Features of the shuttle pair 11 beta-hydroxyprogesterone-11-ketoprogesterone

Autor: Mario D. Galigniana, Gerardo Burton, Guillermo P. Vicent, C.P. Lantos
Rok vydání: 1997
Předmět:
Zdroj: Steroids. 62(4)
ISSN: 0039-128X
Popis: 11β-hydroxyprogesterone (HOP) and 11-ketoprogesterone (KP) are reversible components of a shuttle pair whose interconversion in rat liver is catalyzed by isoform-1 of 11β-hydroxysteroid dehydrogenase. Kidneys also produce this interconversion. The present study was carried out to investigate the shuttle pair and its components in the rat. As in corticosterone/11-dehydrocorticosterone, oxidation is more effective at an alkaline pH, while reduction prevails at a neutral pH. Moreover, both reactions are inhibited by the detergent 3-[(3-cholamido propyl)-dimethylammonio]-1-propane-sulphonate (CHAPS). However, at variance with the 11-ketosteroids cortisone (E) and 11-dehydrocorticosterone (A) thought to be “inactive,” KP has slight direct Na + -retaining properties, and it, as well as HOP, induces glucocorticoids (11β-hydroxycorticoids) to retain sodium. 11-ketoprogesterone exhibits 17 times better affinity for native type I mineralocorticoid receptor than HOP and a 3-fold affinity for partially purified (transcortin free) mineralocorticoid receptor. However, KP, in contrast to HOP, binds only weakly to transcortin, not at all to glucocorticoid receptor, and requires reduction at C 11 for tyrosine aminotransferase (TAT) induction.
Databáze: OpenAIRE