Comparative Molecular Field Analysis(CoMFA) of Curcumin-related Compounds for Anticancer Activity

Three-dimensional （3D） quantitative structure-activity relationship （QSAR） studies of 44 curcumin-related compounds have been carried out based on our previously reported result for their anticancer activity against pancreas cancer Panc-I cells and colon cancer HT-29 cells. The established 3D-QSAR models from the comparative molecular field analysis （CoMFA） in training set showed not only significant statistical quality, but also satisfying predictive ability, with high correlation coefficient values （R12= 0.911, R22= 0.985） and cross-validation coefficient values （q2= 0.580, q22= 0.722）. Based on the CoMFA contour maps, some key structural factors responsible for anticancer activity of these series of compounds were revealed. The results provide some useful theoretical references for understanding the mechanism of action, designing new curcumin-related compounds with anticancer activity and predicting their activities prior to synthesis.

STUDY ON THE SYNTHESIS OF BRASSINOLIDE AND RELATED COMPOUNDS 15.FORMAL SYNTHESIS OF BRASSINOLIDE VIA STEREOSELECTIVE SULFENATE-SULFOXIDE TRANSFORMATION

A formal synthesis of the natural growth promoting steroid brassinolide is described,which involves construction of side chain by 1,3-sulfoxide-hydroxyl transposition with methylation from(24S)- 22-E-24-sulfoxide 6 and(24R)-22-E-24-sulfoxide 9,respectively to (22S)-23-E-24-methyl compound 4.

SYNTHESIS OF 6,7-METHYLENEDIOXY-3-THIA-1(2H,4H)ACRIDONE AND THE RELATED THIA-ACRIDINE-PUSED HETEROCYCLIC COMPOUNDS

6,7-Methylenedioxy-3-thia-1(2H,4H)acridone and the related acridine-fused quinolines and pyridines,and also their flavylium-perchlorates were synthesized.The structures of all these compounds prepared are characterized by elemental analysis.IR and H-NMR spectra.

Effects of different cue positions on evoked potentials in the cerebral cortex during global and local processing of compound stimuli A study of event-related potential

BACKGROUND： Previous studies of attentional control have focused primarily on pre-cue control of attentional cue and direction. OBJECTIVE： To measure the differences in electrical activity of brain cells while processing pre-cue and post-cue compound stimuli, and to explore brain electrical activity during global and local processing of compound stimuli according to electroencephalogram （EEG） recordings. DESIGN, TIME AND SETTING： A within-subject design study was performed at the School of Psychology, State Key Laboratory of Cognitive Neuroscience and Learning, Beijing Normal University, China from March to May 2006. PARTICIPANTS： A total of 30 healthy, undergraduate students, aged 17-24 years, comprising 12 males and 18 females, were voluntarily enrolled from Beijing Normal University. Subjects exhibited normal or corrected-to-normal visual acuity. No significant non signal wave drift was detected during testing. METHODS： A total of 30 subjects were subjected to pre-cue and post-cue compound stimulus processing using event-related potential and EEG recordings. MAIN OUTCOME MEASURES： Evoked potential was recorded in different brain regions utilizing event-related potential to observe hemispheric symmetry, cue consistency and global-local features. RESULTS： Pre-cue compound stimuli resulted in hemispheric asymmetry for early wave （N1） and late wave （P3） in anterior brain regions. Early- and late-wave induced hemispheric asymmetry for electrode points （O1, 02, P3, P4, Pz, F3, F4, F7, F8, Fz, FP1, FP2, T7, TS, C3, C4, and Cz） during processing of pre-cue compound stimuli （P 〈 0.05）. Post-cue compound stimuli did not induce hemispheric asymmetry of brain waves induced by the above-described electrode points. No significant differences in global and local responses were determined during processing of post-cue compound stimuli. Under pre-cue conditions, significant differences were observed in N1 and P3 in the above-mentioned electrode points （P 〈 0.05）. However, under post-cue conditions, no significant differences were observed in N1 and P3 using the above-mentioned electrode points. Significant differences in early waves （N1 and P1） using the above-mentioned electrode points were detected between anterior and posterior brain regions, regardless of consistent or inconsistent, large or small letters （P 〈 0.05）. CONCLUSION： Cue location effected mechanisms underlying global and local processing of compound stimuli. Pre- or post-cue conditions resulted in differences in hemispheric symmetry, cue consistency, and global and local features. Under pre-cue conditions, hemispheric dominance was detected in global and local processing following compound stimuli. Under post-cue conditions, hemispheric dominance was not determined.

Investigating the Effect of Relative Width on Momentum Transfer between Main Channel and Floodplain in Rough Rectangular Compound Channel Sunder Varius Relative Depth Condition

Compound section is referred to a section the surface of which is made of several sub-sections with different flow characteristics. The difference in the hydraulic and geometry characteristics causes a complexity in flow hydraulic and creates an interaction between the main channel and floodplains, resulting in an apparent shear stress and a transverse momentum transfer. The amount of such a stress plays an important role in many river engineering measures [1]. Due to the flow complexity, the common approximate analytical methods are not enough to identify the flow profile. The FLOW3D Software with its great features in three-dimensional analysis of flow field is used as a tool to investigate the shear stress in a direct symmetrical compound rectangular channel. After the simulation of models, it is found that an increase in the relative width and relative depth parameters decreases the percentage of apparent shear stress and an increase in the relative roughness causes it to be increased [2].

Analytical method development of pregabalin and related substances in extended release tablets containing polyethylene oxide

Pregabalin,(S)-3-amino methyl hexanoic acid,is a structural analogue ofγ-amino butyric acid(GABA)which has been widely used to treat partial seizures and neuropathic pain[1].It is soluble in aqueous solution and sparingly soluble in organic solvents such as ethanol,DMSO and DMF.Polyethylene oxide(PEO)has a strong negative effect on analysis of hydrophilic active ingredient and its relative substances due to extremely high viscosity of PEO in aqueous media.The aim of this study is to develop a fast and precise method for the determination of pregabalin and its relative substances in extended release tablets including PEO using sodium sulfate for the treatment of sample solution.

Modified Equation of State for Pure Compounds

Proposed new cubic equation of state is more accurate than others in result and simple in form. The equation has been tried with 23 pure compounds including both polar and non-polar compounds. Experimental values of these compounds collected from various journals were compared with proposed model and found to be more accurate than other widely used cubic equations of state like SRK and Peng Robinson. The form of current EOS best suits to PVT data and total error is almost halved for a set of experimental data in the most cases.

Hypersensitive Inhibition of the Proliferation of Cells with Mutated DNA Repair-Related Genes by the Catalytic Topoisomerase II Inhibitor 20-O-IngenolEZ

We previously reported that many ingenol compounds derived from Euphoria kansui exhibit topoisomerase inhibitory activity. 20-O-ingenolEZ in these compounds exerted inhibitory effects on both topoisomerase II (topo II) activity and cell proliferative activity. Topoisomerase II inhibitors can be divided into the poison and catalytic inhibitor types and 20-O-ingenolEZ is a catalytic inhibitor and inhibits topo IIα through inhibition of ATPase activity, but induces topo II-mediated DNA damage and apoptosis in BLM-/- DT40 cells through the induction of the DNA damage checkpoint, similar to the poison type inhibitor adriamycin. The ATPase inhibitor of topo II ICRF-193 also showed poison-like characteristics in the same cell line. However, the inhibitory effects of ICRF-193 on the proliferation of BLM-/- DT40 cells differed from those of 20-O-ingenolEZ, as did the specificity of its inhibition of the proliferation of other cell lines. 20-O-ingenolEZ showed hypersensitive inhibition of the proliferation of MCF-7 cells and BLM-/- DT40 cells with mutated DNA repair-related genes.

Enantiomer Separation of α-Dimethyl Dicarboxylate Biphenyl and Related Biphenyl Compounds by Normal Phase HPLC on Polysaccharide Based Chiral Stationary Phases

Cellulose tris(4-methylphenylcarbamate), amylosetris(3,5-di-methylphenylcarbamate) and amylose tris (phenylcarbamate) were prepared by the methodreported by Okamoto and were coated onto an aminopropylated mesoporous spherical silica gel. Thesefinal products were used as chiral stationary phases of high performance liquid chromatography forthe eighteen structurally related biphenyl compounds. The resolution was made using normal-phasemethodology with a mobile phase consisting of n-hexane-alcohol (ethanol, 1-propanol, 2-pro-panol or1-butanol). The effects of various aliphatic alcohols in the mobile phase were studied. Thestructural features of the solutes that influence then- k′ were discussed. A dominant effect oftrifluoroacetic acid on chiral separation of acidic solutes was noted.

Differential Gene Expression Profiles in Acute Hepatic Failure Model in Mice Infected with MHV-3 Virus Intervened by Anti-hepatic Failure Compound

Differential gene expression profiles in Balb/cJ mouse model of acute hepatic failure infected with MHV-3 virus intervened by anti-hepatic failure compound （AHFC） and the changes of cytokines regulated by genes were investigated. The Balb/cj mice were divided into AHFC-intervened group and control group randomly. Acute hepatic failure model of Balb/cJ mice infected with MHV-3 virus was established. The survival rate in the two groups was observed. It was found that the survival rate in the AHFC-intervened group and control group was 90% and 50% respectively 48 h after intraperitoneal injection of MHV-3 （P〈0.05）. Before and after the experiment, the cytokines in peripheral blood of the survival mice were determined, and RNA was extracted from survival mouse liver tissue for the analysis of the differential gene expression by a 36 kb mouse oligonuleotide DNA array. In all the genes of microarray there were 332 genes expressed differently in the two groups, in which 234 genes were up-regulated and 78 genes down-regulated. Through clustering analysis, the differential expression of immune related genes, including TNF receptor superfamily, Kctd9, Bcl-2, Fgl2, IL-8, IL-6, IFN-7, TNF-α etc. might be related with the curative effectiveness of AHFC. It was suggested that AHFC can balance the immune state of mouse model of acute hepatic failure infected with MHV-3 virus mainly through regulating the expression of immune related genes, decrease the immune damage and inhibit liver cell apoptosis of mouse acute hepatic failure model obviously so as to increase the survival rate of mouse models of acute hepatic failure.

Ni-Ga BINARY PHASE RELATIONS AT 700℃

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ERR拮抗剂Compound 29抑制破骨细胞改善肥胖引起的骨丢失

目的在高脂饮食(HFD)诱导的肥胖雄鼠中探究雌激素相关受体alpha(ERR)拮抗剂Compound 29对小鼠骨量的改善作用。方法C57BL/6J雄鼠随机分为HFD组、“HFD+Compound 29”组(“HFD+C29”组)和普通饮食组(CD组),每组各6只。在整个实验过程中,HFD组和“HFD+C29”组小鼠用高脂饲料喂养,CD组小鼠用普通饲料喂养。喂养18周后,“HFD+C29”组小鼠每天Compound 29灌胃给药,CD组和HFD组小鼠等量溶剂灌胃,持续3周。最后进行口服葡萄糖耐量试验(OGTT)并处死小鼠收集样品。用微计算机断层扫描技术对右股骨进行骨组织形态学分析,左股骨石蜡包埋切片后分别进行苏木素伊红(HE)和抗酒石酸酸性磷酸酶(TRAP)染色,用酶联免疫吸附测定法检测血浆I型胶原交联羧基末端肽(CTX-I)浓度。结果骨扫描和HE染色结果显示与CD组相比,HFD组小鼠骨密度、骨小梁数量和厚度减少,HFD组小鼠发生骨量丢失;Compound 29给药后,HFD小鼠骨密度和骨量得到明显改善。TRAP染色和CTX-I浓度检测结果表明Compound 29给药后,HFD小鼠破骨细胞数量减少,骨吸收减弱。此外,OGTT结果显示Compound 29提高HFD小鼠糖耐受能力。结论ERR拮抗剂Compound 29改善HFD诱导的肥胖雄鼠的骨丢失。

虑及控制机构运动关联的柱塞泵动态特性研究

针对柱塞泵建模过程中因函数简化控制机构及其运动关系而造成的误差大、不精准问题,提出基于控制机构运动关联的非简化建模方法。结合柱塞泵的控制原理,利用AMESim搭建功率-压力-电比例复合控制的柱塞泵仿真模型。通过对压力、电流和转速的组合控制,对柱塞泵的控制特性进行仿真测试,得到与理论研究相吻合的动态特性曲线。进一步通过台架试验对柱塞泵进行测试,试验结果表明:柱塞泵在实际工作中存在响应时间,系统流量在液压系统开启和闭合瞬间存在冲击振荡。对比两种建模思想的仿真结果,非简化模型最大相对误差分别为3.51%和5.08%,平均相对误差分别为1.74%和1.98%,均小于简化模型。柱塞泵建模准确,为实现产品性能优化和系统数字孪生提供了模型支撑。

复方氨基酸注射液中有关物质N,N′-二乙酰-L-胱氨酸测定

目的:建立测定复方氨基酸注射液中乙酰半胱氨酸有关物质N,N′-二乙酰-L-胱氨酸含量的高效液相色谱法。方法:采用Atlantis dC_(18)色谱柱(4.6 mm×150 mm,3μm),以甲酸铵溶液(取甲酸铵315 mg,加水960 mL溶解,摇匀)-乙腈-甲酸(970∶30∶1)为流动相,流速为0.7 mL·min^(-1),检测波长为210 nm。结果:N,N′-二乙酰-L-胱氨酸浓度在2.697~53.94μg·mL^(-1)范围内线性关系良好(r=0.9999),检测限和定量限分别为1.4μg·mL^(-1)和4.4μg·mL^(-1),平均回收率为100.2%,RSD为0.5%。结论:经方法学验证,证明本法适用于复方氨基酸注射液中N,N′-二乙酰-L-胱氨酸的含量测定。

Syntheses of salvilenone and related compounds——I. A total synthesis of salvilenone

The first total synthesis of a novel phenalenone diterpene salvilenone (1) isolated from a- traditional Chinese medicine, Dan-Shen (Salvia miltiorrhiza.L.), has been achieved in thirteen steps started from resorcinol dimethyl ether(5).

Syntheses of salvilenone and related compounds——Ⅱ.A novel rearrangement of a tetrahydrophenalenone to a naphthopyranone(?)

The reaction of isopropenyl carbinol(2)with aqueous hydrobromic acid and hydroiodic- acid gave salvilenone(1)and naphthopyranone(3)respectively.The reaction mechanism has been investigated.The formation of(3)was undergone a novel rearrangement of a tetrahydrophenalenone to a naphthopyranone.

确认型递进句的互动功能和评价表达

文章详细考察了确认型递进句的互动功能和评价表达,发现该句式用于评价活动是对已有评价进行确认性回应后再推进到言者的评价,在语篇里有相对稳定的位置分布以及弱化分歧或强化赞同的互动功能,可联盟受话者。分句间是否隐含转折性决定其互动功能是弱化分歧还是强化赞同。其评价义来自评价性词语、比较、递进关联等评价性手段,这些手段分别涉及评价参数、评价的本质和评价的量级差异。该句式内部有实施不同评价行为的三种类型,最常实施的评价行为是使用不同词语评价同一对象。其分句关系、互动功能、评价性手段和评价行为有内在联系。

二氧化碳点阵激光联合复方倍他米松治疗白癜风的疗效及对Th17相关细胞因子的影响

目的:探讨二氧化碳点阵激光联合复方倍他米松治疗白癜风的疗效及对Th17相关细胞因子的影响。方法:选取2018年1月至2020年1月该院收治的白癜风患者90例,根据随机数表法分为对照Ⅰ组(二氧化碳点阵激光)、对照Ⅱ组(复方倍他米松)和联合治疗组(二氧化碳点阵激光合并复方倍他米松),每组30例。比较各组患者的疗效、Th17相关细胞因子水平。结果:联合治疗组、对照Ⅰ组和对照Ⅱ组患者的不良反应发生率分别为13.33%(4/30)、10.00%(3/30)和6.67%(2/30),差异无统计学意义(P>0.05)。联合治疗组、对照Ⅰ组和对照Ⅱ组患者的面部-颈部、四肢和手-脚部位白斑复色时间比较,差异均有统计学意义(P<0.05);联合治疗组患者的面部-颈部、四肢和手-脚部位白斑复色时间显著短于对照Ⅰ组、对照Ⅱ组,差异均有统计学意义(P<0.05)。治疗后,联合治疗组、对照Ⅰ组和对照Ⅱ组患者的白细胞介素(IL)17、IL-22和IL-23水平比较,差异均有统计学意义(P<0.05),联合治疗组患者的IL-17、IL-22和IL-23水平显著低于对照Ⅰ组、对照Ⅱ组,差异均有统计学意义(P<0.05)。联合治疗组、对照Ⅰ组和对照Ⅱ组患者的有效率分别为90.00%(27/30)、63.33%(19/30)和56.67%(17/30),联合治疗组患者的有效率显著高于对照Ⅰ组、对照Ⅱ组,差异均有统计学意义(P<0.05)。结论:二氧化碳点阵激光联合复方倍他米松治疗白癜风安全、有效,可降低患者血清Th17细胞相关因子IL-17、IL-22和IL-23水平。

低盐雪菜中呈味核苷酸关联物的检测及贮藏过程中的变化

为探明低盐雪菜中呈味核苷酸关联物在贮运期间的变化规律,建立高效液相色谱检测方法,分析低盐雪菜在(25±5)℃贮藏(J-25)、(4±1)℃贮藏(J-4)、灭菌后(25±5)℃贮藏(M-25)和灭菌后(4±1)℃贮藏(M-4)期间感官品质和呈味核苷酸关联物含量的变化。结果表明,12种呈味核苷酸关联物在33 min内有效分离。灭菌和冷藏均能抑制雪菜贮藏期间感官品质和呈味核苷酸关联物的劣化,且灭菌冷藏组合的效果最佳,M-4组雪菜中三磷酸腺苷(adenosine triphosphate,ATP)和肌苷酸含量在第60天仍分别是初始值的29.7%和66.4%,且感官品质合格。雪菜在(25±5)℃贮藏期间与ATP相关的核苷酸关联物总量呈先增加后迅速降低的趋势,其中J-25组雪菜仅有9 d的感官合格期。灭菌和冷藏能够有效抑制雪菜中核酸代谢的呈味核苷酸(腺苷酸、鸟苷酸、胞苷酸、尿苷酸)在贮藏期内的变化,M-4组雪菜中这4种核苷酸总量在贮藏末期仍有4.30 mg/100 g。低盐雪菜中发酵微生物的代谢和较高的温度加快了呈味核苷酸关联物在贮藏期间的劣变,灭菌和冷藏有利于呈味核苷酸关联物的保持,研究结果可为低盐雪菜的加工和贮藏提供一定的理论支撑。

LRP5基因突变导致骨质疏松症-假性胶质瘤综合征一例报告

报告一例常染色体隐性遗传发病的骨质疏松症-假性胶质瘤综合征。先证者女性,23岁,父母非近亲结婚,出生后发现双目失明,婴儿期因发现右眼视网膜母细胞瘤行右眼球摘除术,9岁开始反复发生轻微外力骨折,诊断为成骨不全。查体发现脊柱侧凸畸形、胸廓畸形、双上肢肘外翻、四肢关节韧带松弛。双能X线吸收检测仪(dual energy X-ray absorptiometry,DXA)骨密度明显低于同龄人,腰椎1-4骨密度Z值-5,左髋骨密度Z值-1.8。X线摄片示全身骨小梁稀疏。Sanger测序显示低密度脂蛋白受体相关蛋白-5(lowdensity lipoprotein receptor-related protein 5,LRP5)基因的6号外显子和23号外显子发生复合杂合突变,导致p.Pro382Leu+p.Cys1611LeufsX33。本文通过文献复习对该病的临床表现和诊疗特点进行讨论及总结,以期帮助临床医生提高对这一疾病的认识。