Synthesis of dihydroxyphenacyl glycosides for biological and medicinal study: β-oxoacteoside from Paulownia tomentosa

The protected structure of -oxoacteoside (tomentoside A), 2-oxo-2-(3,4-dihydroxyphenyl)ethyl 3-O-(2,3,4-tri-O-acetyl--l-rhamnopyranosyl)-4-O-caffeoyl--d-glucopyranoside 14 was synthesized in 14% overall yield in 11 steps, starting from d-glucose for biological and medicinal studies of phenylpropanoid glycosides. The first step was the preparation of a 3-O-rhamnopyranosyl disaccharide sugar core 2 from a suitably protected rhamnosyl trichloroacetimidate 10 and glucose derivative (diacetone-d-glucose 1) in 71% yield. To the glucose moiety of this sugar core, several protection/deprotection procedures were performed sequentially to obtain a fully acetylated sugar core 7 with a 4-OH group on the glucose moiety, in 57% yield in five steps. Thereafter, to the 4-OH group of the glucose moiety, selective 4-O-caffeoylation was achieved by proton-transfer esterification with 3,4-di-O-allylcaffeic acid 16 to give the caffeoyl disaccharide 11 in 97% yield. Then, it was converted to trichloroacetimidate 13 for a glycosylation donor in 90% in two steps. Finally, anomeric glycosylation was conducted with 2-oxo-2-(3,4-di-allyloxyphenyl)ethyl alcohol 19 with catalytic amounts of BF₃·Et₂O to give 2-oxo-2-(3,4-di-allyloxyphenyl)ethyl 2,6-di-O-acetyl-3-O-(2,3,4-tri-O-acetyl--l-rhamnopyranosyl)-4-O-(3,4-di-allyloxycaffeoyl)--d-glucopyranoside 14 in 60% yield. Deprotected intermediates of compounds 2, 11, 14, and 19 which were obtained in high yield would be useful for biological and medicinal studies of phenylpropanoid glycosides.Part of this study was presented at the 52nd Annual Meeting of the Japan Wood Research Society, Gifu, April, 2002     

Probing mode of action in plant cell cycle by the herbicide endothall, a protein phosphatase inhibitor

The mode of action of endothall, an herbicide which was reported to inhibit plant protein phosphatases 1 (PP1) and 2A (PP2A), was investigated. For initial characterization, a series of bioassays was used for comprehensive physiological profiling of endothall effects which suggested a phytotoxic mode of action similar to mitotic disrupter herbicides. Unlike known microtubule disrupters, endothall did not inhibit soybean tubulin polymerization in vitro. As shown in meristematic corn root tips, endothall distorted the orientation of cell division plane and microtubule spindle structures which led to cell cycle arrest in prometaphase. In tobacco BY-2 cells, malformed spindles together with prometaphase arrest of nuclei and abnormal perinuclear microtubule patterns were detected as early as 4 h of endothall treatment. These effects were also observed after treatment with other protein phosphatase inhibitors, cantharidin and okadaic acid, which phenocopied the mitotic changes described in tonneau1 (ton1) and tonneau2 (ton2) Arabidopsis mutants. These mutants are defective in TONNEAU2 (TON2) protein, a regulatory subunit of PP2A, which governs cell division plane and microtubule orientation. Therefore, PP2A/TON2 phosphatase complex is suggested to be an in planta molecular target of endothall. However, in BY-2 cells, additional effects of endothall, including inhibition of S-phase initiation and DNA synthesis, detected by 5-ethynyl-2′-deoxyuridine (EdU) incorporation, and condensed nuclei arrested in late mitosis were observed which were not reported in Arabidopsiston1 and ton2 mutants. This result indicates that two additional checkpoints in cell cycle were blocked by endothall which are probably not associated with TON2-pathway inhibition. Possibly, inhibition of PP1 and/or other PP2A protein phosphatases are involved in the regulation of these cell cycle phenomena.     

Hepatoprotective activity of angiotensin-converting enzyme (ACE) inhibitors, captopril and enalapril, against paraquat toxicity

Paraquat is a highly toxic herbicide that is used in most countries without restriction. The cytotoxic action of paraquat is mediated by reactive radicals that are products of its metabolic reduction in cells. It has already been hypothesized that some angiotensin-converting enzyme inhibitors (e.g., captopril and enalapril) could show antioxidant and radical scavenging activity through their structural thiol groups, increasing antioxidant enzymes production or nitric oxide synthesis. In this study the hepatoprotective effect of captopril and enalapril against paraquat induced oxidative stress cytotoxicity was evaluated in isolated rat hepatocyte. Subtoxic concentrations of captopril (0.2 mM) and enalapril (0.2 mM) significantly (p < 0.05) protected the hepatocytes against paraquat (2 mM) induced oxidative stress cytotoxicity markers including: cell lysis, reactive oxygen species (ROS) generation, lipid peroxidation, glutathione depletion, mitochondrial membrane potential decrease, lysosomal membrane oxidative damage and cellular proteolysis. Moreover, we showed that non-thiol enalapril acts as well as thiol containing captopril at inhibiting oxidative stress cytotoxicity markers. Finally, our results support the hypothesis that it is the increase in nitric oxide synthesis and not the presence of the thiol group that accounts for the antioxidant activity of ACE inhibitors.     

高标准基本农田建设成效评价——以盐亭县为例

基于高标准基本农田建设工作的开展,以盐亭县为例,从建设后的自然质量、建设任务完成情况和综合成效3个方面进行分析,选取土层厚度、土地平整工程量、提高粮食生产能力等14个因子,用熵权法测算各评价单元的建设成效性,将其建设成效评价划分为4个等级。结果表明:在高标准基本农田建设中,成效评价为优良的项目占总项目数的61.90%,占建设总面积的63.39%;只有2个项目所占的4.76%的建设总面积评价结果为差。该研究结果可为后期建设高标准基本农田提供科学依据。     

Response of hot pepper (Capsicum annuum L.) to mulching practices under planted greenhouse condition

Mulch is considered a desirable management technology for conserving soil moisture, improving soil temperature and soil quality. This study aimed to investigate soil conditions and hot pepper (Capsicum annuum L.) performance in terms of leaf photosynthetic capacity, fruit yield and quality, and irrigation water use efficiency (IWUE) under such practices in greenhouse condition. A field experiment across 3 years was carried out with four types of mulch (without mulch [CK], wheat straw mulch [SM], plastic film mulch [FM], and combined mulch with plastic film and wheat straw [CM]). Mulch could improve soil physical properties regardless of mulch materials. FM and CM treatments improved soil moistures status and soil temperature in comparison to CK control, while SM increased soil water content and decreased soil temperature. Mulch increased leaf net photosynthesis rate (P_N), stomatal conductance to water vapor (gs), intercellular CO₂ concentration (Ci), and transpiration rate (E), but declined instant water use efficiency (WUEi). No significant effect of mulch application on chlorophyll fluorescence was existent for the entire growth season. Fruit yield and irrigation water use efficiency (IWUE) showed some increment under all the mulch conditions. Compared to CK, the yield was enhanced by 82.3%, 65.0%, and 111.5% in 2008; 38.1%, 17.4%, and 46.5% in 2009; and 14.3%, 6.5%, and 19.6% in 2010 under SM, FM, and CM conditions, respectively. Although FM produced better fruit quality than other treatments, CM is the recommended practice for hot pepper cultivation in greenhouse condition due to working well to facilitate soil condition (moisture and temperature), plant growth, and marketable yield.     

Organochlorine and Metal Accumulation in Fish (Phoxinus phoxinus) Along a North-South Transect in the Alps

Southern populations of the European minnow fromremote oligotrophic mountain lakes along an Alpinenorth-south transect accumulated more p,p DDE andPCBs than northern populations. As these semi-volatileorganochlorines predominantly evaporate in warmcountries, higher rates of condensation (deposition)are assumed to occur in the southern slopes of theAlps. The higher accumulation of lead and cadmium insouthern population is rather attributed to geogenicand specific environmental impacts than to atmosphericdeposition. Increasing liver ratios of [glutathionedisulfide]/[glutathione], a potential indicator foroxidative stress, from north to south reflect thegenerally higher toxic load at remote sites at thesouthern edge of the Alps. However, histopathologicalchanges in the liver did not correlate withaccumulated toxicants indicating that deposition doesnot lead to severe lesions but induces specificmechanisms for detoxification.     

基于三层结构的基本农田信息管理与辅助决策系统研究

按照基本农田建设和管理的要求,通过选取评价指标,引入背包算法建立耕地入选基本农田的模型。在此基础上,采用C#、Mapinfo MapXtreme 2004和SQL Server2000三者结合开发基于三层结构的基本农田信息管理与辅助决策系统,使GIS技术与空间决策模型有机结合,实现了数据管理、耕地入选基本农田决策模型和用户管理等功能。实例表明,该系统具有较高的灵活性和可扩充性。     

大都市边缘区三级基本农田集中保护区分级划定及调控机制

针对大都市边缘区城市拓展与农地保护矛盾尖锐、景观破碎化、权属细碎化、整体布局稳定性差等问题,开展三级基本农田集中保护区分级划定及调控机制研究,对大都市边缘区保红线保发展促集约促创新具有重要意义。该文以北京市昌平区为例,提出三级基本农田集中保护区划定的总体思路,构建基本农田集中保护区识别指标体系,划定基本农田集中保护区,并将基本农田集中保护区分为市区乡三级,在此基础上探讨基本农田集中保护区分级调控机制。研究划定了1个市级基本农田集中保护区、6个区级基本农田集中保护区、6个乡级基本农田集中保护区,规划土地整治复耕1 149.97 hm2,使单位基本农田经营规模提高到38.76 hm2,使3 hm2以下细小图斑降低至1.21%,实现了昌平区内96.63%的基本农田集中连片保护,建立了规划调控、用途管制、奖惩联动分级调控机制。研究结果可为国家制定基本农田保护区分级保护政策和开展同类研究提供参考,为地方政府提高基本农田保护区保护质量和管理效率提供思路借鉴。     

引入耕地生态价值的咸阳市基本农田划定

为了探索科学客观的基本农田划定方法,实现将集中连片和优质稳定的耕地划为基本农田的目标,有效保护耕地和保障国家农业生产安全。该研究以陕西省咸阳市为例,引入耕地生态价值和政策条件多维度评价耕地质量,结合耕地质量空间集聚类型划定耕地保护分区;采用缓冲区分析法识别耕地连片性,耦合耕地保护分区和耕地连片等级,尝试探索“连片优先、质量优良、数量约束”的基本农田划定流程。结果表明:1)咸阳市耕地质量划分为高、较高、一般、较低、低5个等级,全市超过一半面积的耕地质量等级为低和较低等级(35.81%和29.67%),一般和较高等级的耕地面积占比也均超过了10%;不同耕地质量等级在空间分布上的差异受地形和区域经济发展影响较大,耕地质量等级总体上呈现出“南高北低”的空间分布格局;咸阳市耕地质量在空间上呈现出明显的集聚特征,以高-高值集聚型和低-低值集聚型耕地为主;2)将全市耕地划为优先保护区、适宜保护区、重点整治区和全面治理区4个保护分区并提出一些保护建议。全面治理区内耕地面积最多,占全市耕地总面积的35.50%,适宜保护区内耕地面积最少,仅占11.81%;3)咸阳市共得到49 713个耕地连片地块,面积2...     

基于GIS与耕地质量组合评价模型划定基本农田整备区

针对划定基本农田有质量、数量和空间的多重要求,该文从耕地的自然条件、质量条件、灌溉条件、区位条件、规划用途等5个层面选取16个指标建立了一般农田入选基本农田整备区的指标体系,并运用GIS技术提取各评价指标的空间属性数据;然后根据耕地质量模糊优选模型和属性层次模型2个模型评价结果的平均值对候选耕地进行质量和区位优劣排序;最后根据排序结果,通过GIS空间分析功能,以重庆市秀山县梅江镇为例,划定基本农田整备区的空间分布范围。组合评价模型可形成多角度评价结果的综合平衡,提高评价结果的科学性。