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Human recombinant insulin was successively labeled with [67Ga]-gallium chloride after conjugation with freshly prepared cyclic DTPA-dianhydride (ccDTPA). The best results of the conjugation were obtained by the addition of 0.5 ml of an insulin pharmaceutical solution (5 mg/ml, in phosphate buffer, pH = 8) to a glass tube precoated with DTPA-dianhydride (0.01 mg) at 25°C with continuous mild stirring for 30 min. Radiothin-layer chromatography (RTLC), instant thin-layer chromatography (ITLC) and high-performance liquid chromatography (HPLC) showed overall radiochemical purity higher than 96% in optimized conditions (specific activity = 300 500 MBq/mg, labeling efficiency 77%). Preliminary in vivo studies with normal rats were performed to determine the biodistribution of the radiotracer up to 110 h. They showed a high liver uptake of the tracer which is consistent with other reported radiolabeled insulins.
Słowa kluczowe
Czasopismo
Rocznik
Tom
Strony
145--151
Opis fizyczny
Bibliogr. 24 poz., rys.
Twórcy
autor
autor
autor
autor
autor
autor
- Nuclear Medicine Group, Agriculture, Medicine and Industrial Research School (AMIRS-NSTRI), P. O. Box 31485-498, Karaj, Iran, ajalilian@nrcam.org, arjalilian@yahoo.com
Bibliografia
- 1. Awasthi VS, Gambhir AB, Sewatkar B (1994) 99mTcinsulin:labeling, biodistribution and scintiimaging in animals. Nucl Med Biol 21:251−254
- 2. Dozio N, Sarugeri E, Scavini M et al. (2001) Insulin receptor antibodies inhibit insulin uptake by the liver: in vivo 123Iinsulin scintigraphic scanning and in vitro characterization in autoimmune hypoglycemia. J Investig Med 49:85−92
- 3. Dozio N, Scavini M, Beretta A et al. (1998) Imaging of the buffering effect of insulin antibodies in the autoimmune hypoglycemic syndrome. J Clin Endocrinol Metab 83:643−648
- 4. Eastman RC, Carson RE, Jacobson KE et al. (1992) In vivo imaging of insulin receptors in monkeys using 18F-labeled insulin and positron emission tomography. Diabetes 41:855−860
- 5. Eckelman WC, Karesh SM, Reba RC (1975) New compounds: fatty acid and long chain hydrocarbon derivatives containing a strong chelating agent. J Pharm Sci 64:704−706
- 6. Firestone RB, Shirley VS (1996) Table of isotopes, 8th ed. John Wiley & Sons Inc., New York
- 7. Goethals P, Lemahieu I, Agon P (1991) 66Ga − a promising isotope for positron emission tomography. Acta Radiol 37;Suppl:60−61
- 8. Graham MC, Pentlow KS, Mawlawi O, Finn RD, Daghighian F, Larson SM (1997) An investigation of the physical characteristics of 66Ga as an isotope for PET imaging and quantification. Med Phys 24:317−326
- 9. Green MA, Welch MJ (1989) Gallium radiopharmaceutical chemistry. Nucl Med Biol 16:435−448
- 10. Guenther KJ, Yoganathan S, Garofalo R et al. (2006) Synthesis and in vitro evaluation of 18F- and 19F-labeled insulin: a new radiotracer for PET-based molecular imaging studies. J Med Chem 49:1466−1474
- 11. Hachiya HL, Treves ST, Kahn CR, Sodoyez JC, Sodoyez-Goffaux F (1987) Altered insulin distribution and metabolism in type I diabetics assessed by [123I]insulin scanning. J Clin Endocrinol Metab 64:801−808
- 12. Hnatowich DJ, Layne WW, Child RL (1983) Radioactive labeling of antibody: a simple and efficient method. Science 220:613−619
- 13. Jalilian AR, Khorrami A, Tavakoli MB, Kamali-Dehghan M, Yari Kamrani Y (2007) Development of [201Tl](III)-DTPA-human polyclonal insulin complex for inflammation detection. Radiochim Acta 95:669−675
- 14. Jalilian AR, Mirsadeghi L, Haji-Hosseini R (2007) Preparation and biodistribution of [67Ga]-DTPA-rituximab in normal rats. J Radioanal Nucl Chem 274:175−179
- 15. Jalilian AR, Mirsadeghi L, Yari-Kamrani Y, Rowshanfarzad P, Kamali-Dehghan M, Sabet M (2007) Development of [64Cu]-DOTA-anti-CD20 for targeted therapy. J Radioanal Nucl Chem 274:563−568
- 16. Jalilian AR, Rowshanfarzad P, Shafaii K et al. (2005) Development of 111In-DTPA-human polyclonal antibody complex for long-term inflammation/infection detection. Nukleonika 50:91−96
- 17. Kasuga MY, Karlsson FA, Kahn CR (1982) Insulin stimulates the phosphorylation of the 95,000-dalton subunit of its own receptor. Science 215:185−187
- 18. Kasuga MY, Zick DL, Blithe FA, Karlsson HU, Kahn CR (1982) Insulin stimulation of phosphorylation of the beta subunit of the insulin receptor. Formation of both phosphoserine and phosphotyrosine. J Biol Chem 257:9891−9894
- 19. Lewis MR, Reichert DE, Laforest R et al. (2002) Production and purification of gallium-66 for preparation of tumor-targeting radiopharmaceuticals. Nucl Med Biol 29:701−706
- 20. Sabet M, Rowshanfarzad P, Jalilian AR, Ensaf MR, Rajamand AA (2006) Production and quality control of 66Ga radionuclide. Nukleonika 51:147−154
- 21. Shai Y, Kirk KL, Channing MA et al. (1998) 18F-labeled insulin: a prosthetic group methodology for incorporation of a positron emitter into peptides and proteins.Biochemistry 28:4801−4806
- 22. Sodoyez JC, Sodoyez-Goffaux F, von Frenckell R, De Vos CJ, Treves S, Kahn CR (1985) Differing effects of antiinsulin serum and antiinsulin receptor serum on 123I-insulin metabolism in rats. J Clin Invest 75:1455−1462
- 23. Wunderlich JC, Schick U, Freidenreich J, Werry J (1994) Peroral dosage form for peptide containing medicaments, in particular insulin. United States Patent: 6,468,959 Issued: October 22, 2002 Appl. No 222714
- 24. Zweit J, Sharma H, Downey S (1987) Production of gallium-66, a short-lived, positron emitting radionuclide. Int J Radiat Appl Instrum A 38:499−501
Typ dokumentu
Bibliografia
Identyfikator YADDA
bwmeta1.element.baztech-article-BUJ6-0023-0057