Wang N, Guan M, Zuo X
Institute of Materia Medica, Beijing.
Zhongguo Yi Xue Ke Xue Yuan Xue Bao. 1994 Jun;16(3):210-3.
Treatment with 15-methyl PGF2 alpha methyl ester (PG05) resulted in termination of pregnancy and peristatic effects in mice. (+) PG05 is the active stereoisomer of racemic PG05. The therapeutic index of (+) PG05 was found to be closely similar to that of (+/-) PG05. Pregnancy of ovariectomized rats given progesterone and estrone was maintained normally. PG05 was shown to have no effect on the gestation of ovariectomized rats receiving progesterone and estrone injection. PG05 at a concentration of 20 micrograms/ml reduced cAMP secretion of rat luteal cells in response to hCG in vitro. PG05 at concentration of 10 and 20 micrograms/ml also exerted an inhibitory effect on 8 Br-cAMP-stimulated progesterone production. These results suggest that in luteal cells PG05 inhibits steroidogenesis at the steps of gonadotropin-stimulated cAMP formation and cAMP-induced progesterone production.
用15-甲基前列腺素F2α甲酯(PG05)处理可导致小鼠妊娠终止和蠕动效应。(+)PG05是外消旋PG05的活性立体异构体。发现(+)PG05的治疗指数与(±)PG05的治疗指数非常相似。给予孕酮和雌酮的去卵巢大鼠的妊娠正常维持。结果表明,PG05对接受孕酮和雌酮注射的去卵巢大鼠的妊娠没有影响。浓度为20微克/毫升的PG05可降低体外培养的大鼠黄体细胞对人绒毛膜促性腺激素(hCG)反应时的环磷酸腺苷(cAMP)分泌。浓度为10和20微克/毫升的PG05也对8-溴环磷酸腺苷(8 Br-cAMP)刺激的孕酮产生有抑制作用。这些结果表明,在黄体细胞中,PG05在促性腺激素刺激的cAMP形成和cAMP诱导的孕酮产生步骤中抑制类固醇生成。