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用Wistar系大鼠、昆明种小鼠及肝细胞癌荷瘤裸小鼠模型分别进行~(131)I标记的吡哆-5-甲基色氨酸(~(131)I-PMT)的体内代谢、器官分布作了毒性试验及亲肿瘤性研究。结果表明~(131)I-PMT血液清除较快,血液清除曲线与二项指数曲线相拟合。静脉注射30min后近60％放射性标记物进入肝、胆、肠系统,肾脏内放射性相对较低。7d内60％放射性由粪便排出。药物对肿瘤组织有亲和性,瘤体与肝组织放射性比为2:1。应用10倍于治疗剂量的药物并未引起小鼠有关脏器的病理和血液生化改变,具有亲肿瘤性的~(131)I-PMT,用于肝癌治疗比较安全。
(131 I) -labeled pyridoxine-5-methyltryptophan (~ (131) I-PMT) in vivo in a Wistar rat, a Kunming mouse and a hepatocellular carcinoma tumor-bearing nude mouse model Metabolism and organ distribution were tested for toxicity and tumorigenicity. The results showed that ~ (131) I-PMT had faster blood clearance, and the blood clearance curve fitted with the binominal index curve. Nearly 60% of radioactive markers enter the liver, gall bladder, and intestine system 30 minutes after intravenous injection, and the radioactivity in the kidney is relatively low. 60% of radioactive within 7d discharged from the feces. Drug affinity for tumor tissue, tumor and liver tissue radioactivity ratio of 2: 1. The application of 10 times the therapeutic dose of the drug did not cause pathological and blood biochemical changes in the organs of mice, with the tumor of 131I-PMT, for the treatment of liver cancer more secure.