京尼平衍生物的合成及其抗类风湿关节炎活性  

Synthesis and Anti-rheumatoid Arthritis Activity of Genipin Derivatives

作　　者：柯江涛 何格 李志 董心同 陈芳园 甘珮荣 吴虹 KE Jiangtao;HE Ge;LI Zhi;DONG Xintong;CHEN Fangyuan;GAN Peirong;WU Hong(College of Pharmacy,Anhui University of Chinese Medicine,Hefei 230012,China;Anhui Province Key Laboratory of Research and Development of Chinese Medicine,Key Lab of Xin'an Medicine,Ministry of Education,Hefei 230012,China)

机构地区：[1]安徽中医药大学药学院,安徽合肥230012 [2]新安医学教育部重点实验室中药研究与开发安徽省重点实验室,安徽合肥230012

出　　处：《合成化学》2022年第11期888-892,共5页Chinese Journal of Synthetic Chemistry

基　　金：国家自然科学基金项目(81874360,81473400);安徽高校自然科学研究重大项目(KJ2021ZD0060);安徽中医药大学2020级研究生科技创新基金重点项目(2020ZD05)。

摘　　要：以京尼平(Genipin, GEP)为先导物,设计并合成了4个C-10位含螺环氨甲酸酯片段的GEP衍生物(6a~6d),其结构经HR-MS(ESI),^(1)H NMR和^(13)C NMR确证。采用CCK-8法测试了目标化合物对人类风湿关节炎成纤维滑膜细胞(MH7A)增殖的抑制作用。结果表明:化合物6a的抗增殖活性最强,在200μmol/L下的抑制率为75.81%,具有进一步结构优化的价值。Four genipin(GEP) derivatives characterized by the spirocyclic-containing carbamate fragments at C-10 position were designed and synthesized from GEP, and their structures were confirmed by HR-MS(ESI), ^(1)H NMR and^(13)C NMR. The inhibitory effect of the target compounds on the proliferation of human rheumatoid arthritis synovial cells(MH7 A) was tested using the CCK-8 assay, compound 6 a exerted the most potent anti-proliferative effect, and the inhibition rate was 75.81% at the concentration of 200 μmol/L, thereby meriting further structural modification.

关 键 词：京尼平 合成 类风湿关节炎 成纤维滑膜细胞 增殖活性 螺环 

分 类 号：R914.5[医药卫生—药物化学] O62[医药卫生—药学]