Lee Jisue, Kim Jae-Goo, Lee Haena, Lee Tae Hoon, Kim Ki-Young, Kim Hakwon
Department of Applied Chemistry, Global Center for Pharmaceutical Ingredient Materials, Kyung Hee University, Seocheon, Giheung, Yongin, Gyeonggi-do 1732, Korea.
Graduate School of Biotechnology, Kyung Hee University, Seocheon, Giheung, Yongin, Gyeonggi-do 1732, Korea.
Pharmaceutics. 2021 Feb 27;13(3):312. 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.
尽管 spp. 通常存在于人体皮肤上，但它也是一种机会致病性真菌，可引起念珠菌病。耐药菌株的出现和抗真菌药物的毒性促使开发新型强效抗真菌药物。制备了新型萘 - 2 - 酰基咪唑盐（NAIMSs），特别是由 1,4 - 二羟基萘衍生的 1,4 - 二烷氧基 - NAIMSs，并对其抗真菌活性进行了评估。基于微量稀释抗真菌药敏试验，这些衍生物在 24 小时内显示出显著的抗活性，最低抑菌浓度（MIC）为 3.125 至 6.26 μg/mL。在测试的化合物中，NAIMS 显示出最强的抗真菌活性，MIC 值为 3.125 μg/mL，而咪康唑对 spp. 的 MIC 值为 12.5 μg/mL，更重要的是对 的 MIC 值>100 μg/mL。用 NAIMS 处理后， 中活性氧（ROS）的产生增加，JC - 1 染色显示线粒体膜电位丧失。紫外线（UV）吸收物质释放增加表明 NAIMS 可导致细胞破裂。NAIMS 处理诱导了 中凋亡相关基因的表达。综上所述，鉴于进一步的体内研究，合成的 NAIMSs 作为新型抗真菌药物具有很高的研究价值。
