Mauvais-Jarvis P, Gompel A, Malet C, Kuttenn F
Service de Médecine de la Reproduction, Hôpital Necker, Paris.
Ann Endocrinol (Paris). 1989;50(3):181-8.
Steroidal (progestins) and non steroidal antiestrogens (tamoxifen and derivatives) are strong antiproliferative molecules when added to normal human breast cells in culture. The antiproliferative action of tamoxifen and 4-hydroxytamoxifen isomers is comparable to that observed in cultured breast cell lines. The progestin promegestone (R 5020) is a strong antiproliferative agent in the presence as well as in the absence of estradiol. Identically, at higher concentration the antiprogestin RU 486 slows down cell proliferation probably due to its progesterone agonist activity. Both progestins and antiprogestins stimulate 17 beta-hydroxysteroid dehydrogenase activity, a marker of progesterone receptor but only in estradiol primed cells.
甾体类(孕激素)和非甾体类抗雌激素药物(他莫昔芬及其衍生物)在添加到培养的正常人乳腺细胞中时是强效抗增殖分子。他莫昔芬和4-羟基他莫昔芬异构体的抗增殖作用与在培养的乳腺细胞系中观察到的作用相当。孕激素普美孕酮(R 5020)在有或没有雌二醇存在的情况下都是一种强效抗增殖剂。同样,在较高浓度下,抗孕激素RU 486可能由于其孕激素激动剂活性而减缓细胞增殖。孕激素和抗孕激素都能刺激17β-羟基类固醇脱氢酶活性,这是孕激素受体的一个标志物,但仅在经雌二醇预处理的细胞中如此。