首页|天然产物中酶抑制剂的快速筛选方法研究进展

天然产物中酶抑制剂的快速筛选方法研究进展

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酶是新药发现的重要靶点,酶抑制剂的开发对于疾病治疗具有重要意义.中药及天然产物种类繁多、结构多样、生物活性广泛,是酶抑制剂的重要源泉.然而,中药及天然产物结构复杂、活性成分含量较低,高效准确地从中筛选出酶抑制剂至关重要.近年来,随着生物大分子构象研究的深入及计算机科学的发展以及现代分离分析技术及仪器的创新,一系列酶抑制剂的快速筛选技术与方法应运而生.本文将系统介绍天然产物中酶抑制剂的快速筛选方法,包括计算机虚拟筛选、基于酶分子与配体之间特异性作用的亲和筛选以及结合色谱分离的生物活性测试等,并对此进行优缺点比较,以期为中药及天然产物中酶抑制剂的发掘提供参考.
Advances of rapid screening methods for enzyme inhibitors in natural products
Enzymes are important drug targets,and the development of enzyme inhibitors is significant for treatment of disea-ses.Natural products characterized by various kinds,diverse structures and extensive biological activities are an abundant source of enzyme inhibitors.However,natural products have complex structures and low content of active ingredients,so it is crucial to screen enzyme inhibitors efficiently and accurately.In recent years,with the deepening of research on the conforma-tion of biological macromolecules and the vigorous development of computer science and the innovation of modern separation and analysis techniques and instruments,a series of novel screening techniques and methods of enzyme inhibitors have been developed.In this paper,rapid screening techniques and methods for natural enzyme inhibitors,including computer virtual screening,affinity screening based on the specific interaction between enzyme molecules and ligands,and biological activity assay combined with chromatographic separation,were systematically introduced,then their advantages and disadvantages of these methods were also compared,in order to provide references for the exploration of enzyme inhibitors in natural products from traditional Chinese medicine.

enzyme inhibitorrapid screeningnatural productsresearch review

陈凯华、朱雪艳、郭嘉亮、曾煦欣

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佛山科学技术学院,佛山 528000

暨南大学药学院,广州 510632

酶抑制剂 快速筛选 天然产物 研究综述

国家自然科学基金广东省教育厅重点领域专项广东省岭南中药全过程质量控制与精准分析工程技术研究中心支持项目佛山大学2023年度学生学术基金

821737812020ZDZX2057204266924217xsjj202312kja02

2024

天然产物研究与开发
中国科学院成都文献情报中心

天然产物研究与开发

CSTPCD北大核心
影响因子:0.783
ISSN:1001-6880
年,卷(期):2024.36(7)