Morris D J, Brem A S
Am J Physiol. 1987 Mar;252(3 Pt 2):F365-73. doi: 10.1152/ajprenal.1987.252.3.F365.
Metabolism of aldosterone during the latent period prior to the action of the hormone may be of physiological importance. In the rat, liver metabolizes aldosterone in a sex-dependent manner; larger quantities of neutral polar and reduced aldosterone derivatives are found in male rat kidney; correlating with the larger physiological responses of male rats to aldosterone. The target tissues, mammalian kidney and toad urinary bladder, are also capable of metabolizing aldosterone in situ to neutral polar, 5 alpha- and 5 beta-reduced, and monosulfate derivatives. The 5 alpha-reduced metabolites possess significant antinatriuretic activity and are preferentially synthesized by rat kidney nuclei. The metabolic pathways leading to the synthesis of 5 alpha-reduced metabolites and their subsequent neutral polar derivatives appear to be regulated by dietary sodium and can be inhibited by antimineralocorticoids. At concentrations somewhat higher than aldosterone, these 5 alpha-reduced metabolites also can recreate the development of hypertension and suppress plasma renin activity in young adrenalectomized spontaneously hypertensive rats. Thus, several of the metabolically transformed aldosterone derivatives can be correlated with physiological regulation and/or expression of the actions of the hormone.
在激素发挥作用之前的潜伏期，醛固酮的代谢可能具有生理重要性。在大鼠中，肝脏以性别依赖的方式代谢醛固酮；在雄性大鼠肾脏中发现了更多量的中性极性和还原型醛固酮衍生物，这与雄性大鼠对醛固酮更大的生理反应相关。靶组织，即哺乳动物的肾脏和蟾蜍的膀胱，也能够在原位将醛固酮代谢为中性极性、5α-和5β-还原型以及单硫酸盐衍生物。5α-还原型代谢产物具有显著的抗利尿钠活性，并且优先由大鼠肾细胞核合成。导致5α-还原型代谢产物及其随后的中性极性衍生物合成的代谢途径似乎受膳食钠的调节，并且可以被抗盐皮质激素抑制。在略高于醛固酮的浓度下，这些5α-还原型代谢产物还可以在年轻的肾上腺切除自发高血压大鼠中重现高血压的发展并抑制血浆肾素活性。因此，几种经代谢转化的醛固酮衍生物可与激素作用的生理调节和/或表达相关联。
