11beta-Hydroxyprogesterone (11β-Hydroxyprogesterone)

A metabolite of progesterone

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Background

11β-Hydroxyprogesterone (11β-OHP) is a metabolite of progesterone .¹ It is an agonist of the mineralocorticoid receptor (MR) that induces MR transactivation in a reporter assay (EC₅₀ = 0.05 ?M for COS-7 cells expressing the human receptor).² It increases sodium absorption in mpkCCDc14 murine renal cortical collecting duct cells. 11β-OHP is an inhibitor of 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2) and 11β-HSD1 (IC₅₀s = 0.140 and 1 ?M, respectively).³ It increases blood pressure in rats when administered subcutaneously at a rate of 10 ?g/hour.⁴ Serum levels of 11β-OHP are increased in patients with 21-hydroxylase deficiency, a type of congenital adrenal hyperplasia (CAH), characterized by masculinized genitals in female infants, irregular menses in adult females, and accelerated bone age in adolescent males.⁵

1.van Rooyen, D., Gent, R., Barnard, L., et al.The in vitro metabolism of 11β-hydroxyprogesterone and 11-ketoprogesterone to 11-ketodihydrotestosterone in the backdoor pathwayJ. Steroid Biochem. Mol. Biol.178203-212(2018) 2.Rafestin-Oblin, M.-E., Fagart, J., Souque, A., et al.11β-hydroxyprogesterone acts as a mineralocorticoid agonist in stimulating Na+ absorption in mammalian principal cortical collecting duct cellsMol. Pharmacol.62(6)1306-1313(2002) 3.Souness, G.W., Latif, S.A., Laurenzo, J.L., et al.11α- and 11β-hydroxyprogesterone, potent inhibitors of 11β-hydroxysteroid dehydrogenase (isoforms 1 and 2), confer marked mineralocorticoid activity on corticosterone in the ADX ratEndocrinology136(4)1809-1812(1995) 4.Souness, G.W., and Morris, D.J.11α- and 11β-hydroxyprogesterone, potent inhibitors of 11β-hydroxysteroid dehydrogenase, possess hypertensinogenic activity in the ratHypertension27(3 Pt 1)421-425(1996) 5.Turcu, A.F., Rege, J., Chomic, R., et al.Profiles of 21-carbon steroids in 21-hydroxylase deficiencyJ. Clin. Endocrinol. Metab.100(6)2283-2290(2015)

Protocol

Animal experiment:

Rats: 11α- and 11β-OHP are dissolved in propylene glycol (100%) and infused at 3 and 10 μg/h, respectively, for 14 days. Control rats received vehicle only. BP is measured the day before pumps were implanted and on days 3, 7, 10, and 14 after implantation. Indirect systolic BPs are measured with a modified tail-cuff method[2].

参考文献:

[1]. Rafestin-Oblin ME, et al. 11beta-hydroxyprogesterone acts as a mineralocorticoid agonist in stimulating Na+ absorption in mammalian principal cortical collecting duct cells. Mol Pharmacol. 2002 Dec;62(6):1306-13.
[2]. Souness GW, et al. 11 alpha- and 11 beta-hydroxyprogesterone, potent inhibitors of 11 beta-hydroxysteroid dehydrogenase, possess hypertensinogenic activity in the rat. Hypertension. 1996 Mar;27(3 Pt 1):421-5.