Human Gastrointestinal Metabolism of the Anti-rheumatic Fraction of Dianbaizhu (Gaultheria leucocarpa var. yunnanensis) in Vitro: Elucidation of the Metabolic Analysis in Gastric Juice, Intestinal Juice and Human Intestinal Bacteria by UPLC-LTQ-Orbitrap-MSn and HPLC-DAD

Publication date: Available online 26 July 2019Source: Journal of Pharmaceutical and Biomedical AnalysisAuthor(s): Xiuhuan Wang, Xiao Li, Rufeng Wang, Le Wang, Shusheng Fan, Xiaoping Wang, Xiao Xu, Xin Yan, Ting He, Xueyang Ren, Gaimei SheAbstractThe anti-rheumatic fraction (ARF), is responsible for the anti-inflammatory and analgesic effects of Dianbaizhu derived from the aerial part of Gaultheria leucocarpa var. yunnanensis (Ericaceae). The gastrointestinal metabolism of ARF was investigated in vitro through simulating a series of models–gastric juice, intestinal juice, and human intestinal bacteria, analyzed by HPLC-DAD and UPLC-LTQ-Orbitrap-MSn. ARF includes three categories: methyl salicylate glycosides, organic acids and the others. The primordial and metabolic components of ARF bio-transformed by simulated gastric fluid (36 and 13), intestinal fluid (29 and 7) and two human fecal bacteria (34 and 34, 40 and 25) were characterized, respectively. The methyl salicylate glycosides, MSTG-B, MSTG-A and gaultherin, with terminal-xylosyl-moiety in sugar chain were always being found in the whole gastrointestinal incubation processing. The metabolites were formed through hydrolysis of ester and glucosidic bond, as well as methylation, hydroxylation, acetylation, sulfation, reduction, decarboxylation, deglycosylation and glucuronidation. The metabolic conversion effect of the four index compounds, MSTG-B, MSTG-A, gaultherin, and chlorogenic acid by human intestinal bacteria ex...
Source: Journal of Pharmaceutical and Biomedical Analysis - Category: Drugs & Pharmacology Source Type: research