Synthesis and evolution of S-Porphin sodium as a potential antitumor agent for photodynamic therapy against breast cancer

Abstract

The novel sensitizer S-Porphin sodium can generate ROS by radiation with a long wavelength to cause tumor cell death.

Highly Efficient Water-Soluble Photosensitizer Based on Chlorin: Synthesis, Characterization, and Evaluation for Photodynamic Therapy

“…The PDT effects of HPS were tested in the 4T1- and A549-tumor-bearing mice, and the optimal therapeutic window was chosen on the basis of its biodistribution and pharmacokinetics. The selected illumination conditions and HPS dose (50–120 J/cm 2 , 0.08–0.64 mg/kg) approximate those previously studied for the structurally similar chlorin-based HPPH, S-PS mediated PDT. , The 4T1 model was treated with 0.6 mg/kg HPS or 0.6 mg/kg HPPH, whereas the nude mice bearing A549 tumors were administered different concentrations of HPS (0.08–0.64 mg/kg) or HPPH (0.32 mg/kg). The tumors were exposed to different lasers 6 h later, and the tumor volume and survival were recorded.…”

“…15,16 However, although HPPH achieved excellent antitumor PDT and 1 O 2 quantum yield at low dosage, it cannot be widely used due to its hydrophobicity with administration limitations. 17,18 The aim of our study was to design a novel chlorin-based PS via an optimized synthesis route for fluorescence image-guided PDT. Salt and polar groups are often introduced as structural modifications to improve the water solubility of many drugs.…”

“…Chlorin is a porphyrin derivative obtained through reduction of one of the peripheral cross-conjugated double bonds, and it exhibits absorption maximum in the red/NIR range (650–800 nm), effective singlet oxygen (Φ = 45–60%) generation, superior photoactivity, and lower dark toxicity compared to that of related porphyrins . The chlorin-based second-generation PS 2-[1-hexyloxyethyl]-2-devinyl pyropheophorbide- a (HPPH) was tested in phase I/II clinical trial with satisfactory outcomes, and showed more favorable photophysical properties and deeper tissue penetration compared to porphyrin (665 vs 630 nm). , However, although HPPH achieved excellent antitumor PDT and 1 O 2 quantum yield at low dosage, it cannot be widely used due to its hydrophobicity with administration limitations. , …”