射干苷元衍生物的合成及初步抗氧化活性研究  

Synthesis and antioxidant activity of tectorigenin derivatives

作　　者：陈帅[1] 罗森[1] 谭正怀[1] 刘琪 汤依娜[1] 张磊[1] 竹敏 王笳[1] 袁崇均[1] CHEN Shuai;LUO Sen;TAN Zheng-huai;LIU Qi;TANG Yi-na;ZHANG Lei;ZHU Min;WANG Jia;YUAN Chong-jun(Sichuan Academy of Chinese Medicine Sciences,2 Reproductive&Women-Children Hospital,Chengdu University of Traditional Chinese Medicine,Chengdu 610041,China)

机构地区：[1]四川省中医药科学院,成都 [2]成都中医药大学附属生殖妇幼医院,成都610041

出　　处：《中国新药杂志》2022年第14期1420-1425,共6页Chinese Journal of New Drugs

基　　金：四川省科技厅重点研发项目(2020YFS0370);四川省科研院所基本科研业务专项(A-2020N-23,A-2021N-6)。

摘　　要：目的:寻找高效、低毒的抗氧化损伤的药物。方法:以射干苷元为先导化合物,分别采用酰化、Mannich、脱甲基反应合成射干苷元衍生物1~6,通过^(1)H-和^(13)C-NMR,IR,UV及MS(ESI)数据证实其结构,并采用MTT法和H_(2)O_(2)诱导PC12细胞氧化损伤模型初步测定其抗氧化活性。结果:抗氧化活性表明化合物1~6对H_(2)O_(2)诱导PC12细胞损伤均有保护作用,与H_(2)O_(2)模型对照组相比,多数药物组细胞存活率提高(P<0.05,P<0.01);与射干苷元组相比,化合物2浓度为10μmol·L^(-1)时,能明显提高细胞存活率(P<0.05),化合物5浓度≥0.1μmol·L^(-1),化合物6浓度≥1μmol·L^(-1)时,均能明显提高细胞存活率(P<0.05,P<0.01),所有化合物抗氧化活性未见报道。结论:化合物1、化合物2和化合物5为新化合物,化合物5为磺酸盐,具有一定的水溶性,抗氧化活性强,为较优的候选药物,具有良好的研发价值。Objective:To search for effective and low toxic anti-oxidation drugs.Methods:Tectorigenin derivatives 1~6 were synthesized by acylation,Mannich reaction,and demethylation.Their structures were confirmed by ^(1)H-NMR,^(13)C-NMR,IR,UV and MS(ESI).The antioxidant activities were determined by MTT and oxidative damage model of PC12 cells induced by H_(2)O_(2).Results:Compounds 1~6 could protect PC12 cells from H_(2)O_(2)-induced injury.Compared with the H_(2)O_(2) model group,the survival rates of PC12 cells in most drug groups were increased(P<0.05,P<0.01).Compared with the tectorigenin group,the concentration of compound 2 was 10μmol·L^(-1),the cell survival rate was significantly increased(P<0.05),the concentration of compound 5 was greater than or equal to 0.1μmol·L^(-1),the concentration of compound 6 was greater than or equal to 1μmol·L^(-1),the cell survival rate was significantly increased(P<0.05,P<0.01),the antioxidant activities of all compounds had not been reported.Conclusion:Compounds 1,2 and 5 are new compounds,and compound 5 is sulfonate,which has certain water-soluble,strong antioxidant activity and good development value.

关 键 词：射干苷元衍生物 合成 结构鉴定 PC12细胞 抗氧化活性 

分 类 号：R914[医药卫生—药物化学]