Wellman Center for Photomedicine, Massachusetts General Hospital, Boston, MA 02114, USA.
Department of Dermatology, Harvard Medical School, Boston, MA 02115, USA.
Future Med Chem. 2019 Sep;11(18):2427-2445. doi: 10.4155/fmc-2018-0513. Epub 2019 Sep 23.
Tetracyclines are well established antibiotics but show phototoxicity as a side effect. Antimicrobial photodynamic inactivation uses nontoxic dyes combined with harmless light to destroy microbial cells by reactive oxygen species. Tetracyclines (demeclocycline and doxycycline) can act as light-activated antibiotics by binding to bacterial cells and killing them only upon illumination. The remaining tetracyclines can prevent bacterial regrowth after illumination has ceased. Antimicrobial photodynamic inactivation can be potentiated by potassium iodide. Azide quenched the formation of iodine, but not hydrogen peroxide. Demeclotetracycline (but not doxycycline) iodinated tyrosine after light activation in the presence of potassium iodide. Bacteria are killed by photoactivation of tetracyclines in the absence of oxygen. Since topical tetracyclines are already used clinically, blue light activation may increase the bactericidal effect.
四环素类药物是一种成熟的抗生素,但会产生光毒性副作用。抗菌光动力失活作用利用无毒染料与无害光结合,通过活性氧物质来破坏微生物细胞。四环素类药物(地美环素和多西环素)可以通过与细菌细胞结合,并在光照下杀死细菌,从而作为光激活抗生素发挥作用。其余的四环素类药物可以在光照停止后防止细菌再次生长。碘化钾可以增强抗菌光动力失活作用。叠氮化物会猝灭碘的形成,但不会猝灭过氧化氢。在存在碘化钾的情况下,地美环素(而不是多西环素)在光激活后碘化酪氨酸。在没有氧气的情况下,通过光激活四环素类药物可以杀死细菌。由于局部应用的四环素类药物已在临床上使用,因此蓝光激活可能会增加杀菌效果。