2,6-Diaryl-4-acylaminopyrimidines as potent and selective adenosine A(2A) antagonists with improved solubility and metabolic stability

In this report, the strategy and outcome of expanding SAR exploration to improve solubility and metabolic stability are discussed. Compound 35 exhibited excellent potency, selectivity over A(1) and improved solubility of >4 mg/mL at pH 8.0. In addition, compound 35 had good metabolic stability with a scaled intrinsic clearance of 3 mL/min/kg (HLM) and demonstrated efficacy in the haloperidol induced catalepsy model.     

HBsAg阴性母亲的新生儿接种不同剂量乙型肝炎血源疫苗的效果

HBsAg阴位母亲的新生儿,按0,1、6月程序分别接种10-10-10μg(1组)、20-10-10μg(2组)和30-10-10μg(3组)乙型肝炎血源疫苗。第一针后一年,检查抗-HBs阳转率,分别为87.60％,90.64％和88.97％,无统计学显著差异。3针10μg组免疫后l～4年抗-HBs阳性率分别为88.31％、81.08％、80.10％和78.39％,虽稍下降,但无统计学显著差异。3个剂量组HBsAg阳性率分别为0.71％,0.49％和0.74％,说明HBsAg阴性母亲的新生儿,用国产血源HBsAg疫苗免疫以10μ×3效果较理想。     

含铬重组液激活部分缺失金属原子簇的钼铁蛋白的研究

棕色固氮菌（Ａｚｏｔｏｂａｃｔｅｒ ｖｉｎｅｌａｎｄｉｉ）固氮酶钼铁蛋白经邻菲口罗啉和Ｏ２ 处理后,变为部分缺失ＦｅＭｏｃｏ 和Ｐ－ｃｌｕｓｔｅｒ的失活蛋白。与由Ｋ２ＣｒＯ４、高柠檬酸铁、Ｎａ２Ｓ和二硫苏糖醇组成的重组液保温后,处理蛋白对乙炔和质子还原的活性都得以显著恢复;然而,它的吸收光谱和圆二色谱虽有明显恢复,但仍与还原钼铁蛋白有所不同。这表明,激活蛋白中也许存在功能与钼铁蛋白相似,而结构则有所差异的含铬（ＣｒＦｅ）蛋白     

A B Functional Gene Cloned from Lily Encodes an Ortholog of <Emphasis Type="BoldItalic">Arabidopsis PISTILLATA</Emphasis> (<Emphasis Type="BoldItalic">PI</Emphasis>)

The classical ABC model proposed for flower development in Arabidopsis and Antirrhinum appropriately sheds light on the biological process of flower development and differentiation and serves in manipulating the floral structure of other important ornamental plants. In this study, LLGLO1, a B functional gene from Lilium longiflorum was isolated and characterized. RT-PCR analysis elucidated that temporal and spatial expression pattern of LLGLO1. This putative gene was strongly expressed in 1, 2, and 3 whorl organs, i.e., outer whorl tepals, inner whorl tepals, and stamens. Genetic effect of LLGLO1 was assayed by ectopic expression in model plant Arabidopsis. Transformed plants showed homeotic transformation of sepals into petaloid sepals in the first whorl, which is similar to the transgenic plants of 35S::PI. So LLGLO1 was one member of GLO/PI sub-family gene to function in flower development.     

High altitude flights by ruddy shelduck Tadorna ferruginea during trans‐Himalayan migrations

Birds that migrate across high altitude mountain ranges are faced with the challenge of maintaining vigorous exercise in environments with limited oxygen. Ruddy shelducks are known to use wintering grounds south of the Tibetan Plateau at sea level and breeding grounds north of Himalayan mountain range. Therefore, it is likely these shelducks are preforming high altitude migrations. In this study we analyse satellite telemetry data collected from 15 ruddy shelduck from two populations wintering south of the Tibetan Plateau from 2007 to 2011. During north and south migrations ruddy shelduck travelled 1481 km (range 548–2671 km) and 1238 km (range 548–2689 km) respectively. We find mean maximum altitudes of birds in flight reached 5590 m (range of means 4755–6800 m) and mean maximum climb rates of 0.45 m s^–1 (range 0.23–0.74 m s^–1). The ruddy shelduck is therefore an extreme high altitude migrant that has likely evolved a range of physiological adaptations in order to complete their migrations.     

粉煤灰基质-草坪砖栽培环境对坪草生长的影响

为了解决停车场、甬路、渠坝与草坪争地的矛盾,增加城市绿地面积,在已研究粉煤灰草坪基质最佳混合比例的基础上,进一步探讨草坪砖作为草坪栽培环境(砖孔内填人粉煤灰混合基质,简称砖孔环境)的肥力效应与生物效应。为了对比分析,特此设置了土孔环境(在土壤中挖取与草坪砖形状和容积相同的孔并填入粉煤灰混合基质)与土灰环境(在粉煤灰混合基质中按照草坪砖孔模式划出同样大小的圈)种植黑麦草作为对照。研究结果表明：坪草N、K、Na、Cu、Zn等含量以砖孔环境最高,土灰环境和土孔环境较低,差异显著,说明砖孔环境能为植物生长提供较多的养分元素;砖孔环境中的坪草含有的Fe、Cu、Zn浓度远高于坪草最佳需求量,今后不再需要补充铁肥、铜肥和锌肥。试验还表明砖孔环境的蒸散率最小,基质含水量最大,基质势最高,持续供水能力强,抗旱效果十分明显。砖孔环境与土孔环境中的草坪草屑累积量差异不显著,但均比土灰环境中的高,且差异显著。夏季高温期砖孔环境中的草坪质量显著高于土孔环境和土灰环境中的草坪质量。     

Characterization of proteins by means of their buffer capacity, measured with an ISFET-based coulometric sensor—actuator system

Proteins form the specific selector in many biochemical sensors. A change in one of the properties of such a protein has to be detected by an appropriate transducer, which completes the biochemical sensor. One of these properties is the buffer capacity of a protein. If the binding of a substance to a protein can significantly change the proton binding, which accounts for the buffer capacity of proteins, the detection of this changed buffer capacity enables the construction of a new type of biosensor.

It will be shown that the buffer capacity can be measured with an ISFET-based sensor—actuator device. The alternating generation of protons and hydroxyl ions by alternating current coulometry at a porous noble metal actuator electrode causes an associated small pH perturbation, which is detected by the underlying pH-sensitive ISFET. The amplitude of the measured signal is a function of the buffer capacity of the solute, in which proteins can be present (or these proteins can be adsorbed in the porous actuator electrode of the device). A model describing the transfer function from the electrical input signal of the actuator to the resulting chemical output, which is subsequently detected by the ISFET pH sensor, is presented. Preliminary results of the measured buffer capacity of ribonuclease and lysozyme are presented.     

南海北部陆坡神狐海域HS-PC500 岩心微生物多样性

[目的]本文研究南海北部陆坡神狐HS-PC500重力活塞岩心沉积物中微生物多样性.[方法]使用吖啶橙染色法计数沉积物中微生物丰度;提取沉积物微生物总DNA,使用特异性引物扩增古菌及细菌16SrRNA基因序列;对克隆文库进行系统发育分析.[结果]系统发育分析显示表层PC500-l(0-5 cm below sea floor,bsf)古菌以C3为主要类群,占该层总序列的25.6%;中层PC500-6(350-355 cm bsf)和底层PC500-11(790-795 cm bsf)古菌以Marine Benthic Group(MBG)-B为主要类群,分别占该层总序列的48.1%和38.9%.另有部分克隆序列属于MBG-A、Miscellaneous Crenarchaeotic Group(MCG)、Thermoprotei、NGC、Halobacteriales、MBG-E、South African Gold Mine Euryarchaeotic Group(SAGMEG).表层细菌以变形菌(Proteobacteria)为主要类群,占该层文库的38.3%.中层和底层细菌以绿弯菌(Choloflexi)和JS1为主要类群,分别占该层文库的28.1%、29.2%和39%、24.7%.另有部分克隆序列属于硝化螺旋菌(Nitrospirae)、放线菌(Actinobacteria)、酸杆菌(Acidobacteria)、OP8、螺旋体菌(Spirochaetes)、TM6、脱铁杆菌(Deferribacteres)、浮霉菌(Plantomycete).[结论]结果显示,HS-PC500岩心微生物丰度与甲烷浓度变化相吻合;微生物丰度较低可能与较低的总有机碳量有关;微生物多样性较高,并且随深度的增加群落结构变化明显;岩心中有关硫酸盐还原的微生物类群占优势,说明微生物的硫代谢在该海区沉积物的物质循环过程中占有重要地位.