Light Induced Antimicrobial Properties of a Brominated Boron Difluoride (BF2) Chelated Tetraarylazadipyrromethene Photosensitizer

被引:88
作者
Frimannsson, Daniel O. [1 ]
Grossi, Marco [1 ]
Murtagh, Julie [1 ]
Paradisi, Francesca [1 ]
O'Shea, Donal F. [1 ]
机构
[1] Univ Coll Dublin, Ctr Synth & Chem Biol, Sch Chem & Chem Biol, Dublin 4, Ireland
基金
爱尔兰科学基金会;
关键词
TARGETED PHOTODYNAMIC THERAPY; WOUND INFECTIONS; INACTIVATION; DERIVATIVES; RESISTANCE; PORPHYRIN; BACTERIA;
D O I
10.1021/jm100585j
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Herein we describe a new antimicrobial photodynamic therapeutic (PDT) agent based upon the brominated BF2 chelated tetraarylazadipyrromethene photosensitizer class. Bis-ammonium salt substitution of the photosensitizer promoted a rapid 10 min uptake into Gram-positive and -negative bacterial strains and pathogenic yeasts. A photosensitizer and light dose response analysis for methicillin-sensitive S. aureus showed an impressive antibacterial efficacy with 1, 2, and 5 mu g/mL 6. Specifically, light activation with a dose of 16 J/cm(2) and 5 mu g/mL 6 resulted in a 6.8 and 3.4 log(10) reduction of S. aureus and a clinically defined methicillin-resistant Staphylococcus aureus (M RSA) strain, respectively. Encouragingly, a broad spectrum pathogen response (using 5 mu g/mL 6 and 75 J/cm(2)) was observed with 3.6 and 5.7 log(10) decreases in viable cell numbers achievable for Gram-negative bacterium E. coli and the pathogenic yeast C. albicans, respectively. The photophysical and cell eradicating characteristics of this bis-cationic PDT agent suggest that it has broad potential in antimicrobial therapeutics.
引用
收藏
页码:7337 / 7343
页数:7
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