Salvia miltiorrhiza Roots against Cardiovascular Disease: Consideration of Herb-Drug Interactions.
Salvia miltiorrhiza Roots against Cardiovascular Disease: Consideration of Herb-Drug Interactions.
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丹参根对抗心血管疾病：草药与药物相互作用的考虑
DOI：
10.1155/2017/9868694
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发表时间：
2017
影响因子：
--
通讯作者：
Tian DD
中科院分区：
文献类型：
--
作者：
Chen F;Li L;Tian DD
丹参根（丹参）因其对心血管的益处而在亚洲被广泛使用，并且含有亲水性酚酸和亲脂性丹参酮，这被认为是其治疗功效的原因。这篇综述总结了丹参根中的这些生物活性成分对药物药代动力学的影响，并根据已发表的人体体外和体内研究数据，对蛋白质结合、酶活性和转运蛋白活性的改变进行了机械见解。体外研究表明，细胞色素P450（CYP450）、羧酸酯酶、儿茶酚-O-甲基转移酶、有机阴离子转运蛋白1（OAT1）和OAT3以及P-糖蛋白是参与丹参-药物相互作用的主要靶标。与亲水性酚酸相比，亲脂性丹参酮对 CYP 活性具有更强的抑制作用，前者的 Ki 值低得多。临床丹参-药物相互作用研究主要使用CYP1A2和CYP3A4探针底物进行。此外，共存成分对那些提到的生物活性化合物的药代动力学行为的影响也包括在本文中。
Salvia miltiorrhiza root (Danshen) is widely used in Asia for its cardiovascular benefits and contains both hydrophilic phenolic acids and lipophilic tanshinones, which are believed to be responsible for its therapeutic efficacy. This review summarized the effects of these bioactive components from S. miltiorrhiza roots on pharmacokinetics of comedicated drugs with mechanic insights regarding alterations of protein binding, enzyme activity, and transporter activity based on the published data stemming from both in vitro and in vivo human studies. In vitro studies indicated that cytochrome P450 (CYP450), carboxylesterase enzyme, catechol-O-methyltransferase, organic anion transporter 1 (OAT1) and OAT3, and P-glycoprotein were the major targets involved in S. miltiorrhiza-drug interactions. Lipophilic tanshinones had much more potent inhibitory effects towards CYPs activities compared to hydrophilic phenolic acids, evidenced by much lower Ki values of the former. Clinical S. miltiorrhiza-drug interaction studies were mainly conducted using CYP1A2 and CYP3A4 probe substrates. In addition, the effects of coexisting components on the pharmacokinetic behaviors of those noted bioactive compounds were also included herein.