Laboratoire de Biologie Moléculaire et Cellulaire du Cancer, Fondation de Recherche Cancer et Sang, Hôpital Kirchberg, 9 Rue Edward Steichen, L-2540 Luxembourg, Luxembourg.
Biochem Pharmacol. 2010 Dec 15;80(12):1793-800. doi: 10.1016/j.bcp.2010.08.024. Epub 2010 Sep 15.
Phospholipases A(2) (PLA(2)s) form a family of enzymes catalyzing the hydrolysis of membrane phospholipids into arachidonic acid, which is the major precursor of pro-inflammatory eicosanoids. As a result, PLA(2)s have been considered as potential targets in anti-inflammatory drug discovery. Marine natural products are a rich source of bioactive compounds, including PLA(2) inhibitors. Here, we review the properties of marine PLA(2) inhibitors identified since the first discovery of PLA(2) inhibitory activity in the marine natural product manoalide in the mid 1980s.
磷脂酶 A2（PLA2s）形成了一个酶家族，能够催化膜磷脂水解生成花生四烯酸，后者是促炎类二十烷酸的主要前体。因此，PLA2s 已被视为抗炎药物发现的潜在靶点。海洋天然产物是生物活性化合物的丰富来源，包括 PLA2 抑制剂。本文综述了自 20 世纪 80 年代中期在海洋天然产物 manoalide 中首次发现 PLA2 抑制活性以来，所鉴定的海洋 PLA2 抑制剂的特性。
