Langhoff E, Olgaard K
Br J Clin Pharmacol. 1986 Feb;21(2):125-9. doi: 10.1111/j.1365-2125.1986.tb05165.x.
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.
研究了新型保骨糖皮质激素地夫可特及其生物活性代谢物21-去乙酰地夫可特对植物血凝素(PHA)刺激的人外周血淋巴细胞(PBL)以及自然杀伤(NK)细胞和杀伤(K)细胞活性的体外免疫抑制作用。地夫可特和21-去乙酰代谢物在以剂量依赖方式抑制PHA刺激的淋巴细胞方面与泼尼松龙和氢化可的松一样有效,但均不如甲泼尼龙有效。氢化可的松的生理代谢物二氢皮质醇和四氢皮质醇在体外没有任何免疫抑制作用。地夫可特、21-去乙酰地夫可特和甲泼尼龙抑制NK细胞活性,而氢化可的松和醛固酮对NK细胞没有影响。除高浓度的甲泼尼龙外,K细胞活性对所有测试的糖皮质激素均有抗性。目前的结果表明,地夫可特和21-去乙酰地夫可特在体外是有效的免疫抑制药物,且以摩尔计,与泼尼松龙一样有效。