3-(3′-羟基)丁基苯酞氨基酸酯衍生物的设计与合成

3-(3′-羟基)丁基苯酞是丁苯酞在体内的代谢产物,具有多种药理作用,可以作为一种新的活性成分应用于药物开发中。本文以甘氨酸、甲硫氨酸和亮氨酸为起始原料,经过Boc保护,再与3-(3′-羟基)丁基苯酞进行缩合,脱保护3步反应合成了3-(3′-羟基)丁基苯酞的氨基酸酯。以期提高水溶性和改善药代动力学性质,获得3-(3′-羟基)丁基苯酞的前药。     

Fe(OH)_3胶体与铜离子作用的研究

使用切向流超滤系统得到粒度较均匀的Fe(OH)3胶体,进而对Fe(OH)3胶体粒子与Cu2 的作用进行了研究,并将实验结果与南沙群岛海区表层水中铜与胶体物质结合状况的调查数据进行了比较分析,得到如下结果:(1)在海水介质中,铜在Fe(OH)3胶体上结合的百分率(pH>5)随pH的升高而下降,随着Fe(OH)3胶体浓度的减小而下降?(2)在天然海水介质中,使铜在Fe(OH)3胶体上结合的百分率在50%-70%的有机物浓度为1.0mg·L-1,有机物浓度的增大使铜与无机胶体结合的百分率有下降的趋势?     

Experimental evaluation of the isotopic exchange equilibrium 10B(OH)3+11B(OH)4−=11B(OH)3+10B(OH)4− in aqueous solution

The precision of spectrophotometric measurements of indicator absorbance ratios is sufficient to allow evaluation of small isotopically induced differences in the dissociation constant of boric acid (K_B). The quotient of ¹¹K_B and ¹⁰K_B, obtained using isotopically ⩾99% pure borate/boric acid buffers, provides an equilibrium constant for the reaction ¹⁰B(OH)₃+¹¹B(OH)₄⁻⇔¹¹B(OH)₃+¹⁰B(OH)₄⁻ which heretofore had not been experimentally determined. Previous theoretical and semi-empirical evaluations of this equilibrium, which is important for assessments of the paleo-pH of seawater and the paleo-pCO₂ of the atmosphere, have yielded constants, ^11–10K_B=¹⁰K_B/¹¹K_B, that have ranged between 1.0194 and approximately 1.033. The experimentally determined value ^11–10K_B=1.028₅±0.001₆ (mean±95% confidence interval) obtained at 25 °C and 0.63 molal (mol kg⁻¹ H₂O) ionic strength is in much better agreement with recent theoretical assessments of ^11–10K_B that have ranged between 1.026 and 1.033, than the much-cited original estimate (1.0194) of Kakihana et al. (1977) [Fundamental studies on the ion-exchange separation of boron isotopes. Bulletin of Chemical Society of Japan 50, 158–163]. Since the activity quotient for the fractionation reaction is almost equal to unity, it is expected that the ^11–10K_B value obtained in this study will be applicable over a wide range of solution compositions and ionic strengths.     

(S)-3-苄氧羰基氨基戊酸的合成

以(S)-2-氨基丁酸为起始原料,经过氨基保护、重氮化、Wolff重排三步反应合成了海洋天然环酯肽Obyanamide中的β-氨基酸单元,总收率为65.2%。     

0808号台风"凤凰"登陆过程的三维变分同化试验

主要对0808号台风"凤凰"的登陆过程进行模拟试验.首先,利用GPS掩星资料反演的大气气压、温度和水汽资料以及云导风资料,对台风"凤凰"进行了三维变分同化及数值模拟试验.结果表明:同化不同资料,得到的台风初始场各不相同,对台风预报的影响也各不相同.同时同化GPS资料和云导风资料,对台风初始场的调整最大,对模拟台风登陆前...     

苯并异噻唑啉酮类衍生物的制备与生物活性测试

以1,2-苯并异噻唑-2(3H)-酮为原料合成了3-羰基苯并异噻唑-2(3H)-苯甲酸甲酯衍生物,目标化合物的结构经元素分析、<'1>H NMR和质谱确证.化合物对大肠杆菌、金黄色葡萄球菌、溶藻弧菌、嗜水气单胞菌、枯草芽孢杆菌5种海洋菌的抑菌活性结果表明,化合物对上述菌种均有不同程度的抑制作用,其中对大肠杆菌活性最高,...     

西施舌3 个自然群体杂合性的研究

采用聚丙烯酰胺凝胶电泳技术,对广西北海、福建漳港和江苏启东3个西施舌(Coelomactra antiquata (Spengler))自然群体杂合性进行了研究.共检测分析了7个酶,获得12个位点,25个等位基因.其中4个位点是多态的,分别是Sod-1、Mdh-1、Est-1、Est-3,这些位点分别有1～7个等位基因.结果表明,福建漳港群体的Sod-1和Est-1位点、广西北海群体的勋Sod-1位点符合Hardy-weinberg平衡(P>0.05);江苏启东群体的多态位点中所有位点、福建漳港群体的Mdh-1、Est-3位点,广西北海群体的Mdh-1、Est-1、Est-3位点均非常显著偏离Hardy-weinberg平衡(P<0.01).另外,除了江苏启东和福建漳港群体的Est-1位点表现出杂合子缺失(F>0)外,各群体中每个位点均表现出杂合子过量(F<0).结合各群体中每个多态位点的观察杂合度和期望杂合度,认为中国东南沿海西施舌的种质资源状况良好.     

氢氧化铝-氢氧化铁复合吸附剂对海水吸铀量的研究

本文研究了制备Al(OH)_3-Fe(OH)_3复合吸附剂的最佳条件,在常温和一定浓度下吸附剂沉淀终点pH值的选择,以及在同样条件下纯Al(OH)_3纯Fe(OH)_3、与Al(OH)_3-Fe(OH)_3复合吸附剂对海水中吸铀量的比较。这种吸附剂的吸铀量已达到459μg/g,接近同样条件(40—60目通海水15天)下,以TiCl_4为原料制得的TiO_2吸附剂的最高吸附量。     

Seasonal methyltin and (3-dimethylsulphonio)propionate concentrations in leaf tissue of Spartina alterniflora of the Great Bay estuary (NH)

Concentrations of total recoverable inorganic tin (TRISn), monomethyltin (MeSn³⁺), dimethyltin (Me₂Sn²⁺), trimethyltin (Me₃Sn⁺) and (3-dimethylsulphonio)propionate (DMSP) were determined in leaves of Spartina alterniflora from three sites in the Great Bay estuary (NH) from 8 May to 15 September 1989. Total methyltin concentration increased from 8·9 ng g⁻¹ (fresh weight) on 8 May to 472 ng g⁻¹ on 23 May, decreased to 52 ng g⁻¹ on 7 June and 16ng g⁻¹ on 20 June, and remained low until the last sample on 18 September. Statistical calculations showed that methyltin concentrations varied significantly with sampling week, but not with site. DMSP concentrations showed very different behaviour. During the same sampling period DMSP concentrations varied only from 7·5 to 26 μmol g⁻¹ (fresh weight). DMSP concentrations varied significantly for site, but not sampling week.     

一株大西洋深海酵母菌MAR-MC(3)的鉴定及生理特征分析

从大西洋中脊的深海底质中分离到一株酵母菌MAR-MC(3).该菌细胞为卵圆形,单端芽殖;在温度和NaCl浓度分别为35℃、3.4%条件下生长良好;能利用木糖、麦芽糖、半乳糖、蔗糖以及纤维二糖、阿拉伯糖、棉子糖、肌醇、木醇,但不能利用海藻糖;根据表型特征及rDNA序列分析鉴定为季也蒙毕赤酵母(Pichia guilliermondii).     

3-(1-吲哚基)丙酸及其衍生物的合成

介绍了3-(1-吲哚基)丙酸(3a)及其衍生物3-(5-溴-1-吲哚基)丙酸(3b)和3-(5,6-二氯.1-吲哚基)丙酸(3c)的合成方法.首先以3,3'-二硫代二丙酸二甲酯为原料与吲哚、5-溴-1-氢吲哚、5,6-二氯-1-氢吲哚的阴离子进行迈克尔加成反应.再对其碱性条件下进行水解、酸化,得到目标产物3a～3c,收率分别为49.5%,50.8%和35.1%.通过IR,1HNMR对所有化合物的结构进行了表征.     

一种增强型YOLOv3的合成孔径雷达(SAR)舰船检测方法

近年来,海战场成为现代战争的主要作战区域之一,舰船目标逐渐成为海上重点监测对象,能否快速准确地识别海战场舰船目标的战术意图,给指挥员的决策提供必要的支持,这关系到一场海上战役的成败.随着合成孔径雷达(synthetic aperture radar,SAR)成像技术的不断发展,大量SAR图像可用于舰船目标检测与识别.利用SAR图像进行舰船目标检测与识别,已经成为重要的海洋应用之一.针对传统SAR图像舰船检测方法准确率较低的问题,本文在YOLOv3的基础上,结合感受野(receptive field block,RFB)模块,提出一种增强型的SAR舰船检测方法.该方法在最近公开的SAR图像舰船检测数据集上平均准确率值达到了91.50％,与原YOLOv3相比提高了0.92％.实验结果充分表明本文提出的算法在SAR舰船的检测中具有较好的检测效果.     

Application of a 3-D chemical fate prediction model (FATE3D) to predict dioxin concentrations in the Tokyo Bay

A 3-D chemical fate prediction model (FATE3D) was applied to predict the dioxin concentrations in the seawater of Tokyo Bay, Japan. The simulations were carried out for a period of one year (from September 2002 to August 2003). Parameters such as meteorological data, flow field conditions, concentrations and sinking rates of organic particulate matter, initial and boundary conditions, and loading fluxes and physico-chemical properties of dioxins were used as the model inputs.The simulation results compared favorably with the field measurements of dioxin concentrations in the bay for both the particulate and dissolved phases, indicating the validity and predictive capability of the model. Furthermore, the differences in the seasonal cycles and distributions between the particulate- and dissolved-phase dioxins in the bay were estimated from the simulation results.However, the particulate-phase dioxin concentrations in the bottom layers (+1 m from the bottom) were underestimated, probably because the resuspension process was not taken into account in the model. The improvement of the model's predictive capability, including the resuspension process, shall be the focus of our next study.     

3种经济螺体内4种重金属元素含量及评价

以样品湿法消解消化法和火焰原子吸收光谱仪测定大口乳玉螺扁玉螺、亮螺的肌肉、肝脏、性腺3种器官组织中的As、Pb、Cd、Zn等4种金属元素的含量．分析不同种类的螺各器官重金属含量和重金属污染指数,评价各种螺的重金属污染反映其受污染程度和食用价值．结果表明：重金属在不同种类水产品不同组织器官中的分布不同;3种螺都受到了不同程度的重金属污染;3种螺的As都超过了“海洋生物污染评价标准”和“人体消费卫生标准”,其他的3种重金属含量也都不同程度地超过“两个标准”．     

乳糖诱导重组别藻蓝蛋白基因在大肠杆菌中的表达

以重组别藻蓝蛋白表达工程菌JM109（DE3）／pET28-APC作为研究对象，对于JM109（DE3）菌株在乳糖诱导下表达重组蛋白的规律进行了研究。比较分析了不同生长阶段进行诱导，最佳乳糖浓度、诱导持续时间和诱导温度等参数对重组蛋白表达的影响。实验结果表明，采用JM109（DE3）为宿主菌，经过条件优化，乳糖诱导重组蛋白的表达量可以达到IPTG诱导的水平；较低的诱导培养温度能有效提高可溶性重组蛋白的表达。最后在摇瓶发酵结果的基础上，实现了乳糖诱导工程菌的5L全自动发酵罐培养。研究结果为在大肠杆菌大规模发酵中，运用廉价、无毒的乳糖作为诱导剂提供了一定的借鉴。     

Limit analysis approach for accessing stability of three-dimensional (3-D) slopes reinforced with piles

The stabilization of slopes by placing piles is one of the most innovative and effective slope reinforcement techniques in the coastal engineering in recent years. Due to the simplicity and efficiency, limit analysis method is the most common approach for assessing the stability of slopes. However, the majority of existing limit analysis methods is limited to slope without the presence of piles. In this technical note, a novel upper-bound limit analysis method was proposed to access the stability of three-dimensional slopes reinforced with piles incorporating the admissible rotational failure mechanism where toe failure, face failure, and base failure were taken into account. The effects of key designing parameters, e.g., pile location, pile spacing, slope angle, slope width on the stability of earth slopes, and geometry of critical slip surface were presented and discussed. The results demonstrate that the proposed approach is more appropriate for assessing the stability of slopes reinforced with piles and can be also utilized in the design of piles stabilizing the unstable slopes.