New Small-Size Antifungal Peptides: Design, Synthesis and Antifungal Activity

Title: New Small-Size Antifungal Peptides: Design, Synthesis and Antifungal Activity

Volume: 8 Issue: 6

Author(s): Adriana D. Garro, Francisco M. Garibotto, Ana M. Rodriguez, Marcela Raimondi, Susana A. Zacchino, Andras Perczel, Csaba Somlai, Botond Penke and Ricardo D. Enriz

Affiliation:

Keywords: Antifungals, Conformational and Electronic Study, Molecular Electrostatic Potentials, Peptides, Antifungal Peptides:, Cryptococcus neoformans, Molecular Electrostatic Potentials (MEP), nature's antibiotics, Cell-penetrating peptides (CPPs), LKB Bromma apparatus, Penetratin, Antennapedia, Candida albicans

Abstract: The synthesis, in vitro evaluation and conformational study of small-size peptides acting as antifungal agents are reported. These peptides displayed antifungal activity against human pathogenic strains including Candida albicans and Cryptococcus neoformans. Among the peptides reported here, RQWRRWWQR-NH2 exhibited the strongest activity against Cryptococcus neoformans. Our results allowed us to reduce in size these bioactive peptides from 16 to 11 and to 9 amino acid residues in total. Despite their reduction, they still maintained and even enhanced the antifungal activity detected for penetratin. A conformational and electronic structure analysis on these peptides was also performed by using molecular mechanics calculations in conjunction with Molecular Electrostatic Potentials (MEP) maps.

Cite this article as:

D. Garro Adriana, M. Garibotto Francisco, M. Rodriguez Ana, Raimondi Marcela, A. Zacchino Susana, Perczel Andras, Somlai Csaba, Penke Botond and D. Enriz Ricardo, New Small-Size Antifungal Peptides: Design, Synthesis and Antifungal Activity, Letters in Drug Design & Discovery 2011; 8 (6) . https://dx.doi.org/10.2174/157018011795906785