Phospholipases A2 (PLA2s) and Related Peptides from Bothrops Snake Venoms: History, Structure, Pharmacology, and Inhibitors

I. C. D. Santos,Marcela Romanazzi,G. Malachias-Pires,Ariani R. Aragão,Eloise T. M. Filardi,Guilherme Melo-dos-Santos,Lara C Salvador,Marcos F. Cerveja,Anderson M. Rocha,Ananda Magalhães,I. S. de Oliveira,José R. Almeida,N. Santos-Filho,Manuela B. Pucca

Published 2025 in Biomolecules

ABSTRACT

Lancehead pitvipers, Bothrops snakes, or, popularly, “jararacas”, are common and broadly distributed in the Americas, especially in Brazil, where they are responsible for causing a high number of snakebite accidents. Their venoms are able to induce local and systemic effects, such as hemorrhaging, acute kidney failure, and shock, that can be fatal. Among the compounds of the venom are phospholipases A2 (PLA2s), which are abundant in some Bothrops species. PLA2s can perform different activities during envenoming, such as neurotoxicity, myotoxicity, and cytotoxicity, among others, through the hydrolysis of the ester bond at the sn-2 position of phospholipids, producing free fatty acids and lysophospholipids. Although different PLA2s can be classified into different PLA2 groups and subgroups, according to structure, function, size, localization and Ca2+ dependence, they converge to be available in biotechnological and therapeutic applications, such as antiviral and antitumor, among others, being relevant molecules to be deeply studied. Here, we provide the state of the art of PLA2s, found in snake venoms, focusing on Bothrops venoms, as well as their potential applications, beyond their inhibitors, that also receive attention due their importance in PLA2 studies and diverse applications.

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