Vignon E, Mathieu P, Louisot P, Vilamitjana J, Harmand M F, Richard M
Hôpital Edward Herriot, Lyon, France.
J Rheumatol Suppl. 1989 Aug;18:35-8.
Phospholipase A2 (PLA2) activity was measured in articular cartilage from normal and osteoarthritic (OA) human femoral heads. Protoglycanase and collagenase activity was determined in the same specimens using radiolabelled human proteoglycan subunit and type II collagen, respectively. Grossly normal and fibrillated OA cartilage samples showed a significant increase in PLA2 activity which was not found in osteophytic cartilage. PLA2 activity was found to be correlated with proteoglycanase but unrelated to collagenase activity. Tiaprofenic acid induced in vitro a concomitant increase in PLA2 and a decrease in proteoglycanase activity. PLA2 which may be activated by cytokines as well as mechanical factors is suggested as a key enzyme in chondrocyte metabolism regulation. Tiaprofenic acid is shown as a potential chondroprotective nonsteroidal anti-inflammatory drug.
在正常和骨关节炎(OA)患者的人类股骨头关节软骨中测量了磷脂酶A2(PLA2)活性。分别使用放射性标记的人蛋白聚糖亚基和II型胶原在相同标本中测定蛋白聚糖酶和胶原酶活性。大体正常和纤维化的OA软骨样本显示PLA2活性显著增加,而在骨赘软骨中未发现这种增加。发现PLA2活性与蛋白聚糖酶相关,但与胶原酶活性无关。噻洛芬酸在体外诱导PLA2同时增加,蛋白聚糖酶活性降低。PLA2可能被细胞因子以及机械因素激活,被认为是软骨细胞代谢调节中的关键酶。噻洛芬酸被证明是一种潜在的具有软骨保护作用的非甾体抗炎药。