基于2-羟苯基-苯并噻唑染料的光动力试剂的合成与应用  

Synthesis and Application of Photodynamic Reagent Based on 2-Hydroxyphenyl Benzothiazole

作　　者：苗俊峰 翁嘉劲 霍莹莹 郭炜[1] MIAO Junfeng;WENG Jiajin;HUO Yingying;GUO Wei(School of Chemistry and Chemical Engineering,Shanxi University,Taiyuan 030006,China)

机构地区：[1]山西大学化学化工学院,山西太原030006

出　　处：《山西大学学报（自然科学版）》2022年第5期1362-1368,共7页Journal of Shanxi University(Natural Science Edition)

基　　金：国家自然科学基金(21302114,21904082,22004081)。

摘　　要：为了开发出在肿瘤低氧环境中有良好治疗效果的高单线态氧量子收率的光动力试剂,文章以2-羟苯基-苯并噻唑为染料平台,利用重原子能够提高系间窜跃效率的性质,在其骨架中引入重原子I,设计开发出新型的光动力试剂HBT-I,测得其单线态量子产率高达0.86,并在组织正常含氧量以及低氧条件下进行了抑制细胞增殖实验,测得半抑制浓度(IC_(50))分别为0.38μmol和0.40μmol,表明该光动力试剂治疗时对氧浓度依赖较低,在低氧浓度下依然治疗效果良好,有望成为优异的光动力治疗肿瘤的工具。In order to develop a photodynamic reagent with high singlet oxygen quantum yield that has good therapeutic effect in the tumor hypoxia environment, we used 2-hydroxyphenyl benzothiazole as the dye platform, made use of the property that heavy atoms can improve the transition efficiency between systems, introduced heavy atom iodine(I) into its skeleton, designed and developed a new photodynamic reagent HBT-I, and measured its singlet state quantum yield as high as 0. 86. The experiment of inhibiting cell proliferation was carried out under normal oxygen and hypoxia conditions, and the measured semi inhibitory concentration(IC_(50))was 0. 38 μmol and 0. 40 μmol, respectively. This indicates that the photodynamic reagent has a low dependence on oxygen concentration during treatment, and it still has a good therapeutic effect under hypoxia. It is expected to become an excellent photodynamic tool for tumor treatment.

关 键 词：肿瘤 低氧 重原子 光敏剂 

分 类 号：O626[理学—有机化学]