Discovery of novel mRNA demethylase FTO inhibitors against esophageal cancer

A series of 1,2,3-triazole analogues as novel fat mass and obesity-associated protein (FTO) inhibitors were synthesised in this study. Among all 1,2,3-triazoles, compound C6 exhibited the most robust inhibition of FTO with an IC₅₀ value of 780 nM. It displayed the potent antiproliferative activity against KYSE-150, KYSE-270, TE-1, KYSE-510, and EC109 cell lines with IC₅₀ value of 2.17, 1.35, 0.95, 4.15, and 0.83 μM, respectively. In addition, C6 arrested the cell cycle at G2 phase against TE-1 and EC109 cells in a concentration-dependent manner. Analysis of cellular mechanisms demonstrated that C6 concentration-dependently regulated epithelial mesenchymal transition (EMT) pathway and PI3K/AKT pathway against TE-1 and EC109 cells. Molecular docking studies that C6 formed important hydrogen-bond interaction with Lys107, Asn110, Tyr108, and Leu109 of FTO. These findings suggested that C6 as a novel FTO inhibitor and orally antitumor agent deserves further investigation to treat esophageal cancer.     

基于地理和气象要素的春玉米生育期栅格化方法

本文以黄河流域春玉米生育期和气象站点气象数据为主要数据源,采用多元逐步回归法分析了各生育期和经度、纬度、海拔高度、降水、年均温、≥10℃积温和日照时数等影响因子的关系,建立逐步回归方程,对各生育期空间栅格化方法进行了探讨,结果表明：（1）生育期空间拟合插值的统计检验说明春玉米“播种期”、“抽雄期”和“收获期”三个时期模拟效果最好,“拔节期”效果精度相对较好;（2）播种期基本满足从西南到东北延后的变化趋势,而拔节期、抽雄期和收获期基本上表现了从南北向中部、中部向东西两侧延后的现象。本研究得到的生育期与地理和气象要素之间的逐步回归方程,可为气候条件变化下作物生育期栅格化模拟试验以及农业生产应该采取的适应机制研究提供一定的依据。     

沙化程度和林龄对湿地松叶片及林下土壤C、N、P化学计量特征影响

为阐明沙化程度和林龄对湿地松(Pinus elliottii)叶片及林下土壤碳(C)、氮(N)、磷(P)化学计量特征影响,探讨C、N、P化学计量比对沙山植被恢复的指示意义,在鄱阳湖多宝沙山沿沙化梯度测定了不同林龄湿地松叶片及林下土壤C、N、P含量。结果表明:1)在叶片C、N、P及其化学计量比中叶N与C∶N对沙化程度和林龄变化反应最为敏感。对于轻度与中度沙化区的5年生与10年生湿地松林,林龄、林龄与沙化程度的交互作用均对叶N及C∶N产生显著影响;对于中度与重度沙化区的2年生和10年生湿地松林,林龄和沙化程度均显著影响叶N与C∶N。2)叶片与土壤二者C、N、P及化学计量比对沙化程度与林龄变化的响应不完全一致。林龄、林龄与沙化程度的交互作用对轻度与中度沙化区5年生和10年生湿地松林土壤全N有显著影响;对于中度与重度沙化区2年生和10年生湿地松林,仅沙化程度对土壤全磷以及林龄对土壤有机碳影响显著。3)10年生湿地松叶片N∶P平均值为20.63,10年生以下湿地松叶片N∶P平均值为15.61,随着林龄的增加,湿地松生长由N、P共同限制逐渐转向更受P的限制。     

凤尾蕨内生真菌的研究Ⅱ——1株产芦丁内生真菌初步研究

报道了从凤尾蕨属井栏边草(Pteris multifida)根状茎中分离出一内生真菌——菌株JJF006,对其形态特征进行了初步研究,并用TLC对该菌株培养物进行了分析。初步结果表明:该真菌液体培养基中含有芦丁成分。     

溶藻弧菌群体基因组学研究

溶藻弧菌(Vibrio alginolyticus)是一种能够对人类以及鱼、虾、贝类等水产品致病的弧菌,给人类健康带来威胁,也给水产养殖业造成巨大的经济损失.目前该物种基于全基因组的遗传多样性和重要遗传元件研究报道较少.本研究对采集自全国4个省份的68株溶藻弧菌进行高通量测序,获得全基因组序列,并结合113株公开发表的...     

Quantitative regulation of the thermal stability of enveloped virus vaccines by surface charge engineering to prevent the self-aggregation of attachment glycoproteins

The development of thermostable vaccines can relieve the bottleneck of existing vaccines caused by thermal instability and subsequent poor efficacy, which is one of the predominant reasons for the millions of deaths caused by vaccine-preventable diseases. Research into the mechanism of viral thermostability may provide strategies for developing thermostable vaccines. Using Newcastle disease virus (NDV) as model, we identified the negative surface charge of attachment glycoprotein as a novel determinant of viral thermostability. It prevented the temperature-induced aggregation of glycoprotein and subsequent detachment from virion surface. Then structural stability of virion surface was improved and virus could bind to and infect cells efficiently after heat-treatment. Employing the approach of surface charge engineering, thermal stability of NDV and influenza A virus (IAV) vaccines was successfully improved. The increase in the level of vaccine thermal stability was determined by the value-added in the negative surface charge of the attachment glycoprotein. The engineered live and inactivated vaccines could be used efficiently after storage at 37°C for at least 10 and 60 days, respectively. Thus, our results revealed a novel surface-charge-mediated link between HN protein and NDV thermostability, which could be used to design thermal stable NDV and IAV vaccines rationally.     

基于遥感和GIS的川西绿被时空变化研究

探索出了利用多时相MODIS数据分析绿被时空变化的技术方法,揭示出了川西2002—2008年间绿被的变化特征。建立了绿被提取模型。用其从2002—2008年的多期MODIS影像中提取出川西多期绿被数据。其次,利用GIS技术对2002—2008年间绿被变化,及其与温度、降雨的关系等进行了分析。研究表明:2002年绿被天数在195 d以上的区域有43.3%。终年无绿被的区域有4.3%。西北部植被生长日数短,而东南部生长日数长。2002—2008年间,春季绿被面积变幅最大,秋季最小。最大绿被面积出现在2006年的夏季,最小绿被面积出现在2005年的冬季。平均夏冬绿被面积差占区域面积46.7%。在季节上,绿被面积与温度和降雨量均在0.01的水平上呈显著正相关关系,其相关系数分别为0.82和0.84。该研究成果对植被生长潜力挖掘、农牧生产和生态建设决策等均有重要意义。     

Protein kinase C delta null mice exhibit structural alterations in articular surface,intra-articular and subchondral compartments

IntroductionStructural alterations in intra-articular and subchondral compartments are hallmarks of osteoarthritis, a degenerative disease that causes pain and disability in the aging population. Protein kinase C delta (PKC-δ) plays versatile functions in cell growth and differentiation, but its role in the articular cartilage and subchondral bone is not known.MethodsHistological analysis including alcian blue, safranin O staining and fluorochrome labeling were used to reveal structural alterations at the articular cartilage surface and bone–cartilage interface in PKC-δ knockout (KO) mice. The morphology and organization of chondrocytes were studied using confocal microscopy. Glycosaminoglycan content was studied by micromass culture of chondrocytes of PKC-δ KO mice.ResultsWe uncovered atypical structural demarcation between articular cartilage and subchondral bone of PKC-δ KO mice. Histology analyses revealed a thickening of the articular cartilage and calcified bone–cartilage interface, and decreased safranin O staining accompanied by an increase in the number of hypertrophic chondrocytes in the articular cartilage of PKC-δ KO mice. Interestingly, loss of demarcation between articular cartilage and bone was concomitant with irregular chondrocyte morphology and arrangement. Consistently, in vivo calcein labeling assay showed an increased intensity of calcein labeling in the interface of the growth plate and metaphysis in PKC-δ KO mice. Furthermore, in vitro culture of chondrocyte micromass showed a decreased alcian blue staining of chondrocyte micromass in the PKC-δ KO mice, indicative of a reduced level of glycosaminoglycan production.ConclusionsOur data imply a role for PKC-δ in the osteochondral plasticity of the interface between articular cartilage and the osteochondral junction.

Electronic supplementary material

The online version of this article (doi:10.1186/s13075-015-0720-4) contains supplementary material, which is available to authorized users.     

Kosteletzkya virginica, a halophytic species with potential for agroecotechnology in Jiangsu Province, China

Kosteletzkya virginica (L.) Presl. is a perennial dicot halophytic species, that grows in brackish portions of coastal tidal marshes of the mid-Atlantic and southeastern United States. New saline mudflats have been increasing every year in Northern Jiangsu, China. In 1993, we introduced K. virginica (L.) into China from the Halophyte Biotechnology Center (University of Delaware, USA) as a potential species to improve the soil and develop ecologically sound saline agriculture. Our nearly 10 years of experimental research, both in a test garden and in the field, indicated that K. virginica adapts excellently to the heavy saline soils of Jiangsu Province, China. The average seed yield of K. virginica in 2001 at Yancheng was 638 kg/ha from 1-year old seedlings. There were significant variations among individuals from the unselected population of K. virginica on growth, quality, and seed yield traits. There is great potential to increase the seed yield if superior clones are selected. The seed yield of 35 selected individuals was six times greater than that of the average. Four growth traits of K. virginica were found to have a significant correlation with seed yield. However, there was no strong positive or negative correlation among seed quality traits. The mean seed weight and the germination ratio of the 35 selected individuals of K. virginica were 16.36±0.32 g and 76.11±1.82%, respectively. The percentage content of oil and crude protein in the seeds was 11.28±0.67 and 8.17±0.19%, respectively. The percentage of seed vigor of the selected individuals was 99%, as determined by soft X-ray radiography.