Woodfruticosin (woodfordin C), a new inhibitor of DNA topoisomerase II. Experimental antitumor activity.
Woodfruticosin (woodfordin C) (WFC), a new inhibitor of DNA topoisomerase II (topo-II), was isolated from methanol extract of Woodfordia fruticosa Kurz (Lythraceae) and studied for in vitro and in vivo antitumor activities in comparison with Adriamycin (ADR) and etoposide (ETP), well known inhibitors of topo-II. The inhibitory activity against DNA topo-II shown by WFC was much stronger than that shown by ETP or ADR. WFC inhibited strongly intracellular DNA synthesis but not RNA and protein synthesis. On the other hand, WFC had a weaker growth inhibitory activity against various human tumor cells than ETP or ADR, but it showed remarkable activity against PC-1 cells and moderate activity against MKN45 and KB cells. Furthermore, WFC had in vivo growth inhibitory activity against s.c. inoculated colon38. These results indicate that the mechanism by which WFC exhibits antitumor activity may be through inhibition of topo-II.
Kuramochi-Motegi
A
A
Research Laboratories, Pharmaceuticals Group, Nippon Kayaku Co., Tokyo, Japan.
Kuramochi
H
H
Kobayashi
F
F
Ekimoto
H
H
Takahashi
K
K
Kadota
S
S
Takamori
Y
Y
Kikuchi
T
T
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology*; D016923:Cell Death; D004317:Doxorubicin / Q000494:pharmacology; D005047:Etoposide / Q000494:pharmacology; D006367:HeLa Cells / Q000187:drug effects; D006801:Humans; D047348:Hydrolyzable Tannins; D007941:Leukemia P388 / Q000188:drug therapy; D051379:Mice; D009368:Neoplasm Transplantation; D013634:Tannins / Q000494:pharmacology*; D059005:Topoisomerase II Inhibitors
D000972:Antineoplastic Agents, Phytogenic; D047348:Hydrolyzable Tannins; D013634:Tannins; D059005:Topoisomerase II Inhibitors; C065469:woodfordin C; D005047:Etoposide; D004317:Doxorubicin