay. Results Upon the treatment with 70 μM kaempferol for 4 days, MIA PaCa-2 cell proliferation was significantly inhibited by 79% and 45.7% as determined by direct cell counting and MTS assay, respectively, compared with control cells (Pkaempferol significantly inhibited Panc-1 cell proliferation. Kaempferol treatment also significantly reduced 3H-thymidine incorporation in both MIA PaCa-2 and Panc-1 cells. Combination treatment of low concentrations of kaempferol and 5-fluorouracil (5-FU) showed an additive effect on the inhibition of MIA PaCa-2 cell proliferation. Furthermore, kaempferol had a significantly less cytotoxicity than 5-FU in normal human pancreatic ductal epithelial cells (P=0.029). In both MIA PaCa-2 and Panc-1 cells, apoptotic cell population was increased when treated with kaempferol in a concentration-dependent manner. Conclusions Ginkgo biloba extract kaempferol effectively inhibits pancreatic cancer cell proliferation and induces cancer cell apoptosis, which may sensitize pancreatic tumor cells to chemotherapy. Kaempferol may have clinical applications as adjuvant therapy in the treatment of pancreatic cancer. PMID:18570926

Therapeutic Significance of Loligo vulgaris (Lamarck, 1798) ink Extract: A Biomedical Approach

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Nadarajah, Sri Kumaran; Vijayaraj, Radha; Mani, Jayaprakashvel

2017-01-01

Background: The squid ink extract is well known for its biomedical properties. Objective: In this study, squid Loligo vulgaris was collected from Tuticorin costal water, Bay of Bengal, India. Materials and Methods: Proximate composition of the crude squid ink was studied and found to have protein as the major component over lipid and carbohydrates. Further, bioactive fractions of squid ink were extracted with ethanol, and therapeutic applications such as hemolytic, antioxidant, antimicrobial, and in vitro anti-inflammatory properties were analyzed using standard methods. Results: In hemolytic assay, the squid ink extract exhibited a maximum hemolytic activity of 128 hemolytic unit against tested erythrocytes. In DPPH assay, the ethanolic extract of squid ink has exhibited an antioxidant activity of 83.5%. The squid ink was found to be potent antibacterial agent against the pathogens tested. 200 μL of L. vulgaris ink extract showed remarkable antibacterial activity as zone of inhibition against Escherichia coli (28 mm), Klebsiella pneumoniae (22 mm), Pseudomonas aeruginosa (21 mm), and Staphylococcus aureus (24 mm). The 68.9% inhibition of protein denaturation by the squid ink extract indicated that it has very good in vitro anti-inflammatory properties. The Fourier transform infrared spectroscopy analysis of the ethanolic extracts of the squid ink indicated the presence of functional groups such as 1° and 2° amines, amides, alkynes (terminal), alkenes, aldehydes, nitriles, alkanes, aliphatic amines, carboxylic acids, and alkyl halides, which complements the biochemical background of therapeutic applications. Conclusion: Hence, results of this study concluded that the ethanolic extract of L. vulgaris has many therapeutic applications such as antimicrobial, antioxidant, and anti-inflammatory activities. SUMMARY Squid ink is very high in a number of important nutrients. It’s particularly high in antioxidants for instance, which as well all know help to protect

Inhibition of secretary PLA₂--VRV-PL-VIIIa of Russell's viper venom by standard aqueous stem bark extract of Mangifera indica L.

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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.

The efficacy of sarang semut extract (Myrmecodia pendens Merr & Perry in inhibiting Porphyromonas gingivalis biofilm formation

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Zulfan M. Alibasyah

2017-06-01

Full Text Available Background: Porphyromonas gingivalis (P. gingivalis is a pathogenic bacteria present in the oral cavity involved in the pathogenesis of chronic periodontitis and biofilm. This mass of microorganisms represents one of the virulent factors of P. gingivalis which plays an important role as an attachment initiator in host cells. Sarang semut is a natural material possessing the ability to inhibit the growth of P. gingivalis. Purpose: This study aims to analyze the effect of sarang semut extract on the formation of P. gingivalis biofilm. Methods: The study used methanol sarang semut extract and P. gingivalis ATCC 33277 and phosphomycin as a positive control. Treatment was initiated by means of culturing. Biofilm test and P. gingivalis biofilm formation observation were subsequently performed by means of a light microscope at a magnification of 400x. Results: The formation of P. gingivalis biofilms tended to increase at 3, 6, and 9 hours. Results of the violet crystal test showed that concentrations of 100% and 75% of the sarang semut extract successfully inhibited the formation of P. gingivalis biofilm according to the incubation time. Meanwhile, the sarang semut extracts at concentrations of 50%, 25%, 12.5%, and 6.125% resulted in weak inhibition of the formation of P. gingivalis biofilm. The biofilm mass profile observed by a microscope tended to decrease as an indicator of the effects of the sarang semut extract. Conclusion: Sarang semut extract can inhibit the formation of P. gingivalis biofilm, especially at concentrations of 100% and 75%. Nevertheless, phosphomycin has stronger antibiofilm of P. gingivalis effects than those of the sarang semut extract at all of the concentrations listed above.

Ethanol extracts of Cassia grandis and Tabernaemontana cymosa inhibit the in vitro replication of dengue virus serotype 2

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Carolina Hernández-Castro

2015-02-01

Full Text Available Objective: To determine the antiviral activity of ethanol extracts derived from Cassia grandis leaves and Tabernaemontana cymosa bark against two dengue virus (DENV serotype 2 strains DENV-2/NG and DENV-2/1 6681 in two cell lines susceptible to infection, VERO and U937. Methods: The cytotoxic concentration 50 (CC50 was assessed using the MTT method, and the effective concentration 50 (EC50 was determined using the technique of inhibiting the production of infectious viral particles by the plating method. Further testing of dose-response inhibition was performed, and three experimental approaches were evaluated (pre-, trans- and posttreatment to determine the effect of the extracts according to the time of administration. Finally, a preliminary phytochemical analysis for both extracts was performed. Results: The cytotoxicity of the extracts was low (CC50>300 µg/mL, and the U937 cell line was more sensitive to the antiproliferative effect of both extracts. When the virus strain-dependent selectivities of the extracts were compared, it was found that both extracts were more selective in cultures infected with the DENV-2/NG strain than in those infected with the DENV-2/16681 strain. A dose-dependent inhibitory effect of the extracts was not observed in any of the evaluations. Finally, the highest inhibition was detected with the post-treatment approach with the Tabernaemontana cymosa extract (99.9% in both cell lines. Conclusions: A therapy with compounds derived from these extracts would inhibit viral replication and affect steps after viral internalization.

Chloride channel inhibition by a red wine extract and a synthetic small molecule prevents rotaviral secretory diarrhoea in neonatal mice

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Ko, Eun-A; Jin, Byung-Ju; Namkung, Wan; Ma, Tonghui; Thiagarajah, Jay R.; Verkman, A. S.

2014-01-01

Background Rotavirus is the most common cause of severe secretory diarrhoea in infants and young children globally. The rotaviral enterotoxin, NSP4, has been proposed to stimulate calcium-activated chloride channels (CaCC) on the apical plasma membrane of intestinal epithelial cells. We previously identified red wine and small molecule CaCC inhibitors. Objective To investigate the efficacy of a red wine extract and a synthetic small molecule, CaCCinh-A01, in inhibiting intestinal CaCCs and rotaviral diarrhoea. Design Inhibition of CaCC-dependent current was measured in T84 cells and mouse ileum. The effectiveness of an orally administered wine extract and CaCCinh-A01 in inhibiting diarrhoea in vivo was determined in a neonatal mouse model of rotaviral infection. Results Screening of ~150 red wines revealed a Cabernet Sauvignon that inhibited CaCC current in T84 cells with IC50 at a ~1:200 dilution, and higher concentrations producing 100% inhibition. A >1 kdalton wine extract prepared by dialysis, which retained full inhibition activity, blocked CaCC current in T84 cells and mouse intestine. In rotavirus-inoculated mice, oral administration of the wine extract prevented diarrhoea by inhibition of intestinal fluid secretion without affecting rotaviral infection. The wine extract did not inhibit the cystic fibrosis chloride channel (CFTR) in cell cultures, nor did it prevent watery stools in neonatal mice administered cholera toxin, which activates CFTR-dependent fluid secretion. CaCCinh-A01 also inhibited rotaviral diarrhoea. Conclusions Our results support a pathogenic role for enterocyte CaCCs in rotaviral diarrhoea and demonstrate the antidiarrhoeal action of CaCC inhibition by an alcohol-free, red wine extract and by a synthetic small molecule. PMID:24052273

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.

The standard aqueous stem bark extract of Mangifera indica L. inhibits toxic PLA2 - NN-XIb-PLA2 of Indian cobra venom.

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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.

Corrosion Inhibition of Aluminium by Treculia Africana Leaves Extract in Acid Medium

OpenAIRE

Ejikeme, P.M.; Umana, S.G.; Onukwuli, O.D.

2012-01-01

The inhibitive effect of Treculia Africana leaves extract (TALE) in the corrosion of aluminium in HCl solution was studied using weight loss and thermometric methods at 30-60 °C. The results showed that TALE acted as a corrosion inhibitor of aluminium in HCl. Inhibition efficiency increased with increase in TALE concentration, but decreased with increase in temperature. TALE interaction with the metal surface was found to obey Freundlich and El-Awady adsorption isotherms. The obtained heats o...

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

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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.

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.

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, α-D-Glucose and Tannic acid)

International Nuclear Information System (INIS)

Ostovari, A.; Hoseinieh, S.M.; Peikari, M.; Shadizadeh, S.R.; Hashemi, S.J.

2009-01-01

The inhibitive action of henna extract (Lawsonia inermis) and its main constituents (lawsone, gallic acid, α-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 > α-D-Glucose > tannic acid. Also, inhibition mechanism and thermodynamic parameters are discussed.

Leaf Extracts of Mangifera indica L. Inhibit Quorum Sensing – Regulated Production of Virulence Factors and Biofilm in Test Bacteria

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Iqbal Ahmad

2017-04-01

Full Text Available Quorum sensing (QS is a global gene regulatory mechanism in bacteria for various traits including virulence factors. Disabling QS system with anti-infective agent is considered as a potential strategy to prevent bacterial infection. Mangifera indica L. (mango has been shown to possess various biological activities including anti-QS. This study investigates the efficacy of leaf extracts on QS-regulated virulence factors and biofilm formation in Gram negative pathogens. Mango leaf (ML extract was tested for QS inhibition and QS-regulated virulence factors using various indicator strains. It was further correlated with the biofilm inhibition and confirmed by electron microscopy. Phytochemical analysis was carried out using ultra performance liquid chromatography (UPLC and gas chromatography–mass spectrometry (GC-MS analysis. In vitro evaluation of anti-QS activity of ML extracts against Chromobacterium violaceum revealed promising dose-dependent interference in violacein production, by methanol extract. QS inhibitory activity is also demonstrated by reduction in elastase (76%, total protease (56%, pyocyanin (89%, chitinase (55%, exopolysaccharide production (58% and swarming motility (74% in Pseudomonas aeruginosa PAO1 at 800 μg/ml concentration. Biofilm formation by P. aeruginosa PAO1 and Aeromonas hydrophila WAF38 was reduced considerably (36–82% over control. The inhibition of biofilm was also observed by scanning electron microscopy. Moreover, ML extracts significantly reduced mortality of Caenorhabditis elegans pre-infected with PAO1 at the tested concentration. Phytochemical analysis of active extracts revealed very high content of phenolics in methanol extract and a total of 14 compounds were detected by GC-MS and UPLC. These findings suggest that phytochemicals from the ML could provide bioactive anti-infective and needs further investigation to isolate and uncover their therapeutic efficacy.

Leaf Extracts of Mangifera indica L. Inhibit Quorum Sensing – Regulated Production of Virulence Factors and Biofilm in Test Bacteria

Science.gov (United States)

Husain, Fohad M.; Ahmad, Iqbal; Al-thubiani, Abdullah S.; Abulreesh, Hussein H.; AlHazza, Ibrahim M.; Aqil, Farrukh

2017-01-01

Quorum sensing (QS) is a global gene regulatory mechanism in bacteria for various traits including virulence factors. Disabling QS system with anti-infective agent is considered as a potential strategy to prevent bacterial infection. Mangifera indica L. (mango) has been shown to possess various biological activities including anti-QS. This study investigates the efficacy of leaf extracts on QS-regulated virulence factors and biofilm formation in Gram negative pathogens. Mango leaf (ML) extract was tested for QS inhibition and QS-regulated virulence factors using various indicator strains. It was further correlated with the biofilm inhibition and confirmed by electron microscopy. Phytochemical analysis was carried out using ultra performance liquid chromatography (UPLC) and gas chromatography–mass spectrometry (GC-MS) analysis. In vitro evaluation of anti-QS activity of ML extracts against Chromobacterium violaceum revealed promising dose-dependent interference in violacein production, by methanol extract. QS inhibitory activity is also demonstrated by reduction in elastase (76%), total protease (56%), pyocyanin (89%), chitinase (55%), exopolysaccharide production (58%) and swarming motility (74%) in Pseudomonas aeruginosa PAO1 at 800 μg/ml concentration. Biofilm formation by P. aeruginosa PAO1 and Aeromonas hydrophila WAF38 was reduced considerably (36–82%) over control. The inhibition of biofilm was also observed by scanning electron microscopy. Moreover, ML extracts significantly reduced mortality of Caenorhabditis elegans pre-infected with PAO1 at the tested concentration. Phytochemical analysis of active extracts revealed very high content of phenolics in methanol extract and a total of 14 compounds were detected by GC-MS and UPLC. These findings suggest that phytochemicals from the ML could provide bioactive anti-infective and needs further investigation to isolate and uncover their therapeutic efficacy. PMID:28484444

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

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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.

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

International Nuclear Information System (INIS)

Ramde, Tambi; Rossi, Stefano; Zanella, Caterina

2014-01-01

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.

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.

Flavonoids-Rich Orthosiphon stamineus Extract as New Candidate for Angiotensin I-Converting Enzyme Inhibition: A Molecular Docking Study

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Armaghan Shafaei

2016-11-01

Full Text Available This study aims to evaluate the in vitro angiotensin-converting enzyme (ACE inhibition activity of different extracts of Orthosiphon stamineus (OS leaves and their main flavonoids, namely rosmarinic acid (RA, sinensetin (SIN, eupatorin (EUP and 3′-hydroxy-5,6,7,4′-tetramethoxyflavone (TMF. Furthermore, to identify possible mechanisms of action based on structure–activity relationships and molecular docking. The in vitro ACE inhibition activity relied on determining hippuric acid (HA formation from ACE-specific substrate (hippuryl-histidyl-leucine (HHL by the action of ACE enzyme. A High Performance Liquid Chromatography method combined with UV detection was developed and validated for measurement the concentration of produced HA. The chelation ability of OS extract and its reference compounds was evaluated by tetramethylmurexide reagent. Furthermore, molecular docking study was performed by LeadIT-FlexX: BioSolveIT’s LeadIT program. OS ethanolic extract (OS-E exhibited highest inhibition and lowest IC50 value (45.77 ± 1.17 µg/mL against ACE compared to the other extracts. Among the tested reference compounds, EUP with IC50 15.35 ± 4.49 µg/mL had highest inhibition against ACE and binding ability with Zn (II (56.03% ± 1.26% compared to RA, TMF and SIN. Molecular docking studies also confirmed that flavonoids inhibit ACE via interaction with the zinc ion and this interaction is stabilized by other interactions with amino acids in the active site. In this study, we have demonstrated that changes in flavonoids active core affect their capacity to inhibit ACE. Moreover, we showed that ACE inhibition activity of flavonoids compounds is directly related to their ability to bind with zinc ion in the active site of ACE enzyme. It was also revealed that OS extract contained high amount of flavonoids other than RA, TMF, SIN and EUP. As such, application of OS extract is useful as inhibitors of ACE.

Flavonoids-Rich Orthosiphon stamineus Extract as New Candidate for Angiotensin I-Converting Enzyme Inhibition: A Molecular Docking Study.

Science.gov (United States)

Shafaei, Armaghan; Sultan Khan, Md Shamsuddin; F A Aisha, Abdalrahim; Abdul Majid, Amin Malik Shah; Hamdan, Mohammad Razak; Mordi, Mohd Nizam; Ismail, Zhari

2016-11-09

This study aims to evaluate the in vitro angiotensin-converting enzyme (ACE) inhibition activity of different extracts of Orthosiphon stamineus (OS) leaves and their main flavonoids, namely rosmarinic acid (RA), sinensetin (SIN), eupatorin (EUP) and 3'-hydroxy-5,6,7,4'-tetramethoxyflavone (TMF). Furthermore, to identify possible mechanisms of action based on structure-activity relationships and molecular docking. The in vitro ACE inhibition activity relied on determining hippuric acid (HA) formation from ACE-specific substrate (hippuryl-histidyl-leucine (HHL)) by the action of ACE enzyme. A High Performance Liquid Chromatography method combined with UV detection was developed and validated for measurement the concentration of produced HA. The chelation ability of OS extract and its reference compounds was evaluated by tetramethylmurexide reagent. Furthermore, molecular docking study was performed by LeadIT-FlexX : BioSolveIT's LeadIT program. OS ethanolic extract (OS-E) exhibited highest inhibition and lowest IC 50 value (45.77 ± 1.17 µg/mL) against ACE compared to the other extracts. Among the tested reference compounds, EUP with IC 50 15.35 ± 4.49 µg/mL had highest inhibition against ACE and binding ability with Zn (II) (56.03% ± 1.26%) compared to RA, TMF and SIN. Molecular docking studies also confirmed that flavonoids inhibit ACE via interaction with the zinc ion and this interaction is stabilized by other interactions with amino acids in the active site. In this study, we have demonstrated that changes in flavonoids active core affect their capacity to inhibit ACE. Moreover, we showed that ACE inhibition activity of flavonoids compounds is directly related to their ability to bind with zinc ion in the active site of ACE enzyme. It was also revealed that OS extract contained high amount of flavonoids other than RA, TMF, SIN and EUP. As such, application of OS extract is useful as inhibitors of ACE.

Xanthium strumarium extract inhibits mammalian cell proliferation through mitotic spindle disruption mediated by xanthatin.

Science.gov (United States)

Sánchez-Lamar, Angel; Piloto-Ferrer, Janet; Fiore, Mario; Stano, Pasquale; Cozzi, Renata; Tofani, Daniela; Cundari, Enrico; Francisco, Marbelis; Romero, Aylema; González, Maria L; Degrassi, Francesca

2016-12-24

Xanthium strumarium L. is a member of the Asteraceae family popularly used with multiple therapeutic purposes. Whole extracts of this plant have shown anti-mitotic activity in vitro suggesting that some components could induce mitotic arrest in proliferating cells. Aim of the present work was to characterize the anti-mitotic properties of the X. strumarium whole extract and to isolate and purify active molecule(s). The capacity of the whole extract to inhibit mitotic progression in mammalian cultured cells was investigated to identify its anti-mitotic activity. Isolation of active component(s) was performed using a bioassay-guided multistep separation procedure in which whole extract was submitted to a progressive process of fractionation and fractions were challenged for their anti-mitotic activity. Our results show for the first time that X. strumarium whole extract inhibits assembly of the mitotic spindle and spindle-pole separation, thereby heavily affecting mitosis, impairing the metaphase to anaphase transition and inducing apoptosis. The purification procedure led to a fraction with an anti-mitotic activity comparable to that of the whole extract. Chemical analysis of this fraction showed that its major component was xanthatin. The present work shows a new activity of X. strumarium extract, i.e. the alteration of the mitotic apparatus in cultured cells that may be responsible for the anti-proliferative activity of the extract. Anti-mitotic activity is shown to be mainly exerted by xanthatin. Copyright © 2016 Elsevier Ireland Ltd. All rights reserved.

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.

Inhibition of Platelet Aggregation by the Leaf Extract of Carica papaya During Dengue Infection: An In Vitro Study.

Science.gov (United States)

Chinnappan, Shobia; Ramachandrappa, Vijayakumar Shettikothanuru; Tamilarasu, Kadhiravan; Krishnan, Uma Maheswari; Pillai, Agiesh Kumar Balakrishna; Rajendiran, Soundravally

2016-04-01

Dengue cases were reported to undergo platelet activation and thrombocytopenia by a poorly understood mechanism. Recent studies suggested that Carica papaya leaf extract could recover the platelet count in dengue cases. However, no studies have attempted to unravel the mechanism of the plant extract in platelet recovery. Since there are no available drugs to treat dengue and considering the significance of C. papaya in dengue treatment, the current study aimed to evaluate two research questions: First one is to study if the C. papaya leaf extract exerts its action directly on platelets and second one is to understand if the extract can specifically inhibit the platelet aggregation during dengue viral infection. Sixty subjects with dengue positive and 60 healthy subjects were recruited in the study. Platelet-rich plasma (PRP) and platelet-poor plasma were prepared from both the dengue-infected and healthy control blood samples. Effect of the leaf extract obtained from C. papaya leaves was assessed on plasma obtained as well as platelets collected from both healthy and dengue-infected individuals. Platelet aggregation was significantly reduced when leaf extract preincubated with dengue plasma was added into control PRP, whereas no change in aggregation when leaf extract incubated-control plasma was added into control PRP. Upon direct addition of C. papaya leaf extract, both dengue PRP and control PRP showed a significant reduction in platelet aggregation. Within the dengue group, PRP from severe and nonsevere cases showed a significant decrease in aggregation without any difference between them. From the study, it is evident that C. papaya leaf extract can directly act on platelet. The present study, the first of its kind, found that the leaf extract possesses a dengue-specific neutralizing effect on dengue viral-infected plasma that may exert a protective role on platelets.

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...

Rhus javanica Gall Extract Inhibits the Differentiation of Bone Marrow-Derived Osteoclasts and Ovariectomy-Induced Bone Loss

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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.

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.

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.

Inhibition of fish bacteria pathogen in tilapia using a concoction three of Borneo plant extracts

Science.gov (United States)

Hardi, EH; Saptiani, G.; Kusuma, IW; Suwinarti, W.; Sudaryono, A.

2018-04-01

This study was conducted to evaluate the antibacterial activity of concoction Solanum ferox, Boesenbergia pandurata and Zingimber zerumbetextract (SF, BP, and ZZ) to inhibit pathogenic bacteria in tilapia with the each concentrations 600 ppm BP, 900 ppm SF and 200 ppm ZZ. Antibacterial activity was measured by testing the concoction of three plants extract against single isolate Aeromonas hydrophila and Pseudomonas sp. and combined both bacteria (105 colony-forming units per milliliter). In this research, oxytetracycline was used as a control. Clear zone inhibition was observed at 6, 12, 18 and 24 hours after incubation at 30 °C. The results showed that the different concoction of BP: SF: ZZ have inhibitory zones against both single and joint isolate bacteria. The ratio of3:3:4 and 1:8:1 had higher antibacterial activity towards Pseudomonas sp. and 1:1:3 ratios both inhibit joint bacteria. The ZI% higher of concoction extracts against A.hydrophila is 1:1:8; 1:3:1; 3:4:3. The ZI% concoction extracts against Pseudomonas sp. ware 3:3:4 and 1:8:1 ratio. While the two bacteria combined, just 1:1:3 ratio had higher Z%. The conclusion is that a concoction of SF:BP:ZZ is effective to inhibit the growth of A.hydrophila and Pseudomonas sp., even its antibacterial ability is similar to the effectiveness of antibiotic oxytetracycline.

Synergisms in Alpha-glucosidase Inhibition and Antioxidant Activity of Camellia sinensis L. Kuntze and Eugenia uniflora L. Ethanolic Extracts

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Vinholes, Juliana; Vizzotto, Márcia

2017-01-01

Background: Camellia sinensis, the most consumed and popular beverages worldwide, and Eugenia uniflora, a Brazilian native species, have been already confirmed to have beneficial effects in the treatment of diabetes mellitus. However, their potential acting together against an enzyme linked to this pathology has never been exploited. Objective: The aim of this study was to evaluate the inhibitory properties of individual and combined ethanolic extracts of the leaves of C. sinensis and E. uniflora over alpha-glucosidase, a key digestive enzyme used on the Type 2 diabetes mellitus (T2DM) control. In addition, their inhibitory activity against 2,2-diphenyl-1-picrylhydrazyl radical (DPPH•) and peroxyl radicals was also assayed. Materials and Methods: Enzyme inhibition and antioxidant potential were assessed based on in vitro assays. Total phenolic compounds, carotenoids, and chlorophylls A and B were achieved using spectrophotometric methods. Results: E. uniflora was almost 40 times more active on alpha-glucosidase than C. sinensis and combined extracts showed a significant synergistic effect with an obtained IC50 value almost 5 times lower than the theoretical value. C. sinensis extract was twice more active than E. uniflora concerning DPPH•, in contrast, E. uniflora was almost 10 times more effective than C. sinensis on inhibition of peroxyl radicals with a significant synergistic effect for combined extracts. The extracts activities may be related with their phytochemicals, mainly phenolic compounds, and chlorophylls. Conclusion: Combined C. sinensis and E. uniflora ethanolic extracts showed synergistic effect against alpha-glucosidase and lipid peroxidation. These herbal combinations can be used to control postprandial hyperglycemia and can also provide antioxidant defenses to patients with T2DM. SUMMARY Alfa-glucosidase and antioxidant Interaction between Camellia sinensis L. Kuntze and Eugenia uniflora L. ethanolic extracts was investigated.Extracts showed

Synergisms in Alpha-glucosidase Inhibition and Antioxidant Activity of Camellia sinensis L. Kuntze and Eugenia uniflora L. Ethanolic Extracts.

Science.gov (United States)

Vinholes, Juliana; Vizzotto, Márcia

2017-01-01

Camellia sinensis , the most consumed and popular beverages worldwide, and Eugenia uniflora , a Brazilian native species, have been already confirmed to have beneficial effects in the treatment of diabetes mellitus. However, their potential acting together against an enzyme linked to this pathology has never been exploited. The aim of this study was to evaluate the inhibitory properties of individual and combined ethanolic extracts of the leaves of C. sinensis and E. uniflora over alpha-glucosidase, a key digestive enzyme used on the Type 2 diabetes mellitus (T2DM) control. In addition, their inhibitory activity against 2,2-diphenyl-1-picrylhydrazyl radical (DPPH • ) and peroxyl radicals was also assayed. Enzyme inhibition and antioxidant potential were assessed based on in vitro assays. Total phenolic compounds, carotenoids, and chlorophylls A and B were achieved using spectrophotometric methods. E. uniflora was almost 40 times more active on alpha-glucosidase than C. sinensis and combined extracts showed a significant synergistic effect with an obtained IC 50 value almost 5 times lower than the theoretical value. C. sinensis extract was twice more active than E. uniflora concerning DPPH • , in contrast, E. uniflora was almost 10 times more effective than C. sinensis on inhibition of peroxyl radicals with a significant synergistic effect for combined extracts. The extracts activities may be related with their phytochemicals, mainly phenolic compounds, and chlorophylls. Combined C. sinensis and E. uniflora ethanolic extracts showed synergistic effect against alpha-glucosidase and lipid peroxidation. These herbal combinations can be used to control postprandial hyperglycemia and can also provide antioxidant defenses to patients with T2DM. Alfa-glucosidase and antioxidant Interaction between Camellia sinensis L. Kuntze and Eugenia uniflora L. ethanolic extracts was investigated.Extracts showed synergistic effect over alpha-glucosidase and peroxyl radicals

Extract of Indian green mussel, Perna viridis (L.) shows inhibition of blood capillary formation in vitro

Digital Repository Service at National Institute of Oceanography (India)

Mirshahi, M.; Mirshahi, P.; Negro, S.; Soria, J.; Sreekumar, P.K.; Kotnala, S.; Therwath, A; Chatterji, A

The extract of the Indian green mussel (Perna viridis L.) was found to inhibit the formation of endothelial cell capillary tube in a concentration dependent manner in vitro. At a concentration of 5 mg/ml of crude extract, there no formation...

Evaluation of the antioxidant activity of root extract of pepper fruit (Dennetia tripetala), and it's potential for the inhibition of lipid peroxidation.

Science.gov (United States)

Okolie, Ngozi Paulinus; Falodun, Abiodun; Davids, Oluseyi

2014-01-01

The antioxidant properties of ethanolic root extract of pepper fruit (Donnetia tripetala), and its effect on lipid peroxidation of some fresh beef tissues during frozen storage were investigated. The antioxidant parameters were assessed using standard methods, while malondialdehyde levels of different fresh beef tissue sections treated with the extract prior to freezing, were estimated in a colorimetric reaction with thiobarbituric acid. The H2O2-scavenging ability of the extract was similar to that of ascorbic acid, with a maximum scavenging power of 55.61 ±4.98%, and an IC50 value of 86µg/ml. The extract exhibited a concentration-dependent ferric ion-reducing power, although this was significantly lower relative to that of the ascorbic acid (p capacity of the extract to inhibit lipid peroxidation in frozen heart muscle slices was significantly higher than that of vitamin C (p extract of D. tripetala is rich in antioxidants which can be applied to meat preservation during refrigerated storage.

THE QUORUM SENSİNG INHIBITION ACTIVITY OF THE ETHYL ACETATE EXTRACT OF STREPTOMYCES GRİSEOFLAVUS OC. 124-2

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Gultekin Akdamar

2016-05-01

Full Text Available Streptomyces griseoflavus OC. 124-2 used in this study was isolated from the field soil of Dalaman Directorate of Agricultural Enterprises Muğla. As a result of phenotypic and molecular characterization, the isolate was identified as Streptomyces griseoflavus and named as OC. 124-2. The fermentation liquid of Streptomyces griseoflavus OC. 124-2 was obtained in optimum fermentation conditions, and then it was filtered and extracted with ethyl acetate 1:1. The extract containing the active compounds was obtained by evaporating the solvent. Biomonitor strains, Chromobacterium violaceum CV026 for the determination of anti-quorum sensing activity (anti-QS, Chromobacterium violaceum CV12472 for the determination of inhibition of violacein pigment production and Pseudomonas aeruginosa PA01 for the determination of anti-swarming activity were used at MIC and sub-MIC concentrations. The anti-quorum sensing and anti-swarming activities could not be detected for the extract. Violacein production was inhibited by 100%, 74.86%, 65.74% and 31.99% at MIC, MIC/2, MIC/4 and MIC/8 concentrations of the extract treatment, respectively. While the detected inhibition of violacein pigment production did not inhibit the bacterial growth, it was revealed that it inhibited the quorum-sensing-regulated signaling systems. Accordingly, it was shown that the active compounds obtained from ethyl acetate extract of OC. 124-2 constituted a non-selective pressure for the growth of drug resistant pathogen bacteria and they may be used as an alternative at treatment of these bacteria.

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.

Huaier Extract Induces Autophagic Cell Death by Inhibiting the mTOR/S6K Pathway in Breast Cancer Cells.

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Xiaolong Wang

Full Text Available Huaier extract is attracting increased attention due to its biological activities, including antitumor, anti-parasite and immunomodulatory effects. Here, we investigated the role of autophagy in Huaier-induced cytotoxicity in MDA-MB-231, MDA-MB-468 and MCF7 breast cancer cells. Huaier treatment inhibited cell viability in all three cell lines and induced various large membranous vacuoles in the cytoplasm. In addition, electron microscopy, MDC staining, accumulated expression of autophagy markers and flow cytometry revealed that Huaier extract triggered autophagy. Inhibition of autophagy attenuated Huaier-induced cell death. Furthermore, Huaier extract inhibited the mammalian target of the rapamycin (mTOR/S6K pathway in breast cancer cells. After implanting MDA-MB-231 cells subcutaneously into the right flank of BALB/c nu/nu mice, Huaier extract induced autophagy and effectively inhibited xenograft tumor growth. This study is the first to show that Huaier-induced cytotoxicity is partially mediated through autophagic cell death in breast cancer cells through suppression of the mTOR/S6K pathway.

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.

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

International Nuclear Information System (INIS)

Kumpawat, Nutan; Chaturvedi, Alok; Upadhyay, R. K.

2012-01-01

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 B ), ocimum canum (E C ) and ocimum sanctum (E 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 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

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

International Nuclear Information System (INIS)

Subramanian, Ananth Kumar; Arumugam, Sankar; Mallaiya, Kumaravel; Subramaniam, Rameshkumar

2013-01-01

The corrosion inhibition nature of Ginger affinale extract for the corrosion of mild steel in 0.5N H 2 SO 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 2 SO 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

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. © 2013 Institute of Food Technologists®

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

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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

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

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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.

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.

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...

Inhibition of TNF-α production in LPS-activated THP-1 monocytic cells by the crude extracts of seven Bhutanese medicinal plants.

Science.gov (United States)

Wangchuk, Phurpa; Keller, Paul A; Pyne, Stephen G; Taweechotipatr, Malai

2013-07-30

Seven studied medicinal plants; Aconitum laciniatum, Ajania nubigena, Codonopsis bhutanica, Corydalis crispa, Corydalis dubia, Meconopsis simplicifolia and Pleurospermum amabile, are currently used in the Bhutanese Traditional Medicine (BTM) for the management of different types of disorders including the diseases that bore relevance to various inflammatory conditions. This study aimed to evaluate the inhibition of TNF-α production in LPS-activated THP-1 monocytic cells by the crude extracts of seven selected Bhutanese medicinal plants. It is expected to; (a) generate a scientific basis for their use in the BTM and (b) form a basis for prioritization of the seven plants for further phytochemical and anti-inflammatory studies. Seven plants were selected using an ethno-directed bio-rational approach and their crude extracts were prepared using four different solvents (methanol, hexane, dichloromethane and chloroform). The TNF-α inhibitory activity of these extracts was determined by cytokine-specific sandwich quantitative enzyme-linked immunosorbent assays (ELISAs). The results were quantified statistically and the statistical significance were evaluated by GraphPad Prism version 5.01 using Student's t-test with one-tailed distribution. A p-value ≤0.05 was considered statistically significant. Of the seven plants studied, the crude extracts of six of them inhibited the production of pro-inflammatory cytokine, TNF-α in LPS-activated THP-1 monocytic cells. Amongst the six plants, Corydalis crispa gave the best inhibitory activity followed by Pleurospermum amabile, Ajania nubigena, Corydalis dubia, Meconopsis simplicifolia and Codonopsis bhutanica. Of the 13 extracts that exhibited statistically significant TNF-α inhibitory activity (p<0.05; p<0.01), five of them showed very strong inhibition when compared to the DMSO control and RPMI media. Six medicinal plants studied here showed promising TNF-α inhibitory activity. These findings rationalize the traditional

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

between 200 to 300 mu g.ml sup(-1), whereas, the bacterial inhibition zone around the disc containing about 600-800 mu g of extract ranged between 1-5 mm. The results suggest that the crude extract of the plant is nontoxic and possesses both antibacterial...

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...

Enhanced Glucose Uptake in Human Liver Cells and Inhibition of Carbohydrate Hydrolyzing Enzymes by Nordic Berry Extracts

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Giang Thanh Thi Ho

2017-10-01

Full Text Available A Western lifestyle with low physical activity and a diet rich in sugar, fat and processed food contribute to higher incidences of diabetes and obesity. Enhanced glucose uptake in human liver cells was observed after treatment with phenolic extracts from different Nordic berries. All berry extracts showed higher inhibition against α-amylase and α-glucosidase than the anti-diabetic agent acarbose. Total phenolic content and phenolic profiles in addition to antioxidant activities, were also investigated. The berries were extracted with 80% methanol on an accelerated solvent extraction system (ASE and then purified by C-18 solid phase extraction (SPE. Among the ASE methanol extracts, black chokeberry, crowberry and elderberry extracts showed high stimulation of glucose uptake in HepG2 cells and also considerable inhibitory effect towards carbohydrate hydrolyzing enzymes. SPE extracts with higher concentrations of phenolics, resulted in increased glucose uptake and enhanced inhibition of α-amylase and α-glucosidase compared to the ASE extracts. Crowberry and cloudberry were the most potent 15-lipoxygenase inhibitors, while bog whortleberry and lingonberry were the most active xanthine oxidase inhibitors. These results increase the value of these berries as a component of a healthy Nordic diet and have a potential benefit against diabetes.

Extracts of Coreopsis tinctoria Nutt. Flower Exhibit Antidiabetic Effects via the Inhibition of α-Glucosidase Activity

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Wujie Cai

2016-01-01

Full Text Available The aim of this study was to assay the effects of Coreopsis tinctoria Nutt. flower extracts on hyperglycemia of diet-induced obese mice and the underlying mechanisms. Coreopsis tinctoria flower was extracted with ethanol and water, respectively. The total phenol, flavonoid levels, and the constituents of the extracts were measured. For the animal experiments, C57BL/6 mice were fed with a chow diet, high-fat diet, or high-fat diet mixed with 0.4% (w/w water and ethanol extracts of Coreopsis tinctoria flower for 8 weeks. The inhibitory effects of the extracts on α-glucosidase activity and the antioxidant properties were assayed in vitro. We found that the extracts blocked the increase of fasting blood glucose, serum triglyceride (TG, insulin, leptin, and liver lipid levels and prevented the development of glucose tolerance impairment and insulin resistance in the C57BL/6 mice induced by a high-fat diet. The extracts inhibited α-glycosidase activity and increased oxidant activity in vitro. In conclusion, Coreopsis tinctoria flower extracts may ameliorate high-fat diet-induced hyperglycemia and insulin resistance. The underling mechanism may be via the inhibition of α-glucosidase activity. Our data indicate that Coreopsis tinctoria flower could be used as a beverage supplement and a potential source of drugs for treatment of diabetics.

Meliae cortex extract exhibits anti-allergic activity through the inhibition of Syk kinase in mast cells

International Nuclear Information System (INIS)

Lee, Jun Ho; Ko, Na Young; Kim, Nam Wook; Mun, Se Hwan; Kim, Jie Wan; Her, Erk; Kim, Bo Kyung; Seo, Dong Wan; Chang, Hyun Wook; Moon, Tae Chul; Han, Jeung Whan; Kim, Young Mi; Choi, Wahn Soo

2007-01-01

The anti-allergic action of various Oriental medicinal herbs was investigated using in vitro and in vivo experimental models. Of these extracts, the ethanol extract of Meliae cortex (MC) exhibited the most potent activity in mast cells; its IC 50 values were 29 ± 1.5 μg/ml for antigen stimulation and 57 ± 3.4 μg/ml for thapsigargin stimulation. It inhibited compound-48/80-induced systemic anaphylaxis by 52.9% at a dose of 300 mg/kg in mice; it also inhibited the expression of the proinflammatory mediator TNF-α. With regard to its mechanism of action, MC suppressed the activating phosphorylation of Syk, a key enzyme in mast-cell signaling processes and that of Akt in a dose-dependent manner. It also inhibited the MAP kinase ERK1/2, which is critical for the production of inflammatory cytokines in mast cells, as indicated by the suppression of the activating phosphorylation of ERK1/2. Taken together, these results suggest that the anti-allergic activity of MC may be due to the inhibition of histamine secretion and cytokine expression through the Syk inhibition in mast cells

Buddleja officinalis Maximowicz extract inhibits lipid accumulation on adipocyte differentiation in 3T3-L1 cells and high-fat mice.

Science.gov (United States)

Roh, Changhyun; Park, Min-Kyoung; Shin, Hee-June; Jung, Uhee; Kim, Jin-Kyu

2012-07-23

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.

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

International Nuclear Information System (INIS)

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

2014-01-01

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 a and ΔH * 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

The inhibiting effects of Urtica dioica root extracts on experimentally induced prostatic hyperplasia in the mouse.

Science.gov (United States)

Lichius, J J; Muth, C

1997-08-01

Extracts of stinging nettle roots (Urtica dioica L. Urticaceae) are used in the treatment of benign prostatic hyperplasia (BPH). We established a BPH-model by directly implanting an urogenital sinus (UGS) into the ventral prostate gland of an adult mouse. Five differently prepared stinging nettle root extracts were tested in this model. The 20% methanolic extract was the most effective with a 51.4% inhibition of induced growth.

Inhibition of Steptococcus mutans biofilm formation by extracts of Tenacibaculum sp. 20J, a bacterium with wide-spectrum quorum quenching activity

Science.gov (United States)

Muras, Andrea; Mayer, Celia; Romero, Manuel; Camino, Tamara; Ferrer, Maria D.; Mira, Alex; Otero, Ana

2018-01-01

ABSTRACT Background: Previous studies have suggested the quorum sensing signal AI-2 as a potential target to prevent the biofilm formation by Streptococcus mutans, a pathogen involved in tooth decay. Objective: To obtain inhibition of biofilm formation by S. mutans by extracts obtained from the marine bacterium Tenacibaculum sp. 20J interfering with the AI-2 quorum sensing system. Design: The AI-2 inhibitory activity was tested with the biosensors Vibrio harveyi BB170 and JMH597. S. mutans ATCC25175 biofilm formation was monitored using impedance real-time measurements with the xCELLigence system®, confocal laser microscopy, and the crystal violet quantification method. Results: The addition of the cell extract from Tenacibaculum sp. 20J reduced biofilm formation in S. mutans ATCC25175 by 40–50% compared to the control without significantly affecting growth. A decrease of almost 40% was also observed in S. oralis DSM20627 and S. dentisani 7747 biofilms. Conclusions: The ability of Tenacibaculum sp. 20J to interfere with AI-2 and inhibit biofilm formation in S. mutans was demonstrated. The results indicate that the inhibition of quorum sensing processes may constitute a suitable strategy for inhibiting dental plaque formation, although additional experiments using mixed biofilm models would be required. PMID:29410771

Quercetogetin protects against cigarette smoke extract-induced apoptosis in epithelial cells by inhibiting mitophagy.

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Son, Eun Suk; Kim, Se-Hee; Ryter, Stefan W; Yeo, Eui-Ju; Kyung, Sun Young; Kim, Yu Jin; Jeong, Sung Hwan; Lee, Chang Soo; Park, Jeong-Woong

2018-04-01

Recent studies demonstrate that the autophagy-dependent turnover of mitochondria (mitophagy) mediates pulmonary epithelial cell death in response to cigarette smoke extract (CSE) exposure, and contributes to emphysema development in vivo during chronic cigarette smoke (CS)-exposure, although the underlying mechanisms remain unclear. Here, we investigated the role of mitophagy in regulating apoptosis in CSE-exposed human lung bronchial epithelial cells. Furthermore, we investigated the potential of the polymethoxylated flavone antioxidant quercetogetin (QUE) to inhibit CSE-induced mitophagy-dependent apoptosis. Our results demonstrate that CSE induces mitophagy in epithelial cells via mitochondrial dysfunction, and causes increased expression levels of the mitophagy-regulator protein PTEN-induced putative kinase-1 (PINK1) and the mitochondrial fission protein dynamin-1-like protein (DRP-1). CSE induced epithelial cell death and increased the expression of the apoptosis-related proteins cleaved caspase-3, -8 and -9. Caspase-3 activity was significantly increased in Beas-2B cells exposed to CSE, and decreased by siRNA-dependent knockdown of DRP-1. Treatment of epithelial cells with QUE inhibited CSE-induced mitochondrial dysfunction and mitophagy by inhibiting phospho (p)-DRP-1 and PINK1 expression. QUE suppressed mitophagy-dependent apoptosis by inhibiting the expression of cleaved caspase-3, -8 and -9 and downregulating caspase activity in human bronchial epithelial cells. These findings suggest that QUE may serve as a potential therapeutic in CS-induced pulmonary diseases. Copyright © 2018 Elsevier Ltd. All rights reserved.

INHIBITION EFFECT OF FLAVONOID EXTRACT OF Euphorbia Guyoniana ON THE CORROSION OF MILD STEEL IN H2SO4 MEDIUM

OpenAIRE

S. Chihi; N. Gherraf; B. Alabed; S. Hameurlain

2009-01-01

The influence of flavonoids extracts of three parts of Euphorbia Guyoniana towards the corrosion of type API 5L X52 steel in 15% H2SO4 has been evaluated by weight loss method and polarization technique. The results showed that extracts are a good inhibitors for API 5L X52 steel in this medium. The corrosion inhibition efficiency increases on increasing plant extracts concentration. The inhibition is attributed to the adsorption of the surface of the metal. Potentiodynamic polarization result...

Extract from Edible Red Seaweed (Gelidium amansii) Inhibits Lipid Accumulation and ROS Production during Differentiation in 3T3-L1 Cells.

Science.gov (United States)

Seo, Min-Jung; Lee, Ok-Hwan; Choi, Hyeon-Son; Lee, Boo-Yong

2012-06-01

Gelidium (G.) amansii is a red alga widely distributed in the shallow waters around East Asian countries. We investigated the effect of G. amansii on lipid accumulation and ROS (Reactive Oxygen Species) production in 3T3-L1 cells. G. amansii extracts dose-dependently inhibited lipid formation and ROS generation in cultured cells. Our results showed that anti-adipogenic effect of G. amansii was due to the reduction in mRNA expressions of PPARγ peroxisome proliferator-activated receptor-γ and aP2 (adipocyte protein 2). G. amansii extracts significantly decreased mRNA levels of a ROS-generator, NOX4 (nicotinamide adenine dinucleotide phosphate hydrogen oxidase 4), and increased the protein levels of antioxidant enzymes including SOD1/2 (superoxide dis-mutases), Gpx (glutathione peroxidase), and GR (glutathione reductase), which can lead to the reduction of ROS in the cell. In addition, the G. amansii extract enhanced mRNA levels of adiponectin, one of the adipokines secreted from adipocytes, and GLUT4, glucose uptake protein. Taken together, our study shows that G. amansii extract inhibited lipid accumulation and ROS production by controlling adipogenic signals and ROS regulating genes.

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.

Evaluation of Plants and Weeds Extract on the Corrosion Inhibition of Mild Steel in Sulphuric Acid

Directory of Open Access Journals (Sweden)

Abida Begum

2011-01-01

Full Text Available Experiments were performed in order to determine the inhibitive effects of extracts of plants and weeds namely Parthenium hysterophorus, Dathura stromonium, Azadirachta indica, Helianthus annuus leaves extract for mild steel in sulphuric acid by using weight loss and thermometric technique. Results demonstrated that, all the experimental inhibitors show an adsorption on steel surface according to Langmuir’s isotherm. The inhibition efficiency increased with increase in the concentration of all tested inhibitors to attain a maximum value at 1.0%. Free energy values for adsorption process show that the process is spontaneous. The kinetic treatment of the results shows first order kinetics.

Blackberry extract inhibits UVB-induced oxidative damage and inflammation through MAP kinases and NF-κB signaling pathways in SKH-1 mice skin

International Nuclear Information System (INIS)

Divya, Sasidharan Padmaja; Wang, Xin; Pratheeshkumar, Poyil; Son, Young-Ok; Roy, Ram Vinod; Kim, Donghern; Dai, Jin; Hitron, John Andrew; Wang, Lei; Asha, Padmaja; Shi, Xianglin; Zhang, Zhuo

2015-01-01

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 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 2 (PGE 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. • Blackberry

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. �

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.

Proanthocyanidin-rich Pinus radiata bark extract inhibits mast cell-mediated anaphylaxis-like reactions.

Science.gov (United States)

Choi, Yun Ho; Song, Chang Ho; Mun, Sung Phil

2018-02-01

Mast cells play a critical role in the effector phase of immediate hypersensitivity and allergic reactions. Pinus radiata bark extract exerts multiple biological effects and exhibits immunomodulatory and antioxidant properties. However, its role in mast cell-mediated anaphylactic reactions has not been thoroughly investigated. In this study, we examined the effects of proanthocyanidin-rich water extract (PAWE) isolated from P. radiata bark on compound 48/80-induced or antidinitrophenyl (DNP) immunoglobulin E (IgE)-mediated anaphylaxis-like reactions in vivo. In addition, we evaluated the mechanism underlying the inhibitory effect of PAWE on mast cell activation, with a specific focus on histamine release, using rat peritoneal mast cells. PAWE attenuated compound 48/80-induced or anti-DNP IgE-mediated passive cutaneous anaphylaxis-like reactions in mice, and it inhibited histamine release triggered by compound 48/80, ionophore A23187, or anti-DNP IgE in rat peritoneal mast cells in vitro. Moreover, PAWE suppressed compound 48/80-elicited calcium uptake in a concentration-dependent manner and promoted a transient increase in intracellular cyclic adenosine-3',5'-monophosphate levels. Together, these results suggest that proanthocyanidin-rich P. radiata bark extract effectively inhibits anaphylaxis-like reactions. Copyright © 2017 John Wiley & Sons, Ltd.

Green approach to corrosion inhibition of mild steel in hydrochloric acid and sulphuric acid solutions by the extract of Murraya koenigii leaves

Energy Technology Data Exchange (ETDEWEB)

Quraishi, M.A., E-mail: maquraishi@rediffmail.com [Department of Applied Chemistry, Institute of Technology, Banaras Hindu University, Varanasi 221005 (India); Singh, Ambrish; Singh, Vinod Kumar [Udai Pratap Autonomous College, Varanasi 221002 (India); Yadav, Dileep Kumar; Singh, Ashish Kumar [Department of Applied Chemistry, Institute of Technology, Banaras Hindu University, Varanasi 221005 (India)

2010-07-01

The inhibition of the corrosion of mild steel in hydrochloric acid and sulphuric acid solutions by the extract of Murraya koenigii leaves has been studied using weight loss, electrochemical impedance spectroscopy (EIS), linear polarization and potentiodynamic polarization techniques. Inhibition was found to increase with increasing concentration of the leaves extract. The effect of temperature, immersion time and acid concentration on the corrosion behavior of mild steel in 1 M HCl and 0.5 M H{sub 2}SO{sub 4} with addition of extract was also studied. The inhibition was assumed to occur via adsorption of the inhibitor molecules on the metal surface. The adsorption of the extract on the mild steel surface obeys the Langmuir adsorption isotherm. The activation energy as well as other thermodynamic parameters (Q, {Delta}H*, and {Delta}S*) for the inhibition process was calculated. These thermodynamic parameters show strong interaction between inhibitor and mild steel surface. The results obtained show that the extract of the leaves of M. koenigii could serve as an effective inhibitor of the corrosion of mild steel in hydrochloric and sulphuric acid media.

Acrolein in cigarette smoke inhibits T-cell responses.

Science.gov (United States)

Lambert, Cherie; McCue, Jesica; Portas, Mary; Ouyang, Yanli; Li, JiMei; Rosano, Thomas G; Lazis, Alexander; Freed, Brian M

2005-10-01

Cigarette smoking inhibits T-cell responses in the lungs, but the immunosuppressive compounds have not been fully identified. Cigarette smoke extracts inhibit IL-2, IFN-gamma, and TNF-alpha production in stimulated lymphocytes obtained from peripheral blood, even when the extracts were diluted 100-fold to 1000-fold. The objective of these studies was to identify the immunosuppressive compounds found in cigarette smoke. Gas chromatography/mass spectroscopy and HPLC were used to identify and quantitate volatile compounds found in cigarette smoke extracts. Bioactivity was measured by viability and production of cytokine mRNA and protein levels in treated human lymphocytes. The vapor phase of the cigarette smoke extract inhibited cytokine production, indicating that the immunosuppressive compounds were volatile. Among the volatile compounds identified in cigarette smoke extracts, only the alpha,beta-unsaturated aldehydes, acrolein (inhibitory concentration of 50% [IC50] = 3 micromol/L) and crotonaldehyde (IC50 = 6 micromol/L), exhibited significant inhibition of cytokine production. Although the levels of aldehydes varied 10-fold between high-tar (Camel) and ultralow-tar (Carlton) extracts, even ultralow-tar cigarettes produced sufficient levels of acrolein (34 micromol/L) to suppress cytokine production by >95%. We determined that the cigarette smoke extract inhibited transcription of cytokine genes. The inhibitory effects of acrolein could be blocked with the thiol compound N-acetylcysteine. The vapor phase from cigarette smoke extracts potently suppresses cytokine production. The compound responsible for this inhibition appears to be acrolein.

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. Copyright © 2016 The Authors. Published by Elsevier B.V. All rights reserved.

anti-diarrhoeal and antispasmodic effects of leaf extract

African Journals Online (AJOL)

... diphenoxylate hydrochloride (5 mg/kg). The extract also at 200 mg/kg dose level showed a significant inhibition (P<0.05) on gastrointestinal motility when compared with the vehicle (3 % Tween 80). The extract also exhibited a dose dependent inhibition on the contraction induced by acetylcholine and histamine on rabbit ...

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 (pparsley 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.

Development of extract library from indonesian biodiversity: exploration of antibacterial activity of mangrove bruguiera cylindrica leaf extracts

Science.gov (United States)

Audah, K. A.; Amsyir, J.; Almasyhur, F.; Hapsari, A. M.; Sutanto, H.

2018-03-01

Antibacterial drugs derived from natural sources play significant roles in the prevention and treatment of bacterial infections since antibiotics have become less effective against many infectious diseases. Mangroves are very potential natural antibacterial sources among great numbers of wild medicinal plants. Bruguiera cylindrica is one of the many mangroves species which spread along Indonesian coastline. The aim of this study was to explore the antibacterial activity of B. cylindrica wet and dried leaf extracts. The wet extracts study was conducted with three different solvents system (water, ethanol, and n-Hexane) against Escherichia coli and Staphylococcus aureus. While, the dried extracts study was conducted with four different solvents system (water, ethanol, chloroform and n-Hexane) against three types of bacteria, Escherichia coli, Staphylococcus epidermidis and Staphylococcus aureus. The study showed that ethanol was the best solvent for extraction of phenolic and flavonoid. Antibacterial actitivity was measured by zone of inhibition which obtained from agar-disk diffusion method. The widest area of zone of inhibition was showed by wet extracts with ethanol against S. aureus and E. coli are 14.30 and 13.30 mm, respectively. While, the zone of inhibition dried extracts with ethanol against S. aureus, S. epidermidis and E. coli are 9.32, 6.59 and 6.20 mm, respectively. In conclusion, both type of extracts showed significant antibacterial activity against gram-positive bacteria as crude extracts.

The Effects of Aronia melanocarpa 'Viking' Extracts in Attenuating RANKL-Induced Osteoclastic Differentiation by Inhibiting ROS Generation and c-FOS/NFATc1 Signaling.

Science.gov (United States)

Ghosh, Mithun; Kim, In Sook; Lee, Young Min; Hong, Seong Min; Lee, Taek Hwan; Lim, Ji Hong; Debnath, Trishna; Lim, Beong Ou

2018-03-08

This study aimed to determine the anti-osteoclastogenic effects of extracts from Aronia melanocarpa 'Viking' (AM) and identify the underlying mechanisms in vitro. Reactive oxygen species (ROS) are signal mediators in osteoclast differentiation. AM extracts inhibited ROS production in RAW 264.7 cells in a dose-dependent manner and exhibited strong radical scavenging activity. The extracts also attenuated the number of tartrate-resistant acid phosphatase (TRAP)-positive multinucleated osteoclasts. To attain molecular insights, the effect of the extracts on the signaling pathways induced by receptor activator of nuclear factor kappa B ligand (RANKL) were also investigated. RANKL triggers many transcription factors through the activation of mitogen-activated protein kinase (MAPK) and ROS, leading to the induction of osteoclast-specific genes. The extracts significantly suppressed RANKL-induced activation of MAPKs, such as extracellular signal-regulated kinase (ERK), c-Jun- N -terminal kinase (JNK) and p38 and consequently led to the downregulation of c-Fos and nuclear factor of activated T cells 1 (NFATc1) protein expression which ultimately suppress the activation of the osteoclast-specific genes, cathepsin K, TRAP, calcitonin receptor and integrin β₃. In conclusion, our findings suggest that AM extracts inhibited RANKL-induced osteoclast differentiation by downregulating ROS generation and inactivating JNK/ERK/p38, nuclear factor kappa B (NF-κB)-mediated c-Fos and NFATc1 signaling pathway.

IN VITRO INHIBITION OF CELERY (Apium graveolens L. EXTRACT ON THE ACTIVITY OF XANTHINE OXIDASE AND DETERMINATION OF ITS ACTIVE COMPOUND

Directory of Open Access Journals (Sweden)

Dyah Iswantini

2012-12-01

Full Text Available The objective of this study was to determine the inhibition effect of celery extracts toward xanthine oxidase by in vitro method, and its active compounds. Roots and herb of celery were extracted using water and ethanol solvents. Results indicated that the herbal ethanol extract had the highest inhibition effect (91.40% at 1400 ppm. The components contained in the herbal ethanol extract were then separated by column chromatography using the best eluent (chloroform : ethyl acetate at 7:3. All of the fractions had inhibition effect greater than 50%. The fraction number 4 was the one with the highest inhibition effect followed by fraction 5 with inhibition percentage of both fractions at 200 ppm were 88.62 and 85.44%, respectively. The analysis of the ultraviolet spectrum of fraction 4 showed the presence of π-π* transition which was resulted by the aromatic C=C, -OH, and C-O chromophores, and also showing the n-σ* transition which was given by -C=O chromophore. The infrared spectrum analysis indicated the presence of aromatic -C=C, -OH, and C=O functional groups. Based on the phytochemical assay and both instrumental spectrums, it was thought that the active compounds of fraction 4 and 5 were in the flavonoid group.

Inhibition of 5α-Reductase, IL-6 Secretion, and Oxidation Process of Equisetum debile Roxb. ex Vaucher Extract as Functional Food and Nutraceuticals Ingredients

Directory of Open Access Journals (Sweden)

Wantida Chaiyana

2017-10-01

Full Text Available This study aims to investigate the biological activities related to hair loss of Equisetum debile extracts, including 5α-reductase inhibition, interleukin-6 (IL-6 secretion reduction, and anti-oxidation. E. debile extracts were obtained by maceration in various solvents. Crude extract (CE was obtained by maceration in 95% ethanol. Chlorophyll-free extract (CF was the CE which of the chlorophyll has been removed by electrocoagulation. Hexane extract (HE, ethyl acetate extract (EA, and ethanolic extract (ET were fraction extracts obtained from maceration in hexane, ethyl acetate, and 95% ethanol, respectively. The extracts were investigated for inhibitory activity against 5α-reductase and IL-6 secretion. Total phenolic contents (TPC were investigated and antioxidant activities were determined by means of 2,2′-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS, 2,2′-diphenyl-1-picrylhydrazyl (DPPH, and ferric reducing antioxidant power (FRAP assays. The inhibition of lipid peroxidation was determined by the ferric thiocyanate method. The cytotoxicity of the extracts on dermal papilla cells and irritation test by hen's egg test chorioallantoic membrane assay were also investigated. All extracts could inhibit 5α-reductase and decrease IL-6 secretion in lipopolysaccharide-stimulated macrophage. The antioxidant activity of E. debile extracts was directly related to their TPC. ET which contained the highest TPC (68.8 ± 6.7 mg GA/g showed the highest equivalent concentration (EC1 of 289.1 ± 26.4 mM FeSO4/g, TEAC of 156.6 ± 34.6 mM Trolox/g, and 20.0 ± 6.0% DPPH inhibition. However, EA exhibited the highest inhibition against lipid peroxidation (57.2 ± 0.4%. In addition, EA showed no cytotoxicity on dermal papilla cell line and no irritation on chorioallantoic membrane of hen’s eggs. In conclusion, EA was suggested as the most attractive ingredients for functional food and nutraceuticals because of the high inhibitory activity against 5�

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

Directory of Open Access Journals (Sweden)

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.

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

Science.gov (United States)

Saito, Samuel Takashi; Trentin, Danielle da Silva; Macedo, Alexandre José; Pungartnik, Cristina; Gosmann, Grace; Silveira, Jaqueline de Deos; Guecheva, Temenouga Nikolova; Henriques, João Antonio Pêgas; Brendel, Martin

2012-01-01

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. PMID:22548121

Aqueous extracts of Roselle (Hibiscus sabdariffa Linn.) varieties inhibit α-amylase and α-glucosidase activities in vitro.

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Ademiluyi, Adedayo O; Oboh, Ganiyu

2013-01-01

This study sought to investigate the inhibitory effect of aqueous extracts of two varieties (red and white) of Hibiscus sabdariffa (Roselle) calyces on carbohydrate hydrolyzing enzymes (α-amylase and α-glucosidase), with the aim of providing the possible mechanism for their antidiabetes properties. Aqueous extracts were prepared (1:100 w/v) and the supernatant used for the analysis. The extracts caused inhibition of α-amylase and α-glucosidase activities in vitro.The IC(50) revealed that the red variety (25.2 μg/mL) exhibited higher α-glucosidase inhibitory activity than the white variety (47.4 μg/mL), while the white variety (90.5 μg/mL) exhibited higher α-amylase inhibitory activity than the red variety (187.9 μg/mL). However, the α-glucosidase inhibitory activities of both calyces were higher than that of their α-amylase. In addition, the red variety possessed higher antioxidant capacity as exemplified by the (•)OH scavenging abilities, Fe(2+) chelating ability, and inhibition of Fe(2+)-induced pancreatic lipid peroxidation in vitro. The enzyme inhibitory activities and antioxidant properties of the roselle extracts agreed with their phenolic content. Hence, inhibition of α-amylase and α-glucosidase, coupled with strong antioxidant properties could be the possible underlying mechanism for the antidiabetes properties of H. sabdariffa calyces; however, the red variety appeared to be more potent.

Hot water-extracted Lycium barbarum and Rehmannia glutinosa inhibit proliferation and induce apoptosis of hepatocellular carcinoma cells

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Chao, Jane C-J; Chiang, Shih-Wen; Wang, Ching-Chiung; Tsai, Ya-Hui; Wu, Ming-Shun

2006-01-01

AIM: To investigate the effect of hot water-extracted Lycium barbarum (LBE) and Rehmannia glutinosa (RGE) on cell proliferation and apoptosis in rat and/or human hepatocellular carcinoma (HCC) cells. METHODS: Rat (H-4-II-E) and human HCC (HA22T/VGH) cell lines were incubated with various concentrations (0-10 g/L) of hot water-extracted LBE and RGE. After 6-24 h incubation, cell proliferation (n = 6) was measured by a colorimetric method. The apoptotic cells (n = 6) were detected by flow cytometry. The expression of p53 protein (n = 3) was determined by SDS-PAGE and Western blotting. RESULTS: Crude LBE (2-5 g/L) and RGE (2-10 g/L) dose-dependently inhibited proliferation of H-4-II-E cells by 11% (P < 0.05) to 85% (P < 0.01) after 6-24 h treatment. Crude LBE at a dose of 5 g/L suppressed cell proliferation of H-4-II-E cells more effectively than crude RGE after 6-24 h incubation (P < 0.01). Crude LBE (2-10 g/L) and RGE (2-5 g/L) also dose-dependently inhibited proliferation of HA22T/VGH cells by 14%-43% (P < 0.01) after 24 h. Crude LBE at a dose of 10 g/L inhibited the proliferation of HA22T/VGH cells more effectively than crude RGE (56.8% ± 1.6% vs 70.3% ± 3.1% of control, P = 0.0003 < 0.01). The apoptotic cells significantly increased in H-4-II-E cells after 24 h treatment with higher doses of crude LBE (2-5 g/L) and RGE (5-10 g/L) (P < 0.01). The expression of p53 protein in H-4-II-E cells was 119% and 143% of the control group compared with the LBE-treated (2, 5 g/L) groups, and 110% and 132% of the control group compared with the RGE -treated (5, 10 g/L) groups after 24 h. CONCLUSION: Hot water-extracted crude LBE (2-5 g/L) and RGE (5-10 g/L) inhibit proliferation and stimulate p53-mediated apoptosis in HCC cells. PMID:16874858

Portulaca oleracea extract can inhibit nodule formation of colon cancer stem cells by regulating gene expression of the Notch signal transduction pathway.

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Jin, Heiying; Chen, Li; Wang, Shuiming; Chao, Deng

2017-07-01

To investigate whether Portulaca oleracea extract affects tumor formation in colon cancer stem cells and its chemotherapy sensitivity. In addition, to analyze associated genetic changes within the Notch signal transduction pathway. Serum-free cultures of colon cancer cells (HT-29) and HT-29 cancer stem cells were treated with the chemotherapeutic drug 5-fluorouracil to assess sensitivity. Injections of the stem cells were also given to BALB/c mice to confirm tumor growth and note its characteristics. In addition, the effect of different concentrations of P. oleracea extract was tested on the growth of HT-29 colon cancer cells and HT-29 cancer stem cells, as determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide method. The effects of P. oleracea extract on the expression of β-catenin, Notch1, and Notch2 in the HT-29 cells were studied using reverse transcription polymerase chain reaction and Western blotting. The tumor volume of the HT29 cells was two times larger than that of HT29 cancer stem cells. Treatment with P. oleracea extract inhibited the proliferation of both HT-29 cancer cells and HT-29 cancer stem cells at doses from 0.07 to 2.25 µg/mL. Apoptosis of HT-29 cancer cells and HT-29 cancer stem cells was assessed by flow cytometry; it was enhanced by the addition of P. oleracea extract. Finally, treatment with P. oleracea extract significantly downregulated the expression of the Notch1 and β-catenin genes in both cell types. The results of this study show that P. oleracea extract inhibits the growth of colon cancer stem cells in a dose-dependent manner. Furthermore, it inhibits the expression of the Notch1 and β-catenin genes. Taken together, this suggests that it may elicit its effects through regulatory and target genes that mediate the Notch signal transduction pathway.

Ethanol Extract of Sanguisorbae Radix Inhibits Mast Cell Degranulation and Suppresses 2,4-Dinitrochlorobenzene-Induced Atopic Dermatitis-Like Skin Lesions

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Ju-Hye Yang

2016-01-01

Full Text Available Sanguisorbae Radix (SR is well known as herbal medicine named “Zi-Yu” in Korea, which is the dried roots of Sanguisorba officinalis L. (Rosacease. We investigated the underlying mechanism on the inhibition of atopic dermatitis (AD of an ethanol extract of SR (ESR using 2,4-dinitrochlorobenzene- (DNCB- induced AD mice model. Oral administration of ESR significantly suppressed DNCB-induced AD-like symptoms such as scratching behavior, ear thickness, epidermal thickness, and IgE levels. To investigate the effects of ESR treatment on degranulation of IgE/Ag-activated mouse bone marrow-derived mast cells (BMMCs, we measured the release of β-hexosaminidase (β-HEX, degranulation marker. ESR decreased the infiltration of eosinophils and mast cells into the AD skin lesions. Furthermore, ESR significantly inhibited degranulation of IgE/Ag-activated BMMCs. We have demonstrated that ESR decreased AD symptoms in mice and inhibits degranulation of IgE/Ag-activated mast cells. Our study suggests that ESR may serve as a potential therapeutic candidate for the treatment of AD symptoms.

Inhibition of aflatoxin biosynthesis in Aspergillus flavus by phenolic compounds extracted of Piper betle L.

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Yazdani, Darab; Mior Ahmad, Zainal Abidin; Yee How, Tan; Jaganath, Indu Bala; Shahnazi, Sahar

2013-12-01

Food contamination by aflatoxins is an important food safety concern for agricultural products. In order to identify and develop novel antifungal agents, several plant extracts and isolated compounds have been evaluated for their bioactivities. Anti-infectious activity of Piper betle used in traditional medicine of Malaysia has been reported previously. Crude methanol extract from P. betel powdered leaves was partitioned between chloroform and water. The fractions were tested against A. flavus UPMC 89, a strong aflatoxin producing strain. Inhibition of mycelial growth and aflatoxin biosynthesis were tested by disk diffusion and macrodillution techniques, respectively. The presence of aflatoxin was determined by thin-layer chromatography (TLC) and fluorescence spectroscopy techniques using AFB1 standard. The chloroform soluble compounds were identified using HPLC-Tandem mass spectrometry technique. The results, evaluated by measuring the mycelial growth and quantification of aflatoxin B1(AFLB1) production in broth medium revealed that chloroform soluble compounds extract from P. betle dried leaves was able to block the aflatoxin biosynthesis pathway at concentration of 500μg/ml without a significant effect on mycelium growth. In analyzing of this effective fractions using HPLC-MS(2) with ESI ionization technique, 11 phenolic compounds were identified. The results showed that the certain phenolic compounds are able to decline the aflatoxin production in A. flavus with no significant effect on the fungus mycelia growth. The result also suggested P. betle could be used as potential antitoxin product.

Synergistic Effects of Natural Medicinal Plant Extracts on Growth Inhibition of Carcinoma (KB) Cells under Oxidative Stress

International Nuclear Information System (INIS)

Kim, Jeong Hee; Ju, Eun Mi; Kim, Jin Kyu

2000-01-01

Medicinal plants with synergistic effects on growth inhibition of cancer cells under oxidative stress were screened in this study. Methanol extracts from 51 natural medicinal plants, which were reported to have anticancer effect on hepatoma, stomach cancer or colon cancers which are frequently found in Korean, were prepared and screened for their synergistic activity on growth inhibition of cancer cells under chemically-induced oxidative stress by using MTT assay. Twenty seven samples showed synergistic activity on the growth inhibition in various extent under chemically-induced oxidative stress. Among those samples, eleven samples, such as Melia azedarach, Agastache rugosa, Catalpa ovata, Prunus persica, Sinomenium acutum, Pulsatilla koreana, Oldenlandia diffiusa, Anthriscus sylvestris, Schizandra chinensis, Gleditsia sinensis, Cridium officinale, showed decrease in IC 50 values more than 50%, other 16 samples showed decrease in IC 50 values between 50-25%, compared with the value acquired when medicinal plant sample was used alone. Among those 11 samples, extract of Catalpa ovata showed the highest activity. IC 50 values were decrease to 61% and 28% when carcinoma cells were treated with Catalpa ovata extract in combination of 75 and 100 μM of hydrogen peroxide, respectively

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

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Ding, Hong; Shen, Jinglian; Yang, Yang; Che, Yuqin

2015-01-01

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 ass...

INHIBITION EFFECT OF FLAVONOID EXTRACT OF Euphorbia Guyoniana ON THE CORROSION OF MILD STEEL IN H2SO4 MEDIUM

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S. Chihi

2009-08-01

Full Text Available The influence of flavonoids extracts of three parts of Euphorbia Guyoniana towards the corrosion of type API 5L X52 steel in 15% H2SO4 has been evaluated by weight loss method and polarization technique. The results showed that extracts are a good inhibitors for API 5L X52 steel in this medium. The corrosion inhibition efficiency increases on increasing plant extracts concentration. The inhibition is attributed to the adsorption of the surface of the metal. Potentiodynamic polarization results revealed that the studied inhibitors behave as a mixed type.

Comparative evaluation of 12 immature citrus fruit extracts for the inhibition of cytochrome P450 isoform activities.

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Fujita, Tadashi; Kawase, Atsushi; Niwa, Toshiro; Tomohiro, Norimichi; Masuda, Megumi; Matsuda, Hideaki; Iwaki, Masahiro

2008-05-01

In a previous study we found that 50% ethanol extracts of immature fruits of Citrus unshiu (satsuma mandarin) have anti-allergic effects against the Type I, II and IV allergic reactions. However, many adverse interactions between citrus fruit, especially grapefruit juice, and drugs have been reported due to the inhibition of cytochrome P450 (CYP) activities. The purpose of this study was to examine the competitive inhibitory effects of extracts from immature citrus fruit on CYP activity. Extracts were prepared from 12 citrus species or cultivars, and were tested against three kinds of major CYPs, CYP2C9, CYP2D6 and CYP3A4, in human liver microsomes. We also estimated the amounts of flavonoids (narirutin, hesperidin, naringin and neohesperidin) and furanocoumarins (bergapten, 6',7'-dihydroxybergamottin and bergamottin) in each extract using HPLC. Citrus paradisi (grapefruit) showed the greatest inhibition of CYP activities, while Citrus unshiu which has an antiallergic effect, showed relatively weak inhibitory effects. Extracts having relatively strong inhibitory effects for CYP3A4 tended to contain higher amounts of naringin, bergamottin and 6',7'-dihydroxybergamottin. These results, providing comparative information on the inhibitory effects of citrus extracts on CYP isoforms, suggest that citrus extracts containing high levels of narirutin and hesperidin and lower levels of furanocoumarins such as C. unshiu are favorable as antiallergic functional ingredients.

Acetylcholinesterase inhibition starting from extracts of Bauhinia variegata L., Bauhinia var. candida (Aiton) Buch.-Ham., and Bauhinia ungulata L.

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Santos, Kamilla Monteiro dos; Gonçalves, Priscila Sant'Ana; Paiva, Maria José Nunes de; Lacerda, Guilherme Araújo

2011-01-01

A treatment to the Alzheimer's disease consists inhibition of the acetylcholinesterase, which is responsible for the acetylcholine control in the synapses. 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. Retention factor analysis shows values of 0.31aA, 0.31aA, and 0.46aB for flowers B. variegata, B. var. candida, and B. ungulata, respectively. The flower extract of B. ungulata is the most suitable for further studies on this inhibition.

A Vitex agnus-castus extract inhibits cell growth and induces apoptosis in prostate epithelial cell lines.

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Weisskopf, M; Schaffner, W; Jundt, G; Sulser, T; Wyler, S; Tullberg-Reinert, H

2005-10-01

Extracts of Vitex agnus-castus fruits (VACF) are described to have beneficial effects on disorders related to hyperprolactinemia (cycle disorders, premenstrual syndrome). A VACF extract has recently been shown to exhibit antitumor activities in different human cancer cell lines. In the present study, we explored the antiproliferative effects of a VACF extract with a particular focus on apoptosis-inducing and potential cytotoxic effects. Three different human prostate epithelial cell lines (BPH-1, LNCaP, PC-3) representing different disease stages and androgen responsiveness were chosen. The action of VACF on cell viability was assessed using the WST-8-tetrazolium assay. Cell proliferation in cells receiving VACF alone or in combination with a pan-caspase inhibitor (Z-VAD-fmk) was quantified using a Crystal Violet assay. Flow cytometric cell cycle analysis and measurement of DNA fragmentation using an ELISA method were used for studying the induction of apoptosis. Lactate dehydrogenase (LDH) activity was determined as a marker of cytotoxicity. The extract inhibited proliferation of all three cell lines in a concentration-dependent manner with IC (50) values below 10 microg/mL after treatment for 48 h. Cell cycle analysis and DNA fragmentation assays suggest that part of the cells were undergoing apoptosis. The VACF-induced decrease in cell number was partially inhibited by Z-VAD-fmk, indicating a caspase-dependent apoptotic cell death. However, the concentration-dependent LDH activity of VACF treated cells indicated cytotoxic effects as well. These data suggest that VACF contains components that inhibit proliferation and induce apoptosis in human prostate epithelial cell lines. The extract may be useful for the prevention and/or treatment not only of benign prostatic hyperplasia but also of human prostate cancer.

Significance of wood extractives for wood bonding.

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Roffael, Edmone

2016-02-01

Wood contains primary extractives, which are present in all woods, and secondary extractives, which are confined in certain wood species. Extractives in wood play a major role in wood-bonding processes, as they can contribute to or determine the bonding relevant properties of wood such as acidity and wettability. Therefore, extractives play an immanent role in bonding of wood chips and wood fibres with common synthetic adhesives such as urea-formaldehyde-resins (UF-resins) and phenol-formaldehyde-resins (PF-resins). Extractives of high acidity accelerate the curing of acid curing UF-resins and decelerate bonding with alkaline hardening PF-resins. Water-soluble extractives like free sugars are detrimental for bonding of wood with cement. Polyphenolic extractives (tannins) can be used as a binder in the wood-based industry. Additionally, extractives in wood can react with formaldehyde and reduce the formaldehyde emission of wood-based panels. Moreover, some wood extractives are volatile organic compounds (VOC) and insofar also relevant to the emission of VOC from wood and wood-based panels.

Clerodendrum inerme Leaf Extract Alleviates Animal Behaviors, Hyperlocomotion, and Prepulse Inhibition Disruptions, Mimicking Tourette Syndrome and Schizophrenia

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Hon-Lie Chen

2012-01-01

Full Text Available Previously, we found a patient with intractable motor tic disorder, a spectrum of Tourette syndrome (TS, responsive to the ground leaf juice of Clerodendrum inerme (CI. Here, we examined the effect of the ethanol extract of CI leaves (CI extract on animal behaviors mimicking TS, hyperlocomotion, and sensorimotor gating deficit. The latter is also observed in schizophrenic patients and can be reflected by a disruption of prepulse inhibition of acoustic startle response (PPI in animal models induced by methamphetamine and NMDA channel blockers (ketamine or MK-801, based on hyperdopaminergic and hypoglutamatergic hypotheses, respectively. CI extract (10–300 mg/kg, i.p. dose-dependently inhibited hyperlocomotion induced by methamphetamine (2 mg/kg, i.p. and PPI disruptions induced by methamphetamine, ketamine (30 mg/kg, i.p., and MK-801 (0.3 mg/kg, i.p. but did not affect spontaneous locomotor activity, rotarod performance, and grip force. These results suggest that CI extract can relieve hyperlocomotion and improve sensorimotor gating deficit, supporting the therapeutic potential of CI for TS and schizophrenia.

Inhibition of cholinesterase activity by extracts, fractions and compounds from Calceolaria talcana and C. integrifolia (Calceolariaceae: Scrophulariaceae).

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Cespedes, Carlos L; Muñoz, Evelyn; Salazar, Juan R; Yamaguchi, Lydia; Werner, Enrique; Alarcon, Julio; Kubo, Isao

2013-12-01

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 Ellman's 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.

Extract of corn silk (stigma of Zea mays) inhibits the tumour necrosis factor-alpha- and bacterial lipopolysaccharide-induced cell adhesion and ICAM-1 expression.

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Habtemariam, S

1998-05-01

Treatment of human endothelial cells with cytokines such as tumour necrosis factor-alpha (TNF) or E. coli lipopolysaccharide (LPS) induces the expression of several adhesion molecules and enhances leukocyte adhesion to endothelial cell surface. Interfering with this leukocyte adhesion or adhesion molecules upregulation is an important therapeutic target for the treatment of bacterial sepsis and various inflammatory diseases. In the course of screening marketed European anti-inflammatory herbal drugs for TNF antagonistic activity, a crude ethanolic extract of corn silk (stigma of Zea mays) exhibited significant activity. The extract at concentrations of 9-250 micrograms/ml effectively inhibited the TNF- and LPS-induced adhesiveness of EAhy 926 endothelial cells to monocytic U937 cells. Similar concentration ranges of corn silk extract did also block the TNF and LPS but not the phorbol 12-myristate 13-acetate-induced ICAM-1 expression on EAhy 926 endothelial cell surface. The extract did not alter the production of TNF by LPS-activated macrophages and failed to inhibit the cytotoxic activity of TNF. It is concluded that corn silk possesses important therapeutic potential for TNF- and LPS-mediated leukocyte adhesion and trafficking.

Sodium sulphite inhibition of potato and cherry polyphenolics in nucleic acid extraction for virus detection by RT-PCR.

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Singh, R P; Nie, X; Singh, M; Coffin, R; Duplessis, P

2002-01-01

Phenolic compounds from plant tissues inhibit reverse transcription-polymerase chain reaction (RT-PCR). Multiple-step protocols using several additives to inhibit polyphenolic compounds during nucleic acid extraction are common, but time consuming and laborious. The current research highlights that the inclusion of 0.65 to 0.70% of sodium sulphite in the extraction buffer minimizes the pigmentation of nucleic acid extracts and improves the RT-PCR detection of Potato virus Y (PVY) and Potato leafroll virus (PLRV) in potato (Solanum tuberosum) tubers and Prune dwarf virus (PDV) and Prunus necrotic ringspot virus (PNRSV) in leaves and bark in the sweet cherry (Prunus avium) tree. Substituting sodium sulphite in the nucleic acid extraction buffer eliminated the use of proteinase K during extraction. Reagents phosphate buffered saline (PBS)-Tween 20 and polyvinylpyrrolidone (PVP) were also no longer required during RT or PCR phase. The resultant nucleic acid extracts were suitable for both duplex and multiplex RT-PCR. This simple and less expensive nucleic acid extraction protocol has proved very effective for potato cv. Russet Norkotah, which contains a high amount of polyphenolics. Comparing commercially available RNA extraction kits (Catrimox and RNeasy), the sodium sulphite based extraction protocol yielded two to three times higher amounts of RNA, while maintaining comparable virus detection by RT-PCR. The sodium sulphite based extraction protocol was equally effective in potato tubers, and in leaves and bark from the cherry tree.

dNP2-ctCTLA-4 inhibits German cockroach extract-induced allergic airway inflammation and hyper-responsiveness via inhibition of Th2 responses.

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Lim, Sangho; Ho Sohn, Jung; Koo, Ja-Hyun; Park, Jung-Won; Choi, Je-Min

2017-08-04

German cockroaches are major household allergens that can trigger allergic airway inflammatory diseases with sensitive T-cell responses. Although the use of immune modulatory biologics, such as antibodies, to mediate allergic responses has recently been examined, only systemic administration is available because of the size limitations on intranasal administration. Here we utilized a cell-permeable peptide, dNP2, to deliver the cytoplasmic domain of cytotoxic T-lymphocyte antigen-4 (ctCTLA-4) through the airway epithelium to modulate Th2 responses in a German cockroach extract (GCE)-induced allergic airway inflammation model. The intranasal delivery efficiency of the dNP2-dTomato protein to the lungs was higher in GCE-induced asthmatic lung parenchymal cells compared to the sham cells. Intranasal administration of the dNP2-ctCTLA-4 protein inhibited airway hyper-responsiveness and reduced airway inflammation and remodeling, including goblet cell metaplasia and collagen deposition around the bronchi. The number of infiltrated cells, including eosinophils, and the levels of IL-4, IL-5, IL-13 and IFN-γ in the lungs were significantly reduced, presumably owing to inhibition of Th2 differentiation. However, intranasal administration of CTLA4-Ig did not inhibit airway inflammation. These results collectively suggest that dNP2-ctCTLA-4 is an efficient intranasally applicable candidate biologic for treating allergic asthma.

The Effects of Aronia melanocarpa ‘Viking’ Extracts in Attenuating RANKL-Induced Osteoclastic Differentiation by Inhibiting ROS Generation and c-FOS/NFATc1 Signaling

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Mithun Ghosh

2018-03-01

Full Text Available This study aimed to determine the anti-osteoclastogenic effects of extracts from Aronia melanocarpa ‘Viking’ (AM and identify the underlying mechanisms in vitro. Reactive oxygen species (ROS are signal mediators in osteoclast differentiation. AM extracts inhibited ROS production in RAW 264.7 cells in a dose-dependent manner and exhibited strong radical scavenging activity. The extracts also attenuated the number of tartrate-resistant acid phosphatase (TRAP-positive multinucleated osteoclasts. To attain molecular insights, the effect of the extracts on the signaling pathways induced by receptor activator of nuclear factor kappa B ligand (RANKL were also investigated. RANKL triggers many transcription factors through the activation of mitogen-activated protein kinase (MAPK and ROS, leading to the induction of osteoclast-specific genes. The extracts significantly suppressed RANKL-induced activation of MAPKs, such as extracellular signal-regulated kinase (ERK, c-Jun-N-terminal kinase (JNK and p38 and consequently led to the downregulation of c-Fos and nuclear factor of activated T cells 1 (NFATc1 protein expression which ultimately suppress the activation of the osteoclast-specific genes, cathepsin K, TRAP, calcitonin receptor and integrin β3. In conclusion, our findings suggest that AM extracts inhibited RANKL-induced osteoclast differentiation by downregulating ROS generation and inactivating JNK/ERK/p38, nuclear factor kappa B (NF-κB-mediated c-Fos and NFATc1 signaling pathway.

Inhibition of gap-junctional intercellular communication and activation of mitogen-activated protein kinases by cyanobacterial extracts--indications of novel tumor-promoting cyanotoxins?

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Bláha, Ludĕk; Babica, Pavel; Hilscherová, Klára; Upham, Brad L

2010-01-01

Toxicity and liver tumor promotion of cyanotoxins microcystins have been extensively studied. However, recent studies document that other metabolites present in the complex cyanobacterial water blooms may also have adverse health effects. In this study we used rat liver epithelial stem-like cells (WB-F344) to examine the effects of cyanobacterial extracts on two established markers of tumor promotion, inhibition of gap-junctional intercellular communication (GJIC) and activation of mitogen-activated protein kinases (MAPKs) - ERK1/2. Extracts of cyanobacteria (laboratory cultures of Microcystis aeruginosa and Aphanizomenon flos-aquae and water blooms dominated by these species) inhibited GJIC and activated MAPKs in a dose-dependent manner (effective concentrations ranging 0.5-5mgd.w./mL). Effects were independent of the microcystin content and the strongest responses were elicited by the extracts of Aphanizomenon sp. Neither pure microcystin-LR nor cylindrospermopsin inhibited GJIC or activated MAPKs. Modulations of GJIC and MAPKs appeared to be specific to cyanobacterial extracts since extracts from green alga Chlamydomonas reinhardtii, heterotrophic bacterium Klebsiella terrigena, and isolated bacterial lipopolysaccharides had no comparable effects. Our study provides the first evidence on the existence of unknown cyanobacterial toxic metabolites that affect in vitro biomarkers of tumor promotion, i.e. inhibition of GJIC and activation of MAPKs.

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

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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.

Spasmolytic Mechanism of Aqueous Licorice Extract on Oxytocin-Induced Uterine Contraction through Inhibiting the Phosphorylation of Heat Shock Protein 27

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Lu Yang

2017-08-01

Full Text Available Licorice derived from the roots and rhizomes of Glycyrrhiza uralensis Fisch. (Fabaceae, is one of the most widely-used traditional herbal medicines in China. It has been reported to possess significant analgesic activity for treating spastic pain. The aim of this study is to investigate the spasmolytic molecular mechanism of licorice on oxytocin-induced uterine contractions and predict the relevant bioactive constituents in the aqueous extract. The aqueous extraction from licorice inhibited the amplitude and frequency of uterine contraction in a concentration-dependent manner. A morphological examination showed that myometrial smooth muscle cells of oxytocin-stimulated group were oval-shaped and arranged irregularly, while those with a single centrally located nucleus of control and licorice-treated groups were fusiform and arranged orderly. The percentage of phosphorylation of HSP27 at Ser-15 residue increased up to 50.33% at 60 min after oxytocin stimulation. Furthermore, this increase was significantly suppressed by licorice treatment at the concentration of 0.2 and 0.4 mg/mL. Colocalization between HSP27 and α-SMA was observed in the myometrial tissues, especially along the actin bundles in the oxytocin-stimulated group. On the contrary, the colocalization was no longer shown after treatment with licorice. Additionally, employing ChemGPS-NP provided support for a preliminary assignment of liquiritigenin and isoliquiritigenin as protein kinase C (PKC inhibitors in addition to liquiritigenin, isoliquiritigenin, liquiritin and isoliquiritin as MAPK-activated protein kinase 2 (MK2 inhibitors. These assigned compounds were docked with corresponding crystal structures of respective proteins with negative and low binding energy, which indicated a high affinity and tight binding capacity for the active site of the kinases. These results suggest that licorice exerts its spasmolytic effect through inhibiting the phosphorylation of HSP27 to alter the

Water extract of Acer tegmentosum reduces bone destruction by inhibiting osteoclast differentiation and function.

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Ha, Hyunil; Shim, Ki-Shuk; Kim, Taesoo; An, Hyosun; Lee, Chung-Jo; Lee, Kwang Jin; Ma, Jin Yeul

2014-04-01

The stem of Acer tegmentosum has been widely used in Korea for the treatment of hepatic disorders. In this study, we investigated the bone protective effect of water extract of the stem of Acer tegmentosum (WEAT). We found that WEAT inhibits osteoclast differentiation induced by receptor activator of nuclear factor-κB ligand (RANKL), an essential cytokine for osteoclast differentiation. In osteoclast precursor cells, WEAT inhibited RANKL-induced activation of JNK, NF-κB, and cAMP response element-binding protein, leading to suppression of the induction of c-Fos and nuclear factor of activated T cells cytoplasmic 1, key transcription factors for osteoclast differentiation. In addition, WEAT inhibited bone resorbing activity of mature osteoclasts. Furthermore, the oral administration of WEAT reduced RANKL-induced bone resorption and trabecular bone loss in mice. Taken together, our study demonstrates that WEAT possesses a protective effect on bone destruction by inhibiting osteoclast differentiation and function.

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.

Berberine and a Berberis lycium extract inactivate Cdc25A and induce α-tubulin acetylation that correlate with HL-60 cell cycle inhibition and apoptosis

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Khan, Musa; Giessrigl, Benedikt; Vonach, Caroline; Madlener, Sibylle; Prinz, Sonja; Herbaceck, Irene; Hoelzl, Christine; Bauer, Sabine; Viola, Katharina; Mikulits, Wolfgang; Quereshi, Rizwana Aleem; Knasmueller, Siegfried; Grusch, Michael; Kopp, Brigitte; Krupitza, Georg

2010-01-01

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 2 O) extract. The chemical composition of the BuOH extract was analyzed by TLC and quantified by HPLC. 11.1 μg BuOH extract (that was gained from 1 mg dried root) contained 2.0 μg berberine and 0.3 μg/ml palmatine. 1.2 μg/ml berberine inhibited cell proliferation significantly, while 0.5 μg/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 α-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.

Marijuana extracts possess the effects like the endocrine disrupting chemicals

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Watanabe, Kazuhito; Motoya, Erina; Matsuzawa, Naoki; Funahashi, Tatsuya; Kimura, Toshiyuki; Matsunaga, Tamihide; Arizono, Koji; Yamamoto, Ikuo

2005-01-01

The progesterone 17α-hydroxylase activity, which is one of the steroidogenic enzymes in rat testis microsomes, was significantly inhibited by crude marijuana extracts from Δ 9 -tetrahydrocannabinolic acid (THCA)- and cannabidiolic acid (CBDA)-strains. Δ 9 -Tetrahydrocannabinol, cannabidiol and cannabinol also inhibited the enzymatic activitiy with relatively higher concentration (100-1000 μM). Testosterone 6β- and 16α-hydroxylase activities together with androstenedione formation from testosterone in rat liver microsomes were also significantly inhibited by the crude marijuana extracts and the cannabinoids. Crude marijuana extracts (1 and 10 μg/ml) of THCA strain stimulated the proliferation of MCF-7 cells, although the purified cannabinoids (THC, CBD and CBN) did not show significant effects, such as the extract at the concentration of 0.01-1000 nM. These results indicate that there are some metabolic interactions between cannabinoid and steroid metabolism and that the constituents showing estrogen-like activity exist in marijuana

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.

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

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Lutfi, Zainal; Ahmad, Asmat; Usup, Gires

2014-01-01

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

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

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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.

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.

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

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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.

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

Free radical scavenging activity and lipoxygenase inhibition of Mahonia aquifolium extract and isoquinoline alkaloids

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Kettmann Viktor

2007-07-01

Full Text Available Abstract Roots and stem-bark of Mahonia aquifolium (Oregon grape (Berberidaceae are effectively used in the treatment of skin inflammatory conditions. In the present study, the effect of Mahonia aquifolium crude extract and its two representative alkaloid fractions containing protoberberine and bisbenzylisoquinoline (BBIQ alkaloids on activity of 12-lipoxygenase (12-LOX, was studied. The reactivity with 1,1-diphenyl-2-picryl-hydrazyl (DPPH, a free stable radical, was evaluated to elucidate the rate of possible lipid-derived radical scavenging in the mechanism of the enzyme inhibition. The results indicate that although the direct radical scavenging mechanism cannot be ruled out in the lipoxygenase inhibition by Mahonia aquifolium and its constituents, other mechanisms based on specific interaction between enzyme and alkaloids could play the critical role in the lipoxygenase inhibition rather than non-specific reactivity with free radicals.

The dichloromethane extract of the ethnomedicinal plant Neurolaena lobata inhibits NPM/ALK expression which is causal for anaplastic large cell lymphomagenesis.

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Unger, Christine; Popescu, Ruxandra; Giessrigl, Benedikt; Laimer, Daniela; Heider, Susanne; Seelinger, Mareike; Diaz, Rene; Wallnöfer, Bruno; Egger, Gerda; Hassler, Melanie; Knöfler, Martin; Saleh, Leila; Sahin, Emine; Grusch, Michael; Fritzer-Szekeres, Monika; Dolznig, Helmut; Frisch, Richard; Kenner, Lukas; Kopp, Brigitte; Krupitza, Georg

2013-01-01

The present study investigates extracts of Neuolaena lobata, an anti-protozoan ethnomedicinal plant of the Maya, regarding its anti-neoplastic properties. Firstly, extracts of increasing polarity were tested in HL-60 cells analyzing inhibition of cell proliferation and apoptosis induction. Secondly, the most active extract was further tested in anaplastic large cell lymphoma (ALCL) cell lines of human and mouse origin. The dichloromethane extract inhibited proliferation of HL-60, human and mouse ALCL cells with an IC50 of ~2.5, 3.7 and 2.4 µg/ml, respectively and arrested cells in the G2/M phase. The extract induced the checkpoint kinases Chk1 and Chk2 and perturbed the orchestrated expression of the Cdc25 family of cell cycle phosphatases which was paralleled by the activation of p53, p21 and downregulation of c-Myc. Importantly, the expression of NPM/ALK and its effector JunB were drastically decreased, which correlated with the activation of caspase 3. Subsequently also platelet derived growth factor receptor β was downregulated, which was recently shown to be transcriptionally controlled by JunB synergizing with ALK in ALCL development. We show that a traditional healing plant extract downregulates various oncogenes, induces tumor suppressors, inhibits cell proliferation and triggers apoptosis of malignant cells. The discovery of the 'Active Principle(s)' is warranted.

Adsorption and inhibitive properties of methanol extract of Eeuphorbia Heterophylla for the corrosion of copper in 0.5 M nitric acid solutions

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Fouda A. S.

2017-03-01

Full Text Available The adsorption and the inhibitive properties of methanol extract of Euphorbia heterophylla on copper in 0.5 M HNO3 have been studied by weight loss method at different temperatures (30-50°C, potentiodynamic polarization, electrochemical impedance spectroscopy (EIS and electrochemical frequency modulation (EFM techniques. Also, the surface morphology was analyzed by scanning electron microscopy (SEM. It was found that the inhibition efficiency increases with increasing extract doses and decreased with increasing temperature. The polarization data revealed that this extract acts as mixed type inhibitor. The adsorption process was more favored at lower temperatures with larger negative standard free energy. The extract was adsorbed physically on the copper surface followed Frumkin isotherm.

Evaluation Study Of Inhibition And Regeneration Characters For Substituted Anilines Extracted From Crude Oil

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Dr. Mohammad Jamil Abd-Alghani

2015-08-01

Full Text Available Abstract Aniline derivatives containing carbonyl group in the side chain was extracted from crude oil received from Al- Dora refinery. The crude oil was dissolved in xylene 13 and extracted through a column containing activated cationic resin type Amberlyte 15 then eluted by absolute ethanol and identified by infra red spectroscopy then examined as antioxidant for lubricant oil stock 50. FT-IR spectroscopy for the lubricant oil was performed before employing in an internal combustion engine and 190 hrs after. It was seen that the FT-IR of the oxidized oil contains a new peak in the region 1700 1800 cm1 which is formed due to the oxidation of base oil which belongs to carbonyl group. The FT-IR specter for the formulated crude oil with a specific concentration of the extracted substituted aniline after applying the same conditions of oxidation 190 working hrs. in an internal combustion engine showed a minimum peak intensity at 1710 1770 cm-1 than that observed in FT-IR done in absence of extracted antioxidant. The values of induction periods in presence of 0.20 and 0.30 moll of the extracted sample in the lubricant oil at 393 K were 766 sec. 1630 sec. while in their absence was 55 sec.. The values of maximum rates of oxidation were 3.0x10-4 and 2.0x10-4 moll. sec. These values were still not arrived the value of maximum rate of oxidation for the lubricant oil 3.5 x10-4 mol.l.sec. The same study was applied on the universal antioxidant inhibitor 2 6-diter-butyl-4-methyl phenol phenolic type under the same conditions. The obtained induction periods were 150 290 sec. respectively. This means that the values of induction periods obtained by formulating the lubricant oil with the extracted aniline molecule were 7 times greater than do the 2 6- diter-butyl-4-methyl phenol molecule. From the literatures it is known that the value of stochiometric factor for inhibition f for 2 4 6-triisobutyl phenol is equal to 2 so as a result the value of stochiometric

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

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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.

Comparative analysis of adsorption and corrosion inhibitive properties of ethanol extract of Dialium Guineense leaves for mild steel in 0.5 M HCl

OpenAIRE

Shola Elijah Adeniji; Bamigbola Abiola Akindehinde

2018-01-01

Adsorption and corrosion inhibitive properties of ethanol extract of Dialium guineense leaves for mild steel in 0.5M HCl was studied using the gravimetric method. The results showed that the ethanol extract of Dialium guineense leaves is a good corrosion inhibitor for mild steel in 0.5 M HCl. The inhibition efficiency was found to increase with increase in the concentration of ethanol extract of Dialium guineense leaves up to the maximum of 92 %, but at the same time it decreased as the tempe...

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.

Bioactive chemical constituents of Curcuma longa L. rhizomes extract inhibit the growth of human hepatoma cell line (HepG2).

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Abdel-Lateef, Ezzat; Mahmoud, Faten; Hammam, Olfat; El-Ahwany, Eman; El-Wakil, Eman; Kandil, Sherihan; Abu Taleb, Hoda; El-Sayed, Mortada; Hassenein, Hanaa

2016-09-01

The present study was designed to identify the chemical constituents of the methanolic extract of Curcuma longa L. rhizomes and their inhibitory effect on a hepatoma cell line. The methanolic extract was subjected to GC-MS analysis to identify the volatile constituents and the other part of the same extract was subjected to liquid column chromatographic separation to isolate curcumin. The inhibition of cell growth in the hepatoma cell line and the cytopathological changes were studied. GC-MS analysis showed the presence of fifty compounds in the methanolic extract of C. longa. The major compounds were ar-turmerone (20.50 %), β-sesquiphellandrene (5.20 %) and curcumenol (5.11 %). Curcumin was identified using IR, 1H and 13C NMR. The inhibition of cell growth by curcumin (IC50 = 41.69 ± 2.87 μg mL-1) was much more effective than that of methanolic extract (IC50 = 196.12 ± 5.25 μg mL-1). Degenerative and apoptotic changes were more evident in curcumin- treated hepatoma cells than in those treated with the methanol extract. Antitumor potential of the methanolic extract may be attributed to the presence of sesquiterpenes and phenolic constituents including curcumin (0.051 %, 511.39 μg g-1 dried methanol extract) in C. longa rhizomes.

Comparative analysis of adsorption and corrosion inhibitive properties of ethanol extract of Dialium Guineense leaves for mild steel in 0.5 M HCl

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Shola Elijah Adeniji

2018-05-01

Full Text Available Adsorption and corrosion inhibitive properties of ethanol extract of Dialium guineense leaves for mild steel in 0.5M HCl was studied using the gravimetric method. The results showed that the ethanol extract of Dialium guineense leaves is a good corrosion inhibitor for mild steel in 0.5 M HCl. The inhibition efficiency was found to increase with increase in the concentration of ethanol extract of Dialium guineense leaves up to the maximum of 92 %, but at the same time it decreased as the temperature was increased. Corrosion inhibition by the extract of Dialium guineense leaves is carried out by adsorption mechanism with the kinetics of corrosion following the pseudo first order reaction with high correlation. Thermodynamic consideration revealed that adsorption of the ethanol extract of Dialium guineense leaves on mild steel surface is an exothermic and spontaneous process that fitted the Langmuir adsorption isotherm. The values of activation energy and Gibb’s free energy were found within the range of limits expected for the mechanism of physical adsorption.

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

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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

The Ethanolic Extracts The Gorgonian Isis hippuris Inhibited the Induced Mammary Carcinoma Growth In C3H Mice

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Trianto, Agus; Andriyas, Yogi; Ridlo, Ali; Sedjati, Sri; Susilaningsih, Neni; Murwani, Retno

2018-02-01

The gorgonian Isis hippuris contains secondary metabolites gorgosterol and hippuristanol which are capable of inhibiting cancer cells. However, in vivo test of the gorgonian Isis hippuris extract as the anticancer drug has not been conducted. The research to study of the effect of ethanolic extract of the gorgonian on the induced tumor growth in C3H mice. The I. hippuris was obtained from Karimunjawa water in Jepara. The extract was prepared by maceration using ethanol. A total 20, 8-10 moths old of C3H mice with an initial weight of 20-25 gram were assigned into control, Ih-1, Ih-2, and Ih-3 groups. Control, Ih-1, Ih-2, and Ih-3 groups each received 0, 0.15, 1.5, and 15 mg extract per mouse per day respectively for two weeks. Cancer cells were introduced to all groups from a donor cancer mouse by injection via left or right axilla and allowed to grow. The cancer mass was removed and processed for histological examination, and cancer growth was determined according to Elston and Ellis criteria. The result showed that histological grade of cancer mass from the control group was in grade 2 or differentiated moderately. The histological grade of cancer mass from Ih-1, Ih-2, and Ih-3 groups were in grade 1 (low grade) or similar to a normal cell. Statistical analysis by Kruskal-Wallis test showed a significant difference (ptest found no significant differences among Ih-1, Ih-2, and Ih-3 treated mice. The results indicated the potential of active substances in the ethanol extract of I. hippuris as an anti-cancer drug.

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

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Renato José Silva-Oliveira

2016-11-01

Full Text Available 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.

Pharmacological activities of Vitex agnus-castus extracts in vitro.

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Meier, B; Berger, D; Hoberg, E; Sticher, O; Schaffner, W

2000-10-01

The pharmacological effects of ethanolic Vitex agnus-castus fruit-extracts (especially Ze 440) and various extract fractions of different polarities were evaluated both by radioligand binding studies and by superfusion experiments. A relative potent binding inhibition was observed for dopamine D2 and opioid (micro and kappa subtype) receptors with IC50 values of the native extract between 20 and 70 mg/mL. Binding, neither to the histamine H1, benzodiazepine and OFQ receptor, nor to the binding-site of the serotonin (5-HT) transporter, was significantly inhibited. The lipophilic fractions contained the diterpenes rotun-difuran and 6beta,7beta-diacetoxy-13-hydroxy-labda-8,14-dien . They exhibited inhibitory actions on dopamine D2 receptor binding. While binding inhibition to mu and kappa opioid receptors was most pronounced in lipophilic fractions, binding to delta opioid receptors was inhibited mainly by a aqueous fraction. Standardised Ze 440 extracts of different batches were of constant pharmacological quality according to their potential to inhibit the binding to D2 receptors. In superfusion experiments, the aqueous fraction of a methanolic extract inhibited the release of acetylcholine in a concentration-dependent manner. In addition, the potent D2 receptor antagonist spiperone antagonised the effect of the extract suggesting a dopaminergic action mediated by D2 receptor activation. Our results indicate a dopaminergic effect of Vitex agnus-castus extracts and suggest additional pharmacological actions via opioid receptors.

IN VITRO ANTIMALARIAL ACTIVITY OF THE EXTRACTS OF ...

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a significant inhibition in schizont maturation relative to control (P = 0.05). Ethanolic extract .... Animals were handled according to local rules and regulation of ... graph of percentage mortality converted to probit against log-dose of the extract ...

Soy Pulp Extract Inhibits Angiotensin I-Converting Enzyme (ACE) Activity In Vitro: Evidence for Its Potential Hypertension-Improving Action.

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Nishibori, Naoyoshi; Kishibuchi, Reina; Morita, Kyoji

2017-05-04

Soy pulp, called "okara" in Japanese, is known as a by-product of the production of bean curd (tofu), and expected to contain a variety of biologically active substances derived from soybean. However, the biological activities of okara ingredients have not yet been fully understood, and the effectiveness of okara as a functional food seems necessary to be further evaluated. Then the effect of okara extract on angiotensin I-converting enzyme (ACE) activity was examined in vitro, and the extract was shown to cause the inhibition of ACE activity in a manner depending on its concentration. Kinetic analysis indicated that this enzyme inhibition was accompanied by an increase in the Km value without any change in Vmax. Further studies suggested that putative inhibitory substances contained in the extract might be heat stable and dialyzable, and recovered mostly in the peptide fraction obtained by a spin-column separation and a high performance liquid chromatography (HPLC) fractionation. Therefore, the extract was speculated to contain small-size peptides responsible for the inhibitory effect of okara extract on ACE activity, and could be expected to improve the hypertensive conditions by reducing the production of hypertensive peptide.

Extracts from the edible seaweed, Ascophyllum nodosum, inhibit lipase activity in vitro: contributions of phenolic and polysaccharide components.

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Austin, Ceri; Stewart, Derek; Allwood, J William; McDougall, Gordon J

2018-01-24

A polyphenol-rich extract (PRE) from the edible seaweed, Ascophyllum nodosum, inhibited pancreatic lipase activity in an oil-based turbidimetric assay with an IC 50 of 200 μg gallic acid equivalents (GAE) perassay) [∼230 μg DW] whereas the known inhibitor, Orlistat, gave an IC 50 at 0.4 μg per assay. A phlorotannin-enriched fraction (TRF) purified from the PRE was more potent with an IC 50 = 60 μg GAE per assay (∼65 μg DW). When the assay was started by the addition of lipase, both Orlistat and TRF were much less effective which suggests that pre-incubation of enzyme and inhibitor improved inhibition. Based on phenol content, water extracts from Ascophyllum were more potent lipase inhibitors than PRE (IC 50 ∼ 150 μg GAE per assay). However, this was equivalent to ∼580 μg DW and these extracts contained polysaccharides (e.g. alginate content = 110 μg mL -1 ) which may also contribute to inhibition. Indeed, a polysaccharide-enriched fraction obtained by ethanol precipitation gave an IC 50 of 1000 μg DW which was equivalent to 130 μg GAE and 420 μg alginate per assay. Therefore a >3 fold increase in alginate content did not markedly improve inhibition. Re-precipitation increased alginate content and reduced polyphenol content but lipase inhibition was markedly reduced (i.e. IC 50 at ∼1100 μg DW per assay, 700 μg alginate and 25 μg GAE). Purifying the polysaccharide fraction by ion exchange removed all phenolics but the IC 50 increased to >2500 μg DW, equivalent to >1970 μg alginate per assay. In conclusion, polysaccharides and phlorotannins may inhibit lipase in an additive fashion, with phlorotannins apparently more effective in vitro. However, interactions between these components may be important when food products containing this edible seaweed are consumed.

Inhibition of aldose reductase activity by Cannabis sativa chemotypes extracts with high content of cannabidiol or cannabigerol.

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Smeriglio, Antonella; Giofrè, Salvatore V; Galati, Enza M; Monforte, Maria T; Cicero, Nicola; D'Angelo, Valeria; Grassi, Gianpaolo; Circosta, Clara

2018-02-07

Aldose reductase (ALR2) is a key enzyme involved in diabetic complications and the search for new aldose reductase inhibitors (ARIs) is currently very important. The synthetic ARIs are often associated with deleterious side effects and medicinal and edible plants, containing compounds with aldose reductase inhibitory activity, could be useful for prevention and therapy of diabetic complications. Non-psychotropic phytocannabinoids exert multiple pharmacological effects with therapeutic potential in many diseases such as inflammation, cancer, diabetes. Here, we have investigated the inhibitory effects of extracts and their fractions from two Cannabis sativa L. chemotypes with high content of cannabidiol (CBD)/cannabidiolic acid (CBDA) and cannabigerol (CBG)/cannabigerolic acid (CBGA), respectively, on human recombinant and pig kidney aldose reductase activity in vitro. A molecular docking study was performed to evaluate the interaction of these cannabinoids with the active site of ALR2 compared to known ARIs. The extracts showed significant dose-dependent aldose reductase inhibitory activity (>70%) and higher than fractions. The inhibitory activity of the fractions was greater for acidic cannabinoid-rich fractions. Comparative molecular docking results have shown a higher stability of the ALR2-cannabinoid acids complex than the other inhibitors. The extracts of Cannabis with high content of non-psychotropic cannabinoids CBD/CBDA or CBG/CBGA significantly inhibit aldose reductase activity. These results may have some relevance for the possible use of C. sativa chemotypes based preparations as aldose reductase inhibitors. Copyright © 2018 Elsevier B.V. All rights reserved.

Avaliação da inibição da acetilcolinesterase por extratos de plantas medicinais Evaluation of acetylcholinesterase inhibition by extracts from medicinal plants

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W.M. Mota

2012-01-01

Brazil. E. velutina aqueous extract did not have inhibitory activity, while Maytenus rigida aqueous extract showed low inhibitory activity (percentage of inhibition of 4%. Moderate inhibitory activity was detected for Phoradendron piperoides aqueous extract (percentage of inhibition of 40%, while V. agnus castus L. extract inhibited 74% AChE activity, characterized as a potent inhibitory activity. Evaluation of AChE inhibition by ethanol extracts indicated that the extracts from Sideroxylon obtusifolium, Erythrina velutina, Vitex agnus-castus L., Phoradendron piperoides, Chrysobalanus icaco, Bauhinia cheilantha and Orbignya phalerata did not show inhibitory activity. A low inhibitory activity was observed for ethanol extracts from Maytenus rigida (percentage of inhibition of 7% and Hyptis fruticosa (percentage of inhibition of 11%. Moringa oleifera ethanol extract showed moderate inhibitory activity, inhibiting 47% of the activity of this enzyme. None of the tested ethanol extracts showed potent inhibitory activity against AChE. Results of the studies of acetylcholinesterase inhibition allow the conclusion that V. agnus-castus L. aqueous extract showed to be most effective in inhibiting AChE. This result reinforces the need for continued study of this extract in order to make the partition and the purification of fractions to isolate the molecule responsible for the observed inhibition.

Inhibition of DNA synthesis in cultured lymphocytes and tumor cells by extracts of betel nut, tobacco, and miang leaf, plant substances associated with cancer of the ororespiratory epithelium.

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Yang, J A; Huber, S A; Lucas, Z J

1979-12-01

The high incidence of oropharyngeal, esophageal, and laryngeal cancers in certain parts of the world has been ascribed to conjugated tannins found in certain folk medicinal herbs. We extracted miang leaf and betel nut with phosphate-buffered saline (0.14 M NaCl, 0.15 M potassium phosphate buffer, pH 7.4) and found that the extracts inhibited [3H]thymidine incorporation by phytohemagglutinin-stimulated human lymphocytes and by rat mammary tumor and mouse L-cells in logarithmic growth. Pretreating the lymphocytes for 1 or 4 hr with the extracts inhibited phytohemagglutinin-induced thymidine incorporation 72 hr later. At concentrations of 2.5 volumes % or lower, miang and betel nut extracts inhibited thymidine incorporation by 40 to 98% without any apparent signs of toxicity as demonstrated by the 66Rb equilibrium assay. In addition, neither extract inhibited cytotoxicity of rat mammary tumor cells by immune syngeneic spleen cells. The molecular weights of the inhibitory factors were between 1,000 and 10,000 daltons as determined by ultrafiltration and were unaffected by boiling for 3 min or by treatment with alcohol and, therefore, are probably not proteins. This in vitro demonstration of inhibition of DNA synthesis by these plant extracts presumably enriched for conjugated tannins may relate to inhibition of growth of rats and chicks fed conjugated tanin-contaminated sorghum feed. The carcinogenic potential of either these extracts or conjugated tannins is not yet established.

Syringic Acid Extracted from Herba dendrobii Prevents Diabetic Cataract Pathogenesis by Inhibiting Aldose Reductase Activity

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Xiaoyong Wei

2012-01-01

Full Text Available Objective. Effects of Syringic acid (SA extracted from dendrobii on diabetic cataract (DC pathogenesis were explored. Methods. Both in vitro and in vivo DC lens models were established using D-gal, and proliferation of HLEC exposed to SA was determined by MMT assay. After 60-day treatment with SA, rat lens transparency was observed by anatomical microscopy using a slit lamp. SA protein targets were extracted and isolated using 2-DE and MALDI TOF/TOF. AR gene expression was investigated using qRT-PCR. Interaction sites and binding characteristics were determined by molecule-docking techniques and dynamic models. Results. Targeting AR, SA provided protection from D-gal-induced damage by consistently maintaining lens transparency and delaying lens turbidity development. Inhibition of AR gene expression by SA was confirmed by qRT-PCR. IC50 of SA for inhibition of AR activity was 213.17 μg/mL. AR-SA binding sites were Trp111, His110, Tyr48, Trp20, Trp79, Leu300, and Phe122. The main binding modes involved hydrophobic interactions and hydrogen bonding. The stoichiometric ratio of non-covalent bonding between SA and AR was 1.0 to 13.3. Conclusion. SA acts to prevent DC in rat lenses by inhibiting AR activity and gene expression, which has potential to be developed into a novel drug for therapeutic management of DC.

IN VITRO ANTIOXIDANT AND α-AMYLASE INHIBITION ACTIVITIES OF PANCHSAKAR CHURNA

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Ashok Kumar B.S.

2013-12-01

Full Text Available Panchsakar Churna is the composition of Cassia angustifolia, Terminalia chebula, Zingiber officinale, Foeniculum vulgare and Saindhava lavana. Aqueous extract of churna was used to investigate antioxidant activity by ferrous ion chelating assay and ferric reducing power and alpha amylase inhibition activity by dinitrosalicylic acid method (DNSA. Aqueous extract of churna showed maximum ferrous chelating activity - 42.01 and ferric reducing power - 1.5 and 83.33 % of inhibition protein denaturation at 1000 µg/ml. Panchsakar churna showed significant antioxidant and alpha amylase inhibition activities.

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

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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.

Inhibition of Cytochrome P450 (CYP3A4) Activity by Extracts from 57 Plants Used in Traditional Chinese Medicine (TCM)

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Ashour, Mohamed L; Youssef, Fadia S; Gad, Haidy A; Wink, Michael

2017-01-01

Background: Herbal medicine is widely used all over the world for treating various health disorders. It is employed either alone or in combination with synthetic drugs or plants to be more effective. Objective: The assessment of the effect of both water and methanol extracts of 57 widely used plants from Traditional Chinese Medicine (TCM) against the main phase I metabolizing enzyme CYP3A4 in vitro for the first time. Materials and Methods: The inhibition of cytochrome P450 activity was evaluated using a luminescence assay. The principal component analysis (PCA) was used to correlate the inhibitory activity with the main secondary metabolites present in the plant extracts. Molecular modeling studies on CYP3A4 (PDB ID 4NY4) were carried out with 38 major compounds present in the most active plant extracts to validate the observed inhibitory effect. Results: Aqueous extracts of Acacia catechu, Andrographis paniculata, Arctium lappa, Areca catechu, Bupleurum marginatum, Chrysanthemum indicum, Dysosma versipellis, and Spatholobus suberectus inhibited CYP3A4 is more than 85% (at a dose of 100 μg/mL). The corresponding methanol extracts of A. catechu, A. paniculata, A. catechu, Mahonia bealei, and Sanguisorba officinalis inhibited the enzyme by more than 50%. Molecular modeling studies revealed that two polyphenols, namely hesperidin and rutin, revealed the highest fitting scores in the active sites of the CYP3A4 with binding energies equal to -74.09 and -71.34 kcal/mol, respectively. Conclusion: These results provide evidence that many TCM plants can inhibit CYP3A4, which might cause a potential interference with the metabolism of other concomitantly administered herbs or drugs. SUMMARY In this study, the inhibitory activity of the aqueous and methanol extracts of 57 widely used plants from Traditional Chinese Medicine (TCM) against the main phase I metabolizing enzyme CYP3A4 was tested in vitro for the first time.Aqueous extracts of Acacia catechu, Andrographis

Extract of Stellerachamaejasme L(ESC) inhibits growth and metastasis of human hepatocellular carcinoma via regulating microRNA expression.

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Liu, Xiaoni; Wang, Shuang; Xu, Jianji; Kou, Buxin; Chen, Dexi; Wang, Yajie; Zhu, Xiaoxin

2018-03-20

MicroRNAs(miRNAs)are involved in the initiation and progression of hepatocellular carcinoma. ESC, an extract of Stellerachamaejasme L, had been confirmed as a potential anti-tumor extract of Traditional Chinese Medicine. In light of the important role of miRNAs in hepatocellular carcinoma, we questioned whether the inhibitory effects of ESC on hepatocellular carcinoma (HCC) were associated with miRNAs. The proliferation inhibition of ESC on HCC cells was measured with MTT assay. The migration inhibition of ESC on HCC cells was measured with transwell assay. The influences of ESC on growth and metastasis inhibition were evaluated with xenograft tumor model of HCC. Protein expressions were measured with western blot and immunofluorescence methods and miRNA profiles were detected with miRNA array. Differential miRNA and target mRNAs were verified with real-time PCR. The results showed that ESC could inhibit proliferation and epithelial mesenchymal transition (EMT) in HCC cells in vitro and tumor growth and metastasis in xenograft models in vivo. miRNA array results showed that 69 differential miRNAs in total of 429 ones were obtained in MHCC97H cells treated by ESC. hsa-miR-107, hsa-miR-638, hsa-miR-106b-5p were selected to be validated with real-time PCR method in HepG2 and MHCC97H cells. Expressions of hsa-miR-107 and hsa-miR-638 increased obviously in HCC cells treated by ESC. Target genes of three miRNAs were also validated with real-time PCR. Interestingly, only target genes of hsa-miR-107 changed greatly. ESC downregulated the MCL1, SALL4 and BCL2 gene expressions significantly but did not influence the expression of CACNA2D1. The findings suggested ESC regressed growth and metastasis of human hepatocellular carcinoma via regulating microRNAs expression and their corresponding target genes.

Extracts Obtained from Pterocarpus angolensis DC and Ziziphus mucronata Exhibit Antiplasmodial Activity and Inhibit Heat Shock Protein 70 (Hsp70 Function

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Tawanda Zininga

2017-07-01

Full Text Available Malaria parasites are increasingly becoming resistant to currently used antimalarial therapies, therefore there is an urgent need to expand the arsenal of alternative antimalarial drugs. In addition, it is also important to identify novel antimalarial drug targets. In the current study, extracts of two plants, Pterocarpus angolensis and Ziziphus mucronata were obtained and their antimalarial functions were investigated. Furthermore, we explored the capability of the extracts to inhibit Plasmodium falciparum heat shock protein 70 (Hsp70 function. Heat shock protein 70 (Hsp70 are molecular chaperones whose function is to facilitate protein folding. Plasmodium falciparum the main agent of malaria, expresses two cytosol-localized Hsp70s: PfHsp70-1 and PfHsp70-z. The PfHsp70-z has been reported to be essential for parasite survival, while inhibition of PfHsp70-1 function leads to parasite death. Hence both PfHsp70-1 and PfHsp70-z are potential antimalarial drug targets. Extracts of P. angolensis and Z. mucronata inhibited the basal ATPase and chaperone functions of the two parasite Hsp70s. Furthermore, fractions of P. angolensis and Z. mucronata inhibited P. falciparum 3D7 parasite growth in vitro. The extracts obtained in the current study exhibited antiplasmodial activity as they killed P. falciparum parasites maintained in vitro. In addition, the findings further suggest that some of the compounds in P. angolensis and Z. mucronata may target parasite Hsp70 function.

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.

Inhibition of Cyclic Adenosine Monophosphate-Specific Phosphodiesterase by Various Food Plant-Derived Phytotherapeutic Agents.

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Röhrig, Teresa; Pacjuk, Olga; Hernández-Huguet, Silvia; Körner, Johanna; Scherer, Katharina; Richling, Elke

2017-11-04

Background: Phosphodiesterases (PDEs) play a major role in the regulation of cyclic adenosine monophosphate (cAMP)- and cyclic guanosine monophosphate (cGMP)-mediated pathways. Their inhibitors exhibit anti-inflammatory, vasodilatory and antithrombotic effects. Therefore, consumption of foods with PDE-inhibiting potential may possess beneficial influence on the risk of cardiovascular diseases. Methods: Four plant extracts ( Arbutus unedo , Camellia sinensis , Cynara scolymus , Zingiber officinale ) with promising ingredient profiles and physiological effects were tested for their ability to inhibit cAMP-specific PDE in vitro in a radioactive assay. Results: Strawberry tree fruit ( Arbutus unedo ) and tea ( Camellia sinensis ) extracts did not inhibit PDE markedly. Alternatively, artichoke ( Cynara scolymus ) extract had a significant inhibitory influence on PDE activity (IC 50 = 0.9 ± 0.1 mg/mL) as well as its flavone luteolin (IC 50 = 41 ± 10 μM) and 3,4-dicaffeoylquinic acid (IC 50 > 1.0 mM). Additionally, the ginger ( Zingiber officinale ) extract and one of its constituents, [6]-gingerol, significantly inhibited PDE (IC 50 = 1.7 ± 0.2 mg/mL and IC 50 > 1.7 mM, respectively). Crude fractionation of ginger extract showed that substances responsible for PDE inhibition were in the lipoid fraction (IC 50 = 455 ± 19 μg/mL). Conclusions: A PDE-inhibitory effect was shown for artichoke and ginger extract. Whether PDE inhibition in vivo can be achieved through ingestion of artichoke or ginger extracts leading to physiological effects concerning cardiovascular health should be addressed in future research.

Inhibition of Cyclic Adenosine Monophosphate-Specific Phosphodiesterase by Various Food Plant-Derived Phytotherapeutic Agents

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Teresa Röhrig

2017-11-01

Full Text Available Background: Phosphodiesterases (PDEs play a major role in the regulation of cyclic adenosine monophosphate (cAMP- and cyclic guanosine monophosphate (cGMP-mediated pathways. Their inhibitors exhibit anti-inflammatory, vasodilatory and antithrombotic effects. Therefore, consumption of foods with PDE-inhibiting potential may possess beneficial influence on the risk of cardiovascular diseases. Methods: Four plant extracts (Arbutus unedo, Camellia sinensis, Cynara scolymus, Zingiber officinale with promising ingredient profiles and physiological effects were tested for their ability to inhibit cAMP-specific PDE in vitro in a radioactive assay. Results: Strawberry tree fruit (Arbutus unedo and tea (Camellia sinensis extracts did not inhibit PDE markedly. Alternatively, artichoke (Cynara scolymus extract had a significant inhibitory influence on PDE activity (IC50 = 0.9 ± 0.1 mg/mL as well as its flavone luteolin (IC50 = 41 ± 10 μM and 3,4-dicaffeoylquinic acid (IC50 > 1.0 mM. Additionally, the ginger (Zingiber officinale extract and one of its constituents, [6]-gingerol, significantly inhibited PDE (IC50 = 1.7 ± 0.2 mg/mL and IC50 > 1.7 mM, respectively. Crude fractionation of ginger extract showed that substances responsible for PDE inhibition were in the lipoid fraction (IC50 = 455 ± 19 μg/mL. Conclusions: A PDE-inhibitory effect was shown for artichoke and ginger extract. Whether PDE inhibition in vivo can be achieved through ingestion of artichoke or ginger extracts leading to physiological effects concerning cardiovascular health should be addressed in future research.

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.

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

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Beatriz Badilla

2006-06-01

Full Text Available 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. Rev. Biol. Trop. 54(2: 245-252. Epub 2006 Jun 01.Se investigó la capacidad de los extractos de las hojas de Urera baccifera, Loasa speciosa, Urtica leptuphylla, Chaptalia nutans, Satureja viminea y de la raíz de Uncaria tomentosa para inhibir el edema inducido por el veneno de Bothrops asper por métodos pletismométricos. Los grupos de ratas fueron inyectados intraperitonealmente con varias dosis de cada extracto y una hora mas tarde se inyectó veneno por vía subcutánea en la pata trasera derecha de la rata. Se evaluó el edema en distintos intervalos de tiempo. Los resultados muestran que la actividad edematogénica fue inhibida en los animales que recibieron los extractos de raíz de U. tomentosa, hojas de C. nutans y L. speciosa. Los extractos de hojas de U. baccifera mostraron leve inhibición del efecto del veneno. El extracto de hojas de S. viminea y en menor grado el de U. leptuphylla indujeron un efecto pro inflamatorio.

Antioxidant activities of aqueous extract from Stevia rebaudiana stem waste to inhibit fish oil oxidation and identification of its phenolic compounds.

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Yu, Hui; Yang, Gangqiang; Sato, Minoru; Yamaguchi, Toshiyasu; Nakano, Toshiki; Xi, Yinci

2017-10-01

We investigated the potential for exploiting Stevia rebaudiana stem (SRS) waste as a source of edible plant-based antioxidants finding for the first time that the hot water extract of SRS had significantly higher antioxidant activity against fish oil oxidation than that of the leaf, despite SRS extract having lower total phenolic content, DPPH radical scavenging activity and ORAC values. To locate the major antioxidant ingredients, SRS extract was fractionated using liquid chromatography. Five phenolic compounds (primary antioxidant components in activity-containing fractions) were identified by NMR and HR-ESI-MS: vanillic acid 4-O-β-d-glucopyranoside (1), protocatechuic acid (2), caffeic acid (3), chlorogenic acid (4) and cryptochlorogenic acid (5). Further analysis showed that, among compounds 2-5, protocatechuic acid had the highest capacity to inhibit peroxides formation, but exhibited the lowest antioxidant activities in DPPH and ORAC assays. These results indicate that SRS waste can be used as strong natural antioxidant materials in the food industry. Copyright © 2017 Elsevier Ltd. All rights reserved.

Ethanol extract of mango (Mangifera indica L.) peel inhibits α-amylase and α-glucosidase activities, and ameliorates diabetes related biochemical parameters in streptozotocin (STZ)-induced diabetic rats.

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Gondi, Mahendranath; Prasada Rao, U J S

2015-12-01

Peel is a major by-product during processing of mango fruit into pulp. Recent report indicates that the whole peel powder ameliorated diabetes. In the present study, ethanolic extract of mango peel was analysed for its bioactive compounds, evaluated for α-amylase and α-glucosidase inhibitory properties, oral glucose tolerance test, antioxidant properties, plasma insulin level and biochemical parameters related to diabetes. In addition to gallic and protocatechuic acids, the extract also had chlorogenic and ferulic acids, which were not reported earlier in mango peel extracts. The peel extract inhibited α-amylase and α-glucosidase activities, with IC50 values of 4.0 and 3.5 μg/ml. Ethanolic extract of peel showed better glucose utilization in oral glucose tolerance test. Treatment of streptozotocin-induced diabetic rats with the extract decreased fasting blood glucose, fructosamine and glycated hemoglobin levels, and increased plasma insulin level. Peel extract treatment decreased malondialdehyde level, but increased the activities of antioxidant enzymes significantly in liver and kidney compared to diabetic rats. These beneficial effects were comparable to metformin, but better than gallic acid treated diabetic rats. The beneficial effects of peel extract may be through different mechanism like increased plasma insulin levels, decreased oxidative stress and inhibition of carbohydrate hydrolyzing enzyme activities by its bioactive compounds. Thus, results suggest that the peel extract can be a potential source of nutraceutical or can be used in functional foods and this is the first report on antidiabetic properties of mango peel extract.

Morusinol extracted from Morus alba inhibits arterial thrombosis and modulates platelet activation for the treatment of cardiovascular disease.

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Lee, Jung-Jin; Yang, Hyun; Yoo, Yeong-Min; Hong, Seong Su; Lee, Dongho; Lee, Hyun-Jung; Lee, Hak-Ju; Myung, Chang-Seon; Choi, Kyung-Chul; Jeung, Eui-Bae

2012-01-01

Morus alba (white mulberry) has been used in traditional Chinese medicine as an anti-headache, diuretic, expectorant, and anti-diabetic agent. In previous studies, extracts of Morus alba demonstrated favorable biological properties, such as antioxidant activity, suppression of lipoxygenase (LOX)-1, cytotoxicity against cancer cells, and inhibition of the invasion and migration of cancer cells. This study further evaluated the effects of morusinol, a flavonoid derived from Morus alba root bark, on platelet aggregation and thromboxane B(2) (TXB(2) formation in vitro and thrombus formation in vivo. The antiplatelet potential of morusinol was measured using in vitro rabbit platelet aggregation and TXB(2) formation assays. Arterial thrombus formation was investigated using an in vivo ferric chloride (FeCl(3)-induced thrombosis model. Morusinol significantly inhibited collagen- and arachidonic acid-induced platelet aggregation and TXB(2) formation in cultured platelets in a concentration-dependent manner. Thrombus formation was reduced by 32.1, 42.0, and 99.0% for collagen-induced TXB(2) formation, and 8.0, 24.1, and 29.2% for arachadonic acid-induced TXB(2) formation, with 5, 10, and 30 µg/mL morusinol, respectively. Moreover, oral morusinol (20 mg/kg) or aspirin (20 mg/kg) for three days significantly increased the time to occlusion in vivo by 20.3±5.0 or 6.8±2.9 min, respectively, compared with the control (1% CMC, carboxymethyl cellulose). Taken together, these results indicate that morusinol may significantly inhibit arterial thrombosis in vivo due to antiplatelet activity. Thus, morusinol may exert beneficial effects on transient ischemic attacks or stroke via the modulation of platelet activation.

CYTOTOXIC, α-CHYMOTRYPSIN AND UREASE INHIBITION ACTIVITIES OF THE PLANT Heliotropium dasycarpum L.

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Ghaffari, Muhammad Abuzar; Chaudhary, Bashir Ahmed; Uzair, Muhammad; Ashfaq, Khuram

2016-01-01

The aim of this study was to investigate Cytotoxic, α-Chymotrypsin and Urease inhibition activities of the plant Heliotropium dasycarpum . Dichloromethane and methanol extracts of the plant were evaluated for cytotoxic, α-Chymotrypsin and Urease inhibition by using in vivo Brine Shrimp lethality bioassay and in vitro enzymatic inhibition assays respectively. The methanol extract of the plant exhibited significant cytotoxic activity. Out of 30 brine shrimp larvae, 2 (6%), 26 (86%) and 28 (93%) larvae were survived at concentration of 1000μg/ml, 100μg/ml and 10μg/ml respectively with LD50; 215.837. Similarly 21 (70%), 25 (83%), 29 (96%) larvae were survived of dichloromethane plant extract with LD50; 6170.64. The methanol and dichloromethane extract exhibited 10.50±0.18% and 41.51±0.15% α-chymotrypsin enzyme inhibition respectively with IC 50 values of greater than 500 μmol. The methanol extract showed 24.39±0.21% Urease enzyme inhibition with IC 50 values of greater than 400 μmol While dichloromethane extract has 11.46±0.09% enzyme inhibition with IC 50 values of greater than 500 μmol. The results clearly indicated that Heliotropium dasycarpum has cytotoxic potential and enzyme inhibition properties. Further study is needed to screen out antitumor and anti-ulcerative agents.

Anti-inflammatory and antinociceptive properties of blueberry extract (Vaccinium corymbosum).

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Torri, Eliane; Lemos, Marivane; Caliari, Vinícius; Kassuya, Cândida A L; Bastos, Jairo K; Andrade, Sérgio F

2007-04-01

Blueberries are among the edible fruits that are recognized best for their potential health benefits. The crude extract from Vaccinium corymbosum was assessed in anti-inflammatory and antinociceptive models. The crude hydroalcoholic extract was administered orally at doses of 100, 200 or 300 mg kg (-1) for all the assays. In the carrageenan test, the crude extract reduced rat paw oedema by 9.8, 28.5 and 65.9%, respectively. For the histamine assay, the reductions of oedema were 70.1, 71.7 and 81.9%, respectively. In the myeloperoxidase (MPO) assay, 300 mg kg (-1) crude extract produced a significant inhibition of the MPO activity, at 6 h and 24 h after injection of carrageenan, by 42.8 and 46.2%, respectively. With the granulomatous tissue assay dexamethasone displayed significant activity, whereas the blueberry extract was inactive. For the abdominal constriction test, inhibitions of 49.0, 54.5, 53.5%, respectively, were observed for the crude extract, and 61.4% for indometacin. In the formalin test, the crude extract (200 and 300 mg kg (-1)) and indometacin inhibited only the second phase by 36.2, 35.3 and 45.8%, respectively. Considering that the crude extract of blueberry displayed antinociceptive and anti-inflammatory activity, its consumption may be helpful for the treatment of inflammatory disorders.

The enhanced inhibition of water extract of black tea under baking treatment on α-amylase and α-glucosidase.

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Tong, Da-Peng; Zhu, Ke-Xue; Guo, Xiao-Na; Peng, Wei; Zhou, Hui-Ming

2018-02-01

This paper studied the inhibition of water extract of natural or baked black tea on the activity of α-amylase and α- glucosidase. Baking treatment was found to be one effective way to enhance the inhibition of black tea on both α-amylase and α- glucosidase, and IC 50 of water extract of baked black tea (BBTWE) were 1.213mg/mL and 4.190mg/mL, respectively, while IC 50 of water extract of black tea (BTWE) were 1.723mg/mL and 6.056mg/mL, respectively. This study further studied the mechanism of the effect of water extract on α-amylase and α- glucosidase using HPLC, circular dichroism, and synchronous fluorescence. HPLC analysis of tea polyphenols showed that the content of tea polyphenols with low polarity increased after baking. In addition, BBTWE had higer abilty on decreasing the hydrophobicity of tryptophan residues than BTWE for both α-amylase and α- glucosidase.The increase of α-helix proportion of α-amylase when treated with BBTWE was more obvious than that when treated with BTWE. In a word, thermal process of baked foods may be beneficial for tea polyphenols to reduce the rate of starch digestion. Copyright © 2017 Elsevier B.V. All rights reserved.

Serviceberry [Amelanchier alnifolia (Nutt.) Nutt. ex. M. Roem (Rosaceae)] leaf extract inhibits mammalian α-glucosidase activity and suppresses postprandial glycemic response in a mouse model of diet-induced obesity and hyperglycemia.

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Zhang, Albert J; Rimando, Agnes M; Fish, Wilbert; Mentreddy, Srinivasa R; Mathews, Suresh T

2012-09-28

Serviceberry or Saskatoon berry [Amelanchier alnifolia (Nutt.) Nutt. ex. M. Roem (Rosaceae)], native to the North Glacier forests of the Rocky Mountains in Montana, has been used by the Blackfeet Indian tribe in alleviation of diabetes. Anecdotally, tea made from twigs and leaves have been used for optimum health and diabetes management. However, such traditional knowledge of the medicinal properties of Amelanchier alnifolia has not been validated by scientific studies. The goal of this study was to identify potential antidiabetic mechanisms of serviceberry. Serviceberry plant samples consisting of leaves, twigs, and leaves with berries were extracted and fractionated. Ethyl acetate and water fractions were tested for inhibition of α-glucosidase activity in vitro. Diet-induced obese, hyperglycemic C57Bl6 mice were administered serviceberry leaf extract prior to sucrose-, starch-, or glucose-loading to test for α-glucosidase inhibition and decreased post-prandial glycemic response. In the course of screening for potential antidiabetic mechanisms, serviceberry leaf extracts and subfractions demonstrated potent inhibitory activity against mammalian intestinal α-glucosidase activity (EC 3.2.1.20). Further, in an animal model of diet-induced obesity and hyperglycemia, serviceberry leaf subfraction demonstrated significant inhibition of intestinal α-glucosidase activity, and delayed the absorption of carbohydrates, resulting in significant lowering of post-prandial blood glucose concentrations, similar to the antidiabetic drug Acarbose™. These findings indicating that serviceberry leaf extract may lower post-prandial glycemic response corroborate traditional knowledge of the Blackfeet Indians of Montana, and potentially offer a complementary approach in the treatment of diabetes. Published by Elsevier Ireland Ltd.

Anticancer Effects of Salvia miltiorrhiza Alcohol Extract on Oral Squamous Carcinoma Cells

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Wen-Hung Wang

2017-01-01

Full Text Available Researchers have reported significant effects from Danshen (Salvia miltiorrhiza in terms of inhibiting tumor cell proliferation and promoting apoptosis in breast cancer, hepatocellular carcinomas, promyelocytic leukemia, and clear cell ovary carcinomas. Here we report our data indicating that Danshen extracts, especially alcohol extract, significantly inhibited the proliferation of the human oral squamous carcinoma (OSCC cell lines HSC-3 and OC-2. We also observed that Danshen alcohol extract activated the caspase-3 apoptosis executor by impeding members of the inhibitor of apoptosis (IAP family, but not by regulating the Bcl-2-triggered mitochondrial pathway in OSCC cells. Our data also indicate that the extract exerted promising effects in vivo, with HSC-3 tumor xenograft growth being suppressed by 40% and 69% following treatment with Danshen alcohol extract at 50 and 100 mg/kg, respectively, for 34 days. Combined, our results indicate appreciable anticancer activity and significant potential for Danshen alcohol extract as a natural antioxidant and herbal human oral cancer chemopreventive drug.

Antibacterial and antioxidant activities of Vaccinium corymbosum L. leaf extract

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Mehnaz Pervin

2013-12-01

Full Text Available Objective: To investigate antibacterial and antioxidant activity of the leaf extract of tropical medicinal herb and food plant Vaccinium corymbosum L. (V. corymbosum . Methods: Free radical scavenging activity on DPPH, ABTS, and nitrites were used to analyse phenolic and flavonoid contents of leaf extract. Other focuses included the determination of antioxidant enzymatic activity (SOD, CAT and GPx, metal chelating activity, reduction power, lipid peroxidation inhibition and the prevention of oxidative DNA damage. Antibacterial activity was determined by using disc diffusion method against seven strains of bacteria. Results: Results found that V. corymbosum leaf extract had significant antibacterial activity. The tested extract displayed the highest activity (about 23.18 mm inhibition zone against Salmonella typhymurium and the lowest antibacterial activity was observed against Enterococcus faecalis (about 14.08 mm inhibition zone at 10 mg/ disc. The IC 50 values for DPPH, ABTS and radical scavenging activity were 0.120, 0.049 and 1.160 mg/mL, respectively. V. corymbosum leaf extract also showed dose dependent reduction power, lipid peroxidation, DNA damage prevention and significant antioxidant enzymatic activity. Conclusions: These findings demonstrate that leaf extract of V. corymbosum could be used as an alternative therapy for antibiotic-resistant bacteria and help prevent various free radical related diseases.

Antibacterial and antioxidant activities of Vaccinium corymbosum L. leaf extract

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Pervin, Mehnaz; Hasnat, Md Abul; Lim, Beong Ou

2013-01-01

Objective To investigate antibacterial and antioxidant activity of the leaf extract of tropical medicinal herb and food plant Vaccinium corymbosum L. (V. corymbosum). Methods Free radical scavenging activity on DPPH, ABTS, and nitrites were used to analyse phenoic and flavonoid contents of leaf extract. Other focuses included the determination of antioxidant enzymatic activity (SOD, CAT and GPx), metal chelating activity, reduction power, lipid peroxidation inhibition and the prevention of oxidative DNA damage. Antibacterial activity was determined by using disc diffusion for seven strains of bacteria. Results Results found that V. corymbosum leaf extract had significant antibacterial activity. The tested extract displayed the highest activity (about 23.18 mm inhibition zone) against Salmonella typhymurium and the lowest antibacterial activity was observed against Enterococcus faecalis (about 14.08 mm inhibition zone) at 10 mg/ disc. The IC50 values for DPPH, ABTS and radical scavenging activity were 0.120, 0.049 and 1.160 mg/mL, respectively. V. corymbosum leaf extract also showed dose dependent reduction power, lipid peroxidation, DNA damage prevention and significant antioxidant enzymatic activity. Conclusions These findings demonstrate that leaf extract of V. corymbosum could be used as an alternative therapy for antibiotic-resistant bacteria and help prevent various free radical related diseases.

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.

[Antifungal effect of phenolic and carotenoids extracts from chiltepin (Capsicum annum var. glabriusculum) on Alternaria alternata and Fusarium oxysporum].

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Rodriguez-Maturino, Alfonso; Troncoso-Rojas, Rosalba; Sánchez-Estrada, Alberto; González-Mendoza, Daniel; Ruiz-Sanchez, Esau; Zamora-Bustillos, Roberto; Ceceña-Duran, Carlos; Grimaldo-Juarez, Onecimo; Aviles-Marin, Mónica

2015-01-01

The effect of phenolic and carotenoid extracts from chiltepin fruits on mycelial growth and the inhibition of conidial germination of Alternaria alternata and Fusarium oxysporum were investigated in the present work. Phenolic extracts inhibited mycelial growth of A.alternata by 38.46%, and significantly reduced conidial germination on the fifth day after treatment to 92% in relation to control. No significant changes were observed in the inhibition of mycelial growth in Fusarium oxysporum; however, the number of germinated conidia was reduced, showing 85% inhibition five days after treatment in relation to control. Moreover, carotenoid extracts showed 38.5% inhibition of mycelial growth and 85.3% inhibition of conidial germination of A.alternata, five days after treatment. Carotenoid extracts showed less inhibition of mycelial growth (20.3%) in F.oxysporum, with respect to A.alternata; while there was greater inhibition of conidial germination (96%) on the fifth day after treatment. Phenolic and carotenoid extracts from chiltepin may be a promising alternative as a natural fungicide against fungi of agricultural importance. Copyright © 2014 Asociación Argentina de Microbiología. Publicado por Elsevier España, S.L.U. All rights reserved.

Rhodiolae Kirliowii Radix et Rhizoma and Crataegus pinnatifida Fructus Extracts Effectively Inhibit BK Virus and JC Virus Infection of Host Cells

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San-Yuan Chen

2017-01-01

Full Text Available The human polyomaviruses BK (BKPyV and JC (JCPyV are ubiquitous pathogens long associated with severe disease in immunocompromised individuals. BKPyV causes polyomavirus-associated nephropathy and hemorrhagic cystitis, whereas JCPyV is the causative agent of the fatal demyelinating disease progressive multifocal leukoencephalopathy. No effective therapies targeting these viruses are currently available. The goal of this study was to identify Chinese medicinal herbs with antiviral activity against BKPyV and JCPyV. We screened extracts of Chinese medicinal herbs for the ability to inhibit hemagglutination by BKPyV and JCPyV virus-like particles (VLPs and the ability to inhibit BKPyV and JCPyV binding and infection of host cells. Two of the 40 herbal extracts screened, Rhodiolae Kirliowii Radix et Rhizoma and Crataegus pinnatifida Fructus, had hemagglutination inhibition activity on BKPyV and JCPyV VLPs and further inhibited infection of the cells by BKPyV and JCPyV, as evidenced by reduced expression of viral proteins in BKPyV-infected and JCPyV-infected cells after treatment with Rhodiolae Kirliowii Radix et Rhizoma or Crataegus pinnatifida Fructus extract. The results in this work show that both Rhodiolae Kirliowii Radix et Rhizoma and Crataegus pinnatifida Fructus may be sources of potential antiviral compounds for treating BKPyV and JCPyV infections.

Antioxidant effects of crude extracts from Baccharis species: inhibition of myeloperoxidase activity, protection against lipid peroxidation, and action as oxidative species scavenger

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Tiago O. Vieira

2011-05-01

Full Text Available The objective of this study was to show a comparison of the antioxidant properties of aqueous and ethanolic extracts obtained from Baccharis articulata (Lam. Pers., Baccharis trimera (Less. DC., Baccharis spicata (Lam. Baill. and Baccharis usterii Heering, Asteraceae, by several techniques covering a range of oxidant species and of biotargets. We have investigated the ability of the plant extracts to scavenge DPPH (1,1-diphenyl-2-picryl-hydrazyl free radical, action against lipid peroxidation of membranes including rat liver microsomes and soy bean phosphatidylcholine liposomes by ascorbyl radical and peroxynitrite. Hydroxyl radical scavenger activity was measured monitoring the deoxyribose oxidation. The hypochlorous acid scavenger activity was also evaluated by the prevention of protein carbonylation and finally the myeloperoxidase (MPO activity inhibition. The results obtained suggest that the Baccharis extracts studied present a significant antioxidant activity scavenging free radicals and protecting biomolecules from the oxidation. We can suggest that the supposed therapeutic efficacy of this plant could be due, in part, to these properties.

Inhibition of Group IIA Secretory Phospholipase A2 and its Inflammatory Reactions in Mice by Ethanolic Extract of Andrographis paniculata, a Well-known Medicinal Food

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Kishore, V.; Yarla, N. S.; Zameer, F.; Nagendra Prasad, M. N.; Santosh, M. S.; More, S. S.; Rao, D. G.; Dhananjaya, Bhadrapura Lakkappa

2016-01-01

Andrographis paniculata Nees is an important medicinal plant found in the tropical regions of the world, which has been traditionally used in Indian and Chinese medicinal systems. It is also used as medicinal food. A. paniculata is found to exhibit anti-inflammatory activities; however, its inhibitory potential on inflammatory Group IIA phospholipases A2 (PLA2) and its associated inflammatory reactions are not clearly understood. The aim of the present study is to evaluate the inhibitory/neutralizing potential of ethanolic extract of A. paniculata on the isolated inflammatory PLA2 (VRV-PL-VIIIa) from Daboii rusellii pulchella (belonging to Group IIA inflammatory secretory PLA2 [sPLA2]) and its associated edema-induced activities in Swiss albino mice. A. paniculata extract dose dependently inhibited the Group IIA sPLA2 enzymatic activity with an IC50 value of 10.3 ± 0.5 μg/ml. Further, the extract dose dependently inhibited the edema formation, when co-injected with enzyme indicating that a strong correlation exists between lipolytic and pro-inflammatory activities of the enzyme. In conclusion, results of this study shows that the ethanolic extract of A. paniculata effectively inhibits Group IIA sPLA2 and its associated inflammatory activities, which substantiate its anti-inflammatory properties. The results of the present study warranted further studies to develop bioactive compound (s) in ethanolic extract of A. paniculata as potent therapeutic agent (s) for inflammatory diseases. SUMMARY This study emphasis the anti-inflammatory effect of A. paniculata by inhibiting the inflammatory Group IIA sPLA2 and its associated inflammatory activities such as edema. It was found that there is a strong correlation between lipolytic activity and pro-inflammatory activity inhibition. Therefore, the study suggests that the extract processes potent anti-inflammatory agents, which could be developed as a potential therapeutic agent against inflammatory and related diseases

Release Profile and Inhibition Test of The Nanoparticles A. Paniculata Extract as Inhibitor of α-Glucosidase in The Process of Carbohydrates Breakdown Into Glucose Diabetes Mellitus

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Imansari, Farisa; Sahlan, Muhammad; Arbianti, Rita

2017-07-01

Andrographis paniculata (A.paniculata) contain the main active substances Andrographolide which helps lower glucose levels in diabetics by inhibiting the enzyme α-glucosidase. The ability of the extract A.paniculata in lowering glucose levels will increase with the technique encapsulation with a coating of composition Chitosan-STPP as a drug delivery to the target organ. This study aimed to get an overview of A.paniculata release profile of nanoparticles in a synthetic fluid media with various concentrations of coating and inhibition testing nasty shard extract in inhibiting the enzyme α-glucosidase. This research resulted in nanoparticles by coating efficiency and loading capacity of chitosan greatest variation of 2% and 1% STPP 60% and 46.29%. chitosan greatest variation of 2% and 1% STPP 60% and 46.29%. The ability of A.paniculata extracts as α-glucosidase enzyme inhibitors has been demonstrated in this study, the percent inhibition of 33.17%.

Elucidation of the Corrosion Inhibition of Mild Steel in 1.0 M HCl by Catechin Monomers from Commercial Green Tea Extracts

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Nofrizal, S.; Rahim, Afidah A.; Saad, Bahruddin; Bothi Raja, P.; Shah, Affaizza M.; Yahya, S.

2012-04-01

The inhibitive action of commercial green tea extracts on mild steel (MS) in a 1.0 M hydrochloric acid solution was investigated by weight loss, potentiodynamic polarization, and electrochemical impedance spectroscopy (EIS). A high-performance liquid chromatographic (HPLC) analysis showed conclusively that of the eight catechin monomers and caffeine found in the original extracts, only four components were responsible for the inhibition of MS. The decreasing adsorption capacity of monomers on MS is related to the stereochemistry of molecules and the number of phenolic groups, and it is as follows: epigallocatechin gallate > epicatechin gallate > epigallocatechin > epicatechin. Adsorption of green tea extract constituent was found to follow Langmuir adsorption isotherm and the calculated Gibb's free energy values indicated the physisorption of inhibitor over MS surface. Physisorption was supported well by the potential zero charge (PZC) and molecular surface energy-level calculations.

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

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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.

A comparative study of leaves extracts for corrosion inhibition effect on aluminium alloy in alkaline medium

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Namrata Chaubey

2017-12-01

Full Text Available This paper deals with the comparative inhibition study of some plants leaves extract namely Cannabis sativa (CS, Rauwolfia serpentina (RS, Cymbopogon citratus (CC, Annona squamosa (AS and Adhatoda vasica (AV on the corrosion of aluminium alloy (AA in 1 M NaOH. The corrosion tests were performance by using gravimetric, electrochemical impedance spectroscopy (EIS, potentiodynamic polarization and linear polarization resistance (LPR techniques. RS showed maximum inhibition efficiency (η%, 97% at 0.2 g L−1. Potentiodynamic polarization curves justified that all the inhibitors are mixed-type. Surface morphology of AA is carried by scanning electron microscopy (SEM and atomic force microscopy (AFM.

Traditional Chinese medicine herbal extracts of Cibotium barometz, Gentiana scabra, Dioscorea batatas, Cassia tora, and Taxillus chinensis inhibit SARS-CoV replication

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Chih-Chun Wen

2011-10-01

Full Text Available 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 (龍膽 lóng dǎn; the dried rhizome of Gentiana scabra, Dioscoreae Rhizoma (山藥 shān yào; the tuber of Dioscorea batatas, Cassiae Semen (決明子 jué míng zǐ; the dried seed of Cassia tora and Loranthi Ramus (桑寄生 sāng jì shēng; the dried stem, with leaf of Taxillus chinensis (designated as GSH, DBM, CTH and TCH, respectively, and two from Rhizoma Cibotii (狗脊 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.

Response surface methodology based extraction of Tribulus terrestris leads to an upsurge of antilithiatic potential by inhibition of calcium oxalate crystallization processes

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Kaushik, Jyoti; Tandon, Simran; Gupta, Varun; Nayyar, Jasamrit; Singla, Surinder Kumar; Tandon, Chanderdeep

2017-01-01

Tribulus terrestris has significant antilithiatic efficacy established via both in vitro as well as in vivo studies and is used in numerous anti-urolithiatic herbal formulations viz. Cystone, Uriflow, Uritone and Neeri. However, to fully utilize its antilithiatic potential, the influence of different extraction parameters on antilithiatic ability of T. terrestris aqueous extract needs elucidation. Thus, the current study was undertaken using statistically optimized extraction conditions for aqueous extract preparation. Response surface methodology was employed to observe the influence of three variables i.e. temperature (°C), time (h) and solid: liquid ratio (S: L) on the extraction yield (%) and protein content (mg/g) of T. terrestris aqueous extract. RSM results revealed that the high S:L ratio, low temperature and reduced incubation time were optimal conditions for aqueous extraction. Under such extraction conditions the protein content reached the value of 26.6±1.22 mg/g and the obtained extraction yield was 27.32±1.62%. The assessment of antilithiatic activity of 4 selected extracts (AE1-4), revealed enhanced nucleation and aggregation inhibition of calcium oxalate crystals with AE1 and AE2, which in addition significantly altered the size and morphology of calcium oxalate monohydrate (COM) crystals compared to AE3 and AE4. In vitro cell culture based studies on renal epithelial cells (MDCK, NRK-52E and PK 15) proved that the AE1 showed higher cytoprotective potency by increasing cell viability as compared to the oxalate treated group. The free radical scavenging activity of aqueous extract lowered the reactive oxygen specie’s induced damage and potentially reduced the signals of programmed cell death due to oxalate injury. In addition, modulation of the COM crystal morphology was enhanced by AE1 as compared to AE2. The FTIR and GC-MS analysis of AE1, showed the presence of biomolecules which could aid in the attenuation of lithiatic process. In the light

Response surface methodology based extraction of Tribulus terrestris leads to an upsurge of antilithiatic potential by inhibition of calcium oxalate crystallization processes.

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Kaushik, Jyoti; Tandon, Simran; Gupta, Varun; Nayyar, Jasamrit; Singla, Surinder Kumar; Tandon, Chanderdeep

2017-01-01

Tribulus terrestris has significant antilithiatic efficacy established via both in vitro as well as in vivo studies and is used in numerous anti-urolithiatic herbal formulations viz. Cystone, Uriflow, Uritone and Neeri. However, to fully utilize its antilithiatic potential, the influence of different extraction parameters on antilithiatic ability of T. terrestris aqueous extract needs elucidation. Thus, the current study was undertaken using statistically optimized extraction conditions for aqueous extract preparation. Response surface methodology was employed to observe the influence of three variables i.e. temperature (°C), time (h) and solid: liquid ratio (S: L) on the extraction yield (%) and protein content (mg/g) of T. terrestris aqueous extract. RSM results revealed that the high S:L ratio, low temperature and reduced incubation time were optimal conditions for aqueous extraction. Under such extraction conditions the protein content reached the value of 26.6±1.22 mg/g and the obtained extraction yield was 27.32±1.62%. The assessment of antilithiatic activity of 4 selected extracts (AE1-4), revealed enhanced nucleation and aggregation inhibition of calcium oxalate crystals with AE1 and AE2, which in addition significantly altered the size and morphology of calcium oxalate monohydrate (COM) crystals compared to AE3 and AE4. In vitro cell culture based studies on renal epithelial cells (MDCK, NRK-52E and PK 15) proved that the AE1 showed higher cytoprotective potency by increasing cell viability as compared to the oxalate treated group. The free radical scavenging activity of aqueous extract lowered the reactive oxygen specie's induced damage and potentially reduced the signals of programmed cell death due to oxalate injury. In addition, modulation of the COM crystal morphology was enhanced by AE1 as compared to AE2. The FTIR and GC-MS analysis of AE1, showed the presence of biomolecules which could aid in the attenuation of lithiatic process. In the light

Response surface methodology based extraction of Tribulus terrestris leads to an upsurge of antilithiatic potential by inhibition of calcium oxalate crystallization processes.

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Jyoti Kaushik

Full Text Available Tribulus terrestris has significant antilithiatic efficacy established via both in vitro as well as in vivo studies and is used in numerous anti-urolithiatic herbal formulations viz. Cystone, Uriflow, Uritone and Neeri. However, to fully utilize its antilithiatic potential, the influence of different extraction parameters on antilithiatic ability of T. terrestris aqueous extract needs elucidation. Thus, the current study was undertaken using statistically optimized extraction conditions for aqueous extract preparation. Response surface methodology was employed to observe the influence of three variables i.e. temperature (°C, time (h and solid: liquid ratio (S: L on the extraction yield (% and protein content (mg/g of T. terrestris aqueous extract. RSM results revealed that the high S:L ratio, low temperature and reduced incubation time were optimal conditions for aqueous extraction. Under such extraction conditions the protein content reached the value of 26.6±1.22 mg/g and the obtained extraction yield was 27.32±1.62%. The assessment of antilithiatic activity of 4 selected extracts (AE1-4, revealed enhanced nucleation and aggregation inhibition of calcium oxalate crystals with AE1 and AE2, which in addition significantly altered the size and morphology of calcium oxalate monohydrate (COM crystals compared to AE3 and AE4. In vitro cell culture based studies on renal epithelial cells (MDCK, NRK-52E and PK 15 proved that the AE1 showed higher cytoprotective potency by increasing cell viability as compared to the oxalate treated group. The free radical scavenging activity of aqueous extract lowered the reactive oxygen specie's induced damage and potentially reduced the signals of programmed cell death due to oxalate injury. In addition, modulation of the COM crystal morphology was enhanced by AE1 as compared to AE2. The FTIR and GC-MS analysis of AE1, showed the presence of biomolecules which could aid in the attenuation of lithiatic process. In

Direct contact between dendritic cells and bronchial epithelial cells inhibits T cell recall responses towards mite and pollen allergen extracts in vitro

DEFF Research Database (Denmark)

Papazian, Dick; Wagtmann, Valery R; Hansen, Soren

2015-01-01

(DCs), we have investigated recall T cell responses in allergic patients sensitized to house dust mite, grass, and birch pollen. Conclusions: Using allergen extract-loaded DCs to stimulate autologous allergen-specific T cell lines, we show that AEC-imprinted DCs inhibit T cell proliferation...... production of both Th1 and Th2 cytokines upon re-challenge. The inhibitory effects of AECs' contact with DCs were absent when allergen extract-loaded DCs had only been exposed to AECs supernatants, but present after direct contact with AECs. We conclude that direct contact between DCs and AECs inhibits T...

Herbal Extract SH003 Suppresses Tumor Growth and Metastasis of MDA-MB-231 Breast Cancer Cells by Inhibiting STAT3-IL-6 Signaling

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Youn Kyung Choi

2014-01-01

Full Text Available Cancer inflammation promotes cancer progression, resulting in a high risk of cancer. Here, we demonstrate that our new herbal extract, SH003, suppresses both tumor growth and metastasis of MDA-MB-231 breast cancer cells via inhibiting STAT3-IL-6 signaling path. Our new herbal formula, SH003, mixed extract from Astragalus membranaceus, Angelica gigas, and Trichosanthes kirilowii Maximowicz, suppressed MDA-MB-231 tumor growth and lung metastasis in vivo and reduced the viability and metastatic abilities of MDA-MB-231 cells in vitro. Furthermore, SH003 inhibited STAT3 activation, which resulted in a reduction of IL-6 production. Therefore, we conclude that SH003 suppresses highly metastatic breast cancer growth and metastasis by inhibiting STAT3-IL-6 signaling path.

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.

Chemical content and antimicrobial properties of three different extracts of Mentha pulegium leaves from Mugla Region, Turkey.

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Ceyhan-Güvensen, Nur; Keskin, Dilek

2016-11-01

The extract of ethanol, methanol and DMSO of pennyroyal leaves from Mugla Region (Turkey) were tested for antimicrobial activity against eleven bacterial and one yeast strain by disc diffusion method. Among the extracts assayed, the methanol extract of pennyroyal leaves exhibited significant antimicrobial activity against Salmonella typhimurium and Staphylococcus aureus with 20 mm diameter inhibition zone. The DMSO extract of pennyroyal leaves displayed significant activity against S.aureus (19 mm) and Bacillus subtilis (21mm) showing inhibition zone of 19 mm and 21 mm diameter, while the ethanolic extract showed significant antimicrobial activity against S.aureus (17mm) and Klebsiella pneumoniae (20mm) inhibition zones.? On comparint the MIC value of ethanol, methanol and DMSO leaf extract, methanolic extract of pennyroyal presented best activity (MIC 8 mg ml-1) against S. typhimurium CCM 583 and S.aureus ATCC 6538/P. Analyses of GC/MS determined eleven compounds viz., neophytadiene (69.95%), Pulejon 7.85%, Pinane 4.81%, Bicyclo (3.1.1 Heptane 2.6.6.6 trimethyl) 4.68%. In conclusion, methanolic extracts of M. pulegium showed antimicrobial activity because of high neophytadiene content.

Antifungal activity of root, bark, leaf and soil extracts of Androstachys ...

African Journals Online (AJOL)

Extracts of leaf, root, soil and bark of Androstachys johnsonii Prain (commonly called Lembobo ironwood) screened for antifungal activity had a significant inhibitory effect on the most of fungi tested in this investigation. Of the four fungi tested in the present study Fusarium solani was significantly inhibited by all extracts (that ...

Inhibition of the transcription factor c-Jun by the MAPK family, and not the NF-κB pathway, suggests that peanut extract has anti-inflammatory properties.

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Catalán, Úrsula; Fernández-Castillejo, Sara; Anglès, Neus; Morelló, Jose Ramón; Yebras, Martí; Solà, Rosa

2012-10-01

Tumor necrosis factor-α (TNF-α) is involved in inflammatory responses in atherosclerosis. We propose an in vitro cellular assay to evaluate the anti-inflammatory mechanisms of potential modifiers such as food extracts. In the current model we assessed an anti-inflammatory effect of polyphenol-rich peanut extract in lipopolysaccharide (LPS)-induced THP-1 monocytes. THP-1 monocytes were incubated with peanut extract (5, 25, 50 and 100 μg/mL) consisting of 39% flavonols, 37% flavanols and 24% phenolic acid (or BAY 11-7082 (5 μM) as experiment control) for 1 h and then stimulated with LPS (500 ng/mL) for 4 h. Cytotoxicity was measured as lactate dehydrogenase (LDH) activity release. NF-κB and MAPK family were determined by TransAm kit while TNF-α mRNA levels and its mRNA stability by RT-PCR. Intra- and extracellular TNF-α protein was measured by ELISA, and TNF-α converting enzyme (TACE) activity by a fluorimetric assay. Peanut extract inhibited the maximal LPS-induced extracellular TNF-α protein secretion by 18%, 29% and 47% at 25, 50 and 100 μg/mL, respectively (P<0.05). LPS stimulation revealed that 85% of TNF-α was released extracellularly while 15% remained intracellular. Peanut extract did not modify NF-κB but, instead, reduced c-Jun transcription factor activity (P<0.05), decreased TNF-α mRNA (albeit non-significantly) and had no effect on mRNA stability and TACE activity. Polyphenol-rich peanut extract reduces extracellular TNF-α protein by inhibiting c-Jun transcription factor from MAPK family, suggesting an anti-inflammatory effect. The proposed THP-1 monocyte model could be used to assess food extract impact (site and size effects) on the inflammation pathway. Copyright © 2012 Elsevier Ltd. All rights reserved.

Some plant extracts retarde nitrification in soil

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Abdul–Mehdi S. AL-ANSARI

2015-12-01

Full Text Available An incubation experiment was conducted to evaluate the effect of aqueous extracts of 17 plant materials on nitrification inhibition of urea- N in soil as compared with chemical inhibitor Dicyandiamide (DCD. Plant materials used in study were collected from different areas of Basrah province, south of Iraq. Aqueous extracts were prepared at ratio of 1:10 (plant material: water and added at conc. of 0.05, 0.10 and 0.20 ml g– 1 soil to loamy sand soil. DCD was added to soil at rate of 50 µg g-1 soil . Soil received urea at rate of 1000 µg N g-1 soil. Treated soils were incubated at 30 OC for 40 days. Results showed that application of all plant extracts, except those of casuarina, date palm and eucalyptus to soil retarded nitrification in soil. Caper, Sowthistle ,bladygrass and pomegranate extracts showed highest inhibition percentage (51, 42, 40 and 40 %, respectively and were found to be more effective than DCD (33 %. Highest inhibition was achieved by using those extracts at conc. of 0.1 ml g-1 soil after 10 days of incubation . Data also revealed that treated soil with these plant extracts significantly increased amount of NH4+–N and decreased amount of NO3-–N accumulation in soil compared with DCD and control treatments. Results of the study suggested a possibility of using aqueous extracts of some studied plants as potent nitrification inhibitor in soil.

Evaluation of antioxidant and antimicrobial activity of seaweed ( Sargassum sp.) extract: A study on inhibition of glutathione-S-transferase Activity

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Patra, J.K.; Rath, S.K.; Jena, K.B.; Rathod, V.K.; Thatoi, H.

In the present study, the free radical scavenging potentials (DPPH radical and hydroxyl radical), inhibition of lipid peroxidation, and glutathione-S-transferase and antimicrobial properties of Sargassum sp. extract were investigated. The tested...

Water extractable phytochemicals from Capsicum pubescens (tree pepper) inhibit lipid peroxidation induced by different pro-oxidant agents in brain

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Oboh, G.; Rocha, J.B.T.

2006-03-01

Reactive oxygen species (ROS) is the cause of neurodegenerative disorders such as Lou Gehrig's disease, Parkinson's disease and Huntington's disease; one practical way to prevent and manage neurodegenerative diseases is through the eating of food rich in antioxidants (dietary means). In this study, the antioxidant and neuroprotective properties of aqueous extract of ripe and unripe Capsicum pubescens (popularly known as tree pepper) on different pro-oxidant induced lipid peroxidation in Rat's brain (in vitro) is been investigated. Aqueous extract of freshly harvested pepper was prepared, and the total phenol content, vitamin C, ferric reducing antioxidant property (FRAP) and Fe (II) chelating ability was determined. In addition, the ability of the extracts to protect the Rat's brain against some pro-oxidant FeSO 4 , Sodium nitroprusside and Quinolinic acid) - induced oxidative stress was also determined. The results of the study revealed that ripe Capsicum pubescens had a significantly higher (P 2 O 2 induced decomposition of deoxyribose. Therefore, ripe and unripe Capsicum pubescens would inhibit lipid peroxidation in vitro. However, the ripe potent was a more potent inhibitor of lipid peroxidation, which is probably due to its higher vitamin C and phenol content, reducing power and Fe (II) chelating ability. (author)

[Inhibition of Linseed Oil Autooxidation by Essential Oils and Extracts from Spice Plants].

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Misharina, T A; Alinkina, E S; Terenina, M B; Krikunova, N I; Kiseleva, V I; Medvedeva, I B; Semenova, M G

2015-01-01

Clove bud essential oil, extracts from ginger, pimento and black pepper, or ascorbyl palmytate were studied as natural antioxidants for the inhibition of autooxidation of polyunsaturated fatty acids in linseed oil. Different methods were used to estimate antioxidant efficiency. These methods are based on the following parameters: peroxide values; peroxide concentration; content of degradation products of unsaturated fatty acid peroxides, which acted with thiobarbituric acid; diene conjugate content; the content of volatile compounds that formed as products of unsaturated fatty acid peroxide degradation; and the composition of methyl esters of fatty acids in samples of oxidized linseed oil.

In vivo inhibition of gastric acid secretion by the aqueous extract of Scoparia dulcis L. in rodents.

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Mesía-Vela, Sonia; Bielavsky, Monica; Torres, Luce Maria Brandão; Freire, Sonia Maria; Lima-Landman, Maria Teresa R; Souccar, Caden; Lapa, Antonio José

2007-05-04

The freeze-dried aqueous extract (AE) from the aerial parts of Scoparia dulcis was tested for its effects on experimental gastric hypersecretion and ulcer in rodents. Administration of AE to animals with 4h pylorus ligature potently reduced the gastric secretion with ED(50)s of 195 mg/kg (rats) and 306 mg/kg (mice). The AE also inhibited the histamine- or bethanechol-stimulated gastric secretion in pylorus-ligated mice with similar potency suggesting inhibition of the proton pump. Bio-guided purification of the AE yielded a flavonoid-rich fraction (BuF), with a specific activity 4-8 times higher than the AE in the pylorus ligature model. BuF also inhibited the hydrolysis of ATP by H(+),K(+)-ATPase with an IC(50) of 500 microg/ml, indicating that the inhibition of gastric acid secretion of Scoparia dulcis is related to the inhibition of the proton pump. Furthermore, the AE inhibited the establishment of acute gastric lesions induced in rats by indomethacin (ED(50)=313 mg/kg, p.o.) and ethanol (ED(50)=490 mg/kg, p.o.). No influence of the AE on gastrointestinal transit allowed discarding a possible CNS or a cholinergic interaction in the inhibition of gastric secretion by the AE. Collectively, the present data pharmacologically validates the popular use of Scoparia dulcis in gastric disturbances.

Evaluation of Asteraceae herbal extracts in the management of diabetes and obesity. Contribution of caffeoylquinic acids on the inhibition of digestive enzymes activity and formation of advanced glycation end-products (in vitro).

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Spínola, Vítor; Castilho, Paula C

2017-11-01

The study was performed to assess, for the first time, the in vitro anti-diabetic potential of ten Asteraceae plant extracts to inhibit the activity of digestive enzymes (α-amylase, α-, β-glucosidases and lipase) responsible for hydrolysis/digestion of sugar and lipids. Prevention of advanced glycation end-products (AGEs) formation was evaluated in bovine serum albumin/ribose glycation reaction model. The phytochemical profiles and caffeoylquinic acids (CQAs) contents were determined for the methanolic extract of each plant. Analyzed plant extracts exhibited significant inhibitory activity against key digestive enzymes linked to type II diabetes and obesity. A strong inhibition was observed for glucosidases and mild activity towards amylase and lipase (compared to reference compounds). Moreover, some extracts exhibited potent ability to prevent formation of AGEs, implicated in some diabetic complications. Caffeoylquinic acids were dominant in all plant extracts and findings demonstrate that these compounds are the most relevant hypoglycemic and anti-glycation agents. From the obtained results, Argyranthemum pinnatifidum, Helichrysum melaleucum, and Phagnalon lowei are good candidates for further development of phyto-pharmaceutical preparations as complementary therapy for diabetes and obesity control. Copyright © 2017 Elsevier Ltd. All rights reserved.

Reactor design for minimizing product inhibition during enzymatic lignocellulose hydrolysis: I. Significance and mechanism of cellobiose and glucose inhibition on cellulolytic enzymes

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Andric, Pavle; Meyer, Anne S.; Jensen, Peter Arendt

2010-01-01

Achievement of efficient enzymatic degradation of cellulose to glucose is one of the main prerequisites and one of the main challenges in the biological conversion of lignocellulosic biomass to liquid fuels and other valuable products. The specific inhibitory interferences by cellobiose and glucose...... on enzyme-catalyzed cellulose hydrolysis reactions impose significant limitations on the efficiency of lignocellulose conversion especially at high-biomass dry matter conditions. To provide the base for selecting the optimal reactor conditions, this paper reviews the reaction kinetics, mechanisms......, and significance of this product inhibition, notably the cellobiose and glucose inhibition, on enzymatic cellulose hydrolysis. Particular emphasis is put on the distinct complexity of cellulose as a substrate, the multi-enzymatic nature of the cellulolytic degradation, and the particular features of cellulase...

Novel biological properties of Oenothera paradoxa defatted seed extracts: effects on metallopeptidase activity.

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Kiss, Anna K; Derwińska, Małgorzata; Dawidowska, Anna; Naruszewicz, Marek

2008-09-10

In this study, for the first time, we used the in vitro metallopeptidase model for the identification of a potential novel activity of defatted evening primrose seed extracts. Prepared extracts of different polarity (aqueous, 60% ethanolic, isopropanolic, and 30% isopropanolic) at concentrations of 1.5-100 microg/mL exhibited a significant and dose dependent inhibition of three tested enzymes. The 50% inhibition of enzymes activity showed that aminopeptidase N (APN) was the enzyme affected to the greatest extent with IC50 at the level of 2.8 microg/mL and 2.9 microg/mL for aqueous and 30% isopropanolic extracts, respectively. The activity of neutral endopeptidase (NEP) was quite strongly inhibited by the extracts as well. The HPLC-DAD analysis and bioguided fractionation led to the identification of four active compounds: (-)-epicatechin gallate, proanthocyanidin B3, oenothein B, and penta-O-galloyl-beta-D-glucose (PGG). Oenothein B has been shown previously to inhibit metallopeptidases. The three other compounds are known to inhibit angiotensin-converting enzyme (ACE), but they have not been previously reported to inhibit the NEP and APN activity. PGG and procyanidins with different degrees of polymerization, as the dominating compounds in O. paradoxa seeds, seemed to play a role in the crude extract activity.

Evaluation of the antidiarrhoeal activity of the aqueous leaf extract of ...

African Journals Online (AJOL)

The results showed that the aqueous leaf extract of D. guineense caused a significant (P< 0.001) reduction in the number of stools and frequency of diarrhoea in castor oil induced diarrhoea in mice. The extract produced significant (P< 0.01) inhibition of intestinal transit with the dose of 400 mg/kg having the highest effect.

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

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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.

In vitro antidiabetic activity of various crude extracts of Boletus variipes

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Muniandy, Sutha; Fazry, Shazrul; Daud, Fauzi; Senafi, Sahidan

2015-09-01

Diabetes mellitus is a complex metabolic disease that progressively spread worldwide and difficult to treat due to various physical and metabolic complications. Current treatment using synthetic drugs has lead to various undesirable side effects. Here we determined the effect of Boletus variipes extracts on diabetes related enzymes. In this study, hot water, cold water and methanol extracts of B. variipes were utilized in order to assess their in vitro antidiabetic activity by measuring the effect on α-amylase and α-glucosidase enzyme. Hot water extract possessed the highest inhibition activity of α-amylase and α-glucosidase in a concentration dependent manner with the IC50 value 87 mg/mL and 89 mg/mL respectively. The methanol extract also showed inhibition activity of α-amylase and α-glucosidase but significantly lower than the hot water extract. Whereas cold water extract did not show any inhibition activity towards both the enzymes. Therefore, it is hypothesized that the hot water extract of Boletus variipes contains bioactive compound that can inhibit alpha-amylase and alpha-glucosidase enzyme activity. At the request of all authors of the paper an updated version was published on 11 May 2016. The original version identified the species of mushroom as Boletus variipes, but new findings have proved the species of mushroom to be Boletus qriseipurpureus. The species name has been updated throughout the revised version of this paper.

Antidiarrheal Activity of 80% Methanolic Leaf Extract of Justicia schimperiana

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Belay Mekonnen

2018-01-01

Full Text Available Background. Diarrhea is one of the leading causes of preventable death in developing countries and mainly affects children and infants. It has been reported that the leaf of Justicia schimperiana is used as an antidiarrheal agent in Libo Kemekem district, northwest Ethiopia. Method. The 80% methanolic leaf extract of J. schimperiana was evaluated for its activity against castor oil-induced diarrhea, enteropooling, and gastrointestinal motility in mice. Results. Significant reduction (p<0.001 in the total defecation and diarrheal drops was produced by all the test doses of the extract. Percentage inhibition of wet feces was 42.58, 65.07, and 74.96% at 100, 200, and 400 mg/kg doses of the extract, respectively. The extract also significantly inhibited castor oil-induced enteropooling at all test doses. The percent reduction in mean weight of intestinal contents was 66.96, 67.83, and 76.52% at 100, 200, and 400 mg/kg doses of the extract, respectively. The extract significantly reduced gastrointestinal movement of charcoal meal as well at 200 (p<0.01 and 400 mg/kg (p<0.001 doses. Conclusion. In conclusion, the methanolic leaf extract of J. schimperiana has an antidiarrheal activity and this supports the use of this plant in the treatment of diarrhea in the traditional settings.

Anti-oxidant and anti-inflammatory activity of leaf extracts and fractions of Mangifera indica.

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Mohan, C G; Deepak, M; Viswanatha, G L; Savinay, G; Hanumantharaju, V; Rajendra, C E; Halemani, Praveen D

2013-04-13

To evaluate the anti-oxidant and anti-inflammatory activity of leaf extracts and fractions of Mangifera indica in in vitro conditions. In vitro DPPH radical scavenging activity and lipoxygenase (LOX) inhibition assays were used to evaluate the anti-oxidant and anti-inflammatory activities respectively. Methanolic extract (MEMI), successive water extract (SWMI) and ethyl acetate fraction (EMEMI), n-butanol fraction (BMEMI) and water soluble fraction (WMEMI) of methanolic extract were evaluated along with respective reference standards. In in vitro DPPH radical scavenging activity, the MEMI, EMEMI and BMEMI have offered significant antioxidant activity with IC(50) values of 13.37, 3.55 and 14.19 μg/mL respectively. Gallic acid, a reference standard showed significant antioxidant activity with IC(50) value of 1.88 and found to be more potent compared to all the extracts and fractions. In in vitro LOX inhibition assay, the MEMI, EMEMI and BMEMI have showed significant inhibition of LOX enzyme activity with IC(50) values of 96.71, 63.21 and 107.44 μg/mL respectively. While, reference drug Indomethacin also offered significant inhibition against LOX enzyme activity with IC(50) of 57.75. Furthermore, MEMI was found to more potent than SWMI and among the fractions EMEMI was found to possess more potent antioxidant and anti-inflammatory activity. These findings suggest that the MEMI and EMEMI possess potent anti-oxidant and anti-inflammatory activities in in vitro conditions. Copyright © 2013 Hainan Medical College. Published by Elsevier B.V. All rights reserved.

Control of Rice Weevil, Sitophilus oryzae (L., in Stored Wheat Grains with Mesquite Plant, Prosopis juliflora (SW, D.C. Seed Extracts

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N.H. AI-Moajel

2004-06-01

Full Text Available The effectiveness of mesquite plant, Prosopis juliflora (SW D.C. (Family: Mimosaceae, seed extracts against rice weevil. Sitophilus oryzae (L, reared on wheat grains was investigated in the laboratory. The tested plant extracts of P. juliflora in petroleum ether, chloroform, and acetone, effectively controlled adults and their toxicity based on LC95 and LC5O values respectively was in order: acetone (12.0, 5.8ml/kg < pet ether (8.0, 4.1ml/kg chloroform (6.3, 2.2ml/kg. A highly significant oviposition deterency effect (P< 0.05 was found for all extracts at LC50 levels, while at LC95 levels, oviposition was nearly completely inhibited. Thus, progeny emergence was completely suppressed at Legs levels, also at LCSC, of acetone extract. Chlorofonn extract indicated a slow rate of degradation alter one month of storage (90% mortality. All tested plant extracts reduced weight loss in wheat grains after 45 days of storage, but chloroform extract was the most effective. Most treatments did not significantly affect water absorption but viability was significantly reduced. Petroleum ether and chloroform extracts caused a significant inhibition effect on acetyl choline esterase (AchE in adults while acetone extract caused a significant activation effect. All three different extracts, caused a significant activation effect on phosphases (AcP and AlkP, except for chloroform and acetone extract treatments which caused significant inhibition of AcP in adults. All extracts caused a significant decrease in protein and carbohydrate contents of adults, except the carbohydrate content of adults treated with acetone extract. There was a significant increase in lipid content in adults treated with all three extracts and significant increase of carbohydrate content only in adults treated with acetone extract.

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 Fe(2+)-induced lipid peroxidation in rat pancreas.

Science.gov (United States)

Adefegha, Stephen Adeniyi; Oboh, Ganiyu

2012-10-01

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 Fe(2+)-induced lipid peroxidation in rat pancreas in vitro. 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. 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 (Ppancreas in vitro. This study provides a biochemical rationale by which clove elicits therapeutic effect on type 2 diabetes.

Inhibitory potentials of phenolic-rich extracts from Bridelia ferruginea on two key carbohydrate-metabolizing enzymes and Fe2+-induced pancreatic oxidative stress.

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Afolabi, Olakunle Bamikole; Oloyede, Omotade Ibidun; Agunbiade, Shadrack Oludare

2018-05-01

The current study was designed to evaluate the various antioxidant potentials and inhibitory effects of phenolic-rich leaf extracts of Bridelia ferruginea (BF) on the in vitro activities of some key enzymes involved in the metabolism of carbohydrates. In this study, BF leaf free and bound phenolic-rich extracts were used. We quantified total phenolic and flavonoid contents, and evaluated several antioxidant activities using assays for ferric reducing antioxidant power, total antioxidant activity (phosphomolybdenum reducing ability), 1,1-diphenyl-2-picrylhydrazyl and thiobarbituric acid reactive species. Also, extracts were tested for their ability to inhibit α-amylase and α-glucosidase activity. The total phenolic and total flavonoid contents in the free phenolic extract of BF were significantly greater than in the bound phenolic extract. Also, all the antioxidant activities considered were significantly greater in the free phenolic extract than in the bound phenolic extract. In the same vein, the free phenolic-rich extract had a significantly higher percentage inhibition against α-glucosidase activity (IC 50  = 28.5 µg/mL) than the bound phenolic extract (IC 50  = 340.0 µg/mL). On the contrary, the free phenolic extract (IC 50  = 210.0 µg/mL) had significantly lower inhibition against α-amylase than the bound phenolic-rich extract (IC 50  = 190.0 µg/mL). The phenolic-rich extracts of BF leaves showed antioxidant potentials and inhibited two key carbohydrate-metabolizing enzymes in vitro. Copyright © 2018 Shanghai Changhai Hospital. Published by Elsevier B.V. All rights reserved.

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

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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.

Curcumin longa extract-loaded nanoemulsion improves the survival of endotoxemic mice by inhibiting nitric oxide-dependent HMGB1 release.

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Ahn, Min Young; Hwang, Jung Seok; Lee, Su Bi; Ham, Sun Ah; Hur, Jinwoo; Kim, Jun Tae; Seo, Han Geuk

2017-01-01

High mobility group box 1 (HMGB1) is a well-known damage-related alarmin that participates in cellular inflammatory responses. However, the mechanisms leading to HMGB1 release in inflammatory conditions and the therapeutic agents that could prevent it remain poorly understood. This study attempted to examine whether the Curcumin longa herb, which is known to have anti-inflammatory property, can modulate cellular inflammatory responses by regulating HMGB1 release. The murine macrophage RAW264.7 cells were treated with lipopolysaccharide (LPS) and/or a C. longa extract-loaded nanoemulsion (CLEN). The levels of released HMGB1, nitric oxide (NO) production, inducible NO synthase (iNOS) expression, and phosphorylation of mitogen-activated protein kinases were analyzed in RAW264.7 macrophages. The effects of CLEN on survival of endotoxemic model mice, circulating HMGB1 levels, and tissue iNOS expression were also evaluated. We have shown that a nanoemulsion loaded with an extract from the C. longa rhizome regulates cellular inflammatory responses and LPS-induced systemic inflammation by suppressing the release of HMGB1 by macrophages. First, treatment of RAW264.7 macrophages with the nanoemulsion significantly attenuated their LPS-induced release of HMGB1: this effect was mediated by inhibiting c-Jun N-terminal kinase activation, which in turn suppressed the NO production and iNOS expression of the cells. The nanoemulsion did not affect LPS-induced p38 or extracellular signal-regulated kinase activation. Second, intraperitoneal administration of the nanoemulsion improved the survival rate of LPS-injected endotoxemic mice. This associated with marked reductions in circulating HMGB1 levels and tissue iNOS expression. The present study shows for the first time the mechanism by which C. longa ameliorates sepsis, namely, by suppressing NO signaling and thereby inhibiting the release of the proinflammatory cytokine HMGB1. These observations suggest that identification of

Curcumin longa extract-loaded nanoemulsion improves the survival of endotoxemic mice by inhibiting nitric oxide-dependent HMGB1 release

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Min Young Ahn

2017-09-01

Full Text Available Background High mobility group box 1 (HMGB1 is a well-known damage-related alarmin that participates in cellular inflammatory responses. However, the mechanisms leading to HMGB1 release in inflammatory conditions and the therapeutic agents that could prevent it remain poorly understood. This study attempted to examine whether the Curcumin longa herb, which is known to have anti-inflammatory property, can modulate cellular inflammatory responses by regulating HMGB1 release. Methods The murine macrophage RAW264.7 cells were treated with lipopolysaccharide (LPS and/or a C. longa extract-loaded nanoemulsion (CLEN. The levels of released HMGB1, nitric oxide (NO production, inducible NO synthase (iNOS expression, and phosphorylation of mitogen-activated protein kinases were analyzed in RAW264.7 macrophages. The effects of CLEN on survival of endotoxemic model mice, circulating HMGB1 levels, and tissue iNOS expression were also evaluated. Results We have shown that a nanoemulsion loaded with an extract from the C. longa rhizome regulates cellular inflammatory responses and LPS-induced systemic inflammation by suppressing the release of HMGB1 by macrophages. First, treatment of RAW264.7 macrophages with the nanoemulsion significantly attenuated their LPS-induced release of HMGB1: this effect was mediated by inhibiting c-Jun N-terminal kinase activation, which in turn suppressed the NO production and iNOS expression of the cells. The nanoemulsion did not affect LPS-induced p38 or extracellular signal-regulated kinase activation. Second, intraperitoneal administration of the nanoemulsion improved the survival rate of LPS-injected endotoxemic mice. This associated with marked reductions in circulating HMGB1 levels and tissue iNOS expression. Discussion The present study shows for the first time the mechanism by which C. longa ameliorates sepsis, namely, by suppressing NO signaling and thereby inhibiting the release of the proinflammatory cytokine HMGB1

Evaluation of antioxidant and antimicrobial activities of extract of Crataegus monogyna (hawthorn)

International Nuclear Information System (INIS)

Bouzid, W.; Yahia, M.; Abdeddaim, M.; Aberkane, M.C.; Ayachi, A.

2011-01-01

Various biological activities are attributed to a great variety of compounds isolated from natural plants. This study presents an attempt to evaluate the antimicrobial and antioxidant activity of organic and aqueous extract prepared from the edible part of Crataegus monogyna Jacq. Gualitative analysis of extracts by high performance liquid chromatography revealed the probable presence of quercetin in the EDm. The quantitative estimation of polyphenols (by the Folin-Ciocalteu method),total flavonoids (by the method of aluminium trichloride) and condensed tannins (by the method of iron trichloride) showed that the EDm and EMe extracts are richer in these compounds. The inhibition of couple oxidation of linoleic acid β-carotene was evaluated by the bleaching test of β-carotene, which showed a significant antioxidant activity for the EDm (48.46% inhibition) and EMe (36.40% inhibition). The evaluation of the antimicrobial potency of the extracts by the agar diffusion method showed that the extracts EEp EDm and EMe have an antibacterial activity on staphylococcus aureus strain at high concentration, whereas all extracts tested were inactive on Candida albicans. (author).

Guava leaves polyphenolics-rich extract inhibits vital enzymes implicated in gout and hypertension in vitro.

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Irondi, Emmanuel Anyachukwu; Agboola, Samson Olalekan; Oboh, Ganiyu; Boligon, Aline Augusti; Athayde, Margareth Linde; Shode, Francis O

2016-01-01

Elevated uric acid level, an index of gout resulting from the over-activity of xanthine oxidase (XO), increases the risk of developing hypertension. However, research has shown that plant-derived inhibitors of XO and angiotensin 1-converting enzyme (ACE), two enzymes implicated in gout and hypertension, respectively, can prevent or ameliorate both diseases, without noticeable side effects. Hence, this study characterized the polyphenolics composition of guava leaves extract and evaluated its inhibitory effect on XO and ACE in vitro. The polyphenolics (flavonoids and phenolic acids) were characterized using high-performance liquid chromatography (HPLC) coupled with diode array detection (DAD). The XO, ACE, and Fe(2+)-induced lipid peroxidation inhibitory activities, and free radicals (2,2-diphenylpicrylhydrazyl [DPPH]* and 2,2´-azino-bis-3-ethylbenzthiazoline-6-sulphonic [ABTS]*(+)) scavenging activities of the extract were determined using spectrophotometric methods. Flavonoids were present in the extract in the order of quercetin > kaempferol > catechin > quercitrin > rutin > luteolin > epicatechin; while phenolic acids were in the order of caffeic acid > chlorogenic acid > gallic acids. The extract effectively inhibited XO, ACE and Fe(2+)-induced lipid peroxidation in a dose-dependent manner; having half-maximal inhibitory concentrations (IC50) of 38.24 ± 2.32 μg/mL, 21.06 ± 2.04 μg/mL and 27.52 ± 1.72 μg/mL against XO, ACE and Fe(2+)-induced lipid peroxidation, respectively. The extract also strongly scavenged DPPH* and ABTS*(+). Guava leaves extract could serve as functional food for managing gout and hypertension and attenuating the oxidative stress associated with both diseases.

Plant extracts in the control of Phytophthora cryptogea.

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Orlikowski, L B

2001-01-01

Grapefruit extract at dose 40 micrograms/cm3 inhibited Phytophtora cryptogea linear growth about 50% and almost completely suppressed zoosporangia formation. Drenching of gerbera plants with the extract at dose 165 micrograms/cm3 reduced population density of the pathogen about 70% and this high efficacy was noted at least one month after application. Treatment of gerberas with grapefruit extract resulted in protection of about 50% of plants against the pathogen. Biological activity of purple coneflower extract was lower than extract from grapefruit. Significant decrease of population density of the pathogen during the first 5 days and increase of gerbera healthy stand was observed, however, in peat treated with that extract.

Inhibition of lung cancer cells A549 and H460 by curcuminoid extracts and nanoemulsions prepared from Curcuma longa Linnaeus.

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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.

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

International Nuclear Information System (INIS)

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

1988-01-01

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

Daphne Genkwa Sieb. et Zucc. Water-Soluble Extracts Act on Enterovirus 71 by Inhibiting Viral Entry

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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.

Phytochemical Analysis and Antioxidant Property of Leaf Extracts of Vitex doniana and Mucuna pruriens

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K. N. Agbafor

2011-01-01

Full Text Available Oxidative stress and impaired antioxidant system have been implicated in the pathophysiology of diverse disease states. The phytochemical screening and antioxidant property of fresh leaves of Vitex doniana and Mucuna pruriens, used in the management and treatment of various diseases, were studied. The extracts (ethanol and distilled water were screened for the presence of phytochemicals, and their inhibition of 2,2-diphenyl-1-picryl-hydrazyl (DPPH radical was used to evaluate their free radical scavenging activity. Liver levels of malondialdehyde (MDA, superoxide dismutase (SOD, and catalase (CAT in carbon tetrachloride- (CCl4 treated albino rats were also used to assess the antioxidant activity of the extracts. The animals were treated with 250 mg/kg body weight of the extracts for six consecutive days before a single dose (2.5 mL/kg body weight of CCl4. Vitamin C was used as the standard antioxidant. Phytochemical screening revealed the presence of saponins, tannins, anthraquinones, terpenoids, and flavonoids in all the extracts, while alkaloids were detected in extracts of Vitex doniana only, and cardiac glycosides occurred in extracts of Mucuna pruriens only. All the extracts inhibited DPPH radical in a concentration-dependent manner, water extract of Vitex doniana producing highest inhibition which was not significantly different (P>.05 from vitamin C. The extracts produced a significant decrease (P<.05 in liver MDA, while the levels of SOD and CAT significantly increased (P<.05 relative to the positive control. These results are an indication of antioxidant potential of the extracts and may be responsible for some of the therapeutic uses of these plants.

Phytochemical Analysis and Antioxidant Property of Leaf Extracts of Vitex doniana and Mucuna pruriens

Science.gov (United States)

Agbafor, K. N.; Nwachukwu, N.

2011-01-01

Oxidative stress and impaired antioxidant system have been implicated in the pathophysiology of diverse disease states. The phytochemical screening and antioxidant property of fresh leaves of Vitex doniana and Mucuna pruriens, used in the management and treatment of various diseases, were studied. The extracts (ethanol and distilled water) were screened for the presence of phytochemicals, and their inhibition of 2,2-diphenyl-1-picryl-hydrazyl (DPPH) radical was used to evaluate their free radical scavenging activity. Liver levels of malondialdehyde (MDA), superoxide dismutase (SOD), and catalase (CAT) in carbon tetrachloride- (CCl4) treated albino rats were also used to assess the antioxidant activity of the extracts. The animals were treated with 250 mg/kg body weight of the extracts for six consecutive days before a single dose (2.5 mL/kg body weight) of CCl4. Vitamin C was used as the standard antioxidant. Phytochemical screening revealed the presence of saponins, tannins, anthraquinones, terpenoids, and flavonoids in all the extracts, while alkaloids were detected in extracts of Vitex doniana only, and cardiac glycosides occurred in extracts of Mucuna pruriens only. All the extracts inhibited DPPH radical in a concentration-dependent manner, water extract of Vitex doniana producing highest inhibition which was not significantly different (P > .05) from vitamin C. The extracts produced a significant decrease (P < .05) in liver MDA, while the levels of SOD and CAT significantly increased (P < .05) relative to the positive control. These results are an indication of antioxidant potential of the extracts and may be responsible for some of the therapeutic uses of these plants. PMID:21547085

Innovative approach for urease inhibition by Ficus carica extract-fabricated silver nanoparticles: An in vitro study.

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Borase, Hemant P; Salunkhe, Rahul B; Patil, Chandrashekhar D; Suryawanshi, Rahul K; Salunke, Bipinchandra K; Wagh, Nilesh D; Patil, Satish V

2015-01-01

In the present study, a rapid, low-cost, and ecofriendly method of stable silver nanoparticles (AgNPs) synthesis using leaves extract of Ficus carica (F. carica), a plant with diverse metabolic consortium, is reported for the first time. An absorption peak at 422 nm in UV-Vis spectroscopy, a spherical shape with an average size of 21 nm in transmission electron microscopy, and crystalline nature in X-ray powder diffraction studies were observed for the synthesized AgNPs. Fourier transform infrared analysis indicated that proteins of F. carica might have a vital role in AgNP synthesis and stabilization. AgNPs were found to inhibit urease, a key enzyme responsible for the survival and pathogenesis of the bacterium, Helicobacter pylori. Inhibition of urease by AgNPs was monitored spectrophotometrically by the evaluation of ammonia release. The urease inhibition potential of AgNPs can be explored in the treatment of H. pylori by preparing novel combinations of standard drugs with AgNPs- or AgNPs-encapsulated drug molecules. © 2015 International Union of Biochemistry and Molecular Biology, Inc.

Determination of the potency of a novel saw palmetto supercritical CO2 extract (SPSE) for 5α-reductase isoform II inhibition using a cell-free in vitro test system.

Science.gov (United States)

Pais, Pilar; Villar, Agustí; Rull, Santiago

2016-01-01

The nicotinamide adenine dinucleotide phosphate-dependent membrane protein 5α-reductase catalyses the conversion of testosterone to the most potent androgen - 5α-dihydrotestosterone. Two 5α-reductase isoenzymes are expressed in humans: type I and type II. The latter is found primarily in prostate tissue. Saw palmetto extract (SPE) has been used extensively in the treatment of lower urinary tract symptoms secondary to benign prostatic hyperplasia (BPH). The pharmacological effects of SPE include the inhibition of 5α-reductase, as well as anti-inflammatory and antiproliferative effects. Clinical studies of SPE have been inconclusive - some have shown significant results, and others have not - possibly the result of varying bioactivities of the SPEs used in the studies. To determine the in vitro potency in a cell-free test system of a novel SP supercritical CO2 extract (SPSE), an inhibitor of the 5α-reductase isoenzyme type II. The inhibitory potency of SPSE was compared to that of finasteride, an approved 5α-reductase inhibitor, on the basis of the enzymatic conversion of the substrate androstenedione to the 5α-reduced product 5α-androstanedione. By concentration-dependent inhibition of 5α-reductase type II in vitro (half-maximal inhibitory concentration 3.58±0.05 μg/mL), SPSE demonstrated competitive binding toward the active site of the enzyme. Finasteride, the approved 5α-reductase inhibitor tested as positive control, led to 63%-75% inhibition of 5α-reductase type II. SPSE effectively inhibits the enzyme that has been linked to BPH, and the amount of extract required for activity is comparatively low. It can be confirmed from the results of this study that SPSE has bioactivity that promotes prostate health at a level that is superior to that of many other phytotherapeutic extracts. The bioactivity of SPSE corresponds favorably to that reported for the hexane extract used in a large number of positive BPH clinical trials, as well as to finasteride

Green approach to corrosion inhibition of mild steel in two acidic solutions by the extract of Punica granatum peel and main constituents

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Behpour, M., E-mail: m.behpour@kashanu.ac.ir [Department of Analytical Chemistry, Faculty of Chemistry, University of Kashan, Kashan, I.R. 87317-51167 (Iran, Islamic Republic of); Ghoreishi, S.M.; Khayatkashani, M. [Department of Analytical Chemistry, Faculty of Chemistry, University of Kashan, Kashan, I.R. 87317-51167 (Iran, Islamic Republic of); Soltani, N. [Department of Chemistry, Payame Noor University (PNU), 19395-4697 Tehran (Iran, Islamic Republic of)

2012-01-05

Graphical abstract: Ellagic acid (EA) and tannic acid (TA) were studied as corrosion inhibitors. The electron density HOMO and LUMO of EA and TA were used to explain difference in behavior of them. Highlights: Black-Right-Pointing-Pointer The extract of Punica granatum (PG) and their main constituent (ellagic acid (EA)) are found to be good inhibitors for the corrosion of mild steel in 1 M H{sub 2}SO{sub 4} and 2 M HCl. Black-Right-Pointing-Pointer The electrochemical inhibitive mechanism is explained by potentiodynamic polarization curves and electrochemical impedance spectroscopy (EIS) results. Black-Right-Pointing-Pointer The adsorption of ALLOX on mild steel surface was found to accord with the Temkin adsorption isotherm. Black-Right-Pointing-Pointer The effect of temperature on the corrosion behavior of mild steel in 2 M HCl and 1 M H{sub 2}SO{sub 4} without and with the PG extract was studied. - Abstract: The effect of the extract of Punica granatum (PG) and their main constituents involve ellagic acid (EA) and tannic acid (TA), as mild steel corrosion inhibitor in 2 M HCl and 1 M H{sub 2}SO{sub 4} solutions was investigated by weight loss measurements. The results obtained from the weight loss measurements show that the inhibition efficiency of TA even in high concentration is very low. Thus, potentiodynamic polarization and electrochemical impedance spectroscopy (EIS) investigations were used for different concentrations of PG and EA and best concentration of TA. Potentiodynamic polarization curves indicated that PG and EA behave as mixed-type inhibitors. EIS measurements show an increase of the transfer resistance with increasing inhibitor concentration. The temperature effect on the corrosion behavior of steel without and with the PG extract was studied. The inhibition action of the extract was discussed in view of Langmuir adsorption isotherm.

Green approach to corrosion inhibition of mild steel in two acidic solutions by the extract of Punica granatum peel and main constituents

International Nuclear Information System (INIS)

Behpour, M.; Ghoreishi, S.M.; Khayatkashani, M.; Soltani, N.

2012-01-01

Graphical abstract: Ellagic acid (EA) and tannic acid (TA) were studied as corrosion inhibitors. The electron density HOMO and LUMO of EA and TA were used to explain difference in behavior of them. Highlights: ► The extract of Punica granatum (PG) and their main constituent (ellagic acid (EA)) are found to be good inhibitors for the corrosion of mild steel in 1 M H 2 SO 4 and 2 M HCl. ► The electrochemical inhibitive mechanism is explained by potentiodynamic polarization curves and electrochemical impedance spectroscopy (EIS) results. ► The adsorption of ALLOX on mild steel surface was found to accord with the Temkin adsorption isotherm. ► The effect of temperature on the corrosion behavior of mild steel in 2 M HCl and 1 M H 2 SO 4 without and with the PG extract was studied. - Abstract: The effect of the extract of Punica granatum (PG) and their main constituents involve ellagic acid (EA) and tannic acid (TA), as mild steel corrosion inhibitor in 2 M HCl and 1 M H 2 SO 4 solutions was investigated by weight loss measurements. The results obtained from the weight loss measurements show that the inhibition efficiency of TA even in high concentration is very low. Thus, potentiodynamic polarization and electrochemical impedance spectroscopy (EIS) investigations were used for different concentrations of PG and EA and best concentration of TA. Potentiodynamic polarization curves indicated that PG and EA behave as mixed-type inhibitors. EIS measurements show an increase of the transfer resistance with increasing inhibitor concentration. The temperature effect on the corrosion behavior of steel without and with the PG extract was studied. The inhibition action of the extract was discussed in view of Langmuir adsorption isotherm.

Extraction and inhibition of enzymatic activity of botulinum neurotoxins/A1, /A2, and /A3 by a panel of monoclonal anti-BoNT/A antibodies.

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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.

Modulation of ionizing radiation induced oxidative imbalance by semi-fractionated extract of Piper betle

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Verma, Savita; Dutta, Ajaswrata; Sankhwar, Sanghmitra; Shukla, Sandeep Kumar

2010-01-01

The study was planned to evaluate modulatory effect of aqueous extract of Piper betle leaf (PBL) on ionizing radiation mediated oxidative stress leading to normal tissues damage during radiotherapy and other radiation exposures. The total polyphenols and flavonoids known as free radical scavenger (chelators) were measured in the extract. To ascertain antioxidant potential of PBL extract, we studied free radical scavenging, metal chelation, reducing power, lipid peroxidation inhibition and ferric reducing antioxidant properties (FRAP ) using in vitro assays. Mice were exposed to varied radiation doses administered with the same extract prior to irradiation to confirm its oxidative stress minimizing efficacy by evaluating ferric reducing ability of plasma, reduced glutathione, lipid peroxidation and micro-nuclei frequency. PBL extract was effective in scavenging DPPH (up to 92% at 100 µg/ml) and superoxide radicals (up to 95% at 80 µg/ml), chelated metal ions (up to 83% at 50 µg/ml) and inhibited lipid peroxidation (up to 45.65% at 500 µg/ml) in a dose dependant manner using in vitro model. Oral administration of PBL extract (225 mg/kg body weight) 1 hr before irradiation in mice significantly enhanced (p < 0.01) radiation abated antioxidant potential of plasma and GSH level in all the observed organs. The treatment with extract effectively lowered the radiation induced lipid peroxidation at 24 hrs in all the selected organs with maximum inhibition in thymus (p < 0.01). After 48 hrs, lipid peroxidation was maximally inhibited in the group treated with the extract. Frequency of radiation induced micronucleated cells declined significantly (34.78%, p < 0.01) at 24 hrs post-irradiation interval by PBL extract administration. The results suggest that PBL extract has high antioxidant potential and relatively non-toxic and thus could be assertively used to mitigate radiotherapy inflicted normal tissues damage and also injuries caused by moderate doses of radiation

Insights into significance of combined inhibition of MEK and m-TOR signalling output in KRAS mutant non-small-cell lung cancer.

Science.gov (United States)

Broutin, Sophie; Stewart, Adam; Thavasu, Parames; Paci, Angelo; Bidart, Jean-Michel; Banerji, Udai

2016-08-23

We aimed to understand the dependence of MEK and m-TOR inhibition in EGFR(WT)/ALK(non-rearranged) NSCLC cell lines. In a panel of KRAS(M) and KRAS(WT) NSCLC cell lines, we determined growth inhibition (GI) following maximal reduction in p-ERK and p-S6RP caused by trametinib (MEK inhibitor) and AZD2014 (m-TOR inhibitor), respectively. GI caused by maximal m-TOR inhibition was significantly greater than GI caused by maximal MEK inhibition in the cell line panel (52% vs 18%, PTOR compared with maximal m-TOR+MEK inhibition. However, GI caused by the combination was significantly greater in the KRAS(M) cell lines (79% vs 61%, P=0.017). m-TOR inhibition was more critical to GI than MEK inhibition in EGFR(WT)/ALK(non-rearranged) NSCLC cells. The combination of MEK and m-TOR inhibition was most effective in KRAS(M) cells.

Determination of the potency of a novel saw palmetto supercritical CO2 extract (SPSE for 5α-reductase isoform II inhibition using a cell-free in vitro test system

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Pais P

2016-04-01

Full Text Available Pilar Pais, Agustí Villar, Santiago Rull Euromed, Barcelona, Spain Background: The nicotinamide adenine dinucleotide phosphate-dependent membrane protein 5α-reductase catalyses the conversion of testosterone to the most potent androgen – 5α-dihydrotestosterone. Two 5α-reductase isoenzymes are expressed in humans: type I and type II. The latter is found primarily in prostate tissue. Saw palmetto extract (SPE has been used extensively in the treatment of lower urinary tract symptoms secondary to benign prostatic hyperplasia (BPH. The pharmacological effects of SPE include the inhibition of 5α-reductase, as well as anti-inflammatory and antiproliferative effects. Clinical studies of SPE have been inconclusive – some have shown significant results, and others have not – possibly the result of varying bioactivities of the SPEs used in the studies. Purpose: To determine the in vitro potency in a cell-free test system of a novel SP supercritical CO2 extract (SPSE, an inhibitor of the 5α-reductase isoenzyme type II. Materials and methods: The inhibitory potency of SPSE was compared to that of finasteride, an approved 5α-reductase inhibitor, on the basis of the enzymatic conversion of the substrate androstenedione to the 5α-reduced product 5α-androstanedione. Results: By concentration-dependent inhibition of 5α-reductase type II in vitro (half-maximal inhibitory concentration 3.58±0.05 µg/mL, SPSE demonstrated competitive binding toward the active site of the enzyme. Finasteride, the approved 5α-reductase inhibitor tested as positive control, led to 63%–75% inhibition of 5α-reductase type II. Conclusion: SPSE effectively inhibits the enzyme that has been linked to BPH, and the amount of extract required for activity is comparatively low. It can be confirmed from the results of this study that SPSE has bioactivity that promotes prostate health at a level that is superior to that of many other phytotherapeutic extracts. The

Aqueous Extracts of the Marine Brown Alga Lobophora variegata Inhibit HIV-1 Infection at the Level of Virus Entry into Cells

KAUST Repository

Kremb, Stephan; Helfer, Markus; Kraus, Birgit; Wolff, Horst; Wild, Christian; Schneider, Martha; Voolstra, Christian R.; Brack-Werner, Ruth

2014-01-01

-infection. Anti-viral potency was related to ecological factors and showed clear differences depending on light exposition or epiphyte growth. Assays addressing early events of the HIV-1 replication cycle indicated that L. variegata extracts inhibited entry

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.

Chinese medicinal formula Fufang Xueshuantong capsule could inhibit the activity of angiotensin converting enzyme

Science.gov (United States)

Sheng, Shujing; Wang, Yonggang; Long, Chaofeng; Su, Weiwei; Rong, Xia

2014-01-01

Fufang Xueshuantong (FXST) capsule, a Chinese medicinal formula composed of four herbals – Panax notoginseng, Radix Astragali, Radix Salvia Miltiorrhizae and Radix Scrophulariaceae, has been used to treat cardiovascular diseases for many years, but the pharmacological mechanisms underlying its effects has not been clarified. This study investigates if a connection between FXST and angiotensin converting enzyme (ACE) might be an explanation for its pharmacological effects. ACE inhibition assay was performed on FXST capsule, 50% ethanol extracts from the four herbals and three selected saponins most abundant in P. notoginseng (Ginsenoside Rg1, Ginsenoside Rb1 and Notoginsenoside R1) using a biochemical test. Reversed-phase high-performance liquid chromatography of liberated hippuric acid from the ACE assay was conducted to determine the inhibitory effect. As a result, FXST and extracts from P. notoginseng showed a significant and dose-dependent inhibition on ACE activity with the IC50 values of 115 μg/ml and 179 μg/ml, respectively. But extracts from the other three herbals and the three selected saponins had no significant effect on ACE inhibition. Compared to other reported plant extracts, FXST could be considered as an effective ACE inhibitor. The inhibition of ACE activity supports the traditional use of FXST on blood circulation and the inhibitory property of FXST is mainly caused by P. notoginseng. PMID:26019516

Evaluation of antioxidant potential of citrus peel extracts

International Nuclear Information System (INIS)

Chatha, S.A.S.; Hussain, A.I.; Asi, M.R.

2011-01-01

The antioxidant potential of different solvent extracts of three different locally grown citrus varieties; grape fruit, lemon and mussambi, was assessed using some antioxidant assays like estimation of total phenolic contents (TPC), total flavonoids contents (TFC), percentage inhibition of linoleic acid oxidation and DPPH free radical scavenging capacity. The yield of extracts was found in the range of 17.92-30.8%. TPC, TFC, percent inhibition of linoleic acid oxidation and DPPH radical scavenging capacity of different citrus peel extracts were found in range of 2.72 - 3.77 g/100g as Gallic Acid Equivalent (GAE), 2.20-2.98 g/100g as Catechine Equivalent (CE), 68.20 - 91.78% and 19.53 - 41.88 mg/mL, respectively. Statistical analysis showed significant (p < 0.05) variations in the yield and antioxidant potentials of the extracts with respect to different species and solvent systems. From the results it is reasonable to say that methanolic extracts of citrus peels have exhibited varying degree of antioxidant potentials. (author)

The potential of papaya leaf extract in controlling Ganoderma boninense

Science.gov (United States)

Tay, Z. H.; Chong, K. P.

2016-06-01

Basal Stem Rot (BSR) disease causes significant losses to the oil palm industry. Numerous controls have been applied in managing the disease but no conclusive result was reported. This study investigated the antifungal potential of papaya leaf extracts against Ganoderma boninense, the causal pathogen of BSR. Among the five different solvents tested in extraction of compounds from papaya leaf, methanol and acetone gave the highest yield. In vitro antifungal activity of the methanol and acetone extracts were evaluated against G. boninense using agar dilution at four concentrations: 5 mg mL-1, 15 mg mL-1, 30 mg mL-1and 45 mg mL-1. The results indicated a positive correlation between the concentration of leaf extracts and the inhibition of G. boninense. ED50 of methanol and acetone crude extracts were determined to be 32.016 mg mL-1and 65.268 mg mL-1, respectively. The extracts were later semi-purified using solid phase extraction (SPE) and the nine bioactive compounds were identified: decanoic acid, 2-methyl-, Z,Z-10-12-Hexadecadien-1-ol acetate, dinonanoin monocaprylin, 2-chloroethyl oleate, phenol,4-(1-phenylethyl)-, phenol,2,4-bis(1-phenylethyl)-, phenol-2-(1-phenylethyl)-, ethyl iso-allocholate and 1- monolinoleoylglycerol trimethylsilyl ether. The findings suggest that papaya leaf extracts have the ability to inhibit the growth of G. boninense, where a higher concentration of the extract exhibits better inhibition effects.

Crude Flavonoid Extract of Medicinal Herb Zingibar officinale Inhibits Proliferation and Induces Apoptosis in Hepatocellular Carcinoma Cells.

Science.gov (United States)

Elkady, Ayman I; Abu-Zinadah, Osama A; Hussein, Rania Abd El Hamid

2017-07-05

There is an urgent need to improve the clinical management of hepatocellular carcinoma (HCC), one of the most common causes of global cancer-related deaths. Zingibar officinale is a medicinal herb used throughout history for both culinary and medicinal purposes. It has antioxidant, anticarcinogenic, and free radical scavenging properties. Previously, we proved that the crude flavonoid extract of Z. officinale (CFEZO) inhibited growth and induced apoptosis in several cancer cell lines. However, the effect of the CFEZO on an HCC cell line has not yet been evaluated. In this study, we explored the anticancer activity of CFEZO against an HCC cell line, HepG2. CFEZO significantly inhibited proliferation and induced apoptosis in HepG2 cells. Typical apoptotic morphological and biochemical changes, including cell shrinkage and detachment, nuclear condensation and fragmentation, DNA degradation, and comet tail formation, were observed after treatments with CFEZO. The apoptogenic activity of CFEZO involved induction of ROS, depletion of GSH, disruption of the mitochondrial membrane potential, activation of caspase 3/9, and an increase in the Bax/Bcl-2 ratio. CFEZO treatments induced upregulation of p53 and p21 expression and downregulation of cyclin D1 and cyclin-dependent kinase-4 expression, which were accompanied by G2/M phase arrest. These findings suggest that CFEZO provides a useful foundation for studying and developing novel chemotherapeutic agents for the treatment of HCC.

Andrographis paniculata extracts and major constituent diterpenoids inhibit growth of intrahepatic cholangiocarcinoma cells by inducing cell cycle arrest and apoptosis.

Science.gov (United States)

Suriyo, Tawit; Pholphana, Nanthanit; Rangkadilok, Nuchanart; Thiantanawat, Apinya; Watcharasit, Piyajit; Satayavivad, Jutamaad

2014-05-01

Andrographis paniculata is an important herbal medicine widely used in several Asian countries for the treatment of various diseases due to its broad range of pharmacological activities. The present study reports that A. paniculata extracts potently inhibit the growth of liver (HepG2 and SK-Hep1) and bile duct (HuCCA-1 and RMCCA-1) cancer cells. A. paniculata extracts with different contents of major diterpenoids, including andrographolide, 14-deoxy-11,12-didehydroandrographolide, neoandrographolide, and 14-deoxyandrographolide, exhibited a different potency of growth inhibition. The ethanolic extract of A. paniculata at the first true leaf stage, which contained a high amount of 14-deoxyandrographolide but a low amount of andrographolide, showed a cytotoxic effect to cancer cells about 4 times higher than the water extract of A. paniculata at the mature leaf stage, which contained a high amount of andrographolide but a low amount of 14-deoxyandrographolide. Andrographolide, not 14-deoxy-11,12-didehydroandrographolide, neoandrographolide, or 14-deoxyandrographolide, possessed potent cytotoxic activity against the growth of liver and bile duct cancer cells. The cytotoxic effect of the water extract of A. paniculata at the mature leaf stage could be explained by the present amount of andrographolide, while the cytotoxic effect of the ethanolic extract of A. paniculata at the first true leaf stage could not. HuCCA-1 cells showed more sensitivity to A. paniculata extracts and andrographolide than RMCCA-1 cells. Furthermore, the ethanolic extract of A. paniculata at the first true leaf stage increased cell cycle arrest at the G0/G1 and G2/M phases, and induced apoptosis in both HuCCA-1 and RMCCA-1 cells. The expressions of cyclin-D1, Bcl-2, and the inactive proenzyme form of caspase-3 were reduced by the ethanolic extract of A. paniculata in the first true leaf stage treatment, while a proapoptotic protein Bax was increased. The cleavage of poly (ADP

Ajoene, a Sulfur-Rich Molecule from Garlic, Inhibits Genes Controlled by Quorum Sensing

DEFF Research Database (Denmark)

Jakobsen, Tim Holm; van Gennip, Maria; Phipps, Richard Kerry

2012-01-01

the expression of specific genes involved in pathogenicity, is a possible drug target. Previous in vitro and in vivo studies revealed a significant inhibition of P. aeruginosa QS by crude garlic extract. By bioassay-guided fractionation of garlic extracts, we determined the primary QS inhibitor present in garlic...

Guava leaves polyphenolics-rich extract inhibits vital enzymes implicated in gout and hypertension in vitro

Science.gov (United States)

Irondi, Emmanuel Anyachukwu; Agboola, Samson Olalekan; Oboh, Ganiyu; Boligon, Aline Augusti; Athayde, Margareth Linde; Shode, Francis O.

2016-01-01

Background/Aim: Elevated uric acid level, an index of gout resulting from the over-activity of xanthine oxidase (XO), increases the risk of developing hypertension. However, research has shown that plant-derived inhibitors of XO and angiotensin 1-converting enzyme (ACE), two enzymes implicated in gout and hypertension, respectively, can prevent or ameliorate both diseases, without noticeable side effects. Hence, this study characterized the polyphenolics composition of guava leaves extract and evaluated its inhibitory effect on XO and ACE in vitro. Materials and Methods: The polyphenolics (flavonoids and phenolic acids) were characterized using high-performance liquid chromatography (HPLC) coupled with diode array detection (DAD). The XO, ACE, and Fe2+-induced lipid peroxidation inhibitory activities, and free radicals (2,2-diphenylpicrylhydrazyl [DPPH]* and 2,2´-azino-bis-3-ethylbenzthiazoline-6-sulphonic [ABTS]*+) scavenging activities of the extract were determined using spectrophotometric methods. Results: Flavonoids were present in the extract in the order of quercetin > kaempferol > catechin > quercitrin > rutin > luteolin > epicatechin; while phenolic acids were in the order of caffeic acid > chlorogenic acid > gallic acids. The extract effectively inhibited XO, ACE and Fe2+-induced lipid peroxidation in a dose-dependent manner; having half-maximal inhibitory concentrations (IC50) of 38.24 ± 2.32 μg/mL, 21.06 ± 2.04 μg/mL and 27.52 ± 1.72 μg/mL against XO, ACE and Fe2+-induced lipid peroxidation, respectively. The extract also strongly scavenged DPPH* and ABTS*+. Conclusion: Guava leaves extract could serve as functional food for managing gout and hypertension and attenuating the oxidative stress associated with both diseases. PMID:27104032

Detection of fungi from rice black bug Paraeucosmetus pallicornis Dallas (Hemiptera: Lygaeidae) and inhibition with crude extract of Calatropis gigantea (Asclepiadaceae)

Science.gov (United States)

Sjam, S.; Surapati, U.; Adiwena; Syatri, A.; Dewi, V. S.; Rosmana, A.

2018-05-01

Rice black bug (P. palicornis) is one of the pests that attack the rice plants in the generative phase that causes the rice easily destroyed when milled and tasted bitter after cooking hence reduces the quality and quantity of rice. The bitter taste in rice may be due to the fungus associated with rice black bug. The aimed of this research was to detect the associated fungi with rice black bug P. pallicornis using some sterilization methods and inhibition with of leaf crude extract of C. gigatea. Detection of fungi from P. pallicornis was conducted using three sterilization methods and control (without sterilization) namely: (1) sterilization with aquades + alcohol 70% (5, 10, 15 and 20 times dipping) + aquades; (2) aquades + alcohol 70% (10 and 20 times dipping); (3) Aquades + alcohol 90 %+ NaCl 0.5 % +alcohol 90 % + aquades. Inhibition of fungi from P. pallicornis with crude extract of C. gigantea obtained by maceration method and then made some concentration to see the effect of its inhibition on the fungi associated with the P. pallicornis. The results showed that without sterilization, four microbe were obtained: Gliocladium sp., Aspergillus sp., black hyphae fungus and white hyphae fungus, sterilization method of Aquades + alcohol 70% with 5 times dipping in alcohol obtained Gliocladium sp., 10 and 20 times dipping found Aspergillus sp. and Gliocladium sp and 15 times dipping found Aspergillus sp. Sterilization with 10 and 20 times dipping in alcohol 70% then washing 2 times with aquades found Gliogladium sp. and Aspergillus sp. Sterilization with Aquades + alcohol 90 % + NaCl 0.5% + alcohol 90% + aquades found Gliocladium sp. Crude extract of C. gigantea had the potential to inhibit fungi Aspergillus sp. and Gliocladium sp. from rice black bug.

COMPARATION OF SEVERAL PLANTS EXTRACT AND VITAMIN C INHIBITION ACTIVITY TO TYROSINE PHOTODEGRADATION INDUCED BY KETOPROFEN AND ITS TOTAL PHENOLIC COMPOUNDS

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Tatang Irianti

2016-12-01

Full Text Available Antioxidant is known to inhibit free radical reaction. Tyrosine photodegradation can be caused by radical reaction. Nowadays, plant with antioxidants are widely used to inhibit free radical reaction. Study of inhibition of photodegradation used four groups. Those groups are: P1 consisted of 2mL tyrosine 0,05 %; P2 consisted of 2 mL tyrosine 0,05 %, and 600 μL Rhetoflam (topical ketoprofen 1 %; P3 consisted of 2 mL tyrosine 0,05 %, 60μL Rhetoflam 1 %, and 100 μL tea leaf water ekstract 0,15 %; P4 consisted of 2 mL tyrosine 0,05 %, 600 μL Rhetoflam 1 %, and 100 μL mahkota dewa fruit water ekstract 0,15 %; P5 consisted of 2 mL tyrosine 0,05 %, 600 μL Rhetoflam 1 %, and 100 μL finger root etanolic ekstract 0,15 %; P6 consisted of 2 mL tyrosine 0,05 %, 600 μL Rhetoflam 1 %, and 100 μL vitamin C 0,15 %; each group is added with aquadest up to 5,0 mL and illuminated with mercuric lamp for four hours. Level of remaining tyrosine was measured with visible spectrophotometric method. We used ANOVA to analyse the data with convidence level of 0,95 and then continued by Tukey (HSD. Follin-Ciocalteu method with galic acid calibration curve was used to determine total phenolic level. The level of total phenolic of tea leaf aquoeus extract, mahkota dewa fruit aquoeus extract, fingerroot ethanolic extract were 29.64±0.86 %; 8.29 % 0.27 %; and 7.11 %, 0.15 %, respectively. Our investigation also found gallic acid equivalent (GAE with the inhibition activity of 4.03; 1.58; and 2.09 and they were bigger than Vitamin C with the same concentration of 0.15 %.

Comparison of Anti-inflammatory Activities of Six Curcuma Rhizomes: A Possible Curcuminoid-independent Pathway Mediated by Curcuma phaeocaulis Extract

OpenAIRE

Tohda, Chihiro; Nakayama, Natsuki; Hatanaka, Fumiyuki; Komatsu, Katsuko

2006-01-01

We aimed to compare the anti-inflammatory activities of six species of Curcuma drugs using adjuvant arthritis model mice. When orally administered 1 day before the injection of adjuvant, the methanol extract of Curcuma phaeocaulis significantly inhibited paw swelling and the serum haptoglobin concentration in adjuvant arthritis mice. Also when orally administered 1 day after the injection of adjuvant, the methanol extract of Curcuma phaeocaulis significantly inhibited paw swelling. Other C...

Banana peel extract suppressed prostate gland enlargement in testosterone-treated mice.

Science.gov (United States)

Akamine, Kiichiro; Koyama, Tomoyuki; Yazawa, Kazunaga

2009-09-01

A methanol extract of banana peel (BPEx, 200 mg/kg, p.o.) significantly suppressed the regrowth of ventral prostates and seminal vesicles induced by testosterone in castrated mice. Further studies in the androgen-responsive LNCaP human prostate cancer cell line showed that BPEx inhibited dose-dependently testosterone-induced cell growth, while the inhibitory activities of BPEx did not appear against dehydrotestosterone-induced cell growth. These results indicate that methanol extract of banana peel can inhibit 5alpha-reductase and might be useful in the treatment of benign prostate hyperplasia.

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.

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.

Comparison of Anti-inflammatory Activities of Six Curcuma Rhizomes: A Possible Curcuminoid-independent Pathway Mediated by Curcuma phaeocaulis Extract

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Chihiro Tohda

2006-01-01

Full Text Available We aimed to compare the anti-inflammatory activities of six species of Curcuma drugs using adjuvant arthritis model mice. When orally administered 1 day before the injection of adjuvant, the methanol extract of Curcuma phaeocaulis significantly inhibited paw swelling and the serum haptoglobin concentration in adjuvant arthritis mice. Also when orally administered 1 day after the injection of adjuvant, the methanol extract of Curcuma phaeocaulis significantly inhibited paw swelling. Other Curcuma species (Curcuma longa, Curcuma wenyujin, Curcuma kwangsiensis, Curcuma zedoaria and Curcuma aromatica had no significant inhibitory effects on adjuvant-induced paw swelling. Cyclooxygenase (COX-2 activity was significantly inhibited by the methanol extract of C. phaeocaulis. Curcuminoids' (curcumin, bis-demethoxycurcumin and demethoxycurcumin were rich in C. longa, but less in C. phaeocaulis and C. aromatica, not in C. wenyujin, C. kwangsiensis and C. zedoaria, suggesting that curcuminoids' contents do not relate to inhibition of arthritis swelling. Therefore, C. phaeocaulis may be a useful drug among Curcuma species for acute inflammation, and the active constituents of C. phaeocaulis are not curcuminoids.

Effects of Puerariae Radix extract on the activity of antioxidant

Directory of Open Access Journals (Sweden)

Young-Joon Eun

2007-12-01

Full Text Available Objective : The objective of this study was to investigate the antioxidative effects of Puerariae Radix extract. Method : Total antioxidant capacity (TAC, Total antioxidant response (TAR, Total phenolic content, Reactive oxygen species (ROS, 1,1-Diphenyl-2-picrylhydrazyl (DPPH free radical scavenging activities, lipid peroxidation were examined. Result : Total antioxidant status was examined by total antioxidant capacity(TAC and total antioxidant response(TAR against potent free radical reactions. TAC and TAR of Puerariae Radix extract at the concentration of 5 mg/㎖ were 2.02 and 1.50 mM Trolox equivalents, respectively. Total phenolic content of Puerariae Radix extract at the concentration of 5mg/㎖ was 2.29 mM gallic acid equivalent. Concentration of Puerariae Radix extract at which DPPH radical scavenging activity was inhibited by 50% was 5.91 mg/㎖ as compared to 100% by pyrogallol solution as a reference. The inhibitory effect of the extract on lipid peroxidation was examined using rat liver mitochondria induced by FeSO4/ascorbic acid. Puerariae Radix extract at the concentration of 1 mg/㎖ slightly but significantly decreased TBARS concentration. The extract further prevented lipid peroxidation in a dose-dependent manner. The effect of Puerariae Radix extract on reactive oxygen species (ROS generation was examined using cell-free system induced by hydrogen peroxide/FeSO4. Addition of 1 mg/㎖ of Puerariae Radix extract significantly reduced dichloroflurescein (DCF fluorescence. The extract caused concentration-dependent attenuation of the increase in DCF fluorescence, indicating that the extract significantly prevented ROS generation in vitro. Thus antioxidant effects of Puerariae Radix extract seem to be due to, at least in part, the prevention from free radicals-induced oxidation, followed by inhibition of lipid peroxidation. Conclusion : As a result, Puerariae Radix seems to have antioxitative effect and antioxidant compount.

Antiplatelet Activity of Morus alba Leaves Extract, Mediated via Inhibiting Granule Secretion and Blocking the Phosphorylation of Extracellular-Signal-Regulated Kinase and Akt

Science.gov (United States)

Rhee, Man Hee; Sung, Yoon-Young; Yang, Won-Kyung; Kim, Seung Hyung; Kim, Ho-Kyoung

2014-01-01

Ethnopharmacological Relevance. Morus alba L. leaves (MAE) have been used in fork medicine for the treatment of beriberi, edema, diabetes, hypertension, and atherosclerosis. However, underlying mechanism of MAE on cardiovascular protection remains to be elucidated. Therefore, we investigated whether MAE affect platelet aggregation and thrombosis. Materials and Methods. The anti-platelet activity of MAE was studied using rat platelets. The extent of anti-platelet activity of MAE was assayed in collagen-induced platelet aggregation. ATP and serotonin release was carried out. The activation of integrin α IIb β 3 and phosphorylation of signaling molecules, including MAPK and Akt, were investigated with cytofluorometer and immunoblotting, respectively. The thrombus formation in vivo was also evaluated in arteriovenous shunt model of rats. Results. HPLC chromatographic analysis revealed that MAE contained rutin and isoquercetin. MAE dose-dependently inhibited collagen-induced platelet aggregation. MAE also attenuated serotonin secretion and thromboxane A2 formation. In addition, the extract in vivo activity showed that MAE at 100, 200, and 400 mg/kg significantly and dose-dependently attenuated thrombus formation in rat arterio-venous shunt model by 52.3% (P < 0.001), 28.3% (P < 0.01), and 19.1% (P < 0.05), respectively. Conclusions. MAE inhibit platelet activation, TXB2 formation, serotonin secretion, aggregation, and thrombus formation. The plant extract could be considered as a candidate to anti-platelet and antithrombotic agent. PMID:24701244

Continuous delivery of propranolol from liposomes-in-microspheres significantly inhibits infantile hemangioma growth

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Guo XN

2017-09-01

Full Text Available Xiaonan Guo,1,* Xiaoshuang Zhu,1,* Dakan Liu,1 Yubin Gong,1 Jing Sun,2 Changxian Dong1 1Department of Hemangioma and Vascular Malformation, Henan Provincial People’s Hospital, Zhengzhou, People’s Republic of China; 2Department of Pharmacy, Second Military Medical University, Shanghai, People’s Republic of China *These authors contributed equally to this work Purpose: To reduce the adverse effects and high frequency of administration of propranolol to treat infantile hemangioma, we first utilized propranolol-loaded liposomes-in-microsphere (PLIM as a novel topical release system to realize sustained release of propranolol.Methods: PLIM was developed from encapsulating propranolol-loaded liposomes (PLs in microspheres made of poly(lactic-co-glycolic acid-b-poly(ethylene glycol-b-poly(lactic-co-glycolic acid copolymers (PLGA-PEG-PLGA. The release profile of propranolol from PLIM was evaluated, and its biological activity was investigated in vitro using proliferation assays on hemangioma stem cells (HemSCs. Tumor inhibition was studied in nude mice bearing human subcutaneous infantile hemangioma.Results: The microspheres were of desired particle size (~77.8 µm and drug encapsulation efficiency (~23.9% and achieved sustained drug release for 40 days. PLIM exerted efficient inhibition of the proliferation of HemSCs and significantly reduced the expression of two angiogenesis factors (vascular endothelial growth factor-A [VEGF-A] and basic fibroblast growth factor [bFGF] in HemSCs. Notably, the therapeutic effect of PLIM in hemangioma was superior to that of propranolol and PL in vivo, as reflected by significantly reduced hemangioma volume, weight, and microvessel density. The mean hemangioma weight of the PLIM-treated group was significantly lower than that of other groups (saline =0.28 g, propranolol =0.21 g, PL =0.13 g, PLIM =0.03 g; PLIM vs saline: P<0.001, PLIM vs propranolol: P<0.001, PLIM vs PL: P<0.001. The mean microvessel density of

Lipoxygenase and urease inhibition of extracts of polygonatum verticillatum rhizome: augmented by its isolated compound, santonin

International Nuclear Information System (INIS)

Khan, H.; Saeed, M.; Saeed, M.

2014-01-01

The present study was designed to explore the enzyme inhibitory profile of extracts of rhizome of Polygonatum verticillatum against lipoxygenase and urease. When tested against lipoxygenase, ethyl acetate fraction was found the most potent (IC50: 69 micro g/ml) and the overall IC50 values of different extracts ranged from 69-174 micro g/ml. In urease assay, n-butanol was the most potent fraction (IC50: 169 micro g/ml) while the overall IC50 values were in the range of 169-288 micro g/ml. Bioactivity guided chromatography led to the isolation of compound 1 which was characterized as santonin on the basis of various spectroscopic techniques. When santonin was tested against lipoxygenase and urease, it showed potent inhibition of lipoxygenase (IC50: 27.4 micro M) but did not attenuate the urease activity. Our findings provided strong evidence for the enzyme inhibitory profile of the extracts of P. verticillatum rhizome and its isolated compound. Thus results are consistent with the traditional use of the plant as an anti-inflammatory agent. (author)

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.

Extract of Cordyceps militaris inhibits angiogenesis and suppresses tumor growth of human malignant melanoma cells.

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Ruma, I Made Winarsa; Putranto, Endy Widya; Kondo, Eisaku; Watanabe, Risayo; Saito, Ken; Inoue, Yusuke; Yamamoto, Ken-Ichi; Nakata, Susumu; Kaihata, Masaji; Murata, Hitoshi; Sakaguchi, Masakiyo

2014-07-01

Angiogenesis is essential for tumor development and metastasis. Among several angiogenic factors, vascular endothelial growth factor receptor (VEGF) is important for tumor-derived angiogenesis and commonly overexpressed in solid tumors. Thus, many antitumor strategies targeting VEGF have been developed to inhibit cancer angiogenesis, offering insights into the successful treatment of solid cancers. However, there are a number of issues such as harmful effects on normal vascularity in clinical trials. Taking this into consideration, we employed Cordyceps militaris as an antitumor approach due to its biological safety in vivo. The herbal medicinal mushroom Cordyceps militaris has been reported to show potential anticancer properties including anti-angiogenic capacity; however, its concrete properties have yet to be fully demonstrated. In this study, we aimed to elucidate the biological role of Cordyceps militaris extract in tumor cells, especially in regulating angiogenesis and tumor growth of a human malignant melanoma cell line. We demonstrated that Cordyceps militaris extract remarkably suppressed tumor growth via induction of apoptotic cell death in culture that links to the abrogation of VEGF production in melanoma cells. This was followed by mitigation of Akt1 and GSK-3β activation, while p38α phosphorylation levels were increased. Extract treatment in mouse model xenografted with human melanoma cells resulted in a dramatic antitumor effect with down-regulation of VEGF expression. The results suggest that suppression of tumor growth by Cordyceps militaris extract is, at least, mediated by its anti-angiogenicity and apoptosis induction capacities. Cordyceps militaris extract may be a potent antitumor herbal drug for solid tumors.

Modulatory effects of Thai medicinal plant extract on ...

African Journals Online (AJOL)

Lindau (1 and 100 μg/ml), significantly inhibited the IFN-y/TNF-a- induced HaCaT apoptosis, while members of the Zingiberaceae family, Curcuma longa L. and Alpinia galanga (L.) Willd, significantly enhanced apoptosis when a concentration of 100 μg/ml was used. Furthermore, the ethanolic plant extracts were found to ...

Inhibition of Phytophthora parasitica and P. capsici by Silver Nanoparticles Synthesized Using Aqueous Extract of Artemisia absinthium.

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Ali, Mohammad; Kim, Bosung; Belfield, Kevin D; Norman, David; Brennan, Mary; Ali, Gul Shad

2015-09-01

Application of nanoparticles for controlling plant pathogens is a rapidly emerging area in plant disease management, and nanoparticles synthesis methods that are economical and ecofriendly are extensively investigated. In this project, we investigated the potential of silver nanoparticles (AgNPs) synthesized with aqueous extract of Artemisia absinthium against several Phytophthora spp., which cause many economically important crop diseases. In in vitro dose-response tests conducted in microtiter plates, 10 µg ml⁻¹ of AgNPs inhibited mycelial growth of P. parasitica, P. infestans, P. palmivora, P. cinnamomi, P. tropicalis, P. capsici, and P. katsurae. Detailed in vitro dose-response analyses conducted with P. parasitica and P. capsici revealed that AgNPs synthesized with A. absinthium extract were highly potent (IC50: 2.1 to 8.3 µg ml⁻¹) and efficacious (100%) in inhibiting mycelial growth, zoospore germination, germ tube elongation, and zoospore production. Interestingly, AgNP treatment accelerated encystment of zoospores. Consistent with in vitro results, in planta experiments conducted in a greenhouse revealed that AgNP treatments prevented Phytophthora infection and improved plant survival. Moreover, AgNP in in planta experiments did not produce any adverse effects on plant growth. These investigations provide a simple and economical method for controlling Phytophthora with AgNP without affecting normal plant physiology.

Antimicrobial activity of Antrodia camphorata extracts against oral bacteria.

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Hsiu-Man Lien

Full Text Available Antrodia camphorata (A. camphorata is a unique, endemic and extremely rare mushroom species native to Taiwan, and both crude extracts of and purified chemical compounds from A. camphorata have been reported to have a variety of significant beneficial effects, such as anti-tumor and anti-inflammatory activity. However, reports on the effects of A. camphorata against dental pathogens have been limited. Oral health is now recognized as important for overall general health, including conditions such as dental caries, periodontal disease and rheumatoid arthritis. Streptococcus mutans (S. mutans and Porphyromonas gingivalis (P. gingivalis are the most common bacteria associated with dental plaque and periodontopathic diseases, respectively. Thus, our study examined the ability of five various crude extracts of A. camphorata to inhibit the growth of dental bacteria and anti-adherence in vitro. Among the extracts, the ethanol, ethyl acetate and chloroform extracts exhibited the lowest MICs against P. gingivalis and S. mutans (MIC = 4∼16 µg/mL. The MIC of the aqueous extract was greater than 2048 µg/mL against both P. gingivalis and S. mutans. In vitro adherence of S. mutans was significantly inhibited by the addition of either the ethyl acetate extract or chloroform extract (MIC = 16∼24 µg/mL, while the ethanol extract (MIC = 32∼64 µg/mL exhibited moderate inhibitory activity. Based on the result of this study, the ethyl acetate and chloroform extracts of A. camphorata may be good candidates for oral hygiene agents to control dental caries and periodontopathic conditions.

Analgesic and Anti-inflammatory Activity of Teucrium chamaedrys Leaves Aqueous Extract in Male Rats

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Ali Pourmotabbed

2010-06-01

Full Text Available Objective(sCurrent study was undertaken to investigate the analgesic and anti-inflammatory effects of the aqueous extract of Teucrium chamaedrys in mice and rats. Materials and MethodsFor evaluating of analgesic and anti-inflammatory activity, we used the carrageenan- and dextran-induced paw oedema, acetic acid-induced writhing, tail flick and formalin pain tests.ResultsThe extract of T. chamaedrys (50–200 mg/kg and acetylsalicylic acid (100 mg/kg produced a significant (P< 0.01 inhibition of the second phase response in the formalin pain model, while only the high dose (200 mg/kg of the extract showed an analgesic effect in the first phase. The extract also inhibited acetic acid-induced abdominal writhes in a dose-dependent manner. The tail flick latency was dose dependently enhanced by the extract but this was significantly (P< 0.05 lower than that produced by morphine (10 mg/kg. The extract (25–250 mg/kg administered 1 hr before carrageenan-induced paw swelling produced a dose dependent inhibition of the oedema. No effect was observed with the dextran-induced oedema model. Results of the phytochemical screening show the presence of alkaloids, flavonoids and triterpenoids in the extract.ConclusionThe data obtained also suggest that the anti-inflammatory and analgesic effects of the extract may be mediated via both peripheral and central mechanisms. The role of alkaloids, flavonoids and triterpenoids will evaluate in future studies.

Phenolic-rich extracts of Eurycoma longifolia and Cylicodiscus gabunensis inhibit enzymes responsible for the development of erectile dysfunction and are antioxidants.

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Oboh, Ganiyu; Adebayo, Adeniyi A; Ademosun, Ayokunle O

2018-05-19

Herbs have been used from ages to manage male sexual dysfunction. Hence, this study sought to investigate the effects of Eurycoma longifolia (EL) and Cylicodiscus gabunensis (CG) stem bark extracts on some enzymes implicated in erectile dysfunction in vitro. The extracts were prepared, and their effects on phosphodiesterase-5 (PDE-5), arginase, and angiotensin-1-converting enzyme (ACE) as well as pro-oxidant-induced lipid peroxidation were assessed. Furthermore, phenolic contents were determined, and their components were characterized and quantified using high-performance liquid chromatography with diode array detector (HPLC-DAD). The results revealed that the extracts inhibited PDE-5, arginase, and ACE in a concentration-dependent manner. However, IC50 values revealed that CG had higher inhibitory potential on PDE-5 (IC50=204.4 μg/mL), arginase (IC50=39.01 μg/mL), and ACE (IC50=48.81 μg/mL) than EL. In addition, the extracts inhibited pro-oxidant-induced lipid peroxidation in penile tissue homogenate. HPLC-DAD analysis showed that CG is richer in phenolic compounds than EL, and this could be responsible for higher biological activities observed in CG than EL. Hence, the observed antioxidant property and inhibitory action of CG and EL on enzymes relevant to erectile dysfunction in vitro could be part of possible mechanisms underlying their involvement in traditional medicine for the management of male sexual dysfunction.

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

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Melo-Silveira, Raniere Fagundes; Fidelis, Gabriel Pereira; Costa, Mariana Santana Santos Pereira; Telles, Cinthia Beatrice Silva; Dantas-Santos, Nednaldo; de Oliveira Elias, Susana; Ribeiro, Vanessa Bley; Barth, Afonso Luis; Macedo, Alexandre José; Leite, Edda Lisboa; Rocha, Hugo Alexandre Oliveira

2012-01-01

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. PMID:22312261

Modulation of platelet functions by crude rice (Oryza sativa) bran policosanol extract.

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Wong, Wai-Teng; Ismail, Maznah; Imam, Mustapha Umar; Zhang, Yi-Da

2016-07-28

Rice bran is bioactive-rich and has proven health benefits for humans. Moreover, its source, the brown rice has antioxidant, hypolipidemic and other functional properties that are increasingly making it a nutritional staple especially in Asian countries. This study investigated the antiplatelet aggregation mechanisms of crude hexane/methanolic rice bran extract, in which policosanol was the targeted bioactive. Platelets play a vital role in pathogenesis of atherosclerosis and cardiovascular diseases, and their increased activities could potentially cause arterial thrombus formation or severe bleeding disorders. Thus, in this study, platelet aggregation and adhesion of platelets to major components of basal lamina were examined in vitro. In addition, cellular protein secretion was quantified as a measurement of platelet activation. Adenosine diphosphate (ADP), collagen, and arachidonic acid (AA)-induced aggregation were studied using the microtiter technique. Rat platelets were pre-treated with various concentrations of policosanol extract, and the adhesion of platelets onto collagen- and laminin-coated surface (extracellular matrix) was studied using the acid phosphatase assay. The effect of crude policosanol extract on released proteins from activated platelets was measured using modified Lowry determination method. Rice bran policosanol extract significantly inhibited in vitro platelet aggregation induced by different agonists in a dose dependent manner. The IC50 of ADP-, collagen-, and AA-induced platelet aggregation were 533.37 ± 112.16, 635.94 ± 78.45 and 693.86 ± 70.57 μg/mL, respectively. The present study showed that crude rice bran policosanol extract significantly inhibited platelet adhesion to collagen in a dose dependent manner. Conversely, at a low concentration of 15.625 μg/mL, the extract significantly inhibited platelet adhesion to laminin stimulated by different platelet agonists. In addition to the alteration of cell adhesive

Extracts of Canadian first nations medicinal plants, used as natural products, inhibit neisseria gonorrhoeae isolates with different antibiotic resistance profiles.

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Cybulska, Paulina; Thakur, Sidharath D; Foster, Brian C; Scott, Ian M; Leduc, Renée I; Arnason, John T; Dillon, Jo-Anne R

2011-07-01

Neisseria gonorrhoeae (Ng) has developed resistance to most antimicrobial agents and the antibiotics recommended for therapy are restricted, for the most part, to third generation cephalosporins. In order to investigate new potential sources of antimicrobial agents, the antibacterial properties of 14 Canadian plants used in traditional First Nations' medicine were tested against Ng isolates having differing antimicrobial susceptibility profiles. Ethanolic extracts of 14 Canadian botanicals, analyzed by high-performance liquid chromatography, were tested for their antimicrobial activity (disc diffusion and/or agar dilution assays) against susceptible Ng reference strains and a panel of 28 Ng isolates with various antimicrobial resistance profiles. Extracts of Arctostaphylos uva ursi (kinnikinnick or bearberry), Hydrastis canadensis (goldenseal), Prunus serotina (black cherry), and Rhodiola rosea (roseroot) inhibited the growth of all Ng isolates with minimum inhibitory concentrations of 32 μg/mL, 4 to 32 μg/mL, 16 to >32 μg/mL, and 32 to 64 μg/mL, respectively. Extracts of Acorus americanus (sweet flag), Berberis vulgaris (barberry), Cimicifuga racemosa (black cohosh), Equisetum arvense (field horsetail), Gaultheria procumbens (wintergreen), Ledum groenlandicum (Labrador tea), Ledum palustre (marsh Labrador tea), Oenothera biennis (common evening primrose), Sambucus nigra (elderberry), and Zanthoxylum americanum (prickly ash) had weak or no antimicrobial activity against the Ng isolates with minimum inhibitory concentrations ≥256 μg/mL. The phytochemical berberine from H. canadensis inhibited the growth of all Ng isolates. The phytochemicals, salidroside and rosavin, present in R. rosea, also showed inhibitory activity against Ng strains. Canadian botanicals represent a potential source of novel compounds which inhibit Ng, including isolates resistant to antibiotics.

Antinociceptive and antioxidant activities of the methanolic extract of Telfairia occidentalis Seeds

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Olukemi Adetutu Osukoya

2016-01-01

Full Text Available Context: The seeds of Telfairia occidentalis have been known to possess different biological properties and are used in traditional medicine in Africa and Asia to treat many ailments. The plant is particularly noted traditionally for its healing properties and is usually consumed in the form of herbal decoctions/concoctions as a blood tonic, to treat sudden attacks of convulsions, pain, malaria and anaemia. Aims: In the present study, various phytochemical and pharmacological studies were done on the methanolic extract of the seeds of Telfairia occidentalis to evaluate its antioxidant and antinociceptive properties to substantiate its traditional use. Methods: Phytochemical screening of the extract was done according to standard procedures. Antioxidant potential was ascertained using 2,2-diphenyl-1-picryl hydrazyl (DPPH scavenging activity, total phenolic content and total flavonoid content assays. Analgesic activity was analyzed using formalin induced paw licking test in albino rats at 100, 200 and 400 mg extract per kg body weight. Statistical Analysis Used: All results extrapolated from the experiments were expressed as mean ± SEM. Data obtained was analyzed statistically using ANOVA (one-way followed by Dennett's posthoc test. Results: Phytochemicals present in the extract were alkaloids, flavonoids, saponins, terpenoids, steroid and anthraquinones. The extract significantly inhibited DPPH scavenging activity with percentage inhibition of 147.3%. The methanolic seed extract of T. occidentalis significantly reduced (P < 0.05 formalin induced paw licking in both neurogenic and inflammatory phases of formalin induced paw licking test, with 35.59 and 78.51% inhibition at 400 mg/kg, in albino rats in a dose dependent manner. Conclusions: The seed extract in this study significantly reduced formalin induced hind paw licking, and could be used as an analgesic for treatment of pain and also showed marked antioxidant potential.

Inhibition of Corrosion of Carbon Steel in 3.5% NaCl Solution by Myrmecodia Pendans Extract

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Atria Pradityana

2016-01-01

Full Text Available Inhibitor is a substance that is added to the corrosive media to inhibit corrosion rate. Organic inhibitors are preferred to inorganic ones since they are environmentally friendly. One of the organic compounds which is rarely reported as a corrosion inhibitor is Myrmecodia Pendans. The organic compounds can be adsorbed on the metal surface and block the active surface to reduce the rate of corrosion. In this study, the used pipe was carbon steel API 5L Grade B with 3.5% NaCl solution as the corrosion medium. The objective of this research was to analyze the inhibition mechanism Myrmecodia Pendans towards carbon steel in a corrosion medium. Concentration variations of extract Myrmecodia Pendans were 0–500 ppm. Fourier Transform Infrared (FTIR was used for chemical characterization of Myrmecodia Pendans. Polarization and Electrochemical Impedance Spectroscopy (EIS were used to measure the corrosion rate and behaviour. From the electrochemical measurements, it was found that the addition of 400 mg/L inhibitor gave the highest inhibition efficiency. Myrmecodia Pendans acted as a corrosion inhibitor by forming a thin layer on the metal surface.

Inhibition of lung cancer cells A549 and H460 by curcuminoid extracts and nanoemulsions prepared from Curcuma longa Linnaeus

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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

Optimal Fermentation Conditions of Hyaluronidase Inhibition Activity on Asparagus cochinchinensis Merrill by Weissella cibaria.

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Kim, Minji; Kim, Won-Baek; Koo, Kyoung Yoon; Kim, Bo Ram; Kim, Doohyun; Lee, Seoyoun; Son, Hong Joo; Hwang, Dae Youn; Kim, Dong Seob; Lee, Chung Yeoul; Lee, Heeseob

2017-04-28

This study was conducted to evaluate the hyaluronidase (HAase) inhibition activity of Asparagus cochinchinesis (AC) extracts following fermentation by Weissella cibaria through response surface methodology. To optimize the HAase inhibition activity, a central composite design was introduced based on four variables: the concentration of AC extract ( X 1 : 1-5%), amount of starter culture ( X 2 : 1-5%), pH ( X 3 : 4-8), and fermentation time ( X 4 : 0-10 days). The experimental data were fitted to quadratic regression equations, the accuracy of the equations was analyzed by ANOVA, and the regression coefficients for the surface quadratic model of HAase inhibition activity in the fermented AC extract were estimated by the F test and the corresponding p values. The HAase inhibition activity indicated that fermentation time was most significant among the parameters within the conditions tested. To validate the model, two different conditions among those generated by the Design Expert program were selected. Under both conditions, predicted and experimental data agreed well. Moreover, the content of protodioscin (a well-known compound related to anti-inflammation activity) was elevated after fermentation of the AC extract at the optimized fermentation condition.

Antinociceptive and anti-inflammatory effects of Urtica dioica leaf extract in animal models.

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Hajhashemi, Valiollah; Klooshani, Vahid

2013-01-01

This study was aimed to examine the antinociceptive and anti-inflammatory effects of Urtica dioica leaf extract in animal models. Hydroalcoholic extract of the plant leaves was prepared by percolation method. Male Swiss mice (25-35 g) and male Wistar rats (180-200 g) were randomly distributed in control, standard drug, and three experimental groups (n=6 in each group). Acetic acid-induced writhing, formalin test, and carrageenan-induced paw edema were used to assess the antinociceptive and anti-inflammatory effects. The extract dose-dependently reduced acetic acid-induced abdominal twitches. In formalin test, the extract at any of applied doses (100, 200, and 400 mg/kg) could not suppress the licking behavior of first phase while doses of 200 and 400 mg/kg significantly inhibited the second phase of formalin test. In carrageenan test, the extract at a dose of 400 mg/kg significantly inhibited the paw edema by 26%. The results confirm the folkloric use of the plant extract in painful and inflammatory conditions. Further studies are needed to characterize the active constituents and the mechanism of action of the plant extract.

Protective effects of a standard extract of Mangifera indica L. (VIMANG) against mouse ear edemas and its inhibition of eicosanoid production in J774 murine macrophages.

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Garrido, G; González, D; Lemus, Y; Delporte, C; Delgado, R

2006-06-01

A standard aqueous extract of Mangifera indica L., used in Cuba as antioxidant under the brand name VIMANG, was tested in vivo for its anti-inflammatory activity, using commonly accepted assays. The standard extract of M. indica, administered orally (50-200mg/kg body wt.), reduced ear edema induced by arachidonic acid (AA) and phorbol myristate acetate (PMA) in mice. In the PMA model, M. indica extract also reduced myeloperoxidase (MPO) activity. In vitro studies were performed using macrophage cell line J774 stimulated with pro-inflammatory stimuli lipopolysaccharide-interferon gamma (LPS-IFNgamma) or calcium ionophore A23187 to determine prostaglandin PGE(2) or leukotriene LTB(4) release, respectively. The extract inhibited the induction of PGE(2) and LTB(4) with IC(50) values of 21.7 and 26.0microg/ml, respectively. Mangiferin (a glucosylxanthone isolated from the extract) also inhibited these AA metabolites (PGE(2), IC(50) value=17.2microg/ml and LTB(4), IC(50) value=2.1microg/ml). These results represent an important contribution to the elucidation of the mechanism involved in the anti-inflammatory and anti-nociceptive effects reported for the standard extract of M. indica VIMANG.

Chilean native fruit extracts inhibit inflammation linked to the pathogenic interaction between adipocytes and macrophages.

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Reyes-Farias, Marjorie; Vasquez, Karla; Ovalle-Marin, Angelica; Fuentes, Francisco; Parra, Claudia; Quitral, Vilma; Jimenez, Paula; Garcia-Diaz, Diego F

2015-05-01

Obesity is characterized by an increase in the infiltration of monocytes into the adipose tissue, causing an inflammatory condition associated with, for example, the development of insulin resistance. Thus, anti-inflammatory-based treatments could emerge as a novel and interesting approach. It has been reported that Chilean native fruits maqui (Aristotelia chilensis) and calafate (Berberis microphylla) present high contents of polyphenols, which are known for their antioxidant and anti-inflammatory properties. The aim of this study was to evaluate the ability of extracts of these fruits to block the pathogenic interaction between adipocytes and macrophages in vitro and to compare its effect with blueberry (Vaccinium corymbosum) extract treatment, which has been already described to possess several biomedical benefits. RAW264.7 macrophages were treated with 5 μg/mL lipopolysaccharides (LPS), with conditioned media (CM) from fully differentiated 3T3-L1 adipocytes, or in a coculture (CC) with 3T3-L1 adipocytes, in the presence or absence of 100 μM [total polyphenolic content] of each extract for 24 h. The gene expression and secretion profile of several inflammatory markers were evaluated. Nitric oxide secretion induced by LPS, CM, and CC was reduced by the presence of maqui (-12.2%, -45.6%, and -14.7%, respectively) and calafate (-27.6%, -43.9%, and -11.8%, respectively) extracts. Gene expression of inducible nitric oxide synthase and TNF-α was inhibited and of IL-10 was induced by maqui and calafate extract incubation. In conclusion, the extracts of these fruits present important inhibitory-like features over the inflammatory response of the interaction between adipocytes and macrophages, comprising a potential therapeutic tool against comorbidities associated with obesity development.

Chilean Native Fruit Extracts Inhibit Inflammation Linked to the Pathogenic Interaction Between Adipocytes and Macrophages

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Reyes-Farias, Marjorie; Vasquez, Karla; Ovalle-Marin, Angelica; Fuentes, Francisco; Parra, Claudia; Quitral, Vilma; Jimenez, Paula

2015-01-01

Abstract Obesity is characterized by an increase in the infiltration of monocytes into the adipose tissue, causing an inflammatory condition associated with, for example, the development of insulin resistance. Thus, anti-inflammatory-based treatments could emerge as a novel and interesting approach. It has been reported that Chilean native fruits maqui (Aristotelia chilensis) and calafate (Berberis microphylla) present high contents of polyphenols, which are known for their antioxidant and anti-inflammatory properties. The aim of this study was to evaluate the ability of extracts of these fruits to block the pathogenic interaction between adipocytes and macrophages in vitro and to compare its effect with blueberry (Vaccinium corymbosum) extract treatment, which has been already described to possess several biomedical benefits. RAW264.7 macrophages were treated with 5 μg/mL lipopolysaccharides (LPS), with conditioned media (CM) from fully differentiated 3T3-L1 adipocytes, or in a coculture (CC) with 3T3-L1 adipocytes, in the presence or absence of 100 μM [total polyphenolic content] of each extract for 24 h. The gene expression and secretion profile of several inflammatory markers were evaluated. Nitric oxide secretion induced by LPS, CM, and CC was reduced by the presence of maqui (−12.2%, −45.6%, and −14.7%, respectively) and calafate (−27.6%, −43.9%, and −11.8%, respectively) extracts. Gene expression of inducible nitric oxide synthase and TNF-α was inhibited and of IL-10 was induced by maqui and calafate extract incubation. In conclusion, the extracts of these fruits present important inhibitory-like features over the inflammatory response of the interaction between adipocytes and macrophages, comprising a potential therapeutic tool against comorbidities associated with obesity development. PMID:25302660

Anti-nociceptive and anti-inflammatory activities of ethanolic flower extract of Newbouldia laevis in mice and rats

OpenAIRE

Y Tanko; B Kamba; MI Saleh; K Y Musa; A Mohammed

2008-01-01

Summary: The ethanolic flower extract of Newbouldia laevis was investigated for possible anti-nociceptive and anti-inflammatory effects in rodents. Acetic acid induced writhing (in mice) and formalin tests (in rats) were used to study. The extract caused a significant decrease (P< 0.05), which was not dose a dependent inhibition on acetic acid-induced writhing and the neurogenic pain induced by formalin. The extract at the doses (25, 50 and 100mg/kg) tested showed 59, 71 and 47% inhibition...

Inhibition of Tanshinone IIA, Salvianolic Acid A and Salvianolic Acid B on Areca Nut Extract-Induced Oral Submucous Fibrosis in Vitro

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Jian-Ping Dai

2015-04-01

Full Text Available Salvia miltiorrhiza Bunge has been reported to possess excellent antifibrotic activity. In this study, we have investigated the effect and mechanism of tanshinone IIA (Tan-IIA, salvianolic acid A (Sal-A and salvianolic acid B (Sal-B, the important active compounds of Salvia miltiorrhiza Bunge, on areca nut extract (ANE-induced oral submucous fibrosis (OSF in vitro. Through human procollagen gene promoter luciferase reporter plasmid assay, hydroxyproline assay, gelatin zymography assay, qRT-PCR, ELISA and Western blot assay, the influence of these three compounds on ANE-stimulated cell viability, collagen accumulation, procollagen gene transcription, MMP-2/-9 activity, MMP-1/-13 and TIMP-1/-2 expression, cytokine secretion and the activation of PI3K/AKT, ERK/JNK/p38 MAPK and TGF-β/Smads pathways were detected. The results showed that Tan-IIA, Sal-A and Sal-B could significantly inhibit the ANE-stimulated abnormal viability and collagen accumulation of mice oral mucosal fibroblasts (MOMFs, inhibit the transcription of procollagen gene COL1A1 and COL3A1, increase MMP-2/-9 activity, decrease TIMP-1/-2 expression and inhibit the transcription and release of CTGF, TGF-β1, IL-6 and TNF-α; Tan-IIA, Sal-A and Sal-B also inhibited the ANE-induced activation of AKT and ERK MAPK pathways in MOMFs and the activation of TGF-β/Smads pathway in HaCaT cells. In conclusion, Tan-IIA, Sal-A and Sal-B possess excellent antifibrotic activity in vitro and can possibly be used to promote the rehabilitation of OSF patients.

Aqueous Extracts of the Marine Brown Alga Lobophora variegata Inhibit HIV-1 Infection at the Level of Virus Entry into Cells

KAUST Repository

Kremb, Stephan

2014-08-21

In recent years, marine algae have emerged as a rich and promising source of molecules with potent activities against various human pathogens. The widely distributed brown alga Lobophora variegata that is often associated with tropical coral reefs exerts strong antibacterial and antiprotozoal effects, but so far has not been associated with specific anti-viral activities. This study investigated potential HIV-1 inhibitory activity of L. variegata collected from different geographical regions, using a cell-based full replication HIV-1 reporter assay. Aqueous L. variegata extracts showed strong inhibitory effects on several HIV-1 strains, including drug-resistant and primary HIV-1 isolates, and protected even primary cells (PBMC) from HIV-1-infection. Anti-viral potency was related to ecological factors and showed clear differences depending on light exposition or epiphyte growth. Assays addressing early events of the HIV-1 replication cycle indicated that L. variegata extracts inhibited entry of HIV-1 into cells at a pre-fusion step possibly by impeding mobility of virus particles. Further characterization of the aqueous extract demonstrated that even high doses had only moderate effects on viability of cultured and primary cells (PBMCs). Imaging-based techniques revealed extract effects on the plasma membrane and actin filaments as well as induction of apoptosis at concentrations exceeding EC50 of anti-HIV-1 activity by more than 400 fold. In summary, we show for the first time that L. variegata extracts inhibit HIV-1 entry, thereby suggesting this alga as promising source for the development of novel HIV-1 inhibitors.

Gossipium hirsutum L. extract as green corrosion inhibitor for ...

African Journals Online (AJOL)

Inhibitive effect of Gossipium hirsutum L. leaves extract on the acid corrosion of aluminum in 1 M HCl solution was studied by weight loss technique. The extract at optimum concentration inhibited the corrosion of aluminum, with about 92% inhibition efficiency and the inhibition efficiency increased with increasing ...

Pedilanthus tithymaloides Inhibits HSV Infection by Modulating NF-κB Signaling.

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Durbadal Ojha

Full Text Available Pedilanthus tithymaloides (PT, a widely used ethnomedicinal plant, has been employed to treat a number of skin conditions. To extend its utility and to fully exploit its medicinal potential, we have evaluated the in vitro antiviral activity of a methanolic extract of PT leaves and its isolated compounds against Herpes Simplex Virus type 2 (HSV-2. Bioactivity-guided studies revealed that the extract and one of its constituents, luteolin, had potent antiviral activity against wild-type and clinical isolates of HSV-2 (EC50 48.5-52.6 and 22.4-27.5 μg/ml, respectively, with nearly complete inhibition at 86.5-101.8 and 40.2-49.6 μg/ml, respectively. The inhibitory effect was significant (p<0.001 when the drug was added 2 h prior to infection, and was effective up to 4 h post-infection. As viral replication requires NF-κB activation, we examined whether the observed extract-induced inhibition of HSV-2 was related to NF-κB inhibition. Interestingly, we observed that treatment of HSV-2-infected cells with extract or luteolin suppressed NF-κB activation. Although NF-κB, JNK and MAPK activation was compromised during HSV replication, neither the extract nor luteolin affected HSV-2-induced JNK1/2 and MAPK activation. Moreover, the PT leaf extract and luteolin potently down-regulated the expression of tumor necrosis factor (TNF-α, Interleukin (IL-1β, IL-6, NO and iNOS and the production of gamma interferon (IFN-γ, which are directly involved in controlling the NF-κB signaling pathway. Thus, our results indicate that both PT leaf extract and luteolin modulate the NF-κB signaling pathway, resulting in the inhibition of HSV-2 replication.

Inhibitory effects of rosmarinic acid extracts on porcine pancreatic amylase in vitro.

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McCue, Patrick P; Shetty, Kalidas

2004-01-01

Porcine pancreatic alpha-amylase (PPA) was allowed to react with herbal extracts containing rosmarinic acid (RA) and purified RA. The derivatized enzyme-phytochemical mixtures obtained were characterized for residual amylase activity. These in vitro experiments showed that the amylase activity was inhibited in the presence of these phytochemicals. The extent of amylase inhibition correlated with increased concentration of RA. RA-containing oregano extracts yielded higher than expected amylase inhibition than similar amount of purified RA, suggesting that other phenolic compounds or phenolic synergies may contribute to additional amylase inhibitory activity. The significance of food-grade, plant-based amylase inhibitors for modulation of diabetes mellitus and other oxidation-linked diseases is hypothesized and discussed.

Gardenia jasminoides extracts and gallic acid inhibit lipopolysaccharide-induced inflammation by suppression of JNK2/1 signaling pathways in BV-2 cells

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Wen-Hung Lin

2015-06-01

Conclusion:Taken together, these results indicate that the protective mechanism of the GJ extract involves an antioxidant effect and inhibition of JNK2/1 MAP kinase and COX-2 expressions in LPS-induced inflammation of BV-2 cells.

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.

Osteoprotective effects of Fructus Ligustri Lucidi aqueous extract in aged ovariectomized rats

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Fung Kwok

2010-11-01

Full Text Available Abstract Background Fructus Ligustri Lucidi (FLL is a commonly used herb for treating bone disorders in Chinese medicine. The present study investigates the anti-osteoporotic activity of FLL aqueous extract in the model of postmenopausal bone loss in aged ovariectomized (OVX female rats. Methods After eight weeks of treatment of FLL or water, the lumbar spine was scanned by peripheral quantitative computed tomography (pQCT. Effects of FLL water extract on osteogenic and adipogenic differentiations in rat mesenchymal stem cells (MSCs were assessed by biochemical methods and staining. Results FLL aqueous extract significantly inhibited bone mineral density (BMD loss in total, trabecular and cortical bones without affecting body weight and uterus wet weight. FLL extract significantly promoted osteogenesis and suppressed adipogenesis in MSCs as indicated by the elevated alkaline phosphatase activity, calcium deposition levels and decreased adipocyte number in a dose-dependent manner without cytotoxic effects. Real-time PCR analysis revealed significant increase of osteoprotegerin (OPG-to-receptor activator for nuclear factor-κB ligand (RANKL mRNA, indicating a decrease in osteoclastogenesis. Conclusion The present study demonstrates the osteoprotective effects of FLL aqueous extract on aged OVX rats, stimulation of osteogenesis, inhibition of adipogenesis and osteoclastogenesis in MSCs.

Activity of the aqueous extract of Schinus terebinthifolius Raddi on strains of the Candida genus.

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Torres, Kátia Andrea de Menezes; Lima, Sônia Maria Rolim Rosa; Ueda, Suely Mitoi Ykko

2016-12-01

Objectives  To evaluate the antifungal susceptibility profile of the aqueous extract of the bark of Schinus terebinthifolius Raddi against the strains of the genus Candida . Methods  By using the disk diffusion method, 50 samples of the genus Candida ( Candida albicans ; Candida krusei ; Candida glabrata ; and Candida tropicalis ), isolated from patients receiving treatment at Hospital Santa Casa de Misericórdia de São Paulo, and 1 American Type Culture Collection (ATCC) sample of each species were tested against: the isolated aqueous extract of the bark of Schinus terebinthifolius Raddi, isolated nystatin, and the association of nystatin and the aqueous extract of Schinus terebinthifolius Raddi. Results  There were no significant differences regarding the different strains of Candida tested. In the presence of the aqueous extract of Schinus terebinthifolius Raddi, no inhibition halo was visible. Isolated nystatin formed an inhibition halo measuring respectively 18.50 mm and 19.50 mm for the Candida albicans species and the others referred to as non- Candida albicans ( Candida krusei ; Candida glabrata ; and Candida tropicalis ). The association of nystatin and the aqueous extract of Schinus terebinthifolius Raddi resulted in inhibition halos measuring 14.25 mm and 16.50 mm respectively. The comparisons of these results are statistically significant ( p  Schinus terebinthifolius Raddi showed no antifungal activity in vitro against the strains tested, whereas the association of nystatin and the aqueous extract of Schinus terebinthifolius Raddi caused a decrease in the inhibition halo when compared with isolated nystatin. Thieme-Revinter Publicações Ltda Rio de Janeiro, Brazil.

Comparative Study of Erythrina indica Lam. (Febaceae) Leaves Extracts for Antioxidant Activity

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Sakat, SS; Juvekar, AR

2010-01-01

The present study was designed to investigate the antioxidant activity of aqueous and methanol extracts of Erythrina indica Lam leaves by in vitro methods viz. 1, 1-Diphenyl-2-Picrylhydrazyl, nitric oxide radical scavenging activity, and inhibition of lipid peroxidation by thiobarbituric acid reactive substances (TBARS) method on isolated rat liver tissues. Quantitative analysis of antioxidative components like total amount of phenolics, flavonoids, and flavonols were estimated using the spectrophotometric method. Linear regression analysis was used to calculate the IC50 value. Results showed that the aqueous and methanol extracts exhibited significant DPPH radicals scavenging activity with an IC50 value 342.59 ± 19.59, 283.24 ± 12.28 µg/mL respectively. Nitric oxide radicals were significantly scavenged by the aqueous and methanol extracts (IC50 = 250.12 ± 10.66; 328.29 ± 3.74 µg/mL). Lipid peroxidation induced by the Fe2+ was inhibited by the aqueous extract with low IC50 value (97.29 ± 2.05 µg/mL) as compared to methanol extract (IC50 = 283.74 ± 5.70 µg/mL). Both the extracts were exhibited similar quantities of total phenolics. Total flavonoids were found to be in higher quantities than total flavonols in aqueous extract as compared to methanol extract. From the results, it is concluded that the aqueous and methanol extracts of E. indica leaves possesses significant antioxidant activity that may be due to the presence of flavonoids and related polyphenolic compounds. PMID:21331194

Aspergillus ficuum phytase activity is inhibited by cereal grain components.

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Bekalu, Zelalem Eshetu; Madsen, Claus Krogh; Dionisio, Giuseppe; Brinch-Pedersen, Henrik

2017-01-01

In the current study, we report for the first time that grain components of barley, rice, wheat and maize can inhibit the activity of Aspergillus ficuum phytase. The phytase inhibition is dose dependent and varies significantly between cereal species, between cultivars of barley and cultivars of wheat and between Fusarium graminearum infected and non-infected wheat grains. The highest endpoint level of phytase activity inhibition was 90%, observed with grain protein extracts (GPE) from F. graminearum infected wheat. Wheat GPE from grains infected with F. graminearum inhibits phytase activity significantly more than GPE from non-infected grains. For four barley cultivars studied, the IC50 value ranged from 0.978 ± 0.271 to 3.616 ± 0.087 mg×ml-1. For two non-infected wheat cultivars investigated, the IC50 values were varying from 2.478 ± 0.114 to 3.038 ± 0.097 mg×ml-1. The maize and rice cultivars tested gaveIC50 values on 0.983 ± 0.205 and 1.972 ± 0.019 mg×ml-1, respectively. After purifying the inhibitor from barley grains via Superdex G200, an approximately 30-35 kDa protein was identified. No clear trend for the mechanism of inhibition could be identified via Michaelis-Menten kinetics and Lineweaver-Burk plots. However, testing of the purified phytase inhibitor together with the A. ficuum phytase and the specific protease inhibitors pepstatin A, E64, EDTA and PMSF revealed that pepstatin A repealed the phytase inhibition. This indicates that the observed inhibition of A. ficuum phytase by cereal grain extracts is caused by protease activity of the aspartic proteinase type.

Bioactivity of Neem (Azadirachta indica) callus extract

International Nuclear Information System (INIS)

Ahmed, I.M.

2008-04-01

This study was conducted in order to explore the possibility of utilizing plant tissue culture techniques for production of secondary metabolites from callus culture of Azadirachta indica (Neem) and to investigate the bioactivity of the established callus extract in comparison with the extract from the intact leaves. The presence of secondary metabolites in the extracts was detected by Thin Layer Chromatography (TLC). Both the callus and leaf extracts eluted five fraction of compounds and it were observed that callus extract had a good resolution. various extract concentration (5.10. and 20 mg/ml) were determined for the rate and extent of inhibition kinetics against staphylococcus aureus. Escherichia coli, and candida albicans. Results showed that callus extract of A. indica wiped out all viable cells of C. albicans within 18 hours and the subsequent concentration 5 and 10 mg/ m1 retard the growth after 24 h. A higher concentration of 20 mg/ ml had the same effect on S. aureus after 6 h and the E. coli cells were completely inhibited by the extracts after 24 h. Similar kinetics were showed by leaf extract but in slight rate as compared to the callus extract. In general both extract posses antimicrobial activity with notable efficient rates. For assaying of the inhibitory effect on some phyto pathogens the effect of different concentrations of the callus and leaf extracts on the radial growth of Drechslera rostrata. Fusarium oxysporum and Alterneria alternata were in vitro assessed. Obvious inhibitory effect was observed on the mycelia radial growth of the three treated fungi. The level of inhibition increased with the increase of te extract concentration. The maximum inhibitory effect (84%) was recorded with Drechslera rostrata when inoculated in media contain 20 mg/ ml of callus while the inhibition rate of mycelia growth of the same species reaches 61% when inoculated in a medium contain the same concentration of the neem leaf extract. The subsequent

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.

Effectiveness test of bay leaf extract (Eugenia polyantha on the growth of Staphylococcus aureus in vitro

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Taufik Azhari

2016-06-01

Full Text Available Staphylococcus aureus (S. aureus is a facultative anaerobic bacteria and one of the normal microflora in the mouth. However, if it is influenced by predisposing factors, it would be pathogenic. Bay leaves have an active ingredient that is tannins, flavonoids, and essential oils are believed to have antibacterial effects. The purpose of this study is to determine how much the effectiveness of extracts of leaves produced by the growth of S.aureus. This research is an experimental laboratory. The research sample is S. aureus in preparations. Dilution bay leaf extract, among others, 12.5%, 25%, 50%, 75% and 100%, respectively. Inhibition was obtained by measuring the inhibition zone formed around the paper disks using calipers. Statistical analyzes were performed using one way ANOVA test. The results showed that the diameter of the zone of inhibition for S.aureus at a concentration of 12.5% leaves extract (7.29 mm; 25% (7.7 mm; 50% (8.75 mm; 75% (9.34 mm; 100% (9.78 mm. In the statistical analysis of the results showed a significant difference from the respective bay leaf extract concentration. Bay leaf extract can inhibit the growth of S. aureus bacteria. However, it is still not effective to inhibit bacteria as the result of inhibition zones obtained relatively small at less than 10 mm.

Antioxidant activity, inhibition of nitric oxide overproduction, and in vitro antiproliferative effect of maple sap and syrup from Acer saccharum.

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Legault, Jean; Girard-Lalancette, Karl; Grenon, Carole; Dussault, Catherine; Pichette, André

2010-04-01

Antioxidant activity, inhibition of nitric oxide (NO) overproduction, and antiproliferative effect of ethyl acetate extracts of maple sap and syrup from 30 producers were evaluated in regard to the period of harvest in three different regions of Québec, Canada. Oxygen radical absorbance capacity (ORAC) values of maple sap and syrup extracts are, respectively, 12 +/- 6 and 15 +/- 5 micromol of Trolox equivalents (TE)/mg. The antioxidant activity was also confirmed by a cell-based assay. The period of harvest has no statistically significant incidence on the antioxidant activity of both extracts. The antioxidant activity of pure maple syrup was also determined using the ORAC assay. Results indicate that the ORAC value of pure maple syrup (8 +/- 2 micromol of TE/mL) is lower than the ORAC value of blueberry juice (24 +/- 1 micromol of TE/mL) but comparable to the ORAC values of strawberry (10.7 +/- 0.4 micromol of TE/mL) and orange (10.8 +/- 0.5 micromol of TE/mL) juices. Maple sap and syrup extracts showed to significantly inhibit lipopolysaccharide-induced NO overproduction in RAW264.7 murine macrophages. Maple syrup extract was significantly more active than maple sap extract, suggesting that the transformation of maple sap into syrup increases NO inhibition activity. The highest NO inhibition induced by the maple syrup extracts was observed at the end of the season. Moreover, darker maple syrup was found to be more active than clear maple syrup, suggesting that some colored oxidized compounds could be responsible in part for the activity. Finally, maple syrup extracts (50% inhibitory concentration = 42 +/- 6 microg/mL) and pure maple syrup possess a selective in vitro antiproliferative activity against cancer cells.

Analysis of anti-bacterial and anti oxidative activity of Azadirachta indica bark using various solvents extracts

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Raid Al Akeel

2017-01-01

Full Text Available Herbal medications have been used for relief of symptoms of disease. Regardless of the great advances observed in current medicine in recent decades, plants still make a significant contribution to health care. An alarming increase in bacterial strains resistant to a number of antimicrobial agents demands that a renewed effort be made to seek antibacterial agents effective against pathogenic bacteria resistant to or less sensitive to current antibiotics. Anti-bacterial activity of Azadirachta indica stem bark was tested against pathogenic Salmonella paratyphi and Salmonella typhi using various solvent extracts. The in vitro anti-bacterial activity was performed by agar well diffusion method and the results were expressed as the average diameter of zone of inhibition of bacterial growth around the well. The ethanol and methanol extracts showed better anti-bacterial activity with zone of inhibition (20–25 mm when compared with other tested extracts and standard antibiotic Erythromycin (15 mcg with zone of inhibition (13–14 mm. Using Fisher’s exact test of significance difference was found between two Salmonella strains sensitivity patterns against tested extracts (P ⩽ 0.035. Extracts of A. indica stem bark also exhibited significant antioxidant activity, thus establishing the extracts as an antioxidant. The results obtained in this study give some scientific support to the A. indica stem bark for further investigation of compounds and in future could be used as drug.

Ethanolic Extract of Traditional Chinese Medicine (TCM) Gamboge Inhibits Colon Cancer via the Wnt/Beta-Catenin Signaling Pathway in an Orthotopic Mouse Model.

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Wang, Wei; Li, Youran; Chen, Yiqi; Chen, Hongjin; Zhu, Ping; Xu, Minmin; Wang, Hao; Wu, Minna; Yang, Zhijian; Hoffman, Robert M; Gu, Yunfei

2018-04-01

The aim of the present study was to investigate the efficacy of an ethanolic extract of gamboge (EEG), a traditional Chinese medicine (TCM), both in vitro on colon cancer cells and in vivo in an orthotopic mouse model of human colon cancer. The in vitro cytotoxicity of EEG on colon cancer cells was determined with the CCK8 proliferation assay and the Annexin V-PE/7-AAD apoptosis assay. Efficacy of EEG in vivo was evaluated in an orthotopic mouse model of human colon cancer implated with the green fluorescent protein-expressing human colon cancer cell line SW480-GFP. The tumor-bearing mice were treated with vehicle (0.2 ml/dose normal saline, po, daily), irinotecan (50 mg/kg/dose, ip, twice a week), 5-FU (15 mg/kg/dose, ip, every other day) as positive controls or EEG at doses of 12.5, 25 and 50 mg/kg/dose, po, daily. Real-time fluorescence imaging was performed to determine tumor inhibition in each treated group compared to the untreated controls. The protein expression of β-catenin, MMP-7, cyclin D1 and E-cadherin in the tumors was analyzed by immunohistochemistry. EEG significantly induced proliferation inhibition and apoptosis of SW480 colon cancer cells in vitro in a dose-dependent manner. Tumor growth in the colon-cancer orthotopic model was significantly inhibited by irinotecan, 5-FU and all three doses of EEG. The efficacy of EEG was comparable to irinotecan and 5-FU. Irinotecan, 5-FU and 50 mg/kg EEG significantly decreased the protein expression of β-catenin and MMP-7. Cyclin D1 expression was decreased and E-cadherin expression was increased by irinotecan, 5-FU and all three doses of EEG. The present study demonstrates anti-tumor efficacy of EEG on colon cancer both in vitro and in vivo through inducing proliferation inhibition and apoptosis of SW480 colon cancer cells and inhibiting tumor growth, respectively. EEG exerts anti-tumor activity at least partly via down-regulation of the Wnt/β-catenin signaling pathway. Copyright© 2018, International

Analgesic and anti-inflammatory effects of Mangifera indica L. extract (Vimang).

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Garrido, G; González, D; Delporte, C; Backhouse, N; Quintero, G; Núñez-Sellés, A J; Morales, M A

2001-02-01

Vimang is an aqueous extract of Mangifera indica used in Cuba to improve the quality of life in patients suffering from elevated stress. To assess its possible analgesic and antiinflammatory effects, the results of a standard extract evaluation are presented. Analgesia was determined using acetic acid-induced abdominal constriction and formalin-induced licking. Antiinflammatory effects were evaluated using carrageenan- and formalin-induced oedema. Vimang (50-1000 mg/kg, p.o.) exhibited a potent and dose-dependent antinociceptive effect against acetic acid test in mice. The mean potency (DE(50)) was 54.5 mg/kg and the maximal inhibition attained was 94.4%. Vimang (20-1000 mg/kg, p.o.) dose-dependently inhibited the second phase of formalin-induced pain but not the first phase. The DE(50) of the second phase was 8.4 mg/kg and the maximal inhibition was 99.5%, being more potent than indomethacin at doses of 20 mg/kg. Vimang (20-1000 mg/kg, p.o.) significantly inhibited oedema formation (p Vimang could account for the antinociceptive and antiinflammatory actions reported here for the first time for M. indica bark aqueous extract. Copyright 2001 John Wiley & Sons, Ltd.

The Eschericia coli Growth Inhibition Activity of Some Fermented Medicinal Plant Leaf Extract from the Karo Highland, North Sumatra

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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.

Apple juice inhibits human low density lipoprotein oxidation.

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Pearson, D A; Tan, C H; German, J B; Davis, P A; Gershwin, M E

1999-01-01

Dietary phenolic compounds, ubiquitous in vegetables and fruits and their juices possess antioxidant activity that may have beneficial effects on human health. The phenolic composition of six commercial apple juices, and of the peel (RP), flesh (RF) and whole fresh Red Delicious apples (RW), was determined by high performance liquid chromatography (HPLC), and total phenols were determined by the Folin-Ciocalteau method. HPLC analysis identified and quantified several classes of phenolic compounds: cinnamates, anthocyanins, flavan-3-ols and flavonols. Phloridzin and hydroxy methyl furfural were also identified. The profile of phenolic compounds varied among the juices. The range of concentrations as a percentage of total phenolic concentration was: hydroxy methyl furfural, 4-30%; phloridzin, 22-36%; cinnamates, 25-36%; anthocyanins, n.d.; flavan-3-ols, 8-27%; flavonols, 2-10%. The phenolic profile of the Red Delicious apple extracts differed from those of the juices. The range of concentrations of phenolic classes in fresh apple extracts was: hydroxy methyl furfural, n.d.; phloridzin, 11-17%; cinnamates, 3-27%; anthocyanins, n.d.-42%; flavan-3-ols, 31-54%; flavonols, 1-10%. The ability of compounds in apple juices and extracts from fresh apple to protect LDL was assessed using an in vitro copper catalyzed human LDL oxidation system. The extent of LDL oxidation was determined as hexanal production using static headspace gas chromatography. The apple juices and extracts, tested at 5 microM gallic acid equivalents (GAE), all inhibited LDL oxidation. The inhibition by the juices ranged from 9 to 34%, and inhibition by RF, RW and RP was 21, 34 and 38%, respectively. Regression analyses revealed no significant correlation between antioxidant activity and either total phenolic concentration or any specific class of phenolics. Although the specific components in the apple juices and extracts that contributed to antioxidant activity have yet to be identified, this study

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

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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.

Hexane neem leaf extract more potent than ethanol extract against Aspergillus flavus

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Jenny Hidayat

2015-12-01

Full Text Available BACKGROUND Aspergillus flavus is one of the causes of aspergillosis, with a high virulence and resistance to standard antifungals, resulting in a high mortality rate. Medicinal plants are increasingly used as they are relatively safer with minimal side effects. Previously we found that the ethanol extract of neem (Azadirachta indica A Juss leaves inhibits A. flavus growth in vitro. However, most chemical compounds with antifungal effect are nonpolar. The purpose of this research was to compare the antifungal effect of neem leaves extracted in a nonpolar solvent to that of leaves extracted in a polar solvent. METHODS An in vitro experimental research was conducted between October 2013 and January 2014. Neem leaves were extracted in ethanol or hexane at various concentrations. A macrodilution test with 48-hour incubation time was done in triplicate on 8 groups of samples. These comprised the neem leaf ethanol extract (NLEE at 0.5, 1.0, and 2.0 g/dL, neem leaf hexane extract (NLHE at 0.5, 1.0, and 2.0 g/dL, positive control, and negative control groups. Fungal growth was detected on Sabouroud dextrose agar. Statistical analysis used Chi square and Fisher’s exact test. RESULTS NLHE had a higher, but statistically non-significant, inhibitory effect on A. flavus than NLEE (p=0.996. At higher concentrations, the antifungal effect of NLHE is better than that of NLEE. CONCLUSION There is no significant difference in in-vitro inhibitory effectivity on A. flavus of neem leaves between extracts in polar and nonpolar solvents.

Cinnamic acid amides from Tribulus terrestris displaying uncompetitive α-glucosidase inhibition.

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Song, Yeong Hun; Kim, Dae Wook; Curtis-Long, Marcus J; Park, Chanin; Son, Minky; Kim, Jeong Yoon; Yuk, Heung Joo; Lee, Keun Woo; Park, Ki Hun

2016-05-23

The α-glucosidase inhibitory potential of Tribulus terrestris extracts has been reported but as yet the active ingredients are unknown. This study attempted to isolate the responsible metabolites and elucidate their inhibition mechanism of α-glucosidase. By fractionating T. terristris extracts, three cinnamic acid amide derivatives (1-3) were ascertained to be active components against α-glucosidase. The lead structure, N-trans-coumaroyltyramine 1, showed significant inhibition of α-glucosidase (IC50 = 0.42 μM). Moreover, all active compounds displayed uncompetitive inhibition mechanisms that have rarely been reported for α-glucosidase inhibitors. This kinetic behavior was fully demonstrated by showing a decrease of both Km and Vmax, and Kik/Kiv ratio ranging between 1.029 and 1.053. We progressed to study how chemical modifications to the lead structure 1 may impact inhibition. An α, β-unsaturation carbonyl group and hydroxyl group in A-ring of cinnamic acid amide emerged to be critical functionalities for α-glucosidase inhibition. The molecular modeling study revealed that the inhibitory activities are tightly related to π-π interaction as well as hydrogen bond interaction between enzyme and inhibitors. Copyright © 2016 Elsevier Masson SAS. All rights reserved.

In Vitro Studies on the Antioxidant Property and Inhibition of α-Amylase, α-Glucosidase, and Angiotensin I-Converting Enzyme by Polyphenol-Rich Extracts from Cocoa (Theobroma cacao) Bean.

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Oboh, Ganiyu; Ademosun, Ayokunle O; Ademiluyi, Adedayo O; Omojokun, Olasunkanmi S; Nwanna, Esther E; Longe, Kuburat O

2014-01-01

Background. This study sought to investigate the antidiabetic and antihypertensive mechanisms of cocoa (Theobroma cacao) bean through inhibition of α-amylase, α-glucosidase, angiotensin-1 converting enzyme, and oxidative stress. Methodology. The total phenol and flavonoid contents of the water extractable phytochemicals from the powdered cocoa bean were determined and the effects of the extract on α-amylase, α-glucosidase, and angiotensin-1 converting enzyme activities were investigated in vitro. Furthermore, the radicals [1,1-diphenyl-2 picrylhydrazyl (DPPH), 2,2..-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS), hydroxyl (OH), and nitric oxide (NO)] scavenging ability and ferric reducing antioxidant property of the extract were assessed. Results. The results revealed that the extract inhibited α-amylase (1.81 ± 0.22 mg/mL), α-glucosidase (1.84 ± 0.17 mg/mL), and angiotensin-1 converting enzyme (0.674 ± 0.06 mg/mL [lungs], 1.006 ± 0.08 mg/mL [heart]) activities in a dose-dependent manner and also showed dose-dependent radicals [DPPH (16.94 ± 1.34 mg/mL), NO (6.98 ± 0.886 mg/mL), OH (3.72 ± 0.26 mg/mL), and ABTS (15.7 ± 1.06 mmol/TEAC·g] scavenging ability. Conclusion. The inhibition of α-amylase, α-glucosidase, and angiotensin-1 converting enzyme activities by the cocoa bean extract could be part of the possible mechanism by which the extract could manage and/or prevent type-2 diabetes and hypertension.

In Vitro Studies on the Antioxidant Property and Inhibition of α-Amylase, α-Glucosidase, and Angiotensin I-Converting Enzyme by Polyphenol-Rich Extracts from Cocoa (Theobroma cacao Bean

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Ganiyu Oboh

2014-01-01

Full Text Available Background. This study sought to investigate the antidiabetic and antihypertensive mechanisms of cocoa (Theobroma cacao bean through inhibition of α-amylase, α-glucosidase, angiotensin-1 converting enzyme, and oxidative stress. Methodology. The total phenol and flavonoid contents of the water extractable phytochemicals from the powdered cocoa bean were determined and the effects of the extract on α-amylase, α-glucosidase, and angiotensin-1 converting enzyme activities were investigated in vitro. Furthermore, the radicals [1,1-diphenyl-2 picrylhydrazyl (DPPH, 2,2..-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid (ABTS, hydroxyl (OH, and nitric oxide (NO] scavenging ability and ferric reducing antioxidant property of the extract were assessed. Results. The results revealed that the extract inhibited α-amylase (1.81 ± 0.22 mg/mL, α-glucosidase (1.84 ± 0.17 mg/mL, and angiotensin-1 converting enzyme (0.674 ± 0.06 mg/mL [lungs], 1.006 ± 0.08 mg/mL [heart] activities in a dose-dependent manner and also showed dose-dependent radicals [DPPH (16.94 ± 1.34 mg/mL, NO (6.98 ± 0.886 mg/mL, OH (3.72 ± 0.26 mg/mL, and ABTS (15.7 ± 1.06 mmol/TEAC·g] scavenging ability. Conclusion. The inhibition of α-amylase, α-glucosidase, and angiotensin-1 converting enzyme activities by the cocoa bean extract could be part of the possible mechanism by which the extract could manage and/or prevent type-2 diabetes and hypertension.

In Vitro Studies on the Antioxidant Property and Inhibition of α-Amylase, α-Glucosidase, and Angiotensin I-Converting Enzyme by Polyphenol-Rich Extracts from Cocoa (Theobroma cacao) Bean

Science.gov (United States)

Ademosun, Ayokunle O.; Ademiluyi, Adedayo O.; Omojokun, Olasunkanmi S.; Nwanna, Esther E.; Longe, Kuburat O.

2014-01-01

Background. This study sought to investigate the antidiabetic and antihypertensive mechanisms of cocoa (Theobroma cacao) bean through inhibition of α-amylase, α-glucosidase, angiotensin-1 converting enzyme, and oxidative stress. Methodology. The total phenol and flavonoid contents of the water extractable phytochemicals from the powdered cocoa bean were determined and the effects of the extract on α-amylase, α-glucosidase, and angiotensin-1 converting enzyme activities were investigated in vitro. Furthermore, the radicals [1,1-diphenyl-2 picrylhydrazyl (DPPH), 2,2..-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS), hydroxyl (OH), and nitric oxide (NO)] scavenging ability and ferric reducing antioxidant property of the extract were assessed. Results. The results revealed that the extract inhibited α-amylase (1.81 ± 0.22 mg/mL), α-glucosidase (1.84 ± 0.17 mg/mL), and angiotensin-1 converting enzyme (0.674 ± 0.06 mg/mL [lungs], 1.006 ± 0.08 mg/mL [heart]) activities in a dose-dependent manner and also showed dose-dependent radicals [DPPH (16.94 ± 1.34 mg/mL), NO (6.98 ± 0.886 mg/mL), OH (3.72 ± 0.26 mg/mL), and ABTS (15.7 ± 1.06 mmol/TEAC·g] scavenging ability. Conclusion. The inhibition of α-amylase, α-glucosidase, and angiotensin-1 converting enzyme activities by the cocoa bean extract could be part of the possible mechanism by which the extract could manage and/or prevent type-2 diabetes and hypertension. PMID:25295218

Antiinflammatory Activity of Gynura bicolor (紅鳳菜 Hóng Fèng Cài Ether Extract Through Inhibits Nuclear Factor Kappa B Activation