富勒烯大环多胺衍生物的合成及对铀的促排

Synthesis of a fullerene macrocyclic derivative and its effect on excretion promotion of uranium

本工作对富勒烯进行修饰,将cyclen连接在富勒烯上,成功合成了一种潜在的促排化合物——多取代富勒烯大环多胺衍生物(CB),运用改良寇氏法得到了化合物的半致死剂量,在完成其毒性实验的基础上,建立了染铀的小鼠模型,探究该化合物对小鼠体内铀的促排效果。结果表明,多取代富勒烯大环多胺衍生物的半致死剂量为1.767 mg;CB进入小鼠体内并不会改变铀在小鼠体内的分布规律;与二乙基三胺五乙酸(DTPA)阳性对照组和空白组相比,CB对小鼠肝脏和骨骼中的铀有较明显的促排效果。CB可作为一种潜在的铀促排化合物。

Background： With the development of nuclear technology, radionuclides are widely used in every walk of life, such as reactor, radiation breeding, radiopharmaceutical imaging diagnosis and therapy of disease, etc. While application of radioactive material becomes broader, the possibility of radioactive accident becomes higher. Purpose： In order to effectively treat and timely control the radioactive accident, effective protection therapies are indispensable. Fundamental measure that controls internal exposure is mainly accelerated by reducing absorption and elimination of radionuclides in the body, that is, to look for a suitable suction blocking agent or a radionuclide chelating agent. Methods： We modified fullerenes, and a new chelating agent （fullerene macrocyclic polyamine derivatives, CB） was synthesized via the introduction of Nitrogen-containing Heterocyclic functional perssad onto the surface of fullerene. Improved Karber method was applied, and LDs0 of the compound was obtained. On the base of toxicity experiment, excretion promotion of CB to uranium was explored through the establishment of a mouse model of infection uranium. Results： The experimental results shown that the median lethal dose of CB was 1.767 mg, and CB could not change the bio-distribution of uranium significantly in mice. CB could reduce the accumulation of uranium in liver and bone in mice obviously, as compared with positive control group Diethylene triamine penlaacetic acid （DTPA） and blank control group. Conclusion： Our analyses suggest that CB possesses the potential chelating agent of U in mice.