摘要
黄酮类化合物的开发和研究一直备受关注。淫羊藿素是从中药淫羊藿中提取的一种活性成分,结构上属于异戊二烯黄酮,是一种代表性的黄酮类化合物。淫羊藿素具有多种药理作用,包括抗肿瘤、抗炎、保护骨质和肝脏等,是一个具有开发前景的肝细胞癌和其他癌症治疗的候选药物。然而,体内生物利用度低是限制淫羊藿素等黄酮类化合物药物研发和临床应用的一大难题。研究表明,淫羊藿素在体内被迅速代谢生成葡萄糖醛酸化结合产物,可能是导致其生物利用度低的主要原因。此外,生成的葡萄糖醛酸化代谢产物可以被肝脏转运体摄取进入肝脏,并在肝脏中重新水解生成原形药物,完成“肝肠循环”过程。这可能解释了在生物利用度低的情况下,淫羊藿素在肝脏中仍有较高分布,且能发挥药效的原因。本研究综述了淫羊藿素的药代动力学研究进展,包括其在体内的吸收、分布、代谢和排泄过程,以及药物-药物相互作用,以期为优化给药方案以及评估其临床应用潜力提供借鉴和参考。
The development and research of flavonoids have been highly valued for many years.Icaritin is an active ingredient extracted from the traditional Chinese medicine Epimedium.Structurally,it belongs to isoprene flavonoids and is a representative flavonoid compound.Icaritin has various pharmacological effects,including anti-tumor,anti-inflammatory,bone and liver protection,and so on.However,low bioavailability in vivo is a major challenge limiting the development and clinical application of flavonoids,such as icaritin.Research has shown that icaritin is rapidly metabolized in the body to form glucuronides,which may be the main reason for its low bioavailability.In addition,the generated glucuronide metabolites can be taken up by liver transporters and hydrolyzed in the liver to produce the parent drug,completing the"enterohepatic circulation"process.This may explain why icaritin still has a high distribution in the liver and can exert its pharmacological effects even when its bioavailability is low.This article reviews the pharmacokinetic research progress of icaritin including its absorption,distribution,metabolism,and excretion in the body,as well as drug-drug interactions,in order to provide reference for optimizing drug delivery regimens and evaluating its clinical potential.
作者
戎怿
王士奇
RONG Yi;WANG Shiqi(Center for Drug Evaluation,NMPA,Beijing 100076,China)
出处
《中国医药导刊》
2024年第12期1192-1200,共9页
Chinese Journal of Medicinal Guide
