Improving Photodynamic Inactivation of Bacteria in Dentistry: Highly Effective and Fast Killing of Oral Key Pathogens with Novel Tooth-Colored Type-II Photosensitizers

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• 作者：Andreas Sp盲th ; Christoph Leibl ; Fabian Cieplik ; Karin Lehner ; Johannes Regensburger ; Karl-Anton Hiller ; Wolfgang B盲umler ; Gottfried Schmalz ; Tim Maisch
• 刊名：Journal of Medicinal Chemistry
• 出版年：2014
• 出版时间：June 26, 2014
• 年：2014
• 卷：57
• 期：12
• 页码：5157-5168
• 全文大小：652K
• ISSN：1520-4804

文摘

Increasing antibiotic resistances in microorganisms create serious problems in public health. This demands alternative approaches for killing pathogens to supplement standard treatment methods. Photodynamic inactivation of bacteria (PIB) uses light activated photosensitizers (PS) to generate reactive oxygen species immediately upon illumination, inducing lethal phototoxicity. Positively charged phenalen-1-one derivatives are a new generation of PS for light-mediated killing of pathogens with outstanding singlet oxygen quantum yield 桅<sub>螖sub> of >97%. Upon irradiation with a standard photopolymerizer light (bluephase C8, 1260 卤 50 mW/cm<sup>2sup>) the PS showed high activity against the oral key pathogens Enterococcus faecalis, Actinomyces naeslundii, Streptococcus mutans, and Aggregatibacter actinomycetemcomitans. At a concentration of 10 渭M, a maximum efficacy of more than 6 log<sub>10sub> steps (鈮?9.9999%) of bacteria killing is reached in less than 1 min (light dose 50 J/cm<sup>2sup>) after one single treatment. The pyridinium substituent as positively charged moiety is especially advantageous for antimicrobial action.