Fe(II)-Photoantibioticsfor Potential Antibacterial,Antibiofilm, and Infective Wound Healing Applications in Rat Model

Herein, five Fe(II) complexes, viz., [Fe(<i>N</i>,<i>N</i>,<i>N</i>)<sub>2</sub>](ClO<sub>4</sub>)<sub>2</sub>, where <i>N</i>,<i>N</i>,<i>N</i> = 4′-phenyl-2,2′:6′,2″-terpyridine (Ph-tpy, <b>Fe1</b>), 4′-(4 aminophenyl) 2,2′:6′,2″ terpyridine (NH<sub>2</sub>-Phtpy, <b>Fe2</b>), 4-([2,2′:6′,2′′-terpyridin]-4′-yl)-<i>N</i>,<i>N</i>-dimethylaniline (NMe<sub>2</sub>-Phtpy, <b>Fe3</b>), 4′-(<i>p</i>-nitrophenyl)-2.2′:6′,2″-terpyridine (NO<sub>2</sub>-Phtpy, <b>Fe4</b>), and 4′-(4-trifluoromethylphenyl)-2,2’:6′,2′′-terpyridine (CF<sub>3</sub>-Phtpy, <b>Fe5</b>) were developed and screened for their visible-light-triggered antibacterial activity. <b>Fe1</b>–<b>Fe5</b> exhibited absorption at <i>ca</i>. 450–600 nm, beneficial for antibacterial photodynamic therapy (aPDT) under visible light exposure. The excellent photostability and ideal energy gap between T<sub>1</sub> and S<sub>0</sub> of the complexes made them good photosensitizers for aPDT. <b>Fe5</b> had the best antibacterial activity against <i>Escherichia coli</i> and <i>Bacillus subtilis</i> upon exposure to 400–700 nm (10 J cm<sup>–2</sup>) light due to reactive oxygen species (ROS) generation. Further, <b>Fe5</b> showed antibiofilm activity on different medical-grade biomaterials and devices. Biocompatibility of <b>Fe5</b> was validated using <i>in vivo</i> and chicken embryonic models (<i>in ovo</i>). Moreover, <i>in vivo</i> studies showed that <b>Fe5</b> efficiently healed infected wounds within 9 days.

Publication Details

Journal
Figshare
Published
2025-02-06
DOI
https://doi.org/10.1021/acs.jmedchem.4c02405.s001
Primary Topic
E-commerce and Technology Innovations
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article
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article

Fe(II)-Photoantibioticsfor Potential Antibacterial,Antibiofilm, and Infective Wound Healing Applications in Rat Model

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E-commerce and Technology Innovations
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Fe(II)-Photoantibioticsfor Potential Antibacterial,Antibiofilm, and Infective Wound Healing Applications in Rat Model

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Abstract

Herein, five Fe(II) complexes, viz., [Fe(<i>N</i>,<i>N</i>,<i>N</i>)<sub>2</sub>](ClO<sub>4</sub>)<sub>2</sub>, where <i>N</i>,<i>N</i>,<i>N</i> = 4′-phenyl-2,2′:6′,2″-terpyridine (Ph-tpy, <b>Fe1</b>), 4′-(4 aminophenyl) 2,2′:6′,2″ terpyridine (NH<sub>2</sub>-Phtpy, <b>Fe2</b>), 4-([2,2′:6′,2′′-terpyridin]-4′-yl)-<i>N</i>,<i>N</i>-dimethylaniline (NMe<sub>2</sub>-Phtpy, <b>Fe3</b>), 4′-(<i>p</i>-nitrophenyl)-2.2′:6′,2″-terpyridine (NO<sub>2</sub>-Phtpy, <b>Fe4</b>), and 4′-(4-trifluoromethylphenyl)-2,2’:6′,2′′-terpyridine (CF<sub>3</sub>-Phtpy, <b>Fe5</b>) were developed and screened for their visible-light-triggered antibacterial activity. <b>Fe1</b>–<b>Fe5</b> exhibited absorption at <i>ca</i>. 450–600 nm, beneficial for antibacterial photodynamic therapy (aPDT) under visible light exposure. The excellent photostability and ideal energy gap between T<sub>1</sub> and S<sub>0</sub> of the complexes made them good photosensitizers for aPDT. <b>Fe5</b> had the best antibacterial activity against <i>Escherichia coli</i> and <i>Bacillus subtilis</i> upon exposure to 400–700 nm (10 J cm<sup>–2</sup>) light due to reactive oxygen species (ROS) generation. Further, <b>Fe5</b> showed antibiofilm activity on different medical-grade biomaterials and devices. Biocompatibility of <b>Fe5</b> was validated using <i>in vivo</i> and chicken embryonic models (<i>in ovo</i>). Moreover, <i>in vivo</i> studies showed that <b>Fe5</b> efficiently healed infected wounds within 9 days.

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