The 11 beta-OHSD inhibitor, carbenoxolone, enhances Na retention by aldosterone and 11-deoxycorticosterone.
The 11 beta-OHSD inhibitor, carbenoxolone, enhances Na retention by aldosterone and 11-deoxycorticosterone.
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11 β-OHSD 抑制剂卡苯索隆可通过醛固酮和 11-脱氧皮质酮增强钠保留。
DOI：
10.1152/ajprenal.1990.258.3.f756
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发表时间：
1990
期刊：
影响因子：
--
通讯作者：
Souness,GW
中科院分区：
文献类型：
--
作者：
Morris,DJ;Souness,GW
卡贝诺酮钠（CS）是一种与高血压和钠潴留相关的甘草衍生物，已被证明可抑制11 β -羟基类固醇脱氢酶，这种酶可将皮质醇和皮质酮代谢为它们各自的非活性11-脱氢产物（可的松和11-脱氢皮质酮）。有人提出，在11 β - ohsd抑制后，未代谢的皮质酮和皮质醇的生物利用度增加，使这些类固醇能够作用于肾矿化皮质激素受体，从而引发矿化皮质激素的作用。在这里，我们描述了CS如何增强醛固酮和脱氧皮质酮的抗尿钠活性；后一种类固醇尤其重要，因为它在类固醇环的C-11位置不具有羟基，这表明除了11 β - ohsd抑制外，还有另一种机制负责增强脱氧皮质酮的作用。
Carbenoxolone sodium, CS, a liquorice derivative associated with hypertension and sodium retention, has been demonstrated to inhibit 11 beta-hydroxysteroid dehydrogenase, an enzyme that metabolizes cortisol and corticosterone to their respective inactive 11-dehydro products (cortisone and 11-dehydrocorticosterone). It has been proposed that the increased bioavailability of unmetabolized corticosterone and cortisol following 11 beta-OHSD inhibition allows these steroids to act on renal mineralocorticoid receptors to elicit the mineralocorticoid action. Here we describe how CS amplifies the antinatriuretic activity of aldosterone and deoxycorticosterone; the latter steroid is of particular importance in that it does not possess a hydroxyl group at the C-11 position in the steroid ring, indicating that another mechanism(s) in addition to 11 beta-OHSD inhibition is responsible for the amplification of the action of deoxycorticosterone.