活性化合物泽兰素的合成研究进展  

Synthetic Research Progress on the Active Structure of Euparin

作　　者：陈振羽 王金强 徐文静 郭骥 邹坤 曹燕来 黄年玉 CHEN Zhen-yu;WANG Jin-qiang;XU Wen-jing;GUO Ji;ZOU Kun;CAO Yan-lai;HUANG Nian-yu(Key Laboratory of Functional Yeast(China National Light Industry),Key Laboratory of Natural Products Research and Development,College of Biological and Pharmaceutical Sciences,China Three Gorges University,Yichang 443002;Hubei Guangchen Pharmaceutical Co.,Ltd.,Yichang 443000,China)

机构地区：[1]三峡大学生物与制药学院,天然产物研究与利用湖北省重点实验室,中国轻工业功能酵母重点实验室,湖北宜昌443002 [2]湖北广辰药业有限公司,湖北宜昌443000

出　　处：《化学试剂》2023年第6期131-138,共8页Chemical Reagents

基　　金：国家自然科学基金项目(22207063);高等学校学科创新引智计划项目(111计划,D20015);湖北省自然科学基金项目(2022CFB838);湖北省教育厅项目(D20221204,Q20221212)。

摘　　要：泽兰素是来源于泽兰属植物的苯并呋喃活性成分,具有抗肿瘤、抗炎、杀菌、降糖、抗抑郁和抗氧化等多种生物活性,具有进一步开发利用的前景。由于泽兰素的获取主要从泽兰属植物中提取分离,为快速获取泽兰素,目前文献中主要有酰基苯并呋喃衍生化法、水杨醛环化法、烯炔偶联环化法和炔醇偶联环化法等4种方法可用于泽兰素的全合成;在泽兰素的结构衍生方面,主要有泽兰素类似物和多聚体两类活性成分报道。系统综述了近50年来关于泽兰素的生物活性、合成方法和结构修饰的文献研究进展,以期为泽兰素的进一步开发利用提供参考。Euparin is an active benzofuran component from Eupatorium chinense.Literature research shows that euparin has a variety of biological activities including anti-tumor,anti-inflammatory,bactericidal,hypoglycemic,antidepressant and antioxidant effects,which has a prospect of further development and utilization.Currently the acquisition of euparin is mainly extracted from Eupatorium plants.In order to quickly obtain abundant euparin for further activity evaluation,there are four methods of total synthesis of euparin,including the derivation reaction of acyl benzofuran,cyclization of salicylaldehyde,coupling cyclization enyne and aryl halide,and coupling cyclization of alkynol.Two kinds of active euparin derivatives(euparin analogues and polymers) were also reported.In this paper,the research progress of biological activity,synthetic methods and structure modification of euparin in the past 50 years was reviewed systematically,in order to provide reference for further development and utilization of euparin.

关 键 词：泽兰素 全合成 结构修饰 生物活性 研究进展 

分 类 号：O626.3[理学—有机化学]