两种保护剂对C离子诱导小鼠急性肝损伤的应答；Response of Two Protective Agents to Acute Injury Induced by ~(12)C~(6+) Ions in Mouse Liver

比较了N-乙酰半胱氨酸(NAC)及乙酰左旋肉毒碱(ALCAR)对12C6+离子照射小鼠的损伤效应,并探讨了其可能的作用机制。利用4Gy剂量的12C6+离子束对预先给予NAC(100mg/kg)和ALCAR(100mg/kg)保护的昆明小鼠进行单次全身照射。随后检测肝组织中总抗氧化能力(TAC)、DNA单链断裂和细胞凋亡率。结果显示,与照射对照组相比,提前给予NAC和ALCAR均极显著地增强了肝组织的抗氧化能力(P<0.001),减轻了12C6+离子导致的肝组织中DNA断裂(P<0.001)和细胞凋亡(P<0.001)。此外,还发现ALCAR组抗重离子辐照损伤的能力显著地高于NAC组(P<0.05)。实验结果提示了NAC和ALCAR可通过抵御组织内的氧化胁迫,阻止DNA链的断裂和细胞的凋亡,实现对C离子辐照损伤的保护效应。而且ALCAR比NAC可能更适合成为有潜力、有希望的抗C重离子辐射药物。

Functional gold nanoparticle-peptide complexes as cell-targeting agents

In this paper, we report a novel approach using peptide CALNN and its derivative CALNNGGRRRRRRRR (CALNNR(8)) to functionalize gold nanoparticles for intracellular component targeting. The translocation is effected by the nanoparticle diameter and CALNNR8 surface coverage. The intracellular distributions of the complexes are change from the cellular nucleus to the endoplasmic reticulum by increasing the density of CALNNR8 at a constant nanoparticle diameter. Additionally, increasing the nanoparticle diameter at a constant density of CALNNR8 leads to less cellular internalization.

Mn~(2+)-NaY型分子筛作为口服胃肠道MRI造影剂的研究

用离子交换法制备了Mn2+交换的NaY分子筛MnNaY,用红外光谱(IR)和X射线粉末衍射(XRD)等方法进行了表征.研究了Mn2+含量为3.2%的样品在酸性水溶液中的稳定性和离子交换选择性.弛豫时间测量和体内磁共振成像实验表明其弛豫效率变化范围为4.9～9.7mmol·L·s-1,高于目前临床所用造影剂Gd-DTPA,对胃部MRI信号具有良好的增强效果.它是比较好的潜在口服胃肠道造影剂.

Effect of nucleating agents on the crystallization of poly(3-hydroxybutyrate-co-3-hydroxyvalerate)

The effect of nucleating agents on the crystallization behavior of poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) was studied. A differential scanning calorimeter was used to monitor the energy of the crystallization process from the melt and melting behavior. During the crystallization process from the melt, nucleating agent led to an increase in crystallization temperature (T-c) of PHBV compared with that for plain PHBV (without nucleating agent). The melting temperature of PHBV changed little with addition of nucleating agent. However, the areas of two melting peaks changed considerably with added nucleating agent. During isothermal crystallization, dependence of the relative degree of crystallization on time was described by the Avrami equation. The addition of nucleating agent caused an increase in the overall crystallization rate of PHBV, but did not influence the mechanism of nucleation and growth of the PHB crystals. The equilibrium melting temperature of PHBV was determined as 187degreesC. Analysis of kinetic data according to nucleation theories showed that the increase in crystallization rate of PHBV in the composite is due to the decrease in surface energy of the extremity surface.

电中性的GdDTPA双酰胺衍生物作为MRI造影剂

1988年德国卫生局批准(NMG)_2[Gd(DTPA)·H_2O]可作为 MRI 造影剂临床应用(商品名为 Magnevist),NMG 为 N-甲基葡萄糖胺根。从药物动力学角度看,Gd(DTPA)具有弛豫性强、毒性小、细胞外分布、不通过正常的血脑屏障、迅速由肾脏排出、在人体内结构稳定、具有高溶解度等特征。Gd(DTPA)对中枢神经系统病变增强效果良好,但是组织分布无特异性,对腹部器官如肝脏、脾脏的成像效果较差。为了改善其器官选择性,而且使生物体更易接受,减少毒副作用,人们在电中性的 GdDTPA 衍生物方面作了许多努力。

Synthesis, characterization, stability and relaxation behaviours of rare earth heteropolymetalates

Two rare earth heteropolymetalates K9GdW10O36 and K-11[Gd(PW11O39)(2)] have been synthesized and characterized by IR and elemental analysis. Their stability has been studied by TG - DTA. The TG - DTA analysis show that both complexes are of good thermal stability. Their relaxivity in D2O is 6.89 and 5.27 mmol(-1).s(-1) respectively. Interaction with BSA has also been investigated. The results indicate that the two rare earth heteropolymetalate may be potential contrast agent for MRI.

Studies of Gd-diethylenetriamine pentaacetic acid in boving serum albumin solution by nuclear magnetic resonance spectroscopy

In this paper, the water relaxation enhancement behavior of Gd-diethylenetriamine pentaacetic acid(DTPA) in water and in aqueous solution of bovine serum albumine(BSA) has been studied. The T-1 relaxivity of Gd-DTPA in BSA solution is higher than that in aqueous solution. The results indicate that Gd-DTPA can integrate non-covalently with BSA mainly in forms of (Gd-DTPA) . BSA, (Gd-DTPA)(2) . BSA, for which the apparent equilibrium constant is 0.026 mmol(-1).L,0.0018 mmol(-2).L-2 respectively. This method would be used to study the interactivities between protein and contrast agent.

NMR titration and molecular model MOPAC calculation of protonation processes of two MRI ligands

The protonation process of two DTPA bis(amide) derivatives, DTPA-BDMA and DTPA-BDEA, was studied by using H-1 NMR titration and MOPAC calculation. Their protonation process was proposed in the order of the central amine, the terminal amines, the central carboxyl, the terminal carboxyl, the other terminal carboxyl and central amine. During the protonation of the terminal amine, there existed a large fraction of proton transfer from the central amine to the other terminal amine.

Studies on structure-property relationship between color reagents and contrast of their color reactions with cerium by topological indices

In this paper, three topological indices A(m1), A(m2) and A(m3) have been applied to multivariate analysis in structure property relationship studies. The topological indices oi fourty-three asymmetrical phosphono bisazo derivatives of chromotropic acid have been calculated, The structure-property relationship between color reagents and contrast of color reactions with cerium has been studied by A, indices and structure selective factors, Good results have been obtained.

稀土化合物的一种新用途(上)——核磁共振成像(MRI)用造影剂

磁共振成像(Magnetic Resonance Imaging简称MRI)是近十几年来发展起来的一种新的医疗诊断手段,与x-射线计算机断层扫描(Computed Tomography简称x-CT)相比,具有明显的优点,如对脑部、腹腔部、椎间盘组织等的病变有较高的灵敏度。同时,由于磁场和射频电波对人体健康的损害远远小于x-CT产生的x-射线,因此,MRI法已成为当前

稀土化合物的一种新用途(下)——核磁共振成像(MRI)用造影剂

对选择MRI造影剂的要求及其应用MRI造影剂的选择除需遵循生物药剂的一般要求,如溶解性、稳定性等外,尚需有以下特殊要求。弛豫性质:所选择的试剂必须能大大增强靶组织被观测核的弛豫速率。能使弛豫速率增强10～20%的试剂,则可在MRI中应

High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections

The high mortality rate of immunocompromised patients with fungal infections and the limited availability of highly efficacious and safe agents demand the development of new antifungal therapeutics. To rapidly discover such agents, we developed a high-throughput synergy screening (HTSS) strategy for novel microbial natural products. Specifically, a microbial natural product library was screened for hits that synergize the effect of a low dosage of ketoconazole (KTC) that alone shows little detectable fungicidal activity. Through screening of approximate to 20,000 microbial extracts, 12 hits were identified with broadspectrum antifungal activity. Seven of them showed little cytotoxicity against human hepatoma cells. Fractionation of the active extracts revealed beauvericin (BEA) as the most potent component, because it dramatically synergized KTC activity against diverse fungal pathogens by a checkerboard assay. Significantly, in our immunocompromised mouse model, combinations of BEA (0.5 mg/kg) and KTC (0.5 mg/kg) prolonged survival of the host infected with Candida parapsilosis and reduced fungal colony counts in animal organs including kidneys, lungs, and brains. Such an effect was not achieved even with the high dose of 50 mg/kg KTC. These data support synergism between BEA and KTC and thereby a prospective strategy for antifungal therapy.

Extraction of phosphorus in natural waters and sediments by ignition method

Phosphorus recoveries from selected inorganic and organic P-containing compounds after ignition with auxiliaries, such as MgSO4, Mg (NO3)(2), MgCl2, Mg (Ac)(2) and CaCl2 were studied. It was found that the phosphorus could not be completely recovered when most P-containing compounds were ignited with MgSO4 at temperature not higher than 500degreesC if the baked residue was extracted with 0.2 mol/L HCl for 30 min at 80degreesC or at room temperature. In contrast, MgCl2, Mg(Ac)(2) and CaCl2, as well as Mg(NO3)(2), could all yield complete P recoveries. We suggest that MgCl2 rather than MgSO4, which is usually used, should be utilized as ashing auxiliary agent in the P extraction by ignition method. Although Mg (NO3)(2) is a highly effective auxiliary agent, yet interference from MgSO4, danger of explosion, toxicity of nitrogen dioxide and more manipulation steps may limit its widespread utilization. It is suggested that if sediment is ignited with MgCl2, the extraction of residue with 0.2 mol/L HCl for 30 min at 80degreesC could give good result.

Synthesis and QSAR studies of novel triazole compounds containing thioamide as potential antifungal agents

Eighteen novel triazole compounds containing thioamide were designed and synthesized. Their structures were confirmed by elemental analysis, H-1 NMR, IR, and MS. The title compounds exhibited certain antifungal activity. And the geometry structures of the title compounds were optimized by means of the density functional theory (DFT) method at B3LYP/6-31G* level. The quantitative structure-activity relationship (QSAR) of the title compounds was systematically investigated. A correlative equation between FA and DELH, V was well established by using the multiple linear regression (MLR). (c) 2006 Elsevier Ltd. All rights reserved.