秦皮乙素及其衍生物的合成与药理学研究进展

Advances in the synthesis and pharmacological activities of esculetin and its derivatives

秦皮乙素是陕西道地药材秦皮的主要有效成分,化学名为6,7-二羟基香豆素,俗称七叶亭.秦皮乙素因其独特的结构及理化性质正日益引起科研人员的浓厚兴趣.科学家已研究发现秦皮乙素具有良好的抗肿瘤、抗炎及抗菌活性,显示了其广阔的应用前景.本文综述了近年来国内外学者对秦皮乙素及其合成与药理研究成果,以及近十年来秦皮乙素衍生物的合成与生物活性研究成果,包括抗溶组织梭菌胶原酶(ChC),灭杀白蚁,以及显著的抗大肠杆菌与抗念珠菌活性等.随着各种结构新颖的秦皮乙素衍生物不断地被合成报道,其生物活性与作用机制逐步被阐明,陕西道地药材秦皮及其主要成分秦皮乙素的开发与临床应用前景将会变得更加广阔.

Esculetin is the main active ingredient of Cortex Fraxini,its chemical name is 6,7-dihydroxycoumarin.In recent years,scientists have found that esculetin possessed good antitumor,anti-inflammatory and antibacterial activities,which showed a broad pharmaceutical application prospects.This review covered recent studies on the synthesis,pharmacological activities and mechanism of esculetin and its derivatives over the past decade,including anticlostridium histolyticum collagenase（ChC）,eradicating termites,as well as significant activity against Escherichia coli and Candida.With a variety of novel esculetin derivatives being continuously synthesized,the development and clinical application of Shaanxi Cortex Fraxini and its main ingredient esculetin will be more prospective.