Mineralocorticoid and renal receptor binding activity of 21-deoxy aldosterone

Hideo Koshida, Isamu Miyamori, Ryuichiro Soma, Takao Matsubara, Masatoshi Ikeda, Ryoyu Takeda, Shinichi Nakamura, Fumiyuki Kiuchi, Yoshisuke Tsuda

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Since several aldosterone metabolites are known to be active, we have assessed the mineralocorticoid biological and renal receptor binding activities of the aldosterone metabolites, 21-deoxyaldosterone (21-deoxy-Aldo), 21-deoxytetrahy-droaldosterone (21-deoxy-THAldo), and 3α, 5 β-tetrahydroaldos-terone (THAldo). We synthesized these steroids by bioreduction of aldosterone with intestinal bacteria. Mineralocorticoid agonist activity of 21-deoxy-Aldo, 21-deoxy-THAldo and THAldo, determined by bioassay using adrenalectomized rats, was 1-5%, less than 0.01%, and 0.1-0.5% that of aldosterone, respectively. 21-De.oxy-Aldo showed no antagonist activity. The relative affinity in competing with [3H] aldosterone for binding to mineralocorticoid receptors in adrenalectomized rat kidney cytosols was 94%, less than 0.01%, and less than 0.01% that of aldosterone. The relative binding affinity for rat renal glucocorticoid receptors was 23%, less than 0.01%, and less than 0.01% that of dexamethasone, and for corticosteroid-binding globulin 17%, less than 0.01%, and less than 0.01% that of Cortisol. These results show that the naturally occurring steroid, 21-deoxy-Aldo, possesses mineralocorticoid agonist activity which is equivalent to that of 11-deoxycorticosterone, and has substantial affinity for rat renal mineralocorticoid and glucocorticoid receptors. The results also implicate the pathophysiological role of 21-deoxy-Aldo as a potential mineralocorticoid in 21-hydroxylase defi-ciency, where urinary excretion of this steroid is invariably elevated.

Original languageEnglish
Pages (from-to)1410-1415
Number of pages6
Issue number3
Publication statusPublished - 1990 Mar

ASJC Scopus subject areas

  • Endocrinology

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    Koshida, H., Miyamori, I., Soma, R., Matsubara, T., Ikeda, M., Takeda, R., Nakamura, S., Kiuchi, F., & Tsuda, Y. (1990). Mineralocorticoid and renal receptor binding activity of 21-deoxy aldosterone. Endocrinology, 126(3), 1410-1415. https://doi.org/10.1210/endo-126-3-1410