Selective induction of cell death in cancer cells by gallic acid.
Gallic acid (3,4,5-trihydroxybenzoic acid) is a naturally occurring plant phenol obtained by the hydrolysis of tannins and is know to show some pharmacological activities. In screening anti-cancer agents in traditional Chinese medicines, gallic acid was found to show cytotoxicity against all cancer cells that we examined in this study (IC50s: 4.8-13.2 micrograms/ml). Gallic acid was found to show cytotoxicity against primary cultured rat hepatocytes and macrophages, and lesser cytotoxicity against fibroblasts and endothelial cells. Cell death in dRLh-84 cells occurred within 6h after gallic acid treatment at a concentration of more than 20 micrograms/ml. A study of structurally related compounds suggested that the cytotoxicity shown by gallic acid was not a common feature in phenolic compounds, but was a fairly specific characteristic of gallic acid. That is, three adjacent phenolic hydroxyl groups of gallic acid were responsible for the cytotoxicity, and the carboxyl group was not responsible, but seemed to be implicated in distinguishing between normal cells and cancer cells.
Inoue
M
M
Department of Pharmacognosy, Faculty of Pharmaceutical Sciences, Nagoya City University, Japan.
Suzuki
R
R
Sakaguchi
N
N
Li
Z
Z
Takeda
T
T
Ogihara
Y
Y
Jiang
B Y
BY
Chen
Y
Y
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology*; D000975:Antioxidants / Q000494:pharmacology; D016923:Cell Death / Q000187:drug effects*; D004354:Drug Screening Assays, Antitumor; D005707:Gallic Acid / Q000494:pharmacology*; D006801:Humans; D051379:Mice; D010946:Plants, Medicinal / Q000737:chemistry; D051381:Rats; D014407:Tumor Cells, Cultured
D000972:Antineoplastic Agents, Phytogenic; D000975:Antioxidants; D005707:Gallic Acid