Pang Chaohai, Luo Jinhui, Liu Chunhua, Wu Xuejin, Wang Dingyong
Analysis and Test Center of Chinese Academy of Tropical Agricultural Science, Haikou, 571101, P. R. China.
College of Pharmacy, Guangdong Pharmaceutical University, Guangzhou, Guangdong, 510006, P. R. China.
Chem Biodivers. 2018 May;15(5):e1800059. doi: 10.1002/cbdv.201800059. Epub 2018 Apr 29.
The synthesis of celastrol analogues containing amino acid ester at the C(29) position and their evaluation for cytotoxic activities in vitro were reported. The MTT test showed that a set of derivatives with lower IC values than that of the positive control group cisplatin and the parent compound celastrol, which exhibited greater antiproliferative activities. The most potent title compounds 2a and 2e exhibited cytotoxic activities in vitro against HeLa and A549 cell lines with IC values of 0.371 and 0.237 μm, 0.235 and 0.109 μm, respectively. The apoptosis assay demonstrated that 2a and 2e can induces of A549 cell apoptosis in low concentrations. These results showed that 2a and 2e may be promising for further research as antitumor agents.
报道了在C(29)位含有氨基酸酯的雷公藤红素类似物的合成及其体外细胞毒活性评价。MTT试验表明，一组衍生物的IC值低于阳性对照组顺铂和母体化合物雷公藤红素，表现出更强的抗增殖活性。最有效的目标化合物2a和2e在体外对HeLa和A549细胞系表现出细胞毒活性，IC值分别为0.371和0.237μm、0.235和0.109μm。凋亡试验表明，2a和2e在低浓度下可诱导A549细胞凋亡。这些结果表明，2a和2e作为抗肿瘤药物可能具有进一步研究的前景。
