Showande Segun Johnson, Fakeye Titilayo Oyelola, Kajula Marena, Hokkanen Juho, Tolonen Ari
Faculty of Pharmacy Department of Clinical Pharmacy and Pharmacy Administration University of Ibadan Ibadan Nigeria.
Admescope Ltd Oulu Finland.
Food Sci Nutr. 2018 Nov 19;7(1):44-55. doi: 10.1002/fsn3.789. eCollection 2019 Jan.
Increasing use of medicinal herbs as nutritional supplements and traditional medicines for the treatment of diabetes, hypertension, hyperlipidemia, and malaria fever with conventional drugs poses possibilities of herb-drug interactions (HDIs). The potential of nine selected widely used tropical medicinal herbs in inhibiting human cytochrome P450 (CYP) isoenzymes was investigated.
In vitro inhibition of eight major CYP isoenzymes by aqueous extracts of , , and was estimated in human liver microsomes by monitoring twelve probe metabolites of nine probe substrates with UPLC/MS-MS using validated N-in-one assay method.
moderately inhibited CYP2C8, CYP2B6, CYP2D6, CYP1A2, and CYP2C9 with IC values of 37.93, 57.83, 67.39, 54.83, and 107.48 μg/ml, respectively, and inhibited CYP2D6 (IC = 77.19 μg/ml). inhibited CYP3A4 (IC = 45.58 μg/ml) and CYP2C19 (IC = 73.06 μg/ml) moderately but strongly inhibited CYP2D6 (IC = 1.19 μg/ml). Other aqueous extracts of and showed weak inhibitory activities against CYP1A2. and did not inhibit the CYP isoenzymes investigated.
Potential for clinically important CYP-metabolism-mediated HDIs is possible for and with drugs metabolized by CYP 2C8, 2B6, 2D6, 1A2, 2C9, 2C19, and 3A4. Inhibition of CYP2D6 by is of particular concern and needs immediate in vivo investigations.
随着药用草药越来越多地被用作营养补充剂以及与传统药物联合用于治疗糖尿病、高血压、高脂血症和疟疾热，存在草药 - 药物相互作用（HDIs）的可能性。研究了九种选定的广泛使用的热带药用草药抑制人细胞色素P450（CYP）同工酶的潜力。
使用经过验证的N合一测定法，通过UPLC/MS-MS监测九种探针底物的十二种探针代谢物，在人肝微粒体中评估 、 、 和 的水提取物对八种主要CYP同工酶的体外抑制作用。
适度抑制CYP2C8、CYP2B6、CYP2D6、CYP1A2和CYP2C9，IC 值分别为37.93、57.83、67.39、54.83和107.48 μg/ml， 抑制CYP2D6（IC = 77.19 μg/ml）。 适度抑制CYP3A4（IC = 45.58 μg/ml）和CYP2C19（IC = 73.06 μg/ml），但强烈抑制CYP2D6（IC = 1.19 μg/ml）。 和 的其他水提取物对CYP1A2表现出较弱的抑制活性。 和 未抑制所研究的CYP同工酶。
、 与由CYP 2C8、2B6、2D6、1A2、2C9、2C19和3A4代谢的药物之间，临床上重要的CYP代谢介导的HDIs有可能发生。 对CYP2D6的抑制尤其值得关注，需要立即进行体内研究。
