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Antifungal peptides at membrane interaction.

Abstract：

:Many drugs are available for the treatment of systemic or superficial mycoses, but only a limited number of them are effective antifungal drugs, devoid of toxic and undesirable side effects. Furthermore, resistance development and fungistatic rather than fungicidal activities represent limitations of current antifungal therapy. Therefore an urgent need for a new generation of antifungal agents remains. We recently synthesised a set of linear and cyclic peptides characterized by sequences typical of membrane-active antimicrobial peptides (AMP). AMT2, cyclo-AMT2, AMT3 and cyclo-AMT3 (Scheme 1) were tested against different yeast species and exhibited general antifungal activity, with a specificity against Cryptococcus neoformans. To evaluate the role of the membrane cell in the mechanism of antifungal activity, we investigated the conformational behaviour of AMT2, cyclo-AMT2, AMT3 and cyclo-AMT3 in different bio-membrane mimicking systems using a combined approach based on spectroscopy and microscopy techniques. Our data highlight the behaviour of the peptides to interact with the bilayer surface, excluding their ability to destabilize or permeabilize the fungal cell wall. Microbial membrane, indeed, may be an important platform for specific interactions of peptides with specific targets involved in the cell wall synthesis.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Di Marino S,Scrima M,Grimaldi M,D'Errico G,Vitiello G,Sanguinetti M,De Rosa M,Soriente A,Novellino E,D'Ursi AM

doi

10.1016/j.ejmech.2012.02.037

subject

Has Abstract

pub_date

2012-05-01 00:00:00

pages

154-62

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(12)00128-6

journal_volume

51

pub_type

杂志文章

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