基于Analog Discovery 2的巨磁阻效应实验系统

将口袋式仪表Analog Discovery 2及其配套控制软件WaveForms引入巨磁阻效应实验,替代直流电源、信号发生器、示波器、数字信号控制器等传统仪表,完成信号的激发、采集以及处理.由Analog Discovery 2驱动螺线管、巨磁阻传感器、直流电机和步进电机等部件,可以实现巨磁阻传感器R-B基本特征曲线和高速转动转速的快速测量,还可以结合齿轮状铁磁体,实现低速转动的准确测量及微小角位移的定标和测量.各主要部件采用三维调整架固定,偏置永磁铁也配备了不同形状的导磁头,方便学生观察不同条件下的实验现象,完成更具有开放性和创新性的实验内容.

Biological Evaluation of a Novel 2’-Fluoro Derivative 5-Azacytidine as a Potent DNA Methyltransferase Inhibitor

Background: DNA methyltransferases (DNMTs) are key epigenetic regulatory enzymes involved in the expression of many genes and are considered as an attractive target for cancer treatment, especially hematological malignancies. Therefore, promising DNMT inhibitors characterized by low toxicity, target activity and high selectivity are crucial for the development of new cancer therapy and research on the inhibitory mechanism. We had previously demonstrated that the novel 2’-fluoro-2’-deoxy-arabinofuranosyl 5-azacytosine nucleoside (2’F-araAC) showed high antiproliferative activity in vitro and increased hydrolytic stability compared to the known agents like azacitidine and decitabine. Objective: The objective of the present study was to investigate the effect of novel 2’F-araAC as potent anti-leukemia agent and DNMTs inhibitor on nuclear extract of the HCT-116 human colorectal cell line and P388 and L1210 mouse leukemia cell lines. Methods: The DNMTs activity was evaluated using the fluorometric DNMT Activity Quantification Kit (Abcam) and were reported as the percentage of control. Nuclear proteins were extracted from HCT-116 cell line using the Nuclear Extraction Kit (Abcam). To explore the mechanism of anti-leukemic activity of 2’F-araAC, cell cycle and apoptosis analyses were performed on P388 and L1210 cell lines. Results: It has been shown that the DNMTs activity was significantly reduced at 1 and 10 µM of 2’F-araAC compared to controls. Moreover, 2’F-araAC can induce G2/M cell cycle arrest and apoptosis in P388 and L1210 mouse leukemia cell lines as shown by flow cytometry method. Apoptosis was 54.53% and 43.35% for 2’F-araAC vs. 2.88% and 5.25% for the control P388 and L1210 cell lines, respectively. Conclusions: Thus, our study presents a new and promising compound to further develop new epigenetic regulators to be used as antitumor agents.

Analog Discovery 2在模拟电子技术实验案例中的应用

通过实际案例介绍了Analog Discovery 2(简称AD2)在模拟电子技术实验中的应用。简要介绍了AD2的功能和使用方法,并且以模电实验中的积分电路为例,详细介绍了基于Multisim、AD2和Waveforms开展实验的步骤和结果,并对仿真结果和实际结果进行对比。教学实践表明,将该套件应用在模电实验中,弥补了传统虚拟仿真实验的不足,摆脱了空间、时间限制,灵活便携,可操作性强,便于拓展,结果清楚直观,值得推广。

Effects of glucagon-like peptide 1 analogs in combination with insulin on myocardial infarct size in rats with type 2 diabetes mellitus

AIM To evaluate the effects of glucagon-like peptide-1 analogs(GLP-1 a) combined with insulin on myocardial ischemiareperfusion injury in diabetic rats.METHODS Type 2 diabetes mellitus(T2 DM) was induced in maleWistar rats with streptozotocin(65 mg/kg) and verified using an oral glucose tolerance test. After anesthesia, the left coronary artery was occluded for 40 min followed by 80 min reperfusion. Blood glucose level was measured during surgery. Rats were randomized into six groups as follows:(1) control rats;(2) insulin(0.1 U/kg) treated rats prior to ischemia;(3) insulin(0.1 U/kg) treated rats at reperfusion;(4) GLP-1 a(140 mg/kg) treated rats prior to ischemia;(5) GLP-1 a(140 mg/kg) treated rats at reperfusion; and(6) rats treated with GLP-1 a(140 mg/kg) prior to ischemia plus insulin(0.1 U/kg) at reperfusion. Myocardial area at risk and infarct size was measured planimetrically using Evans blue and triphenyltetrazolium chloride staining, respectively.RESULTS There was no significant difference in the myocardial area at risk among groups. Insulin treatment before ischemia resulted in a significant increase in infarct size(34.7% ± 3.4% vs 18.6% ± 3.1% in the control rats, P < 0.05). Post-ischemic administration of insulin or GLP-1 a had no effect on infarct size. However, pre-ischemic administration of GLP-1 a reduced infarct size to 12% ± 2.2%(P < 0.05). The maximal infarct size reduction was observed in the group treated with GLP-1 a prior to ischemia and insulin at reperfusion(8% ± 1.6%, P < 0.05 vs the control and GLP-1 a alone treated groups).CONCLUSION GLP-1 a pre-administration results in myocardial infarct size reduction in rats with T2 DM. These effects are maximal in rats treated with GLP-1 a pre-ischemia plus insulin at reperfusion.

The novel chalcone analog L2H17 protects retinal ganglion cells from oxidative stress-induced apoptosis

Chalcone is a plant metabolite widely found in fruits,vegetables,spices and tea,and has anti-tumor,anti-inflammation,immunomodulation,antibacterial and anti-oxidation activities,as well as many other pharmacological and biological effects.Our team has shown that its analogs have antioxidant activity,and oxidative stress is a pathological hallmark of retinal ischemia/reperfusion injury that can lead to retinal damage and visual loss.This investigation aims to identify a chalcone that protects retinal ganglion cells in vitro from the effects of oxidative stress and examine its mechanism.Rat retinal ganglion cell-5 cells were pretreated with chalcones and then exposed to tert-butyl hydroperoxide that causes oxidative damage.Controls received dimethyl sulfoxide only or tert-butyl hydroperoxide in dimethyl sulfoxide.Only（E）-3,4-dihydroxy-2′-methylether ketone（L2 H17）,of the five chalcone analogs,markedly increased the survival rate of oxidatively injured RGC-5 cells.Thus,subsequent experiments only analyzed the results of the L2 H17 intervention.Cell viability and apoptosis were measured.Intracellular superoxide dismutase and reactive oxygen species levels were used to assess induced oxidative stress.The mechanism of action by L2 H17 was explored by measuring the ER stress/UPR pathway and the expression and localization of Nrf2.All results demonstrated that L2 H17 could reduce the apoptosis of oxidatively injured cells,inhibit caspase-3 activity,increase Bcl-2 expression,decrease Bad expression,increase the activity of superoxide dismutase,inhibit the production of reactive oxygen species,increase Nrf2 immunoreactivity,and reduce the activating transcription factor 4,phospho-eukaryotic initiation factor 2 and CHOP expression.L2 H17 protects retinal ganglion cells induced by oxidative stress by regulating Nrf2,which indicates that it has the potential to become a drug for retinal ischemia/reperfusion.

Characteristic fragmentation behavior of the analogs of endomorphin-2 with phenylglycine in position 3 or 4 by ESI-FT tandem mass spectrometry

A series of analogs of endomorphin-2 （EM-2） with phenylglycine （Phg） in position 3 or 4 were synthesized. In electrospray ionization Fourier transform ion cyclotron resonance （ESI-Fr-ICR） MS/MS spectra of these compounds, some b, y, a, and internal ions were observed and slight mass differences between the calculated and observed results are obtained. Their sequences were derived successfully. However, the MS/MS patterns of these analogs with Dphg and Lphg were very similar. It is hard to distinguish them by MS/MS spectra. Moreover, if the third position was substituted by phenylglycine （L or D）, a rearrangement could occur in MS/MS experiment to lose proline residue.

DESIGN，SYNTHESIS AND ACTIVITIES OF ANALOGS AND SEGMENTS OF THE PAPAVER SOMNIFERUM POLLEN PEPTIDE PSPP2~1

Four analogs and three segments of the Papaver somniferum pollen peptide 2 (PSPP2)were desiged and synthesized by using Merrifield solid phase peptide synthesis method. Their antitumour activities were detrminde by the tetrazolium salt MTT (3-(4,5-dimethylthiazol-2-yl)-2,5diphenyl tetraolium bromide) method and the relationship of tructure -activity was discussed.

基于Analog Discovery 2的电机解码系统设计

介绍了一种适用于高性能电机转子位置解码系统的设计方案。在阐明旋变基本工作原理的基础上,给出了该系统的详细设计思路及参数选择。重点介绍了围绕Analog Discovery 2芯片的外围电路、激励驱动电路以及与TC1782的接口电路。

基于类1-3-2型压电复合材料高频水声相控阵换能器研究

对基于类1-3-2型压电复合材料的高频相控阵换能器进行了理论分析和实验研究。通过切割与填充去耦材料制作类1-3-2型压电复合材料,并对类1-3-2型压电复合材料的基元进行布阵,在二维方向上形成4个子阵。通过对子阵适当相移,抑制主瓣和保留栅瓣,在空间上形成所需的发射与接收波束。实现了通过一个多元平面阵列形成4个所需的指向性波束,测速时避免了声学补偿。与传统使用4个活塞型收发换能器形成指向性波束的方法相比,相控阵换能器的几何尺寸显著减小。研究结果表明,基于类1-3-2型压电复合材料高频水声相控阵换能器具有高发射响应,宽频带,波束一致性好,结构紧凑,制作工艺简单可靠等优点。

2-茚酮基姜黄素类似物对酪氨酸酶的抑制作用

酪氨酸酶抑制剂可作为食品添加剂用作果蔬保鲜和防腐,芳香醛在适宜的条件下与2-茚酮进行缩合反应,合成5种含2-茚酮基的对称姜黄素类似物(A1～A5)。利用紫外分光光度法测定其对酪氨酸酶的抑制作用。结果表明:合成的对称性姜黄素类似物均对酪氨酸酶有较强的抑制作用,其中A2～A4的半数抑制浓度(IC50)分别为25.42、13.51、10.71μmol/L,比广泛使用的食品添加剂曲酸(IC50为28.59μmol/L)的抑制作用强。

仿真模拟改良倒置A^2/O工艺的优化运行策略

以上海嘉定某污水处理厂改良倒置A2/O工艺的调试过程为基础,通过仿真模拟计算,确定了其在不同工况下的最佳运行模式,并优化了最佳模式下的关键运行参数,从而实现达标排放及节能降耗的目的。结果表明,在夏季最佳模式和最优运行参数下,供气量可比优化前减少25%,并且不需要内回流;在冬季最佳模式和最优运行参数下,排泥量减少了17.8%,出水氨氮浓度比优化前低2.3 mg/L。模拟结果对整个污水处理厂的优化运行和节能降耗具有指导意义。

人GLP-1类似物对2型糖尿病患者血清IL-6、TNF-α、CRP及脂联素的影响

目的探讨人胰升血糖素样肽-1(GLP-1)类似物利拉鲁肽对2型糖尿病患者血清白介素-6(IL-6)、肿瘤坏死因子-α(TNF-α)、人高敏C反应蛋白(hs-CRP)及脂联素的影响。方法选择本院住院的2型糖尿病患者40例作为实验组,健康体检者40例作为对照组,实验组改用利拉鲁肽治疗24周。分别于治疗前、治疗第12周、第24周测空腹血糖(FPG)、餐后2 h血糖(2 h PG)、空腹胰岛素(FINS)、糖化血红蛋白(Hb A1c)、hs-CRP、IL-6、TNF-α及脂联素,计算胰岛素抵抗指数(HOMA-IR)。结果利拉鲁肽治疗后,FPG、2 h PG、HOMA-IR、IL-6、TNF-α、hs-CRP显著下降(P<0.01),Hb A1c逐步降低(P<0.05),FINS、脂联素显著升高(P<0.01)。结论人GLP-1类似物可使2型糖尿病患者血清IL-6、TNF-α、hs-CRP浓度降低、脂联素浓度升高,从而抑制炎症反应,在一定程度上延缓2型糖尿病及其并发症的发生、发展。

从核糖核苷合成2′,3′-不饱和核苷的研究进展

综述了从核糖核苷合成2′,3′ 不饱和核苷及其类似物的方法,主要包括2′,3′ 溴代乙酰氧基同时脱除法、2′,3′ O 甲氧基次甲基核苷脱除法、2′,3′ O 硫酸酯脱除法、2′,3′ O 甲烷磺酸酯脱除法等6种方法。引用文献23篇。

重组人胰岛素和人胰岛素类似物治疗2型糖尿病疗效对照

目的比较人胰岛素(诺和灵30R)与人胰岛素类似物(诺和锐30)治疗2型糖尿病的疗效。方法选取82例2型糖尿病患者,随机分成A组(诺和灵30R)41例,皮下注射诺和灵30R;B组(诺和锐30)41例,皮下注射诺和锐30,根据血糖水平调节胰岛素剂量,直至血糖满意达标。相关数据应用医学t检验。结果两组患者经人胰岛素治疗13周后,均能有效控制高血糖,两组间胰岛素平均剂量没有差异(P>0.05),但人胰岛素类似物组能更为理想达标,而且餐后2小时血糖控制更好,两组间比较有统计学差异(P<0.05)。结论使用人胰岛素类似物较人胰岛素能更为有效的控制血糖,尤其是餐后血糖,有助于血糖长期达标。

1,2-二芳基环戊烯类环氧合酶-2抑制剂的3D-QSAR研究

采用三维全息原子场作用矢量(3D-HoVAIF)对26个1,2-二芳基环戊烯类环氧合酶-2抑制剂进行结构参数化表征并与其活性建立定量构效关系(QSAR)模型。运用偏最小二乘回归(PLS)建模,同时采用内部和外部双重验证的方法对所得模型稳定性进行分析和检验。所得模型的复相关系数(R2cum)、留一法(LOO)交互校验(CV)复相关系数(Q2cum)和外部样本校验复相关系数(Q2ext)分别为0.820,0.734和0.749。结果表明,3D-HoVAIF能较好地表征1,2-二芳基环戊烯类环氧合酶-2抑制剂分子结构信息,所建模型具有较好稳定性能和预测能力。

2,4,6-三硝基苯酚在掺杂了铕(Ⅲ)离子的类普鲁士蓝膜修饰的玻碳电极上的电催化还原反应

摘要：制备了用掺杂铕（111）离子的类普鲁士蓝膜修饰的玻碳电极，并研究了2，4，6-三硝基苯酚在此修饰电极上的电化学行为。试验结果表明：与裸玻碳电极相比，2，4，6-三硝基苯酚在此修饰电极上的还原峰电流显著提高，还原电位大大降低，且工作曲线的线性范围明显增宽。在此基础上提出了-种高灵敏度直接测定2，4，6-三硝基苯酚的伏安测定法。在优化的条件下，测得特征还原峰的电流值与2，4，6-三硝基苯酚浓度在4．0×10-5～2．0×10-3mol·L-1及2．0×10-7～8．0×10-6mol·L-1范围内呈线性关系，方法的检出限（3σ）为6．0×10-8mol．L-1。以黄河水样作为基体，用标准加入法做回收试验，测得回收率在97．7％～103．3％之间。

SnCl_4·5H_2O高效催化-锅法合成1-乙酰胺基苯甲基-2-萘酚

采用SnCl_4·5H_2O为催化剂催化2-萘酚、苯甲醛和乙酰胺的三组分一锅法类Ritter反应合成了1-乙酰胺基苯甲基-2-萘酚(AAN)。考察了原料配比、催化剂用量、反应温度和反应时间等因素对AAN收率的影响.确定了适宜反应条件为:n(2-萘酚):n(苯甲醛):n(乙酰胺)=1:1.4:1,催化剂用量为反应物总质量的6%、85℃反应35min,AAN的收率可达96.2%。该合成工艺路线简捷,催化剂价廉易得,催化活性高,使用方便,反应条件温和,收率可观。

胰岛素类似物与重组人胰岛素多点注射治疗2型糖尿病的疗效研究

目的比较胰岛素类似物与重组人胰岛素多点注射治疗2型糖尿病的临床疗效。方法选取2014年8月—2016年2月成都市第三人民医院收治的2型糖尿病患者148例,按照随机双盲法分为观察组与对照组,各74例。观察组患者皮下注射胰岛素类似物(诺和锐30),对照组皮下注射重组人胰岛素(诺和灵30R)。比较两组患者治疗后血糖达标率、血糖达标时间、糖化血红蛋白(Hb A1c)、C-肽及餐后2h C-肽水平、不良反应发生情况及患者满意率。结果两组患者达标率比较,差异无统计学意义(P>0.05)。观察组患者血糖达标时间短于对照组,Hb A1c低于对照组,C-肽、餐后2h C-肽水平高于对照组,差异有统计学意义(P<0.05)。两组患者不良反应发生率比较,差异无统计学意义(P>0.05)。观察组患者总满意率高于对照组,差异有统计学意义(P<0.05)。结论胰岛素类似物与重组人胰岛素治疗2型糖尿病的效果均良好,患者血糖达标率高,不良反应少,而胰岛素类似物治疗2型糖尿病时患者血糖达标时间更短,且患者胰岛B细胞功能改善更好。