The results of this study strongly indicate the protective effect of S. xanthocarpum against liver injury which may be attributed to its hepatoprotective activity, and thereby scientifically support its traditional use.

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BackgroundThe current perspective for the search of 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase inhibitor has been shifted towards a natural agent also having antioxidant property. Thus, this study was intended to isolate and identify the bioactive compounds from methanolic extract of Ficus virens bark (FVBM) and to evaluate their antioxidant, HMG-CoA reductase inhibitory and hypolipidemic activity.MethodsBioactivity guided fractionation and isolation of bioactive compound from FVBM extract has been done to isolate and characterize the potent HMG-CoA reductase (HMGR) inhibitor with antioxidant activity by using repeated extensive column chromatography followed by spectroscopic methods, including Infrared (IR), 1H & 13C nuclear magnetic resonance (NMR) and Mass spectrum analysis. The in vitro HMGR inhibition and enzyme kinetic assay was determined using HMG-CoA as substrate. In addition, antioxidant activity of the new isolated compound, was measured using 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay and FRAP value. In-silico molecular informatics of HMGR enzyme type inhibition and pharmacokinetics data of the new compound was further evaluated through molecular docking and ADME-T studies. Further, in-vivo hypolipidemic property of FVBM extract and newly isolated compound was also analyzed in triton-WR 1339 induced rats.ResultsThereby, we report the discovery of n-Octadecanyl-O-α-D-glucopyranosyl(6′ → 1″)-O-α-D-glucopyranoside (F18) as a novel HMG-CoA reductase inhibitor with strong antioxidant property. This inhibitor exhibited not only higher free radical scavenging activity but also marked HMG-CoA reductase inhibitory activity with an IC50 value of 84 ± 2.8 ng/ml. This inhibitory activity concurred with kinetic study that showed inhibition constant (Ki) of 84 ng/ml via an uncompetitive mode of inhibition. The inhibition was also corroborated by molecular docking analysis and in silico pharmacokinetics data. The in vivo study revealed that administration of FVBM extract (at higher dose, 100 mg/rat) and the inhibitor (1 mg/rat) to Triton WR-1339-induced hyperlipidemic rats significantly ameliorated the altered levels of plasma lipids and lipoproteins including hepatic HMG-CoA reductase activity; this effect was comparable to the effect of standard drug atorvastatin.ConclusionsThe in vitro, in silico and in vivo results clearly demonstrated the antioxidant potential and therapeutic efficacy of the inhibitor as an alternate drug against hyperlipidemia.Electronic supplementary materialThe online version of this article (doi:10.1186/s12944-015-0013-6) contains supplementary material, which is available to authorized users.

We have evaluated the efficacy of ondansetron in the prevention of opioid-induced pruritus in a prospective, randomized, double-blind, placebo-controlled study. Using a 'human model' of opioid-induced pruritus, 80 ASA I-II patients about to undergo routine surgery were given either ondansetron 4 mg i.v. or 0.9% saline i.v. (40 in each group), 30 min before alfentanil 10 mg kg-1 i.v. During the following 5 min, patients were observed for signs of perinasal scratching and at 5 min were asked about symptoms of pruritus. The study was then terminated and anaesthesia was induced. There was a significant reduction in the incidence of scratching in patients receiving ondansetron compared with placebo (42.5% vs 70%, respectively, P = 0.013). The incidence of itching in the ondansetron group was less than that in the placebo group but this was not statistically significant (30% vs 42.5%, respectively, P = 0.245). We conclude that the 5-HT3 antagonist ondansetron may have a role in the management of opioid-induced pruritus.