Department of Obstetrics and Gynecology, Xiaolan People’s Hospital Affiliated to Southern Medical University, Zhongshan, Guangdong, China.
Curr Pharm Des. 2011;17(4):357-407. doi: 10.2174/138161211795164194.
Herbal medicines, an important group of multicomponent therapeutics, are widely and increasignly used worldwide. Despite the popularitiy of herbal medicines, the clinical evidence that support the use of most herbal medicines is weak. Pharmacokinetic and absorption, distribution, metabolism and excretion (ADME) studies have been integrated into modern drug development, but ADME studies are generally not needed for herbal remedy discovery and development. For the majority of herbal medicines, data on their ADME and pharmacokinetic properties in humans are lacking or scant. An extensive literature search indicates that there are limited data on ADME properties of herbal medicines in humans. Many herbal compounds undergo Phase I and/or Phase II metabolism in vivo, with cytochrome P450s (CYPs) and uridine diphosphate glucuronosyltransferases (UGTs) playing a major role. Some herbal ingredients are substrates of P-glycoprotein (P-gp/MDR1/ABCB1) which is highly expressed in the intestine, liver, brain and kidney. As such, the activities of these drug metabolizing enzymes and drug transporters are critical determining factors for the in vivo ADME processes of herbal remedies. There are increasing ADME studies of herbal remedies, but these studies are mainly focused on a small number of herbal medicines including St John's wort, milk thistle, curcumin, echinacea, ginseng, ginkgo, and ginger. For an herbal medicine, the pharmacological activity is gained when the active agents or the active metabolites reach and sustain proper levels at their sites of action. Both the dose levels and ADME processes of active herbal components in the body govern their target-site concentrations and thus the therapeutic responses. In this regard, a safe and optimal use of herbal medicines requires a full understanding of their ADME profiles. To optimize the use of herbal remedies, further studies to explore their ADME properties in humans are certainly warranted.
草药作为多成分治疗药物的重要组成部分，在全球范围内得到了广泛而日益增加的应用。尽管草药受到广泛欢迎，但支持大多数草药使用的临床证据仍然薄弱。药代动力学和吸收、分布、代谢和排泄（ADME）研究已被纳入现代药物开发中，但 ADME 研究通常不需要用于草药发现和开发。对于大多数草药来说，其在人体内的 ADME 和药代动力学性质的数据缺乏或稀少。广泛的文献检索表明，关于草药在人体内的 ADME 性质的数据有限。许多草药化合物在体内经历 I 相和/或 II 相代谢，细胞色素 P450s（CYPs）和尿苷二磷酸葡萄糖醛酸转移酶（UGTs）起着主要作用。一些草药成分是 P-糖蛋白（P-gp/MDR1/ABCB1）的底物，P-gp/MDR1/ABCB1 在肠道、肝脏、大脑和肾脏中高度表达。因此，这些药物代谢酶和药物转运体的活性是决定草药体内 ADME 过程的关键因素。越来越多的草药治疗药物的 ADME 研究，但这些研究主要集中在少数几种草药上，包括贯叶连翘、奶蓟草、姜黄素、紫锥菊、人参、银杏和生姜。对于一种草药，当活性药物或其活性代谢物在其作用部位达到并维持适当水平时，就会获得药理活性。体内活性草药成分的剂量水平和 ADME 过程控制着它们的靶位浓度，从而影响治疗反应。在这方面，安全和优化使用草药需要充分了解其 ADME 概况。为了优化草药的使用，进一步研究探索其在人体内的 ADME 特性是非常必要的。
