肉桂酰酪胺类似物的合成与抗血小板聚集评价

为了探究肉桂酰酪胺的苯环上甲氧基取代、酪胺上羟基和酰胺上胺基被甲基化对衍生物抗血小板聚集活性的影响,以8种苯甲醛衍生物为原料,经过缩合反应及甲基化等反应制得肉桂酰酪胺类似物,经核磁共振波谱仪(NMR)、质谱(MS)、单晶衍射等技术手段表征了目标化合物结构。 基于变温核磁,探讨了化合物4a~4h中旋转异构及酰胺C-N键双键性质对氢核磁谱的影响。 采用Born比浊法对目标化合物进行活性筛选,9个类似物的活性均强于柄果花椒酰胺,特别是化合物2c、4c、4f在200 μmol/L时显示出强的抑制率,分别为50.03%、60.87%、53.33%。 该类化合物的构效关系是4位甲氧基取代对化合物的抗ADP(二磷酸腺苷)诱导血小板聚集活性最为有利,甲基化B环中的羟基和结构中的酰胺氮原子时,在某种程度上可增强化合物活性。     

Effect of magnetic fields on viscous liquid column with finite length in a vertical straight tube

ＥＦＦＥＣＴＯＦＭＡＧＮＥＴＩＣＦＩＥＬＤＳＯＮＶＩＳＣＯＵＳＬＩＱＵＩＤＣＯＬＵＭＮＷＩＴＨＦＩＮＩＴＥＬＥＮＧＴＨＩＮＡＶＥＲＴＩＣＡＬＳＴＲＡＩＧＨＴＴＵＢＥＷｅｎＧｏｎｇ－ｂｉ（温功碧）;ＳｕｎＫｅ－ｌｉ（孙克利）（ＤｅｐａｒｔｍｅｎｔｏｆＭ...     

Preparation and properties of a biodegradable inferior vena cava filter

In this study, a new type of biodegradable inferior vena cava filter was designed and prepared based on polylactic acid. In addition to having the main functions of a common filter, it is also completely biodegradable in the human body without secondary surgical removal. The changes of surface morphology, molecular weight, viscosity, and radial support strength with degradation time were systematically investigated via degradation experiments in vitro. The results of crimping and expansion tests of the filter showed that reducing the crimping time and increasing the release time make it easier for the filter to recover to its original diameter. Further, the results of a thrombus capture experiment in vitro showed that the thrombus filtration ratio for the filter with double‐layer connection structure is 90%.     

新型噻吩并四氢吡啶类化合物的合成及其抗血小板聚集活性

噻吩并［3,2-c］四氢吡啶和噻吩并［2,3-c］四氢吡啶分别与取代苄溴(2a~2g)经取代反应后,用2 mol·L^-1氯化氢乙醚溶液成盐合成了噻吩并四氢吡啶衍生物(3b~3e, 3g和5a~5g);噻吩并［3,2-c］四氢吡啶酮与取代苄溴经取代反应,再与乙酸酐缩合,最后经2 mol·L^-1氯化氢乙醚溶液成盐合成了噻吩并四氢吡啶衍生物(7d, 7e, 7g~7i)。 3, 5和7均为新化合物,其结构经¹H NMR 和ESI-MS表征。大鼠体内抗血小板聚集活性研究结果表明：3, 5和7均有一定的抗血小板聚集活性,其中7d, 7h和7i的抑制率分别为66.2%, 86.8%和88.3%,活性优于阳性对照药噻氯匹啶。     

HEMODYNAMIC CHANGES OF THE LEFT CORONARY ARTERY DURING PERCUTANEOUS CORONARY WEI Chijun*, QIU Yue*, FAN Yubo†, PENG Liqing**, ZHENG Tinghui*,2)*

经皮冠状动脉介入治疗(percutaneous coronary intervention, PCI)是检查和治疗冠心病的常用手段,冠状动脉支架植入过程中可能引发急性血栓的发生。本文通过血流动力学计算探究PCI支架植入手术过程对急性血栓形成的影响。根据真实的冠状动脉计算机断层扫描影像进行建模,在脉动生理血流条件下模拟该手术过程中导丝介入的5个阶段,获得各项血流动力学参数。计算结果表明,导丝介入过程会导致冠状动脉内各项血流动力学参数发生改变,即冠状动脉内血流出现偏心现象,时均壁面剪切力升高,振荡剪切指数下降,粒子相对停留时间降低,横向壁面剪切应力小幅上升,使得血管的内皮细胞暴露在高壁面剪切力的环境下。虽然较短的相对粒子 停留时间、 较小的振荡剪切指数对急性血栓的形成具有阻碍作用,但高时均壁面剪切力与血流偏心对急性血栓形成的诱导作用可能更加明显。     

在磁场作用下竖直管中有限长液柱的粘性流体运动

血栓的形成与血液动力学有密切关系．Ｃｈａｎｄｌｅｒ环的实验及进一步的研究表明，Ｃｈａｎｄｌｅｒ环中下弯月面处血栓的形成或许是因为流冲击下弯月面，使血小板和红细胞发生聚集所致。本文研究了竖直管中有限长液柱的粘性流体在磁场作用下的流动状况，应用有限差分方法进行了数值求解。计算结果表明，在适当的磁场强度下，管的下半部分管轴附近的轴向流速度较未加磁时有所减弱，从而减轻了流对下弯月面的撞击作用，可以有效地防止下弯月面处血栓的形成，而且磁场越强，这种减弱作用越明显，这一结果为进一步探求血栓的防治及其形成机制的实验研究有一定指导意义。     

Visualization of microvasculature and thrombi by X‐ray phase‐contrast computed tomography in hepatocellular carcinoma

Visualization of the microvascular network and thrombi in the microvasculature is a key step to evaluating the development of tumor growth and metastasis, and influences treatment selection. X‐ray phase‐contrast computed tomography (PCCT) is a new imaging technique that can detect minute changes of density and reveal soft tissues discrimination at micrometer‐scale resolution. In this study, six human resected hepatocellular carcinoma (HCC) tissues were investigated with PCCT. A histological stain was added to estimate the accuracy of PCCT. The results showed that the fine structures of the microvasculature (measuring 30–100 µm) and thrombi in tiny blood vessels were displayed clearly on imaging the HCC tissues by PCCT. Moreover, density distributions of the thrombi were obtained, which could be reliably used to distinguish malignant from benign thrombi in HCC. In conclusion, PCCT can clearly show the three‐dimensional subtle structures of HCC that cannot be detected by conventional absorption‐based computed tomography and provides a new method for the imageology of HCC.     

脂肪颗粒在颈动脉中的运动及其对血液动力学的影响

很多研究表明, 动脉粥样硬化通常发生在具有复杂血液动力学的区域, 比如分叉动脉和弯曲动脉. 这些地方常伴随有低壁面剪切力或震荡壁面剪切力, 这是动脉粥样硬化形成的一大诱因. 使用计算流体力学软件对2D颈动脉分叉血管进行了模拟, 研究了脂肪颗粒在颈动脉中的运动及其对血液动力学的影响. 研究表明: 1)血管狭窄对于脂肪颗粒的运动有重要影响, 同时也影响栓塞的形成; 2)脂肪颗粒可能会黏附在血管壁面, 但由于血流的冲击作用, 脂肪颗粒会随后在壁面略微铺展; 3)颈动脉狭窄区域后方是下一个血栓的可能生长位点; 4)当栓塞形成时, 速度和壁面剪切力分布将变得复杂多变, 这对于血管是有害的.