Terpene Esters from Natural Products: Synthesis and Evaluation of Cytotoxic Activity

ABSTRACT Natural steroids and triterpenes such as b-sitosterol, stigmasterol, lupeol, ursolic and betulinic acids were transformed into its hexanoic and oleic esters, to evaluate the influence of chemical modification towards the cytotoxic activities against tumor cells. The derivatives were evaluated against five tumor cell lines [OVCAR-8 (ovarian carcinoma); SF-295 (glioblastoma); HCT-116 (colon adenocarcinoma); HL-60 (leukemia); and PC-3 (prostate carcinoma)] and the results showed only betulinic acid hexyl ester exhibits cytotoxic potential activity.

摘要：本研究将β-谷甾醇（β-sitosterol）、豆甾醇（stigmasterol）、羽扇豆醇（lupeol）、熊果酸（ursolic acid）与白桦脂酸（betulinic acid）等天然甾族化合物与三萜类化合物，转化为己酸酯与油酸酯衍生物，以探究化学修饰对其抗肿瘤细胞毒活性的影响。研究针对五种肿瘤细胞系对所得衍生物开展活性评价，所涉细胞系包括OVCAR-8（卵巢癌，ovarian carcinoma）、SF-295（胶质母细胞瘤，glioblastoma）、HCT-116（结肠腺癌，colon adenocarcinoma）、HL-60（白血病，leukemia）以及PC-3（前列腺癌，prostate carcinoma）。实验结果表明，仅白桦脂酸己酯展现出潜在的细胞毒活性。