Radio Labeling of 2-Aminonicotinic Acid with 131I and Biodistribution on the Albino Wistar Rats

Year 2013, Volume: 13 Issue: 1, 1 - 8, 01.04.2013

Muhsin Sarıkaya Hüseyin Enginar

https://doi.org/10.5578/fmbd.5418

Abstract

Türk In this study, labeling of 2-aminonicotinic acid (2-ANA) with 131I, radiolabeling efficiency, the effect of pH and oxidizing agent on the labeling yield, in vitro stability and biodistribution of radiolabelling substance were made. Electrophoresis and Radio Thin Layer Chromatography (RTLC) methods were used in the quality control study of radiolabeled substance (131I-2-ANA). Biodistribution studies were done in nine male Albino Wistar rats which were categorized 3 groups. The rats were sacrificed at various time intervals (15, 60 and 180 min), their organs were removed, and percentage of injected dose per gram (% ID/g) was calculated. The labeling yield of 2-ANA was determined as % 86.41±3.11. Maximum uptake of 131I-2-ANA was seen in the stomach, kidneys, pancreas, liver, thyroid small intestine and fat. We concluded that the binding efficiency of 131I-2-ANA was high and it had sufficient stability for diagnostic studies. © Afyon Kocatepe Üniversitesi 1.Giriş İnsanlardaki bulaşıcı veya bulaşıcı olamayan hastalıkların belirlenmesi (tümör, iltihap, vb) klinik uygulamalarda büyük bir sorun olarak devam etmektedir (Boerman et al., 2001; Rennen et al., 2001). incelemelerle ortaya çıkarılmaktadır (Cindas et al., 2001; De Bois et al., 1996). Sintigrafik çalışmalar ise genelde radyofarmasötiklerle yapılmaktadır. Bu tür yerlerin tanısı için kullanılan radyofarmasötiklerin

Keywords

2-Aminonicotinic acid; Biodistribution

2-Aminonikotinik Asit'in 131I ile Radyo işaretlenmesi ve Albino Wistar Sıçanlarda Biyodağılımının Yapılması

Abstract

Bu çalışmada, 2-aminonikotinik asit (2-ANA) radyoişaretleme verimi üzerine pH ve yükseltgen ajanın etkisi, in vitro kararlılığı ve radyoişaretli bileşiğin biyodağılımı çalışması yapılmıştır. Radyoişaretli bileşiğin kalite kontrol çalışmalarında Elektroforez ve Radyo İnce Tabaka Kromatografisi (RİTK) kullanılmıştır. Biyodağılım 9 adet erkek Albino wistar sıçanlar üzerinde ve üç gruba ayrılarak yapıldı. Radyoişaretli bileşik(131I-2-ANA) sıçanlara verildikten sonra 15, 60 ve 180 dakika sonra hayvanlar sakrifiye edilerek belirli organlar çıkarılarak bu organlardaki enjekte edilen dozun gram basına doz dağılımları ölçüldü. 131I-2-ANA bileşiğinin verimi % 86,41±3,11 olarak bulundu. Biyodağılım sunucunda 131I-2-ANA bileşiği yüksek oranda mide, böbrek, pankreas, akciğer, tiroid, incebağırsak ve yağda tutulum yaptığı görüldü. Bu çalışmanın sonucunda, 131I-2-ANA’nnn radyoişaretleme veriminin yüksek olduğu ve diagnostik çalışmalar için yeterli kararlılığa sahip olduğu bulunmuştur

Keywords

2-Aminonikotinik asit, Biyodağılım, 131I, Sıçan

References

• Babich, J.W., Fischman, A.J., 1995. Effect of “Co-ligand” on the Biodistribution of 99mTc-Labeled Hydrazino Nicotinic Acid Derivatized Chemotactic Peptides. Nuclear Medicine and Biology, 22, 25–30.
• Bechgaard, H., and Jesperson, S., 1977. Gastrointestinal absorption of niacin in humans. Journal of Pharmaceutical Sciences, 66, 871-872.
• Bergström, K.A., Lötjönen, S., Kuikka, J. T., Penttilä, P., Mussalo, H., Hiltunen, J., Länsimies, E., 1993. Synthesis biodistribution in rat. Journal of Labelled Compounds and Radiopharmaceuticals, 33(7), 593–599. and
• Boerman, O.C., Dams, Eth.M., Oyen, W.J.G., Corstens, F.H.M., Storm, G., 2001. Radiopharmaceuticals for scintigraphic imaging of infection and inflammation. Inflammation Research, 50, 55–64.
• Brown, J.M., Lemmon, M.J., Horsman, M.R., Lee, W.W., 1991. Structure–activity relationships for tumour radiosensitization by analogues of nicotinamide and benzamide. International Journal Radiation Biology, 59, 739–748.
• Bruckert, E., Labreuche, J., Amarenco, P., 2010. Meta- analysis of the effect of nicotinic acid alone or in combination atherosclerosis. Atherosclerosis 210 (2), 353–61.
• Carlson, L.A., Oro, L., Ostman, J., 1968. Effect of a single dose of nicotinic acid on plasma lipids in patients with Scandınavıca, 183, 457-465. Acta Medıca
• Cindas, A., Gökce-Kutsal, Y., Kirtli, P.Ö., Caner, B., 2001, Scintigraphic evaluationof synovial inflammation in rheumatoid arthritis with Technetium 99m-labelled human polyclonal immunoglobulin G. Rheumatology International, 20, 71–77.
• Cox, M., Lehninger, A.L., Nelson, D.R., 2000. Lehninger principles of biochemistry. Worth Publishers, New York.
• De Bois, M.H., Pauwels, E.K., Breedveld, F.C., 1996, New agents for scintigraphy in rheumatoid arthritis. European Journal of Nuclear Medicine, 23, 1339– 1346.
• Decristoforo, C., Mather, S.J., 1999. Technetium-99m Somatostatin Analogues: Effect of Labelling Methods and Peptide Sequence. European Journal of Nuclear Medicine, 26, 869–876.
• Gass, J.D., 1973. Nicotinic Acid Maculopathy. American Journal of Ophthalmology, 76, 500-510.
• Girgis A.S., Hosni, H.M., Barsoum, F.F., 2006. Novel synthesis of nicotinamide derivatives of cytotoxic properties. Bioorg anic Medical Chemistry, 14, 4466–4476.
• Goodman, L. S., , A., 1975. The Pharmacological Basis of Therapeutics. Macmillan. New York.
• Hankes, L.V., 1984. Handbook of Vitamins. Dekker, New York.
• Hnatowich, D.J., Winnard, P.Jr., Virzi, F., Fogarsi, M., Sano, T., Smith, C.L., Cantor, C.L., Rusckowski, M., 1995. Technetium-99m Labeling of DNA. Journal of Nuclear Medicine, 36, 2306–2314.
• Jacob, R. A., Swendseid, M. E., McKee, R. W., Fu, C. S., Clemens, R. A., 1989. Biochemical markers for assessment of niacin status in young men: urinary and blood levels of niacin metabolites. The Journal of Nutrition, 119, 591-598.
• Jurisson, S., Berning, D., Jia, W., Ma, D., 1993. Coordination Compounds in Nuclear Medicine. Chemistry Review, 93, 1137–1156.
• Karczmarczyk, U., Markiewicz, A., Mikołajczak, R., Lisiak, E., Bilski, M., Pietrzykowski, J., Michalik, J., 2004. (99m)Tc human IgG radiolabelled by HYNIC, Biodistribution and scintigraphy of experimentally induced inflammatory lesions in animal model. Nuclear Medicine Review. Central and Eastern Europe, 7(2), 107-12.
• Katzung, B.G., 2006. Basic and clinical pharmacology. McGraw-Hill Medical Publishing Division, New York.
• Liu, X., Pham T. Q., Berghofer, P., Chapman, J., Greguric, I., Mitchell, P., Mattner, F., Loc’h, C., Katsifis, A., 2008. radioiodinated melanoma. Nuclear Medicine and Biology, 35, 769– 781. evaluation of malignant for
• McGovern M.E., 2005. Taking aim at HDL-C, Raising levels to reduce cardiovascular risk. Postgraduate Medicine, 117 (4), 29–30.
• Pero, R.W., Axelsson, B., Siemann, D., Chaplin, D., Dougherty, G., 1999. Newly discovered anti- inflammatory properties of the benzamides andnicotinamides. Biochemistry, 193, 119–25. and Cellular
• Pitsavas, S., Andreou, C., Bascialla, F., Bozikas, VP.., Karavatos, A., 2004. Pellagra encephalopathy following B-complex vitamin treatment without niacin. International Journal of Psychiatry in Medicine, 34 (1), 91–95.
• Ravi, P., Gandotra, S., Singh, L.K., Das, B., Lakra, A., 2008. Rapid resolution of delusional parasitosis in pellagra with niacin augmentation therapy. General Hospital Psychiatry, 30 (6), 581–584.
• Rennen, H.J.J.M., Makarewicz, J., Oyen, W.J.G., Laverman, P., Corstens, F.H.M., Boerman. O.C., 2001. Imaging infection/inflammation in the new millennium. European Journal of Nuclear Medicine, 28, 243–251.