Liquid chromatography-electrospray ionization mass spectrometry for metabolism and pharmacokinetic studies of ginsenoside Rg3
Liquid chromatography-electrospray ionization mass spectrometry for metabolism and pharmacokinetic studies of ginsenoside Rg3
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DOI：
10.1016/s0003-2670(03)00719-0
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发表时间：
2003-09-15
影响因子：
6.2
通讯作者：
Jiang, ZH
中科院分区：
文献类型：
--
作者：
Cai, ZW;Qian, TX;Jiang, ZH
采用四极杆-飞行时间检测器液相色谱-电喷雾质谱联用技术测定大鼠血浆中的人参皂苷Rg 3及其主要代谢产物。生物样品经甲醇沉淀蛋白质后直接进样至反相高效液相色谱柱中，采用溶剂梯度程序进行分离。大鼠静脉注射人参皂苷Rg_3后，Rg_3的半衰期为14 min。代谢物鉴定和MS-MS和高分辨率MS分析的确认表明，半衰期短可能是由于在胃肠道条件下的代谢清除率高。Rg 3的水解产物，如Rh 2 Rh 3和原人参二醇被确定为与0.1 M HCl孵育的主要代谢产物，并检测到原人参二醇的水合产物作为与人工胃液的代谢产物，而在与大鼠肝S9组分孵育的样品中确定了单氧代谢产物。(C)2003 Elsevier B. V.保留所有权利。
A sensitive and specific liquid chromatography (LC)-electrospray ionization (ESI) mass spectrometry (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 vitro metabolism studies. The biological samples were prepared by protein precipitation with methanol and the sample extracts were directly injected into a reversed-phase HPLC column with solvent gradient program. Pharmacokinetic study of Rg3 on rat gave a half-life of 14 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 M HCl, and a hydrated product of protopanaxadiol was detected as the metabolite with artificial gastric juice, while a monooxygenated metabolite was identified in the incubated samples with rat liver S9 fraction. (C) 2003 Elsevier B.V. All rights reserved.