三苯乙烯衍生物及具有甾体骨架的化合物对人和大鼠肝脏抗雌激素结合位点（AEBS）的物种特异性。

Species specificity of triphenylethylene derivatives and of compounds with a steroidal backbone for human and rat liver antioestrogen binding site (AEBS).

作者信息

van den Koedijk C D, Govers R M, Thijssen J H, Blankenstein M A

机构信息

Faculty of Pharmacy, Utrecht University, The Netherlands.

出版信息

Biochem Pharmacol. 1993 Nov 17;46(10):1870-2. doi: 10.1016/0006-2952(93)90597-p.

DOI:10.1016/0006-2952(93)90597-p

PMID:8250976

Abstract

The binding affinity of derivatives of the triphenylethylene (TPE) antioestrogen tamoxifen and of steroidal compounds for human liver antioestrogen binding sites (AEBS) was compared with their binding affinity for rat liver AEBS. Despite the observation of some quantitative differences overall a highly significant correlation between the relative binding affinity (RBA) for human and rat liver AEBS was found for all compounds tested (r = 0.93, N = 19, P < 0.001). This was more pronounced for TPE derivatives (r = 0.83, N = 12, P < 0.01) than for cholesterol derived compounds (r = 0.64, N = 7, not significant). We conclude that AEBS from rat liver can be used instead of human livers as a model to study the interactions of antioestrogens with AEBS.

摘要

将三苯乙烯（TPE）抗雌激素他莫昔芬的衍生物以及甾体化合物与人肝抗雌激素结合位点（AEBS）的结合亲和力，与其对大鼠肝AEBS的结合亲和力进行了比较。尽管总体上观察到了一些数量差异，但对于所有测试化合物，人肝和大鼠肝AEBS的相对结合亲和力（RBA）之间发现了高度显著的相关性（r = 0.93，N = 19，P < 0.001）。这在TPE衍生物中（r = 0.83，N = 12，P < 0.01）比在胆固醇衍生化合物中（r = 0.64，N = 7，不显著）更为明显。我们得出结论，大鼠肝的AEBS可替代人肝作为模型来研究抗雌激素与AEBS的相互作用。