银杏叶提取物对动脉粥样硬化大鼠斑块及血脂水平影响

目的:研究银杏叶提取物是否具有延缓大鼠斑块进程、调节动脉粥样大鼠血脂水平的作用。方法:建立动脉粥样硬化大鼠模型36只,分为3组:银杏叶提取物组、辛伐他汀组、高脂未干预组,每组12只。干预4周后分别处死大鼠,取血样进行血脂水平分析;对大鼠主动脉病理切片进行形态学比较。采用Stata6.0统计软件分析:①血清学指标、相对光密度值采用x軃±s表示;②两组间比较采用t检验;以P<0.05为差异有显著性,均为双侧检验。结果:银杏叶提取物组和辛伐他汀组脂蛋白水平:TC、TG、LDL-C、ox-LDL均明显低于高脂未干预组(P<0.01),但前两者之间也有统计学差异:银杏叶提取物组血脂水平要高于辛伐他汀组(P<0.05);经银杏叶提取物和辛伐他汀干预组斑块进展明显慢于高脂未干预组。结论:银杏叶提取物具有调节动脉粥样硬化大鼠血脂水平,保护血管内皮、延缓动脉粥样硬化斑块进展的作用,但是其作用要弱于辛伐他汀。     

孙锦标与《通俗常言疏证》

孙锦标<通俗常言疏证>受明清以来俗语研究学风的影响,把一般性俗语溯源研究与南通方言俗语辑录结合起来,对5595条俗语词进行了立体性的疏证考释.其篇幅和疏证特点堪与<通俗编>媲美.其文献学意义和俗语词研究史料价值、南通方言研究史料价值不可低估.     

Mn(ii)-Catalysed ortho-alkenylation of aromatic amines and its application in reproductive diseases

A Mn(ii)-catalysed ortho-alkenylation of aromatic amines and its application in reproductive diseases were developed. The use of MnCl₂ was critical for the ortho-alkenylation of aromatic amines. The general applicability of this procedure was highlighted by the synthesis of 27 vinylanilines, with good regioselectivities. The value of our approach in practical applications was investigated by studying the effects of one of the compounds 3m on 8 week-old adult male rats with azoospermia as a mammalian model. The results show that a small amount of sperm will gradually be produced in the epididymis and testes by treatment of 8 week-old adult male rats with azoospermia with 1 mg kg⁻¹3m after two weeks, while treatment with 10 mg kg⁻¹3m led to obvious sperm production. Notably, if we increase the dose to 100 mg kg⁻¹, there will be a lot of sperm production in the epididymis and testes after two weeks of treatment. The results of this study will be of great significance in research on drugs for treating azoospermia and oligospermia diseases.

A Mn(ii)-catalysed ortho-alkenylation of aromatic amines and its application in reproductive diseases were developed.

Alkenyl arylamines are very important intermediates for the synthesis of drug molecules, such as carbamazepine,¹ opipramol,² and indopan³ (Scheme 1). O-Alkenyl arylamines have attracted much attention because of their widespread presence in a variety of heterocycles including indoles, quinolines and cinnolines, which are key structural units for many biologically important compounds.⁴ Moreover, they have also been used as synthetic intermediates in several total synthetic methods.⁵ Therefore, it is of great significance to carry out the ortho-alkenylation reaction of aromatic amines. But it is not an easily accessible process under normal Friedel–Crafts conditions due to the coordination of the Lewis acid with the nitrogen atom of amino group, which leads to the deactivation of the aromatic ring.⁶ To overcome this challenge, chemists began to try other methods to achieve ortho-alkenylation of aromatic amines. Subsequently, several related ortho-alkenylation of aromatic amines with phenylacetylene was reported in the literature.^4a,7 However, the ortho-alkenylation of aromatic amines catalyzed by base metals has not yet been developed, especially manganese. Therefore, it is still very important to develop a Mn-catalyzed ortho-alkenylation reaction of aromatic amines. Notably, there have been more C–H bond functionalization reactions catalyzed by monovalent manganese in recent years, but few of them were catalyzed by divalent manganese.⁸ Ackermann''s research group reported several Mn(ii)-catalyzed ortho-functionalization reactions of arylamides.⁹ In addition, a Mn(ii)-catalysed dehydrogenative annulation of N-aryl anilines with alkenes or alkynes was reported by our group last year.¹⁰Open in a separate windowScheme 1Drug molecules containing alkenyl arylamine skeleton.Herein, we report an example of Mn(ii)-catalysed ortho-alkenylation of aromatic amines and its application in reproductive diseases (Scheme 2). In our previous work, divalent manganese is easily oxidized to tetravalent manganese by K₂S₂O₈.¹⁰ This work, we hypothesis the ortho-alkenylation product of aromatic amine will be generated after the oxidant was removed in the system. Based on this hypothesis, we tried a series of manganese catalysts.Open in a separate windowScheme 2Proposed strategy.We began by treating N-benzylaniline and phenylacetylene with toluene as a solvent. Initially, we attempted using various Mn(ii) catalysts to catalyse the ortho-alkenylation of aromatic amines at 120 °C, i.e., MnO, MnSO₄, Mn(OAc)₂, and Mn(acac)₂, as detected by GC analysis, while 73% and 61% yields were observed when MnBr₂ and MnI₂ were used as catalysts (Table 1, entries 1–7). Fortunately, a 80% yield of N-benzyl-2-(1-phenylvinyl)aniline was obtained when using MnCl₂. To improve the reaction efficiency, different solvents, including N,N-dimethylformamide (DMF), dimethyl sulfoxide (DMSO), acetonitrile (CH₃CN), 1,4-dioxane, tetrahydrofuran (THF), 1,2-dichloroethane (DCE), p-xylene, mesitylene and n-hexane were tested (Table 1, entries 8–16). The optimal reaction solvent was found to be toluene. To increase conversion to the N-benzyl-2-(1-phenylvinyl) aniline, we examined a wide range of reaction temperatures (Table 1, entries 17–22). The results show that 120 °C was the optimum temperature, and the corresponding N-benzyl-2-(1-phenylvinyl)aniline was obtained the best yield. It is worth noting that more cyclization products were formed when the temperature is raised to 130 °C. Therefore, temperature is another key factor that drives the reaction forward. Notably, the addition of oxidant will terminate this reaction (see the ESI Table 1^† for details). These results therefore support our initial hypothesis that the ortho-alkenylation product of aromatic amine will be generated after the oxidant was removed.Effects of catalyst, temperature, and solvent. N-Benzylaniline (0.2 mmol), phenylacetylene (0.4 mmol), catalyst (0.04 mmol), solvent (2.0 mL), at 120 °C for 24 h

统分结合测量居民幸福指数

针对已有幸福指数测量方法中的两个主要缺点,借鉴幸福指数单测法的合理成分,由幸福分数构成幸福指数的综合指标。依据马斯洛需要层次理论,由生存需要满足层次的幸福指数、安全需要满足层次的幸福指数、社交需要满足层次的幸福指数、尊重需要满足层次的幸福指数和自我实现需要满足层次的幸福指数这样五个一级指标以及23个二级指标构成幸福指数的分指标。居民幸福指数统分结合测量具有独特的优势和功能。     

南通沿江沿海开发的统筹发展

随着江苏沿海开发上升为国家战略,位于江海交汇处的南通正处于长三角一体化和江苏沿海开发两大国家战略的叠加区,将承担支撑长三角、拓展大上海、带动长江北、辐射中西部的独特作用。沿江地区与沿海地区存在着较大差距,南通沿江开发已实施多年,而沿海开发刚刚起步,应从产业布局、基础设施建设、港口联动、生态环保、社会事业等方面,整合沿江、沿海两种资源,统筹发展、江海联动,实现区域均衡发展,加快推进南通市经济、社会的跨越式发展。     

基于CT医学图像的边缘提取研究

为了实现人体器官的三维重建,如何准确、有效地提取二维医学图像的边缘成了首要解决的问题.我们提出一种新的图像边缘提取方法,该方法先将原始CT图像二值化,然后利用数学形态运算对二值化图像进行预处理,最后利用Canny算子提取图像边缘.通过肾脏CT图像边缘提取结果表明,该方法简单、高效、性能优越.     

诗词格律与古诗词校勘——以校勘张謇诗词为例

诗词与散文不同之明显处在于其独有的格律,诗词在流布过程中所产生的隐蔽性讹误,常常由于诗词格律的存在而留下印记.因此,诗词校勘除了掌握散文校勘的各种知识与手段外,还须掌握诗词的格律,运用诗词格律发现与改正隐蔽的讹误,以提高诗词校勘质量.     

民生思想与社会主义思潮及其在中国的发展

空想社会主义以对民生关注作为未来理想社会设计的起点.19世纪三大空想社会主义的民生思想主要在于发展社会生产,建立平等社会;承认分配差别,保障社会福利;主张权利平等,促进人的自由发展.马克思主义民生观.是社会主义由空想到科学的转变的重要基石:人的全面发展是民生的最高境界;无产阶级国家政权是民生的根本保障:民生是创立历史唯物主义的基础;解决民生问题是未来社会的重要价值目标.中国特色社会主义的民生思想,则经历了"经济建设为中心"、"始终代表中国最广大人民的根本利益"、"以人为本"为特征的历史演进.     

创新型城市建设的企业路径——具有竞争优势的深圳企业自主创新模式分析

建立企业自主创新能力持续提升机制、形成具有竞争优势的企业自主创新路径是创新型国家和创新型城市建设的基本条件.而作为创新型城市建设的主要创新微观主体,企业自主创新路径及其绩效高低直接决定着创新型城市的建设水平.企业自主创新能力的竞争优势形成模式是深圳创新型城市的重要来源,是深圳创新型城市自主创新能力持续提升的核心和基础.深圳创新型城市建设的主要经验就是因为初步成功建立起了具有竞争优势的企业自主创新路径与制度安排.     

CCL2/CCR2 Contributes to the Altered Excitatory-inhibitory Synaptic Balance in the Nucleus Accumbens Shell Following Peripheral Nerve Injury-induced Neuropathic Pain

The medium spiny neurons (MSNs) in the nucleus accumbens (NAc) integrate excitatory and inhibitory synaptic inputs and gate motivational and emotional behavior output. Here we report that the relative intensity of excitatory and inhibitory synaptic inputs to MSNs of the NAc shell was decreased in mice with neuropathic pain induced by spinal nerve ligation (SNL). SNL increased the frequency, but not the amplitude of spontaneous inhibitory postsynaptic currents (sIPSCs), and decreased both the frequency and amplitude of spontaneous excitatory postsynaptic currents (sEPSCs) in the MSNs. SNL also decreased the paired-pulse ratio (PPR) of evoked IPSCs but increased the PPR of evoked EPSCs. Moreover, acute bath application of C–C motif chemokine ligand 2 (CCL2) increased the frequency and amplitude of sIPSCs and sEPSCs in the MSNs, and especially strengthened the amplitude of N-methyl-D-aspartate receptor (NMDAR)-mediated miniature EPSCs. Further Ccl2 overexpression in the NAc in vivo decreased the peak amplitude of the sEPSC/sIPSC ratio. Finally, Ccr2 knock-down improved the impaired induction of NMDAR-dependent long-term depression (LTD) in the NAc after SNL. These results suggest that CCL2/CCR2 signaling plays a role in the integration of excitatory/inhibitory synaptic transmission and leads to an increase of the LTD induction threshold at the synapses of MSNs during neuropathic pain.