Staples L D, Heap R B, Brown D, Marrs R W
Steroids. 1984 Nov;44(5):419-33. doi: 10.1016/s0039-128x(84)80002-1.
The inhibitory effects of different steroids and related compounds on sheep peripheral blood lymphocytes (PBL) during exposure to the mitogen, phytohemagglutinin (PHA), have been measured by the reduction of [3H]thymidine incorporation into DNA. Dose-response curves showed that a maximum (or near maximum effect) was achieved at a steroid concentration of 12.5 microM. At this dose 19 of 41 compounds significantly reduced thymidine incorporation by activated PBL (P less than 0.01 to P less than 0.001). The greatest reduction was observed with 17-hydroxyprogesterone (-59%, i.e. reduced by 59% compared with vehicle control, 100%) greater than androstenedione greater than epitestosterone greater than estradiol-3-methyl ether greater than 20 alpha-dihydroprogesterone greater than medroxyprogesterone acetate greater than 5 beta-pregnane-3,20-dione greater than 5 alpha-pregnane-3,20-dione (-24%). Among the steroids which showed the greatest inhibitory effect, 6 had a 4-en-3-one group in ring A, 4 had a saturated ring A (pregnane or androstane) and one had a 3-methyl ether group and a phenolic ring A. The wide range of structures represented by these inhibitory steroids suggests that inhibition of lymphocyte mitogenesis involves more than one mechanism.
通过测量[³H]胸苷掺入DNA的减少量，已测定了不同类固醇及相关化合物在有丝分裂原植物血凝素（PHA）存在的情况下对绵羊外周血淋巴细胞（PBL）的抑制作用。剂量反应曲线表明，在类固醇浓度为12.5微摩尔时达到最大（或接近最大）效应。在此剂量下，41种化合物中的19种显著降低了活化PBL的胸苷掺入量（P小于0.01至P小于0.001）。观察到17-羟孕酮的抑制作用最大（-59%，即与溶剂对照相比减少了59%，溶剂对照为100%），大于雄烯二酮大于表睾酮大于雌二醇-3-甲醚大于20α-二氢孕酮大于醋酸甲羟孕酮大于5β-孕烷-3,20-二酮大于5α-孕烷-3,20-二酮（-24%）。在显示出最大抑制作用的类固醇中，6种在A环中有一个4-烯-3-酮基团，4种有饱和的A环（孕烷或雄烷），1种有一个3-甲醚基团和一个酚性A环。这些具有抑制作用的类固醇所代表的结构范围很广，这表明淋巴细胞有丝分裂的抑制涉及多种机制。
