RSK1 vs. RSK2 Inhibitory Activity of the Marine β-Carboline Alkaloid Manzamine A: A Biochemical,Cervical Cancer Protein Expression,and Computational Study

Manzamines are complex polycyclic marine-derived β-carboline alkaloids with reported anticancer, immunostimulatory, anti-inflammatory, antibacterial, antiviral, antimalarial, neuritogenic, hyperlipidemia, and atherosclerosis suppression bioactivities, putatively associated with inhibition of glycogen synthase kinase-3, cyclin-dependent kinase 5, SIX1, and vacuolar ATPases. We hypothesized that additional, yet undiscovered molecular targets might be associated with Manzamine A’s (MZA) reported pharmacological properties. We report here, for the first time, that MZA selectively inhibited a 90 kDa ribosomal protein kinase S6 (RSK1) when screened against a panel of 30 protein kinases, while in vitro RSK kinase assays demonstrated a 10-fold selectivity in the potency of MZA against RSK1 versus RSK2. The effect of MZA on inhibiting cellular RSK1 and RSK2 protein expression was validated in SiHa and CaSki human cervical carcinoma cell lines. MZA’s differential binding and selectivity toward the two isoforms was also supported by computational docking experiments. Specifically, the RSK1-MZA (N- and C-termini) complexes appear to have stronger interactions and preferable energetics contrary to the RSK2–MZA ones. In addition, our computational strategy suggests that MZA binds to the N-terminal kinase domain of RSK1 rather than the C-terminal domain. RSK is a vertebrate family of cytosolic serine-threonine kinases that act downstream of the ras-ERK1/2 (extracellular-signal-regulated kinase 1/2) pathway, which phosphorylates substrates shown to regulate several cellular processes, including growth, survival, and proliferation. Consequently, our findings have led us to hypothesize that MZA and the currently known manzamine-type alkaloids isolated from several sponge genera may have novel pharmacological properties with unique molecular targets, and MZA provides a new tool for chemical-biology studies involving RSK1.     

Frequency shift domain iterative analysis for frequency estimation of equilong signals

From the view of trick recognition, features of signal decomposition structure in existing frequency estimation methods were analyzed, based on which, a frequency shift domain decomposition structure was proposed. A compound signal was constructed by combining several simple signals corresponding to different times. The given information in the time domain can be adopted to form an information accumulation effect, such that the interference frequency and noise can be suppressed effectively by decreasing the calculation. To match the use of a frequency shift domain decomposition structure, a frequency shift equilong iterative algorithm suitable for equilong signals was proposed. Simulated experiments were carried out in numerous application environments. The results show better noise immunity and real time performance as well as higher frequency estimation precision.     

Soil water in relation to irrigation, water uptake and potato yield in a humid climate

Efficiently controlling soil water content with irrigation is essential for water conservation and often improves potato yield. Volumetric soil water content (θ_v) in relation to irrigation, plant uptake, and yield in potato hills and replicated plots was studied to evaluate four water management options. Measurements of θ_v using a hammer driven probe were used to derive a θ_v index representing the relative θ_v status of replicated plots positioned along a hill slope. Time series for θ_v were determined using time domain reflectometry (TDR) probes at 5 and 15 cm depths at the center, shoulder, and furrow locations in potato hills. Sap flow was determined using flow collars in replicated field plots for four treatments: un-irrigated, sprinkler, surface drip, and sub-surface drip irrigation (40 cm depth). Irrigated yields were high/low as the θ_v index was low/high suggesting θ_v excess was a production problem in the wetter portions of the study area. The diurnal pattern of sap flow was reflected in the θ_v fluctuation it induces at hill locations with appreciable uptake. Hill locations with higher plant uptake were drier as was the case for the 5 cm (dry) depth relative to the 15 cm (wet) depth and for locations in the hill (dry) relative to the furrow (wet). The surface drip system had the lowest water use requirement because it delivers water directly to the hill locations where uptake is greatest. The sub-surface drip system wetted the hill gradually (1-2 days). Measurement of the θ_v index prior to experimental establishment could improve future experimental design for treatment comparisons.     

Does spatial arrangement of 3D plants affect light transmission and extinction coefficient within maize crops?

Row spacing effects on light interception and extinction coefficient have been inconsistent for maize (Zea mays L.) when calculated with field measurements. To avoid inconsistencies due to variable light conditions and variable leaf canopies, we used a model to describe three-dimensional (3D) shoot structures combined with a model of 3D light transfer. The MODICA model mimics 3D shoot structures of maize plants from digitizations in the field and makes it possible to simulate associated hypothetical canopies by re-arranging plants into different row spacings. All row spacings examined with the model had 10 plants m⁻². By using the light model RIRI, simulations showed the relative importance of development stage and time integration on fraction of light transmitted and on the extinction coefficient. Narrow row spacings consistently had less transmitted light and greater values of extinction coefficient. This modelling tool shows promise to effectively evaluate row spacing to optimize light interception.     

工作状态下不同驾驶员心率变异性对比分析

本文从人机工程学的角度出发,运用了时域分析方法,通过设计行车实验,分析了驾驶员在正常驾驶状态时影响心率交化的各种因素.初步获得驾驶员本身、外界因素对驾驶员生理变化的影响程度.     

蒸渗仪测定滴灌枣树不同时间尺度下腾发强度特征

为精确测定、准确模拟阿克苏地区滴灌枣树腾发过程,基于大型称重式蒸渗仪测定枣树全生育期逐时及逐日腾发强度（ET）,利用水量平衡方程、PM公式及经典统计原理,分析不同时间尺度下叶面积指数（LAI）、气象因素[温度（I）、风速（V）、净辐射（R_n）]、表层土壤含水率（W）与枣树腾发强度的相关关系并建立预测模型。结果表明：枣树日内腾发强度呈单峰型变化趋势,夜间变化幅度较小且腾发贡献率低。枣树全生育期逐日腾发强度变化呈先增大后减小的趋势,花期的腾发强度最大,为4.42 mm·d^-1;全生育期腾发总量为640.83 mm,其中花期和果实生长发育期耗水量占比较大,分别为38.61%和32.72%。在小时和日时间尺度上,影响腾发强度的主要因素不完全相同,且影响程度有所差异。综合考虑各影响因素,以萌芽期、花期、果实发育期为基础,分别建立以小时、日尺度下估算腾发强度的经验模型ET₁（h）=0.153+0.004T+0.012V+0.176R_n+0.002W+0.067LAI、ET₂（d）=-3.325+0.081T+0.163R_n+0.069W+2.089LAI,拟合度R²均在0.7以上,以果实发育期与成熟期数据对模型进行检验,纳什效率系数分别达0.63、0.80。经偏相关检验,冠层净辐射（R_n）对两种尺度的腾发强度均影响最显著,因此以枣树全生育期数据量为基础,仅建立冠层净辐射（R_n）与腾发强度的回归模型ET₁（h）=-0.063 3R_n²+0.361 2R_n—0.003 7、ET₂（d）=-0.018 3R_n²+0.684 7R_n–1.642 1,R²分别为0.704 7与0.743 6,可满足缺少数据支撑情况下的腾发过程估算。这些模型明确了阿克苏地区滴灌枣树腾发机制及影响程度,可为水分管理精准化提供计算基础。     

Simulation of the growth ring density of Larix olgensis plantation wood with the ARMA model

Because growth ring data have temporal features, time series analysis can be used to simulate and reveal changes in the life of a tree and contribute to plantation management. In this study, the autoregressive(AR) and moving average modeling method was used to simulate the time series for growth ring density in a larch plantation with different initial planting densities. We adopted the Box–Jenkins method for the modeling, which was initially based on an intuitive analysis of sequence graphs followed by the augmented Dickey–Fuller stationarity test. The order p and q of the ARMA(p, q) model was determined based on the autocorrelation and partial correlation coefficient figure truncated on the respective order.Through the residual judgment, the model AR(2) was only fitted to the larch growth ring density series for the plantation with the 1.5 9 2.0 m^2 initial planting density.Because the residuals series for the other three series was not shown as a white noise sequence, the modeling was rerun. Larch wood from the initial planting density of2.0 9 2.0 m^2 was modeled by ARMA(2, 1), and ARMA((1, 5), 3) fitted to the 2.5 9 2.5 m^2 initial planting density,and the 3.0 9 3.0 m^2 was modeled by AR(1, 2, 5).Although the ARMA modeling can simulate the change in growth ring density, data for the different growth ring time series were described by different models. Thus, time series modeling can be suitable for growth ring data analysis, revealing the time domain and frequency domain of growth ring data.     

汽车道路模拟试验载荷谱的研究

室内道路模拟试验需要重现测试车辆在试验场道路行驶状态,而时域损伤编辑法与传统编制载荷谱的方法相比更能满足其需求。以测试车辆后独立悬架和副车架试验场载荷谱为原始谱,应用时域损伤编辑法,通过研究损伤时间窗口和损伤保留比例对加速谱时间保留长短和加速前后功率谱峰值差异的影响,选取适当时间窗口对原始谱进行编辑,生成台架加速谱。并从时域、幅值域、频域3个方面对原始谱和加速谱进行分析对比,验证了该方法的合理性。     

Wheat quality and productivity as affected by varieties and sowing time in Haryana, India

Of the wheat grown in North-West India the majority is consumed as traditional Indian flat bread (chapatti). Chapatti quality is important to consumers and people are willing to pay more for better quality wheat flour, but farmers do not specifically target quality outcomes as the majority of their wheat is sold with no segregation. For farmers the main objective is to harvest maximum yields, but in the last decade productivity growth for wheat yields has slowed in the areas where the wheat is grown in a double cropping pattern. Nutrient depletion and temperature-related stress are possible causes for this decline in productivity growth. Farmers meanwhile are looking to opportunities to maintain profitability and, with consumers willing to pay a higher price for better chapatti wheat, an opportunity exists for farmers to manage their wheat to improve both the yield as well as quality of wheat. In this paper we evaluate management practices that best achieve high yield and better chapatti quality, and assess the temperature environment for the winter wheat growing season. A step-wise analysis of the long-term temperature trend for sites in NW India showed that mean annual temperature has increased by 0.7-1.0 °C during the last decade. Field experiments with wheat varieties (C-306, WH-283, DBW-17, PBW-343, PBW-502, PBW-550, Raj-3765 and WH-1025) were conducted at farmers’ fields under 4 different sequential cropping rotations for the 2007-08 and 2008-09 winter seasons in Haryana (India). C-306 and WH-283 are varieties with excellent chapatti quality but are lower yielding by 15-26% than the more widely grown varieties such as PBW-343 and PBW-502. The replicated experiments involved three sowing times, these being an early sowing (late October to early November, timely sowing (mid November) and a late sowing (early December). A differential response of varieties was observed to sowing time with the yield of C-306 better whereas that of WH-283 and Raj-3765 was poor in early sown conditions. The varieties DBW-17, PBW-343 and PBW-502 were the highest yielding wheat with similar performance under early as well as timely sowing. All the varieties had lowest yield in December sowing. In general, late sowing had lower thousand grain weight but higher protein content. Of the quality measure grain hardness was the only attribute with a consistent positive correlation with chapatti quality. The chapatti score was higher for varieties C-306 and WH-283 compared to the other varieties but grain hardness and chapatti score was not much affected by sowing time. With all varieties included in the analysis there was no correlation between protein and chapatti score, but within an individual variety usually higher protein resulted in a higher chapatti score. There was no association of grain test weight or sedimentation value with chapatti score. From the results shown here it is evident that farmers will be able to manage with variety choice and timely sowing to obtain chapatti quality without losing grain yield benefits.     

1960—2007年福建省雷暴气候特征分析

[目的]研究福建省雷暴活动特点和气候规律。[方法]利用1960～2007年福建省67个气象站的逐日雷暴资料,采用气候倾向率、趋势系数等方法,分析了福建省雷暴的时空分布特征。[结果]1960～2007年福建省的雷暴日数分布呈东北—西南走向,并从沿海向内陆逐渐递增。高值区在龙岩地区,沿海岛屿最少。48年福建省雷暴日数有明显减少的趋势,中部沿海地区减少速率为3.5d/10a,内陆山区大部分为4.5d/10a,宁德北部、三明东部及南平部分地区为5.5d/10a。雷暴日趋势系数变化有明显的区域特征,特别是内陆山区比沿海减少的趋势更加明显;减少最多的地方是南平地区的北部,趋势系数达-0.65;而中部沿海地区减少趋势不太明显,系数仅为-0.15。雷暴日有明显的季节变化,3～9月是雷暴的多发期,8月达最高值,9月开始迅速减少,从10月开始一直到次年2月都较少雷暴发生。平均初雷日西北部地区早于东南部地区,平均终雷日北部地区和南部地区差异不大。由于福建省北部和西部地区初雷日出现早,终雷日出现晚,造成全年雷暴活动时间比沿海长,两者相差近一个月。[结论]该研究为重大工程项目的气候可行性论证提供科学依据,为防雷减灾提供天气气候方面的理论依据,也对进一步研究福建雷暴的形成机理奠定基础。