ArticleBMC complementary and alternative medicine2013
Trans-chalcone and quercetin down-regulate fatty acid synthase gene expression and reduce ergosterol content in the human pathogenic dermatophyte Trichophyton rubrum.
Article in BMC complementary and alternative medicine, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers, 1 of them a synthesis that pooled it.
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Who cites it
29 citing papers in PubMed, 1 synthesis or guideline pooled it, 70 citations in OpenAlex.
- Exploring the therapeutic potential and chemical properties of trans-chalcone: a comprehensive review.Future medicinal chemistry · 2024Pooled it
- Role of Polyphenols in Dermatological Diseases: Exploring Pharmacotherapeutic Mechanisms and Clinical Implications.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Integration of Transcriptomics and Proteomics to Elucidate Inhibitory Effect and Mechanism of Antifungalmycin B from MarineMarine drugs · 2025Article
- The Role of Quercetin, a Flavonoid in the Management of Pathogenesis Through Regulation of Oxidative Stress, Inflammation, and Biological Activities.Biomolecules · 2025Review
- Multi-target mechanisms and potential applications of quercetin in the treatment of acne vulgaris.Frontiers in pharmacology · 2025Review
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- Azorean Black Tea (Molecules (Basel, Switzerland) · 2023Article
- Screening antibiofilm activity of invasive plants growing at the Slope Merapi Mountain, Central Java, against Candida albicans.BMC complementary medicine and therapies · 2023Article
- The Chemical Profile, and Antidermatophytic, Anti-Inflammatory, Antioxidant and Antitumor Activities ofPlants (Basel, Switzerland) · 2023Article
- Novel eco-friendly [1,2,4]triazolo[3,4-a]isoquinoline chalcone derivatives efficiency against fungal deterioration of ancient Egyptian mummy cartonnage, Egypt.Archives of microbiology · 2023Article
- Hepatoprotective and antifibrotic effects ofIranian journal of basic medical sciences · 2023Article
- Synergistic activity of the combination of falcarindiol and itraconazoleFrontiers in cellular and infection microbiology · 2023Article
- 2Microbiology spectrum · 2022Article
- Antimicrobial Activity of Quercetin: An Approach to Its Mechanistic Principle.Molecules (Basel, Switzerland) · 2022Review
- Review
- Appraisal of selected ethnomedicinal plants as alternative therapies against onychomycosis: Evaluation of synergy and time-kill kinetics.Frontiers in pharmacology · 2022Article
- Profiling of Antifungal Activities and In Silico Studies of Natural Polyphenols from Some Plants.Molecules (Basel, Switzerland) · 2021Article
- Epidemiology and Diagnostic Perspectives of Dermatophytoses.Journal of fungi (Basel, Switzerland) · 2020Review
- Antifungal Activity of Phenolic and Polyphenolic Compounds from Different Matrices ofMolecules (Basel, Switzerland) · 2020Review
- Anti-Fungal Efficacy and Mechanisms of Flavonoids.Antibiotics (Basel, Switzerland) · 2020Review
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundFatty acid synthase (FAS) is a promising antifungal target due to its marked structural differences between fungal and mammalian cells. The aim of this study was to evaluate the antifungal activity of flavonoids described in the scientific literature as FAS inhibitors (quercetin, trans-chalcone, ellagic acid, luteolin, galangin, and genistein) against the dermatophyte Trichophyton rubrum and their effects on fatty acid and ergosterol synthesis.
methodsThe antifungal activity of the natural products was tested by the microdilution assay for determination of the minimum inhibitory concentration (MIC). The effect of the compounds on the cell membrane was evaluated using a protoplast regeneration assay. Ergosterol content was quantified by spectrophotometry. Inhibition of FAS by flavonoids was evaluated by an enzymatic assay to determine IC50 values. Quantitative RT-PCR was used to measure transcription levels of the FAS1 and ERG6 genes involved in fatty acid and ergosterol biosynthesis, respectively, during exposure of T. rubrum to the flavonoids tested.
resultsThe flavonoids quercetin and trans-chalcone were effective against T. rubrum, with MICs of 125 and 7.5 μg/mL for the wild-type strain (MYA3108) and of 63 and 1.9 μg/mL for the ABC transporter mutant strain (ΔTruMDR2), respectively. The MICs of the fluconazole and cerulenin controls were 63 and 125 μg/mL for the wild-type strain and 30 and 15 μg/mL for the mutant strain, respectively. Quercetin and trans-chalcone also reduced ergosterol content in the two strains, indicating that interference with fatty acid and ergosterol synthesis caused cell membrane disruption. The MIC of quercetin reduced the number of regenerated protoplasts by 30.26% (wild-type strain) and by 91.66% (mutant strain). Half the MIC (0.5 MIC) of quercetin did not reduce the number of regenerated wild-type fungal colonies, but caused a 36.19% reduction in the number of mutant strain protoplasts. In contrast, the MIC and 0.5 MIC of trans-chalcone and cerulenin drastically reduced protoplast regeneration in the two strains. The FAS1 gene was repressed in the presence of MICs of quercetin, trans-chalcone, fluconazole and cerulenin. The ERG6 gene was induced in the presence of MICs of fluconazole and cerulenin and was repressed in the presence of MICs of trans-chalcone and quercetin. Trans-chalcone and quercetin inhibited the enzymatic activity of FAS, with IC50 values of 68.23 and 17.1 μg/mL, respectively.
conclusionTrans-chalcone and quercetin showed antifungal activity against T. rubrum, reducing ergosterol levels and modulating the expression of FAS1 and ERG6.
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