醋酸棉酚和15甲基PGF2α甲酯对大鼠子宫胞浆雌激素受体的影响

假孕大鼠口服醋酸棉酚40和80 mg/kg连续5天,平均每个子宫的胞浆蛋白和雌激素受体量明显减少。以每mg蛋白计,雌激素受体浓度同对照组差异不显著。幼大鼠口服醋酸棉酚40mg/kg连续8天,作饱和分析测得对照组和给药组K_d值分别为1.04×10^-10和1.09×10^-10mol。最大受体结合数分别为432.0和358.8 fmol/子宫。实验发现棉酚在高浓度时对³H-雌二醇同其受体的结合有抑制作用。15甲基PGF_2α甲酯对假孕大鼠子宫胞浆蛋白水平和雌激素受体均无明显影响。

Effect of gossypol acetic acid (GAA) and 15-methyl PGF2 alpha-methyl ester (PG05) on estrogen receptors of rat uteri

Treatment of pseudopregnant rats with GAA at the dosage of 40 or 80 mg/kg for 5 days caused a decrease of cytoplasmic protein and estrogen receptor level per uterus, even though the estrogen receptor concentration per mg protein did not show significant change between the control and treated animals.Saturation analysis showed that in immature rats GAA at 40 mg/kg for 8 days reduced the amount of estrogen receptor per uterus. Bmax in the control and treated groups Was found by Scatchard analysis to be 432.0 and 358.8 fmol/uterus respectively. Kd was calculated to be 1.04×10^-10 and 1.09×10^-10 mol respectively.The IC₅₀ of GAA was shown to be 7.0 × 10^-5 mol indicating that GAA at high concentrations was capable of inhibiting the binding of ³H-estradiol with the receptor.PG 05,however, was found to have no effect on the level of protein and estrogen receptor per uterus or per mg protein.