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Study on the Crystallization Process of Labeled GL-7-ACA Acylase CA130 Complex 7β-bromoacetyl amino cephalosporanic acid (BA-7-ACA), an analog of glutaryl-7-amino cephalosporanic acid (GL-7-ACA), can inhibit and specifically alkylate GL-7-ACA acylase (CA130) from Pseudomonas sp. 130, forming a carbon-carbon bond between BA-7-ACA and the C-2 on indole ring of Trp-β4 residue of CA130.Here we reported that BA-7-ACA labeled CA130 (BA-C130) could self-catalyze the hydrolysis of BA-7-ACA during crystallization process. The hydrolysis was confirmed to be a reaction analogous to the one of GL-7-ACA by comparative MALDI-TOF (matrix-assisted laser desorption/ionization-time of flight) spectrometry analysis.

二、GL-7-AcA酰化酶CA130标记复合物的结晶过程研究溴乙酰氨基头孢烷酸(7β-bromoacetyl amino cephalosporanic acid,BA-7-ACA)作为戊二酰-7-氨基头孢烷酸(GL-7-ACA)的类似物,不仅能够抑制GL-7-ACA酰化酶CA130的活力,而且能通过在BA-7-ACA和CA130的β亚基第四位色氨酸吲哚环二位碳原子之间形成碳-碳共价键而将CA130特异的烷基化。

Dimethylhexane-1,6-dimethyleurethane is the key material for preparation of 1,6-hexamethylene diisocyanate by non-phosgene route. Our work mainly focuses on the study of the catalytic performances of metal oxysalts and metal oxides for the ammonolysis of DMC to HDU-M. Experiment effect showed the ammonolysis was omposed by two steps, in which the first step was easier to occur than the second.

中文摘要六亚甲基-1,6-二氨基甲酸甲酯是非光气合成六亚甲基二异氰酸酯的关键原料,本文主要对金属含氧酸盐和金属氧化物这两类用于碳酸二甲酯胺解合成HDU-M 的催化剂进行了初步研究并优化了工艺条件。

The important role of hydroxycinnamic acids,i.e.,caffeic acid, chlorogenic acid,sinapic acid,ferulic acid,3-hydroxycinnamic acid (3-HCA) and 4-hydroxycinnamic acid(4-HCA) as the pBR322 plasmid DNA-Cleaving agents in the presence of Cu ions was investigated.

我们研究了羟基肉桂酸衍生物即咖啡酸、绿原酸、芥子酸、阿魏酸、3-羟基肉桂酸(3-HCA)和4-羟基肉桂酸(4-HCA)在Cu存在下诱导pBR322质粒DNA链断裂损伤情况,结果发现HCAs的促氧化活性与它们的分子结构有密切的关系,具有邻二羟基结构和邻二甲氧基羟基结构的化合物表现出了更高的促氧化活性,其中CaA的活性最高。

Influences of initiator,sulphonate,acrylic acid and diethylmaleate on fluidity of cement paste were studied in detailsAddition of diethyl maleate helped to reduce slump loss.

详细研究了引发剂、磺酸盐、丙烯酸和马来酸二乙酯等因素对净浆流动度的影响;马来酸二乙酯的加入,减小了流动度损失。

Aggregation Behavior and the Hard Water Resistant Ability of Linear Alkylbenzene Sulphonate :MesoDyn Simulation and Quantum Calculation Study The quantum calculation and MesoDyn simulation were combined in this paper, the Critical Micella Concentration difference of LAS and AS was studied by the simulation, and aggregation morphology as well as aggregation behavior of linear alkylbenze sulfonate in aqueous solution was investigated by MesoDyn simulation in the presence and absence of shear.

水溶液中直链烷基苯磺酸盐的介观模拟及其抗硬水能力的量子化学计算将介观模拟和量子化学计算方法相结合,通过模拟的方法从介观角度研究了十二烷基苯磺酸盐和十二烷基磺酸盐临界聚集浓度的差异,考察了LAS水溶液体系的聚集形貌以及微相分离时发生的复杂行为。

In order to obtain versatile ulitity of host molecules, three new chiral calix [4] crown ethers containing aza, thio atoms bearing two chiral sites provided by -cysteine ester were synthesized by the condensation of calix [4] arene diacid dichloride with oligoethylene glycol bridged bis-amino acid methyl ester. All new compounds were characterized by NMR, MS and elemental analysis.

以-半胱氨酸为手性源,利用多甘醇二氯醚在碱性条件下对半胱氨酸巯基进行烷基化反应,成功地合成了多甘醇醚链桥联的半胱氨酸衍生物,醚化反应后,在高度稀释条件下与对叔丁基杯[4]芳烃二乙酰氯进行双功能基缩合反应成功地合成了新型的手性杯[4]含氮、硫杂冠醚,并利用〓H NMR、MS等谱图手段对其结构进行了表征。

TrithiocarbonatesS,S\'-bis (α,α′-dimethyl-α-acetic acid) trithiocarbonate (TTC1),3-(2-carboxyethylsulfanylthiocarbonylsulfanyl) propionic acid (TTC3),2-(2-carboxyethylsulfanylthiocarbonylsulfanyl) propionic acid (TTC4) and2-(2-carboxyethylsulfanylthiocarbonylsulfanyl)-2-methylpropionic acid (TTC5) weresynthesized by phase transfer method.

用相转移法合成了S,S′-二(α,α′-甲基-α&-乙酸)三硫代碳酸酯(TTC1)、S,S′-二丙酸三硫代碳酸酯(TTC3)、S-丙酸-S′-三硫代碳酸酯(TTC4)和S-丙酸-S′-(α,α′-甲基-α&-乙酸)三硫代碳酸酯(TTC5)。

PGA and CMC-Na (FH-9) were the chosen stabilizers. Based on the orthogonal experiment,the optimum added amount of stabilizers and homogenizing and sterilization parameters wereobtained. The results indicated that the best formula of this kind of fermented soybean drink withthe greatest stability were: 0.4% of CMC-Na(FH-9),0.2% of PGA, 0.067% of MG and 0.083%ofSE, homogenizing twice under 40℃,30MPa and pasteurizing twice under 80℃ for 20min. Thesensory ,physical, chemical and microorganism target of fermented soybean drink were studiedand conformed to the Chinese Standards.

对发酵纯豆乳饮料的调配工艺和稳定性进行了研究,选出对提高酸豆乳饮料稳定性有良好作用的稳定剂配方为羧甲基纤维素钠FH-90.4%、藻酸丙二醇酯0.2%,乳化剂为单甘酯0.067%和蔗糖酯(SE-15)0.083%,确定了最佳均质条件为30MPa 40℃二次均质,杀菌条件为80℃20min的两次常压杀菌,并测定了纯酸豆乳饮料的感官、理化和微生物指标。

Sibiricum samples. Conclusion: 5-O-caffeoylquinic acid, 1,4-di-O-caffeoylquinic acid and 4,5-di-O-caffeoylquinic acid were isolated from Xanthium plant for the first time.

5-O-咖啡酰奎宁酸,1,4-二-O-咖啡酰奎宁酸和4,5-二-O-咖啡酰奎宁酸是从苍耳属植物中首次分离获得。

The effects and mechanism of GABAergic neurons, NOergic neurons, opioid peptide and cyclic adenosine monophosphate in the nucleus reticularis thalami on sleep-wakefulness cycle of rats and the effects and mechanism of the 5-HTergic nerve fibers project from the nucleus raphes dorsalis to RT on sleep-wakefulness cycle of rats were investigated with the methods of brain stereotaxic, nucleus spile, microinjection and polysomngraphy.1. The effects of GABAergic neurons in RT on sleep-wakefulness cycle of rats1.1 Microinjection of 3-mercaptopropionic acid (3-MP, a kind of glutamate decarboxylase inhibitor) into RT. On the day of microinjection, sleep only decreased a litter. On the second day, sleep marked decreased and wakefulness marked increased. On the third and fourth day, sleep and wakefulness stages resumed to normal.1.2 Microinjection of gamma-amino butyric acid (GABA 1.0μg) into RT enhanced sleep and reduced wakefulness compared with control; while microinjection of L-glutamate (L-Glu, 0.2μg) decreased sleep and increased wakefulness; microinjection of bicuculline (BIC, 1.0μg), a GABAA receptor antagonist, enhanced wakefulness and reduced sleep; microinjection of baclofen (BAC, 1.0μg), GABAB receptor agonist, had the same effects as GABA.2. The effects of NOergic neurons in RT on sleep-wakefulness cycle of rats2.1 Microinjection of L-arginine (L-Arg, 0.5μg) into RT decreased sleep compared with control, but there were on statistaical difference between L-Arg group and control; while microinjection of sodium nitroprusside (SNP, 0.2μg), a NO donor into RT, sleep marked decreased and wakefulness marked increased. Microinjection of nitric oxide synthase inhibitor, N-nitro-L-arginine (L-NNA, 2.0μg) into RT enhanced sleep and reduced wakefulness.2.2 After simultaneous microinjection of L-NNA (2.0μg) and SNP (0.2μg) into RT, SNP abolished the sleep-promoting effect of L-NNA compared with L-NNA group; after simultaneous microinjection of L-NNA (2.0μg) and L-Arg(0.5μg) into RT, we found that L-NNA could not blocked the wakefulness-promoting effect of L-Arg.3. The effects of opioid peptide in RT on sleep-wakefulness cycle of rats3.1 Microinjection of morphine sulfate (MOR, 1.0μg) into RT increased wakefulness and decreased sleep compared with control; while microinjection of naloxone hydrochloride (NAL, 1.0μg), the antagonist of opiate receptors, into RT, enhanced sleep and reduced wakefulness.3.2 After simultaneous microinjection of MOR (1.0μg) and NAL (1.0μg) into RT, the wakefulness-promoting effect of MOR and the sleep-promoting effect of NAL were not observed compared with control.4. The effects of cAMP in RT on sleep-wakefulness cycle of rats Microinjection of cAMP (1.0μg) into RT increased sleep and decreased wakefulness compared with control; microinjection of methylene blue (MB,1.0μg) into RT enhanced sleep and reduced wakefulness compared with control.5. The effects of the 5-HTergic nerve fibers project from DRN to RT on sleep-wakefulness cycle of rats5.1 When L-Glu (0.2μg) was microinjected into DRN and normal sodium (NS,1.0μg) was microinjected into bilateral RT. We found that sleep was decreased and wakefulness was increased compared with control; when L-Glu (0.2μg) was microinjected into DRN and methysergide (MS,1.0μg), a non-selective 5-HT antagonist, was microinjected into bilateral RT, We found that sleep was enhanced and wakefulness was reduced compared with L-Glu group.5.2 When p-chlorophenylalanine (PCPA, 10μg) was microinjected into DRN and NS (1.0μg) was microinjected into bilateral RT, We found that sleep was increased and wakefulness was decreased compared with control; microinjection of 5-hydroxytryptaphan (5-HTP, 1.0μg), which can convert to 5-HT by the enzyme tryptophane hydroxylase and enhance 5-HT into bilateral RT, could block the effect of microinjection of PCPA into DRN on sleep-wakefulness cycle.

本研究采用脑立体定位、核团插管、微量注射、多导睡眠描记等方法,研究丘脑网状核(nucleus reticularis thalami,RT)中γ-氨基丁酸(gamma-amino butyric acid ,GABA)能神经元、一氧化氮(nitrogen monoxidum,NO)能神经元、阿片肽类神经递质、环一磷酸腺苷(cyclic adenosine monophosphate,cAMP)及中缝背核(nucleus raphes dorsalis,DRN)至RT的5-羟色胺(5-hydroxytryptamine,5-HT)能神经纤维投射对大鼠睡眠-觉醒周期的影响及其作用机制。1 RT内GABA能神经元对大鼠睡眠-觉醒周期的影响1.1大鼠RT内微量注射GABA合成关键酶抑制剂3-巯基丙酸(3-MP,5μg),注射当天睡眠时间略有减少,第二日睡眠时间显著减少,觉醒时间明显增多,第三、四日睡眠和觉醒时间逐渐恢复至正常。1.2大鼠RT内微量注射GABA受体激动剂GABA( 1.0μg)后,与生理盐水组比较,睡眠时间增加,觉醒时间减少;而RT内微量注射L-谷氨酸(glutamic acid, L-Glu, 0.2μg)后,睡眠时间减少,觉醒时间增加;RT内微量注射GABAA受体阻断剂荷包牡丹碱(bicuculline,BIC,1.0μg)后,睡眠时间减少,觉醒时间增加;RT内微量注射GABAB受体激动剂氯苯氨丁酸(baclofen,BAC,1.0μg)后,产生了与GABA相似的促睡眠效果。2 RT内NO能神经元对大鼠睡眠-觉醒周期的影响2.1大鼠RT内微量注射NO的前体L-精氨酸(L-Arg,0.5μg)后,与生理盐水组对比,睡眠时间略有减少,但无显著性意义;而RT内微量注射NO的供体硝普钠(Sodium Nitroprusside,SNP,0.2μg)后可明显增加觉醒时间,缩短睡眠时间;微量注射一氧化氮合酶抑制剂L-硝基精氨酸(L-arginine,L-NNA,2.0μg)后,引起睡眠时间增多,觉醒时间减少。2.2大鼠RT内同时微量注射L-NNA(2.0μg)和SNP(0.2μg)后与L-NNA组比较发现SNP逆转了L-NNA的促睡眠作用;RT内同时微量注射L-NNA(2.0μg)和L-Arg(0.5μg)后,与L-NNA(2.0μg)组比较发现L-Arg可以增加觉醒而缩短睡眠,其促觉醒作用未能被NOS的抑制剂L-NNA所逆转。3 RT内阿片肽对大鼠睡眠-觉醒周期的影响3.1大鼠RT内微量注射硫酸吗啡(morphine sulfate,MOR,1.0μg)后与生理盐水组对比,睡眠时间减少而觉醒时间增加; RT内微量注射阿片肽受体拮抗剂盐酸纳洛酮(naloxone hydrochloride,NAL,1.0μg)后与生理盐水组比较,睡眠时间增加而觉醒时间减少。3.2大鼠RT内同时微量注射MOR(1.0μg)和NAL(1.0μg)后,与生理盐水组对比,原有的MOR促觉醒效果和NAL的促睡眠效果都没有表现。4 RT内环一磷酸腺苷信使对大鼠睡眠-觉醒周期的影响大鼠RT内微量注射cAMP(1.0μg)后与NS(1.0μg)组比较,睡眠时间增多而觉醒时间减少;RT内微量注射亚甲蓝(methylene blue,MB,1.0μg)后,与NS组比较,睡眠时间增多而觉醒时间减少。5中缝背核投射到丘脑网状核的5-羟色胺能神经纤维对大鼠睡眠-觉醒周期的影响5.1大鼠DRN内微量注射L-Glu(0.2μg),同时在双侧RT内微量注射NS (1.0μg)后,与对照组(DRN和双侧RT注射NS, 0.2μg)比较,睡眠时间减少,觉醒时间增多;大鼠DRN内微量注射L-Glu(0.2μg),同时在双侧RT内微量注射二甲基麦角新碱(methysergide, MS, 1.0μg )后,与对照组(DRN注射L-Glu 0.2μg,双侧RT注射NS 1.0μg)比较,睡眠时间增多,觉醒时间减少。5.2大鼠DRN内微量注射对氯苯丙氨酸(p-chlorophenylalanine,PCPA,10μg),同时在双侧RT内微量注射NS (1.0μg)后,与对照组(DRN和双侧RT注射NS, 1.0μg)比较,睡眠时间增多,觉醒时间减少;大鼠DRN内微量注射PCPA(10μg),产生睡眠增多效应后,在双侧RT内微量注射5-羟色胺酸(5-hydroxytryptaphan , 5-HTP, 1.0μg )后,与对照组(DRN注射PCPA 10μg,双侧RT注射NS 1.0μg)比较,睡眠时间减少,觉醒时间增多。

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