Falke H E, Degenhart H J, Abeln G J, Visser H K
Mol Cell Endocrinol. 1976 Jan;4(2):107-14. doi: 10.1016/0303-7207(76)90030-7.
The production of corticosterone from 25-hydroxycholesterol by isolated rat adrenal cells is inhibited by aminoglutethimide phosphate (AGI); half-maximal inhibition is obtained at ca. 10 muM. AGI also inhibits ACTH-stimulated steroid production from endogeneous substrates; here half-maximal inhibition is obtained with ca. 40 muM AGI. In the presence of ACTH + AGI, 25-hydroxycholesterol causes additive inhibition. This effect of 25-hydroxycholesterol is dose-dependent. ACTH-stimulated steroid production from endogeneous substrates is partially inhibited by 5-cholene-3 beta,24-diol. These results may just reflect substrate competition for the side-chain cleaving system or may be due to some seocndary toxic effect on the cells.
磷酸氨鲁米特(AGI)可抑制离体大鼠肾上腺细胞从25-羟胆固醇生成皮质酮;在约10μM时可获得半数最大抑制作用。AGI还可抑制促肾上腺皮质激素(ACTH)刺激的内源性底物类固醇生成;此处约40μM AGI可获得半数最大抑制作用。在ACTH + AGI存在的情况下,25-羟胆固醇会产生累加抑制作用。25-羟胆固醇的这种作用具有剂量依赖性。5-胆烯-3β,24-二醇可部分抑制ACTH刺激的内源性底物类固醇生成。这些结果可能仅反映了底物对侧链裂解系统的竞争,也可能是由于对细胞的某些继发性毒性作用所致。