Abstract
The local anti-inflammatory potency of steroid-21-oate esters derived from prednisolone was determined by cotton pellet granuloma bioassay. The doses which inhibited granuloma formation by 50% (ID50) were: prednisolone, 0.5 mg/pellet; methyl 20 alpha-dihydroprednisolonate, 5.8 mg/pellet; methyl 20 beta-dihydroprednisolonate, 1.2 mg/pellet; methyl 17,20 alpha-acetonidodihydroprednisolonate, 6.0 mg/pellet. When administered at these equipotent local anti-inflammatory doses, only prednisolone depressed plasma corticosterone and promoted thymus involution. Prednisolone reduced neutrophil migration into saline-soaked polyester sponges and depressed the levels of 6-keto PGF1 alpha, PGE2 and elastase in the sponge-induced inflammatory exudate. Methyl 20 alpha- and 20 beta-dihydroprednisolonate had no effect on cell migration, but depressed the levels of 6-keto PGF1 alpha and elastase. The liberation of 6-keto PGF1 alpha, PGE2 and elastase and neutrophil migration were inhibited by methyl 17,20 alpha- and beta-acetonidodihydroprednisolonate, but the effect of the beta-epimer on cell migration was transient. These data suggest that steroid acid esters which have local and topical anti-inflammatory properties exert their effect in a similar fashion to glucocorticoids with a ketol side-chain (e.g. prednisolone) with respect to liberation of prostaglandins and lysosomal enzymes. However, their effect on neutrophil migration was variable, depending on their structural features. Furthermore, the systemic effects of these new derivatives were drastically reduced indicating that they may be of potential benefit in prolonged treatment.
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