64Cu放射性药物化学

64Cu半衰期为12.7 h,其衰变过程既发射β+粒子(β+,0.655 MeV,17.8%),又发射β-粒子(β-,0.573 MeV,38.4%)。近20年来,随着铜配位化学的发展,新型配体不断出现(如DOTA、TETA、NOTA、CB-TE2A、C3B-DO2A等)。Cu(Ⅱ)的络合物在生物体内/外的稳定性不断提高,64Cu已经成功标记在氨基酸、多肽、蛋白、核酸等分子以及纳米颗粒上。64Cu可制成正电子显像药物用作诊断,同时也有发展为放射性治疗药物的潜力。新型铜配体和标记方法以及新的药物靶标的研究已经成为64Cu放射性药物研究的热点,至今已研制出了多种64Cu标记的放射性药物,如64Cu-ATSM是有效的肿瘤乏氧显像剂,64Cu-PTSM是优良的血流示踪剂等。本文旨在介绍64Cu(Ⅱ)几种主要类型的含氮配体以及64Cu标记的放射性药物在显像和治疗方面的最新研究进展,并展望其发展趋势。     

适合低PH范围测量的新型中性载体膜PH电极的研究

本文设计合成了一种在低ＰＨ范围对氢离子有很好Ｎｅｒｎｓｔ响应的新型中性载体－Ｎ，Ｎ－二辛基菸酰胺，并把它制成ＰＶＣ膜ＰＨ电极，测试了该电极的线性范围、选择性、稳定、重现性和内阻等各项性能参数，并试验了电极抗氢氟酸腐蚀的能力，该该电极用于氢氟酸的电离常数测定时获得了满意的结果。     

Study of chromium-containing proteins in subcellular fractions of rat liver by enriched stable isotopic tracer technique and gel filtration chromatography

Ten male Wistar rats were intravenously injected with a single approximately physiological dose of enriched stable isotopic Cr-50 tracer solution (200 ng (50)Cr(3+)/100 g body wt). The fundamental distribution patterns of the chromium-containing proteins in the nucleic, mitochondrial, lysosomal, microsomal, and cytosolic subcellular fractions of the rat liver were investigated by means of Sephadex G-100 gel chromatography combined with neutron activation analysis via (50)Cr (n, gamma) (51)Cr reaction. In total, nine kinds of Cr-containing proteins were found in the five subcellular fractions, whose relative molecular masses were 96.6+/-6.2, 68.2+/-1.4, 57.9+/-4.7, 36.6+/-1.2, 24.2+/-1.8, 14.0+/-1.5, 8.8+/-0.6, 6.9+/-0.4, and 4.2+/-0.4 kDa. Approximately 64.5% of Cr proteins accumulated in the cytosolic fraction. The second enriched part was the nucleic fraction; about 12.2% Cr proteins were stored in this section. The 4.2-kDa molecular mass might contain the so-called low molecular weight chromium-containing substance; however, in this research, it was only observed in the mitochondria, lysosome, and microsome. In the mitochondrial fraction, most of the Cr proteins were present as relatively low molecular weight substances: about 56% of chromium-containing proteins had molecular masses < or =6.9 kDa. Nevertheless, more than 69% of Cr-containing proteins were observed with molecular masses > or =57.9 kDa in the liver cytosolic fraction.     

A new neutron activation technique for simultaneous determination of inorganic and total mercury contents in human hair

A simple method for simultaneous determination of inorganic and total mercury contents in human hair by neutron activation analysis (NAA) has been developed. The method is based on the selective extraction of methylmercury from hair by hydrochloric acid. Thus, the residual phase containing inorganic mercury can be determined by NAA. Further, the methylmercury contents in hair samples are easily calculated by subtracting the inorganic mercury contribution from the total Hg simultaneously given by INAA. Several reference materials of human hair, including IAEA hair RM 085 and 086, Chinese hair RMs GBW 09101 and 07601, were analyzed by this method. Our results show that the method is reliable.     

超临界CO2萃取薰衣草的挥发性组分

1.1样品来源及制备薰衣草：购于新疆远馨香料开发公司。超临界CO2萃取：薰衣草经农用粉碎机粉碎后,用自制的0．5L超临界装置进行萃取(萃取压力：10MPa,萃取温度：321K,萃取时间：120min),得到橙色透明油状物,得率约为2．0％～2．5％,水汽蒸馏：薰衣草粉碎后,经共水蒸馏同时用油水分离器分离精油,3h后收集精油并用无水硫酸钠干燥,得淡黄色油状物,得率约为0．8％～1．0％。     

Computational Screening for the Anticancer Potential of Seed-Derived Antioxidant Peptides: A Cheminformatic Approach

Some seed-derived antioxidant peptides are known to regulate cellular modulators of ROS production, including those proposed to be promising targets of anticancer therapy. Nevertheless, research in this direction is relatively slow owing to the inevitable time-consuming nature of wet-lab experimentations. To help expedite such explorations, we performed structure-based virtual screening on seed-derived antioxidant peptides in the literature for anticancer potential. The ability of the peptides to interact with myeloperoxidase, xanthine oxidase, Keap1, and p47^phox was examined. We generated a virtual library of 677 peptides based on a database and literature search. Screening for anticancer potential, non-toxicity, non-allergenicity, non-hemolyticity narrowed down the collection to five candidates. Molecular docking found LYSPH as the most promising in targeting myeloperoxidase, xanthine oxidase, and Keap1, whereas PSYLNTPLL was the best candidate to bind stably to key residues in p47^phox. Stability of the four peptide-target complexes was supported by molecular dynamics simulation. LYSPH and PSYLNTPLL were predicted to have cell- and blood-brain barrier penetrating potential, although intolerant to gastrointestinal digestion. Computational alanine scanning found tyrosine residues in both peptides as crucial to stable binding to the targets. Overall, LYSPH and PSYLNTPLL are two potential anticancer peptides that deserve deeper exploration in future.     

三辛胺从盐酸介质中萃取金（Ⅲ）

三辛胺(TOA)从盐酸介质中萃取、富集金,已应用于原子吸收光谱法测定金,其高灵敏度及选择性使该方法成为金的十分理想的测定方法。本文考查了TOA从盐酸介质中萃取金(Ⅲ)的机理,试图对金(Ⅲ)的萃取分离及测定提供理论依据。 TOA系Fluka进口分装,使用时按计算量配成所需浓度的CCl_4溶液;HAuCl_4用纯金(99.99%)制备;NaCl为基准试剂;其它试剂均不低于分析纯。水相由HAuCl_4-HCl-NaCl配     

Interactions of phosphorylated cyclohexapeptides with uranyl: insights from experiments and theoretical calculations

Two phosphorylated cyclohexapeptides (CPs) bearing one (CP1) or two phosphates (CP2) were synthesized to explore the interactions between uranyl ions and very small cyclic peptides. According to the results of the ESI–MS and fluorescence titrations, the 1:1 uranyl-CPs complexes are the main products with the affinity constants of 7.3?×?10⁴ and 2.0?×?10⁵ for CP1 and CP2, respectively. Density functional theory calculations indicate phosphoryl and carboxyl groups coordinate uranyl in mono-dentate and bi-dentate fashions due to steric effects, which is consistent with the results of extended X-ray absorption fine structure spectroscopy.

     

Influence of compound danshen tablet on the pharmacokinetics of losartan and its metabolite EXP3174 by liquid chromatography coupled with mass spectrometry

Losartan is an effective anti‐hypotension drug frequently used in clinic. Compound danshen tablet (CDST) is an important traditional Chinese multiherbal formula composed of Danshen, Sanqi and Bingpian, which is widely used for the treatment of cardiovascular and cerebrovascular diseases in China. More often, losartan and CDST are simultaneously used for the treatment of anti‐hypertension in the clinic. The aim of this study was to compare the pharmacokinetics of losartan and EXP3174 after oral administration of single losartan and both losartan and CDST, and to investigate the influence of CDST on the pharmacokinetics of losartan and its metabolite EXP3174. Male Sprague–Dawley rats were randomly assigned to two groups: a losartan‐only group and a losartan and CDST group. Plasma concentrations of losartan and EXP3174 were determined by LC‐MS at designated points after drug administration, and the main pharmacokinetic parameters were estimated. It was found that there were significant differences (p < 0.05) between the pharmacokinetic parameters of losartan and EXP3174, which showed that CDST influenced the metabolism and excretion of losartan in vivo. The result could be used for clinical medication guidance of losartan and CDST to avoid the occurrence of adverse reactions. Copyright © 2013 John Wiley & Sons, Ltd.