豚肢関節滑膜における酸性ムコ多糖の生合成に対する各種抗炎症性ステロイド剤の影響
1975 年 35 巻 4 号 p. 325-331
詳細
1975 年 35 巻 4 号 p. 325-331
To assess the in vitro effect of various steroidal antiinflammatory agents, the biosyn-thetic activity of acid mucopolysaccharide was examined in the pig leg synovial membrane, in which the radioactive mucopolysaccharide was extracted and determined after the in-cubation with 13C-glucose.
The results were as follows:
1. The dose of 50% inhibition was proved to be 0.2 mg/ml of dexamethasone disodium phosphate, while the corresponding dose of prednisolone sodium hemisuccinate was 0.5 mg/m1-0.6 mg/ml.
2. Anti-inflammatory effect of a steroid varied according to its different water soluble derivatives. Thus, the drug concentration, in which the acid mucopolysaccharide synthesis was inhibited to 50%, was 0.18 mg/ml for dexamethasone disodium phosphate, while it was 1.23 mg/ml for dexamethasone sodium sulfate.
3. Acetylsalicylic acid was found not to show any appreciable inhibitory effect.
4. The results of preincubation indicated that prednisolone inhibited the biosynthesis of acid mucopolysaccharides to a similar extent as in the control. In contrast, dexametha-sone rather enhanced the biosynthesis of acid mucopolysaccharides, giving rise to the so-called “rebound phenomenon ”.
5. Among steroidal anti-inflammatory preparations, only water soluble ones were de-monstrated to be nearly equipotent with the preparations for per oral administration cur-rently in wide use.
