Centre de Recherche en Cancérologie de Marseille (CRCM), CNRS, UMR 7258, Institut Paoli Calmette, Aix-Marseille Université UM 105, Inserm, U1068, Faculté de Pharmacie, 13385, Marseille, France.
Faculté de Médecine, Aix-Marseille Université, IRBA, TMCD2 UMR-MD1, 13385, Marseille, France.
ChemMedChem. 2018 May 23;13(10):1018-1027. doi: 10.1002/cmdc.201800073. Epub 2018 Apr 10.
The emergence of multidrug-resistant bacteria and pathogens has created an urgent need for the development of new antibiotics. Herein we report our investigations into the broad-spectrum activity of an easily prepared water-soluble polyaminosterol compound, namely claramine A1, against both drug-sensitive and drug-resistant Gram-negative and Gram-positive bacterial strains. We also report its peculiar mechanism of action, which differs from that of all the other well-known classes of antibiotics, toward Gram-negative and Gram-positive bacteria. Given their low cytotoxicity, this class of compounds based on claramine A1 could constitute an effective response to combat the emergence of multidrug-resistant bacteria and nosocomial diseases.
多药耐药菌和病原体的出现，催生了对新型抗生素的迫切需求。在此，我们报告了一种易于制备的水溶性聚氨基甾醇化合物——即克拉霉素 A1，对敏感和耐药的革兰氏阴性和革兰氏阳性菌的广谱活性的研究。我们还报告了其针对革兰氏阴性菌和革兰氏阳性菌的独特作用机制，该机制不同于所有其他已知类别的抗生素。鉴于其低细胞毒性，基于克拉霉素 A1 的此类化合物可能成为应对多药耐药菌和医院获得性疾病的有效手段。
