Introduction.Candidaspp. are commensal fungal pathogens of humans, but when there is an imbalance in the microbiota, or weak host immunity, these yeasts can become pathogenic, generating high medical costs.Gap Statement.With the increase in resistance to conventional antifungals, the development of new therapeutic strategies is necessary.This study evaluated thein vitroantifungal activity of chlorogenic acid against fluconazole-resistant strains ofCandidaspp.Mechanism of action through flow cytometry andin silicoanalyses, as well as molecular docking assays with ALS3 and SAP5, important proteins in the pathogenesis ofCandida albicansassociated with the adhesion process and biofilm formation.Results.The chlorogenic acid showedin vitroantifungal activity against the strains tested, causing reduced cell viability, increased potential for mitochondrial depolarization and production of reactive oxygen species, DNA fragmentation and phosphatidylserine externalization, indicating an apoptotic process. Concerning the analysis through docking, the complexes formed between chlorogenic acid and the targetsThymidylate Kinase, CYP51, 1Yeast Cytochrome BC1 ComplexeExo-B-(1,3)-glucanasedemonstrated more favourable binding energy. In addition, chlorogenic acid presented significant interactions with the ALS3 active site residues ofC. albicans,important in the adhesion process and resistance to fluconazole. Regarding molecular docking with SAP5, no significant interactions were found between chlorogenic acid and the active site of the enzyme.Conclusion.We concluded that chlorogenic acid has potential use as an adjuvant in antifungal therapies, due to its anti-Candidaactivity and ability to interact with important drug targets.
1 March 2020 in Complementary Therapies in Medicine
Two lipidic α-amino acids 1a and 1b were isolated from the zoanthid Protopalythoa variabilis using a bioguided fractionation for cytotoxic activity. The structures of the metabolites were determined by spectroscopic methods, including NMR (nuclear magnetic resonance) ¹H e 13C, IR (infrared) and high resolution mass spectrometry (positive mode). The cytotoxic activity of the crude extract, as well as of the mixture of 1a and 1b were measured in vitro using the MTT assay for four human tumor cell lines. This finding has important biological and chemical implications for this type of compound. This is the first report of lipidic α-amino acids from natural sources, as well as of their cytotoxic activity.