α-山道年光催化重排衍生物的制备及细胞毒活性研究

Photocatalysis Synthesis and Cytotoxicity of α-Santonin Rearrangement Derivatives

以α-山道年为原料,经光异构化、水解、氧化、还原等多步反应,设计并合成了20个愈创木内酯型衍生物1-20和一个桉烷化合物6-epi-santonin.其结构经1H NMR,13 CNMR及MS确证.采用噻唑蓝（MTT）法,测试所有化合物对A549和Hep G2细胞的增殖抑制作用.结果表明愈创木内酯环氧化合物9和15显示较好的抑制所测肿瘤细胞增殖活性,对人类A549和Hep G2细胞IC50分别为（14.5±0.1）和（10.6±0.3）,（6.4±1.3）和（8.1±0.7）μmol/L.

20 guaianolide derivatives 1-20 and 6-epi-santonin were synthesized from α-santonin through rearrangement, oxidation, and reduction, hydrolysis. The structures of all compounds were characterized by 1H NMR, 13 C NMR and MS. The cell proliferation inhibiting activities of the target compounds were evaluated against A549 and Hep G2 cell lines by thiazolyl blueterazolium bromide（MTT） method. The results showed that the epoxy guaiane 9 had obvious inhibitory effect on A549 and Hep G2 cell lines with IC50 values of（14.5±0.1）,（10.6±0.3） μmol/L while epoxy guaiane 15 showed IC50 values of（6.4±1.3） and（8.1±0.7） μmol/L.