Antitumor effect of resorcinol derivatives from the roots of Ardisia brevicaulis by inducing apoptosis.

Two new resorcinol derivatives 2-methoxy-4-hydroxy-6-(8Z-pentadecenyl)-benzene-1-O-acetate (1) and 2-methoxy-4-hydroxy-6-pentadecyl-benzene-1-O-acetate (2), together with four known compounds 2-methoxy-4-hydroxy-6-tridecyl-benzene-1-O-acetate (ardisiphenol D, 3), 5-(8Z-pentadecenyl)resorcinol (4), 5-pentadecylresorcinol (5), 5-tridecylresorcinol (6), have been isolated from the roots of Ardisia brevicaulis in our previous work. In the present study, the inhibitory effect of 1-6 on the proliferation of human pancreatic PANC-1, human lung A549, human gastrointestinal carcinoma SGC 7901, human breast MCF-7, and human prostate PC-3 cancer cells was evaluated by the methyl thiazolyl tetrazolium method. Compounds 1-6 all showed inhibitory activities against the proliferation of PANC-1, A549, SGC7901, MCF-7, and PC-3 cancer cells. Compound 3, the most active agent and the main constituent with the highest yield, induced apoptosis of PANC-1 cells (the most sensitive cell line among the cell lines screened) via the activation of caspase-3 and caspase-9, up-regulation of the ratio of bax/bcl-2 protein expression.