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一般认为,实体瘤中的乏氧细胞是肿瘤放射治疗存在的主要问题。解决这一问题的最有希望的疗法之一是应用亲电子制剂,增强放射对乏氧细胞的致死效应。最有效的放射增敏剂是硝基咪唑类化合物Misonidazole(MISO)和第二代类似物SR2508与RO03-8799。这三个化合物现已进行广泛的临床试用,但由于神经毒副作用限制了疗效。本文作者试图克服神经毒副作用,研究了结构与硝基咪唑不同、特别是不含硝基的化合物,报告烟酰胺在小鼠体内作用特性的实验结果。资料指出了烟酰胺对小鼠的一般毒性、药代动力学和三种不同肿瘤与二种正常组织的放射增敏作用,并讨论了
It is generally believed that hypoxic cells in solid tumors are a major problem in tumor radiotherapy. One of the most promising treatments for this problem is the use of electrophilic agents to enhance the lethal effects of radiation on hypoxic cells. The most effective radiosensitizers are the nitroimidazole compounds Misonidazole (MISO) and the second generation analogues SR2508 and RO03-8799. These three compounds have now undergone extensive clinical trials but have limited efficacy due to neurotoxic side effects. The authors of this article attempted to overcome the side effects of neurotoxicity and studied different structures, particularly nitro-imidazole-containing compounds, and reported the experimental results of nicotinamide in vivo in mice. The data indicate the general toxicity, pharmacokinetics, and radiosensitization effects of nicotinamide on three different tumors and two normal tissues and discusses