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Antifungal Activity of 1,4-Dialkoxynaphthalen-2-Acyl Imidazolium Salts by Inducing Apoptosis of Pathogenic <i>Candida</i> spp.
oleh: Jisue Lee, Jae-Goo Kim, Haena Lee, Tae Hoon Lee, Ki-Young Kim, Hakwon Kim
Format: | Article |
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Diterbitkan: | MDPI AG 2021-02-01 |
Deskripsi
Even though <i>Candida</i> spp. are staying commonly on human skin, it is also an opportunistic pathogenic fungus that can cause candidiasis. The emergence of resistant <i>Candida</i> strains and the toxicity of antifungal agents have encouraged the development of new classes of potent antifungal agents. Novel naphthalen-2-acyl imidazolium salts (NAIMSs), especially 1,4-dialkoxy-NAIMS from 1,4-dihydroxynaphthalene, were prepared and evaluated for antifungal activity. Those derivatives showed prominent anti-<i>Candida</i> activity with a minimum inhibitory concentration (MIC) of 3.125 to 6.26 μg/mL in 24 h based on microdilution antifungal susceptibility test. Among the tested compounds, NAIMS <b>7c</b> showed strongest antifungal activity with 3.125 μg/mL MIC value compared with miconazole which showed 12.5 μg/mL MIC value against <i>Candida</i> spp., and more importantly >100 μg/mL MIC value against <i>C. auris</i>. The production of reactive oxygen species (ROS) was increased and JC-1 staining showed the loss of mitochondrial membrane potential in <i>C. albicans</i> by treatment with NAIMS <b>7c</b>. The increased release of ultraviolet (UV) absorbing materials suggested that NAIMS <b>7c</b> could cause cell busting. The expression of apoptosis-related genes was induced in <i>C. albicans</i> by NAIMS <b>7c</b> treatment. Taken together, the synthetic NAIMSs are of high interest as novel antifungal agents given further in vivo examination.