Optimization of a series of quinazolinone-derived antagonists of CXCR3

The evaluation of the CXCR3 antagonist AMG 487 in clinic trials was complicated due to the formation of an active metabolite. In this Letter, we will discuss the further optimization of the quinazolinone series that led to the discovery of compounds devoid of the formation of the active metabolite that was seen with AMG 487. In addition, these compounds also feature increased potency and good pharmacokinetic properties. We will also discuss the efficacy of the lead compound 34 in a mouse model of cellular recruitment induced by bleomycin.     

塔里木河下游河水漫溢后胡杨幼苗分布格局初探

采用最近邻体法,将Clark-Evans指数作为度量胡杨幼苗分布格局的指标,并用标准正态分布检验实际CE指数值偏离1的显著性,分析塔里木河下游河水漫溢后胡杨幼苗的分布格局。结果表明:(1)在3m×3m的样方尺度上,河水漫溢后0～1年和1～2年的胡杨幼苗呈聚集分布,漫溢后2～3年的胡杨幼苗呈均匀分布,漫溢后4～5年和5～7年的胡杨幼苗呈随机分布。(2)在3m×3m的样方尺度上,随着胡杨幼苗年龄的增长,胡杨幼苗的空间分布格局由聚集分布转变为均匀分布,最终呈现为随机分布的格局。(3)在2m×2m至10m×10m的样方尺度上,漫溢后5～7年的胡杨幼苗空间分布格局均表现为随机分布。(4)标准正态分布检验结果显示,各个尺度上胡杨幼苗的CE值与理论值1之间的偏离均不显著,说明随着尺度的增大,胡杨幼苗的空间分布格局并没有发生显著变化,始终呈现出随机分布的格局。     

Root growth dynamics of Deyeuxia angustifolia seedlings in response to water level

A greenhouse experiment was performed to investigate root growth dynamics, plant growth, root porosity and root morphology of a marsh plant Deyeuxia angustifolia, one of the dominant species in the Sanjiang Plain, China. The aim of this study was to elucidate how this plant adjusts its root system to acclimate to different hydrological environments. Experimental treatments included three water depths: −5, 0 and 5 cm (relative to the soil surface). Biomass accumulation was higher in the −5 cm (0.90 g per plant) and 0 cm water-depth (1.18 g per plant) than that in the 5 cm water-depth treatments (0.66 g per plant), indicating that plant growth was inhibited in the high water level. Root:shoot ratio (0.67 versus 0.42–0.43), the length (16 cm versus 12–13 cm) and diameter of adventitious roots (0.47 mm versus 0.41 mm), and root number (167 versus 81–119 number of roots per plant) were higher in the 0 cm water-depth than those in the high and low water-depth treatments. Enhanced water level led to slightly increased porosity of main roots, but porosity was about 7% in all treatments. After 8 weeks, roots had been distributed into 14, 11 and 7 cm soil depth in the 0, −5 and 5 cm water-depth treatments, respectively, indicating that both high and low water levels led to shallow root systems. Our data suggest that D. angustifolia can adjust root morphology and root growth pattern according to water level, and that this plant has limited oxygen diffusion potential to the roots due to the reduced biomass in the high water level.     

基于集对分析的城市生态系统健康评价—以兰州为例

城市生态系统是城市社会经济发展的基础和载体,但城市生态系统健康状况问题中包含多种不确定性因素,而集对分析可以有效处理这种不确定性.论文以特大型综合性城市兰州为研究案例,基于集对分析方法,构建包括生产力、生活态、生态势和生机度的城市生命力指数,诊断兰州城市生态系统2002至2008年间的健康状态.研究结果表明:2002～2008年,兰州市城市生态系统健康状况呈上升趋势,其健康联系度由2002年的0.451增至2008年的0.519,但总体水平仍不高.该研究为兰州市城市规划和生态建设推荐了重点行动领域,同时也可为兰州市实施可持续发展战略提供决策依据.     

The relationship between human cytomegalovirus infection and atherosclerosis development

Transport characteristics of essential trace elements as zinc, copper, selenium and iron have been studied in maternal–fetal direction in normal pregnancies, using in vitro perfusion of human placental lobules. Solutions of trace elements corresponding to twice the physiological concentrations were injected (100 l bolus) into the maternal arterial perfusate. Serial perfusate samples were collected every 30 sec from venous outflows for a study period of 5 min. Concentrations of these trace elements and their transport kinetics were determined. Transport fractions (TF) of zinc, copper, selenium and iron averaged 0.21, 0.49, 0.55 and 0.10% of maternal load respectively. Other parameters such as area under the curve, clearance, elimination constant, absorption and elimination rates showed some significant differences between the various elements. Copper and selenium appear to be transported passively in maternal–fetal direction, while for iron and zinc, role of active transport for transfer across the human placental membrane cannot be discounted. We speculate that alterations in copper: zinc TR50 (transport rate for 50% efflux) and TF ratios could serve as useful indicators for assessing placental transport status of these essential elements in complicated pregnancy states.     

内蒙古毕拉河林区近十年森林景观变化及驱动力浅析

基于遥感信息和地理信息系统,在景观总体和斑块个体两个层次上,从景观总体特征、斑块个体特征及斑块相间相关特征等3个方面对大兴安岭毕拉河林区近10年来森林景观的变化进行了系统的研究．结果表明,由于近10年来人类对森林生态系统干扰的不断增强,研究区森林景观在类型、景观总体特征、斑块个体与相关特征等方面发生了较大的变化．近10年林区森林景观的发展趋势是：受人为干扰正逐步加强,作为人工景观标志的耕地、居民点面积正逐步增加．面积转移矩阵分析结果表明,1997年耕地面积增加主要是由柞树林转化而来的,占耕地构成的30．87％．景观异质性分析结果表明,研究区森林景观耕地斑块数量增加68．80％,平均面积减少4．82％,景观的优势度减少,多样性增加,斑块之间的聚集程度减弱,1988年由柞树林和针叶林等少数几种斑块在景观中占绝对优势的情况有所改变．对研究区和相关地区的自然地理、社会经济等研究表明,火干扰、森林采伐与毁林开荒等是森林景观变化的关键性趋动力．