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Type-I photosensitizers (PSs) are among the most potential candidates for photodynamic therapy (PDT), as their low dependence on oxygen endow them with many advantages for treating hypoxic tumor. However, most of the reported type-I PSs have a contingency of molecular design, because electron transfer (ET) reaction is more difficult to achieve than energy transfer (EET) process. Therefore, it is urgent to understand molecular design mechanisms for type-I PSs.

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Molecular acceptor engineering to precisely design a NIR type I photosensitizer for efficient PDT-based synergistic therapy.

Chem Commun (Camb)

January 2025

Department of Chemistry and the Tsinghua Center for Frontier Polymer Research, Tsinghua University, Beijing, 100084, P. R. China.

Molecular design plays a crucial role in regulating the photophysical properties and photodynamic therapy (PDT) performance of photosensitizers (PSs); however, realizing PDT-based synergistic therapy based on sole PSs is still rarely reported. Herein, three near-infrared red type I PSs (named TP1, TP2, and TP3) were synthesized by adjusting their electron acceptors. The results demonstrated that these PSs exhibited aggregation-enhanced reactive oxygen species (ROS) generation efficiency and cyano groups on PSs can reduce ROS generation in solution while achieving efficient PDT-based synergistic therapy in cells glutathione depletion.

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Bright deep red/near-infrared red (DR/NIR) active type I photosensitizers (PSs) with generating superoxide anion and hydroxyl radical have been regarded as powerful functional materials to fight the "Achilles's heel" of hypoxia from solid tumor. But some problems have still existed, for example, lacking effective molecular designed strategy or typical building block to design precisely type I PSs. In addition, the relationship between fluorescent quantum efficiency and NIR fluorescent color is inconsistent according to energy gap rule.

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PEGylated BODIPY Photosensitizer for Type I Dominant Photodynamic Therapy and Afterglow Imaging.

ACS Appl Mater Interfaces

November 2024

Key Laboratory of Polymer Ecomaterials, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, China.

Type I photodynamic therapy (PDT) exhibits outstanding therapeutic effects in hypoxic environments in tumors, but the design of type I photosensitizers (PSs), especially those with simple structures but dramatic properties, remains a challenge. Herein, we report a design strategy for developing type I PSs in one molecule with afterglow luminescence. As a proof concept, a 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene (BODIPY) PS (BIP) bearing water-soluble poly(ethylene glycol) (mPEG) chains is synthesized, and BIP can self-assemble into nanoparticles (BIPNs).

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design of type-l photosensitizer agents based on structure-inherent low triplet energy for hypoxia photodynamic therapy.

Mater Horiz

November 2024

Key Laboratory of Green Chemistry and Technology of Ministry of Education, College of Chemistry, Sichuan University, Chengdu 61064, P. R. China.

Photodynamic therapy (PDT), owing to its low invasiveness, high efficiency, fewer side effects, spatiotemporal controllability and good selectivity, has attracted increasing attention for its tremendous potential in revolutionizing conventional strategies of tumor treatment. However, hypoxia is a common feature of most malignancies and has become the Achilles' heel of PDT. Currently, Type II photosensitizers (PSs) have inadequate efficacy for PDT due to the inherent oxygen consumption of the anoxic tumor microenvironment.

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