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）及桦木酸（betulinic acid）等天然甾体与三萜类化合物（natural steroids and triterpenes）转化为其己酸酯与油酸酯衍生物，以考察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[OVCAR-8（卵巢癌）、SF-295（胶质母细胞瘤）、HCT-116（结肠腺癌）、HL-60（白血病）及PC-3（前列腺癌）]对所得衍生物进行了活性评估，结果显示仅桦木酸己酯（betulinic acid hexyl ester）展现出潜在的细胞毒活性。