Nishino Y, Neumann F
Steroids. 1977 Aug;30(2):179-92. doi: 10.1016/0039-128x(77)90080-0.
The vaginotrophic and uterotrophic activities of 1-OH-8-alpha-E2 and its acetate in comparison with E2 and E3 were assessed on the basis of the effect on weights, water/fat-and RNA/DNA-contents of mouse vagina and uterus. The multiple doses of 8 alpha-steroids or E3 sufficient to achieve a maximal effect on the vagina were not enough to stimulate the uterus fully. At various periods of time after multiple injections, 1-OH-8 alpha-E2 acetate was found to have a higher vaginotrophic potency than the uterotrophic potency, when compared with E2 as a standard. The study on the time course of organ response to 8 alpha-steroids, E2 and E3 after a single injection of daily dose, being equipotent when injected one daily for 3 days, demonstrated that 1-OH-8-alpha-E2 and E3 were less vaginotrophic and uterotrophic than E2 and had a short duration of action. 1-OH-8 alpha-E2 acetate in comparison with E2 produced a long-lasting vaginotrophic effect and an early regressing uterotrophic effect. It can be confirmed that 8 alpha-steroids, like E3, are a special type of estrogen having a high vaginotrophic activity and a low uterotrophic activity.
基于对小鼠阴道和子宫重量、水/脂肪及RNA/DNA含量的影响,评估了1-OH-8-α-E2及其醋酸酯与E2和E3相比的促阴道营养和促子宫营养活性。对阴道产生最大效应的多剂量8α-类固醇或E3不足以充分刺激子宫。多次注射后的不同时间段,以E2为标准时,发现1-OH-8α-E2醋酸酯的促阴道营养效力高于促子宫营养效力。单次注射日剂量时,8α-类固醇、E2和E3在连续3天每日注射时等效,对其器官反应时间进程的研究表明,1-OH-8-α-E2和E3的促阴道营养和促子宫营养作用均低于E2,且作用持续时间较短。与E2相比,1-OH-8α-E2醋酸酯产生持久的促阴道营养作用和早期消退的促子宫营养作用。可以确认,8α-类固醇与E3一样,是一类具有高促阴道营养活性和低促子宫营养活性的特殊雌激素。