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Cortisol 21-mesylate exerts glucocorticoid action on the induction of milk protein synthesis in cultured mammary gland.

Abstract
Cortisol 21-mesylate, an alkylating derivatives of cortisol, was previously shown to exert an anti-glucocorticoid action in rat hepatoma cell culture (Simons, Thompson and Johnson 1980). In this study the effect of cortisol 21-mesylate on milk protein synthesis induced in cultured mouse mammary gland by glucocorticoid, insulin, and prolactin was investigated. Addition of cortisol 21-mesylate at concentrations ranging from 10(-8) M to 10(-6) M produced no inhibition of casein synthesis that was induced by glucocorticoid, insulin and prolactin in mammary explants from midpregnant mice. On the other hand, cortisol 21-mesylate in combination with insulin and prolactin stimulated casein synthesis in cultured tissue. The potency of cortisol mesylate was about 1/10 to 1/30th of that of cortisol. Cortisol 21-mesylate, like cortisol, also augmented the accumulation of alpha-lactalbumin in midpregnant rat mammary tissue cultured in the presence of insulin and prolactin. A cell-free competition study of glucocorticoid receptors using cytoplasmic extracts from mouse mammary tissue showed that cortisol 21-mesylate competitively inhibited the binding of dexamethasone on glucocorticoid receptors. The apparent affinity of cortisol 21-mesylate for glucocorticoid receptors is about 1/10th of that of cortisol. These results indicate that cortisol 21-mesylate acts as a glucocorticoid but not as an antiglucocorticoid in the mammary gland.
AuthorsN Terada, T Oka
JournalHormone and metabolic research = Hormon- und Stoffwechselforschung = Hormones et metabolisme (Horm Metab Res) Vol. 15 Issue 10 Pg. 508-12 (Oct 1983) ISSN: 0018-5043 [Print] Germany
PMID6357980 (Publication Type: Journal Article)
Chemical References
  • Caseins
  • Glucocorticoids
  • Insulin
  • Milk Proteins
  • Receptors, Glucocorticoid
  • cortisol 21-mesylate
  • Dexamethasone
  • Prolactin
  • Lactalbumin
  • Hydrocortisone
Topics
  • Animals
  • Binding, Competitive
  • Caseins (biosynthesis)
  • Dexamethasone (pharmacology)
  • Drug Interactions
  • Female
  • Glucocorticoids (pharmacology)
  • Hydrocortisone (analogs & derivatives, pharmacology)
  • Insulin (pharmacology)
  • Lactalbumin (metabolism)
  • Mammary Glands, Animal (drug effects, metabolism)
  • Mice
  • Milk Proteins (biosynthesis)
  • Organ Culture Techniques
  • Pregnancy
  • Prolactin (pharmacology)
  • Rats
  • Receptors, Glucocorticoid (metabolism)

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