title: Antitumor activity of two gelsemine metabolites in rat liver microsomes.
abstract: Gelsemine is one of the major alkaloids from Gelsemium elegans Benth., which has been used as an antitumor remedy in clinic. In this paper, metabolism of gelsemine has been investigated in vitro in phenobarbital-treated rat liver microsomes. The metabolites of gelsemine were separated and evaluated using the flash silica gel column, preparative HPLC, using NMR and MS methods. According to the spectral data, two metabolites, M1 and M2, were identified as 4-N-demethylgelsemine and 21-oxogelsemine, respectively. By the MTT method in vitro, the antitumor activities between gelsemine and its metabolites were compared in the HepG2 and HeLa cell lines. Moreover, the main metabolic pathway was further proposed.
authors.affiliation: Shenyang Northern Hospital, Shenyang Pharmaceutical University, Shenyang, China. zhaoqc53@yahoo.com.cn
authors.forename: Qing-Chun
authors.initials: QC
authors.lastname: Zhao
authors.forename: Wei
authors.initials: W
authors.lastname: Hua
authors.forename: Lin
authors.initials: L
authors.lastname: Zhang
authors.forename: Tao
authors.initials: T
authors.lastname: Guo
authors.forename: Ming-Hong
authors.initials: MH
authors.lastname: Zhao
authors.forename: Ming
authors.initials: M
authors.lastname: Yan
authors.forename: Guo-Bing
authors.initials: GB
authors.lastname: Shi
authors.forename: Li-Jun
authors.initials: LJ
authors.lastname: Wu
mesh_terms: D000470:Alkaloids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D002851:Chromatography, High Pressure Liquid; D004354:Drug Screening Assays, Antitumor; D031450:Gelsemium / Q000737:chemistry; D006367:HeLa Cells; D056945:Hep G2 Cells; D006801:Humans; D008862:Microsomes, Liver / Q000187:drug effects / Q000378:metabolism*; D015394:Molecular Structure; D019906:Nuclear Magnetic Resonance, Biomolecular; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: C552582:21-oxogelsemine; C552583:4-N-demethylgelsemine; D000470:Alkaloids; D000972:Antineoplastic Agents, Phytogenic; C063230:gelsemine