Marcussi Silvana, Sant'Ana Carolina D, Oliveira Clayton Z, Rueda Aristides Quintero, Menaldo Danilo L, Beleboni Rene O, Stabeli Rodrigo G, Giglio José R, Fontes Marcos R M, Soares Andreimar M
Departamento de Análises Clínicas, Toxicológicas e Bromatológicas, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto-SP, Brazil.
Curr Top Med Chem. 2007;7(8):743-56. doi: 10.2174/156802607780487614.
Phospholipases A2 (PLA2s) are commonly found in snake venoms from Viperidae, Hydrophidae and Elaphidae families and have been extensively studied due to their pharmacological and physiopathological effects in living organisms. This article reports a review on natural and artificial inhibitors of enzymatic, toxic and pharmacological effects induced by snake venom PLA2s. These inhibitors act on PLA2s through different mechanisms, most of them still not completely understood, including binding to specific domains, denaturation, modification of specific amino acid residues and others. Several substances have been evaluated regarding their effects against snake venoms and isolated toxins, including plant extracts and compounds from marine animals, mammals and snakes serum plasma, in addition to poly or monoclonal antibodies and several synthetic molecules. Research involving these inhibitors may be useful to understand the mechanism of action of PLA2s and their role in envenomations caused by snake bite. Furthermore, the biotechnological potential of PLA2 inhibitors may provide therapeutic molecular models with antiophidian activity to supplement the conventional serum therapy against these multifunctional enzymes.
磷脂酶A2（PLA2s）常见于蝰蛇科、海蛇科和眼镜蛇科的蛇毒中，由于其在生物体中的药理和生理病理作用而受到广泛研究。本文报道了对蛇毒PLA2s诱导的酶促、毒性和药理作用的天然和人工抑制剂的综述。这些抑制剂通过不同机制作用于PLA2s，其中大多数机制仍未完全清楚，包括与特定结构域结合、变性、特定氨基酸残基的修饰等。已经评估了几种物质对蛇毒和分离毒素的作用，包括植物提取物、海洋动物、哺乳动物和蛇血清血浆中的化合物，此外还有多克隆或单克隆抗体以及几种合成分子。涉及这些抑制剂的研究可能有助于了解PLA2s的作用机制及其在蛇咬伤所致中毒中的作用。此外，PLA2抑制剂的生物技术潜力可能提供具有抗蛇毒活性的治疗分子模型，以补充针对这些多功能酶的传统血清疗法。
