Abstract
Aspergillus genus causes many diseases, and the species Aspergillus flavus is highly virulent. Treatment of aspergillosis involves azole derivatives such as voriconazole and polyenes such as amphotericin B. Due to an increase in fungal resistance, treatments are now less effective; the search for new compounds with promising antifungal activity has gained importance. The aims of this study were to evaluate the effects of the synthetic amide 2-chloro-N-phenylacetamide (A1Cl) against strains of Aspergillus flavus and to elucidate its mechanism of action. Thus, the minimum inhibitory concentration, minimum fungicidal concentration, conidial germination, associations with antifungal agents, cell wall activities, membrane activities and molecular docking were evaluated. A1Cl presented antifungal activity against Aspergillus flavus strains with a minimum inhibitory concentration of between 16 and 256 μg/mL and a minimum fungicidal concentration between 32 and 512 μg/mL. The minimum inhibitory concentration of A1Cl also inhibited conidial germination, but when associated with amphotericin B and voriconazole, it promoted antagonistic effects. Binding to ergosterol on the fungal plasma membrane is the likely mechanism of action, along with possible inhibition of DNA synthesis through the inhibition of thymidylate synthase. It is concluded that the amide 2-chloro-N-phenylacetamide has promising antifungal potential.
Highlights
Aspergillus genus comprises more than 250 species; it is one of the largest genera of filamentous fungi that cause human disease (Rudramurthy et al 2019)
The product A1Cl presented Minimum inhibitory concentration (MIC) that varied from 16 to 256 μg/mL, as shown in Table II, inhibiting visible growth of A. flavus strains used in this study
Regarding the standard antifungal amphotericin B, it was noted that the strains presented MICs that varied between 1 and 16 μg/mL, with 8 out of 12 presenting MICs of > 2 μg/mL, while the minimum fungicidal concentration (MFC) of amphotericin B for the tested strains ranged from 2 to 32 μg/mL (Table II)
Summary
Aspergillus genus comprises more than 250 species; it is one of the largest genera of filamentous fungi that cause human disease (Rudramurthy et al 2019). Aspergillus species A. fumigatus, A. flavus, A. niger, A. terreus and A. versicolor are frequently involved in diseases, such as rhinosinusitis, cutaneous and subcutaneous aspergillosis, pulmonary infections, cardiac infections, otomycosis, among others (Barnes & Marr 2006, Sugui et al 2014, Rudramurthy et al 2019). The genus, in general, presents low pathogenicity for humans, and it requires a large inoculum to infect immunocompromised individuals if their physiological performance is intact. A. fumigatus species is the agent most commonly involved in aspergillosis and it is one of the most commonly studied species
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