Inhibitory activities of (-)-epigallocatechin-3-O-gallate against topoisomerases I and II.
The substitution of gallic acid at the 3 position of (-)-epigallocatechin-3-O-gallate (EGCG) increased the inhibition against topoisomerase I from calf thymus gland and topoisomerase II from human placenta, and the substitution of a hydroxyl group at the 3' position increased the inhibition against the topoisomerase I. These results suggested that the 3 and 3' positions of the EGCG molecule play important roles in the process of inhibition of topoisomerases I and II. EGCG showed strong inhibition against topoisomerases I from wheat germ, calf thymus gland and Vero cells, and showed weak or no inhibition against topoisomerases I from carcinoma cells such as A549, HeLa and COLO 201 cells. EGCG differentially inhibited the topoisomerases I from different sources.
Suzuki
K
K
Faculty of Pharmaceutical Sciences, Kumamoto University, Japan.
Yahara
S
S
Hashimoto
F
F
Uyeda
M
M
D000818:Animals; D002392:Catechin / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*; D002417:Cattle; D004264:DNA Topoisomerases, Type I / Q000737:chemistry; D004250:DNA Topoisomerases, Type II / Q000737:chemistry; D004278:DNA, Superhelical / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D013329:Structure-Activity Relationship; D013662:Tea / Q000737:chemistry; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors
D004278:DNA, Superhelical; D004791:Enzyme Inhibitors; D013662:Tea; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors; D002392:Catechin; C045651:epigallocatechin gallate; D004264:DNA Topoisomerases, Type I; D004250:DNA Topoisomerases, Type II