| 李五岭,杨新海,赵毅强,沈磊,蔡松君,路新华.3-硝基三氮唑类衍生物体外放射增敏作用的生物学评价[J].中华放射医学与防护杂志,1997,17(5):324-327 |
| 3-硝基三氮唑类衍生物体外放射增敏作用的生物学评价 |
| A biological evaluation on in vitro radiosensitization of nitrotriazole derivatives |
| 投稿时间：1996-06-11 修订日期：1996-12-19 |
| DOI： |
| 中文关键词: 放射增敏作用 3-硝基三氮唑类衍生物 |
| 英文关键词:Radiosensitization Nitrotriazole derivatives |
| 基金项目:国家自然科学基金 |
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| 摘要点击次数: 2480 |
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| 中文摘要: |
| 目的 探讨3-硝基三氮唑衍生物的放射增敏作用,并对其生物学效应作出评价。方法 本文用克隆形成法研究了22个3-硝基-1,2,4-三氮唑衍生物的体外放射增敏活性和乏氧、富氧细胞毒性。结果 两个化合物的活性胜过MISO,有三个化合物与MISO和SR-2508相当,其余的其活性均较低。3-硝基三唑衍生物也像2-硝基咪唑类那样,其放射增敏活性与电子亲和性(用半波还原电位E1/2表示)有关。亲和性越大,即E1/2值越偏正,增敏活性越强。环核N1位和5位上取代基的结构和性质影响着化合物的E1/2、分配系数p和细胞毒性。结论 3-硝基三唑衍生物对乏氧和富氧(空气)细胞的毒性差别是很有限的,所以它们不是有效的乏氧调节细胞毒剂。但某些的放射增敏作用是值得深入研究的。 |
| 英文摘要: |
| Objective To assess the radiosensitization of nitrotriazole derivatives and elucidate the structure activity relationships within this group of compounds. Method The partition coefficient (p), reduction potential (E1/2),cytotoxicity and sensitization activity were determined by HPLC, polarography and colony formation, respectively. Results It was found that among these 22 derivatives,two compounds were more efficient than MISO,and other three were of the same efficiency as MISO was in radiosensitizing hypoxic cells,the rest showed poor radiosensitizing properties.As 2-nitroimidazoles,the radiosensitizing activity of a 3-nitrotriazole derivative correlates with its electron affinity,determined as E1/2,half wave reduction potential.The greater is the electron affinity i.e.the more positive the E1/2,the greater is the radiosensitizing efficiency.The value of E1/2,partition coefficient p value and cytotoxicity of a nitrotriazole derivative are influenced by the structure and chemical properties of the substituent at N1 or 5 position of triazole ring.The nitrotriazoles examined show only limited defferential hypoxic:aerobic toxicity. Conclusion Although the nitrotriazole derivative are not viable hypoxia-mediated cytotoxins, the radiosensitization of some of them should be studied thoroughly. |
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