First Total Synthesis of Hyacinthacine A6 from the Protected Derivative of Polyhydroxylated Pyrrolidine

（1S、2R、3R、5R、7aR）-1,2-Dihydroxy-3-hydroxy methyl-5-methylpyrrolizidine（hyacinthacine A6, I） was synthesized by Wittig＇s methodology via the reaction of aldehyde 6, prepared from the partially protected derivative of polyhydroxylated pyrrolidine, with appropriated ylides, followed by cyclization through the intemal reductive amination process of the resulting a,B-unsaturated ketone 7, and total deprotection.     

β-环糊精与土霉素的相互作用研究及分析应用

以荧光法研究了土霉素（OTC）与环糊精（β-CD）的包合作用,并利用β-CD对OTC荧光的增敏作用建立了一种高灵敏度测定OTC的新方法,土霉素在9.19×10^-8-1.66×10^-5mol/L范围内与荧光强度成正比,方法的检出限为7.4×10^-9mol/L,方法用于药物制剂中土霉素的测定,结果与标示量吻合。荧光光度法测得OTC与β-CD形成1∶1包合物,包合物形成常数为3.68×10^2L/mol。从土霉素和环糊精的分子结构出发,对包合物的形成机理进行了探讨。     

Determination of the composition,encapsulation efficiency and loading capacity in protein drug delivery systems using circular dichroism spectroscopy

Peptides and proteins have become very promising drug candidates in recent decades due to their unique properties. However, the application of these drugs has been limited by their high enzymatic susceptibility, low membrane permeability and poor bioavailability when administered orally. Considerable efforts have been made to design and develop drug delivery systems that could transport peptides and proteins to targeted area. Although it is of great importance to determine the composition after loading a drug to the carrier, the ability to do so is significantly limited by current analytical methods. In this letter, five important proteins, α₁-antitrypsin, hemoglobin human, human serum albumin, human transferrin and r-globulin were chemically conjugated to two model drug carriers, namely carbon dots and polymer O-(2-carboxyethyl) polyethylene glycol. A simple yet convenient method based on circular dichroism spectroscopy was developed to determine the compositions of the various protein-carrier conjugates.     

Formation,characterization and stabilization of water-soluble colloidal MnO<Subscript>2</Subscript> in the oxidation of methionine,thiourea and thioacetamide by permanganate

Stabilization and characterisation of water soluble colloidal MnO₂ during the oxidation of sulphur-containing organic reductants “thiourea, thioactamide and methionine” by permanganate in aqueous neutral media are reported for the first time. Upon addition of permanganate to a solution of methionine, a transient species appears within the time of mixing, which is stable for several weeks. On the other hand, the transient species is unstable in the presence of thiourea and thioacetamide, respectively. The nature of manganese (IV) species present in the solution was characterized by spectrophotometric and coagulation measurements. On addition of HClO₄, there is a decrease in the absorbance of the reaction mixture. Under pseudo first-order conditions ([reductants] > []), the reduction rate was very fast up to the formation of water soluble colloidal MnO₂. The effect of various parameters, such as hydrogen ion concentration, amount of and concentration of reductants were investigated. Mechanisms consistent with the observed results have been proposed and discussed.     

新型二硫杂环戊烯硫酮化合物的合成及其对谷氨酸诱导损伤HT22细胞的保护作用

在保留ADT-OH的3H-1,2-二硫杂环戊烯-3-硫酮结构的基础上,用芳乙烯基替换4-羟基苯环,设计并合成了6个二硫杂环戊烯硫酮化合物（L₁~L₆,其中L₂, L₃, L₅和L₆为新化合物）,其结构经¹H NMR, ¹³C NMR和HR-MS(ESI)表征。采用MTT法研究了L₁~L₆对谷氨酸诱导损伤的海马神经元HT22细胞的影响。药理初筛结果表明:给药浓度为10~100 μmol·L^-1时,L₁, L₂, L₄和L₆均能提高受损HT22细胞的存活率(P<0.01);给药浓度为1 μmol·L^-1时,L₃和L₅均可提高损伤HT22细胞的存活率(P<0.01)。     

胭脂鱼消化道黏膜上皮扫描电镜观察

应用扫描电镜观察了胭脂鱼食管、胃、前肠、中肠和后肠黏膜上皮表面细微结构。发现消化道黏膜皱褶形态差异显著,胃黏膜上皮细胞表面有微绒毛,分布密集,但在部分区域有成簇的壁细胞,呈柱状;肠黏膜上皮表面的微绒毛似苔藓状覆盖在细胞的表面,扫描电镜观察发现前肠上皮细胞分泌孔较多,微绒毛密集且高度参差不齐;中肠上皮细胞分泌孔明显减少,微绒毛比前肠密且平整;后肠分泌孔孔径变小,数量最少,且微绒毛较稀疏,表面最平滑,细胞呈梭形环绕,形成杯状结构。亚成体鱼与幼鱼的消化道黏膜上皮结构相似,但其分泌孔孔径和分泌孔密度有差异,亚成体鱼的分泌孔孔径和分泌孔密度更大,说明亚成体鱼消化能力强于幼鱼。 更多还原     

共面对称条件下Mg原子(e,2e)反应的三重微分截面的计算

采用修正的扭曲波玻恩近似(DWBA)方法,本文计算了共面对称几何条件下电子碰撞Mg(3s2) 原子(e,2e)反应的三重微分截面.理论方法通过引入Gamow因子来表示(e,2e)反应的后碰撞相互作用(PCI).将计算结果与实验结果及标准DWBA计算结果进行了比较,发现PCI效应起着重要的作用.     

1-苯并噻唑基-吡唑啉类荧光化合物的合成及其荧光光谱

合成了几种苯并噻唑基 -吡唑啉类化合物 ,经红外吸收光谱和荧光发射光谱测定 ,此类化合物具有一定的荧光性 ,其荧光强度的大小与衍生物中不同的取代基有关。     

一种紫外-可见光谱法检测水质COD的浊度影响实验研究

消除浊度影响是直接光谱法检测水质COD的关键技术问题。此源于紫外-可见光谱法检测水质参数的关键依赖于化学计量法所建立的准确的水质参数分析模型,而浊度是影响其建模的一个重要参数。为此,选取福尔马肼浊度液和邻苯二甲酸氢钾标准溶液,开展了紫外-可见吸收光谱法检测水质COD的浊度影响实验研究,获得了选定溶液在245,300,360和560 nm几个特征波长点的吸光度随浊度变化的最小二乘法拟合曲线,分析了吸光度随浊度的变化规律。研究结果表明,在240～380 nm的紫外光谱段,由于引起浊度的颗粒物对有机物产生了吸附,致使浊度对水样的紫外光谱影响较为复杂;在380～780 nm的可见光谱区域,浊度对光谱的影响则是随着波长的增大而减弱。基于此,开展了多元散射校正法对受浊度影响的水样光谱进行校正试验。对某溪水水样的紫外-可见吸收光谱进行多元散射校正,通过处理前后光谱对比表明,浊度引起各个波长点的基线偏移都得到了有效的校正,而在紫外区域特征并未减弱。接着对选取的三种液体的紫外-可见吸收光谱进行多元散射校正,实验结果表明：该方法可在不影响水样紫外-可见吸收光谱特征的前提下对其吸收曲线进行有效的校正,这不仅提高了光谱法检测水质COD的信噪比,而且还为化学计量法建立准确、有效的水质检测COD分析模型进行数据预处理提供了一种新途径。     

二维流场、热结构松耦合模拟研究

本文针对轴对称型飞行器前缘部位,采用松耦合方法,开展了二维高超声速流固界面的热耦合计算。满足非稳态N-S方程的外部流场和内部非稳态热传导均采用商用软件FLUENT进行计算。通过对相同时刻,不同松耦合推进时间步长引起的壁面热流密度、壁面温度、表面传热系数的差异对比,得出了松耦合推进时间对以上参数的影响规律,这对有效实施松耦合方法进行高超声速飞行器模拟具有积极意义。