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Antimicrobial Octapeptin C4 Analogues Active against Cryptococcus Species.

ABSTRACT: Resistance to antimicrobials is a growing problem in both developed and developing countries. In nations where AIDS is most prevalent, the human fungal pathogen Cryptococcus neoformans is a significant contributor to mortality, and its growing resistance to current antifungals is an ever-expanding threat. We investigated octapeptin C4, from the cationic cyclic lipopeptide class of antimicrobials, as a potential new antifungal. Octapeptin C4 was a potent, selective inhibitor of this fungal pathogen with an MIC of 1.56 ?g/ml. Further testing of octapeptin C4 against 40 clinical isolates of C. neoformans var. grubii or neoformans showed an MIC of 1.56 to 3.13 ?g/ml, while 20 clinical isolates of C. neoformans var. gattii had an MIC of 0.78 to 12.5 ?g/ml. In each case, the MIC values for octapeptin C4 were equivalent to, or better than, current antifungal drugs fluconazole and amphotericin B. The negatively charged polysaccharide capsule of C. neoformans influences the pathogen's sensitivity to octapeptin C4, whereas the degree of melanization had little effect. Testing synthetic octapeptin C4 derivatives provided insight into the structure activity relationships, revealing that the lipophilic amino acid moieties are more important to the activity than the cationic diaminobutyric acid groups. Octapeptins have promising potential for development as anticryptococcal therapeutic agents.

SUBMITTER: Chitty JL

PROVIDER: S-EPMC5786788 | biostudies-literature | 2018 Feb

REPOSITORIES: biostudies-literature

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Antimicrobial Octapeptin C4 Analogues Active against Cryptococcus Species.

Chitty Jessica L JL Butler Mark S MS Suboh Azzah A Edwards David J DJ Cooper Matthew A MA Fraser James A JA Robertson Avril A B AAB

Antimicrobial agents and chemotherapy 20180125 2

Resistance to antimicrobials is a growing problem in both developed and developing countries. In nations where AIDS is most prevalent, the human fungal pathogen <i>Cryptococcus neoformans</i> is a significant contributor to mortality, and its growing resistance to current antifungals is an ever-expanding threat. We investigated octapeptin C4, from the cationic cyclic lipopeptide class of antimicrobials, as a potential new antifungal. Octapeptin C4 was a potent, selective inhibitor of this fungal ...[more]

PMID: 29158283

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Project description:Background and aim Honey has been recognized worldwide for its antioxidant, anti-tumor, anti-inflammatory and antimicrobial properties. Among them, the antifungal properties associated to honey make it an attractive alternative treatment for Candida-associated infections, particularly for topical application to the mucous membranes and skin. In this sense, the main purpose of this work was to evaluate physicochemical properties of five Portuguese honeys and Manuka honey (an Australian honey with well recognized medical proprieties, used as control) and to evaluate the antifungal activity in Candida species planktonic and biofilm assays. Experimental procedure Pollen analysis, pH determination, color, concentration of protein and methylglyoxal, conductivity, total phenolics and flavonoids, hydrogen peroxide concentration, and characterization by differential scanning calorimetry in honey samples were determined. Additionally, the effect of honeys on planktonic growth of Candida was initially evaluated by determination of the minimum inhibitory concentrations. Then, the same effect of those honeys was evaluated in biofilms, by Colony Forming Units enumeration. Results and conclusion It has been shown that Portuguese heather (Erica cinereal) honey presented the most similar physicochemical properties to manuka honey (specially phenolic and flavonoids contents). The five Portuguese honeys under study, presented in general a potent activity against planktonic multi-resistant yeast pathogens (several clinical isolates and reference strains of Candida species) and S. aureus and P. aeruginosa bacteria cultures. Additionally, it was also concluded that Portuguese heather honey (50% and 75% (w/v)) can also act as a good Candida species biofilm reducer, namely for C. tropicalis. Graphical abstract Image 1 Highlights • The several physicochemical properties of five Portuguese honeys were determined.• The effect of honey on planktonic and biofilms of Candida species was assessed.• The five Portuguese honeys present in general a potent activity antimicrobial.

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Antimicrobial Octapeptin C4 Analogues Active against Cryptococcus Species.

Publications

Antimicrobial Octapeptin C4 Analogues Active against Cryptococcus Species.

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