Effect of astrocyte on synchronization of thermosensitive neuron-astrocyte minimum system

Astrocytes have a regulatory function on the central nervous system (CNS), especially in the temperature-sensitive hippocampal region. In order to explore the thermosensitive dynamic mechanism of astrocytes in the CNS, we establish a neuron-astrocyte minimum system to analyze the synchronization change characteristics based on the Hodgkin-Huxley model, in which a pyramidal cell and an interneuron are connected by an astrocyte. The temperature range is set as 0 ℃-40 ℃ to juggle between theoretical calculation and the reality of a brain environment. It is shown that the synchronization of thermosensitive neurons exhibits nonlinear behavior with changes in astrocyte parameters. At a temperature range of 0 ℃-18 ℃, the effects of the astrocyte can provide a tremendous influence on neurons in synchronization. We find the existence of a value for inositol triphosphate (IP₃) production rate and feedback intensities of astrocytes to neurons, which can ensure the weak synchronization of two neurons. In addition, it is revealed that the regulation of astrocytes to pyramidal cells is more sensitive than that to interneurons. Finally, it is shown that the synchronization and phase transition of neurons depend on the change in Ca²⁺ concentration at the temperature of weak synchronization. The results in this paper provide some enlightenment on the mechanism of cognitive dysfunction and neurological disorders with astrocytes.     

Delannoy数与Schröder数的一些和式公式

研究了Delannoy数与Schr?der数.利用分析方法和组合技巧,建立了任意多个Delannoy数乘积的一些和式公式,并对Schroder数的和式公式进行了类似的研究.     

基于DNA酶催化的卟啉金属化检测锌

利用G-四链体DNA（T30695）催化Zn²⁺插入到中卟啉IX（MPIX）中，引起荧光偏移的特点，建立了检测Zn²⁺的方法。在40μmol/L MPIX、0.6μmol/L Pb²⁺、5μmol/L T30695和1%Triton的最优实验条件下，该方法在Zn²⁺浓度为0.5～5μmol/L范围内呈现良好的线性关系，相关系数R²=0.95，检出限为73.5 nmol/L。离子选择性实验表明该方法对Zn²⁺具有较好的选择性，用于实际样品测定，回收率在94.7%～100.4%之间。     

粒子法中自由表面粒子识别

针对移动粒子半隐式法MPS(Moving Particle Semi-implicit Method)基于粒子数密度来判断自由表面会出现将内部粒子误判为自由表面粒子的问题,提出了一种结合几何法和体积法的自由表面粒子判定方法。通过对溃坝问题进行数值模拟,结果表明,全新的自由表面粒子判定方法对流体平稳运动以及剧烈运动两种工况,都能准确地判断出自由表面粒子,解决了基于粒子数密度判断方法因粒子分布稀疏产生误判的问题。这种全新的自由表面粒子判定方法对今后采用MPS方法计算两相流问题时,两种介质在界面处的传热传质计算有重要意义。     

GPR40 受体苯丙酸类激动剂三维定量构效关系研究

苯丙酸类化合物是G蛋白偶联受体40(GPR40)潜在的生物活性药物。本文基于比较分子力场分析法(Co MFA)和比较分子相似性指数分析法(CoMSIA),分别建立了40个已知活性的GPR40受体苯丙酸类激动剂的三维定量构效关系(3D-QSAR)模型,研究该类激动剂与生物活性之间的关系。CoMFA和CoMSIA模型的交叉验证系数(q~2)分别为0. 527和0. 500,拟合验证系数(r~2)分别为0. 901和0. 860,两个3D-QSAR模型预测值与实验值基本一致,表明模型具有良好的可信度和预测能力。根据两个3D-QSAR模型提供的立体场、静电场、疏水场、氢键供体场和氢键受体场所提供的信息提出优化该类抑制剂结构的药物设计思路,为指导设计更高活性的GPR40激动剂以及GRR40新分子激动活性的预测提供理论依据。     

3-芳基-5-噻吩基二氢吡唑磺酰胺衍生物的合成及其抗炎活性研究

二氢吡唑是一类含有多种生物活性的五元氮杂环化合物,广泛存在于各种活性天然产物结构中。本文由4-氟苯乙酮和N-甲基哌嗪经取代反应后,再与2-噻吩甲醛发生羟醛缩合生成哌嗪取代噻吩查尔酮(2)。化合物2与水合肼环化得到中间体化合物3,最后经磺酰氯衍生化,合成得到8个未见报道的3-芳基-5-噻吩基二氢吡唑磺胺衍生物(4a～4h),其结构均经IR、~1H NMR和~(13)C NMR确证。采用小鼠巨噬细胞Raw264. 7模型初步测试了衍生物的抗炎活性,结果表明,化合物4a、4e和4h具有潜在的体外抗炎活性,特别是化合物4a抑制NO生成的IC_(50)值为12. 64μmol/L,与阳性对照药地塞米松活性相当。     

固相萃取/液相色谱-串联质谱法测定油脂中的3-氯-1,2-丙二醇棕榈酸二酯

建立了固相萃取/液相色谱-串联质谱检测油脂中3-氯-1,2-丙二醇棕榈酸二酯(3-MCPD-DP)的分析方法。油脂经溶解后,以自填装PSA+C_(18)吸附剂的固相萃取柱净化,ThermoFisher Accucore C_(18)色谱柱分离,以10 mmol/L甲酸铵甲醇溶液和10 mmol/L甲酸铵异丙醇溶液为流动相梯度洗脱,电喷雾正离子模式扫描,多反应监测模式定性分析,内标法定量。对离子化条件、固相萃取吸附剂用量、洗脱条件、定容溶液等条件进行了考察。在优化条件下,3-MCPD-DP在0.5～1 000 ng/mL范围内线性关系良好(r~20.999),方法检出限(S/N≥3)与定量下限(S/N≥10)分别为0.025 mg/kg和0.050 mg/kg。在橄榄油样品中加标量为0.1～0.5 mg/kg时,3-MCPD-DP的平均回收率为90.8%～102%,相对标准偏差(RSD,n=6)为1.1%～3.0%。该方法前处理简单快速、灵敏度较高,可满足油脂中3-MCPD-DP的检测要求。     

Identification of Residue Involved in Nucleotidyltransferase Activity of LinA from Staphylococci by Site-directed Mutagenesis

The lincosamide class of antibacterials is widely used for the treatment of a broad spectrum of infections, and one prevalent route of resistance to lincosamides in pathogenic gram-positive cocco is antibiotic modification. Enzymes encoded by lin genes, belonging to nucleotidyltransferase superfamily, catalyze adenylylation to inactivate lincosamides. LinA can adenylylate lincosamides at either 3?-or 4?-OH of the methylthiolincosamide sugar. The crystal structure of LinA/lincomycin has confirmed its active site. However, the residue interacting with nucleotidyl donors remains elusive. Here, we modeled the complex structure of LinA/lincomycin/Mg~(2+)/AMPCPP to reveal a putative pocket for nucleotidyl donors and suggested the residue R45 in this pocket involved in the recognition of donor substrates NTP and catalysis. ITC and enzyme activity assays show that the mutation of residue R45 impairs LinA nucleotidyltransferase activity in vitro. This work provides insights into the molecular mechanism of the nucleotide binding and transferring activity of antibiotic NTases.     

3位间接连接有叔胺(仲胺)氮原子的3-季碳氧化吲哚化合物的合成

以3-卤氧化吲哚为起始原料，1,8-二氮杂二环十一碳-7-烯为催化剂，在二氯甲烷中与1-甲基吲哚经取代反应，或在甲苯溶液中于120 ℃条件下与吲哚（吲哚苯环上可连接有取代基）直接发生取代反应，合成了7个3位间接连接有叔胺（仲胺）氮原子的3-季碳氧化吲哚化合物，收率分别为80%~89%和 53%~70%，其结构经¹H NMR, ¹³C NMR和HR-MS（ESI-TOF）表征。