Title: Genotoxic evaluation of [DOTA, Tyr³]octreotate labelled with ¹³¹I and ¹⁷⁷Lu in human peripheral lymphocytes in vitro by micronucleus assay

Authors: Miriam Fussae Suzuki, Marcia Augusta Da Silva, Jose De Souza Caldeira Filho, Maria Tereza Colturato, Elaine Bortoleti de Araujo, Paolo Bartolini, Kayo Okazaki

Addresses: Instituto de Pesquisas Energeticas e Nucleares – IPEN – CNEN/SP, Av. Professor Lineu Prestes 2242, CEP: 05508–000, Sao Paulo, SP, Brazil. ' Instituto de Pesquisas Energeticas e Nucleares – IPEN – CNEN/SP, Av. Professor Lineu Prestes 2242, CEP: 05508–000, Sao Paulo, SP, Brazil. ' Instituto de Pesquisas Energeticas e Nucleares – IPEN – CNEN/SP, Av. Professor Lineu Prestes 2242, CEP: 05508–000, Sao Paulo, SP, Brazil. ' Instituto de Pesquisas Energeticas e Nucleares – IPEN – CNEN/SP, Av. Professor Lineu Prestes 2242, CEP: 05508–000, Sao Paulo, SP, Brazil. ' Instituto de Pesquisas Energeticas e Nucleares – IPEN – CNEN/SP, Av. Professor Lineu Prestes 2242, CEP: 05508–000, Sao Paulo, SP, Brazil. ' Instituto de Pesquisas Energeticas e Nucleares – IPEN – CNEN/SP, Av. Professor Lineu Prestes 2242, CEP: 05508–000, Sao Paulo, SP, Brazil. ' Instituto de Pesquisas Energeticas e Nucleares – IPEN – CNEN/SP, Av. Professor Lineu Prestes 2242, CEP: 05508–000, Sao Paulo, SP, Brazil

Abstract: [DOTA, Tyr³]octreotate has been used for cancer diagnosis and therapy because of its high affinity to somatostatin subtype receptors sstr₂ and sstr₅. The aim of this study was to evaluate the cytogenetic effect of radio-labelled [DOTA, Tyr³]octreotate in blood cells in vitro, using the cytokinesis-block micronucleus assay. Blood samples of healthy donors were exposed to different activities of [DOTA, Tyr³]octreotate labelled with ¹³¹I (n = 3) and ¹⁷⁷Lu (n = 3), where radioactive concentration ranged from 600 to 5600 kBq/mL. The cells were cultivated according to criteria adopted by the IAEA (Vienna). The results showed a positive correlation between radioactive concentrations (X) and the frequency of binucleated cells with micronuclei (Y) (P < 0.05). The linear equations were similar: for the ¹³¹I labelled, Y = (1.634 ± 0.236) = (0.912 ± 0.137) 10–3 X and for the ¹⁷⁷Lu labelled, Y = (1.715 ± 0.342) = (0.743 ± 0.135) 10–3 X.

Keywords: micronucleus assay; octreotate; somatostatin; human lymphocyte; ¹³¹I; ¹⁷⁷Lu; DNA damage; genotoxic evaluation; low radiation; cytogenetic effect; blood cells; radioactive concentrations; binucleated cells.

DOI: 10.1504/IJLR.2007.015440

International Journal of Low Radiation, 2007 Vol.4 No.2, pp.161 - 168

Published online: 17 Oct 2007 *

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