具有双壬基链的阳离子脂基苯甲酰胺分子的生物膜抑制和抗念珠菌活性
Biofilm inhibition and anti-Candida activity of a cationic lipo-benzamide molecule with twin-nonyl chain.
作者信息
Jain Tushar, Muktapuram Prathap Reddy, Sharma Komal, Ravi Owk, Pant Garima, Mitra Kalyan, Bathula Surendar Reddy, Banerjee Dibyendu
机构信息
Molecular and Structural Biology Division, CSIR-Central Drug Research Institute, Lucknow 226 031, UP, India; Academy of Scientific and Innovative Research (AcSIR), Chennai, India.
Natural Products Chemistry Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India.
出版信息
Bioorg Med Chem Lett. 2018 Jun 1;28(10):1776-1780. doi: 10.1016/j.bmcl.2018.04.024. Epub 2018 Apr 12.
A series of cationic lipo-benzamide compounds with varying lengths of hydrocarbon chains (C2M-C18M) were evaluated for anti-Candida activity. Four compounds harbouring 8-11 hydrocarbon chains demonstrated concentration-dependent inhibition of fungal cell growth with Minimum Inhibitory Concentration (MIC) of ≤6.2 µg ml. The most active compound (C9M) inhibited growth of both Candida albicans and non-albicans strains and is equally active against pairs of azole sensitive and resistant clinical isolates of C. albicans. Compound C9M also inhibited different stages of Candida biofilms. Scanning Electron Microscopy (SEM) of Candida cells after C9M treatment was also done and no significant cell lysis was observed. Hemolysis assay was performed and only 2.5% haemolysis was observed at MIC concentration.
评估了一系列具有不同碳氢链长度（C2M - C18M）的阳离子脂基苯甲酰胺化合物的抗念珠菌活性。四种含有8 - 11个碳氢链的化合物表现出对真菌细胞生长的浓度依赖性抑制，最低抑菌浓度（MIC）≤6.2 µg/ml。活性最强的化合物（C9M）抑制白色念珠菌和非白色念珠菌菌株的生长，并且对白色念珠菌的唑类敏感和耐药临床分离株对同样有效。化合物C9M还抑制念珠菌生物膜的不同阶段。对经C9M处理后的念珠菌细胞进行了扫描电子显微镜（SEM）观察，未观察到明显的细胞裂解。进行了溶血试验，在MIC浓度下仅观察到2.5%的溶血。
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