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Broth Microdilution In Vitro Screening: An Easy and Fast Method to Detect New Antifungal Compounds
Published on: February 14, 2018
In Silico and In Vitro Analysis of Sulforaphane Anti-Candida Activity
Bruna L R Silva1, Gisele Simão2,3, Carmem D L Campos4
1Programa de Pós-Graduação em Biodiversidade e Biotecnologia da Rede BIONORTE, Universidade Federal do Maranhão, São Luís 65085-040, MA, Brazil.
Abstract:
Oropharyngeal candidiasis/candidosis is a common and recurrent opportunistic fungal infection. Fluconazole (FLZ), one of the most used and effective antifungal agents, has been associated with a rise of resistant Candida species in immunocompromised patients undergoing prophylactic therapy. Sulforaphane (SFN), a compound from cruciferous vegetables, is an antimicrobial with yet controversial activities and mechanisms on fungi. Herein, the in silico and antifungal activities of SFN against C. albicans were investigated. In silico analyzes for the prediction of the biological activities and oral bioavailability of SFN, its possible toxicity and pharmacokinetic parameters, as well as the estimates of its gastrointestinal absorption, permeability to the blood-brain barrier and skin, and similarities to drugs, were performed by using different software. SFN in vitro anti-Candida activities alone and in combination with fluconazole (FLZ) were determined by the broth microdilution method and the checkerboard, biofilm and hyphae formation tests. Amongst the identified probable biological activities of SFN, nine indicated an antimicrobial potential. SFN was predicted to be highly absorbable by the gastrointestinal tract, to present good oral availability, and not to be irritant and/or hepatotoxic. SFN presented antifungal activity against C. albicans and prevented both biofilm and hyphae formation by this microorganism. SFN was additive/synergistic to FLZ. Overall, the data highlights the anti-Candida activity of SFN and its potential to be used as an adjuvant therapy to FLZ in clinical settings.
Insights
Sulforaphane (SFN) shows antifungal activity against Candida albicans and prevents biofilm formation. SFN demonstrates additive/synergistic effects with fluconazole (FLZ), suggesting its potential as an adjuvant therapy for fungal infections.
Area of Science:
- Mycology
- Pharmacology
- Computational Biology
Background:
- Oropharyngeal candidiasis is a common opportunistic fungal infection.
- Fluconazole resistance in Candida species is increasing, particularly in immunocompromised patients.
- Sulforaphane (SFN), a cruciferous vegetable compound, has antimicrobial properties with debated efficacy against fungi.
Purpose of the Study:
- To investigate the in silico and in vitro antifungal activities of Sulforaphane (SFN) against Candida albicans.
- To evaluate SFN's potential as an adjuvant therapy in combination with fluconazole (FLZ).
Main Methods:
- In silico analyses predicted SFN's biological activities, bioavailability, toxicity, and pharmacokinetic parameters.
- In vitro antifungal activity was assessed using broth microdilution and checkerboard assays.
- Biofilm and hyphae formation inhibition by SFN were evaluated.
Main Results:
- In silico predictions indicated SFN possesses antimicrobial potential, good oral bioavailability, and low toxicity.
- SFN demonstrated significant in vitro antifungal activity against Candida albicans.
- SFN effectively inhibited biofilm and hyphae formation by Candida albicans.
- SFN exhibited additive to synergistic effects when combined with fluconazole.
Conclusions:
- SFN possesses notable anti-Candida activity and favorable pharmacokinetic predictions.
- SFN effectively inhibits Candida albicans biofilm and hyphae development.
- SFN shows promise as an adjuvant therapy to fluconazole for treating candidiasis.

