N-乙酰基-S-烯丙基-L-半胱氨酸的合成及其抗辐射活性  

Synthesis and anti-irradiation activities of N-acetyl-S-allyl-L-cysteine

作　　者：牟感恩 龙伟[1] 李园园[1] 于光允[1] 沈秀[1] 周则卫[1] MU Gan＇en LONG Wei LI Yuanyuan YU Guangyun SHEN Xiu ZHOU Zewei(Institute of Radiation Medicine, Chinese Academy of Medical Sciences ＆ Peking Union Medical College, Tianjin 300192, China)

机构地区：[1]中国医学科学院北京协和医学院放射医学研究所,天津300192

出　　处：《辐射研究与辐射工艺学报》2017年第5期9-16,共8页Journal of Radiation Research and Radiation Processing

基　　金：天津市自然科学基金重点项目(15JCZDJC33400)资助~~

摘　　要：以L-半胱氨酸为原料,经取代和酰化两步反应合成目标产物N-乙酰基-S-烯丙基-L-半胱氨酸(N-acetyl-S-allyl-L-cysteine,NAc-SAC)。以^(137)Csγ射线照射至不同剂量的ICR小鼠作为研究对象,通过30 d存活率实验、血相和免疫系统实验、各项脏器指数以及外周血淋巴细胞彗星实验,研究目标化合物分别在200、400、600 mg/kg给药剂量下的抗辐射活性。ICR小鼠经伽马射线照射至致死剂量7.5 Gy后,其存活率由单纯照射对照组的41.6%,分别提高到NAc-SAC给药组的58.3%、50.0%和66.7%,平均存活天数明显延长。^(137)Csγ射线照射至亚致死剂量6.0 Gy后,NAc-SAC在不同程度上增加了受照小鼠的脾指数、脾结节数(CFU-S)、骨髓DNA含量和白细胞数。彗星实验中7.0 Gy伽马射线照射联合NAc-SAC给药组小鼠外周血淋巴细胞的尾长、尾矩、Olive尾矩和尾部DNA百分含量明显低于7.0 Gy伽马射线单纯照射组(p<0.01),提示NAc-SAC可明显降低辐射导致的DNA损伤。本研究表明,目标化合物NAc-SAC具有一定的抗辐射损伤作用。The N-acetyl-S-allyl-L-cysteine（NAc-SAC） was synthesized by substitution and acylation reactions with L-cysteine as raw materials. Experiments on blood and immune-organs indexes, and survival rates of ICR mice within 30 d after ^137Csγ-rays irradiation at different doses, as well as the comet assay were carried out to investigate the anti-irradiation effects of NAc-SAC. The survival rates of mice irradiated at 7.5 Gy with the dose of NAc-SAC at 200 mg/kg, 400 mg/kg, and 600 mg/kg increased to 58.3%, 50.0% and 66.7%, respectively, and the average survival time was significantly prolonged compared with that in the control group. The spleen indexes, colony forming cell-spleen（CFU-S）, percentages of DNA, number of white blood cells of mice irradiated at 6.0 Gy increased under the action of NAc-SAC. The tail length, tail moment, olive tail moment, and tail DNA percentage of peripheral blood lymphocytes of mice irradiated at 7.0 Gy combined with NAc-SAC were higher than those for the control group（p〈0.05）. To conclude, NAc-SAC has a protective effect against damage induced by irradiation.

关 键 词：N-乙酰基-S-烯丙基-L-半胱氨酸 辐射防护剂 小鼠 抗辐射活性 137Csγ射线 

分 类 号：TL7[核科学技术—辐射防护及环境保护]