α-戊(己)基肉桂醛的合成

采用聚乙二醇 ( PEG 2 0 0 )作相转移催化剂 ,用氢氧化钾醇水溶液代替氢氧化钾醇溶液合成了 α 戊 (己 )基肉桂醛 ,收率提高到 85%以上。用此工艺合成的产品纯度高 ,香气好 ,具有较高的工业实用价值。     

油溶性减阻功能聚合物的研制

介绍了以混合α-烯烃为原料,制备了具有减阻功能的共聚物。讨论了催化剂浓度、聚合温度、预聚合时间、原料单体中杂质含量对共聚物特性粘度和转化率的影响。试验表明,在较低的催化剂浓度和预聚合温度下,能得到较高分子量的聚合物。气相色谱法和DSC法测定其组成和单体混合物的组成基本一致,表明共聚物是一种无规的梳状结构聚合物。该聚合物达到较高特性粘度时,能获得较好的减阻率。     

Deposition and characterization of alumina films produced by combustion flame pyrolysis

Alumina coatings have been deposited by combustion flame pyrolysis on amorphous silica and stainless steel substrates with the objective to study the effect of solvent composition, Fe³⁺ addition and determine the thermal fatigue lifetime. The effect of solvent composition on crystallinity, transformation temperature and hardness are studied, three different solvent compositions are chosen for preparing the aluminium nitrate solution. Using 100% water, as-deposited films are amorphous and transform to α-alumina only upon annealing, while this equilibrium phase is directly obtained but with a porous microstructure by using 100% methanol. The hardness of the coatings varies with the flammability of the solvents. The effect of Fe³⁺ addition on the crystallization of alumina is studied by combustion pyrolysis of aqueous solutions of Al³⁺ and Fe³⁺ nitrates. Small amount of ferric nitrate reduced the transformation temperature by 100 °C. Thermal cycling of as-deposited amorphous alumina on stainless steel substrate is carried out at different temperatures to determine the thermal fatigue lifetime.     

带有局部控制因子的图割光流估计

提出一种带有局部空间项控制因子的图割光流估计算法,能判断和处理光流场的平移遮挡现象。文中分析了平移遮挡的形成机理,构造了遮挡判别公式,基于本次的正向和反向光流场,依靠遮挡判别结果调节局部空间项控制因子,建立下次的能量泛函,加强背景区域对遮挡区域的平滑作用,隔绝运动区域对遮挡区域的平滑作用,从而构造出新结构的网络流图。另外,该算法被证明可以阻断遮挡误判在各次图割优化过程间的传递,从而使逐次α-扩散移动图割光流算法具有自适应处理遮挡的能力。通过与Ground-truth光流场的实验对比,表明该算法能较好地判断与处理遮挡导致的光流场无效区域。     

The Antithrombotic Agent Pterostilbene Interferes with Integrin αIIbβ3-Mediated Inside-Out and Outside-In Signals in Human Platelets

Platelets play a crucial role in the physiology of primary hemostasis and pathological processes such as arterial thrombosis; thus, developing a therapeutic target that prevents platelet activation can reduce arterial thrombosis. Pterostilbene (PTE) has remarkable pharmacological activities, including anticancer and neuroprotection. Few studies have reported the effects of pterostilbene on platelet activation. Thus, we examined the inhibitory mechanisms of pterostilbene in human platelets and its role in vascular thrombosis prevention in mice. At low concentrations (2–8 μM), pterostilbene strongly inhibited collagen-induced platelet aggregation. Furthermore, pterostilbene markedly diminished Lyn, Fyn, and Syk phosphorylation and hydroxyl radical formation stimulated by collagen. Moreover, PTE directly hindered integrin α_IIbβ₃ activation through interfering with PAC-1 binding stimulated by collagen. In addition, pterostilbene affected integrin α_IIbβ₃-mediated outside-in signaling, such as integrin β₃, Src, and FAK phosphorylation, and reduced the number of adherent platelets and the single platelet spreading area on immobilized fibrinogen as well as thrombin-stimulated fibrin clot retraction. Furthermore, pterostilbene substantially prolonged the occlusion time of thrombotic platelet plug formation in mice. This study demonstrated that pterostilbene exhibits a strong activity against platelet activation through the inhibition of integrin α_IIbβ₃-mediated inside-out and outside-in signaling, suggesting that pterostilbene can serve as a therapeutic agent for thromboembolic disorders.     

Exogenous Integrin αIIbβ3 Inhibitors Revisited: Past,Present and Future Applications

The integrin αIIbβ3 is the most abundant integrin on platelets. Upon platelet activation, the integrin changes its conformation (inside-out signalling) and outside-in signalling takes place leading to platelet spreading, platelet aggregation and thrombus formation. Bloodsucking parasites such as mosquitoes, leeches and ticks express anticoagulant and antiplatelet proteins, which represent major sources of lead compounds for the development of useful therapeutic agents for the treatment of haemostatic disorders or cardiovascular diseases. In addition to hematophagous parasites, snakes also possess anticoagulant and antiplatelet proteins in their salivary glands. Two snake venom proteins have been developed into two antiplatelet drugs that are currently used in the clinic. The group of proteins discussed in this review are disintegrins, low molecular weight integrin-binding cysteine-rich proteins, found in snakes, ticks, leeches, worms and horseflies. Finally, we highlight various oral antagonists, which have been tested in clinical trials but were discontinued due to an increase in mortality. No new αIIbβ3 inhibitors are developed since the approval of current platelet antagonists, and structure-function analysis of exogenous disintegrins could help find platelet antagonists with fewer adverse side effects.     

Effect of ammonia concentrations on SCC of α-brass under mode III loading

Stress corrosion cracking (SCC) of α-brass in ammonia solution was studied under mode III loading. The results showed that SCC occurred on the principal stress planes where shear stresses are zero. No SCC occurred on the maximum shear stress plane. Ammonia concentration affected fracture behaviour. When the concentration was low, many cracks with spacing of 10–150 μm were found on 45 ° planes, i.e., the principal stress planes. When the concentration was high, the cracks on 45 ° planes were not clearly visible because of serious general corrosion.     

重组人干扰素α2b阴道泡腾片抗豚鼠单纯疱疹病毒性阴道炎的疗效

目的观察重组人干扰素α2b阴道泡腾片对单纯疱疹病毒性阴道炎动物模型的疗效。方法采用单纯疱疹病毒感染建立豚鼠实验性阴道炎模型,并分别用重组人干扰素α2b阴道泡腾片600、3 000和15 000 IU/只进行治疗。以阿昔洛韦(无环鸟苷)和干扰素α2b栓剂15 000 IU/只作为对照。对治疗前后豚鼠阴道外观及组织切片进行评分。结果应用重组人干扰素α2b阴道泡腾片对豚鼠实验性单纯疱疹病毒性阴道炎进行治疗后,豚鼠阴道外观病变与组织切片病变评分均显著降低,其中15 000 IU/只效果最好。同样剂量的α2b泡腾片药效优于栓剂。结论重组人干扰素α2b阴道泡腾片对实验性单纯疱疹病毒性阴道炎有明显的疗效。     

重组人干扰素α2b内毒素检查法的研究

目的研究鲎试剂法与家兔法检测重组人干扰素α2b内毒素结果的相关性,并参照家兔热原试验的阈值量,来确定本制品质量标准中内毒素的限量标准。方法分别用不同浓度的内毒素溶液和含不同浓度内毒素的供试品溶液进行家兔热原质试验,确定供试品内毒素限值,并在此限值下进行内毒素检测,方法均参照2000年版《中国药典》和2000年版《中国生物制品规程》进行。结果在含不同浓度内毒素溶液的家兔热原质试验中,致热阈值小于5.0EUml。在含不同浓度内毒素供试品溶液的家兔热原质试验中,致热阈值小于1.25EUml。以此确定本品内毒素限值,检测该制品的内毒素含量,结果均符合规定。结论本品在内毒素含量小于3.5EU500万单位dose的范围内,根据具体的对照实验及制品的用途来规定细菌内毒素限值,可用鲎试剂法代替家兔法检测注射用重组人干扰素α2b冻干制剂的热原质。     

重组人干扰素α2b栓剂的检定及其临床疗效

目的对重组人干扰素α2b栓剂进行质量检定及临床疗效观察。方法连续试制3批样品,进行各项质控指标的检定及宫颈糜烂的临床疗效观察。结果本品各项检定指标均符合质量要求。治疗组宫颈糜烂的有效率为74·8%,对照组的有效率为60·0%。治疗组和对照组的副反应发生率分别为9·1%和8·3%。结论重组人干扰素α2b栓剂质量稳定,安全性好,疗效确切。