ArticleFrontiers in microbiology2015
Screening of Pharmacologically Active Small Molecule Compounds Identifies Antifungal Agents Against Candida Biofilms.
Article in Frontiers in microbiology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 37 citations in OpenAlex.
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- A novel pan-fungal screening platform for antifungal drug discovery: proof of principle study.Antimicrobial agents and chemotherapy · 2025Article
- Identification of polycystin 2 missense mutants targeted for endoplasmic reticulum-associated degradation.American journal of physiology. Cell physiology · 2025Article
- Recent drug development and treatments for fungal infections.Brazilian journal of microbiology : [publication of the Brazilian Society for Microbiology] · 2023Review
- High-Throughput Screening of the Repurposing Hub Library to Identify Drugs with Novel Inhibitory Activity againstJournal of fungi (Basel, Switzerland) · 2023Article
- Imaging-Based Screening Identifies Modulators of theAntimicrobial agents and chemotherapy · 2023Article
- Imaging-based screening identifies modulators of thebioRxiv : the preprint server for biology · 2023Article
- Triazine-Based Small Molecules: A Potential New Class of Compounds in the Antifungal Toolbox.Pathogens (Basel, Switzerland) · 2023Article
- High-Throughput In Vitro Screening Identified Nemadipine as a Novel Suppressor of Embryo Implantation.International journal of molecular sciences · 2022Article
- Cell-Based Double-Screening Method to Identify a Reliable Candidate for Osteogenesis-Targeting Compounds.Biomedicines · 2022Article
- Identification of a small molecule 0390 as a potent antimicrobial agent to combat antibiotic-resistantFrontiers in microbiology · 2022Article
- Platforms for High-Throughput Screening and Force Measurements on Fungi and Oomycetes.Micromachines · 2021Review
- A Screen for Small Molecules to TargetJournal of fungi (Basel, Switzerland) · 2020Article
- Antifungal drug screening: thinking outside the box to identify novel antifungal scaffolds.Current opinion in microbiology · 2020Review
- Screening Repurposing Libraries for Identification of Drugs with Novel Antifungal Activity.Antimicrobial agents and chemotherapy · 2020Review
- Current Antimycotics, New Prospects, and Future Approaches to Antifungal Therapy.Antibiotics (Basel, Switzerland) · 2020Review
- Synthesis and Evaluation of Novel Ellipticines and Derivatives as Inhibitors ofPathogens (Basel, Switzerland) · 2020Article
- Inhibitory Properties of Aldehydes and Related Compounds againstPathogens (Basel, Switzerland) · 2020Article
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Authors and funding
4 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Candida species have emerged as important and common opportunistic human pathogens, particularly in immunocompromised individuals. The current antifungal therapies either have toxic side effects or are insufficiently effect. The aim of this study is develop new small-molecule antifungal compounds by library screening methods using Candida albicans, and to evaluate their antifungal effects on Candida biofilms and cytotoxic effects on human cells. Wild-type C. albicans strain SC5314 was used in library screening. To identify antifungal compounds, we screened a small-molecule library of 1,280 pharmacologically active compounds (LOPAC(1280TM)) using an antifungal susceptibility test (AST). To investigate the antifungal effects of the hit compounds, ASTs were conducted using Candida strains in various growth modes, including biofilms. We tested the cytotoxicity of the hit compounds using human gingival fibroblast (hGF) cells to evaluate their clinical safety. Only 35 compounds were identified by screening, which inhibited the metabolic activity of C. albicans by >50%. Of these, 26 compounds had fungistatic effects and nine compounds had fungicidal effects on C. albicans. Five compounds, BAY11-7082, BAY11-7085, sanguinarine chloride hydrate, ellipticine and CV-3988, had strong fungicidal effects and could inhibit the metabolic activity of Candida biofilms. However, BAY11-7082, BAY11-7085, sanguinarine chloride hydrate and ellipticine were cytotoxic to hGF cells at low concentrations. CV-3988 showed no cytotoxicity at a fungicidal concentration. Four of the compounds identified, BAY11-7082, BAY11-7085, sanguinarine chloride hydrate and ellipticine, had toxic effects on Candida strains and hGF cells. In contrast, CV-3988 had fungicidal effects on Candida strains, but low cytotoxic effects on hGF cells. Therefore, this screening reveals agent, CV-3988 that was previously unknown to be antifungal agent, which could be a novel therapies for superficial mucosal candidiasis.
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