氚示踪法研究吲哚美辛在C57小鼠体内的分布及其抗肿瘤作用

采用氚标记吲哚美辛(Indomethacin,IN)示踪技术,观察3H-IN在Lewis肺癌C57小鼠体内的分布及IN治疗Lewis肺癌的效果。结果显示:3H-IN选择性浓聚于肿瘤组织,服药后4 h肿瘤组织的放射性摄取(ID％／g)达较高水平,此后其清除速率明显慢于其它组织;服药后7 h,肿瘤组织与肌肉、脂肪、血液之间的放射性摄取有差异(P<0.05),12 h差异显著(P<0.01)。肿瘤组织与肌肉、脂肪、血液的放射性摄取比4 h开始>1,12 h达最高。IN的抑瘤和抗癌作用结果显示:用IN治疗的Lewis肺癌C57小鼠在接种后第20天肿瘤体积为3.59 cm2,仅服用生理盐水的小鼠(对照组)肿瘤体积为8.37 cm2,其抑瘤率为57.1％;接种肿瘤早期即口服IN的小鼠未见肿瘤生长。以上结果表明IN有较强的肿瘤靶器官亲和性,可选择性浓聚于肿瘤组织,并长时间存留,具有较强的抑制肿瘤及抗肿瘤作用。     

Nuclear Data Sheets for A = 211

The evaluated spectroscopic data are presented for 11 known nuclides of mass 211 (Hg, Tl, Pb, Bi, Po, At, Rn, Fr, Ra, Ac, Th). The ²¹¹Pa nuclide is included here but its identification remains uncertain. For ²¹¹Hg, ²¹¹Tl, ²¹¹Ac and ²¹¹Th nuclei, only the ground–state information is available. Their decay characteristics are mostly unknown. ²¹¹Fr is suggested to decay partially through ε decay mode, but its decay scheme remains poorly known. While high–spin excitations, including several isomers, are well studied in ²¹¹Pb, ²¹¹Bi, ²¹¹Po, ²¹¹At, ²¹¹Rn and ²¹¹Fr, the particle–transfer data are available for only ²¹¹Po and ²¹¹Bi.This evaluation was carried out as part of joint IAEA–ICTP workshop for Nuclear Structure and Decay Data, organized and hosted by the IAEA, Vienna and ICTP, Trieste, August 6–17, 2012. This work supersedes previous A=211 evaluation (2004Br45) published by E. Browne which covered literature before January 2003.     

~(211)At标记蛋白质和多肽的制备

砹是重卤素,它是一个不存在稳定性同位素的放射性元素,半衰期7.2小时;它的α衰变分支比为42％,K电子俘获衰变分支比为58％;α粒子的平均能量为6.8MeV,在生物组织内的平均射程约为60μm。由于α粒子具有极强的电离效应,因而砹化的亲肿瘤化合物具有杀伤肿瘤细胞的潜在能力。从六十年代末就开始制备了多种~(211)At标记的化合物,1983年中国原子能科学研究院在我国首次制得了Na~(211)At。我们采用固相酶、H_2O_2和氯胺-T等方法对BSA、IgG和甲硫-脑啡肽等进行了砹化标记。     

211At标记放射治疗药物进展

^211At具有良好的放射生物学性质，是一种有希望的肿瘤放射性治疗核素。本文在参考39偏论文的基础上，综述了^211At标记放射治疗物近年来取得的一些可喜进展，对^211At标记放射治疗药物研究存在的问题，现状及临床应用前景也进行了探讨。     

~（99）Tc~m直接标记单克隆抗体的研究Ⅰ．用~（99）Tc~m标记Fab（3

总结了一种简便、可靠的直接标记法，并成功地运用此法对含巯基较少的Ｆａｂ片段进行了标记，得到了很好的标记率和体外稳定性以及较好的对荷瘤裸鼠的体内分布和显像结果。     

3H11的~(123)I标记及其生物分布

采用Iodogen氧化法对胃癌单克隆抗体3 H11进行了123I标记,用PD-10层析柱分离纯化标记物,纸层析法测定标记物的标记率和放化纯度,评价标记物的体外稳定性,并观察了标记物在正常小鼠体内的生物分布。标记结果显示,123I-3 H11的优化标记条件为:Iodogen 10μg、3 H11 30μg、Na123I溶液20μL(13.3 MBq)、磷酸盐缓冲溶液100μL(pH7.4、0.2 mol/L)、常温下反应8 min,123I-3 H11标记率70%~80%;稳定性结果显示,标记物在4℃人血清中的体外稳定性较好,放置48 h后放化纯度92%;正常昆明鼠体内生物学分布显示,全抗3 H11血液半清除时间为12.25±0.25 h,胃组织有明显摄取。以上结果提示,123I-3 H11是一种很有前景的肿瘤放射免疫显像剂。     

^211At通过DTPA酸酐标记IgG

研究了２１１Ａｔ通过二乙撑三胺五乙酸（ＤＴＰＡ）酸酐标记人免疫球蛋白Ｇ（ＩｇＧ）的方法。合成ＤＴＰＡ酸酐后与人ＩｇＧ反应，制得ＤＴＰＡ－ＩｇＧ。Ｎａ２１１Ａｔ溶液与分离纯化后的ＤＴＰＡ－ＩｇＧ在室温下反应３０ｍｉｎ，经ＳｅｐｈａｄｅｘＧ５０柱分离纯化，得２１１Ａｔ－ＤＴＰＡ－ＩｇＧ的０．１ｍｏｌ／ＬＰＢＳ淋洗液。整个标记过程可在１．５ｈ完成，全程标记率在６０％以上。测定了２１１Ａｔ－ＤＴＰＡ－ＩｇＧ在体外的稳定性，并通过比较标记物与Ｎａ２１１Ａｔ注射液在ＮＩＨ小鼠体内的分布和代谢，评价了２１１Ａｔ－ＤＴＰＡ－ＩｇＧ在体内的稳定性。     

离子型~(211)At致体外艾氏腹水癌细胞超微结构的改变

报道离体培养的小鼠艾氏腹水癌细胞用37—222kBq/ml的离子型~(221)At分四个剂量处理,透射电镜观察,发现细胞内膜系统受到严重辐射损伤。剂量越大,损伤越严重。辐射敏感的靶部位为细胞核(核膜)、线粒体,其形态变化最为显著。     

人参皂甙20(S)-protopanaxadiol的氘、氚标记及其在A549细胞内的浓度

分别用钠硼氘、钠硼氚还原人参皂甙Rh1的活性形式20(S)-protopanaxadiol（aPPD）的氧化前体aPPD=O，制备氘、氚标记的aPPD。标记物经板层析（TLC）、质谱(MS)、核磁共振（NMR）分析鉴定，结果与标准品的测量数据一致；氚标记的aPPD放化纯度为98%，放射性比活度为7.64×1011Bq/g。将3H-aPPD作用于人肺腺癌A549细胞，检测不同时间细胞浆及细胞核中氚的活度，结果提示aPPD在A549细胞浆、核内均于24 h达到最高浓度，表明aPPD作为一个与甾体类激素结构相类似的药物，可以进入细胞甚至细胞核发挥药理作用     

利用γ-32P-ATP，51Cr研究蛋白激酶C对血管内皮细胞CD44表达及内皮粘附功能的影响

分别用钠硼氘、钠硼氚还原人参皂甙Rh1的活性形式20(S)-protopanaxadiol（aPPD）的氧化前体aPPD=O，制备氘、氚标记的aPPD。标记物经板层析（TLC）、质谱(MS)、核磁共振（NMR）分析鉴定，结果与标准品的测量数据一致；氚标记的aPPD放化纯度为98%，放射性比活度为7.64×1011Bq/g。将3H-aPPD作用于人肺腺癌A549细胞，检测不同时间细胞浆及细胞核中氚的活度，结果提示aPPD在A549细胞浆、核内均于24 h达到最高浓度，表明aPPD作为一个与甾体类激素结构相类似的药物，可以进入细胞甚至细胞核发挥药理作用。     

^188Re—labeled McAb 3H11 used as preventive for the peritoneal micrometasis of gastric cancer

In advancing gastric cancer, especially when the serous is invaded, the plantation of cancer cells in peritoneal is common and it affects patients' survival time severely. Based on successfully labeled McAb (monoclonal antibody) 3H11 with ~(188)Re, we investigated the effect of RIT (Radioimmuno-Therapy) with ~(188)Re-3H11 on preventing the peritoneal micrometastasis of gastric cancer cells in nude micc to increase the survival time. After 1×10~6 BGC-823 gastric cancer cells were injected into the peritoneal cavity of each mouse, 45BABL/C nude mice were divided into 9 groups. Each group received different doses of ~(188)Re-3H11 or ~(188)Re-IgG, or saline I.P.16 hours postoperation. The injected volume of each mouse was 1.0mL. The results showed that the survival time depended on the injected doses during 0 to 37 MBq. The survival time was 170±25.3d after 37MBq ~(188)Re-3H11 were treated. It was over 5 times more than that for the saline group and about 3 times more than that for 37 MBq ~(188)-Re IgG gro     

Effect of ^211At treating pollen and stigma on generative cells and seed setting of rice

Low specific radioactivity (7.4kBq/ml) ^211At treating pollen and stigma can obviously affect morphological structures and physiological functions of pollen,stigma and ovule or embryo sac cells,and cause injury.Results showed that because of the radiation effects the seed setting rate of rice was decreased,and the development of some embryos were affected and others became abnormal.     

Atmospheric-pressure dielectric barrier discharge generation by a full-bridge flying capacitor multilevel inverter

A new configuration of a resonant full-bridge flying capacitor multicell inverter has been designed and constructed with the aim of achieving an extended output voltage frequency range with low harmonic distortion and reduced semiconductor commutation losses. This configuration was tested as a power supply for two different coaxial dielectric barrier discharge reactors, one of them employed for electric characterization and the other one for inorganic compound elimination in an aqueous solution. Two different gas mixtures, 90% Ar–10% O_2 and80% Ar–20% O_2, were individually supplied during the experiments; the results showed a highefficiency removal of meta-cresol(m-cresol) to the order of 98%, which was obtained by adding more oxygen to the plasma gas mixture.     

188Re-labeled McAb 3H11 used as preventive for the peritoneal micrometasis of gastric cancer

In advancing gastric cancer,especial1y when the serous is invaded,the p1antation of cancer cells in peritoneal is common and it affectspatients' survival time severe1y. Based on successfully labeledMcAb (monoclonal antibody) 3H11 with ¹⁸⁸Re,we investigated the effect of RIT (Radioimmuno-Therapy) with¹⁸⁸Re-3Hll on preventing the peritoneal micrometastasis ofgastric cancer cells in nude mice to     

近年来211At放射性药物研究的新进展

加速器制备的α核素²¹¹At是最适宜于靶向内放射治疗的理想核素之一。本文在参考最新文献的基础上,简要介绍了²¹¹At标记放射治疗药物近年来取得的一些可喜进展,包括²¹¹At的制备方法、标记物实验和临床研究以及标记方法等。对²¹¹At标记放射治疗药物研究存在的问题、现状及临床应用前景也进行了探讨。     

Tensile properties of ferritic/martensitic steels irradiated in STIP-I

Specimens of ferritic/martensitic (FM) steels T91, F82H, Optimax-A and the electron beam weld (EBW) of F82H were irradiated in the Swiss spallation neutron source (SINQ) Target-3 in a temperature range of 90-370 °C to displacement doses between 3 and 12 dpa. Tensile tests were performed at room temperature and the irradiation temperatures. The tensile test results demonstrated that the irradiation hardening increased with dose up to about 10 dpa. Meanwhile, the uniform elongation decreased to less than 1%, while the total elongation remained greater than 5%, except for an F82H specimen of 9.8 dpa tested at room temperature, which failed in elastic deformation regime. At higher doses of 11-12 dpa, the ductility of some specimens recovered, which could be due to the annealing effect of a short period of high temperature excursion. The results do not show significant differences in tensile properties for the different FM steels in the present irradiation conditions.     

125I籽源持续低剂量率照射诱导人肺癌细胞的旁效应

观察125I籽源持续低剂量率照射诱导人肺癌细胞损伤的旁效应.选择对高剂量率外照射敏感性不同的A549人肺腺癌细胞和NCI-H446人小细胞肺癌细胞,采用125I籽源离体照射细胞模式,将直接受照细胞与未受照细胞共培养24h,应用CB微核法和γH2AX荧光免疫分析法,检测2Gy和4Gy125I籽源持续低剂量率照射诱导人肺癌细胞的微核形成和DNA双链断裂水平.结果表明,125I籽源照射能显著诱导A549和NCI-H446细胞的微核形成率和γH2AX位点形成率增加的旁效应,显示增强对肿瘤细胞的杀伤作用.旁效应强弱与累积照射剂量、肿瘤细胞的辐射敏感性相关:对高剂量率外照射敏感的NCI-H446细胞对低剂量率照射及其旁效应的敏感性高于A549细胞,但与直接辐射效应相比,125I籽源照射诱导A549细胞旁效应高于NCI-H446细胞,这两种细胞的辐射旁效应均随累积照射剂量增加而降低,提示介导旁效应的信号因子水平可能随细胞损伤程度的增加而下降.     

α放射核素靶向治疗研究进展

α放射核素在内照射时具有极强的细胞毒性,对肿瘤细胞具有较强的杀灭作用,而其短射程对正常组织影响较小,因此α放射核素类药物是放射性药物研究的重要领域和研究热点之一。α放射核素类药物的生产和研究关键在于核素的选择、高纯度核素的稳定可靠供应、核素载体及合适的体内动力学。目前国内外研究比较活跃的α放射核素主要包括223 Ra、225 Ac、213 Bi、211 At、212 Bi、149 Tb和227 Th等。本文主要介绍了以上核素的来源制备及用于肿瘤靶向治疗的最新进展,对存在的问题、现状及临床应用前景进行了简要的探讨。     

几种治疗核素标记抗体在肿瘤治疗方面的应用与进展

放射性核素标记的单克隆抗体不仅具有可以减少因外照射引起的正常组织损伤及全身性副作用,而且还能杀灭McAb不能达到的癌细胞以及受抗原修饰作用小等优点,因此逐渐成为实用价值较大的导向治疗方法。迄今,用于肿瘤放射免疫治疗(RIT)的放射性核素主要有131I,90Y,188Re,186Re,153Sm,211At等。文章主要介绍了几个治疗核素标记抗体在肿瘤治疗方面的应用与进展。     

Preparation and biological evaluation of ^99Tc^m-labelled fatty acids

The aim of the present work was to develop radiolabelling fatty acids based on ^99Tc^m carbonyl chemistry for heart imaging. Undecanoic acids functionalised with iminodiacetatic acid and cysteine were radiolabelled with [^99Tc^m（CO）3（H2O）3]^＋ intermediates, and their radiolabelling conditions were carefully studied. Biodistribution of ^99Tc^m（CO）3-CYST FAC 11 and ^99Tc^m（CO）3-IDA FAC 11 were observed in normal mice. The results showed that two ^99Tc^m-labelled compounds had similar profile in terms of high initial radioactivity uptake and rapid washout of radiotracers in the heart. ^99Tc^m （CO）3-IDA FACII was mainly excreted via hepatobiliary system in contrast to ^99Tc^m （CO）3-CYST FAC11, which was excreted from urinary system. It may be in part attributed to the more lipophilicity of ^99Tc^m （CO）3-IDA FAC11 than ^99Tc^m （CO）3-CYST FAC11.