Radiopharmaceutical evaluation of 131I-protohypericin as a necrosis avid compound. (6th February 2015)

• Record Type: Journal Article
• Authors: Liu, Xuejiao; Feng, Yuanbo; Jiang, Cuihua; Lou, Bin; Li, Yue; Liu, Wei; Yao, Nan; Gao, Meng; Ji, Yun; Wang, Qingqing; Huang, Dejian; Yin, Zhiqi; Sun, Ziping; Ni, Yicheng; Zhang, Jian
• Is Part Of: Journal of drug targeting. Volume 23:Number 5(2015)
• Page Start: 417
• Page End: 426
• Publication Date: 2015-02-06
• Subjects: Aggregation -- biodistribution -- necrosis affinity -- pharmacokinetics -- protohypericin; Drug delivery systems -- Periodicals; Drug Delivery Systems; Vehicles; Drug Administration Routes; Drug Evaluation; 615.7
• DOI: 10.3109/1061186X.2014.1002787
• Languages: English
• ISSNs: 1061-186X

Abstract

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 131 I-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 131 I-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 131 I-protohypericin in necrotic tissues. These results suggest that 131 I-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.