Antitumor activity of two gelsemine metabolites in rat liver microsomes.
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.
Zhao
Qing-Chun
QC
Shenyang Northern Hospital, Shenyang Pharmaceutical University, Shenyang, China. zhaoqc53@yahoo.com.cn
Hua
Wei
W
Zhang
Lin
L
Guo
Tao
T
Zhao
Ming-Hong
MH
Yan
Ming
M
Shi
Guo-Bing
GB
Wu
Li-Jun
LJ
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
C552582:21-oxogelsemine; C552583:4-N-demethylgelsemine; D000470:Alkaloids; D000972:Antineoplastic Agents, Phytogenic; C063230:gelsemine