In vitro amiodarone protein binding and its interaction with warfarin

Summary The binding of amiodarone to human plasma protein and to bovine serum, albumin was studied by three different methods, ultracentrifugation, equilibrium dialysis and fluorescence spectroscopy. The fraction of amiodarone bound to plasma protein amounted to 96.3%. The changes in the binding properties of 1-anilino-naphthalene-8-sulfonate for bovine serum albumin using warfarin and amiodarone as independent inhibitors were analyzed in terms of binding site specificity. The findings indicated that amiodarone and warfarin have two different binding sites on bovine serum albumin, so a noncompetitive inhibition mechanism was indicated. On the basis of our data we cannot exclude other mechanisms of interaction besides direct displacement of one drug by another; nevertheless, metabolite interference between amiodarone and coagulation cofactors may better explain the enhancement of warfarin's pharmacological action in association with amiodarone.This work was partially funded by the CNR (National Research Council, Rome, Italy), Program on Clinical Pharmacology and Rare Diseases. The authors would like to thanks Drs E. Marzi and E. riva for their help.     

Loss of antibody production accompanied by chromosome loss in a cloned hybrid line secreting antibodies to sheep red blood cells

Summary Somatic cell hybrids between Sp2/O-Ag14 mouse myeloma cells and lymphocytes derived from BALB/c mice hyperimmunized with sheep red blood cells (SRBC) were produced. One hybrid producing IgG₁ antibody to SRBC was selected, cloned twice and subsequently transferred to BALB/c mice. After a number of transfers it was found that the antibody titer in ascitec fluid gradually decreased. Cytogenetic analysis revealed gradual chromosome loss in the hybrid clone, which produced progressively less antibody.     

Selective protection of cells against X-irradiation. Isoproterenol protects only those cells that possesβ-adrenoreceptors

Summary In mixed culture of Chinese hamster fibroblatst, clone 431, and transformed murine L fibroblasts, clone B-82, isoproterenol was found to protect only 431 cells against ionizing radiation. It was shown that 431 cells, in contrast to B-82 cells, possess-adrenoreceptors, and the radioprotective effect of isoproterenol can be realized only if this agent interacts with-adrenoreceptors coupled with the cAMP system. Since malignization often causes the disappearance of-adrenergic and other hormone receptors, the combined culturing and irradiation of the cells studied can be regarded as a model of the growth of malignant cells (B-82) among normal tissue cells (431 cells) under conditions of radiation therapy. A possibility of selective protection against radiation damage of normal tissue cells, with retention of the former radiosensitivity of tumor cells, is discussed.     

Bicuculline and picrotoxin block γ-aminobutryic acid-gated Cl− conductance by different mechanisms

Summary Using isolated, internally perfused bullfrog dorsal root ganglion cells we have studied the dose-response curves for -aminobutyric acid (GABA) in the presence of internally or externally applied GABA antagonists. With external application of antagonists the inhibition of the GABA current by bicuculline was competitive and that by picrotoxin was noncompetitive. Picrotoxin but not bicuculline blocked when internally perfused.To whom reprint requests should be addressed.Acknowledgments. We thank Drs S. Minakami and S. Yasui for helpful discussions and comments.     

Adrenocortical metabolism and plasma corticosterone in soman intoxicated rabbits

Summary The organophosphate neurotoxin soman produced impairments in adrenocortical RNA and protein metabolism. Fasciculate and reticular cell RNA and protein contents were supporessed with sublethal to acutely lethal dosages (20, 30 and 40 g/kg, s.c.) during the acute excitatory phase of intoxication and at 6–8 h post injection. All three dosages produced ca 90% inactivation of plasma cholinesterase. A transient elevation of plasma corticosterone occurred with 20 g/kg soman whereas there was a protracted increase with 30 g/kg. Corticosterone was not significantly elevated with 40 g/kg, but death occurred at 13±4 min. Thus, the magnitude and/or nature of soman-induced metabolic impairments does not appear to prevent adrenal activation.Supported by US Army Medical Research and Development Command Contract DAMD 17-81-C-1202.     

联合实体边界检测的命名实体识别方法

针对传统命名实体识别方法无法有效利用实体边界信息的问题,提出一种联合实体边界检测的命名实体识别方法,即将实体边界检测作为辅助任务,增强模型对实体边界的判断能力,进而提升模型对实体的识别效果。首先,利用Bert预训练语言模型对原始文本进行特征嵌入获取词向量,并引入自注意力机制增强词对上下文信息的利用;其次,在命名实体识别任务的基础上,添加实体边界检测辅助任务,增强模型对实体边界的识别能力;再次,对比联合实体边界检测的命名实体识别方法与基线方法的有效性,并对测试结果进行消融实验;最后,进行样例分析,分析损失权重β对实体边界检测的影响。实验结果表明,在英文社交媒体数据集Twitter-2015上,联合实体边界检测的命名实体识别方法相较于基线模型取得了更高的精准率、召回率和F1值,其中F1值达到了73.57%;并且,边界检测辅助任务提升了基线方法的检测效果。所提方法能有效利用实体边界信息,从而获得更好的实体识别效果,促进了人机交互系统的发展,对自然语言处理下游任务有重要意义。     

数据驱动下交通异常行为的双层识别模型

为实现对车辆异常行为的准确识别,提高车辆行驶的安全性,提出了一种基于支持向量机(support vector machine, SVM)、监督学习与长短期记忆(long short term memory, LSTM)深度学习的交通异常驾驶行为双层识别模型。首先,对车辆轨迹数据筛除和滤波,构建异常行为数据集;其次,从异常行为轨迹特征中提取出特定异常行为的特征标签,并人为标定在训练集中;再次,构建SVM模型对训练集进行粗识别,基于SVM的二分法原理,从测试集中筛选出异常行为;最后,通过LSTM时间序列模型构建具体种类的异常行为模型,并通过深度学习的方法,从异常行为数据中细分为蛇形驾驶、急速变向、侧滑、大半径转弯、快速U型转弯、急刹车等具体的异常驾驶行为。本次实验选用下一代仿真(next generation simulation, NGSIM)数据中US-101高速公路和peachtree城市道路的数据集的轨迹数据验证SVM和LSTM双层识别模型的性能,包括均方根误差、识别准确率等。结果表明,构建的双层识别模型在第一层有98%的识别准确率,第二层有超过80%的识别准确率,可以较为准确地识...     

蛋白质组学技术在动物科学中的研究进展

蛋白质组学在后基因组时代以其独特的角度和重要的作用已成为生命科学领域研究的热点内容。动物科学作为生命科学的一个重要分支,其相关研究对人类的生活有着重要意义。为了系统地了解和展望蛋白质组学技术在动物科学中的研究进展,综述了蛋白质组学的概念及其相关技术,归纳和评析了近年来蛋白质组学在动物繁殖、营养、遗传育种和疾病防治方面的研究现状。     

基于变换域注意力机制的压缩伪影去除的方法

图像有损压缩过程往往会导致图像质量退化,使图像出现压缩伪影。针对现有基于深度学习的方法缺乏对联合图像专家组(Joint Photographic Experts Group,JPEG)压缩算法先验信息的利用,提出一种基于变换域注意力机制的去伪影方法。该方法利用卷积神经网络在像素域和离散余弦变换(discrete cosine transform,DCT)域分别提取特征,再将双域学习的特征信息进行融合。利用量化表设计了DCT注意力机制,该模块根据DCT系数的损失程度给予各频率系数不同的权值,使网络自适应补偿量化引起的误差。于此基础上,在像素域引入通道注意力机制,从而更好地利用量化表的先验信息。在主要数据集上,提出的去伪影方法以固定的模型参数对多种质量因子的压缩图像进行伪影去除实验。实验结果表明,所提出的方法在各评价指标和主观视觉上取得较好的效果。     

等衰落轨道角动量索引调制系统的信道容量性能分析

射频轨道角动量(orbital angular momentum,OAM)提供了一种可以在同一载波频率物理信道上复用一组正交模式以提高信道容量的方法。现有研究大多专注于信道容量提升,对系统复杂度的研究相对较少。在基于均匀圆形阵列(uniform circular array,UCA)的OAM通信系统中,发射机需要完成大量调制运算以生成OAM信号。于是,提出了一种等衰落轨道角动量索引调制(equal fading orbital angular momentum index modulation,EOAM-IM)方案,其中,IM有效降低了OAM调制运算复杂度,且等衰落发射机也保证了不同模式OAM子信道传输增益。此外,还详细推导了所提EOAM-IM方案的系统信道容量。仿真结果表明,所提EOAM-IM方案能以更低的调制复杂度获得比传统OAM方案更高的信道容量。