Exploring the anti-biofilm activity of cinnamic acid derivatives in Candida albicans

Daniela De Vita; Giovanna Simonetti; Fabiana Pandolfi; Roberta Costi; Roberto Di Santo; Felicia Diodata D'Auria; Luigi Scipione

doi:10.1016/j.bmcl.2016.10.091

Exploring the anti-biofilm activity of cinnamic acid derivatives in Candida albicans

Bioorg Med Chem Lett. 2016 Dec 15;26(24):5931-5935. doi: 10.1016/j.bmcl.2016.10.091. Epub 2016 Nov 1.

Authors

Daniela De Vita¹, Giovanna Simonetti², Fabiana Pandolfi¹, Roberta Costi³, Roberto Di Santo³, Felicia Diodata D'Auria², Luigi Scipione⁴

Affiliations

¹ Department of Chimica e Tecnologie del Farmaco, Sapienza University of Rome, P.le A. Moro, 5, I-00185 Rome, Italy.
² Department of Public Health and Infectious Diseases, "Sapienza" University of Rome, Piazzale Aldo Moro 5, 00185 Rome, Italy.
³ Department of Chimica e Tecnologie del Farmaco, Sapienza University of Rome, P.le A. Moro, 5, I-00185 Rome, Italy; "Istituto Pasteur-Fondazione Cenci Bolognetti", Department of Chimica e Tecnologie del Farmaco, Sapienza University of Rome, P.le A. Moro, 5, I-00185 Rome, Italy.
⁴ "Istituto Pasteur-Fondazione Cenci Bolognetti", Department of Chimica e Tecnologie del Farmaco, Sapienza University of Rome, P.le A. Moro, 5, I-00185 Rome, Italy. Electronic address: luigi.scipione@uniroma1.it.

PMID: 27838185
DOI: 10.1016/j.bmcl.2016.10.091

Abstract

Some compounds, characterized by phenylethenyl moiety, such as methyl cinnamate and caffeic acid phenethyl ester, are able to inhibit C. albicans biofilm formation. On these bases, and as a consequence of our previous work, we synthesized a series of cinnamoyl ester and amide derivatives in order to evaluate them for the activity against C. albicans biofilm and planktonically grown cells. The most active compounds 7 and 8 showed ⩾50% biofilm inhibition concentrations (BMIC₅₀) of 2μg/mL and 4μg/mL respectively, against C. albicans biofilm formation; otherwise, 7 showed an interesting activity also against mature biofilm, with BMIC₅₀ of 8μg/mL.

Keywords: Biofilm; Candida albicans; Cinnamic esters; Cinnamoyl amides.

MeSH terms

Antifungal Agents / chemical synthesis
Antifungal Agents / chemistry
Antifungal Agents / pharmacology*
Biofilms / drug effects*
Candida albicans / drug effects*
Candida albicans / metabolism
Cinnamates / chemical synthesis
Cinnamates / chemistry
Cinnamates / pharmacology*
Dose-Response Relationship, Drug
Microbial Sensitivity Tests
Molecular Structure
Structure-Activity Relationship

Substances

Antifungal Agents
Cinnamates
cinnamic acid