转运蛋白介导黄酮类化合物葡萄糖醛酸化产物的研究进展  

Research Progress on Transporter-Mediated Glucuronides of Flavonoids

作　　者：戎怿 姜凯迪 RONG Yi;JIANG Kaidi(Center for Drug Evaluation,National Medical Products Administration,Beijing 100076,China)

机构地区：[1]国家药品监督管理局药品审评中心,北京100076

出　　处：《中国医药导刊》2024年第10期981-988,共8页Chinese Journal of Medicinal Guide

摘　　要：黄酮类化合物是广泛存在于自然界中的一类物质,具有多种药理作用,包括预防及治疗癌症、心脑血管疾病、骨质疏松等。然而,多数黄酮类化合物在口服给药后的生物利用度低,限制了药物的开发和临床应用。国内外诸多学者对其吸收代谢机制进行了研究,发现药物转运蛋白与黄酮类化合物及其主要代谢产物——葡萄糖醛酸化结合物的相互作用是影响其体内生物利用度的主要因素之一。本研究总结了有关摄取和外排转运蛋白与黄酮类化合物及其葡萄糖醛酸代谢产物转运相互作用的研究进展,概述了与其相关的文献,以期为提高黄酮类化合物的生物利用度和临床合理应用提供理论依据。Flavonoids are a class of substances widely existing in nature,which have various pharmacological effects,including the prevention and treatment of cancer,cardiovascular and cerebrovascular diseases,osteoporosis,etc.However,the low bioavailability of most flavonoids after oral administration limits the development and clinical application of related drugs.Many scholars at home and abroad have studied its absorption and metabolism mechanisms,and found that the interaction between drug transporters and flavonoids and their main metabolites–glucuronides,is one of the main factors affecting its in vivo bioavailability.This article reviews the research progress on the interaction between transporters and glucuronides of flavonoids,and summarizes the relevant literature,in order to provide theoretical basis for improving the bioavailability and clinical rational application of flavonoids.

关 键 词：转运蛋白 药物-药物相互作用 肠肝循环 葡萄糖醛酸转移酶 

分 类 号：R91[医药卫生—药学]