A study of ¹³¹iodine labeling of indomethacin, its in vivo biological distribution in Lewis-bearing lung cancer, and its induction of apoptosis in lung cancer.

OBJECTIVES: To study the synthesis of 131iodine (I) labeled histamine-indomethacin (His-IN), its in vivo distribution in Lewis-bearing mice, and its effects on suppression of Lewis lung cancer growth and induction of apoptosis.

METHODS: The present study was carried out in the Experimental Research Center, Sheng Jing Hospital of China Medical University Hospital, Shenyang China between December 2008 and October 2009. Chemical synthesis of His-IN was carried out. Ninety-five C57 mice were allocated into 12 groups, and a series of experiments including the in vivo biological distribution of 131I-His-IN in C57 mice bearing Lewis lung cancer was explored, and the therapeutic effects of IN and 131I-His-IN in lung cancer-bearing mice were assessed through tumor suppression experiments, flow cytometry, and detection of tumor necrosis factor.

RESULTS: The 131I-His-IN radionuclide count ratio of the tumor site and surrounding region significantly increased with time, namely, the retention time of 131I-His-IN radionuclide was longer in the tumor site. A 3.0 mg/kg and 3.5 mg/kg 131I-His-IN, as well as 3.0 mg/kg and 3.5 mg/kg IN all had tumor suppression and apoptosis induction effects on tumors, among which the 3.5 mg/kg 131I-His-IN group had significant differences compared with all other groups.

CONCLUSIONS: The 131I-His-IN not only retains the tumor-affinity property of IN, the synergistic effect of these 2 also enhances the tumor suppression and pro-apoptotic function.