Synthesis of radioiodinated carnosine for hepatotoxicity imaging induced by carbon tetrachloride and its biological assessment in rats

Author:

Challan Safaa B.1,Marzook Fawzy A.2,Massoud Ayman3ORCID

Affiliation:

1. Chemistry Unite of Cyclotron, Nuclear Research Center, Egyptian Atomic Energy Authority , P.O. Code 13759 , Cairo , Egypt

2. Department of Labeled Compounds , Hot Labs Center, Egyptian Atomic Energy Authority , P.O. Code 13759 , Cairo , Egypt

3. Chemistry Unite of Cyclotron, Nuclear Research Center, Nuclear Chemistry Department, Egyptian Atomic Energy Authority , P.O. Code 13759 , Cairo , Egypt , E-mail:

Abstract

Abstract The imaging of organs is very important in the field of diagnosis especially in case of liver diseases. In the present work, carnosine was successfully labeled with iodine-131 at room temperature in acidic medium using chloramine-T (Ch-T) as moderate oxidizing agent. The parameters affecting labeling of carnosine such as amount of oxidizing agent, amount of substrate, pH value of the reaction mixture, reaction temperature and reaction time, were investigated. The best conditions for formation of 131I-carnosine (131I-CAR) complex were 40 μg of chloramine-T (Ch-T), 75 μg of carnosine, pH 4 and 45 min reaction time at room temperature. The radiochemical yield for 131I-CAR complex was (91 ± 0.11) % at optimum conditions and the labeled complex was stable for 2 h after labeling process. Biodistribution study was achieved using three groups of rats (normal, treated by inactive carnosine and hepatotoxicity rats induced by CCl4). Hepatotoxicity of liver was evaluated using different biochemical markers such as ALT, AST and ALK.P. The 131I-CAR complex showed selective bio-localization in stomach and liver and its selectivity increases in acquired hepatotoxicity. The biological distribution indicates that the suitability of 131I-CAR as a potential hepatotoxicity imaging to detect hepatitis and medical prognosis.

Publisher

Walter de Gruyter GmbH

Subject

Physical and Theoretical Chemistry

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