Anti-Inflammatory Effect of Deflazacort.

ABSTRACT

We compared the effects of deflazacort (DFZ) a methyloxazoline derivative of prednisolone (PRED), PRED and dexamethasone (DEX) on the IgE-mediated release of preformed (histamine) and de novo synthesized (leukotriene C4 (LTC4)) proinflammatory mediators from human peripheral blood basophils. Eighteen-hour incubation of basophils with pharmacological concentrations of DFZ (10--8 to 3 × 10--6M)concentration dependently inhibited (9-50%) the IgE-dependent release of histamine and LTC4 from basophils. DFZ had a similar anti-inflammatory efficacy as DEX (10--9 to 10--6M)and similar efficacy and potency as PRED (10--8 to 3 × 10--6M). We also evaluated the effects of DFZ (10--8 to 10--7M)in combination with cyclosporin A (CsA) on the IgE-mediated histamine and LTC4 release from basophils. Eighteen-hour incubation of basophils with low concentrations of DFZ (10--8 to 10--7M) produced an additive inhibition of the release of histamine and LTC4 caused by short-term incubation with CsA (30 ng/ml).