Department of Pharmaceutical Science & Technology, College of Chemistry and Biology, Donghua University, Shanghai, 201620, China.
Ningbo Dongmi Pharmaceutical Co., Ltd, Ningbo, 315899, China; Shanghai Xianhui Pharmaceutical Co., Ltd, Shanghai, 200433, China.
Eur J Med Chem. 2018 Dec 5;160:146-156. doi: 10.1016/j.ejmech.2018.10.005. Epub 2018 Oct 11.
The development of novel photosensitizers is a challenging task for photodynamic therapy (PDT). Twelve novel photosensitizers (PSs), including porphins (P1-4), chlorins (C1-4) and bacteriochlorins (B1-4) were synthesized. The bacteriochlorins exhibited the longest absorption wavelength (λ = 736 nm), which is higher than that of porphins (λ = 630 nm) and chlorins (λ = 644 nm). In vitro photodynamic activities on Eca-109 human esophageal carcinoma cells were evaluated by standard assays and all PSs showed photodynamic activity. Among them, B2 displayed the highest phototoxicity and the lowest dark toxicity. In addition, B2 exhibited best photodynamic antitumor efficacy on BALB/c nude mice bearing Eca-109 cells tumor. Therefore, B2 is a powerful and promising antitumor photosensitizer for PDT.
新型光敏剂的开发是光动力疗法（PDT）的一项具有挑战性的任务。我们合成了 12 种新型光敏剂（PS），包括卟啉（P1-4）、氯卟啉（C1-4）和细菌叶绿素（B1-4）。细菌叶绿素表现出最长的吸收波长（λ=736nm），高于卟啉（λ=630nm）和氯卟啉（λ=644nm）。通过标准测定法评估了新型光敏剂在 Eca-109 人食管癌细胞上的体外光动力活性，所有 PS 均表现出光动力活性。其中，B2 显示出最高的光毒性和最低的暗毒性。此外，B2 在荷瘤 BALB/c 裸鼠上表现出最佳的光动力抗肿瘤疗效。因此，B2 是一种强大且有前途的 PDT 抗肿瘤光敏剂。
