Radiopharmaceutical evaluation of 131I-protohypericin as a necrosis avid compound |
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Authors: | Xuejiao Liu Yuanbo Feng Cuihua Jiang Bin Lou Yue Li Wei Liu |
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Institution: | 1. Laboratory of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing, Jiangsu Province, PR China,;2. College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, Jiangsu Province, PR China,;3. Theragnostic Laboratory, Campus Gasthuisberg, KU Leuven, Belgium,;4. Laboratory of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing, Jiangsu Province, PR China,;5. Department of Nuclear Medicine, The First Affiliated Hospital of Nanjing Medical University, Nanjing, Jiangsu Province, PR China, |
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Abstract: | Hypericin is a necrosis avid agent useful for nuclear imaging and tumor therapy. Protohypericin, with a similar structure to hypericin except poorer planarity, is the precursor of hypericin. In this study, we aimed to investigate the impact of this structural difference on self-assembly, and evaluate the necrosis affinity and metabolism in the rat model of reperfused hepatic infarction. Protohypericin appeared less aggregative in solution compared with hypericin by fluorescence analysis. Biodistribution data of 131I-protohypericin showed the percentage of injected dose per gram of tissues (%ID/g) increased with time and reached to the maximum of 7.03 at 24?h in necrotic liver by gamma counting. The maximum ratio of target/non-target tissues was 11.7-fold in necrotic liver at 72?h. Pharmacokinetic parameters revealed that the half-life of 131I-protohypericin was 14.9?h, enabling a long blood circulation and constant retention in necrotic regions. SPECT-CT, autoradiography, and histological staining showed high uptake of 131I-protohypericin in necrotic tissues. These results suggest that 131I-protohypericin is a promising necrosis avid compound with a weaker aggregation tendency compared with hypericin and it may have a broad application in imaging and oncotherapy. |
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Keywords: | Aggregation biodistribution necrosis affinity pharmacokinetics protohypericin |
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