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高脂血症是现代社会高发的代谢性疾病，其临床治疗主要依赖于他汀类药物及降脂中药。小檗碱作为一种源于中药的季铵异喹啉类生物碱，近年来在降脂领域展现出良好的应用潜力。然而，小檗碱水溶性差且生物利用度低，限制了其临床转化与应用。因此，研究者们通过结构修饰策略，对小檗碱开展了多元化结构优化，旨在提高其衍生物的降脂活性。本文作者系统综述了小檗碱的结构修饰方法、衍生物的降脂活性以及相应的构效关系，以期为开发具有小檗碱母核的新型降脂药物提供理论参考和实践指导。
Abstract：Hyperlipidemia is a highly prevalent metabolic disease in modern society.Its clinical treatment mainly relies on statins and lipid-lowering traditional Chinese medicine.Berberine, as a naturally occurring quaternary ammonium isoquinoline alkaloid, has shown promising application potential in the lipid-lowering field in recent years.However, the poor water solubility and low bioavailability limit its clinical translation and application.Therefore, researchers used diversified structural modification methods to optimize the structure of berberine, in order to enhance its lipid-lowering effect.This review systematically summarized the structural modification methods of berberine, the lipid-lowering effects of its derivatives, and the corresponding structure-activity relationship, aiming to provide theoretical reference and practical guidance for the development of new lipid-lowering drugs with berberine scaffold.
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基本信息:
DOI：10.14142/j.cnki.cn21-1313/r.20240129
中图分类号:R284.1
引用信息:
[1]尹梦轩,肖桂芝,赵翔翔,等.小檗碱的结构修饰及其衍生物的降脂作用研究进展[J].中国药物化学杂志,2026,36(01):67-80.DOI:10.14142/j.cnki.cn21-1313/r.20240129.
基金信息:
国家自然科学基金项目(82274221、82274236)
2024-07-16
2024
2024-10-05
2024
1
2026-02-25
2026-02-25