In vitro immunosuppressive potency of deflazacort, a new bone-sparing corticosteroid on T lymphocytes, NK and K cells.
The in vitro immunosuppressive effect of deflazacort, a new bone-sparing glucocorticoid, and its biologically active metabolite, 21-deacetyl-deflazacort, was examined on phytohaemagglutinin (PHA) stimulated human peripheral blood lymphocytes (PBL) as well as on natural killer (NK) and killer (K) cell activity. Deflazacort and the 21-deacetyl metabolite were as potent as prednisolone and hydrocortisone in suppressing PHA stimulated lymphocytes in a dose dependent way, but all were less potent than methylprednisolone. The physiological metabolites of hydrocortisone, dihydrocortisol and tetrahydrocortisol were without any immunosuppressive effects in vitro. Deflazacort, 21-deacetyl-deflazacort, and methylprednisolone suppressed NK cell activity, while hydrocortisone and aldosterone had no effect on NK cells. K cell activity was resistent to all tested glucocorticoids except methylprednisolone at high concentrations. The present results indicate that deflazacort and 21-deacetyl-deflazacort are potent immunosuppressive drugs in vitro and, on a molar basis, equally as potent as prednisolone.
D000450:Aldosterone / Q000494:pharmacology; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D000920:Antibody-Dependent Cell Cytotoxicity / Q000187:drug effects; D006801:Humans; D006854:Hydrocortisone / Q000494:pharmacology; D007166:Immunosuppressive Agents; D007694:Killer Cells, Natural / Q000187:drug effects / Q000276:immunology*; D008213:Lymphocyte Activation / Q000187:drug effects; D008775:Methylprednisolone / Q000494:pharmacology; D011282:Pregnenediones / Q000494:pharmacology*; D013601:T-Lymphocytes / Q000187:drug effects / Q000276:immunology*
D000893:Anti-Inflammatory Agents; D007166:Immunosuppressive Agents; D011282:Pregnenediones; C048465:21-deacetyldeflazacort; D000450:Aldosterone; C021988:deflazacort; D006854:Hydrocortisone; D008775:Methylprednisolone