Proteomics

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A Water-Soluble Aggregation-Induced Emission Photosensitizer with Intrinsic Antibacterial Activity as an Antiplanktonic and Antibiofilm Therapeutic Agent


ABSTRACT: Photosensitizers (PS)s with aggregation-induced emission (AIE) properties have gained popularity in treating bacterial infections. However, most AIE PSs have poor water solubility and low selectivity, which greatly limit their applications in biological systems. Herein, we report a water-soluble and bacteria-targeting AIE PS, TPA-1, which showed minimum cytotoxicity towards human cells with and without light irradiation. Without light irradiation, TPA-1 acts as a narrow-spectrum antibacterial agent, eradicating planktonic S. aureus and inhibiting their biofilm formation. The mechanism study showed that TPA-1 targets S. aureus membrane, inhibits the supercoiling activity of S. aureus DNA gyrase, and causes downregulation of mulitple essential proteins. With light irradiation, TPA-1 showed excellent antiplanktonic and antibiofilm activities against S. aureus and P. aeruginosa by generating reactive oxygen species that cause membrane damage. Furthermore, TPA-1 under light irradiation can significantly reduce the number of viable bacteria in biofilms and promote wound healing in methicillin-resistant S. aureus (MRSA) and P. aeruginosa-infected mice models

INSTRUMENT(S): Orbitrap Fusion Lumos

ORGANISM(S): Staphylococcus Aureus

SUBMITTER: Wai Po Kong  

LAB HEAD: Kwok-yin Wong

PROVIDER: PXD060538 | Pride | 2025-05-07

REPOSITORIES: Pride

Dataset's files

Source:
Action DRS
2X1.raw Raw
2X2.raw Raw
2X3.raw Raw
BPA1.raw Raw
BPA2.raw Raw
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Publications

A Water-Soluble Aggregation-Induced Emission Photosensitizer with Intrinsic Antibacterial Activity as an Antiplanktonic and Antibiofilm Therapeutic Agent.

Hung Cheung-Hin CH   Chan Ka Hin KH   Kong Wai-Po WP   Du Ruo-Lan RL   Ding Kang K   Liang Zhiguang Z   Wang Yong Y   Wong Kwok-Yin KY  

Journal of medicinal chemistry 20250405 8


Photosensitizers (PSs) with aggregation-induced emission (AIE) properties have gained popularity for treating bacterial infections. However, most AIE PSs have a poor water solubility and low selectivity, limiting their applications in biological systems. Herein, we report a water-soluble and bacteria-targeting AIE PS that exhibits minimum cytotoxicity toward human cells with and without light irradiation. Acting as a narrow-spectrum antibacterial agent without light irradiation, TPA-1 eradicates  ...[more]

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