Synthesis and in vitro antiproliferative evaluation of novel N-alkylated 6-isobutyl- and propyl pyrimidine derivatives

A series of novel N-alkylated C-6-isobutyl- or -propyl pyrimidine derivatives were synthesized and their antiproliferative effect was evaluated on a panel of tumor cell lines including leukemia cell line K562 and normal diploid human fibroblasts. N-methoxymethylated 5-methylpyrimidin-2,4-dione with di(benzyloxy)isobutyl at C-6 (14b) showed the strongest effect on the cell growth at micromolar concentrations. Mechanisms of action for the lipophilic compound 14b predicted in silico, pointed to its anticancer and antimetastatic potential exerted through inhibition of DNA or RNA polymerases and adhesion molecules. The latter mechanism has been supported in vitro for adherent tumor cell lines.     

退耕还林还草工程对陕北地区生态系统服务价值时空演变的影响

基于陕北地区1990、2000、2015年土地利用数据，运用单位面积生态系统价值当量因子法、格网法、探索性空间数据法（ESDA），分析了退耕还林还草工程实施前后生态系统服务价值（ESV）的空间分布和演化规律，探讨了退耕还林还草工程对ESV的影响。结果表明：（1）陕北地区退耕还林还草工程实施效果显著，工程实施后共有297066.15 hm2耕地转化为林地和草地，林草覆盖率由57.33%增长至60.50%。（2）退耕还林还草工程使得陕北地区ESV得到了显著提升。25年间陕北地区ESV共增加了32.82亿元，ESV在工程实施后比工程实施前多增加了5.93亿元，增长主要源于退耕引起林地和草地面积的增加。（3）ESV空间分布上呈显著的“南高北低”分布格局，并表现出正向的集聚性和依存性，ESV热点区和冷点区集聚效果明显，热点区集聚与林地、草地的空间分布相吻合，冷点区集聚与未利用地、耕地和建设用地的空间分布相吻合。（4）受退耕还林还草工程影响，陕北地区中部中等等级和次高ESV分布区域逐渐增大、次热点区空间集聚性逐渐增强，北部次低等级和低等级ESV分布区域逐渐减少、冷点区空间集聚性逐渐减弱。整体而言，陕北地区土地利用类型转移和ESV的增减变化与推行退耕还林还草工程在时间上相呼应、在空间上相匹配，退耕还林还草工程实施使得陕北地区生态环境得到了有效改善，ESV得到了显著提升。     

Biodiversity on the brink: Evaluating a transdisciplinary research collaboration

Global biodiversity is facing an extinction crisis. Australia has one of the highest terrestrial species extinction rates in the world. Scientists, policy advisors and governments have recommended that the issue be addressed at a landscape-scale, while noting that there are significant knowledge gaps that are hampering implementation of such an approach. From 2011–2015, the Australian Government funded a transdisciplinary research program, the Landscapes and Policy Hub, to meet this need. Transdisciplinary research is widely acknowledged as essential to address the complexity of contemporary environmental problems. Given that such research programs are in their infancy, it is important to evaluate their efficacy and provide an empirical basis for improving their design. This paper presents an evaluation of the strategies fostering transdisciplinarity adopted by the Landscapes and Policy Hub. A heavy emphasis on communication, with skilled knowledge brokering, regular face-to-face meetings using participatory activities and shared field engagements enhanced transdisciplinary interaction between researchers and research users. However, establishing a fully integrated interdisciplinary research program remained a challenge. Efforts to enable shared conceptual frameworks to emerge through adaptive application of theory in practice could have been balanced with increased effort at the outset for researchers and research users to collaboratively formulate shared research questions, leading to the establishment of teams that could address these questions through cross-mobilisation of interdisciplinary expertise.     

Unpacking chimpanzee (Pan troglodytes) patch use: Do individuals respond to food patches as predicted by the marginal value theorem?

The marginal value theorem is an optimal foraging model that predicts how efficient foragers should respond to both their ecological and social environments when foraging in food patches, and it has strongly influenced hypotheses for primate behavior. Nevertheless, experimental tests of the marginal value theorem have been rare in primates and observational studies have provided conflicting support. As a step towards filling this gap, we test whether the foraging decisions of captive chimpanzees (Pan troglodytes) adhere to the assumptions and qualitative predictions of the marginal value theorem. We presented 12 adult chimpanzees with a two-patch foraging environment consisting of both low-quality (i.e., low-food density) and high-quality (i.e., high-food density) patches and examined the effect of patch quality on their search behavior, foraging duration, marginal capture rate, and its proxy measures: giving-up density and giving-up time. Chimpanzees foraged longer in high-quality patches, as predicted. In contrast to predictions, they did not depress high-quality patches as thoroughly as low-quality patches. Furthermore, since chimpanzees searched in a manner that fell between systematic and random, their intake rates did not decline at a steady rate over time, especially in high-quality patches, violating an assumption of the marginal value theorem. Our study provides evidence that chimpanzees are sensitive to their rate of energy intake and that their foraging durations correlate with patch quality, supporting many assumptions underlying primate foraging and social behavior. However, our results question whether the marginal value theorem is a constructive model of chimpanzee foraging behavior, and we suggest a Bayesian foraging framework (i.e., combining past foraging experiences with current patch sampling information) as a potential alternative. More work is needed to build an understanding of the proximate mechanisms underlying primate foraging decisions, especially in more complex socioecological environments.     

Evaluation of environmentally conscious manufacturing programs using a three-hybrid multi-criteria decision analysis method

Environmental management, being an important component in strategies for achieving sustainable development of processes and products, has emerged as a proactive approach in majority of the manufacturing organizations. From the strategic perspective environmentally conscious manufacturing (ECM) programs lead to better environmental management practice. The objective of the current paper is to present an integrated and holistic framework to evaluate ECM programs. This framework combines three multi-criteria decision analysis (MCDA) methods to consider eight major environmentally conscious manufacturing indicators (ECMI) in order to identify the efficiency of each ECM program. First the interdependence relationship among the ECMIs is established using decision-making trail and evaluation laboratory (DEMATEL). Then a range of weightage (i.e. upper and lower bounds) is created for each ECMI using analytic network process (ANP) to include managerial preferences. Finally, this range of weightage for each indicator is applied to perform restricted multiplier data envelopment analysis (RMDEA). Results show that the technical efficiency of the inefficient ECM programs for integrated RMDEA, on average, is calculated as 53.2% whereas traditional input oriented DEA provides the same score as 72.3%. This clearly indicates that integrated RMDEA is better than the input oriented DEA because same level of output could be produced with lesser resources if the ECM programs perform on the frontier. Hence, the advantage of this methodology is that the managerial preferences are successfully implemented through this newly developed hybrid methodology that will help to reduce less resource consumption and lead to better environmental policy.     

Fisher information for a multivariate extreme value distribution

Explicit algebraic formulae for the Fisher information matrixof the multivariate extreme value distribution with generalisedextreme value margins and logistic dependence structure aregiven.     

基于可持续发展目标的资源型城市可持续发展评价技术及应用——以湖南省郴州市为例

资源型城市作为我国重要战略保障基地，面临较为突出的不可持续问题，定量化开展可持续发展水平监测评估是推动其绿色转型发展、激活再生动力的重要途径。基于联合国可持续发展目标体系(SDGs),结合行星边界理论，从资源型城市可持续发展特征出发，建立了由2个系统、4个支柱、12个领域和48项指标组成的资源型城市可持续发展评价指标体系。借鉴全球SDGs监测评估实践经验，考虑指标属性，综合确定各指标的阈值，并采用改进的离差标准化、障碍度分析及耦合协调度分析等方法建立综合评价技术体系。以拥有“有色金属之乡”称号的郴州市国家可持续发展议程创新示范区为评价对象，对其2005—2019年连续15年的可持续发展水平进行实证分析。结果表明：(1)郴州市可持续发展水平整体上呈现稳步上升趋势，得分由0.398上升到0.610。(2)4个支柱中，自然资源支柱的得分进步幅度最大，高达71.3%,说明郴州市已经逐步提高对资源利用效率的重视，同时意识到挖掘替代资源的重要性，资源保障与利用能力不断提升；而发展动力支柱得分始终处于较弱或中等水平，已成为制约郴州市可持续发展和绿色转型的主要因素，其中科技创新驱动是该支柱发展关键障碍...     

大型煤电基地开发生态累积效应及定量分析方法研究

大型煤电基地(CEBs)是我国煤基能源和材料集中开发区域和国家能源战略安全重要支撑，合理评价CEBs开发生态影响是CEBs可持续协调开发、科学管理中的难点问题。研究将CEBs开发视为系统工程，与自然生态系统(NES)相关联，深入研究大型煤电基地生态系统(CEBES)的驱动行为、内在结构及主要关系、生态影响途径、生态累积过程和生态累积效应及阈值分析方法。基于CEBs空间和功能定位提出CEBs的概念、内涵和特点，融合构建的CEBES涵盖到自然资源、能源开发行为(煤、电等)、其他人类活动(农、牧、城)和大气、水、土壤及生物域；研究表明CEBES的生态累积状态受三种行为驱动和影响(自然行为、能源开发行为和其他人类活动),通过融合、传导和辐射耦合作用，表现为生态要素损伤、系统结构变化和系统状态失衡三级状态，生态累积具有影响多态性、空间多尺度和过程渐变性特点；明确了生态累积过程、累积效应和阈值及其相互关系，引入反映生态影响累积程度的生态损伤系数，提出四类生态阈值(生态要素、内部结构、系统状态和行为调控);基于系统性和实用性筛选反映生态累积相对状态的60项指标，构建具有“三力”驱动、分区要素耦合和系...     

Phytochemical profile of Juniperus oxycedrus ssp. oxycedrus berries: A new monoterpene glucoside and evaluation of the effects on cancer cell lines

Phytochemical investigation of polar extract from Juniperus oxycedrus spp. oxycedrus berries leds to the isolation of one new monoterpene glucoside (3R,6E)-3,7 dimethyl 8-hydroxy-6-octenoic acid 8-O-β-d-glucopyranoside along with seven known components, some of them were initially isolated from Juniperus communis L. berries. Their structures were established on the basis of extensive 1D and 2D NMR (¹H, ¹³C, COSY, HMBC, HSQC, ROESY) and ESI-MS studies. The n-butanol fraction and isolated components, shikimic acid (2), compound 3, 4 and 5 were evaluated, in vitro, for their effect on cell viability against human malignant melanoma (A375), breast (MCF-7) and lung (H460) cancer cell lines. Shikimic acid exhibited selective effect on cell viability only against breast MCF-7 cell lines reaching IC₅₀ value at dose of 30 μM and also induced the level decrease of vascular endothelial growth factor (VEGF) and five pro-inflammatory cytokines suggesting its potential anti-inflammatory effect.