广东三水盆地晚白垩世的介形类动物群

依据24口钻井及4条地表剖面372个样品的采集和分析,三水盆地晚白垩世的介形类动物群含介形类化石28属81种,本文描述其中24属62种,包括1新种.此介形类动物群在数量上以女星介科和玻璃介科最繁盛,次为背足介科、湖花介科和类女星介科,依其横向分布及纵向变化规律,划分为Talicypridea和Porpocypris两个动物群及Talicypridea amoena带、Porpocypris globra带和Porpocypris sphaeroidalis带等3个化石带.依据介形类化石三水组可与南雄群对比,时代属晚白垩世早--中期.大塱山组与上湖组坪岭段对比,时代应属晚白垩世晚期.     

广东南雄盆地罗佛寨群的介形类动物群

作者依据坪岭、武台岗、罗佛寨、城南、枫门坳、修仁、黄茅坪、暖水塘等8条剖面725个样品的研究,系统描述了罗佛寨群的介形类化石21属78种,包括2个新种;建立了罗佛寨群介形类序列,自下而上划分出.Porpocypris globra,Porpocypris sphaeroidalis,Cypris concina,Sinocypris excelsa和Cyprois reniformis 5个介形类化石带.前两个带合称.Porpocypris动物群,时代属晚白垩最晚期.后三带称为Cypris-Sinocypris动物群,时代分别为早、中、晚古新世.     

Obestatin与GPR39受体的最新研究进展

肥胖抑制素(obestatin)是新近发现的一种与食欲刺激素有关的多肽(ghrelin-associated peptide,GAP),可以结合孤儿G蛋白GPR39受体,抑制摄食、胃肠功能和体重的增加,被认为是食欲刺激激素(ghrelin)的生物学拮抗剂或阴阳活性多肽.但最新研究认为,obestatin不能与GPR39受体特异性结合,也不能改变ghrelin所诱导的生物学效应.鉴于上述不同的研究报道,就其相关研究成果作一概述.     

小果博落回中2种杀虫活性成分的分离及鉴定

以粘虫(Mythimna separata)3龄幼虫为试虫,采用生物活性示踪法从小果博落回(Macleaya microcarpa)乙醇提取物中分离纯化出2种活性成分,经MS1、H-NMR1、3C-NMR分析鉴定为二氢血根碱和二氢白屈菜红碱。采用小叶碟添加法测试了2种化合物对粘虫3龄幼虫的拒食及毒杀活性。结果表明,2种化合物对粘虫3龄幼虫均具有较高的拒食活性,48 h的拒食AFC50分别为0.168和0.231 mg.mL-1,同时,二氢血根碱对粘虫3龄幼虫具有一定的毒杀活性,96 h的LC50为0.085 mg.mL-1。分析认为二氢血根碱可能是小果博落回的主要杀虫活性成分之一。     

水分胁迫对2种科尔沁沙地植物光合和水分利用特性的影响

选用内蒙古科尔沁沙地1年生植物狗尾草(Setaria viridis)和沙米(Agriophyllum squarrosum)为材料,采用盆栽方法研究了它们在不同土壤水分处理下的光合参数和水分利用效率的日变化特征及其与环境因子的相关关系。结果表明,狗尾草和沙米的净光合速率日变化曲线在充分供水条件下均呈单峰型,在轻度干旱胁迫下均呈双峰型,而在重度干旱胁迫下分别呈双峰型和左偏单峰型。狗尾草和沙米的蒸腾速率在不同水分处理下都近似呈双峰型曲线,然而变化程度却不相同。重度干旱胁迫下,狗尾草日平均净光合速率(11.52μmol.m-2.s-1)和蒸腾速率(3.62 mmol.m-2.s-1)分别比相应充分供水处理增加7%和43%,而沙米的日平均净光合速率(7.07μmol.m-2.s-1)和蒸腾速率(5.56 mmol.m-2.s-1)则分别较相应充分供水处理降低13%和36%。重度干旱胁迫下,狗尾草水分利用效率(2.84 mmol.mol-1)比相应充分供水处理降低3.1%,而沙米水分利用效率(1.14mmol.mol-1)则较充分供水处理提高了34%。光合速率下降在充分供水条件下主要是由气孔调节,但在轻度干旱胁迫和重度干旱胁迫处理下非气孔因素调节却起到十分重要的作用。在重度干旱胁迫下,狗尾草仍具有显著高于沙米的的净光合速率和水分利用效率,这可能是其仍然能够在固定沙地分布的原因之一。     

Design and synthesis of macrocyclic peptidyl hydroxamates as peptide deformylase inhibitors

Macrocyclic peptidyl hydroxamates were designed, synthesized, and evaluated as peptide deformylase (PDF) inhibitors. The most potent compound exhibited tight, slow-binding inhibition of Escherichia coli PDF (K(I)(*)=4.4 nM) and had potent antibacterial activity against Gram-positive bacterium Bacillus subtilis (MIC=2-4 microg/mL).     

Aglycone exploration of C-arylglucoside inhibitors of renal sodium-dependent glucose transporter SGLT2

Inhibition of sodium-dependent glucose transporter 2 (SGLT2), the transporter that is responsible for renal re-uptake of glucose, leads to glucosuria in animals. SGLT-mediated glucosuria provides a mechanism to shed excess plasma glucose to ameliorate diabetes-related hyperglycemia and associated complications. The current study demonstrates that the proper relationship of a 4′-substituted benzyl group to a β-1C-phenylglucoside is important for potent and selective SGLT2 inhibition. The lead C-arylglucoside (7a) demonstrates superior metabolic stability to its O-arylglucoside counterpart (4) and it promotes glucosuria when administered in vivo.     

Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors

A series of structurally novel stearoyl-CoA desaturase1 (SCD1) inhibitors has been identified via molecular scaffold manipulation. Preliminary structure–activity relationship (SAR) studies led to the discovery of potent, and orally bioavailable piperidine-aryl urea-based SCD1 inhibitors. 4-(2-Chlorophenoxy)-N-[3-(methyl carbamoyl)phenyl]piperidine-1-carboxamide 4c exhibited robust in vivo activity with dose-dependent desaturation index lowering effects.