Suppr超能文献

酚衍生的双(吲哚基)甲烷与氟康唑联合抗白色念珠菌的合成及抗真菌活性评价。

Synthesis and antifungal evaluation of phenol-derived bis(indolyl)methanes combined with FLC against Candida albicans.

机构信息

School of Chinese Materia Medica, Yunnan University of Chinese Medicine, Kunming 650500, PR China.

School of Chinese Materia Medica, Yunnan University of Chinese Medicine, Kunming 650500, PR China.

出版信息

Bioorg Med Chem Lett. 2022 Feb 15;58:128525. doi: 10.1016/j.bmcl.2022.128525. Epub 2022 Jan 5.

Abstract

With the widespread use of azole antifungals in the clinic, the drug resistance has been emerging continuously. In this work, we focus on boron trifluoride etherate catalyzed condensation of indole and salicylaldehydes to form bis(indolyl)methanes (BIMs) in high yields, and in vitro antifungal activity against Candida albicans were evaluated. The results showed that most phenol-derived BIMs combined with fluconazole (FLC) exhibited good antifungal activity against sensitive and drug-resistant C. albicans. Further mechanism study demonstrated that BI-10 combined with FLC could inhibit hyphal growth, result in ROS accumulation, and decrease mitochondrial membrane potential (MMP) as well as altering membrane permeability.

摘要

随着唑类抗真菌药物在临床上的广泛应用,耐药性不断出现。在这项工作中,我们专注于三氟化硼乙醚催化吲哚和水杨醛缩合形成双(吲哚基)甲烷(BIMs),产率高,并对体外抗白色念珠菌的活性进行了评估。结果表明,大多数酚衍生的 BIMs 与氟康唑(FLC)结合表现出对敏感和耐药白色念珠菌的良好抗真菌活性。进一步的机制研究表明,BI-10 与 FLC 联合使用可以抑制菌丝生长,导致 ROS 积累,并降低线粒体膜电位(MMP)以及改变膜通透性。

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验