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首页> 外文期刊>Food Science & Nutrition >Potential inhibition of major human cytochrome P450 isoenzymes by selected tropical medicinal herbs—Implication for herb–drug interactions
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Potential inhibition of major human cytochrome P450 isoenzymes by selected tropical medicinal herbs—Implication for herb–drug interactions

机译：某些热带药用植物对主要人类细胞色素P450同工酶的潜在抑制作用-对药草相互作用的影响

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Background 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. Materials and methods In vitro inhibition of eight major CYP isoenzymes by aqueous extracts of Allium sativum, Gongronema latifolium, Moringa oleifera , Musa sapientum, Mangifera indica, Tetracarpidium conophorum , Alstonia boonei, Bauhinia monandra, and Picralima nitida 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. Results Mangifera indica moderately inhibited CYP2C8, CYP2B6, CYP2D6, CYP1A2, and CYP2C9 with IC 50 values of 37.93, 57.83, 67.39, 54.83, and 107.48?μg/ml, respectively, and Alstonia boonei inhibited CYP2D6 (IC 50 ?=?77.19?μg/ml). Picralima nitida inhibited CYP3A4 (IC 50 ?=?45.58?μg/ml) and CYP2C19 (IC 50 ?=?73.06?μg/ml) moderately but strongly inhibited CYP2D6 (IC 50 ?=?1.19?μg/ml). Other aqueous extracts of Gongronema latifolium, Bauhinia monandra, and Moringa oleifera showed weak inhibitory activities against CYP1A2. Musa sapientum, Allium sativum, and Tetracarpidium conophorum did not inhibit the CYP isoenzymes investigated. Conclusion Potential for clinically important CYP‐metabolism‐mediated HDIs is possible for Alstonia boonei, Mangifera indica, and Picralima nitida with drugs metabolized by CYP 2C8, 2B6, 2D6, 1A2, 2C9, 2C19, and 3A4. Inhibition of CYP2D6 by Picralima nitida is of particular concern and needs immediate in vivo investigations.
机译：背景技术使用常规药物越来越多地使用草药作为营养补充剂和传统药物来治疗糖尿病，高血压，高血脂和疟疾，这带来了药-药相互作用（HDI）的可能性。研究了九种精选的广泛使用的热带草药在抑制人细胞色素P450（CYP）同工酶方面的潜力。材料和方法在人肝微粒体中，估计了大蒜，大蒜，辣木，辣木，红景天，曼陀罗，四叶草，Alstonia boonei，Bauhinia monandra和nital Picnitar nitidas的水提取物对八种主要CYP同工酶的体外抑制作用。使用经过验证的N合一测定方法，使用UPLC / MS-MS对9种探针底物的12种探针代谢物进行分析。结果印度芒果对CYP2C8，CYP2B6，CYP2D6，CYP1A2和CYP2C9有中等程度的抑制作用，IC 50值分别为37.93、57.83、67.39、54.83和107.48？μg/ ml，Alstonia boonei抑制CYP2D6（IC 50为77？微克/毫升）。 Picralima nitida适度抑制CYP3A4（IC 50？=？45.58？μg/ ml）和CYP2C19（IC 50？=？73.06？μg/ ml），但强烈抑制CYP2D6（IC 50？=？1.19？μg/ ml）。 Gongronema latifolium，Bauhinia monandra和Moringa oleifera的其他水提取物对CYP1A2的抑制活性较弱。 Musa sapientum，Allium sativum和Tetracarpidium conophorum不会抑制所研究的CYP同工酶。结论CYP 2C8、2B6、2D6、1A2、2C9、2C19和3A4代谢的药物可能对Alstonia boonei，Mangifera indica和Picralima nitida产生具有重要临床意义的CYP代谢介导的HDI。 CYP2D6被尼古拉霉素的抑制特别令人关注，需要立即进行体内研究。

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