title: In vitro metabolism study of saikosaponin d and its derivatives in rat liver microsomes.
abstract: 1. Saikosaponins, one of the representative bioactive ingredients in Radix Bupleuri, possess hepatoprotective, anti-inflammatory, antiviral, antitumor, and other pharmacological activities. Up to now, few studies focused on the further metabolism of saikosaponins and their secondary metabolites absorbed into the circulatory system. 2. To understand the in vivo efficacy of saikosaponin d, the in vitro metabolism of saikosaponin d, and its two derivatives formed in the gastrointestinal tract, prosaikogenin G and saikogenin G was investigated in rat liver microsomes, respectively. 3. Fifteen metabolites were detected using high-performance liquid chromatography hybrid ion trap and time-of-flight mass spectrometry and triple-quadrupole mass spectrometry, and the predominant metabolic reactions were hydroxylation, carboxylation and combinations of these steps on the aglycone moiety. 4. The metabolic pathways of saikosaponin d, prosaikogenin G, and saikogenin G were proposed in vitro and the results contribute to the understanding of saikosaponins in vivo metabolism.
authors.affiliation: a Key Laboratory of Drug Quality Control & Pharmacovigilance (China Pharmaceutical University), Ministry of Education , Nanjing , China.|b State Key Laboratory of Natural Medicine, China Pharmaceutical University , Nanjing , China , and.
authors.forename: Pei
authors.initials: P
authors.lastname: Yu
authors.affiliation: c Guangxi Key Laboratory of Traditional Chinese Medicine Quality Standards (Guangxi Institute of Traditional Medical and Pharmaceutical Sciences) , Nanning , China.
authors.forename: Hongcong
authors.initials: H
authors.lastname: Qiu
authors.affiliation: a Key Laboratory of Drug Quality Control & Pharmacovigilance (China Pharmaceutical University), Ministry of Education , Nanjing , China.|b State Key Laboratory of Natural Medicine, China Pharmaceutical University , Nanjing , China , and.
authors.forename: Min
authors.initials: M
authors.lastname: Wang
authors.affiliation: a Key Laboratory of Drug Quality Control & Pharmacovigilance (China Pharmaceutical University), Ministry of Education , Nanjing , China.|b State Key Laboratory of Natural Medicine, China Pharmaceutical University , Nanjing , China , and.
authors.forename: Yuan
authors.initials: Y
authors.lastname: Tian
authors.affiliation: a Key Laboratory of Drug Quality Control & Pharmacovigilance (China Pharmaceutical University), Ministry of Education , Nanjing , China.|b State Key Laboratory of Natural Medicine, China Pharmaceutical University , Nanjing , China , and.
authors.forename: Zunjian
authors.initials: Z
authors.lastname: Zhang
authors.affiliation: a Key Laboratory of Drug Quality Control & Pharmacovigilance (China Pharmaceutical University), Ministry of Education , Nanjing , China.|b State Key Laboratory of Natural Medicine, China Pharmaceutical University , Nanjing , China , and.
authors.forename: Rui
authors.initials: R
authors.lastname: Song
mesh_terms: D000818:Animals; D002851:Chromatography, High Pressure Liquid; D004365:Drugs, Chinese Herbal / Q000378:metabolism; D006900:Hydroxylation; D008862:Microsomes, Liver / Q000378:metabolism*; D009828:Oleanolic Acid / Q000031:analogs & derivatives* / Q000378:metabolism; D051381:Rats; D012503:Saponins / Q000378:metabolism*
chemical_list: D004365:Drugs, Chinese Herbal; D012503:Saponins; D009828:Oleanolic Acid; C025759:saikosaponin D
keywords: In vitro metabolism; prosaikogenin G; rat liver microsomes; saikogenin G; saikosaponin d