Radioiodinated of Gambogic Acid and Its Biodistribution in Mice
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Graphical Abstract
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Abstract
The preparation of radioiodinated gambogic acid and its cell uptake in MCF-7 and biodistribution in mice were investigated. Gambogic acid was labeled with 131I using hydrogen peroxide. The radiolabeled compound was characterized by polyamide TLC, in which the substratum of V(trichoromethane )∶V( methanol ) =40∶1 was used as developing agent. The uptake of 131Igambogic acid in cancer cells was measured. Biodistribution studies were carried out in KM mice. At different time after radiopharmaceutical i.v. administration (185 kBq 131Igambogic acid /mouse), the animals were sacrificed. Blood samples and the tissues of interested were collected, weighted and counted. The percent injected dose per gram (%ID/g) was calculated for each sample. The labeling yield of 131Igambogic acid is 86% and its radiochemistry purity are 97.2%, 95.4%, and 93.3% at 1, 4, and 20 d, respectively. The uptake of 131Igambogic acid in MCF-7 shows markedly higher compared with Na131I(P<0.01).The in vivo biodistribution in mice indicates that 131I gambogic acid is mainly uptaked in liver, kidney, and intestines. The radioactivity in thyroid increases with time. 131Igambogic acid is stable and is markedly uptaked in cancer cells MCF-7. In mice, it is mainly metabolized by liver and excreted through kidney.
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