Ultra-performance liquid chromatography and time-of-flight mass spectrometry analysis of ginsenoside metabolites in human plasma.
Ultra-performance liquid chromatography and time-of-flight mass spectrometry analysis of ginsenoside metabolites in human plasma.
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DOI：
10.1142/s0192415x11009470
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发表时间：
2011
期刊：
影响因子：
--
通讯作者：
Yuan CS
中科院分区：
文献类型：
--
作者：
Wang CZ;Kim KE;Du GJ;Qi LW;Wen XD;Li P;Bauer BA;Bissonnette MB;Musch MW;Chang EB;Yuan CS
西洋参是美国常用的草药。据报道，当人参口服时，其活性成分人参皂苷被肠道微生物群生物转化。以前对人参在人体内的药代动力学评价主要集中在其母体成分上。然而，代谢产物，尤其是肠道微生物群转化的代谢产物，尚未得到仔细研究。我们使用超高效液相色谱/飞行时间质谱（UPLC/TOF-MS）方法测定了15种皂苷和/或代谢物及其人体生物利用度。6名健康人受试者接受单次口服剂量的10 g西洋参根粉末，之后在0、2、4、7、9和12 h收集他们的血液样品用于测量血浆中的β-D-半乳糖/代谢物水平。在不同时间点检测人血浆样品中人参皂苷Rb 1、Rd、Rg 2和化合物K（C-K）。Rb 1浓度峰值为19.90 ± 5.43 ng/ml。C-K在7 ~ 12 h内均能检测到，12 h为7.32 ± 1.35 ng/ml。由于最后一个时间点为12 h，因此未观察到C-K峰水平。0 ~ 12 h的药时曲线下面积（AUC）分别为155.0 ± 19.5ng·h/ml和26.4 ± 6.4ng·h/ml。在人类受试者中观察到的Rb 1水平的逐渐降低和C-K水平的延迟增加支持了先前的报告，即肠道微生物群在Rb 1转化为C-K中发挥了关键作用。
American ginseng is a commonly used herbal medicine in the United States. When ginseng is taken orally, its active components, ginsenosides, are reportedly biotransformed by intestinal microbiota. Previous pharmacokinetic evaluations of ginseng in humans have focused on its parent constituents. However, the metabolites, especially those transformed by intestinal microbiota, have not been carefully studied. We used an ultra-performance liquid chromatography/time-of-flight mass spectrometry (UPLC/TOF-MS) method to determine 15 ginsenosides and/or metabolites and their bioavailability in humans. Six healthy human subjects received a single oral dose of 10 g of American ginseng root powder, after which samples of their blood were collected at 0, 2, 4, 7, 9 and 12 h for measurement of ginsenoside/metabolite levels in plasma. Ginsenosides Rb1, Rd, Rg2 and compound K (C-K) were detected in human plasma samples at different time points. The Rb1 concentration peak was 19.90 ± 5.43 ng/ml at 4 h. C-K was detected from 7 h to 12 h with 7.32 ± 1.35 ng/ml at 12 h. Since the last time point was at 12 h, C-K peak level was not observed. The areas under the concentration curves (AUC) from 0 to 12 h were 155.0 ± 19.5 ng•h/ml for Rb1 and 26.4 ± 6.4 ng•h/ml for C-K, respectively. The gradual decrease of Rb1 levels and the delayed increase in levels of C-K observed in human subjects supported previous reports that enteric microbiota played a key role in transforming Rb1 to C-K.