期刊
JOURNAL OF SEPARATION SCIENCE
卷 37, 期 3, 页码 237-243出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/jssc.201300898
关键词
Derivatization; Gentiopicroside; Iridoid compounds; Metabolism
资金
- National Natural Science Foundation of China [81102896, 21272023]
- Overseas People Fund of Ministry of Education [1155h018]
- Heilongjiang Province, China
- Fundamental Research Funds for the Central Universities
The metabolism of gentiopicroside (GPS) in vivo was studied for the first time by LC-MS following picolinoyl derivatization. Incubation of erythrocentaurin, one of the main in vitro metabolites of GPS by intestinal bacteria, with liver microsome indicated that GPS might be metabolized to a final metabolite 3,4-dihydro-5-(hydroxymethyl) isochroman-1-one (HMIO) in vivo. After hydrolysis with sulfatase, HMIO was successfully detected in rat plasma after oral administration of GPS by LC-MS following picolinoyl derivatization. 4-Methoxyphenyl methanol was used as an internal standard to quantify HMIO in rat plasma. A metabolic pathway of GPS in rats is proposed. The monoterpene compound GPS was found to be metabolized to dihydroisocoumarin, which may be responsible for the pharmacological effect of GPS.
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