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Isolation and structural characterization of bioactive compound from Aristolochia sprucei aqueous extract with anti-myotoxic activity

2020; Elsevier BV; Volume: 7; Linguagem: Inglês

10.1016/j.toxcx.2020.100049

2590-1710

Isela I. González Rodríguez, Áleff Ferreira Francisco, Leandro S. Moreira-Dill, Aristides Quintero Rueda, César L.S. Guimarães, Carlos A. H. Fernandes, Agnes A. S. Takeda, Fernando Berton Zanchi, Cleópatra Alves da Silva Caldeira, Paulo Sérgio Pereira, Marcos R.M. Fontes, Juliana P. Zuliani, Andreimar M. Soares,

Drug-Induced Hepatotoxicity and Protection

A bioactive compound isolated from the stem extract of Aristolochia sprucei through High Performance Liquid Chromatography (HPLC) was identified via Nuclear Magnetic Resonance (NMR) as the aristolochic acid (AA). This compound showed an inhibitory effect over the myotoxic activity of Bothrops jararacussu and Bothrops asper venoms, being also effective against the indirect hemolytic activity of B. asper venom. Besides, AA also inhibited the myotoxic activity of BthTX-I and MTX-II with an efficiency greater than 60% against both myotoxins. Docking predictions revealed an interesting mechanism, through which the AA displays an interaction profile consistent with its inhibiting abilities, binding to both active and putative sites of svPLA2. Overall, the present findings indicate that AA may bind to critical regions of myotoxic Asp 49 and Lys49-PLA2s from snake venoms, highlighting the relevance of domains comprising the active and putative sites to inhibit these toxins.