1. Necrosis affinity evaluation of 131I-hypericin in a rat model of induced necrosis.
- Author
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Kong, Ming, Zhang, Jian, Jiang, Cuihua, Jiang, Xiao, Li, Yue, Gao, Meng, Yao, Nan, Huang, Dejian, Wang, Xiaoning, Fang, Zhijun, Liu, Wei, Sun, Ziping, and Ni, Yicheng
- Subjects
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NECROSIS , *HYPERICIN , *GENERIC drugs , *DRUG development , *LABORATORY rats , *THERAPEUTICS - Abstract
Cancers are often with spontaneous or therapeutic necrosis that could be utilized as a generic target for developing new treatments. The purpose of this study was to investigate the biodistribution and pharmacokinetics of radioiodinated hypericin (Hyp), a naturally occurring compound, after intravenous (i.v.) injection in a rat model of liver and muscle necrosis ( n = 42), and evaluate its necrosis affinity. Hyp was labeled with 131I with labeling efficiency >99%. After incubating in solution/rat plasma for 8 days, radiochemical purity of 131I-Hyp remained 98.1 and 97.1%, respectively, indicating good in vitro stability. SPECT-CT images at 24 h after i.v. injection of 131I-Hyp in rats with induced liver and muscle necrosis showed obvious tracer absorption in necrotic tissues. Biodistribution studies revealed that the percentage of the injected dose per gram of tissue (%ID/g) evolved from 1.9 %ID/g at 6 h, through a maximum 3.0 %ID/g at 12 h, to 1.0 %ID/g at 192 h in necrotic liver. Pharmacokinetics studies revealed that the terminal elimination half-life, total body clearance and area under the curve of 131I-Hyp were 32.7 h, 9.2 L/h/kg and 1.6 MBq/L*h, respectively. These results demonstrated that 131I-Hyp features a long blood circulation in animals and persistent retention in necrotic tissues. Therefore, 131I-labeled Hyp could be a broad-spectrum anti-tumor agent with a cost much cheaper relative to the biological agents such as monoclonal antibodies. [ABSTRACT FROM AUTHOR]
- Published
- 2013
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