穿心莲内酯衍生物抗肿瘤、解热抗炎构效关系研究进展

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。

Advances in research on the anti-tumor,anti-pyretic and anti-inflammatory activity of andrographolide derivatives

Objective To summarize the advances of structure-activity relationships(SARs) of andrographolide derivatives,and to provide a theoretical basis for andrographolide research and development.Method The corresponding literatures were reviewed and synthesized.Results The complete α-alkylidene-γ-butyrolactone moiety,the exocyclic double bond Δ12,13,Δ8,17 of a double or cyclization and C14 hydroxyl are the essential groups of andrographolide derivatives;The anti-inflammatory has no relation with the α-alkylidene-γ-butyrolactone.The position of the double bond determines the anti-inflammatory effects of andrographolide derivatives,and compounds with exocyclic double bond has more anti-inflammatory effect than with endocyclic double bond.Conclusion Andrographolide derivatives are promising for forther development.We should pay more attention to the research of SARs of andrographolide derivatives.