DNA topoisomerases i and II inhibitory activity and cytotoxicity of compounds from the stems of Parthenocissus tricuspidata

Abstract

Activity-directed isolation of the methylene chloride fraction from the stems of Parthenocissus tricuspidata have led to the identification of two new compounds (1-2): 1-(2′,3′,5′-trihydroxyphenyl)-2-(4″- hydroxyphenyl)-ethane-1,2-(E)-epoxide (1, tricuspidatin A) and erythro-1-(3′,5′-dihydroxyphenyl)-2-(4″-hydroxyphenyl) -ethane-1,2-diol (2, tricuspidatin B), together with four known compounds (3-6): β-sitosterol (3), nonacosan-1-ol (4), 3-(4-hydroxy-3-methoxyphenyl)-2- propenoic acid hexacosyl ester (5) and betulinic acid (6). Their chemical structures were elucidated based on spectroscopic (IR, UV, MS, 1D and 2D NMR) and physicochemical analyses. Compounds 1 and 2 showed strong DNA topoisomerase II inhibitory activity at both concentrations of 20 and 100 μM. In addition, 3 exhibited strong cytotoxic activity against the HT-29 and HepG2 cancer cell lines, and 6 showed strong cytotoxicity against the HT-29 and MCF-7 ones.