PACOCF3

PACOCF3是一种Ca2+依赖性胞质cPLA2和Ca2 +非依赖性磷脂酶A2 iPLA2的抑制剂,IC50值为45μM和3.8 μM[1,2],是一种新型的和潜在的炎症\动脉粥样硬化\糖尿病\治疗性休克\癌症治疗的候选药物[3,4,5,6].据报道,PACOCF3能抑制PLA2并减轻炎症反应.在基底葡萄糖水平(2 mmol/l)下,PACOCF3也可以刺激胰岛素释放.应用PACOCF3可以抑制内源性花生四烯酸产生,其显著降低20 mmol/l葡萄糖引起的胰岛素分泌反应的幅度[7,8].PACOCF3在糖尿病中有双重保护作用,可最小化β细胞功能障碍,同时通过增强内源性花生四烯酸水平,维持胰岛素分泌产量.

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