Portal de Periódicos da CAPES

Inhibitory Activities of (-)-Epigallocatechin-3-O-gallate against Topoisomerases I and II.

2001; Pharmaceutical Society of Japan; Volume: 24; Issue: 9 Linguagem: Inglês

10.1248/bpb.24.1088

1347-5215

Keitarou Suzuki, Shoji Yahara, Fumio Hashimoto, Masaru Uyeda,

Synthesis and biological activity

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.