四种卤代PTP1B抑制剂的化学合成及其活性研究

从松节藻中分离的含卤素化合物表现出显著PTP1B抑制活性。其中BPN效果最佳。为研究BPN侧链基团极性对其抑制活性的影响,本文以香兰素(1)为起始原料,经过溴代、氧化、还原、傅克烷基化以及酯化等反应,成功合成了新化合物2,3-二溴-1-(2-溴-3,4-二甲氧基-6-((4-硝基苯氧基)甲基)苯甲基)-4,5-二甲氧基苯(10)、4-((3-溴-2-(2,3-二溴-4,5-二甲氧基苄基)-4,5-二甲氧基苄基)醚)苯胺(11)、4-((3-溴-2-(2,3-二溴-4,5-二甲氧基苄基)-4,5-二甲氧基苄基)醚)-4-乙酰乙酸(12)和3-溴-2-(2,3-二溴-4,5-二甲氧基苄基)-4,5-二甲氧基苯甲醛肟(14)。通过1 H-NMR,13C-NMR等方法对目标产物进行了结构表征。并对化合物进行了PTP1B酶抑制活性的测定,结果表明化合物侧链极性对PTP1B酶抑制活性有显著影响。     

凡纳滨对虾(Litopenaeus Vannamei)高位池养殖中几个单项因子试验

在高位池养殖凡纳滨对虾中,分别采用150×104尾/ha、135×104尾/ha、135×104尾/ha、120×104尾/ha、113×104尾/ha、105×104尾/ha、90×104尾/ha的放养密度。经过120d的的饲养,结果表明:在相同的养殖条件下,随着放养密度的增加,水中亚硝酸氮、氨氮的含量也相应增加;产量虽有所提高,但对虾生长缓慢。波吉卵囊藻可降低水中亚硝酸氮、氨氮的含量,增加溶解氧;养殖后期,保持1.5m的水深较为适宜。     

马氏珠母贝水通道蛋白基因AQP4 cDNA克隆和表达分析

水通道蛋白4(aquaporin4, AQP4)是一类被动运输水的通道蛋白。本研究根据转录组测序获得的马氏珠母贝AQP4片段, 采用RACE技术获得了AQP4的全长cDNA, 命名为PfAQP4, 其5′非翻译区(untranslated region, UTR)为114bp, 3′UTR为839bp, 开放阅读框(open reading frame, ORF)为858bp, 编码285个氨基酸。PfAQP4含有6个α螺旋跨膜区、5个环、1个主要内嵌蛋白(major intrinsic protein, MIP)结构域、2个NPA(Asn-Pro-Ala)基序, 属于AQP1-like型。利用qPCR技术分析PfAQP4在不同组织、不同发育时期以及盐度胁迫条件下的mRNA表达模式。结果显示: (1) PfAQP4在所有被检测组织中均表达, 其中在闭壳肌、足和鳃中表达量较高; (2) PfAQP4在不同的发育时期均有表达, 其表达量整体呈现先升高后降低的趋势, 其中在2—4细胞期表达量最高, 在眼点幼虫期表达量最低; (3) 在高盐度组(36‰)盐度胁迫24、72、120h后, PfAQP4表达量显著上升, 在168h降至对照组水平; 在低盐(16‰)组, PfAQP4表达量在24h显著上调, 在72h恢复至对照组水平, 说明盐度影响鳃组织中PfAQP4的表达量, 也表明PfAQP4在马氏珠母贝渗透压调节中起着非常重要的作用。     

Study and application of an improved four-dimensional variational assimilation system based on the physical-space statistical analysis for the South China Sea

The four-dimensional variational assimilation (4D-Var) has been widely used in meteorological and oceanographic data assimilation. This method is usually implemented in the model space, known as primal approach (P4D-Var). Alternatively, physical space analysis system (4D-PSAS) is proposed to reduce the computation cost, in which the 4D-Var problem is solved in physical space (i.e., observation space). In this study, the conjugate gradient (CG) algorithm, implemented in the 4D-PSAS system is evaluated and it is found that the non-monotonic change of the gradient norm of 4D-PSAS cost function causes artificial oscillations of cost function in the iteration process. The reason of non-monotonic variation of gradient norm in 4D-PSAS is then analyzed. In order to overcome the non-monotonic variation of gradient norm, a new algorithm, Minimum Residual (MINRES) algorithm, is implemented in the process of assimilation iteration in this study. Our experimental results show that the improved 4D-PSAS with the MINRES algorithm guarantees the monotonic reduction of gradient norm of cost function, greatly improves the convergence properties of 4D-PSAS as well, and significantly restrains the numerical noises associated with the traditional 4D-PSAS system.     

胶州湾及周边海域大气和海水中N_2O和CH_4的分布及海气交换通量

分别于2006年8月,12月和2007年4月,10月采集胶州湾及周边海域大气和海水样品,对氧化亚氮(N2O)和甲烷(CH4)浓度进行了测定,并设置1个连续站进行24 h连续观测.结果表明:大气中N2O春、夏、秋、冬的平均浓度(体积分数)分别为(3.17±0.03)×10-7,(3.24±0.15)×10-7,(3.19±0.02)×10-7和(3.08±0.25)×10-7;大气中CH4春、夏、秋、冬的平均浓度(体积分数)分别为(1.89±0.04)×10-6,(1.79±0.04)×10-6,(2.09±0.21)×10-6和(2.01±0.09)×10-6.胶州湾表、底层海水中N2O和CH4的浓度和饱和度表现出明显的季节变化,其中N2O浓度和饱和度冬季最高,春、秋季次之,夏季最低;CH4浓度和饱和度夏季最高,冬季最低.利用Liss and Merlivat(1986)公式和Wanninkhof(1992)公式估算出胶州湾海域N2O的年平均海-气交换通量分别为(11.16±14.15)和(22.42±27.56)μmol m-2·d-1;CH4分别为(7.75±6.19)和(17.76±14.84)μmol m-2·d-1.胶州湾大部分海域表层海水中N2O和CH4呈过饱和状态,是大气中N2O和CH4的净源.     

抗鳗弧菌单克隆抗体免疫保护作用的实验研究

本文对鳗弧菌感染牙鲆幼鱼为动物模型,对我们制备的五株抗鳗弧菌单抗４Ａ６,３Ｂ２,４Ｅ１２,３Ｅ７,３Ａ４的免疫保护效果进行了研究,结果表明：４Ａ６,３Ｂ２和４Ｅ１２具有明显提高受５ＬＤ＾５０鳗弧菌感染的牙鲆存活率的作用,同时它们还可明显延长受大齐量鳗弧菌（１０ＬＤ＾５０）感染的牙鲆的平均存活时间,揭示：４Ａ６,３Ｂ２和４Ｅ１２具有中和或减弱鳗弧菌毒性的作用。     

溴素的有机化学 Ⅳ．单取代苯甲酸多溴代芳酯的合成

报导合成了四种新的单取代苯甲酸多溴代芳酯：４－溴苯甲酸－２＇，４＇，６＇－三溴苯酯，双（４－溴苯甲酸）－２＇，３＇，５＇，６＇－四溴－１＇，４＇－苯二酯，双（４－羟基苯甲酸）－２＇，３＇５＇，６＇－四溴－１＇，４＇－苯二酯和双（２－羟基苯甲酸）－２＇，３＇，５＇，６＇－四溴－１＇，４＇－苯二酯。     

Storm surge simulation along the Meghna estuarine area: an alternative approach

In this study, numerical prediction of surges associated with a storm was made through the method of lines (MOL) in coordination with the newly proposed RKARMS (4, 4) method for the meghna estuarine region, along the coast of Bangladesh. For this purpose, the vertically integrated shallow water equations (SWEs) in Cartesian coordinates were firstly transformed into ordinary differential equations (ODEs) of initial valued, which were then soloved using the new RKARMS (4, 4) method. Nested grid technique was employed for resolving the complexities of the region of interest with minimum cost. Fresh water discharge through the lower Meghna River was taken into account along the north east corner of the innermost child scheme. Numerical experiments were performed with the severe cyclone on April 1991 that crossed the coast over the study area. Simulated results by the study were found to be in good agreement with some reported data and were found to compare well with the results obtained by the MOL in addition with the classical 4th order Runge-Kutta (RK (4, 4)) method and the standard finite difference method (FDM).     

4-tert-octylphenol and 17beta-estradiol applied by feeding to flounder Platichthys flesus: induction of vitellogenin and accumulation in tissues

In order to simulate a possible natural administration route of xenoestrogens male flounder Platichthys flesus were exposed via the diet to the alkylphenol 4-tert-octylphenol. Treatment with 4-tert-octylphenol (10, 50 and 100 mg OP kg(-1) BW) or 17beta-estradiol (0.05 mg kg(-1) BW) every second day during a period of 11 days resulted in a significant increase in plasma vitellogenin (Vtg) concentrations. The induction of Vtg was greatest in the fish receiving 50 mg OP kg-' BW. A significant accumulation of 4-tert-octylphenol was found in liver and muscle tissue of the OP treated groups. The tissue concentrations of 4-tert-octylphenol and the plasma vitellogenin concentration were positively correlated. The results show that 4-tert-octylphenol accumulates in liver and muscles of flounder P. flesus, and exerts estrogenic effects such as vitellogenin induction.     

Preformed Cd and PO4 and the relationship between the two elements in the northwestern Pacific and the Okhotsk Sea

Preformed Cd and PO₄ were investigated in the northwestern Pacific (Station CM05) and the Okhotsk Sea (Station CM06), and the relationship between the two elements was examined. At CM05, from the apparent oxygen utilization (AOU)–Cd and PO₄ plot, the different molecular ratios of consumed O₂ to regenerated Cd and PO₄ were calculated to be 254,000 (Cd) and 96 (PO₄) for the shallow layer (30–99 m) and 613,000 (Cd) and 170 (PO₄) for the deep layer (below the oxygen minimum layer), which suggested the preferential remineralization of Cd and PO₄ in the shallow layer. At CM06, regeneration ratios of O₂/Cd, PO₄ were obtained only in the shallow layer (29–124 m) as 227,000 (Cd) and 75 (PO₄). The calculated preformed Cd and PO₄ concentrations in the shallow layer were 0.59 nM of Cd and 1.6 μM of PO₄ at CM05 and 0.35 nM of Cd and 0.95 μM of PO₄ at CM06. These concentrations were much higher than those (close to 0) in the low-latitude area, which was attributable to the supply of these constituents from deep water by the strong winter convection. In the deep layer, at CM05, preformed concentrations were 0.64 nM of Cd and 1.4 μM of PO₄. Preformed PO₄ generally agreed with previously reported values in the Pacific, which suggested that the concentrations of the initial PO₄ in the deep water were preserved as preformed through the movement to the northwestern Pacific. On the other hand, obtained preformed Cd in the northwestern Pacific deep water showed a somewhat higher value than that in the southwest Pacific. The possibility of the terrestrial input and remineralization of Cd by CaCO₃ dissolution during the northward movement was considered. A plot of Cd and PO₄ showed a linear relationship with slopes of 0.34 and 0.40 (nM/μM) at CM05 and CM06, respectively, which generally agreed with the reported values in the North Pacific.     

The Regional Ocean Modeling System (ROMS) 4-dimensional variational data assimilation systems: Part I - System overview and formulation

The Regional Ocean Modeling System (ROMS) is one of the few community ocean general circulation models for which a 4-dimensional variational data assimilation (4D-Var) capability has been developed. The ROMS 4D-Var capability is unique in that three variants of 4D-Var are supported: a primal formulation of incremental strong constraint 4D-Var (I4D-Var), a dual formulation based on a physical-space statistical analysis system (4D-PSAS), and a dual formulation representer-based variant of 4D-Var (R4D-Var). In each case, ROMS is used in conjunction with available observations to identify a best estimate of the ocean circulation based on a set of a priori hypotheses about errors in the initial conditions, boundary conditions, surface forcing, and errors in the model in the case of 4D-PSAS and R4D-Var. In the primal formulation of I4D-Var the search for the best circulation estimate is performed in the full space of the model control vector, while for the dual formulations of 4D-PSAS and R4D-Var only the sub-space of linear functions of the model state vector spanned by the observations (i.e. the dual space) is searched. In oceanographic applications, the number of observations is typically much less than the dimension of the model control vector, so there are clear advantages to limiting the search to the space spanned by the observations. In the case of 4D-PSAS and R4D-Var, the strong constraint assumption (i.e. that the model is error free) can be relaxed leading to the so-called weak constraint formulation. This paper describes the three aforementioned variants of 4D-Var as they are implemented in ROMS. Critical components that are common to each approach are conjugate gradient descent, preconditioning, and error covariance models, which are also described. Finally, several powerful 4D-Var diagnostic tools are discussed, namely computation of posterior errors, eigenvector analysis of the posterior error covariance, observation impact, and observation sensitivity.     

海南东部沿岸河流和潟湖中溶存甲烷的分布及通量

甲烷(CH4)作为大气中重要的温室气体,直接或间接地影响全球气候变化。于2009年3月27日至4月15日对海南东部河流(文昌河、文教河、万泉河)、潟湖(八门湾、博鳌、小海和老爷海)等进行了调查,采集了表层和部分底层水样,对溶解CH4浓度进行了测定并初步估算了其水-气交换通量。结果表明,文昌河、文教河受人为活动影响较大,表层CH4饱和度较高,分别为(60664±25118)%、(38582±26339)%,污水输入、红树林输入和现场产生是其CH4的主要来源。万泉河表层CH4饱和度为(9472±5594)%,现场产生是其水体溶存CH4的主要源。八门湾、博鳌、小海和老爷海潟湖表层水体溶存CH4均处于过饱和状态,但其饱和度远小于入湖河流,分别为(2471±2937)%、(5692±3435)%、(546±251)%和(6878±4635)%,其中河流输入、地下水和红树林间隙水输入、现场产生是潟湖中CH4的主要来源,水体中CH4的氧化和水-气交换是潟湖中CH4的主要汇。初步估算出文昌河和万泉河CH4的水-气交换通量分别为5967.0±5142.1和496.2±335.9μmol·m 2·d 1,八门湾、博鳌、小海和老爷海潟湖的水-气交换通量分别为528.7±625.0、441.7±473.3、26.6±21.6和1287.8±1453.3μmol·m 2·d 1。海南东部河流、潟湖是近岸水体及大气CH4的净源。     

苯并（a）芘诱导下岩虫CYP基因的表达特征

Rapid amplification of cDNA ends(RACE) and real-time polymerase chain reaction(RT-PCR) were carried out to analyze the CYP4 gene expression in polychaete Marphysa sanguinea exposed to benzo[a]pyrene(BaP) in this study. The full length of MsCYP4 cDNA was 2 470 bp, and it encoded 512 amino acids. The deduced amino acid sequence showed 47% identity with CYP4 F from frog Xenopus tropicalis and shared high homology with other known CYP4 sequences. To analyse the role of CYP4 in protecting M. sanguinea from BaP exposure, three BaP groups were established: 0.5, 5 and 50 μg/L. Polychaetes were sampled after 3, 7 and 12 d. At 0.5 μg/L, the effect of BaP on MsCYP4 gene expression increased with time prolonged. MsCYP4 gene expression curve showed Ushaped trend with time in 5 and 50 μg/L BaP groups. Therefore, MsCYP4 gene may play an important role in maintaining the balance of cellular metabolism and protecting M. sanguinea from BaP toxicity.     

Effects of three fungicides alone and in combination on glutathione S-transferase activity (GST) and cytochrome P-450 (CYP 1A1) in the liver and gill of brown trout (Salmo trutta)

In order to evaluate the gill glutathione S-transferase (GST) activity as a biomarker of effect of fungicide exposure in juvenile brown trout (Salmo trutta), the fungicides propiconazole [(R,S)-1-[2-(2,4-diclophenyl)-4-propyl-1,3-dioolan-2-ylmetyl]-1H-1,2,4-triazole] and fenpropimorph [(+/-)-cis-4-[3-(4-tert-butylphenyl)-2-metyl propyl]-2,6 dimetylmorfolinc] were administrated in the water separately and together in a static system (80 microg/l for each pesticide) for 5 days. The combined fungicides gave a significant decrease in gill GST activity towards 1-chloro-2,4-dinitrobenzene (CDNB), whilst hepatic GST-activity was not significantly changed. Furthermore, continuous exposure to 540 ug/l thiabendazole[2-(thiazol-4'-yl)benzimidazole] in a flow-through system for 4 days significantly increased the gill glutathione S-transferase (GST) activity towards CDNB, whilst hepatic GST and cytochrome P450 (CYP 1A) activities were not increased by the treatment.     

温度和盐度对短节硬毛藻(Chaetomorpha brachygona Harvey)生长发育的影响研究

利用双因素实验和单藻培养等方法,对采自广东南澳岛的短节硬毛藻(Chaetomorpha brachygona Harvey)进行研究,在不同温度和盐度条件下,对该硬毛藻的生长、活力以及形态进行了观察与测定。结果表明,温度和盐度对短节硬毛藻的生长均有一定影响,当温度为20°C时,藻体培养第3、6和12天活力分别为0.70—0.75Y、0.60—0.70Y和0.55—0.65Y,培养12天时藻体有生殖细胞形成,此温度有利于藻体维持活力;温度为25—30°C时,培养第3天时会大量形成生殖细胞;在盐度10、20、40和50时,藻体的生长与温度相关,即30°C25°C20°C;在盐度20—30时,藻体长度最大达4.55 cm;在盐度10—30时,更有利于藻体生长,整体趋势为2030104050。因此,实验条件下,温度25—30°C、盐度10—30更利于短节硬毛藻的生长和形成生殖细胞。本实验表明,短节硬毛藻为暖水、广盐性种,有可能在我国南方海区大量生长并扩散,具有引发绿潮的潜力。     

海洋沉积物孔隙水中阴阳离子含量的离子色谱法分析方法

分别采用Metrosep A Supp4-250型阴离子柱和Metrosep C 2-150型阳离子柱,以1.8 mmol/L Na2CO3 1.7 mmol/L NaHCO3和4 mmol/L酒石酸 0.75 mmol/L吡啶二羧酸为阴阳离子淋洗液,用离子色谱仪来测定海洋沉积物孔隙水中阴离子Cl-、Br-和SO42-浓度和阳离子Na 、NH4 、K 、Ca2 、Mg2 的浓度。特别是针对高Cl-和高Na 背景下Br-和NH4 的测定做了专门分析,得到了较理想的结果,建立了一套离子色谱法测定海洋沉积物孔隙水中常见的阴阳离子含量的实验方法。     

南海北部海洋四维变分同化试验研究

为了研究四维变分同化方法在南海北部海洋数值预报中的适用性,使用海洋区域模式(ROMS),建立了南海北部海洋资料四维变分同化系统,进行了温盐廓线和海面温度数据同化试验,初步对比分析了三种四维变分实现方法的同化效果。研究结果表明,四维变分同化方法具有较好的同化效果,其中,增量强约束方法(I4DVar)具有较好的稳定性,其稳定性高于4DPSAS和R4DVar。本文研究成果为建立南海业务化海洋四维变分同化及预报系统奠定技术基础。     

胶州湾大肠菌群丰度变化及对环境污染的指示

采用MPN计数法对胶州湾大肠菌群丰度进行7年（84个月）连续监测,结果表明,大肠菌群丰度的周年变化明显,全年最高丰度与最低丰度相差约2.2倍。胶州湾大肠菌群丰度自2005—2009年明显下降,降幅达67%,说明胶州湾环境质量有所好转。研究还发现大肠菌群丰度变化具有明显的区域特征,河口区最高,湾内区最低,差异近11倍。大...     

Metabolism and mutagenicity of 4-nitroquinoline N-oxide by microsomes and cytosol of digestive gland of the mussel Mytilus edulis L.

The modulation of the mutagenicity of 4-nitroquinoline N-oxide (4-NQO) by M. edulis digestive gland cytosolic and microsomal fractions was studied by monitoring the induction of the umu operon by 4-NQO in Salmonella typhimurium 1535/pSK1002. The mutagenicity of 4-NQO was increased by M. edulis cytosol and microsomes in dose-dependent manner with respect to protein and toxicant concentration. The mutagenic enhancement reflected increased NAD(P)H-dependent oxygen consumption by microsomes in the presence of 4-NQO and enhanced nitroreductase activity in cytosol. The former was stimulated by azide, indicating 4-NQO-enhanced oxyradical production by microsomes, and the latter was inhibitable by dicoumarol, indicating involvement of DT-diaphorase in nitroreduction by M. edulis cytosol. Neither dicoumarol nor allopurinol (inhibitors of DT-diaphorase and xanthine oxidase, respectively) affected the enhanced mutagenic expression of 4-NQO by cytosol. The results support the possibility of oxidative stress as a pollution-mediated mechanism of toxicity.     

胶州湾营养盐的现状和变化

报道了１９９１年５月至１９９４年２月１２个航次胶州湾ＮＯ３－Ｎ，ＮＯ２－Ｎ，ＮＨ４－Ｎ，ＰＯ４－Ｐ和ＳｉＯ３－Ｓｉ的时空分布基本特征，６０年代于至９０年代的变化表明，胶州湾营养盐的浓度和分布已发生显变化。尤其从６０年代至８０年代，３０年来，胶州湾中东部水城ＰＯ４－Ｐ，ＮＯ３－Ｎ和ＮＨ４－Ｎ浓度分别增加２．２，７．３和７．１倍，ＴＯＮ浓度也增加了３．５倍，ＴＩＮ／ＰＯ４－Ｐ从１０增加至２４．２；Ｔ