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

Dereplication of cytotoxic compounds from different parts of Sophora pachycarpa

Sophora pachycarpa Schrenk ex C.A.Mey. is an annual plant belonging to the family Fabaceae. The cytotoxic activities of methanol-dichloromethane extracts (1:1) of different parts of S. pachycarpa were investigated on DU145 (prostate cancer cell line) and MCF-7 (breast cancer cell line) cell lines. The root extract of S. pachycarpa was the only extract that showed significant cytotoxic activity with IC50 values of 39.88 and 16.49 μg/mL on DU145 and MCF-7 cell lines, respectively. The root extract was then subjected to RP-HPLC for further fractionations. Among the isolated fractions from root extract, only one of them had remarkable cytotoxic effects with IC50 value of 26.43 on MCF-7 and 7.54 μg/mL on DU145 cell lines. Further purification led to isolation of a compound with IC50 values of 5.44 and 2.44 μg/mL on MCF-7 and DU145 cell lines, respectively. Based on 1H NMR and 13C NMR spectra, together with LC-MS, the structure of the purified compound was assigned as the flavonostilbene alopecurone A.No Full Tex