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Castanopsis tribuloides belongs to the oak species (Fagaceae) and it is commonly distributed in evergreen forests of Bangladesh, India, Myanmar, Nepal, China, and Thailand. Our present study aimed at uncovering the antipyretic potential of methanol extract of C. tribuloides bark (CTB) in the mice models. Baker's yeast pyrexia model was employed to determine the antipyretic potentials of the extract. Besides, molecular docking and dynamics simulation of CTB phenolic compounds were explored to validate the experimental results and gain insight into the possible antipyretic mechanism of action that can lead to the design and discovery of novel drugs against mPGES-1. The results revealed that CTB (400 mg/kg) significantly inhibited (P < 0.001) the elevated body temperature of mice since 0.5 h, which is more prominent than the standard. At dose 200 mg/kg, the bark extract also produced significant (P < 0.05) antipyretic activity since 2 h. HPLC-DAD analysis identified and quantified nine polyphenolic compounds from the extract, including rutin hydrate, (-) epicatechin, caffeic acid, catechin hydrate, catechol, trans-ferulic acid, p-coumaric acid, vanillic acid, and rosmarinic acid. Molecular docking study suggested probable competition of these phenolic compounds with glutathione, an essential cofactor for microsomal prostaglandin E synthase-1 (mPGES-1) activity. Additionally, RMSF, RMSD, Rg, and hydrogen bonds performed during MD simulations revealed that rutin hydrate (rich in CTB) bound to the mPGES-1 active site in a stable manner and thus inactivating mPGES-1. Therefore, it can be concluded that rutin hydrate reduces pyrexia in mice via downregulating PGE2 synthesis by inhibiting mPGES-1 activity., (Copyright © 2022 The Authors. Published by Elsevier Masson SAS.. All rights reserved.)

The aim of the current study was to analyze the polyphenols and determines the antioxidant, analgesic and diuretic properties of the methanolic extract of C.speciosus rhizome. DPPH and ferric reducing antioxidant power (FRAP) assays were used to determine the antioxidant activity. Acetic acid-induced writhing and formalin-induced licking experiments were used to assess the analgesic effect. The total phenolic, flavonoid and flavonol contents were found 51.73± 0.25 mg GAE/g dry weight, 3.41± 0.07mg QE/g dry weights and 44.19± 2.24 mg QE/g dry weight, respectively. The plant extract exhibited weak antioxidant activity in the DPPH and FRAP assays, with an IC50 value of 1699±62 µg/mL and an EC50 value of 125±2 µg/mL, respectively. The extract significantly reduced the number of writhes at both doses (200 and 400 mg/kg body weight) as compared to the control. The extract (400 mg/kg) also significantly reduced the percent inhibition of licking by 31.96 and 62.69% compared to the control in the early and late phase, respectively. Compared to the standard drug furosemide, the plant extract also showed a weak diuretic effect. The docking study supported the analgesic activity of rhizome extract. The potent analgesic activity of the plant extract justifies the traditional and medicinal aspects. [ABSTRACT FROM AUTHOR]

Objective: The purpose of the current study was to investigate the in vivo (analgesic, antidiarrheal, neurological, and cytotoxic) and in vitro (antioxidant, antimicrobial, thrombolytic and anthelmintic) activity of different fractions of methanolic extract of Momordica charantia. Materials and Methods: The antioxidant property was evaluated by DPPH radical scavenging assay, while antimicrobial activity was examined against three Gram (+) and one Gram (-) bacteria. Thrombolytic and anthelmintic activities were evaluated by using human blood serum and by recording paralysis and death time in earthworm, respectively. Cytotoxic activity was investigated in brine shrimp nauplii. Analgesic and antidiarrheal activities were evaluated in Swiss albino mice and neurological effect was evaluated by open field and Elevated plus-maze test (EPM). Results: All fractions (n-hexane, carbon tetrachloride and chloroform) possess significant (p<0.05) cytotoxic activity. In case of thrombolytic activity, the highest concentration of methanolic extract produced a remarkable percentage of clot lysis (46.12%). The concentration of 1000 μg/ml produced a significant antibacterial activity against Gram positive Staphylococcus aureus and Gram negative E. coli. Aqueous fraction at a dose of 400 mg/kg body weight, was found to show promising analgesic activity. In case of antidiarrheal and anthelmintic activity, plant extract showed dose-dependent activity. Methanolic extract and its fractions failed to produce any neurological effect in both methods. Conclusion: The overall results of the study tend to suggest that the methanolic extract and its fractions have promising pharmacological activities. [ABSTRACT FROM AUTHOR]