New non-hydroxamic ADAMTS-5 inhibitors based on the 1,2,4-triazole-3-thiol scaffold

In this Letter we describe the design, synthesis, screening, and optimization of a new family of ADAMTS-5 inhibitors. These inhibitors display an original 1,2,4-triazole-3-thiol scaffold as a putative zinc binding-group. In vitro results are rationalized by in silico docking of the compounds in ADAMTS-5’s crystal structure.     

小麦T型细胞质雄性不育系与相应保持系线粒体DNA的RAPD分析

利用RAPD技术对小麦T型细胞质雄性不育系75-3369A和相应保持系75-336 9B 的线粒体DNA(mtDNA)进行了81个单引物和14组双引物的多态性研究。结果有73个单引物和全部的双引物有扩增结果,表现出多态性的有10个单引物和一组双引物。 Abstract:Using 81 single-primers and 14 double-primers,T-type CMS(cytoplasmic male sterile)line 75-3369 A and is maintainer 75-3369B were studied by means of RAPD.73 single-primers and all double-primers gave amplified products in the experiment,among them 10 single-primers and one double-primer presented polymorphism.     

耕作措施对冬小麦田杂草生物多样性及产量的影响

在连续5a秸秆全量还田的免耕、旋耕、耙耕、深松和常规耕作试验地中,设置了除草和不除草处理,研究了其对杂草总密度、优势杂草种类、生物多样性指数和冬小麦产量的影响,并分析了杂草与小麦间的竞争关系。结果表明,麦田杂草主要有7种,分别是麦蒿(Descuminia sophia (L.) Webb ex Prantl)、荠菜(Capsella bursa-pastoris (L.) Medik)、燕麦(Avena sativa L.)、田旋花(Convolvulus arvensis L.)、刺儿菜(Cirsium setosum (Willd.) Bieb.)、繁缕(Stellaria media (L.) Vill.)、麦家公(Lithospermum arvense L.)。在未除草条件下,免耕、深松的杂草总密度显著提高;而在除草条件下,杂草密度显著下降。免耕、深松、常规耕作在未除草条件下,优势杂草种类为麦蒿、荠菜,旋耕、耙耕条件下的优势杂草为麦蒿;而除草后各处理的优势杂草均只有麦蒿。耙耕、常规耕作措施在未除草条件下杂草群落具有较高的物种丰富度和均匀度。无论哪种耕作措施,除草能提高冬小麦产量,其中以深松耕作结合除草处理的小麦产量最高。在小麦抽穗期,未除草处理杂草株高接近或高于小麦株高,会造成杂草与小麦间的光竞争,对小麦的生长状况有显著影响,从而导致小麦产量降低。     

氯喹与氟康唑联合对新生隐球菌的体外药敏实验

目的研究氯喹与氟康唑体外联合应用对隐球菌生长作用的影响。方法参考M27-A方案,检测10μmol/L,100μmol/L与1 000μmol/L 3种浓度氯喹与氟康唑联合后对20株菌株的氟康唑对隐球菌最小抑菌浓度与最小杀菌浓度的变化。结果与10μmol/L氯喹组相比,100μmol/L以上浓度的氯喹组可以显著降低氟康唑对隐球菌的M IC与MFC。结论氯喹在体外可以提高氟康唑抗隐球菌的作用,与氟康唑具有协同抗隐球菌的作用。     

Structural prediction and analysis of endothelial cell protein C/activated protein C receptor.

The endothelial cell receptor (EPCR) for protein C (PC)/activated protein C (APC) is a 221 amino-acid residues long transmembrane glycoprotein with unclear physiological function. To facilitate future studies and to rationalize recently reported experimental data about this protein, we have constructed three-dimensional models of human, bovine and mouse EPCR using threading and comparative model building. EPCR is homologous to CD1/MHC class I molecules. It consists of two domains, which are similar to the alpha1 and alpha2 domains of MHC class I molecules, whereas the alpha3 domain of MHC is replaced in EPCR by a transmembrane region followed by a short cytosolic tail. The alpha1 and alpha2 domains of CD1/MHC proteins form a groove, which binds short peptides. These domains are composed of an eight-stranded antiparallel beta-pleated sheet with two long antiparallel alpha-helices. The distance between the helical segments dictates the width of the groove. The cleft in EPCR appears to be relatively narrow and it is lined with hydrophobic/aromatic and polar residues with a few charged amino acids. Analysis of the human EPCR model predicts that (a) the protein does not contain any calcium binding pockets; (b) C101 and C169 form a buried disulphide bridge, while C97 is free, and buried in the core of the molecule; and (c) four potential glycosylation sites are solvent exposed.     

Myxinidocotyle gen.n. and Lophocotyle Braun (Platyhelminthes, Monogenea, Acanthocotylidae) with descriptions of three new species from hagfishes (Chordata, Myxinidae)

Three new species of monogencans parasitizing hagfish are described: Myxinidocotyle californica gen. et sp.n., M. japonica sp.n. and Lophocotyle novaezeelandica sp.n. The pseudohaptor of Myxinidocotyle has 8+8 transverse ridges that never attain the radial arrangement characterizing Lophocotyle and Acanthocotyle . There are no sclerites in the pseudohaptoral ridges of Myxinidocotyle and Lophocotyle . The male reproductive system of Myxinidocotyle and Lophocotyle differs from that of Acanthocotyle in having a bilateral accessory gland apparatus and an armed copulatory organ. The femrle reproductive system has a large vaginal receptaculum scminis; in Myxinidocotyle with two vagino-intestinal canals. The uterine pore and the male genital pore are close together and the vaginal pore is situated posterior to them, on the left ventral side of the body. We conclude that Myxinidocotyle, Lophocotyle and Acunrkocotyle represent different levels of acanthocotylid evolution. Myxinidocotyle being the most primitive. The family Acanthocotylidac is divided into the subfamilies Myxinidoeutylinae subfam.n., Lophocotylinae and Acanthoeutylinae.     

Design and synthesis of novel bis-thiazolone derivatives as micromolar CDC25 phosphatase inhibitors: Effect of dimerisation on phosphatase inhibition

CDC25 phosphatases are involved in deregulated cell cycle progression and tumor development with poor prognosis. Among the most potent CDC25 inhibitors, quinonoid-based derivatives have been extensively studied. Dimerisation of heterocyclic quinones has led to IRC-083864, a bis-quinone compound with increased CDC25B inhibitory activity. Thirty-one bis-thiazolone derivatives were synthesized and assayed for CDC25 inhibitory activity. Most of the dimers displayed enhanced inhibitory activities with micromolar IC₅₀ values lower than that observed for each thiazolone scaffold separately. Moreover, most of these compounds were selective CDC25 inhibitors. Dimer 40 showed an IC₅₀ value of 2.9 μM and could inhibit CDC25 activity without generating reactive oxygen species which is likely to occur with quinone-based inhibitors. Molecular docking studies suggested that the dimers could bind simultaneously to the active site and the inhibitor binding pocket.     

水温对刀鲚幼鱼耗氧率、窒息点、血糖及肌肝糖元指标的影响

实验测定了不同水温条件下刀鲚(Coilia nasus)幼鱼的耗氧率和窒息点,并对耗氧率的昼夜变化规律以及水温对刀鲚幼鱼血糖及肌肝糖元指标的影响进行了研究,旨在为刀鲚运输、养殖生产中制定合理的放养密度和养殖工艺提供参考依据.结果表明:在试验水温(16℃～28C)条件下,刀鲚幼鱼的耗氧率随水温的升高而增大,耗氧率(R)与水温(T)的回归方程为R=0.988T2-32.36T+343.7,相关系数为0.96;刀鲚幼鱼的耗氧率具有昼夜节律性,耗氧高峰出现在7:00,低谷在21:00;刀鲚幼鱼的窒息点与水温显著相关,窒息点A(mg·L-1)与水温T(℃)的回归关系为A=0.9397T0.8001,R2=0.98.刀鲚幼鱼血清中血糖含量在水温16℃～24℃阶段保持相对稳定,血糖含量在17.24 ～ 19.79 mmol·L-1,肌肉和肝脏糖元含量均呈波浪式变动;但在水温24℃～28℃阶段,血糖含量随水温上升而显著升高,而肌肉和肝脏糖元含量均显著降低.     

南方红豆杉人工引种及野生植株活性成分含量与分布

南方红豆杉是我国特有的濒危植物,因其具有抗癌药用价值而被过度采集,导致现存种群减少.采用超声辅助提取和HPLC检测人工引种及野生南方红豆杉植株中紫杉醇、7-木糖紫杉醇、三尖杉宁碱等活性成分含量,分析其在不同部位、年限和坡向的分布规律.结果表明:南方红豆杉人工引种后,植株中的紫杉醇、7-木糖紫杉醇和三尖杉宁碱含量变化明显,野生植株中紫杉醇含量显著高于人工栽培植株,约为栽培植株的1.8倍,其他2种物质含量以人工栽培略高.不同部位、冠层样品中3种活性物质含量差异显著,以茎皮、高冠层枝叶含量较高.不同年限南方红豆杉植株中紫杉醇、7-木糖紫杉醇和三尖杉宁碱含量以4年生植株较高,分别为0.08、0.91和0.32 mg·g-1.不同坡向植株中3种活性成分含量以阳坡植株较高,紫杉醇和7-木糖紫杉醇含量差异显著,三尖杉宁碱含量差异不显著.南方红豆杉中3种活性成分的积累与光照条件密切相关,栽培过程中适当增加光照有利于3种活性成分的积累.