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Antioxidant and Cholinesterase Inhibitory Activities of Ethyl Acetate Extract of Terminalia chebula: Cell-free In vitro and In silico Studies.

ABSTRACT: Background:Alzheimer's disease (AD) is a progressive neurodegenerative disorder clinically characterized by memory loss and impaired cognitive function. Cholinergic enzyme deficiency and oxidative stress are the two major factors implicated in the pathogenesis of AD. The symptomatic treatment, as of now, is the use of cholinesterase inhibitors toward cholinergic "downturn." Therefore, there is a search for compounds that will be useful in focused therapies. There has been suggestion that Terminalia chebula fruit would be a potential source. Objective:To assess the anticholinesterase and antioxidant activities of T. chebula fruit which is widely practiced in the Ayurvedic medicines for memory enhancement. Materials and Methods:Ethyl acetate extract of T. chebula fruit (TCEA) was subjected to phytochemical investigation of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities and cell-free antioxidant activity. TCEA was further subjected to gas chromatography-mass spectrum (GC-MS) analysis. The bioactive compounds were analyzed for molecular docking with AChE and BuChE proteins. Results:TCEA exhibited potent AChE and BuChE inhibitory activities comparable to the standard drug donepezil. In vitro cell-free antioxidant assays demonstrated that TCEA possesses excellent free radical scavenging activity, reducing power, and potent metal-chelating activity. Total polyphenolic content of TCEA was 596.75 ± 0.35 µg gallic acid equivalents/mg of extract, which correlates with the antioxidant activity of TCEA. Molecular docking of compounds expounded in GC-MS analysis for AChE and BuChE enzyme activities revealed that methyl N-(N-benzyloxycarbonyl-beta-l-aspartyl)-beta-d-glucosaminide as the most potent compound with good predicted activities. Conclusion:Overall, the results revealed that the bioactive molecule methyl N-(N-benzyloxycarbonyl-beta-l-aspartyl)-beta-d-glucosaminide present in TCEA is a potential depressant for the treatment of AD and related neurodegenerative disorders. SUMMARY:The present study was carried out to assess the neuroprotective effect of Terminalia chebula fruit and its phytoconstituent. Phytochemical analysis of fruit ethyl acetate extract of T. chebula (TCEA) showed the presence of alkaloid, cardiac glycoside, and tannin. TCEA showed potent acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities when compared to standard drug donepezil. Results of in vitro antioxidant assays revealed excellent free radical scavenging activity, reducing power, and potent metal-chelating activity. Gas chromatography-mass spectrum analysis illustrated the presence of 22 active compounds, among which methyl N-(N-benzyloxycarbonyl-beta-l-aspartyl)-beta-d-glucosaminide exhibited potent AChE and BuChE inhibition analyzed through in silico studies. Abbreviations used: AD: Alzheimer's disease; TCEA: Ethyl acetate extract of Terminalia chebula; GC-MS: Gas chromatography-mass spectrum; ROS: Reactive oxygen species; RNS: Reactive nitrogen species; AChE: Acetylcholinesterase; BuChE: Butyrylcholinesterase; NFT: Neurofibrillary tangles; A?: ?-amyloid; NSAIDS: Nonsteroidal anti-inflammatory drugs; FDA: Food and Drug Administration; RT: Room temperature; HCl: Hydrochloric acid; ATCI: Acetylthiocholine iodide; BTCI: Butyrylthiocholine iodide; BHT: Butylated hydroxytoluene; DPPH: 2,2-diphenyl-1-picrylhydrazyl; TCA: Trichloroacetic acid; GAE: Gallic acid equivalent; NICT: National Institute of Information and Communications Technology; 3D: Three-dimensional; PDB: Protein data bank; OPLS: Optimized potentials for liquid simulations; XP: Extra precision; SD: Standard deviation; ANOVA: Analysis of variance; EDTA: Ethylenediaminetetraacetic acid.

SUBMITTER: Rajmohamed MA

PROVIDER: S-EPMC5669079 | biostudies-literature | 2017 Oct

REPOSITORIES: biostudies-literature

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Antioxidant and Cholinesterase Inhibitory Activities of Ethyl Acetate Extract of <i>Terminalia chebula</i>: Cell-free <i>In vitro</i> and <i>In silico</i> Studies.

Rajmohamed Mohamed Asik MA Natarajan Suganthy S Palanisamy Premkumar P Abdulkader Akbarsha Mohammad AM Govindaraju Archunan A

Pharmacognosy magazine 20171011 Suppl 3

<h4>Background</h4>Alzheimer's disease (AD) is a progressive neurodegenerative disorder clinically characterized by memory loss and impaired cognitive function. Cholinergic enzyme deficiency and oxidative stress are the two major factors implicated in the pathogenesis of AD. The symptomatic treatment, as of now, is the use of cholinesterase inhibitors toward cholinergic "downturn." Therefore, there is a search for compounds that will be useful in focused therapies. There has been suggestion that ...[more]

PMID: 29142396

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Project description:Terminalia chebula extract (TCE) has many physiological functions and is potentially helpful in maintaining poultry health, but its specific effect on the growth of broilers is not yet known. This research investigated the effects of dietary Terminalia chebula extract (TCE) supplementation on growth performance, immune function, antioxidant capacity, and intestinal health in yellow-feathered broilers. A total of 288 one-day-old yellow-feathered broilers were divided into four treatment groups (72 broilers/group), each with six replicates of 12 broilers. The broilers were given a basal diet of corn-soybean meal supplemented with 0 (control), 200, 400, and 600 mg/kg TCE for 56 d. The results demonstrated that, compared with the basal diet, the addition of TCE significantly increased (linear and quadratic, p < 0.05) the final body weight and overall weight gain and performance and decreased (linear and quadratic, p < 0.05) the feed-to-gain ratio in the overall period. Dietary TCE increased (linear, p < 0.05) the levels of IgM, IL-4, and IL-10 and decreased (linear and quadratic, p < 0.05) the level of IL-6 in the serum. Dietary TCE increased (linear and quadratic, p < 0.05) the levels of IL-2 and IL-4, decreased (linear and quadratic, p < 0.05) the level of IL-1β, and decreased (linear, p < 0.05) the level of IL-6 in the liver. Dietary TCE increased (linear and quadratic, p < 0.05) the level of IgM and IL-10, increased (linear, p < 0.05) the level of IgG, and decreased (linear and quadratic, p < 0.05) the levels of IL-1β and IL-6 in the spleen. Supplementation with TCE linearly and quadratically increased (p < 0.05) the catalase, superoxide dismutase, glutathione peroxidase, and total antioxidant capacity activities while decreasing (p < 0.05) the malonic dialdehyde concentrations in the serum, liver, and spleen. TCE-containing diets for broilers resulted in a higher (linear and quadratic, p < 0.05) villus height, a higher (linear and quadratic, p < 0.05) ratio of villus height to crypt depth, and a lower (linear and quadratic, p < 0.05) crypt depth compared with the basal diet. TCE significantly increased (linear, p < 0.05) the acetic and butyric acid concentrations and decreased (quadratic, p < 0.05) the isovaleric acid concentration. Bacteroidaceae and Bacteroides, which regulate the richness and diversity of microorganisms, were more abundant and contained when TCE was added to the diet. In conclusion, these findings demonstrate that supplementing broilers with TCE could boost their immune function, antioxidant capacity, and gut health, improving their growth performance; they could also provide a reference for future research on TCE.

Project description:A potentially novel actinobacterium isolated from forest soil, Streptomyces sp. KSF103 was evaluated for its insecticidal effect against several mosquito species namely Aedes aegypti, Aedes albopictus, Anopheles cracens and Culex quinquefasciatus. Mosquito larvae and adults were exposed to various concentrations of the ethyl acetate (EA) extract for 24 h. Considerable mortality was evident after the EA extract treatment for all four important vector mosquitoes. Larvicidal activity of the EA extract resulted in LC50 at 0.045 mg/mL and LC90 at 0.080 mg/mL for Ae. aegypti; LC50 at 0.060 mg/mL and LC90 at 0.247 mg/mL for Ae. albopictus; LC50 at 2.141 mg/mL and LC90 at 6.345 mg/mL for An. cracens; and LC50 at 0.272 mg/mL and LC90 at 0.980 mg/mL for Cx. quinquefasciatus. In adulticidal tests, the EA extract was the most toxic to Ae. albopictus adults (LD50 = 2.445 mg/mL; LD90 = 20.004 mg/mL), followed by An. cracens (LD50 = 5.121 mg/mL; LD90 = 147.854 mg/mL) and then Ae. aegypti (LD50 = 28.873 mg/mL; LD90 = 274.823 mg/mL). Additionally, the EA extract exhibited ovicidal activity against Ae. aegypti (LC50 = 0.715 mg/mL; LC90 = 6.956 mg/mL), Ae. albopictus (LC50 = 0.715 mg/mL; LC90 = 6.956 mg/mL), and An. cracens (LC50 = 0.715 mg/mL; LC90 = 6.956 mg/mL), evaluated up to 168 h post-treatment. It displayed no toxicity on the freshwater microalga Chlorella sp. Beijerinck UMACC 313, marine microalga Chlorella sp. Beijerinck UMACC 258 and the ant Odontoponera denticulata. In conclusion, the EA extract showed promising larvicidal, adulticidal and ovicidal activity against Ae. aegypti, Ae. albopictus, An. cracens, and Cx. quinquefasciatus (larvae only). The results suggest that the EA extract of Streptomyces sp. KSF103 has the potential to be used as an environmental-friendly approach in mosquito control. The current study would serve as an initial step toward complementing microbe-based bioinsecticides for synthetic insecticides against medically important mosquitoes.

Dataset Information

Antioxidant and Cholinesterase Inhibitory Activities of Ethyl Acetate Extract of Terminalia chebula: Cell-free In vitro and In silico Studies.

Publications

Antioxidant and Cholinesterase Inhibitory Activities of Ethyl Acetate Extract of <i>Terminalia chebula</i>: Cell-free <i>In vitro</i> and <i>In silico</i> Studies.

Similar Datasets

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