天然产物研究与开发 ›› 2021, Vol. 33 ›› Issue (2): 342-351.doi: 10.16333/j.1001-6880.2021.2.019

• 综述 • 上一篇    

石蒜碱药理活性及构效关系研究进展

曾炳麟1,赵茹1,潘显道1,2*   

  1. 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
  • 出版日期:2021-02-28 发布日期:2021-03-04
  • 基金资助:
    国家十三五重大专项子课题(2018ZX09721003-008-026)

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

ZENG Bing-lin1,ZHAO Ru1,PAN Xian-dao1,2*   

  1. 1Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,China; 2Shandong Dayin Marine Biopharmaceutical Co.,Ltd.,Rongcheng 264300,China

  • Online:2021-02-28 Published:2021-03-04

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。


关键词: 石蒜碱, 药理活性, 作用机制, 构效关系

Abstract:

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.

Key words: lycorine, pharmacological activities, mechanism of action, structure-activities relationships

中图分类号:  R914.5