用于体内癌症靶向近红外成像的甘氨酸修饰七甲川吲哚菁染料的合成与表征

Synthesis and characterization of a glycine-modified heptamethine indocyanine dye for in vivo cancer-targeted near-infrared imaging.

作者信息

Liu Tao, Luo Shenglin, Wang Yang, Tan Xu, Qi Qingrong, Shi Chunmeng

机构信息

Institute of Combined Injury, State Key Laboratory of Trauma, Burns and Combined Injury, Chongqing Engineering Research Center for Nanomedicine, College of Preventive Medicine, Third Military Medical University, Chongqing, People's Republic of China.

Key Laboratory of Drug-Targeting and Drug-Delivery Systems of the Ministry of Education, Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu, People's Republic of China.

出版信息

Drug Des Devel Ther. 2014 Sep 9;8:1287-97. doi: 10.2147/DDDT.S65696. eCollection 2014.

DOI:10.2147/DDDT.S65696

PMID:25246770

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4166911/

Abstract

Near-infrared (NIR) fluorescent sensors have emerged as promising molecular tools for cancer imaging and detection in living systems. However, cancer NIR fluorescent sensors are very challenging to develop because they are required to exhibit good specificity and low toxicity as an eligible contrast agent. Here, we describe the synthesis of a new heptamethine indocyanine dye (NIR-27) modified with a glycine at the end of each N-alkyl side chain, and its biological characterization for in vivo cancer-targeted NIR imaging. In addition to its high specificity, NIR-27 also shows lower cytotoxicity than indocyanine green, a nonspecific NIR probe widely used in clinic. These characteristics suggest that NIR-27 is a promising prospect as a new NIR fluorescent sensor for sensitive cancer detection.

摘要

近红外（NIR）荧光传感器已成为用于活体系统中癌症成像和检测的有前景的分子工具。然而，开发癌症近红外荧光传感器极具挑战性，因为作为合格的造影剂，它们需要表现出良好的特异性和低毒性。在此，我们描述了一种新的七甲川吲哚菁染料（NIR-27）的合成，该染料在每个N-烷基侧链末端用甘氨酸修饰，并对其用于体内癌症靶向近红外成像的生物学特性进行了研究。除了具有高特异性外，NIR-27的细胞毒性也低于吲哚菁绿，后者是临床上广泛使用的非特异性近红外探针。这些特性表明，NIR-27作为一种用于灵敏癌症检测的新型近红外荧光传感器具有广阔的应用前景。