Examining topoisomers of a snake-venom-derived peptide for improved antimicrobial and antitumoral properties

Carrera-Aubesart, Adam; Defaus, Sira; Pérez-Peinado, Clara, 1991-; Sandín, Daniel; Torrent Burgas, Marc; Jiménez, M. Ángeles; Andreu Martínez, David

doi:http://dx.doi.org/10.3390/biomedicines10092110

Examining topoisomers of a snake-venom-derived peptide for improved antimicrobial and antitumoral properties

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Carrera-Aubesart A, Defaus S, Pérez-Peinado C, Sandín D, Torrent M, Jiménez MÁ, Andreu D. Examining topoisomers of a snake-venom-derived peptide for improved antimicrobial and antitumoral properties. Biomedicines. 2022 Aug 29;10(9):2110. DOI: 10.3390/biomedicines10092110

Abstract

Ctn[15-34], the C-terminal section of crotalicidin (Ctn), a cathelicidin from a South American pit viper, is an antimicrobial and antitumoral peptide with remarkably longer stability in human serum than the parent Ctn. In this work, a set of topoisomers of both Ctn and Ctn[15-34], including the retro, enantio, and retroenantio versions, were synthesized and tested to investigate the structural requirements for activity. All topoisomers were as active as the cognate sequences against Gram-negative bacteria and tumor cells while slightly more toxic towards normal cells. More importantly, the enhanced serum stability of the D-amino-acid-containing versions suggests that such topoisomers must be preferentially considered as future antimicrobial and anticancer peptide leads.