柔荑软珊瑚Nephthea sp.中两种具有细胞毒活性的甾醇化合物

Two Cytotoxic Sterols from the Soft Coral Nephthea sp.

采用抗肿瘤活性追踪法对采自中国南海西沙群岛永兴岛柔荑软珊瑚Nephthea sp.中抗肿瘤活性成分进行研究,报道了两种具有细胞毒活性的甾醇化合物,经过MS,IR,1H NMR,13C NMR(DEPT),HSQC和HMBC等光谱技术鉴定为:24-甲基胆甾-5-烯-3β,8β-二醇(1)和24-亚甲基胆甾-4-烯-3β,6β-二醇(2),化合物1为新化合物,利用X-ray单晶衍射技术验证化合物2的立体结构.化合物1对肝癌细胞(BEL-7402),小鼠白血瘤细胞(P388)和人结肠癌细胞(LOVO)作用的IC50值分别为18.0,25.5和20.6μg/mL;化合物2对肿瘤细胞P388和人乳腺癌细胞(MCF)作用的IC50值分别为1.0和2.5μg/mL.

Two cytotoxic sterols have been isolated from Nephthea sp. collected from Xisha islands of the South China Sea by bioassay-guided isolation. Their structures were established as 24-methylcholestan-5- ene-3β,8β-diol （1） and 24-methylenecholestan-4-ene-3β,6β-diol （2） by MS, IR, ^1H NMR, ^13C NMR （DEPT）, HSQC and HMBC analysis. Sterol 1 is a previously unknown compound and the stereochemistry of sterol 2 has been validated by X-ray diffraction analysis for the first time. Sterol 1 exhibited cytotoxicity against BEL-7402, P388 and LOVO cells （IC50 18.0, 25.5 and 20.6 μg/mL, respectively）. Sterol 2 also showed significant cytotoxicity against P388 and MCF cells （IC50 1.0 and 2.5 μg/mL, respectively）.