Food Science & Nutrition · 2019 · 75 citations · 52 references
PharmacyMedicinal ChemistryPharmacologyDrug DiscoveryHepatotoxicologyLead OptimizationHit-to-lead OptimizationLead Compound DesignLead DiscoveryNatural Product Drug DiscoveryAnimal Model PharmacologyCarbon Tetrachloride ToxicityExtractLead Compound DiscoveryLead Compound IdentificationLead Compound ScreeningLead Discovery From Natural ProductsToxicity Testing Of Plants
Abstract This research describes an investigation of the antipyretic and hepatoprotective properties of both a crude organic extract and various subfractions of the ethnomedicinal plant Tinospora crispa , using appropriate animal models. In an attempt to identify potential lead hepatoprotective compounds, in silico experiments were utilized. Antipyretic activity was assessed via the Brewer's yeast‐induced pyrexia method, while hepatoprotective effects were evaluated in a carbon tetrachloride (CCl 4 )‐induced animal model. A computer‐aided prediction of activity spectra for substances (PASS) model was applied to a selection of documented phytoconstituents, with the aim of identifying those compounds with most promising hepatoprotective effects. Results were analyzed using Molinspiration software. Our results showed that both the methanol extract (METC) and various subfractions (pet ether, PEFTC; n ‐hexane, NHFTC; and chloroform, CFTC) significantly ( p < .05) reduced pyrexia in a dose‐dependent manner. In CCl 4 ‐induced hepatotoxicity studies, METC ameliorated elevated hepatic markers including serum alanine amino transferase (ALT), aspartate amino transferase (AST), alkaline phosphatase (ALP), and total bilirubin. Malondialdehyde (MDA) levels were significantly reduced, while superoxide dismutase (SOD) levels were significantly increased. Among a selection of metabolites of T. crispa , genkwanin was found to be the most potent hepatoprotective constituent using PASS predictive models. These results demonstrate that both the methanolic extract of T. crispa and those fractions containing genkwanin may offer promise in reducing pyrexia and as a source of potential hepatoprotective agents.
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