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

A. GARRO; F. M. GARIBOTTO; A. M. RODRIGUEZ; M. RAIMONDI; S. A. ZACCHINO; A. PERCZEL; C. SOMLAI; B. PENKE; R. D. ENRIZ

LETTERS IN DRUG DESIGN & DISCOVERY

BENTHAM SCIENCE PUBL LTD

Lugar: Oak Park; Año: 2011 vol. 8 p. 562 - 567

1570-1808

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.