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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Research Article

A UBI 31-38 Peptide-coumarin Conjugate: Photophysical Features, Imaging Tracking and Synergism with Amphotericin B Against Cryptococcus

Author(s): Soraya M.Z.M.D. Ferreira, Hellem C. Carneiro, Rosemeire B. Alves, Ana Carolina S. Batista, Eufranio N. da Silva Junior, Gleiston G. Dias, Jarbas M. Resende, Daniel A. Santos, Debora L. Oliveira, Marcio L. Rodrigues and Rossimiriam P. Freitas*

Volume 18 , Issue 2 , 2018

Page: [157 - 163] Pages: 7

DOI: 10.2174/1568026618666180221113137

Price: $65

Abstract

Cryptococcosis is a fungal disease of global significance for which new effective treatments are needed. The conjugation of the synthetic antimicrobial peptide fragment UBI 31-38 to a coumarin derivative showed to be an effective approach for the design of a novel anticryptococcal agent. In addition to antifungal activity, the conjugate exhibited intense fluorescence, which could be valuable for mechanistic investigations of this molecule. In this work, we studied the photophysical properties of the conjugate and confocal scanning laser microscopy was used to inspect the distribution of the peptide-coumarin conjugate in Cryptococcus cell. The synergism of this compound with amphotericin B or fluconazole against C. gattii and C. neoformans strains was also investigated. The results indicated that the fluorescent conjugate alone as well as its combination with amphotericin B are promising tools against cryptococcosis.

Keywords: UBI 31-38, peptide-coumarin conjugate, fluorescent, anticryptococcal activity, interaction studies, confocal scanning laser microscopy.

Graphical Abstract

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