90Y标记的不同氨基酸序列的RGD环肽的制备及在荷人神经胶质瘤动物模型中的评价

制备⁹⁰Y-DTPA-Bz-NH-SA-c(KRGDf) 和⁹⁰Y-DTPA-Bz-NH-c(ERGDf),并对其体内外性质进行比较。ITLC和HPLC分析结果表明,在pH=5.5和80 ℃条件下反应20 min, 2种标记物的标记率均大于99%,并且2种标记物均具有良好的体外稳定性。荷人神经胶质瘤裸鼠生物分布实验数据表明,2种标记物在各组织的摄取没有显著性差异,且均具有良好的肿瘤靶向性和体内稳定性。2种标记物主要通过肾脏排泄,同时也有一部分标记物通过肝胆系统排泄。良好的体内外性质证明,KRGDf环肽和ERGDf环肽均可进一步用于聚合物多肽药物的开发。     

铼羰基化合物标记含RGD的多肽

αvβ3是一种在包括肿瘤引起的血管增生及肿瘤转移中起重要作用的细胞黏附受体,含RGD序列的肽及其类似物可以作为拮抗剂与αvβ3正常配体进行竞争结合.本工作以三羰基铼为前体标记了2个含有RGD序列的多肽,实验结果表明,2个多肽的标记率和放化纯度均大于90%,体外稳定性良好.将进一步对其进行生物评价,以判别其是否有潜力发展成为肿瘤治疗剂.     

Eu(Ⅲ)和Am(Ⅲ)在Th4(PO4)4P2O7上的吸附行为

通过静态法研究了Am(Ⅲ)和Eu(Ⅲ)在Th4(PO4)4P2O7上的吸附行为,主要包括吸附平衡时间、固液比、pH值、离子强度以及富里酸(FA)等因素对吸附的影响.实验结果表明,Am(Ⅲ)和Eu(Ⅲ)在Th4(PO4)4P2O7上的吸附具有相似的pH吸附曲线,pH值的变化对吸附的影响较大,吸附率在pH=2~5时出现剧增;在其他条件相同时,KNO3离子强度从0.01 mol/L增大到0.1 mol/L,吸附率随着离子强度的增大而减小.通过对比实验发现,FA对Am(Ⅲ)和Eu(Ⅲ)在Th4(PO4)4P2O7上的吸附具有促进作用.Am(Ⅲ)和Eu(Ⅲ)在Th4(PO4)4P2O7表面可能形成了表面络合物.吸附剂的表面特征及其吸附机理研究是进一步深入研究的重点.     

177Lu-DOTA-Bz-RGD dimer和177Lu-DOTA-Bz-PEG4-RGD dimer的制备及生物评价

制备了177Lu-DOTA-Bz-RGD dimer和177Lu-DOTA-Bz-PEG4-RGD dimer,并比较4个PEG分子的引入对标记条件标记化合物体外稳定性、标记化合物的药代动力学性质及其在小鼠体内生物分布的影响。薄层色谱法(TLC)和高效液相色谱法(HPLC)分析结果表明,反应液pH分别为4.0和6.0时,100℃反应15~20 min,两种标记化合物的标记率均>95%。在生理盐水体系中,二者均保持良好的稳定性,放置72 h放化纯度仍>90%。HPLC的分析结果和脂水分配系数lgPow的测定结果显示,177Lu-DOTA-Bz-PEG4-RGDdimer的脂溶性有所提高。引入4个PEG分子没有显著改变标记化合物的药代动力学性质及其在小鼠体内的生物分布。     

多巴胺D4受体PET显像剂18F-FHTP的生物学评价

为研究多巴胺D4受体在精神分裂症、注意力缺乏多动症等疾病病因分析中的作用,开展了多巴胺D4受体PET显像剂3-(4-[18F]氟苄基)-8-羟基-1, 2, 3, 4-四氢苯并吡喃[3, 4-c]吡啶-5-酮(18F-FHTP)的体内外生物学评价.通过体外受体竞争抑制结合分析,测定了FHTP对多巴胺D2样受体的亲和性;通过辛醇实验,测定了18F-FHTP的脂水分配系数;通过大鼠体内的生物分布和阻断分布实验,测定了18F-FHTP在大鼠体内的各感兴趣区域的摄取率.实验测得FHTP对D2, D3受体的亲和常数Ki值分别大于5 800, 3 000 nmol/L;对D4.2受体的Ki值为2.9 nmol/L;测得其脂水分配系数为1.11;大鼠生物分布实验显示,18F-FHTP能通过血脑屏障进入脑,并在纹状体、下丘脑、额叶皮质、海马、小脑等已知的D4受体分布区域有较高的摄取率.体外受体结合分析、脂水分布实验、大鼠体内分布和阻断分布研究表明, 18F-FHTP可作为多巴胺D4受体显像剂用于体内显像研究.     

99Tcm(CO)3-CNRGD的制备及生物学评价

合成了含异腈基团的多肽偶联物（CNRGD）,并用［⁹⁹Tc^m(CO)₃(H₂O)₃］⁺标记,得到具有与整合素α_vβ₃受体多结合位点的⁹⁹Tc^m(CO)₃-CNRGD,并对其进行了体内外生物学评价。结果表明,在优化的标记条件下,⁹⁹Tc^m(CO)₃-CNRGD的标记率达到77%,纯化后,标记物放射化学纯度大于96%。体外稳定性实验显示其具有很高的稳定性;脂水分配系数显示其具有较好的脂溶性。正常小鼠体内分布显示,⁹⁹Tc^m(CO)₃-CNRGD在血液中清除较快,主要通过肝肾代谢。荷MCF-7人乳腺癌裸鼠体内分布显示,注射1、4h后,标记物在肿瘤部位的摄取值达(2.38±0.37)%ID/g和(1.57±0.21)%ID/g,瘤/血比分别达0.71±0.09、1.15±0.15,表明该标记物在肿瘤细胞中有一定的摄取和较长的滞留时间。     

乏氧显像剂99Tcm-HL91衍生物的制备及其活性评价

为寻找性能优良的乏氧显像剂,设计合成了2种HL91衍生物4, 9-二氮-3, 10-二甲基十二烷-2, 11-二酮肟 (TMBAO)和4, 9-二氮-3, 10-二氧基十二烷-2, 11-二酮肟 (H2Pab),并进行99Tcm标记.与已知乏氧显像剂99Tcm-HL91进行比较,并对新标记物的体内外活性进行了评价.乏氧细胞实验结果表明:与99Tcm-HL91相比,99Tcm-TMBAO和99Tcm-H2Pab具有一定的乏氧选择性;荷瘤小鼠体内生物分布数据显示,尽管两种新的99Tcm标记物在肝脏的摄取比99Tcm-HL91低,但其乏氧选择性也同时显著降低.     

整合素素αⅤβ3受体显像剂18F标记RGD肽的研究进展

血管新生是肿瘤生长、转移过程中不可缺少的生物过程。整合素α_Ⅴβ₃受体在新生血管内皮细胞和多种肿瘤细胞表面高表达,在肿瘤血管新生中起着关键作用,目前已成为肿瘤诊断与治疗的一个重要靶点。精氨酸-甘氨酸-天冬氨酸（Arg-Gly-Asp, RGD）肽可特异性地与整合素α_Ⅴβ₃受体结合,¹⁸F标记的RGD肽类化合物PET显像可无创、动态地定量监测整合素α_Ⅴβ₃受体表达,在肿瘤早期诊断、疗效监测及抗血管新生评价上发挥着重要作用。本文就近年来国内外¹⁸F标记RGD 肽在肿瘤α_Ⅴβ₃受体显像中的研究进展作简要综述。     

177Lu-DOTA/DTPA-Bz-Cys-RGDdimer的制备及正常鼠体内生物分布

制备177Lu-DOTA-Bz-Cys-RGD dimer和177Lu-DTPA-Bz-Cys-RGD dimer,并对其体内外性质进行比较.TLC和HPLC分析结果表明,在pH=5.0和100 ℃条件下反应15～20 min,2种标记物的标记率均大于95%,并且在室温条件下2种标记物均保持良好的体外稳定性.HPLC分析结果和脂水分配系数lg P测定结果证实,177Lu-DOTA-Bz-Cys-RGD dimer的脂溶性高于177Lu-DTPA-Bz-Cys-RGD dimer.生物分布实验数据显示,注射后4 h,除了血液和脾,177Lu-DTPA-Bz-Cys-RGD dimer在其它组织中的摄取明显高于177Lu-DOTA-Bz-Cys-RGD dimer,177Lu-DOTA-Bz-Cys-RGD dimer的体内稳定性远好于177Lu-DTPA-Bz-Cys-RGD dimer.Bz-DOTA更适于作为双功能螯合剂用于RGD dimer的177Lu标记.     

负载型Ru/γ-Al2O3催化剂上甲烷与氘化氢之间的氢氘交换性能

实验研究了以浸渍法制备的负载型Ru/γ-Al2O3催化剂体系上甲烷与氘化氢之间的氢氘交换性能,考察了各反应工艺条件包括反应温度、反应原料气流量、反应原料气中HD/CH4的比等因素对Ru/γ-Al2O3催化剂上甲烷与氘化氢之间的氢氘交换性能的影响,采用程序升温还原（H2-TPR）和X射线粉末衍射（XRD）手段对催化剂进行了检测。实验结果表明,Ru和载体γ-Al2O3发生了强相互作用;在对甲烷与氘化氢间的氢氘交换反应中,Ru/γ-Al2O3催化剂显示出较好的催化活性和稳定性。     

PVA和PEG对电子束辐照制备的Fe3O4纳米粒子的影响

常温常压下不加入任何催化剂，用两种不同的活性剂聚乙烯醇（Polyvinyl alcohol，PVA）和聚乙二醇（Polyethylene glycol，PEG），在水溶液中通过电子束辐照可以成功地制备纳米Fe3O4粒子。通过紫外可见光分光光度计（Ultraviolet-visible spectrophotometer，UV）、X射线衍射（x-ray diffraction）、透射电子显微镜（Transmission electron microscopy，TEM）对辐照后的样品的光学特性、结构、形貌、大小进行表征。发现不同的活性剂对纳米粒子的尺寸会产生影响。     

Swelling and thermal properties of porous PNIPAM/PEG hydrogels prepared by radiation polymerization

In this study,a series of porous intelligent hydrogels were synthesized by radiation exhibiting the lower critical solution temperature（LCST） and fast response involving a combination of A’-isopropyl acrylamideas monomer, polyethylene glycol（PEG） as pore-forming agent and N,N-methylene-bis-acrylamide as crosslinking agent.The hydrogels were analyzed by Fourier transform infrared spectroscopy,and the influence of radiation doses on their swelling and thermal behaviors were studied.Their surface morphologies were examined by scanning electron microscopy.The results showed that PEG molecules only acted as pore-forming agent in the cross-linked polymerization.Their swelling ratios reduced with increasing radiation doses.The LCST was around 37℃,and varied little with the radiation doses.The frozen water content of PNIPAM/PEG₆₀₀₀ hydrogel reduced with increasing the radiation dose,and was greater than that of PN1PAM hydrogel at 15 kGy.Hydrogel macropores were prepared by PEG agent,and the hydrogels without PEG had a dense surface.The porous hydrogels are expected to be applied in the field of artificial intelligence material.     

PEG-β-CD/NIPAAm水凝胶的辐射制备及药物控制释放研究

采用聚乙二醇缩水甘油酯(PEGDE)对β-环糊精(β-CD)进行改性,合成了新型水溶性的β-环糊精大分子单体(PEG-β-CD).以电子柬为辐射源对PEG-β-CD和N-异丙基丙烯酰胺(NIPAAm)混合物水溶液进行辐照,制备了poly(PEG-β-CD/NWAAm)水凝胶.与PNIPAAm相比,poly(PEG-β-CD/NIPAAm)水凝胶在室温下具有更高的溶胀率以及在温度升到LCST(Lower Critical Solution Temperature,32℃)后具有更快的收缩响应性.以5-氟尿嘧啶(5-FU)作为模型药物的体外释放实验表明,poly(PEG-β-CD/NIPAAm)水凝胶比PNIPAAm的释放时间有所延长.此现象可能归因于环糊精分子与药物分子形成了包合物.     

Theoretical energy level spectra and transition data for 4p4d, 4p4d4f,and 4p4d configurations of W

The ab initio   quasirelativistic Hartree–Fock method developed specifically for the calculation of spectral parameters of heavy atoms and highly charged ions is used to derive transition data for a multicharged tungsten ion. The configuration interaction method is applied to include electron correlation effects. The relativistic effects are taken into account in the Breit–Pauli approximation for quasirelativistic Hartree–Fock radial orbitals. The energy level spectra, radiative lifetimes and Lande g$g$-factors are calculated for the 4p⁶4d², 4p⁶4d4f, and 4p⁵4d³ configurations of the ion W³⁶⁺. The transition wavelengths, spontaneous transition probabilities, oscillator strengths, and line strengths for the electric dipole, electric quadrupole, electric octupole, and magnetic dipole transitions among the levels of these configurations are tabulated.     

Failure initiation and propagation of Li4SiO4 pebbles in fusion blankets

Lithium orthosilicate (Li₄SiO₄) pebbles are considered to be a candidate as solid tritium breeder in the helium cooled pebble bed (HCPB) blanket. These ceramic pebbles might be crushed during thermomechanical loading in the blanket. In this work, the failure initiation and propagation of pebbles in pebble beds is investigated using the discrete element method (DEM). Pebbles are simplified as mono-sized elastic spheres. Every pebble has a contact strength in terms of critical strain energy, which is derived from a validated strength model and crush test data for pebbles from a specific batch of Li₄SiO₄ pebbles. Pebble beds are compressed uniaxially and triaxially in DEM simulations. When the strain energy absorbed by a pebble exceeds its critical energy it fails. The failure initiation is defined as a given small fraction of pebbles crushed. It is found that the load level for failure initiation can be very low. For example, if failure initiation is defined as soon as 0.02% of the pebbles have been crushed, the pressure required for uniaxial loading is about 2.5 MPa. Therefore, it is essential to study the influence of failure propagation on the macroscopic response of pebble beds. Thus a reduction ratio defined as the size ratio of a pebble before and after its failure is introduced. The macroscopic stress–strain relation is investigated with different reduction ratios. A typical stress plateau is found for a small reduction ratio.     

Theoretical energy level spectra and transition data for 4p4d, 4p4f and 4p4d configurations of W ion

The ab initio quasirelativistic Hartree-Fock method developed specifically for the calculation of spectral parameters of heavy atoms and highly charged ions was applied to determine atomic data for tungsten ions. The correlation effects were included by adopting the configuration interaction method. The Breit-Pauli approximation for quasirelativistic Hartree-Fock radial orbitals was employed to take into account relativistic effects. The energy level spectra, radiative lifetimes, Lande factors g were calculated for the 4p⁶4d, 4p⁶4f and 4p⁵4d² configurations of W³⁷⁺ ion. The atomic data, namely, the transition wavelengths, spontaneous emission rates and oscillator strengths for the electric dipole, electric quadrupole and magnetic dipole transitions among and within the levels of these configurations are tabulated.     

Fluid-to-fluid modeling of critical heat flux in 4 × 4 rod bundles

Fluid-to-fluid modeling of critical heat flux (CHF) is to simulate the CHF behaviors for water by employing low cost modeling fluid, and the flow scaling factor is the key to apply the technique to fuel bundles. The CHF experiments in 4×4 rod bundles have been carried out in Freon-12 loop in equivalent nuclear reactor water conditions (P=10.0–16.0 MPa, G=488.0–2100.0 kg/m² s, X_cr=−0.20–0.30). The models in fluid-to-fluid modeling of CHF is verified by the CHF data for Freon-12 obtained in the experiment and the CHF correlation for water obtained by Nuclear Power Institute of China (NPIC) in the same 4×4 rod bundles. It has been found that the S.Y. Ahmad Compensation Distortion model, the Lu Zhongqi model, the Groeneveld model and Stevens–Kirby model overpredict the bundles CHF values for water. Then an empirical correlation of flow scaling factor is proposed. Comparison of the CHF data in two kinds of test sections for Freon-12, in which the distance of the last grid away the end of heated length is different, shows that the spacer grid, which is located at 20 mm away from the end of the heated length, has evidently influenced on the CHF value in the 4×4 rod bundles for Freon-12. This is different from that for water, and the need for further work is required.     

像素CdZnTe探测器的研制

介绍了研究的像素CdZnTe探测器的研发情况,包括探测器的制作和性能检测.4×4面阵CdZnTe的尺寸为11 mm×11 mm×6.3 mm,像素为2 mm×2mm.性能最好的一个像素对137Cs 662keV伽玛射线的能量分辨率达到了1.4%,在加保护环并进行各像素峰位归一修正后,整个CdZnTe探测器对 137Cs 662keVγ射线的能量分辨率为2.08%.