【作者】 钱天秀； 蔡宗苇； 黄岳顺； 姜志宏；

【Author】 QIAN Tian-xiu~1, CAI Zong-wei~(1,*), HUANG Yue-shun~2, JIANG Zhi-hong~3(1. Department of Chemistry; Hong Kong Baptist University, Hong Kong, China;2. Department of Biology, Hong Kong Baptist University, Hong Kong, China;3. Schoold of Chinese Medicine, Hong Kong Baptist University, Hong Kong, China)

【机构】 香港浸会大学化学系； 香港浸会大学生物系； 香港浸会大学中医药学院；

【摘要】 <正>Rg3是从红参(Red Panaxginseng)中发现的一种微量人参皂甙。药理实验表明,它在小鼠体内具有抑制肿瘤转移的活性及在体外有抑制肿瘤细胞扩散的活性。对其体外代谢的研究目前只见一例用人体肠道菌群体外厌氧培养产生水解脱糖的代谢产物的报导,而对其体内的研究目前只见于人口服后在人体内的动力学报导,但其在动物体内的代谢尚不清楚,因此有必要研究其在动物体内的动力学及代谢详情。更多还原

【Abstract】 A sensitive and specific LC-ESI-MS method with quadrupole-time of flight detection was applied for the determination of ginsenoside Rg3 in rat plasma and its major metabolites in samples from in vivo pharmacokinetics and metabolism studies. The biological samples were prepared by protein precipitation with methanol and the sample extracts were directly injected into a reversedphase HPLC column with solvent gradient program. Pharmacokinetic study of Rg3 on rat gave a half-life of 18 min after the ginsenoside was intravenously dosed. Metabolite identification and confirmation from the MS/MS and high-resolution MS analyses indicated that the short half-life might be due to the high rate of metabolic clearance of the ginsenoside under gastrointestinal conditions.Hydrolysis products of Rg3 such as ginsenoside Rh2 and protopanaxadiol were identified as the major metabolites from the incubation with 0.1 mol/L HC1. The monooxygenated and deoxygenated products of protopanaxadiol were detected as the metabolites of Rg3 from rat feces after oral administration, as well as ginsenoside Rh2 and protopanaxadiol.更多还原