石蒜碱药理活性及构效关系研究进展  

Research progress on the pharmacological activities and structure-activity relationships of lycorine

作　　者：曾炳麟 赵茹 潘显道[1,2] ZENG Bing-lin;ZHAO Ru;PAN Xian-dao(Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,China;Shandong Dayin Marine Biopharmaceutical Co.,Ltd.,Rongcheng 264300,China)

机构地区：[1]中国医学科学院北京协和医学院药物研究所,北京100050 [2]山东达因海洋生物制药股份有限公司,荣成264300

出　　处：《天然产物研究与开发》2021年第2期342-351,341,共11页Natural Product Research and Development

基　　金：国家十三五重大专项子课题(2018ZX09721003-008-026)。

摘　　要：石蒜碱是药用石蒜科植物的有效成分之一,是重要的异喹啉类生物碱。石蒜碱拥有刚性的环系骨架、连续的手性中心、三级胺等独特的化学结构特征。同时其药理活性丰富多样,近年来,针对其抗癌、抗病毒、抗炎、抗寄生虫、抑制乙酰胆碱酯酶活性的研究越来越多,尤其在抗癌、抗病毒方面石蒜碱表现出较大潜力,特别是新型冠状病毒SARS-CoV-2研究。石蒜碱各种药理活性的作用机制复杂且新颖,是当前的研究热点。为了更好地梳理有关石蒜碱的研究进展,为其机制探讨和结构修饰提供思路,本文着眼于石蒜碱的药理活性和构效关系进行了系统的总结。Lycorine,an important isoquinoline alkaloid,is the effective component of Amaryllidaceae family plants.Lycorine possesses unique structures including a rigid ring skeleton,contiguous chiral centers and tertiary amine,increasing the difficulty to rich the structural diversities.In recent years,accumulated evidence shows that lycorine can be a lead compound for many therapeutic applications,including anti-cancer,anti-virus,anti-inflammation,anti-parasitic and AChE inhibition.Especially,lycorine exhibits great potential in anti-cancer and anti-virus applications because of its broad-spectrum activity and novel mechanism.However,it is still a complicated issue to identify the specific targets of lycorine.The relationship among its various mechanisms of action for a certain pharmacological activity is also elusive.To take full advantage of this natural resource for drug discovery,more interest has been drawn to the structural modification and mechanism study of lycorine.For the sake of facilitating future research,this review systematically summarized the updating research progress on the pharmacological activities and structure-activity relationships of lycorine.

关 键 词：石蒜碱 药理活性 作用机制 构效关系 

分 类 号：R914.5[医药卫生—药物化学]