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Antiestrogenic activity of vitamin A in in vivo uterotrophic assay.

机译:体内子宫营养试验中维生素A的抗雌激素活性。

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摘要

All-trans-retinoic acid (ATRA), the primary active metabolite of vitamin A, was examined for its antiestrogenic activity in rats using an in vivo uterotrophic assay. All rats were ovariectomized 2 weeks prior to receiving 5 mg/kg/day ATRA or 0.3 micro g/kg/day ethynyl estradiol (EE) subcutaneously once a day for 3 consecutive days. Rats were sacrificed 1, 3, 6, 12 or 24 h after the last treatment. EE increased uterine weight and the coinjection of ATRA with EE significantly suppressed this effect 3 and 24 h after treatment. mRNA expression was examined during this 24-h period and the mRNA expression levels of estrogen receptor alpha (ER alpha), retinoic acid receptor beta (RAR beta), retinoid X receptor gamma (RXR gamma) and cellular retinol-binding protein I (CRBP I) were found to have significantly increased in the ATRA+EE group compared with those in the EE group. This is the first report on the antiestrogenic activity of ATRA determined using an in vivo adult rat uterotrophic assay. The up-regulation of RAR or RXR mRNA expression level was probably responsible for the antiestrogenic activity of ATRA.
机译:使用体内子宫营养测定法检查了维生素A的主要活性代谢物全反式维甲酸(ATRA)的抗雌激素活性。在连续3天每天皮下接受5 mg / kg /天ATRA或0.3 micro g / kg /天乙炔基雌二醇(EE)之前2周,将所有大鼠卵巢切除。最后一次治疗后1、3、6、12或24小时处死大鼠。 EE增加了子宫重量,ATRA与EE共同注射在治疗后3和24 h显着抑制了这种作用。在这24小时内检查mRNA表达,并检测雌激素受体α(ER alpha),视黄酸受体beta(RAR beta),类视色素X受体γ(RXRγ)和细胞视黄醇结合蛋白I(CRBP)的mRNA表达水平与EE组相比,ATRA + EE组的I)明显增加。这是关于使用体内成年大鼠子宫营养测定法测定的ATRA抗雌激素活性的首次报道。 RAR或RXR mRNA表达水平的上调可能与ATRA的抗雌激素活性有关。

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