Ethnopharmacological Relevance: Candida auris poses a severe global health threat, with many strains resistant to antifungal treatments, complicating therapy. Exploring natural compounds alongside conventional drugs offers promising therapeutic avenues. The antifungal potential of the ethanolic extract from Caryocar brasiliense (Cb-EE), a plant native to the Brazilian cerrado and renowned for its medicinal properties, was investigated against C. auris.
Aim Of The Study: The study examined the chemical composition, antifungal activity, mechanisms of action, and in vivo effects of Cb-EE.
Materials And Methods: Leaves of C. brasiliense were processed to extract ethanolic extract, which was evaluated for phenolic compounds, flavonoids, and tannins. The antifungal capacity was determined through broth microdilution and checkerboard methods, assessing interaction with conventional antifungals.
Results: Cb-EE demonstrated fungistatic activity against various Candida species and Cryptococcus neoformans. Synergy with fluconazole and additive effects with other drugs were observed. Cb-EE inhibited C. auris growth, with the combination of fluconazole extending inhibition. Mechanistic studies revealed interference with fungal membranes, confirmed by sorbitol protection assays, cellular permeability tests, and scanning electron microscopy (SEM). Hemocompatibility and in vivo toxicity tests on Tenebrio molitor showed safety.
Conclusion: Cb-EE, alone or in combination with fluconazole, effectively treated C. auris infections in vitro and in vivo, suggesting its prospective role as an antifungal agent against this emerging pathogen.
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http://dx.doi.org/10.1016/j.jep.2024.118240 | DOI Listing |
J Agric Food Chem
January 2025
State Key Laboratory of Green Pesticides, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals, Guizhou University, Guiyang 550025, PR China.
A total of 38 new benzohydrazide derivatives bearing the 4-aminoquinazoline moiety were designed and synthesized based on the active subunit combination approach and tested in detail for their inhibition activities against eight agricultural phytopathogenic fungi. The bioassay results indicated that many of the synthesized compounds exhibited extraordinary fungicidal activities in vitro against the tested fungi. For example, compounds , , , and had EC (half-maximal effective concentration) values of 0.
View Article and Find Full Text PDFBiofilm
June 2025
Department of Infectious Diseases and Clinical Microbiology, Beijing Institute of Respiratory Medicine and Beijing Chao-Yang Hospital, Capital Medical University, Beijing, China.
The biofilm formation of , a major human fungal pathogen, represents a crucial virulence factor during candidiasis. Eicosapentaenoic acid (EPA), a polyunsaturated fatty acid, has emerged as a potential antibiofilm agent against . .
View Article and Find Full Text PDFJ Struct Biol X
June 2025
Bioorganic Chemistry and Bio-Crystallography Laboratory (B2Cl) Faculty of Agricultural, Environmental and Food Sciences, Libera Università di Bolzano, Piazza Università, 1, 39100 Bolzano, Italy.
Siderophore-mediated iron acquisition is essential for the virulence of , a fungus causing life-threatening aspergillosis. Drugs targeting the siderophore biosynthetic pathway could help improve disease management. The transacetylases SidF and SidL generate intermediates for different siderophores in .
View Article and Find Full Text PDFChirality
February 2025
Faculty of Chemistry, 'Alexandru Ioan Cuza' University of Iasi, Iasi, Romania.
Chirality plays a crucial role in the pharmacological activity of triazoles, a key scaffold in antifungal agents and various therapeutic applications. This study focuses on optimizing the enantiomeric resolution of chiral triazoles using supercritical fluid chromatography (SFC) and 10 different columns, either immobilized or coated, chlorinated or nonchlorinated, cellulose or amylose-based chiral stationary phases (CSPs). Four novel triazoles and two marketed ones (tebuconazole and hexaconazole) were separated to determine optimal resolution conditions.
View Article and Find Full Text PDFCurr Org Synth
January 2025
Department of Chemistry, Constituent Govt. College, (MJP. Rohilkhand University Bareilly) Hasanpur, (UP), 244241, India.
Introduction: Quinazoline holds significant importance in pharmaceutical chemistry, which is included in a range of drugs, clinical contenders, and bioactive compounds. N-contain-ing heterocyclic compounds of quinazoline have a wide and distinct range of biopharmaceutical activities.
Methods: A series of newly synthesized heterocyclic compounds, namely, N-(4-substituted ben-zylidene)-2-(2-aminothiazol-4-yl)-6-methylquinazolin-3(4H)-amines (3a'-3e') and N-(4-substi-tuted benzylidene)-2-(2-aminooxazol-4-yl)-6-methylquinazolin-3(4H)-amines (3a-3e), were synthesized starting from 6-methylquinazolin-3(4H)-amine and 4-substituted benzaldehyde and their antibacterial and antifungal properties were evaluated.
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