Sato Y, Murai T, Oda T, Saitô H, Kodama M, Hirata A
Biochemistry Division, Kyoritsu College of Pharmacy, Tokyo.
J Biochem. 1987 May;101(5):1247-52. doi: 10.1093/oxfordjournals.jbchem.a121988.
Dienestrol, meso-hexestrol, and dl-hexestrol, synthetic nonsteroidal estrogens, were shown to be inhibitors of microtubule assembly in vitro using microtubule proteins isolated from porcine brains. The order of activity of the synthetic estrogens as inhibitors of microtubule assembly is: dienestrol greater than diethylstilbestrol greater than meso-hexestrol greater than dl-hexestrol greater than isodienestrol. The activity of dienestrol as an inhibitor was of the same order as that of (+)-griseofulvin, as determined by turbidity measurement. Electron microscopic observation revealed that twisted ribbon structures are formed from microtubule proteins in the presence of some synthetic estrogens (dienestrol, meso-hexestrol, and dl-hexestrol).
已证明，合成的非甾体雌激素己二烯雌酚、内消旋己烯雌酚和消旋己烯雌酚，在体外使用从猪脑分离的微管蛋白时，是微管组装的抑制剂。这些合成雌激素作为微管组装抑制剂的活性顺序为：己二烯雌酚＞己烯雌酚＞内消旋己烯雌酚＞消旋己烯雌酚＞异己二烯雌酚。通过浊度测量确定，己二烯雌酚作为抑制剂的活性与（+）-灰黄霉素的活性处于同一水平。电子显微镜观察显示，在某些合成雌激素（己二烯雌酚、内消旋己烯雌酚和消旋己烯雌酚）存在的情况下，微管蛋白会形成扭曲的带状结构。
