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

作者：Garro Adriana D; Garibotto Francisco M; Rodriguez Ana M; Raimondi Marcela; Zacchino Susana A; Perczel Andras; Somlai Csaba; Penke Botond; Enriz Ricardo D^*

来源：Letters in Drug Design and Discovery, 2011, 8(6): 562-567.

• Antifungals
• Conformational and Electronic Study
• Molecular Electrostatic Potentials
• Peptides

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-NH(2) 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.

• 出版日期2011-7