Gervasi Teresa, Ginestra Giovanna, Mancuso Francesca, Barreca Davide, De Luca Laura, Mandalari Giuseppina
Department of Biomedical and Dental Sciences and Morphofunctional Imaging, University of Messina, 98125 Messina, Italy.
Department of Chemical, Biological, Pharmaceutical and Environmental Science, University of Messina, 98166 Messina, Italy.
Microorganisms. 2021 Oct 1;9(10):2070. doi: 10.3390/microorganisms9102070.
Given the increased antimicrobial resistance, global effort is currently focused on the identification of novel compounds, both of natural and chemical origin. The present study reports on the antifungal potential of 1-(1-indol-3-yl) derivatives, previously known as tyrosinase inhibitors. The effect of seven compounds (indicated as -) was determined against ATCC 10531, three clinical isolates of , two clinical isolates of , two clinical isolates of and ATCC 16404. The effect of these derivatives on tyrosinase enzymatic activity was also evaluated. Results showed a fungicidal activity of compounds , and against all tested strains at concentrations ranging between 0.250 and 1 mg/mL. Furthermore, the association between and fluconazole and between and caspofungin showed a trend of indifference tending toward synergism. Compound was also able to inhibit microbial tyrosinase up to ~28% at the concentration of 0.250 mg/mL. These data could help provide novel therapeutics for topical use to treat fungal infections and increase the potential effectiveness of the association between novel compounds and commercial antifungals in order to combat drug resistance.
鉴于抗菌耐药性的增加，目前全球的努力集中在鉴定新型化合物，包括天然来源和化学合成的化合物。本研究报道了1-(1-吲哚-3-基)衍生物（以前称为酪氨酸酶抑制剂）的抗真菌潜力。测定了七种化合物（标记为 -）对ATCC 10531、三种 临床分离株、两种 临床分离株、两种 临床分离株以及ATCC 16404的作用。还评估了这些衍生物对酪氨酸酶酶活性的影响。结果表明，化合物、和 在浓度为0.250至1 mg/mL范围内对所有测试菌株均具有杀菌活性。此外，与氟康唑以及与卡泊芬净的联合使用显示出从无相互作用趋向协同作用的趋势。化合物在浓度为0.250 mg/mL时还能够抑制微生物酪氨酸酶活性高达约28%。这些数据有助于为局部治疗真菌感染提供新型疗法，并提高新型化合物与商业抗真菌药物联合使用的潜在有效性，以对抗耐药性。
