3-溴-2-(2′,3′-二溴-4′,5′-二甲氧基苯甲基)-4,5-二甲氧基苯甲酸甲酯的合成及其PTP1B 酶抑制活性研究

为了研究海洋溴系列化合物的生物活性,以香兰素(1)为起始原料,经过溴代、还原、氧化、傅克酰基化及酯化等反应,成功的合成了新化合物3-溴-2-(2′,3′-二溴-4′,5′-二甲氧基苯甲基)-4,5-二甲氧基苯甲酸甲酯(9),总收率为19.6%。通过1H-NMR,13C-NMR等方法对目标产物进行了结构表征。通过比色法对目标化合物进行了PTP1B酶抑制活性测定,结果显示化合物浓度为20 mg/L时,PTP1B酶抑制率为55.84%,表明该化合物有一定的PTP1B酶抑制活性。     

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.     

1,4-蒽醌衍生物的合成

通过高酞酸酐与2-氯-5-甲基-1,4-苯醌反应,经过最长线性步骤6步和3步反应,分别以16%和47%的总产率合成了2个1,4-蒽醌衍生物12和14。其中,化合物14的合成为首次报道。所有合成的化合物均采用核磁共振波谱和质谱方法对其进行了表征和确证,并对高酞酸酐与苯醌反应生成1,4-蒽醌的反应机理进行了探讨。     

四种齐墩果酸皂苷的合成

为获得高活性齐墩果酸皂苷药物候选分子，报道了4种单糖(葡萄糖、半乳糖、木糖、阿拉伯糖)与齐墩果酸的D3羟基进行糖苷化反应合成皂苷的方法。在合成中采用糖的全苯甲酰化三氯乙酰亚胺酯为糖基供体，齐墩果酸烯丙醇酯为糖基受体，在三氟甲磺酸三甲基硅醇酯(TMSOTf)的作用下，糖基供体与齐墩果酸的C-3羟基进行糖苷化，以较高的收率和专一的立体选择性得到4种齐墩果酸单糖皂苷。化合物结构经核磁共振波谱得以确证。     

新型防污剂辣素衍生物的合成、抑菌性及防污性能研究

合成了3种新型含辣素衍生结构的丙烯酰胺衍生物HMOBA、BMA和HMMBA,通过红外光谱(IR)和核磁波谱(1 HNMR)对其结构进行了表征。抑菌性实验证明了合成的化合物对金黄色葡萄球菌和大肠杆菌均有良好的抑制作用,抑菌效果为BMA>HMOBA>HMMBA,其中BMA的对两种菌的最小抑菌浓度均可达0.062 5mg/mL。以合成的化合物为防污剂制备了海洋防污涂料,186d的实海挂板几乎没有附着任何海洋污损生物。     

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,...     

Fe3+胁迫对假微型海链藻中性脂累积及DGAT 表达的影响

二酰甘油酰基转移酶(DGAT)是脂类合成途径中的关键酶,其表达水平的高低影响着脂类含量的高低。微量元素Fe3+对于微藻的生长不可或缺,且影响着微藻中油脂的累积。本实验以假微型海链藻(Thalassiosira pseudonana)为研究对象,分析了铁限制(0.000 03mmol/L)和高铁胁迫(0.3 mmol/L)2种Fe3+胁迫条件下,不同种群生长期中性脂累积及二酰甘油酰基转移酶(DGAT)的基因表达受到的影响。结果显示:铁限制条件下,微藻种群生长及其中性脂的合成受到抑制,DGAT的表达量下降;高铁胁迫条件下,高浓度Fe3+可促进中性脂合成与DGAT的表达,但抑制微藻种群生长。因此,富铁条件下更利于总脂的收集。     

苯并异噻唑啉酮衍生物的合成及其抑菌性能

以1,2-苯并异噻唑-2(3H)-酮为原料合成了其新的衍生物2-(1,2-苯并异噻唑-2(3H)-酮)-乙酰肼和系列N'-(芳基亚甲基)-2-(1,2-苯并异噻唑-2(3H)-酮)-乙酰肼衍生物,目标化合物的结构经元素分析、IR、UV、1HNMR和质谱确证,并对其波谱性质进行了讨论。测试了苯并异噻唑啉酮化合物对5种水生菌大肠杆菌(Escherichia coli)、金黄色葡萄球菌(Staphyloccus aurueus)、溶藻弧菌(Vibrio alginolyticus)、嗜水气单胞菌(Aeromonas hydrophila)、枯草芽孢杆菌(Bacillus subtilis)的抑制活性。结果表明,此类化合物在100×10-6mol/L下抑菌率均达到90%以上,有良好的抑菌活性。     

溴素的有机化学──Ⅴ.溴代脂肪酸—2,3,5,6—四溴—1,4—苯二酯的合成

以1，4—苯二酚和不同的短链脂肪酸为基本原料，经溴代、加成、形成酰卤和酰化等反应，合成了六种新的溴化脂肪酸—2，3，5，6—四溴—1，4—苯二酯。通过对产物的碳、氢、溴等元素的定量分析，以及红外吸收光谱和氢核磁共振谱的研究，验证了化合物的结构。     

壳聚糖磺酸盐表面活性剂的合成、表征及表面性能研究

以环氧氯丙烷、亚硫酸氢钠为原料合成了中间体2-羟基-3-氯丙磺酸钠,在碱性条件下经环氧化反应后与壳聚糖合成了1种易溶于水的壳聚糖磺酸盐表面活性剂,用红外光谱、核磁共振对产物进行了结构表征。分别采用电导率法、吊环法、最大气泡法测试了该产物的临界胶束浓度(CMC)。结果表明:3种方法测得产物的CMC值分别为:2.3×10-4,5.6×10-4和2.5×10-4mol.L-1,吊环法和最大气泡法测得的临界胶束浓度时的表面张力分别为46和48 mN.m-1。     

Microbial Biomass and Organic Nutrients in the Deep-Sea Sediments of the Central Indian Ocean Basin

In order to assess the impact of deep-sea mining on the in situ benthic life, we measured the microbial standing stock and concentration of organic nutrients in the deep-sea sediments of the Central Indian Ocean Basin in the Indian pioneer area. Sediments were collected using box core and grab samples during September 1996. The total bacterial numbers ranged from 10 10 -10 11 cells per g -1 dry weight sediment. There was a marginal decrease in the number of bacteria from surface to 30 cm depth, though the subsurface section registered a higher number than did the surface. The highest numbers were encountered at depths of 4-8 cm. The retrievable number of bacteria were two orders less in comparison with the direct total counts of bacteria. An almost homogeneous distribution of bacteria, total organic carbon, living biomass, and lipids throughout the depth of cores indicates active microbial and benthic processes in the deep sea sediments. On the other hand, a uniform distribution of total counts of bacteria, carbohydrates, and total organic carbon in all the cores indicates their stable nature and suggests that they can serve as useful parameters for long-term monitoring of the area after the benthic disturbance. Further studies on temporal variability in this region would not only verify the observed norms of distribution of these variables but would also help to understand restabilization processes after the simulated benthic disturbance.     

海上大直径钢管桩打桩过程中桩周土强度弱化研究

海上大直径钢管桩打桩过程中,桩周土体受到强烈扰动而发生强度弱化,掌握桩周土体强度弱化规律对于准确预测打桩过程、保证工程安全具有重要意义。为研究土体强度弱化规律,开展了环剪试验模拟打桩对桩周土体的扰动,测试土体强度随剪切速率的变化规律,建立了描述土体强度弱化规律的拟合公式,引入到打桩分析软件中。研究结果表明：土体的强度折减程度不仅与土体本身的性质有关还受到土体的埋深和剪切速率的影响,埋深越深土体强度折减程度越低,剪切速率越高土体强度折减越高,在打桩分析中可采用这里推荐的线性折减方法来模拟不同深度处土体强度的折减规律。     

Geoacoustic Inversion via Genetic Algorithm and Its Application to Manganese Sediment Identification

An acoustic inversion method using a wide-band signal and two near field receivers is proposed and applied to multiple layered seabed models including a manganese sediment. The inversion problem can be formulated into a probabilistic model comprised of signals, a forward model, and additive noise. The forward model simulates wide-band signals, such as chirp signals, and is chosen to be the source-waveletconvolution plane wave modeling method. The wavelet matching technique, using weighted least-squares fitting, estimates the sediment sound-speed and thickness on which determination of the possible numerical ranges for a priori uniform distribution is based. The genetic algorithm is applied to a global optimization problem to find a maximum a posteriori solution for determined a priori search space. Here the object function is defined by an L 2 norm of the difference between measured and modeled signals. Not only the marginal pdf but also its statistics are calculated by numerical evaluation of integrals using the samples selected during importance sampling process of the genetic algorithm.     

Phylogenetic diversity and phenotypic characterization of cultivable bacterioplankton isolated from polar oceans

A set of 27 marine planktonic bacteria isolated from the polar regions was characterized by 16S rDNA sequencing and physiological and biochemical testing. More than half of these bacteria were positive for caseinase, gelatinase and 13-glucosidase, and could utilize glucose, maltose or malic acid as carbon source for cell growth. Twelve isolates expressed nitrate reduction activities. Except for one antarctic isolate BSwlO175 belonging to Actinobacteria phylum, these isolates were classified as γ-Proteobacteria, suggesting that γ-Proteobacteria dominated in cultivable marine bacterioplankton at both poles. Genus Pseudoalteromonas was the predominant group in the Chukchi Sea and the Bering Sea, and genus ShewaneUa dominated in cultivable bacterioplankton in the Prydz Bay. With sequence similarities above 97%, genus Psychrobacter was found at both poles. These 27 isolates were psychrotolerant, and significant 16S rDNA sequence similarities were found not only between arctic and antarctic marine bacteria （ 〉 99% ）, but also between polar marine bacteria and bacteria from other aquatic environments （ ≥ 98.8% ）, including temperate ocean, deep sea, pond and lake, suggesting that in the polar oceans less temperature-sensitive bacteria may be cosmopolitan and have a bipolar, even global, distribution at the species level.     

Deep-Sea Sediment Compression Curves: Some Controlling Factors, Spurious Overconsolidation, Predictions, and Geophysical Reproduction

Oedometer tests have been carried out on 70 undisturbed surficial clays (at approximately 250 mm below the mudline), mostly collected by free-fall corers from sites widely scattered throughout the deep-sea North Atlantic. Acoustic measurements were also made, initially on contiguous samples and ultimately on the same sample using a geophysically instrumented oedometer which also collected electrical resistivity data. Apart from those quiescent areas below the carbonate compensation depth, such as north of the West Indies where very fine clays exist, most of the samples are silty clays whose geotechnical-geophysical properties are dependent on the type of clay minerals present (and their ability to take in moisture), the sand-size fraction, and the quantity of carbonate present. Thus the pure clays have high compressibilities which decrease on the addition of coarse particles, while the converse is true for the acoustic parameters, these increasing with the sand fraction. Using the notion of the intrinsic compression line for all samples, and comparison to it of the measured compression curves, it is clear that, contrary to some previously held ideas, most deep-sea clays are normally consolidated; the addition of carbonate has the effect of creating an open, stronger sediment skeleton. Interestingly, where information is available, the variation with depth of a sample's acoustic velocity follows the void ratio pressure relationship of the compression curve. This allows the construction of an in-situ sediment compression curve using the in-situ geophysical observations.     

INFORMATION FOR AUTHORS

<正>Acta Oceanologica Sinica(AOS)is a comprehensive academic journal edited by the Editorial Committee of Acta Oceanologica Sinica and is designed to provide a forum for important research papers of the marine scientific community which reflect the information on a worldwide basis.The journal publishes scholarly papers on marine science and technology,including physics,chemistry,biology,     

Evaluation of the Risk of Marine Slope Instability: A Pseudo-3D Approach for Application to Large Areas

This article presents a methodology developed to evaluate the instability of submarine slopes that extend over a large area. Special attention was paid to (1) the complex geometry (bathymetry) and the expanse of the slope, (2) the heterogeneity of the sediment, and (3) the distribution of the pore pressure. The safety factor was considered as a spatially varying quantity. The General Formulation (GLE, Fredlund and Krahn 1977), which fully satisfies equilibrium conditions, was used for evaluating the stability of the marine slope. The submarine slope failure, which occurred on 16 October 1979 during the construction of the new Nice airport, was studied in order to test the developed model. Geotechnical parameters were taken from experimental tests carried out by IFREMER on 19 cores extracted at different depths (from 27 m to 1300 m) (Cochonat, Bourillet, and Savoye, 1993; Mulder et al., 1994). Many scenarios were proposed in order to explain the cause of the Nice slope failure (Habib, 1994). In this article, two of those scenarios were tested. Simulation results are presented and discussed.