New Strategies for Novel Drugs: Antimicrobial Peptides Containing Ferrocene with Improved Antifungal and Antiplasmodial Biological Activity.

Autor:	Costa NCS; Department of Biochemistry and Organic Chemistry, Institute of Chemistry, São Paulo State University (UNESP), São Paulo, Brazil., Santos-Filho NA; Department of Biochemistry and Organic Chemistry, Institute of Chemistry, São Paulo State University (UNESP), São Paulo, Brazil., Piccoli JP; Department of Biochemistry and Organic Chemistry, Institute of Chemistry, São Paulo State University (UNESP), São Paulo, Brazil., Fusco-Almeida AM; Department of Clinical Analysis, School of Pharmaceutical Sciences, São Paulo State University (UNESP), São Paulo, Brazil., Santos CT; Department of Clinical Analysis, School of Pharmaceutical Sciences, São Paulo State University (UNESP), São Paulo, Brazil., de Souza JO; São Carlos Institute of Physics, University of Sao Paulo (USP), São Paulo, Brazil., Zanini CL; São Carlos Institute of Physics, University of Sao Paulo (USP), São Paulo, Brazil., Aguiar ACC; São Carlos Institute of Physics, University of Sao Paulo (USP), São Paulo, Brazil., Oliva G; São Carlos Institute of Physics, University of Sao Paulo (USP), São Paulo, Brazil., Guido RVC; São Carlos Institute of Physics, University of Sao Paulo (USP), São Paulo, Brazil., Cilli EM; Department of Biochemistry and Organic Chemistry, Institute of Chemistry, São Paulo State University (UNESP), São Paulo, Brazil.
Jazyk:	angličtina
Zdroj:	Protein and peptide letters [Protein Pept Lett] 2022; Vol. 29 (12), pp. 1088-1098.
DOI:	10.2174/0929866529666220929162509
Abstrakt:	Background: Fungal and parasitic diseases are global health problems, and the available treatments are becoming ineffective, mainly due to the emergence of resistant strains of pathogens. Furthermore, the drugs currently in use exhibit high toxicity and side effects. The scarcity of efficient treatments for fungal and parasitic diseases has motivated the search for new drug candidates, including antimicrobial peptides. The chemokine class RP1 peptide shows inhibitory activity against bacteria, viruses, cancer cells and parasites. In addition, the organometallic compound ferrocene showed antiparasitic activity. Objective: Study aimed to assess the effect of conjugation of the RP1 peptide with ferrocene in terms of its structure, biological activity against fungi and parasites and toxicity. Methods: Peptides and conjugates were synthesized using solid phase peptide synthesis (SPPS). The Fc-RP1 peptide showed antifungal and antimalarial activities with low toxicity in the U87 and HepG2 cell lines. Results: The mechanism of action of these peptides, analyzed by flow cytometry in the fungus Cryptococcus neoformans, was through membrane permeabilization, with an emphasis on the Fc-RP1 peptide that presented the highest rate of PI-positive cell marking. Conclusion: In conclusion, ferrocene conjugated to antimicrobial peptide RP1 is an attractive biomolecule for drug discovery against fungal and parasitic diseases. (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)
Databáze:	MEDLINE
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