Terada N, Oka T
Horm Metab Res. 1983 Oct;15(10):508-12. doi: 10.1055/s-2007-1018770.
Cortisol 21-mesylate, an alkylating derivatives of cortisol, was previously shown to exert an anti-glucocorticoid action in rat hepatoma cell culture (Simons, Thompson and Johnson 1980). In this study the effect of cortisol 21-mesylate on milk protein synthesis induced in cultured mouse mammary gland by glucocorticoid, insulin, and prolactin was investigated. Addition of cortisol 21-mesylate at concentrations ranging from 10(-8) M to 10(-6) M produced no inhibition of casein synthesis that was induced by glucocorticoid, insulin and prolactin in mammary explants from midpregnant mice. On the other hand, cortisol 21-mesylate in combination with insulin and prolactin stimulated casein synthesis in cultured tissue. The potency of cortisol mesylate was about 1/10 to 1/30th of that of cortisol. Cortisol 21-mesylate, like cortisol, also augmented the accumulation of alpha-lactalbumin in midpregnant rat mammary tissue cultured in the presence of insulin and prolactin. A cell-free competition study of glucocorticoid receptors using cytoplasmic extracts from mouse mammary tissue showed that cortisol 21-mesylate competitively inhibited the binding of dexamethasone on glucocorticoid receptors. The apparent affinity of cortisol 21-mesylate for glucocorticoid receptors is about 1/10th of that of cortisol. These results indicate that cortisol 21-mesylate acts as a glucocorticoid but not as an antiglucocorticoid in the mammary gland.
21-甲磺酸皮质醇是皮质醇的一种烷基化衍生物，先前已证明其在大鼠肝癌细胞培养中具有抗糖皮质激素作用（西蒙斯、汤普森和约翰逊，1980年）。在本研究中，研究了21-甲磺酸皮质醇对糖皮质激素、胰岛素和催乳素诱导的培养小鼠乳腺中乳蛋白合成的影响。添加浓度范围为10^(-8) M至10^(-6) M的21-甲磺酸皮质醇，对妊娠中期小鼠乳腺外植体中由糖皮质激素、胰岛素和催乳素诱导的酪蛋白合成没有抑制作用。另一方面，21-甲磺酸皮质醇与胰岛素和催乳素联合使用可刺激培养组织中的酪蛋白合成。甲磺酸皮质醇的效力约为皮质醇的1/10至1/30。与皮质醇一样，21-甲磺酸皮质醇也增加了在胰岛素和催乳素存在下培养的妊娠中期大鼠乳腺组织中α-乳白蛋白的积累。使用小鼠乳腺组织的细胞质提取物进行的糖皮质激素受体无细胞竞争研究表明，21-甲磺酸皮质醇竞争性抑制地塞米松与糖皮质激素受体的结合。21-甲磺酸皮质醇对糖皮质激素受体的表观亲和力约为皮质醇的1/10。这些结果表明，21-甲磺酸皮质醇在乳腺中起糖皮质激素的作用，而不是抗糖皮质激素的作用。
