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

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. [ABSTRACT FROM AUTHOR]