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丹红注射液及其主要成分对人细胞色素P450酶的体外抑制作用。

Inhibitory effects of Danhong Injection and its major constituents on human cytochrome P450 enzymes in vitro.

作者信息

Ye Lin-Hu, Zhao Xin-Qian, Kong Ling-Ti, Wang Li-Sha, Tao Xue, Wu Hui, He Mei, Chang Qi

机构信息

Department of Pharmacy, The First People's Hospital of Bijie, Bijie, China.

Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China.

出版信息

Biomed Chromatogr. 2018 Aug;32(8):e4250. doi: 10.1002/bmc.4250. Epub 2018 May 24.

DOI:10.1002/bmc.4250
PMID:29578591
Abstract

Danhong Injection (DHI) as a Chinese patent medicine is mainly used to treat ischemic encephalopathy and coronary heart disease in combination with other chemotherapy. However, the information on DHI's potential drug interactions is limited. The goal of this work was to examine the potential P450-mediated metabolism drug interaction arising from DHI and its active components. The results showed that DHI inhibited CYP2C19, CYP2D6, CYP3A4, CYP2E1 and CYP2C9 with IC values of 1.26, 1.42, 1.63, 1.10 and 1.67% (v/v), respectively. Danshensu and rosmarinic acid inhibited CYP2E1 and CYP2C9 with IC values of 36.63 and 75.76 μm, and 34.42 and 76.89 μm, respectively. Salvianolic acid A and B inhibited CYP2D6, CYP2E1 and CYP2C9 with IC values of 33.79, 21.64 and 31.94 μm, and 45.47, 13.52 and 24.15 μm, respectively. The study provides some useful information for safe and effective use of DHI in clinical practice.

摘要

丹红注射液(DHI)作为一种中成药,主要用于联合其他化疗药物治疗缺血性脑病和冠心病。然而,关于DHI潜在药物相互作用的信息有限。这项工作的目的是研究DHI及其活性成分引起的潜在细胞色素P450(P450)介导的代谢药物相互作用。结果表明,DHI对CYP2C19、CYP2D6、CYP3A4、CYP2E1和CYP2C9有抑制作用,其半数抑制浓度(IC)值分别为1.26%(v/v)、1.42%(v/v)、1.63%(v/v)、1.10%(v/v)和1.67%(v/v)。丹酚酸和迷迭香酸对CYP2E1和CYP2C9有抑制作用,其IC值分别为36.63和75.76 μmol/L,以及34.42和76.89 μmol/L。丹酚酸A和B对CYP2D6、CYP2E1和CYP2C9有抑制作用,其IC值分别为33.79、21.64和31.94 μmol/L,以及45.47、13.52和24.15 μmol/L。该研究为丹红注射液在临床实践中的安全有效应用提供了一些有用信息。

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