Chasserot-Golaz S, Flaig C, Beck G
Cancer Biochem Biophys. 1985 Dec;8(2):95-101.
The metabolism of the potent antagonist RU38486 has been studied in cultured liver cells and in two hepatoma cell lines. In the liver cells, this steroid undergoes a rapid degradation, whereas in hepatoma cells grown in similar conditions only a minor degradation occurs. Moreover the rate of degradation is much higher for the antagonist steroid than for the agonist steroid tested, dexamethasone. The high antiglucocorticoid potency and the relative instability of the RU38486 molecule are very important to define its different effects and its mechanism of action in liver and in liver derived tumor cells. RU38486 may represent a useful drug in cancerotherapy.
强效拮抗剂RU38486的代谢已在培养的肝细胞和两种肝癌细胞系中进行了研究。在肝细胞中，这种甾体迅速降解，而在相似条件下生长的肝癌细胞中，仅发生少量降解。此外，与所测试的激动剂甾体地塞米松相比，拮抗剂甾体的降解速率要高得多。RU38486的高抗糖皮质激素效力和相对不稳定性对于确定其在肝脏和肝源性肿瘤细胞中的不同作用及其作用机制非常重要。RU38486可能是癌症治疗中的一种有用药物。
