己烯雌酚与子宫核雌激素受体的相对结合亲和力：血清和血清白蛋白的影响

The relative binding affinity of diethylstilbestrol to uterine nuclear estrogen receptor: effect of serum and serum albumin.

作者信息

Okulicz W C, Johnson L D

出版信息

Proc Soc Exp Biol Med. 1987 Sep;185(4):478-83. doi: 10.3181/00379727-185-42573.

Abstract

The relative binding affinity (RBA) of diethylstilbestrol (DES) was determined in nuclear fractions of the rat uterus. DES displayed a two- to threefold greater affinity (RBA = 245 +/- 36) than estradiol (RBA = 100) for nuclear E receptor. The RBA of DES to nuclear E receptor was lowered significantly in the presence of rat serum (43 +/- 1) or human serum (52 +/- 7). Dilution of human serum resulted in a progressive increase in the RBA of DES which approached that observed in the absence of serum. Addition of purified human serum albumin mimicked the decrease in RBA of DES that was observed with serum. The IC50 of estradiol was not changed in the presence of either rat serum or albumin. These data show that DES possesses a greater affinity for nuclear E receptor than estradiol and that serum albumin can modulate DES binding to uterine E receptor.

摘要

在大鼠子宫的细胞核组分中测定了己烯雌酚（DES）的相对结合亲和力（RBA）。与雌二醇（RBA = 100）相比，DES对细胞核雌激素受体的亲和力高两到三倍（RBA = 245±36）。在存在大鼠血清（43±1）或人血清（52±7）的情况下，DES与细胞核雌激素受体的RBA显著降低。人血清的稀释导致DES的RBA逐渐增加，接近在无血清情况下观察到的数值。添加纯化的人血清白蛋白模拟了血清中观察到的DES的RBA降低。在存在大鼠血清或白蛋白的情况下，雌二醇的IC50没有变化。这些数据表明，DES对细胞核雌激素受体的亲和力高于雌二醇，并且血清白蛋白可以调节DES与子宫雌激素受体的结合。