新型诺万古霉素-荧光素缀合物用于枯草芽孢杆菌的光动力灭活。

Novel conjugation of norvancomycin-fluorescein for photodynamic inactivation of Bacillus subtilis.

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, P. R. China.

出版信息

Bioconjug Chem. 2011 Nov 16;22(11):2217-21. doi: 10.1021/bc200382d. Epub 2011 Oct 26.

DOI:10.1021/bc200382d

PMID:21999249

Abstract

A simple and unique conjugation of norvancomycin-fluorescein (VanF) has been achieved. It was characterized by UV-vis and fluorescence spectra and confirmed by MALDI-TOF mass spectrum. The photodynamic assay indicated that VanF effectively inactivated the Gram-positive Bacillus subtilis (ATCC 6633) from clinic with inactivation rate of 30-70% within 1-7.5 μM. In vitro, VanF showed low antimicrobial activity with value of >128 μg/mL, binding affinity with value of 180 nM per 10(8) cells/mL against the bacteria strains. The fluorescence imaging showed that VanF could label the B. subtilis strain, but not the Escherichia coli (ATCC 25922), Enterococcus faecalis (ATCC 51299, VanD), and VRE strains from clinic.

摘要

已实现了一种简单而独特的诺万古霉素-荧光素（VanF）缀合物。通过紫外可见光谱和荧光光谱对其进行了表征，并通过 MALDI-TOF 质谱进行了确认。光动力测定表明，VanF 能有效灭活临床革兰阳性枯草芽孢杆菌（ATCC 6633），在 1-7.5 μM 范围内的灭活率为 30-70%。体外实验中，VanF 的抗菌活性值>128 μg/mL，与细菌菌株的结合亲和力值为 180 nM/每 10(8)个细胞/mL。荧光成像表明，VanF 可以标记枯草芽孢杆菌菌株，但不能标记大肠埃希菌（ATCC 25922）、粪肠球菌（ATCC 51299、VanD）和临床分离的 VRE 菌株。