New analytical method for the study of the metabolism of gentiopicroside in rats after oral administration by LC–TOF‐MS following picolinoyl derivatization |
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| Authors: | Zhigang Wang Shanshan Wang Yujia Sun Huiyu Wang Guang Chen Xijun Wang Masao Hattori Hailong Zhang |
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| Institution: | 1. National TCM Key Lab of Serum Pharmacochemistry, Department of Pharmaceutical Analysis, Heilongjiang University of Chinese Medicine, Harbin, China;2. Institute of Natural Medicine, University of Toyama, Toyama, Japan;3. College of Life Science and Technology, Beijing University of Chemical Technology, Beijing, China;4. School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Shaanxi, China |
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| Abstract: | 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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| Keywords: | Derivatization Gentiopicroside Iridoid compounds Metabolism |
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