Ianicello C M, Okey A B
Oncology. 1976;33(5-6):225-8. doi: 10.1159/000225151.
A single oral carcinogenic (20 mg) dose of 7,12-dimethylbenz(a)anthracene (DMBA) significantly reduced the uterine nuclear uptake of estrogen-receptor complex with immature Sprague-Dawley rats were injected with 0.05 microng of tritiated estradiol-17beta (E2) 24 hours after DMBA. Incubation experiments with whole uteri or with isolated uterine nuclei showed that DMBA in vitro does not act by reducing estrogen-receptor transformation or transport into nuclei. DMBA may act in vivo by stimulating hepatic degradation of injected estradiol-17beta so that less active form of the steroid reaches target tissues.
给未成熟的斯普拉格-道利大鼠口服单剂量致癌的7,12-二甲基苯并(a)蒽(DMBA,20毫克),在给予DMBA 24小时后注射0.05微克氚标记的雌二醇-17β(E2),可显著降低子宫核内雌激素受体复合物的摄取。对整个子宫或分离出的子宫核进行的孵育实验表明,DMBA在体外并不会通过减少雌激素受体转化或转运至细胞核来发挥作用。DMBA在体内可能通过刺激肝脏对注射的雌二醇-17β进行降解,从而使活性较低的类固醇形式到达靶组织来发挥作用。