新型荧光头孢菌素：合成、抗菌活性及光动力灭活耐药菌。
Novel fluorescent cephalosporins: synthesis, antimicrobial activity and photodynamic inactivation of antibiotic resistant bacteria.
机构信息
Key Laboratory of Synthetic and Natural Functional Molecule Chemistry of Ministry of Education, College of Chemistry and Materials Science, Northwest University, Xi'an 710069, PR China.
出版信息
Eur J Med Chem. 2013 Jan;59:150-9. doi: 10.1016/j.ejmech.2012.11.019. Epub 2012 Nov 21.
Two novel fluorescent cephalosporins, TCA and TBCA, were synthesized and characterized by (1)H NMR, (13)C NMR, UV-vis, and fluorescence spectroscopies. Biological activity assays demonstrated that TCA inactivated a Klebsiella pneumonia strain that expressed extended-spectrum β-lactamases. Incubation of 6 μM TCA with K. pneumonia cultures resulted in cell death for 84% of the cells after 126 J/cm(2) of light irradiation. In vitro, TCA exhibited a MIC = 0.5 μg/mL with Staphylococcus aureus. Kinetic evaluation revealed that TCA and TBCA were substrates for B1 and B3 subclass metallo-β-lactamases. TBCA exhibited stronger binding affinities to the Gram-positive bacterial strains MRSA1, MRSA2, and S. aureus with value of 2.95-6.59 μM per 10(8) cells/mL.
两种新型荧光头孢菌素 TCA 和 TBCA 通过 1H NMR、13C NMR、UV-vis 和荧光光谱学进行了合成和表征。生物活性测定表明，TCA 使表达超广谱β-内酰胺酶的肺炎克雷伯菌菌株失活。用 6 μM TCA 孵育肺炎克雷伯菌培养物，在 126 J/cm(2)的光照射后，84%的细胞发生细胞死亡。在体外，TCA 对金黄色葡萄球菌的 MIC = 0.5 μg/mL。动力学评估表明，TCA 和 TBCA 是 B1 和 B3 亚类金属β-内酰胺酶的底物。TBCA 与革兰氏阳性菌菌株 MRSA1、MRSA2 和金黄色葡萄球菌的结合亲和力更强，每个 10(8)个细胞/mL 的值为 2.95-6.59 μM。
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