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Abstract Bleomycin (BLM), labeled with radioisotopes, is widely used in therapy and diagnosis. In this study, BLM was labeled with 62Zn for oncologic PET studies. The complex was obtained at pH = 2 in saline at 90°C in 25 min. Radio-TLC showed an overall radiochemical yield of 95 97% (radiochemical purity > 97%). Stability of complex was checked in vitro in mice and human plasma/urine. Preliminary in vivo studies were performed to determine complex stability and distribution of 62Zn BLM in normal and fibrosarcoma-bearing mice. 62Zn BLM accumulated significantly in induced fibrosarcoma tumors in mice according to biodistribution/imaging studies. 62Zn BLM can be used in PET oncology studies due to its suitable physicochemical properties as a diagnostic complex in vitro and in vivo. Further studies should be performed for evaluation of the complex behavior in larger mammals.
Słowa kluczowe
Czasopismo
Rocznik
Tom
Strony
143--148
Opis fizyczny
Bibliogr. 19 poz., rys.
Twórcy
autor
- Cyclotron and Nuclear Medicine Department, Nuclear Research Center for Agriculture and Medicine (NRCAM), Atomic Energy Organization of Iran (AEOI), P. O. Box 31485-498, Karaj, Iran, Tel./Fax: +98 261 4436397
autor
- Cyclotron and Nuclear Medicine Department, Nuclear Research Center for Agriculture and Medicine (NRCAM), Atomic Energy Organization of Iran (AEOI), P. O. Box 31485-498, Karaj, Iran, Tel./Fax: +98 261 4436397
autor
- Research and Science Unit, Faculty of Engineering, Islamic Azad University of Iran, Tehran, Iran
autor
- Cyclotron and Nuclear Medicine Department, Nuclear Research Center for Agriculture and Medicine (NRCAM), Atomic Energy Organization of Iran (AEOI), P. O. Box 31485-498, Karaj, Iran, Tel./Fax: +98 261 4436397
autor
- Cyclotron and Nuclear Medicine Department, Nuclear Research Center for Agriculture and Medicine (NRCAM), Atomic Energy Organization of Iran (AEOI), P. O. Box 31485-498, Karaj, Iran, Tel./Fax: +98 261 4436397
autor
- Cyclotron and Nuclear Medicine Department, Nuclear Research Center for Agriculture and Medicine (NRCAM), Atomic Energy Organization of Iran (AEOI), P. O. Box 31485-498, Karaj, Iran, Tel./Fax: +98 261 4436397
autor
- Medical Physics Department, Shahid Beheshti University of Medical Sciences, Tehran, Iran
Bibliografia
- 1. Bleomycin monograph, vol. 1 (1996) In: Reynolds J (ed.) Martindale: the extra pharmacopoeia, 31st ed. Royal Pharmaceutical Press, King of Prussia, pp 546−547.
- 2. Brooks RC, Carnochan P, Vollano JF et al. (1999) Metal complexes of bleomycin. b: evaluation [Rh-105]-bleomycin for use in targeted radiotherapy. Nucl Med Biol 26:421−430.
- 3. de Kleijn EM, Oyen WJ, Claessens RA et al. (1995) Utility of scintigraphic methods in patients with fever of unknown origin. Arch Intern Med 155;18:1989−1994.
- 4. Green MA, Mathias CJ, Welch MJ et al. (1990) Copper-62-labeled pyruvaldehyde Bis (N4-methylthio-semicarba-zonato) copper(II): Synthesis and evaluation as a positron emission tomography tracer for cerebral and myocardial perfusion. J Nucl Med 31:1989−1996.
- 5. Hoehn ST, Junker HD, Bunt RC et al. (2001) Solution structure of Co(III)-bleomycin-OOH bound to a phosphoglycolate lesion containing oligonucleotide: implications for bleomycin-induced double-strand DNA cleavage. Biochemistry 40:5894−5905.
- 6. Jaaskela-Saari HA, Kairemo KJ, Ramsay HA et al. (1998) Labelling of bleomycin with Auger-emitter increases cytotoxicity in squamous-cell cancer cell lines. Int J Radiat Biol 73:565−570.
- 7. Jekunen AP, Kairemo KJ, Ramsay HA et al. (1996) Imaging of olfactory neuroblastoma by In-111 bleomycin complex. Clin Nucl Med 21:129−131.
- 8. Kairemo KJ, Ramsay HA, Tagesson M et al. (1997) Indium-111 bleomycin complex for radiochemotherapy of head and neck cancer-dosimetric and biokinetic aspects. Eur J Nucl Med 23:631−638.
- 9. Korppi-Tommola T, Huhmar H, Aronen HJ et al. (1999) 111In-labelled bleomycin complex for the differentiation of high- and low-grade gliomas. Nucl Med Commun 20:145−152.
- 10. Lyman S, Ujjani B, Renner K et al. (1986) Properties of the initial reaction of bleomycin and several of its metal complexes with Ehrlich cells. Cancer Res 49:4472−4478.
- 11. Naganawa H, Muraoka Y, Takita T et al. (1977) Chemistry of bleomycin. XVIII. Carbon-13 NMR studies. J Antibiot 30:388−396.
- 12. Neirinckx RD (1977) Excitation function for the 60Ni (a,2n) 62Zn reaction and production of 62Zn bleomycin. Int J Appl Radiat Isot 28:808−809.
- 13. Sausville EA, Paisach J, Harwitz SB (1978) Effect of chelating agents and metal ions on the degradation of DNA by bleomycin. Biochemistry 11:2740−2746.
- 14. Terrissol M, Pomplun E, Martin C (2002) Computer simulation of 57Fe-bleomycin Auger effects in DNA. Radiat Prot Dosim 99;1/4:69−72.
- 15. Umezawa HT (1965) Bleomycin and other antitumor antibiotics of high molecular weight. Antimicrob Agents Chemother 5:1079−1085.
- 16. Umezawa HT, Suhara Y, Takita T et al. (1966) Purification of bleomycins. J Antibiot 5:210−215.
- 17. Umezawa HT, Takeuchi S, Hori T et al. (1972) Studies on the mechanism of antitumor effect of bleomycin of squamous cell carcinoma. J Antibiot 7:409−420.
- 18. Vanbelle C, Muhle-Goll C, Remy MH et al. (2000) 1H, 13C, and 15N assignment of a bleomycin resistance protein in its native form and in a complex with Zn2+ligated bleomycin. J Biomol NMR 18:177−178.
- 19. Williamson D, McLenna IJ, Bax A et al. (1990) Two-dimensional NMR study of bleomycin and its zinc(II) complex: reassignment of 13C resonances. J Biomol Struct Dyn 8:375−398.
Typ dokumentu
Bibliografia
Identyfikator YADDA
bwmeta1.element.baztech-article-BUJ6-0004-0082