当前位置：
X-MOL 学术
›
J. Med. Chem.
›
论文详情
Our official English website, www.x-mol.net, welcomes your
feedback! (Note: you will need to create a separate account there.)
Pyridine-Embedded Phenothiazinium Dyes as Lysosome-Targeted Photosensitizers for Highly Efficient Photodynamic Antitumor Therapy.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2020-04-21 , DOI: 10.1021/acs.jmedchem.0c00280 Qicai Xiao 1, 2 , Huirong Lin 3 , Juan Wu 2 , Xin Pang 2, 3 , Quanming Zhou 1 , Yue Jiang 2 , Pan Wang 2 , Wingnang Leung 2 , Hungkay Lee 4 , Sheng Jiang 5 , Shao Q Yao 6 , Liqian Gao 1 , Gang Liu 3 , Chuanshan Xu 2, 7
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2020-04-21 , DOI: 10.1021/acs.jmedchem.0c00280 Qicai Xiao 1, 2 , Huirong Lin 3 , Juan Wu 2 , Xin Pang 2, 3 , Quanming Zhou 1 , Yue Jiang 2 , Pan Wang 2 , Wingnang Leung 2 , Hungkay Lee 4 , Sheng Jiang 5 , Shao Q Yao 6 , Liqian Gao 1 , Gang Liu 3 , Chuanshan Xu 2, 7
Affiliation
|
Development of new photosensitizers (PSs) with high photodynamic efficacy and minimal side effects is of great interest in photodynamic therapy (PDT). In this work, we reported several pyridine-embedded phenothiazinium (pyridophenothiazinium) dyes, which could be conveniently synthesized in a few short steps and acted as highly efficient and potent PSs to selectively localize to lysosomes and photosensitively kill cancer cells. Among them, compound 5, which possessed the ability of promoting intracellular reactive oxygen species (ROS) upon light irradiation by almost 40-fold higher than that of methylene blue (MB, a general phenothiazinium-based PS), exhibited a remarkable phototherapeutic index (PI = 53.8) against HT29 cancer cells, leading to eradication of large solid tumors (∼300 mm3) in a xenograft mouse model without apparent side effects. These results suggest that the pyridophenothiazinium dyes developed herein, especially compound 5, may serve as promising lysosome-targeted PSs for efficient photodynamic antitumor therapy.
中文翻译：
吡啶嵌入的吩噻嗪鎓染料作为靶向溶酶体的光敏剂，用于高效光动力抗肿瘤治疗。
具有高光动力功效和最小副作用的新型光敏剂（PSs）的开发在光动力疗法（PDT）中引起了极大的兴趣。在这项工作中，我们报道了几种吡啶嵌入的吩噻嗪鎓（pyridophenothiazinium）染料，可以在短短几个步骤内方便地合成它们，并且可以作为高效有效的PS，选择性地定位于溶酶体并光敏杀死癌细胞。其中，化合物5在光照射下具有促进细胞内活性氧（ROS）的能力的能力比亚甲基蓝（MB，一种基于吩噻嗪鎓的PS）几乎高40倍，具有显着的光疗指数（ PI = 53.8）对抗HT29癌细胞，导致在异种移植小鼠模型中消除了大型实体瘤（〜300 mm3），而没有明显的副作用。
更新日期：2020-04-08
中文翻译：
吡啶嵌入的吩噻嗪鎓染料作为靶向溶酶体的光敏剂，用于高效光动力抗肿瘤治疗。
具有高光动力功效和最小副作用的新型光敏剂（PSs）的开发在光动力疗法（PDT）中引起了极大的兴趣。在这项工作中，我们报道了几种吡啶嵌入的吩噻嗪鎓（pyridophenothiazinium）染料，可以在短短几个步骤内方便地合成它们，并且可以作为高效有效的PS，选择性地定位于溶酶体并光敏杀死癌细胞。其中，化合物5在光照射下具有促进细胞内活性氧（ROS）的能力的能力比亚甲基蓝（MB，一种基于吩噻嗪鎓的PS）几乎高40倍，具有显着的光疗指数（ PI = 53.8）对抗HT29癌细胞，导致在异种移植小鼠模型中消除了大型实体瘤（〜300 mm3），而没有明显的副作用。
京公网安备 11010802027423号