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Effects of Standardized Medicinal Plant Extracts on Drug Metabolism Mediated by CYP3A4 and CYP2D6 Enzymes.
Chemical Research in Toxicology ( IF 4.1 ) Pub Date : 2020-07-29 , DOI: 10.1021/acs.chemrestox.0c00182
Clarissa Feltrin 1 , Ingrid Vicente Farias 1 , Louis Pergaud Sandjo 2 , Flávio Henrique Reginatto 1 , Cláudia Maria Oliveira Simões 1
Affiliation  

The use of medicinal plants concomitantly with conventional drugs can result in herb–drug interactions that cause fluctuations in drug bioavailability and consequent therapeutic failure and/or toxic effects. The CYP superfamily of enzymes plays an important role in herb–drug interactions. Among CYP enzymes, CYP3A4 and CYP2D6 are the most relevant since they metabolize about 50% and 30% of the drugs on the market, respectively. Thus, the main goal of this study was to evaluate the occurrence of in vitro interactions between medicinal plant extracts and drug substrates of CYP3A4 and CYP2D6 enzymes. Standardized extracts from nine medicinal plants (Bauhinia forficata, Cecropia glaziovii, Cimicifuga racemosa, Cynara scolymus, Echinacea sp., Ginkgo biloba, Glycine max, Ilex paraguariensis, and Matricaria recutita) were evaluated for their potential interactions mediated by CYP3A4 and CYP2D6 enzymes. Among the extracts tested, C. glaziovii (red embaúba) showed the most relevant inhibitory effects of CYP3A4 and CYP2D6 activity, while I. paraguariensis (yerba mate) inhibited CYP3A4 activity. Both extracts were chemically analyzed by UPLC-MS/MS, and these inhibitory effects could lead to clinically potential and relevant interactions with the drug substrates of these isoenzymes.

中文翻译:

标准化药用植物提取物对 CYP3A4 和 CYP2D6 酶介导的药物代谢的影响。

药用植物与常规药物同时使用会导致药草相互作用,从而导致药物生物利用度的波动,从而导致治疗失败和/或毒性作用。CYP 酶超家族在草药-药物相互作用中起着重要作用。在 CYP 酶中,CYP3A4 和 CYP2D6 最为相关,因为它们分别代谢了市场上约 50% 和 30% 的药物。因此,本研究的主要目标是评估药用植物提取物与 CYP3A4 和 CYP2D6 酶的药物底物之间的体外相互作用。来自九个药用植物标准化提取物(紫荆forficata天蚕glaziovii黑升麻朝鲜蓟紫锥花属、银杏Glycine maxIlex paraguariensisMatricaria recutita ) 评估了它们由 CYP3A4 和 CYP2D6 酶介导的潜在相互作用。在测试的提取物中,C. glaziovii (red embaúba) 显示出最相关的 CYP3A4 和 CYP2D6 活性抑制作用,而I. paraguariensis (yerba mate) 抑制 CYP3A4 活性。两种提取物均通过 UPLC-MS/MS 进行化学分析,这些抑制作用可能导致与这些同工酶的药物底物的临床潜力和相关相互作用。
更新日期:2020-09-21
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