Anti-proliferative metabolites from the root of calophyllum inophyllum L.

Abstract

This study aimed to isolate secondary metabolites from the root of C. inophyllum L. and to evaluate their anti-proliferative activities against hepatocellular carcinoma and colorectal cancer cells. Chromatographic fractionation of the n-hexane and ethyl acetate crude extracts led to the isolation of two new (1 and 2) and twelve known xanthones (3-14). In addition, metabolites 4, 6 and 8 were isolated from the genus Calophyllum for the first time. All metabolites were evaluated for their anti-proliferative activity against Hep-G2 and HCT-116 cell lines. Metabolites 5 and 14 showed the most active metabolites against both cancer cells, as well as they displayed strong activities toward HCT-116 with the same IC50 value of 3.04 µM. Moreover, both of them exhibited potent activities against Hep-G2 with IC50 values of 6.07 and 5.94 µM, respectively. Further, metabolite 14 was subjected to western blot analysis to study its mechanism of action against Hep-G2 cells. The result demonstrated that 14 induced apoptosis in a concentration-dependent manner by the down-regulation of the expression of both Bcl-2 and Bcl-XL proteins.