,131I-Evans blue: evaluation of necrosis targeting property and preliminary assessment of the mechan

• 作 者: Qiaomei Jin Xin Shan Qi Luo Dongjian Zhang Yuanyu Zhao Nan Yao Fei Peng Dejian Huang Zhiqi Yin Wei Liu Jian Zhang
• 机 构: Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Ch
• 出 处: 药学学报（英文版）
• 发表日期: 2018年3期
• 关键词: 131I-Evans blue Necrosis avidity Radioactivity DNA binding Necrosis imaging

Necrosis is a form of cell death, which is related to various serious diseases such as cardiovascular disease, cancer, and neurodegeneration. Necrosis-avid agents (NAAs) selectively accumulated in the necrotic tissues can be used for imaging and/or therapy of related diseases. The aim of this study was to preliminarily investigate necrosis avidity of 131I-evans blue (131I-EB) and its mechanism. The biodistribution of 131I-EB at 24 h after intravenous administration showed that the radioactivity ratio of necrotic to viable tissue was 3. 41 in the liver and 11. 82 in the muscle as determined by y counting in model rats. Autoradiography and histological staining displayed preferential uptake of 131I-EB in necrotic tissues. In vitro nuclear extracts from necrotic cells exhibited 82. 3％ of the uptake in nuclei at 15 min, as well as 79. 2％ of the uptake at 2 h after 13lI-EB incubation. The DNA binding study demonstrated that evans blue (EB) has strong binding affinity with calf-thymus DNA (CT-DNA) (Ksv = 5. 08×105 L/(mol/L)). Furthermore, the accumulation of 131I-EB in necrotic muscle was efficiently blocked by an excess amount of unlabeled EB. In conclusion, 131I-EB can not only detect necrosis by binding the DNA released from necrotic cells, but also image necrotic tissues generated from the disease clinically.