EFFECTS OF 2-{4-(2-IMIDAZO[1, 2-a]PYRIDYL)PHENYL} PROPIONIC ACID (Y-9213) AND ANTI-INFLAMMATORY DRUGS ON ERYTHROCYTES, POLYMORPHONUCLEAR LEUKOCYTES AND LYSOSOMES IN VITRO

[摘要] References(31)Cited-By(4)2-{4-(2-Imidazo[1, 2-a]pyridyl)phenyl}propionic acid (Y-9213) with analgesic, antipyretic and anti-inflammatory activities significantly inhibited hemolysis of rat erythrocytes. Activity of Y-9213 (100-500 μM) on hemolysis was more potent than that of phenylbutazone, and less potent than that of indomethacin. The spontaneous release of enzymes from rat liver lysosomes by incubation alone was significantly inhibited by Y-9213 (1-100 μM) to the same degree as phenylbutazone or tinoridine hydrochloride. Release of enzymes from the lysosomes by addition of phospholipase C (PLC, 0.03 units/ml) was slightly inhibited by Y-9213 (10-100 μM) and phenylbutazone (100 μM). Dexamethasone, prednisolone, hydrocortisone and tinoridine hydrochloride (1-10 μM) inhibited more potently the PLC-induced release than the spontaneous release. Y-9213 (1-100 μM) inhibited considerably the release of enzymes from intact lysosomes of rabbit polymorphonuclear (PMN) leukocytes. The release of enzymes from the PMN leukocyte lysosomes preincubated at 37°C for 15 min was strongly inhibited by dexamethasone, prednisolone and hydrocortisone (1-100 μM), but not by Y-9213, phenylbutazone and indomethacin (100 μM). Y-9213 (0.1-10 μM) also inhibited significantly the phagocytic secretion of lysosomal enzymes from PMN leukocytes without affecting phagocytosis of the particles. Activity of this agent was similar to that of phenylbutazone, and less active than that of indomethacin, dexamethasone or prednisolone. Our results suggest that Y-9213 may stabilize membranes of erythrocytes and lysosomes and inhibit phagocytic secretion of lysosomal constituents from PMN leukocytes.

[学科分类] 药理学