Antitumor activity of phenylahistin in vitro and in vivo.
Phenylahistin is a new cell cycle inhibitor produced by Aspergillus ustus. Since phenylahistin was produced as a scalemic mixture of (-)-phenylahistin and its enantiomer, we separated each enantiomer and evaluated their antitumor activity in vitro. (-)-Phenylahistin exhibited antitumor activity against 8 tumor cell lines with IC50 values ranging from 1.8 x 10(-7) to 3.7 x 10(-6), while (+)-phenylahistin exhibited 33-100-fold less potent activity than (-)-phenylahistin did. (-)-Phenylahistin also showed antitumor activity against P388 leukemia and Lewis lung carcinoma cells in vivo.
Kanoh
K
K
Life Science Research Center, Advanced Technology Research Laboratories, Nippon Steel Corporation, Kawasaki, Japan. kanoh@LAB1.nsc.co.jp
Kohno
S
S
Katada
J
J
Hayashi
Y
Y
Muramatsu
M
M
Uno
I
I
D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000494:pharmacology*; D018827:Carcinoma, Lewis Lung / Q000188:drug therapy; D002453:Cell Cycle / Q000187:drug effects; D054659:Diketopiperazines; D007941:Leukemia P388 / Q000188:drug therapy; D008297:Male; D051379:Mice; D010879:Piperazines / Q000494:pharmacology*; D013237:Stereoisomerism; D014407:Tumor Cells, Cultured
D000903:Antibiotics, Antineoplastic; D054659:Diketopiperazines; D010879:Piperazines; C119340:phenylahistin