Enhanced Energy Transfer in a Donor-Acceptor Photosensitizer Triggers Efficient Photodynamic Therapy

Photosensitizers (PSs) play a vital role in photodynamic therapy (PDT) for combating bacterial resistance and treating tumor. In this study, we report new donor-acceptor porphyrin PSs with a cationic conjugated oligomer (OPV) as a donor unit and porphyrin (TPP) as an acceptor unit by covalent linkage and achieved a fluorescence resonance energy transfer efficiency of 99% owing to their strong spectral overlap and short distance. The ¹O₂ yield of porphyrin derivatives is 121% (rose bengal as the standard reference) by virtue of OPVs' excellent light-harvesting ability and high fluorescence resonance energy transfer efficiency, greatly exceeding those of oligomer and porphyrin derivatives reported in the literature. Additionally, the cationic donors significantly improved the water solubility, decreased the aggregation of porphyrin, and promoted the adherence of the PSs to cell membranes through electrostatic interactions. As a result, the D-A porphyrin PSs exhibit dramatic PDT treatment efficiency. The half-inhibitory concentration is as low as 33 and 88 nM for methicillin-resistant Staphylococcus aureus and Escherichia coli, respectively. Therefore, this study provides a new strategy to construct PSs with high ¹O₂ yield and an excellent treatment effect at a low dose of PSs, which is promising for application in PDT used to treat cancer and microbial infections.