GPCRs 组成性活性的研究进展及意义

GPCRs是体内最大的蛋白质亚家族,其活性涉及体内绝大部分重要的生理和病理进程。研究表明,GPCRs或其突变体能在无配体结合的情况下自发产生部分甚至完全活性程度的生理活性,称之为组成性活性。据此研究者提出了GPCRs激活过程中存在多个中间激活态的观点,从而丰富了配体受体相互作用的经典模型,并使组成性活性突变体(constitutive active mutant,CAM)成为研究GPCRs的新方法。本文系统介绍了组成性活性的研究历程,以及近年来利用CAM的方法研究GPCRs的结构、激活机制和活性调节的历程和进展,和体内组成性活性突变的成因和与疾病的关系,以及CAM在研究药物作用机理和新药研发中的意义。     

新乡市水源地土壤重金属含量特征及其对地下水的影响

对新乡市自来水水源地土壤和地下水重金属含量特征进行分析,结果表明:土壤中Pb含量达标,Zn、Cr、Ni和Cu含量超标,其平均含量分别为1213.80、115.22、189.56和60.39mg.kg-1;用化学连续浸提法对超标元素化学形态分布进行研究表明,Zn、Cr、Ni和Cu残渣态含量最高,所占比例分别为87.81%、78.38%、84.26%和59.33%,可交换态含量最低,所占比例分别为0.21%、2.56%、1.00%和3.51%,由于Zn、Cr、Ni、Cu主要以迁移性最弱的残渣态为主,未发现地下水中重金属含量超标。     

The role of the pro-apoptotic protein Siva in the pathogenesis of Familial Mediterranean fever: A structural and functional analysis

Familial Mediterranean fever (FMF) is an autosomal, recessive disease, attributed to mutations in MEFV gene encoding pyrin, which is characterized by recurrent, acute and self-limiting attacks of fever as well as an increased neutrophil and monocyte apoptosis. Most disease-associated mutations in MEFV gene reside on the C-terminal PRYSPRY (B30.2) domain of pyrin, an area found to interact with the pro-apoptotic protein Siva. Because apoptotic events may be contributing to endogenous inflammation we hypothesized that mutations in pyrin may affect Siva-mediated apoptosis. The confirmation of this hypothesis would be of a great biological significance since it would be demonstrated a connection between apoptosis and inflammation. We used homology modeling to construct a 3-D model of Siva protein and the constructed model of Siva defined structural elements with potential of binding other proteins to induce apoptosis. Given that Siva protein binds pyrin as shown by transfection and immunoprecipitation experiments, apoptosis was assessed by FACS and Western blotting. No differences in rates of apoptosis in myeloid cells (THP-1) upon transfection with either wt pyrin or mutant forms of pyrin were found. Patients with FMF did not display any mutations in the Siva-1 (full length) gene. Siva-1 was not linked to pyrin in the major predicted FMF gene network constructed using a literature-curated gene signature for FMF. These results suggest that Siva-mediated unprovoked apoptosis is not likely to be involved in the pathogenesis of FMF.     

湖北大戟根中的环阿尔廷型三萜

从湖北神农架地区产湖北大戟(Euphorbia hylonomaHand.-Mazz.)根中分离得到4个环阿尔廷型三萜化合物,分别鉴定为:24-烯环阿尔廷软脂酸酯(1),环阿尔廷-23-烯-3β,25-二醇-3-乙酸酯(2),环阿尔廷-25-烯-3β,24ξ-二醇(3),环阿尔廷-23-烯-3β,25,28-三醇(4)。化合物1~4均为首次从该植物中得到。     

升温对超富营养型浅水湖泊沉积物营养盐动态迁移的影响

在实验室控制条件下,以超富营养型浅水湖泊——武汉南湖表层沉积物和表层水为研究对象,设置18℃和22.5℃两个温度处理组,模拟武汉地区预测的21世纪末春季变暖的情景,研究升温对沉积物营养盐释放的影响。实验结果表明:整个实验过程中,22.5℃处理组水体中正磷酸盐(o-P)和总磷(TP)含量显著高于18℃处理组,说明气温升高可以显著促进富营养化浅水湖泊沉积物磷的释放,促进水体中磷含量的显著升高;此外,在实验的初始阶段,升温能够加速水体中氨氮(NH+4-N)向硝态氮(NO-3-N)转化的过程,同时水体与沉积物中氮含量的下降可能是水体与沉积物中的氮通过反硝化作用从系统中溢出以及被系统中的底栖生物利用所致,没有观察到气温升高对沉积物中总氮的释放产生显著影响。     

Leaf morphology and anatomy of Camellia section Camellia (Theaceae)

The delimitations of species in Camellia section Camellia have been disputed for many years, resulting from uncertain relationships among species. Leaf morphological and anatomical characters for 54 species and three varieties in this section were investigated to reveal the relationships. Principal component analysis and cluster analysis were conducted using the transformed data for quantitative and qualitative characters from leaf morphology and anatomy. Combining the results of statistical analysis with comparative leaf characters of morphology and anatomy, we discussed the taxonomic treatment of section Camellia by Chang compared with that of Ming and we conclude that section Camellia consists of c. 50 species. © 2009 The Linnean Society of London, Botanical Journal of the Linnean Society, 2009, 159 , 456–476.     

纳米载药系统在肿瘤多药耐药中的应用

当今世界,肿瘤已经成为威胁人类健康的重大疾病。在肿瘤疾病中,化疗可控制肿瘤的生长和转移,增强放疗的疗效,是治疗肿瘤疾病的主要手段之一。而肿瘤多药耐药是影响化疗药物疗效、引起化疗失败的重要原因,影响肿瘤患者的治愈效果,降低生存率。如何提高化疗的疗效,延长肿瘤患者的寿命成为医学界的难题。纳米载药系统是生物医学领域研究的热点,相对于单一药物,纳米载药体现了许多优越性,具有良好的应用前景。纳米级颗粒更有利于药代动力学,这些纳米载药颗粒通过被动和主动的机制表现出在全身血液循环寿命延长,持续的药物释放动力,使其能更好的在肿瘤细胞中积累而发挥作用,提高化疗的疗效。本文综述了肿瘤多药耐药研究中主要的纳米载体以及它们在逆转多药耐药方面的应用,并展望载药系统的有更多更好的发展趋势。     

广东顺德生态乐园夏季鸟类资源和保护

报道了顺德生态乐园夏季鸟类资源的调查 ,记录了该乐园鸟类有 55种 ,隶属 6目2 0科 ,其中属国家二级重点保护鸟类 9种。对鸟类的生态作用、种类和组成作了讨论 ,并提出了保护鸟类的重要性和保护措施。     

Insulin-mediated suppression of apolipoprotein B mRNA translation requires the 5' UTR and is characterized by decreased binding of an insulin-sensitive 110-kDa 5' UTR RNA-binding protein

Insulin has been shown to acutely regulate hepatic apolipoprotein B (apoB) secretion at both translational and post-translational levels; however, mechanisms of apoB mRNA translational control are largely unknown. Recent studies of apoB untranslated regions (UTRs) revealed a potentially important role for cis-trans interactions at the 5' and 3' UTRs. In the present paper, deletion constructs of the UTR regions of apoB revealed that the 5' UTR was necessary and sufficient for insulin to inhibit synthesis of apoB15. Metabolic radiolabeling and in vitro translation experiments in the presence of protease inhibitors confirmed that the effect of insulin on the apoB 5' UTR was translational in nature. Using the nondenaturing electrophoretic mobility shift assay (EMSA), protein-RNA complexes were detected binding to the apoB 5' and 3' UTRs. Denaturing EMSA identified a 110-kDa protein interacting at the 5' UTR. Nondenaturing EMSA determined that insulin altered binding of large protein complexes to the 5' UTR. Binding specificity was determined by competition with both specific and nonspecific competitors. Insulin treatment decreased binding of the 110-kDa protein to the 5' UTR as visualized by EMSA. Absence of insulin increased binding of this trans-acting factor to the 5' UTR by 2-fold. Analysis of the 3' UTR showed no significant insulin-mediated changes in binding of trans-acting factors. We thus propose the existence of a novel RNA-binding insulin-sensitive factor that binds to the 5' UTR and may regulate apoB mRNA translation. Perturbations in hepatic insulin signaling as observed in insulin-resistant states may alter cis-trans interactions at the 5' UTR, leading to alterations in the rate of apoB mRNA translation, thus contributing to apoB-lipoprotein overproduction.     

中药库拉索芦荟化学成分的液质定性分析

为阐明中药库拉索芦荟(Aloe barbadensis)叶的汁液浓缩干燥物的化学成分,该研究采用HPLC-DAD-ESI-IT-TOF-MSⁿ技术,结合对照品对比和文献检索,对其进行系统的定性分析。以水(A)-乙腈(B)为流动相进行梯度洗脱,流速为1.0 mL·min^-1,质谱使用ESI离子源,采用负离子模式分析液质数据。结果表明：(1)首次阐明中药库拉索芦荟中蒽醌类(芦荟大黄素、大黄素甲醚、大黄素-8-O-β-D-吡喃葡萄糖苷)、蒽酮类(芦荟素A、芦荟糖苷A)、色酮类(芦荟新苷D、7-O-甲基芦荟新苷A、altechromone A、芦荟苦素、芦荟新苷G、芦荟新苷C)、α-吡喃酮类(芦荟宁A、芦荟宁B)四类成分的主要化合物的裂解途径。蒽醌类化合物的裂解途径以失去CO₂和CO为主,蒽酮类化合物的裂解途径以己糖苷的裂解和失去CO为主,色酮类化合物的裂解途径以己糖苷的裂解和酯基的水解为主,α-吡喃酮类的裂解途径主要包括己糖苷的裂解、CO₂和H₂O的丢失等。(2)共检测到168种化学...