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A Water-Soluble Galactose-Decorated Cationic Photodynamic Therapy Agent Based on BODIPY to Selectively Eliminate Biofilm
journal contribution
posted on 2017-11-15, 00:00 authored by Xiaomei Dai, Xuelei Chen, Yu Zhao, Yunjian Yu, Xiaosong Wei, Xinge Zhang, Chaoxing LiA multitude
of serious chronic infections are involved in bacterial biofilms that
are difficult to eradicate. Here, a water-soluble galactose-functionalized
cationic 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene (BODIPY)-based
photodynamic therapy agent was synthesized for selectively eliminating
the bacterial biofilm. These conjugates can capture bacteria to form
aggregations through electrostatic interaction and then generate a
large number of reactive oxygen species (ROS) under visible light
irradiation to kill the bacteria without the emergence of bacterial
resistance. Simultaneously, this agent could effectively inhibit and
eradicate both Gram-positive and Gram-negative bacterial biofilms.
The in-depth analysis of the antimicrobial mechanism confirmed that
the conjugates can quickly bind on the bacterial surface, irreversibly
disrupt the bacterial membrane, and distinctly inhibit intracellular
enzyme activity, ultimately leading to the bacterial death. Importantly,
these conjugates are highly selective toward bacterial cells over
mammalian cells as well as no cytotoxicity to A549 cells and no discernible
hemolytic activity. Collectively, this water-soluble galactose-decorated
cationic BODIPY-based photodynamic therapy agent design provides promising
insights for the development of therapy for antibiotic-resistant bacteria.
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biofilmreactive oxygen speciesconjugateantibiotic-resistant bacterialight irradiationintracellular enzyme activityWater-Soluble Galactose-Decorated Cationic Photodynamic Therapy Agentantimicrobial mechanismROSform aggregations549 cellsgalactose-decorated cationic BODIPY-based photodynamic therapy agent design
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