Design,synthesis and evaluation of novel dehydroabietic acid-dithiocarbamate hybrids as potential multi-targeted compounds for tumor cytotoxicity

In the present study, novel representatives of the important group of biologically-active, dehydroabietic acid-bearing dithiocarbamate moiety, were synthesized and characterized by ¹H NMR, ¹³C NMR, HR-MS. The in vitro antiproliferative activity evaluation (MTT) indicated that these compounds exhibited potent inhibitory activities in various cancer cell lines (HepG-2, MCF-7, HeLa, T-24, MGC-803). Particularly, compound III-b possessed extraordinary cytotoxicity with low micromolar IC₅₀ values ranging from 4.07 to 38.84 µM against tested cancer cell lines, while displayed weak cytotoxicity on two normal cell lines (LO-2 and HEK 293 T). Subsequently, the potential mechanisms of representative compound III-b were elementarily investigated by Transwell experiment, which showed III-b can inhibit cancer cells migration. Annexin-V/PI dual staining showed that the compound can induce HepG-2 cells apoptosis in a dose-dependent manner. Meanwhile this apoptosis may be related to the upregulated protein expression of cleaved-caspase 3, cleaved-caspase 9, Bax and downregulated of Bcl-2 indicated by Western Blot. Later study further confirmed that ROS levels in HepG-2 cells increased significantly with the rise of concentrations. In addition, through the network pharmacology data analyzing, the core targets and signaling pathways of compound III-b for treatment of liver neoplasms were forecasted. Molecular docking model showed that compound III-b had high affinity with hub targets (CASP3, EGFR, HSP90AA1, MAPK1, ERBB2, MDM2), suggesting that compound III-b might target the hub protein to modulate signaling activity. Taken together, these data indicated that dehydroabietic acid structural modification following the “Molecular hybridization” principle is a feasible way to discover the potential multi-targeted antitumor compounds.     

A Structural Entropy Measurement Principle of Propositional Formulas in Conjunctive Normal Form

The satisfiability (SAT) problem is a core problem in computer science. Existing studies have shown that most industrial SAT instances can be effectively solved by modern SAT solvers while random SAT instances cannot. It is believed that the structural characteristics of different SAT formula classes are the reasons behind this difference. In this paper, we study the structural properties of propositional formulas in conjunctive normal form (CNF) by the principle of structural entropy of formulas. First, we used structural entropy to measure the complex structure of a formula and found that the difficulty solving the formula is related to the structural entropy of the formula. The smaller the compressing information of a formula, the more difficult it is to solve the formula. Secondly, we proposed a λ-approximation strategy to approximate the structural entropy of large formulas. The experimental results showed that the proposed strategy can effectively approximate the structural entropy of the original formula and that the approximation ratio is more than 92%. Finally, we analyzed the structural properties of a formula in the solution process and found that a local search solver tends to select variables in different communities to perform the next round of searches during a search and that the structural entropy of a variable affects the probability of the variable being flipped. By using these conclusions, we also proposed an initial candidate solution generation strategy for a local search for SAT, and the experimental results showed that this strategy effectively improves the performance of the solvers CCAsat and Sparrow2011 when incorporated into these two solvers.     

数学建模对高中生构建数学底层思维的作用及其教学实施建议

数学底层思维即用数学的眼光观察世界、用数学的思维分析世界以及用数学的语言表达世界,是人们面对自然和社会中纷繁多样的现象和问题时,所展现的自发的、不依赖监督的、融汇数学学科核心素养的思维方式.作为国家高中新课程标准中数学六大核心素养之一的数学建模,是培养学生数学底层思维的良好载体,对人才培养和社会发展均起到良好的促进作用.本文主要阐述了数学建模对高中生构建数学底层思维的作用,并结合教学实例给出教学实施建议.     

基于模糊综合评判的大学数学考核方式改革

独立高校数学课程的开设旨在让学生掌握数学知识的基础上,提高数学应用能力.然而现行的考核方式存在重考试结果,轻学习过程等问题.从传统考核方式入手,指出其不足之处,基于模糊综合评判法建立新型评价体系和数学模型,通过试点运行验证了新的考核方式的可行性、客观性、合理性和科学性.     

不同补贴对象下闭环供应链信息共享价值研究

在一个制造商和一个零售商组成的二级闭环供应链中,为研究政府补贴下供应链需求信息共享对决策的影响及共享价值,针对两种补贴对象,构建并求解无信息共享和信息共享博弈模型,并进行仿真验证.研究表明:1)两种补贴对象下,制造商均能从信息共享中获益,零售商仅在绿色成本和回收成本较低时才会从信息共享中获益;绿色成本和回收成本稍高时,设计基于谈判势力的信息补偿机制能有效促进零售商共享信息.2)产品绿色度和回收率随预测需求量的提高而提高,批发价和零售价仅在回收成本较低时,才会随预测需求量的提高而提高.3)在仅补贴一方情况下,当补贴对象为低补贴一方时,两个主体所获的信息共享价值大;若对两者的补贴均较低,两个主体均希望补贴对象为零售商;若对两者的补贴均较高,零售商不愿共享需求信息.     

基于PI法的门源MS6.4地震前震中附近地震热点图像异常变化研究

基于1980年以来青海省和甘肃省区域地震台网的定位地震目录，分析了研究区最小完备震级，选取空间网格尺度为0.2°×0.2°、地震活动异常学习时间段和预测时间段均为3 a，应用图像信息（PI）法，分析了门源M_S6.4地震发生前震中附近地震热点图像的异常变化过程。结果表明，在2013年1月1日至2016年1月1日的预测时间窗内，冷龙岭断裂和祁连山北缘断裂附近存在明显的地震热点，且地震热点图像颜色偏深，发震概率较高，向前滑动至2014年1月1日至2017年1月1日，2015年1月1日至2018年1月1日和2016年1月1日至2019年1月1日3个预测时间窗，此两断裂附近仍存在地震热点，地震热点图像颜色逐渐由深变浅，而门源M_S6.4地震就落在PI法得到的地震热点内。门源M_S6.4地震前存在明显的地震热点，且地震热点相对集中，地震热点图像颜色由深变浅，震后消失；在祁连山北缘断裂附近，地震热点持续存在，分布较集中，地震热点图像颜色也呈由深变浅的过程。未来需关注祁连山北缘断裂，附近有发生强震的可能。     

Corners of self-conjugate (s,s + 1)-cores and (s‾,s+1‾)-cores

In this paper, we describe a result on self-conjugate $(s,s+1)$-core partitions with the fixed number of corners. We also define shifted corners of a distinct partition and find formulas for the number of $(\stackrel{￣}{s},\stackrel{￣}{s+1})$-core partitions and the number of $(s,s+1)$-core shifted Young diagrams with the fixed number of shifted corners.     

改革开放以来高中化学教科书物质结构内容选择及演变

以1978年改革开放以来人民教育出版社出版的5套高中化学教科书作为研究对象，梳理其物质结构内容的演变，发现近40年来高中化学教科书中物质结构内容选择呈钟摆现象，同时其内容组织的结构化理念日益清晰。此外，为新时期我国高中化学教科书的编写提供了一些建议。