Gallic acid (3,4,5-trihydroxybenzoic acid) is a naturally occurring pl
ant phenol obtained by the hydrolysis of tannins and is known to show
some pharmacological activities. In screening anti-cancer agents in tr
aditional Chinese medicines, gallic acid,vas found to show cytotoxicit
y against all cancer cells that we examined in this study (IC(50)s: 4.
8-13.2 mu g/ml). Gallic acid, however, showed no cytotoxicity against
primary cultured rat hepatocytes and macrophages, and lesser cytotoxic
ity against fibroblasts and endothelial cells. Cell death in dRLh-84 c
ells occurred within 6 h after gallic acid treatment at a concentratio
n of more than 20 mu g/ml. A study of structurally related compounds s
uggested that the cytotoxicity shown by gallic acid was not a common f
eature in phenolic compounds, but was a fairly specific characteristic
of gallic acid. That is, three adjacent phenolic hydroxyl groups of g
allic acid were responsible for the cytotoxicity, and the carboxyl gro
up was not responsible, but seemed to be implicated in distinguishing
between normal cells and cancer cells,