Introduction:

Nonsteroidal anti-inflammatory drugs (NSAIDs) are widely used for pain therapy, despite its side effects in renal, stomach and coagulant systems. Phospholipases A2 (PLA2) enzymes, present in snakes and bees’ venoms, and even in the human organism, are responsible for several physiological and pathological processes. These enzymes hydrolyze membrane phospholipids, releasing arachidonic acid, a precursor of pro-inflammatory eicosanoids, which give rise to inflammatory mediators.

Objective:

The aim of the present work is to review new molecules able to block the cleavage of membrane phospholipids by the action of phospholipases A2, preventing the formation of inflammatory mediators.

Methodology:

A bibliographic revision from literature published from 2011 to 2021 focused on PLA2 inhibitors was carried out. The potential of structure-activity relationship studies is discussed as a strategy to find active compounds against PLA2.

Results:

26 studies including natural and synthetic compounds were reviewed and data from 93 molecules with inhibitory activity were collected, highlighting its potential as PLA2 inhibitors. Conclusion: The inhibitory activity of the reviewed compounds could be associated with the substitution patterns in the benzene ring of the molecules. The evaluation of molecular moieties with relevant capacity to inhibit PLA2 will lead to the identification of candidates for synthesis of new enzymes inhibitors.

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