Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, SCME, East China Normal University, Shanghai 200062, China.
Center for Research and Development of Fine Chemicals of Guizhou University, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guiyang 550225, China; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Eur J Med Chem. 2017 Feb 15;127:424-433. doi: 10.1016/j.ejmech.2017.01.012. Epub 2017 Jan 9.
A series of novel 9, 13-disubstituted berberine derivatives have been synthesized and evaluated for the antibacterial activities against Staphylococcus aureus, including Newman strain and multidrug-resistant strains (NRS-1, NRS-70, NRS-100, NRS-108, and NRS-271). Compound 20 shows the most potent activity against the growth of Newman strain, with a MIC value of 0.78 μg/mL, which is comparable with the positive control vancomycin. In addition, compound 20, 21, and 33 are highly antistaphylococcal active against five strains of multidrug-resistant S. aureus, with MIC values of 0.78-1.56 μg/mL. Of note, theses antibacterial active compounds have no obvious toxicity to the viability of human fibroblast (HAF) cells at the MIC concentration.
已经合成了一系列新型的 9,13-二取代小檗碱衍生物，并评估了它们对金黄色葡萄球菌（包括 Newman 株和多药耐药株（NRS-1、NRS-70、NRS-100、NRS-108 和 NRS-271）的抗菌活性。化合物 20 对 Newman 株的生长表现出最强的抑制活性，MIC 值为 0.78 μg/mL，与阳性对照万古霉素相当。此外，化合物 20、21 和 33 对五种多药耐药金黄色葡萄球菌株具有高度的抗葡萄球菌活性，MIC 值为 0.78-1.56 μg/mL。值得注意的是，这些具有抗菌活性的化合物在 MIC 浓度下对人成纤维细胞（HAF）的活力没有明显的毒性。
