穿心莲内酯衍生物抗肿瘤、解热抗炎构效关系研究进展

摘要

目的 对近年来穿心莲内酯衍生物抗肿瘤、解热抗炎的构效关系研究进展综述,为穿心莲内酯的进一步研究提供思路.方法 对相应文献进行归纳、总结和综述.结果 穿心莲内酯及其衍生物发挥抗肿瘤活性的必需基团是完整的α-亚烷基-γ-丁内酯,Δ12,13双键,Δ8,17双键或成环及C14羟基等活性基团;而α-亚烷基-γ-丁内酯环打开与否和抗炎无关,穿心莲内酯及其衍生物的双键位置决定其抗炎作用,具有环内双键的化合物抗炎作用强于具有环外双键的化合物.结论 穿心莲内酯衍生物具有良好的开发前景,应加强其衍生物与构效关系的研究.%Objective To summarize the advances of structure-activity relationships (SARs) of andrographolidc derivatives, and to provide a theoretical basis for andrographolidc research and development. Method The corresponding literatures were reviewed and synthesized. Results The complete α-alkylidcnc-γ-butyrolactonc moiety, the exocyclic double bond Δ12 ,13 , Δ8 ,17 of a double or cy-clization and CM hydroxyl arc the essential groups of andrographolidc derivatives;The anti-inflammatory has no relation with the α-alkylidcnc-y-butyrolactonc. The position of the double bond determines the anti-inflammatory effects of andrographolidc derivatives, and compounds with cxocyclic double bond has more anti-inflammatory effect than with endocyclic double bond. Conclusion Andrographolidc derivatives arc promising for forther development. We should pay more attention to the research of SARs of andrographolidc derivatives.