Cytotoxicity of estradiol, equilin, equilenin, and their derivatives on Chinese hamster V79 cells.
Recently, we investigated the inhibitory effects of 17 beta-estradiol and diethylstilbestrol on microtubule assembly, cytotoxicity, and aneuploidy in V79 cells. The present study analyzes the effects of equilin and equilenin (amongst the natural estrogens originally isolated from the urine of pregnant horses) and their related compounds, on the relative plating efficiency of Chinese hamster V79 cells. The results showed that a hydroxyl group on 17-C and a methoxyl group on 3-C of the estrogen skeleton were important for cytotoxicity. Of the various compounds analyzed, 2-methoxyestradiol had the strongest cytotoxicity, suggesting also the importance of a methoxyl group on 2-C.
Oda
Taiko
T
Kyoritsu College of Pharmacy, Shibakoen 1-chome, Minato-ku, Tokyo 105-8512, Japan. Oda-ti@kyoritsu-ph.ac.jp
Ikeda
Noriko
N
Nakashima
Shoko
S
Sato
Yoshihiro
Y
D000077584:2-Methoxyestradiol; D000818:Animals; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D006224:Cricetinae; D004305:Dose-Response Relationship, Drug; D004855:Equilenin / Q000737:chemistry / Q000633:toxicity*; D004857:Equilin / Q000737:chemistry / Q000633:toxicity*; D004958:Estradiol / Q000031:analogs & derivatives* / Q000737:chemistry / Q000633:toxicity*; D004970:Estrone / Q000633:toxicity; D013329:Structure-Activity Relationship; D018675:Toxicity Tests
D004857:Equilin; D004970:Estrone; D004958:Estradiol; D000077584:2-Methoxyestradiol; D004855:Equilenin