Tawab Mona Abdel, Bahr Ute, Karas Michael, Wurglics Mario, Schubert-Zsilavecz Manfred
Institute of Pharmaceutical Chemistry, Johann Wolfgang Goethe University, Frankfurt, Germany.
Drug Metab Dispos. 2003 Aug;31(8):1065-71. doi: 10.1124/dmd.31.8.1065.
Even though the degradation of ginsenosides has been thoroughly studied in animals and in vitro using acids, enzymes, and intestinal bacteria, knowledge concerning the systemic availability of ginsenosides and their degradation products in humans is generally lacking. Therefore, the attention in this article is focused on the identification of ginsenosides and their hydrolysis products reaching the systemic circulation in man. This is of great importance in understanding clinical effects, preventing herb-drug interactions, and optimizing the biopharmaceutical properties of ginseng preparations. Using a sensitive mass spectrometric method, which is specific for the identification of ginsenosides in complex biological matrices, the degradation pathway of ginsenosides in the gastrointestinal tract of humans could be elucidated following the oral administration of ginseng. Within the frame of a pilot study, human plasma and urine samples of two subjects were screened for ginsenosides and their possible degradation products. In general, the urine data coincided well with the plasma data. In both volunteers the same hydrolysis products, which are not originally present in the Ginsana extract (Pharmaton S.A., Lugano, Switzerland) ingested, were identified in plasma and urine. It was shown that two hydrolysis products of the protopanaxatriol ginsenosides, namely G-Rh1 and G-F1 may reach the systemic circulation. In addition, compound-K, the main intestinal bacterial metabolite of the protopanaxadiol ginsenosides, was detected in plasma and urine. These products are probably responsible for the action of ginseng in humans. In opposition to previous reports, G-Rb1 was identified in plasma and urine of one subject.
尽管人参皂苷在动物体内以及利用酸、酶和肠道细菌进行的体外实验中其降解情况已得到充分研究，但关于人参皂苷及其降解产物在人体中的全身可用性的知识普遍匮乏。因此，本文重点关注人参皂苷及其水解产物进入人体体循环的鉴定。这对于理解临床效果、预防草药与药物相互作用以及优化人参制剂的生物药剂学性质至关重要。采用一种对复杂生物基质中人参皂苷鉴定具有特异性的灵敏质谱方法，在口服人参后可阐明人参皂苷在人体胃肠道中的降解途径。在一项初步研究框架内，对两名受试者的人血浆和尿液样本进行了人参皂苷及其可能降解产物的筛查。总体而言，尿液数据与血浆数据吻合良好。在两名志愿者的血浆和尿液中均鉴定出了原本不存在于所摄入的金纳多提取物（瑞士卢加诺的Pharmaton S.A.公司）中的相同水解产物。结果表明，原人参三醇型人参皂苷的两种水解产物，即G-Rh1和G-F1可能进入体循环。此外，在血浆和尿液中检测到了原人参二醇型人参皂苷的主要肠道细菌代谢产物Compound-K。这些产物可能是人参在人体中发挥作用的原因。与之前的报道不同，在一名受试者的血浆和尿液中鉴定出了G-Rb1。
