基于微通道技术合成2-氨基-5-氟-3',4'-二氯联苯

2-氨基-5-氟-3',4'-二氯联苯是琥珀酸脱氢酶抑制剂(SDHI)类杀菌剂—联苯吡菌胺的重要中间体。基于微通道技术,以3,4-二氯苯胺为原料,经重氮化、中和、与对氟苯胺偶联得到2-氨基-5-氟-3',4'-二氯联苯。系统考察了影响重氮化、中和、偶联3步对反应的影响,并得出优化条件:盐酸与3,4-二氯苯胺当量6:1,亚硝酸钠与3,4-二氯苯胺当量1.1︰1,成盐反应温度60℃,重氮反应温度25℃,氢氧化钠当量6.5︰1,中和温度25℃,偶联最佳温度120℃,对氟苯胺当量10︰1。在此优化条件下合成2-氨基-5-氟-3',4'-二氯联苯粗品含量85%,精制后含量可以达到98.5%,2步总收率65%。

NOTCH1基因3＇-UTR段双荧光素酶报告载体的构建及其活性鉴定

目的:构建含NOTCH1基因3'-UTR段双荧光素酶报告载体,并验证其活性。方法:使用PCR方法扩增含NOTCH1基因3'-UTR区序列,插入到双酶切的双荧光素酶报告载体中;使用生物信息学方法预测可能与NOTCH1基因3'-UTR相互作用的miRNA;使用lipofectamine 2000转染试剂将重组质粒或空质粒和miR-34a inhibitor或control真核表达载体共转染HEK293T细胞,双荧光素酶检测试剂盒测定荧光素酶活性。结果:得到含NOTCH1基因3'-UTR(1 648 bp)序列的双荧光素酶报告重组质粒,并用凝胶电泳和基因测序的方法验证。NOTCH1基因3'-UTR上可能有miR-34a的调控作用靶点;用重组质粒和miR-34a inhibitor共转染的HEK293T组的荧光素酶活性比空质粒组高45%。结论:含NOTCH1基因3'-UTR双荧光素酶报告载体构建成功,miR-34a对NOTCH1基因有调控作用。

Application of "3S" Technology in Ecological Environment Protection Area of Qinling

On the basis of briefly introduction of the status of eco-environmental protection work in Qinling,remote sensing,geographic information systems,global positioning system (short for '3S' technology) in the construction of eco-environmental protection information in Qinling,especially in the application of eco-environmental investigation,eco-environmental monitoring,environmental quality evaluation,were described in this study.Meanwhile,the existing problems and countermeasures for the application '3S' technology in the eco-environmental protection were also summarized.

Protective effects of 5,4'-dihydroxy-3',5'- dimethoxy-7-O-β-D -glucopyranosyloxy-flavone on experimental hepatic injury

AIM: To investigate the pharmacological effects of rice flavone (5,4'-dihydroxy-3',5'-dimethoxy-7-0-β-D-glucopyranosyloxy-flavone, RF) separated from panicle-differentiating to flowing rice on rat experimental hepatic injury. METHODS: Models of rat acute hepatic injury induced by carbon tetrachloride (CCl4) administration, rat hepatic fibrosis induced by thioacetamide, injury of primary cultured rat hepatocytes induced by CCl4, respectively, were established. After treated with RF, content of serum alanine transaminase (ALT), aspartate aminotransferase (AST) and albumin (Alb), hyaluronic acid (HA), the activity of glutathione peroxidase (GSH-Px), superoxide dismutase (SOD), and hydroxyproline (Hyp) were measured and liver tissue was observed pathologically by hematoxylin-eosin (HE) staining. Effects of RF on pathological changes, function index, enzyme of scavenging free radicals and blood rheology were evaluated. RESULTS: In model of rat acute hepatic injury induced by CCI4, RF can significantly decrease the contents of serum ALT, AST, increase the content of Alb, improve the dropsy and fat denaturalization of hepatocytes. In model of rat hepatic fibrosis induced by thioacetamide, RF can inhibit the increase of HA, Hyp and whole blood viscosity, and improve the activities of GSH-Px and SOD, and inauricular microcirculation. CONCLUSION: RF has apparent protective effects on hepatic injury by increasing activity of GSH-Px and SOD, scavenging free radicals produced by CCI4, reducing blood viscosity, and improving microcirculation and blood supply.

A Novel Three-dimensional Mn(Ⅱ) Coordination Polymer Constructed from Biphenyl-3,3',5,5'-tetracarboxylic Acid and Water

The title Mn（Ⅱ） coordination polymer,poly{[heptaaqua-（μ4-bi-phenyl-3,3？,5,5？-tetracarboxylate）-bimanganese（Ⅱ）] pentahydrate},[Mn_2（bpta）（H_2O）_7]_n·5n H_2O（I）,is crystallized from a mixture of biphenyl-3,3？,5,5？-tetracarboxylic acid（H_4bpta） and MnCl_2·4H_2O in waterethanol under room temperature. Its asymmetric unit consists of one and two halves of crystallographically independent Mn（Ⅱ） cations,one fully deprotonated H4 bpta ligand,seven coordinated water molecules and five solvent water as guest molecules. In I,each Mn（Ⅱ） atom is octahedrally coordinated by six oxygen atoms from bpta^（4-） anions and coordinated water molecules. In the Mn（Ⅱ） cations,one half Mn（Ⅱ） ion of them located at a 2-fold axis generating a trinuclear [Mn_3（H_2O）_2（RCOO）_2] linker by μ1,1-O（water） and μ1,3-O,O？（carboxylate） bridges and another half Mn（Ⅱ） ion with an inversion is a mononuclear linker. These neighbouring trinuclear and mononuclear Mn（Ⅱ） cations are linked together by biphenyl-3,3？,5,5？-tetracarboxylates to form a three-dimensional framework with a（42.84） topology of a（4,4）-connected net,in which the positions of the trinuclear [Mn_3（H_2O）_2（R-COO）_2] linker as a 4-connector linking four bpta^（4-） ligands in I reproduce an eagle-shaped arrangement. The polymeric structure exhibits a water channel with an accessible void of 797.1 ？~3,amounting to 15.7% of the total unit-cell volume. Each of the cavities in the network is occupied by solvent water molecules.

Synthesis of a dithieno[3,2-b∶2',3'-d]silole-based conjugated polymer and characterization of its short wave near-infrared fluorescence properties

Short wave near-infrared(SWIR,900-1700 nm)fluorescence imaging has attracted extensive research interest from scientists due to its high imaging quality.However,the variety of SWIR fluorescence imaging agents are quite limited and the corresponding quantum efficiency is rela-tively low.In this work,a novel conjugated polymer PDTSDTBT was reported,consisting of a donor unit with a tetrahedral Si(sp3)named DTS and an acceptor unit named DTBT with branched side chains.The design approach of endowing the donor-acceptor structure with the branched side chains successfully increase the fluorescence quantum efficiency.The polymer was prepared into nanoparticles by nanoprecipitation.The PDTSDTBT nanoparticles showed an absorption peak of 626 nm and fluorescence emission peak of 924 nm.The quantum efficiency of the nanoparticles is 0.53%,which is higher than that of nanotube fluorophores(0.4%).The nanoparticles also demonstrate a photothermal effect,the temperature of nanoparticles solution could reach 45℃under excitation by 660 nm laser.Therefore,the PDTSDTBT nanoparticles is an excellent fluorescent imaging agent with potential photothermal applications.

Pd/C催化Suzuki反应合成2,3',5'-三氯联苯

本文通过无配体Pd/C催化Suzuki-Miyaura偶联反应,以2-氯溴苯和3,5-二氯苯硼酸为原料,以碳酸钾作为碱,研究了不同反应温度对2,3',5'-三氯联苯合成的影响。作为对比,本文平行进行了Pd(PPh_(3))_(4)催化合成目标产物的实验,涉及Pd(PPh3)4催化的反应要求惰性气体反应氛围,且需在80℃下反应12小时。GC-MS跟踪监测显示:Pd/C催化的反应室温下反应12小时,几无产物生成。反应温度升至50℃时,反应2小时得到较多产物。50℃时,增加3,5-二氯苯硼酸至2倍当量,最终产率达到90%。有关催化剂回收方面,Pd(PPh3)4对空气敏感,反应结束后,未能回收,而无配体的Pd/C催化剂可循环使用5次以上而几无活性损失。与传统的含配体的Pd催化剂比较,无配体Pd/C催化在经济、环保以及实验操作方面表现出巨大的优势。

On the Rare Earth Chelates of(1'-Phenyl-3'-Methyl-5'-Pyrazolone-4')-Carbonylmethanoic Acid and 1,10-Phenanthroline

Some rare earth chelates of(1'-phenyl-3'-methyl-5'-phrazolone-4')-carbonylmethanoic acid and 1, 10-phenanthroline have been synthesized.The composition of the complexes were confirmed by elemental analy. sis.The molar conductance,IR,~4H-NMR,electronic spectra and thermogravimetric analysis of the chelates have been measured and discussed.

Systematic pharmacology analysis of Sodium 8-(((carboxymethyl)amino)methyl)-4',7-bishydroxy-isoflavone-3'-sulfonate

The purpose of this study is to use the newly synthesized molecule Sodium 8-(((carboxymethyl)amino)methyl)-4',7-bishydroxy-isoflavone-3'-sulfonate(M)as a research object,the pharmacological mechanism of the molecule was analyzed by using a series of Systematic pharmacology methods.The results show that the M molecule has a higher drug-like DL value of 0.59 and better molecular property parameters,namely Hdon=4,Hacc=10 and AlogP=0.94;A total of 11 M molecules related targets,namely F2,ESR1,AR,F10,CA2,DPP4,CCNA2,PRSS1,CDK2,GSK3B and PTPN1;A total of 140 diseases are associated with M molecule targets,and these diseases are mainly related to cancer and cardiovascular diseases;A total of 52 pathways involve the pharmacological mechanisms of M molecules,which are mainly related to cancer and other related diseases;GO-enriched analysis showed that these targets are closely related to the regulation of peptidase activity and biological processes such as blood coagulation and hemostasis.This article clearly demonstrated the pharmacological mechanism of M molecule,which provides references for exploring the pharmacological mechanism of new compounds.

关岭牛MSTN基因3'-UTR与bta-miR-27b的靶向验证

【目的】明确关岭牛bta-miR-27b与肌肉生长抑制素基因(MSTN)的结合位点及靶向调控关系,为通过调控miRNA改良关岭牛产肉量提供理论依据,也为贵州地方黄牛分子遗传改良工作提供新的切入点。【方法】通过TargetScan预测牛MSTN基因3'端非翻译区(3'-UTR)的潜在miRNA结合区域及互作miRNA,对比关岭牛与不同关岭牛杂交品种的生理表型及MSTN基因和3'-UTR端miRNA表达差异,并分析bta-miR-27b在不同关岭牛杂交群体中的靶位点特异性。将MSTN基因3'-UTR序列野生型(WT)和3'-UTR序列突变型(MUT)分别克隆至pMIR-REPORT Luciferase(H306)载体构建重组双荧光素酶报告基因载体,与bta-miR-27b共转染293T细胞以验证bta-miR-27b与MSTN基因的作用关系,并利用实时荧光定量PCR验证bta-miR-27b对MSTN基因表达的影响。【结果】在牛MSTN基因3'-UTR端发现7个miRNA结合位点;关岭牛各系杂交品种的3个miRNA(bta-miR-27a-3p、bta-miR-27b和bta-miR-128)相对表达量均极显著高于关岭牛(P<0.01,下同),MSTN基因相对表达量极显著低于关岭牛,体质量、体高、体斜长、胸围等生长指标却明显优于关岭牛。关岭牛及其杂交牛MSTN基因3'-UTR端的bta-miR-27b结合区域均无突变、无缺失;MSTN-3'-UTR(WT)与bta-miR-27bmimics共转染293T细胞后其相对荧光值下降53.80%,极显著低于MSTN-3'-UTR(MUT)+bta-miR-27bmimics共转染;转染bta-miR-27b mimics后,bta-miR-27b在关岭牛原代成肌细胞株(N2)中成功超表达,而MSTN基因相对表达量呈极显著下调趋势,表明bta-miR-27b能抑制MSTN基因表达。【结论】bta-miR-27b与MSTN基因的结合区域位于3'-UTR端第62~69位碱基处,且靶位点保守性较高。bta-miR-27b对MSTN基因有很强的靶向调控作用,表现为bta-miR-27b能抑制MSTN基因表达。

高花青苷高淀粉甘薯品种‘徐紫薯3号’的创制及特性鉴定

高花青苷高淀粉甘薯品种‘徐紫薯3号’是以高花青苷品种绫紫为母本,‘徐薯18’为父本,通过有性杂交,多年多点综合鉴定选育而成。该品种2011年通过国家甘薯新品种鉴定,鉴定编号为国品鉴甘薯2011019。通过对‘徐紫薯3号’的形态特征、品质性状、抗病性和生产力等研究,结果表明‘徐紫薯3号’全生育期长势平稳,薯形长纺锤形,结薯习性集中整齐,薯块紫皮紫肉,商品性好;薯块烘干率和淀粉率分别为35.44%和24.46%,极显著超过其双亲‘绫紫’和‘徐薯18’;鲜薯花青苷含量高达1105.4μg/g,花青苷产量达23 kg/hm2以上,比‘绫紫’提高26.98%;抗茎线虫病和黑斑病,极显著优于其双亲;4年25点次鉴定,鲜薯和薯干平均产量分别为23.87 t/hm2和8.36 kg/hm2;与其双亲相比,鲜薯产量比双亲平均值提高3.42%,薯干产量和淀粉产量均极显著超过其高亲‘徐薯18’,分别提高12.22%和22.60%;是一个适合花青苷提取和紫薯淀粉加工的优异品种,同时可以作为甘薯品种选育的花青苷源、黑斑病抗源和高淀粉源加以利用。

黄肉鲜食桃品种‘黄金蜜桃3号’的选育

白肉桃占据我国鲜食桃品种的主导地位,黄肉桃由于富含类胡萝卜素等健康有益成分,近年来受到部分消费者的青睐。‘黄金蜜桃3号’是中国农业科学院郑州果树研究所选用桃优系‘92-3-39’(母本)和‘91-2-2’(父本),通过人工杂交培育出的黄肉鲜食桃品种。该品种果实近圆形,果顶圆平,偶有小突尖,平均单果质量258 g,大果质量363 g,成熟时果皮底色黄,茸毛长度中等,大部分果面着深红色,套袋果呈金黄色。果肉橙黄色,可溶性固形物含量(w,后同)11.8%~13.6%,近核处红色素多,肉质致密,味甜,黏核。花铃型,花粉多,自花结实,丰产。郑州地区2月底花芽萌动,3月下旬开花,果实7月底至8月初成熟。

‘红阳’猕猴桃cDNA文库构建及F3H基因的表达初探

利用SMART（switching mechanism at 5’end of the RNA transcript）技术构建了红肉猕猴桃品种‘红阳’（Actinidia chinesis cv‘Hongyang’）内果皮组织的全长cDNA文库，此文库的构建有助于克隆与次生代谢相关的基因，特别是红肉猕猴桃花青素特异合成代谢的基因。文库滴度为6．7×10^4cfu／mL，库容为2．72×10^8cfu／mL，文库重组率99．8％，插入片段多数分布在700～1000bp。随机挑选1014个克隆进行测序，测序成功963个，经过序列拼接去除低质量序列后获得632个unigenes，包括92个contigs和540个singletons，获得已知功能unigenes共441个。从所测克隆中得到一个花青素途径的结构基因AcF3H，其cDNA序列长1369bp（GenBank登录号：FJ542819），CDS区为1101bp，编码366个氨基酸的多肽。与拟南芥、葡萄及龙胆已知乃日氨基酸序列比对，发现该基因十分保守。通过RT—PCR技术对苍溪栽培的不同发育时期‘红阳’猕猴桃果实AcF3H基因的表达进行了分析。结果表明，果肉转色前AcF3H基因表达量较高，而转色初期表达量降低，此后随着果实着色加深表达量维持在较高水平。

氮素形态对‘甘农3号'苜蓿不同生育期氮代谢的影响

为探讨紫花苜蓿(Medicago sativa)不同生育期需氮规律,采用砂培法研究3种氮素形态配比(NO_3^--N,NH_4^+-N以及NO_3^--N:NH_4^+-N为1:1)和3个氮素水平(0,105,210 mg·L^(-1))对‘甘农3号'(Medicago sativa‘Gannong No.3')整个生育期氮代谢的影响。结果表明:不同氮素形态处理下,‘甘农3号'的根瘤数、根瘤重、固氮酶活性、NO_3^--N含量、NH_4^+-N含量、硝酸还原酶活性和全氮含量均显著高于CK,混合态氮对于增加‘甘农3号'根瘤数、根瘤重、固氮酶活性和全氮含量效果最好,NH_4^+~N次之,NO_3^--N效果最差。氮素浓度为210 mg·L^(-1)时,各形态配比下7项测定指标均高于105 mg·L^(-1),其中根瘤数、根瘤重、固氮酶活性和全氮含量在NO_3^--N+NH_4^+-N的浓度为210 mg·L^(-1)最大;NO_3^--N含量和硝酸还原酶活性在NO_3^--N浓度为210 mg·L^(-1)时最大;NH_4^+-N含量在NH_4^+-N浓度为210 mg·L^(-1)时最大。各项测定指标均随着生育期的推进呈先增大后减小的趋势,全氮含量始终呈减小趋势。整个生育期,根瘤数与根瘤重成极显著正相关关系;根瘤数、根瘤重与固氮酶活性成显著正相关关系。

无核葡萄新品种——‘沪培3号’的选育

采用杂交技术和胚培养技术相结合的方法,选育出了无核葡萄新品种‘沪培3号’,其杂交亲本是‘喜乐’（二倍体）和‘藤稔’（四倍体）。在避雨栽培条件下,上海地区4月上旬萌芽,8月上中旬果实成熟。平均单穗质量460 g,平均单粒质量6.7 g,果粒椭圆形,紫红色,果肉细腻,可溶性固形物含量为16%-18%,口感较好。该品种树势强健,丰产稳产、适应性强。

反相离子对色谱法分析3′,5′反向寡核苷酸

3＇，5＇反向寡核苷酸是碱基组成和长度完全相同、碱基顺序相反的两个寡核苷酸序列。以三乙胺为离子对试剂，研究了缓冲液浓度（0．025～0．15mol／L）、pH（5．0～6．8）、柱温（25～45℃）、流速（0．3～0．7mL／min）以及不同初始洗脱强度和洗脱梯度条件下，6个3＇，5＇反向寡核苷酸模拟样品保留和分离的变化特点。三组反向序列在缓冲液浓度为0．05mol／L，pH6．8和流速0．4mL／min条件下获得最大分离，温度对分离的影响不大，而初始洗脱强度对反向序列的影响远大于洗脱梯度。实验结果表明3＇，5＇反向寡核苷酸的分离和保留趋势不完全一致，色谱条件的优化应有利于实现样品在柱上的弱保留。研究结果还显示寡核苷酸序列中5＇末端的保留强于3＇末端。

真核mRNA3′非翻译区在基因表达中的作用

真核生物ｍＲＮＡ的３′非翻译区（３′ＵＴＲ）在基因表达调控中发挥重要作用．它不仅调控ｍＲＮＡ在体内的稳定性和降解速率，控制着ｍＲＮＡ的利用效率，还参与ｍＲＮＡ翻译过程的调控．

甜糯型玉米新品种‘苏科糯3号'选育技术报告

‘苏科糯3号'是江苏省农业科学院粮食作物研究所育成的甜糯型玉米杂交种。在江苏省2007-2008年区域试验中,‘苏科糯3号'2年平均鲜穗产量为121 14.0kg/hm^2,比对照‘苏玉糯1号'增产12.3%;2009年生产试验中鲜穗平均产量为12 859.5 kg/hm^2,比对照‘苏玉糯5号'增产11.7%。该品种具有产量高、品质好、熟期较早等特点,适宜江苏省玉米种植区域种植。

葡萄新品种——‘桂葡3号’的选育

‘桂葡3号’是从欧美杂交种葡萄品种‘金香’群体中选育的优良芽变单株,该品种平均穗质量430.0 g,果穗大小中等,平均单果质量5.5 g,果粒长椭圆形,成熟时果皮黄绿色,成熟期一致,具有浓郁玫瑰香味,可溶性固形物含量19.0%,666.7 m^2产量850.0 kg,在广西等亚热带地区可进行一年两收生产,丰产性能好,品质优。植株生长势中庸,坐果率高,栽培容易。

早熟油桃新品种‘紫金红3号’的选育

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