title: Identification of the metabolites of anti-inflammatory compound clematichinenoside AR in rat intestinal microflora.
abstract: Clematichinenoside AR (C-AR), a pentacyclic triterpenoid saponin with anti-inflammatory and anti-rheumatoid activities, is the main active component of the traditional Chinese medicine Clematidis Radix et Rhizoma. However, its poor oral absorption indicated that not only the parent compound C-AR itself, but also its metabolites could be responsible for the pharmacological effects in rats. The present study aimed to investigate the metabolism of C-AR in rat intestinal microflora, where C-AR was extensively metabolized. C-AR was incubated with the content of the large intestine. The culture solution was collected at different time points and analyzed for the metabolites of C-AR. Eight metabolites were identified by liquid chromatography/quadrupole time-of-flight mass spectrometry. M1, M2 and M5 were the major metabolites. In addition, it was proposed that deglycosylation was the only pathway contributing to the biotransformation of C-AR in rat intestinal microflora.
authors.affiliation: Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, 210009, China.
authors.forename: Feng
authors.initials: F
authors.lastname: Li
authors.forename: Dawei
authors.initials: D
authors.lastname: Wang
authors.forename: Ping
authors.initials: P
authors.lastname: Xu
authors.forename: Jie
authors.initials: J
authors.lastname: Wu
authors.forename: Li
authors.initials: L
authors.lastname: Liu
authors.forename: Xiaodong
authors.initials: X
authors.lastname: Liu
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000032:analysis / Q000737:chemistry* / Q000378:metabolism*; D001711:Biotransformation; D002853:Chromatography, Liquid; D005766:Gastrointestinal Contents / Q000382:microbiology*; D006031:Glycosylation; D008297:Male; D013058:Mass Spectrometry; D064307:Microbiota; D051381:Rats; D017207:Rats, Sprague-Dawley; D012503:Saponins / Q000032:analysis / Q000737:chemistry* / Q000378:metabolism*
chemical_list: D000893:Anti-Inflammatory Agents; D012503:Saponins; C581539:clematichinenoside
keywords: LC-Q/TOF MS; clematichinenoside AR; intestinal microflora; metabolite identification