Examining Topoisomers of a Snake-Venom-Derived Peptide for Improved Antimicrobial and Antitumoral Properties

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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.
Funding Information
  • Spanish Ministry of Economy and Innovation (AGL2017-84097-C2-2-R, PID2020-113184RB-C22, PID2020-112821GB-I00, PID2020-114627RB-I00, PDC2021-121544-I00, Next GenerationEU/PRTR, HR17-00409)
  • Spanish Ministry of Science and Innovation (AGL2017-84097-C2-2-R, PID2020-113184RB-C22, PID2020-112821GB-I00, PID2020-114627RB-I00, PDC2021-121544-I00, Next GenerationEU/PRTR, HR17-00409)
  • eu (AGL2017-84097-C2-2-R, PID2020-113184RB-C22, PID2020-112821GB-I00, PID2020-114627RB-I00, PDC2021-121544-I00, Next GenerationEU/PRTR, HR17-00409)
  • la Caixa Banking Foundation (AGL2017-84097-C2-2-R, PID2020-113184RB-C22, PID2020-112821GB-I00, PID2020-114627RB-I00, PDC2021-121544-I00, Next GenerationEU/PRTR, HR17-00409)

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