Antifungal Activity of 1,4-Dialkoxynaphthalen-2-Acyl Imidazolium Salts by Inducing Apoptosis of Pathogenic Candida spp

• Published in: Pharmaceutics Vol. 13; no. 3; p. 312
• Main Authors: Lee, Jisue, Kim, Jae-Goo, Lee, Haena, Lee, Tae Hoon, Kim, Ki-Young, Kim, Hakwon
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI 27.02.2021; MDPI AG
• Subjects: 1,4-Dialkoxynaphthalen-2-acyl imidazolium salts; antifungal agent; apoptosis; Candida sp; antifungal agent; apoptosis; 1,4-Dialkoxynaphthalen-2-acyl imidazolium salts; Candida sp
• ISSN: 1999-4923; 1999-4923
• DOI: 10.3390/pharmaceutics13030312

Even though spp. are staying commonly on human skin, it is also an opportunistic pathogenic fungus that can cause candidiasis. The emergence of resistant 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- 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 showed strongest antifungal activity with 3.125 μg/mL MIC value compared with miconazole which showed 12.5 μg/mL MIC value against spp., and more importantly >100 μg/mL MIC value against . The production of reactive oxygen species (ROS) was increased and JC-1 staining showed the loss of mitochondrial membrane potential in by treatment with NAIMS . The increased release of ultraviolet (UV) absorbing materials suggested that NAIMS could cause cell busting. The expression of apoptosis-related genes was induced in by NAIMS treatment. Taken together, the synthetic NAIMSs are of high interest as novel antifungal agents given further in vivo examination.