Cytotoxic Potential of a-Azepano- and 3-Amino-3,4-SeCo-Triterpenoids

Semi-synthetic triterpenoids, holding an amino substituted seven-membered A-ring (azepano-ring), which could be synthesized from triterpenic oximes through a Beckmann type rearrangement followed by a reduction of lactame fragment, are considered to be novel promising agents exhibiting anti-microbial, alpha-glucosidase, and butyrylcholinesterase inhibitory activities. In this study, in an attempt to develop new antitumor candidates, a series of A-ring azepano- and 3-amino-3,4-seco-derivatives of betulin, oleanolic, ursolic, and glycyrrhetinic acids were evaluated for their cytotoxic activity against five human cancer cell lines and non-malignant mouse fibroblasts by means of a colorimetric sulforhodamine assay. Azepanoallobetulinic acid amide derivative 11 was the most cytotoxic compound of this series but showed little selectivity between the different human tumor cell lines. Flow cytometry experiments showed compound 11 to act mainly by apoptosis (44.3%) and late apoptosis (21.4%). The compounds were further screened at the National Cancer Institute towards a panel of 60 cancer cell lines. It was found that compounds 3, 4, 7, 8, 9, 11, 15, 16, 19, and 20 showed growth inhibitory (GI₅₀) against the most sensitive cell lines at submicromolar concentrations (0.20–0.94 μM), and their cytotoxic activity (LC₅₀) was also high (1–6 μM). Derivatives 3, 8, 11, 15, and 16 demonstrated a certain selectivity profile at GI₅₀ level from 5.16 to 9.56 towards K-562, CCRF-CEM, HL-60(TB), and RPMI-8226 (Leukemia), HT29 (Colon cancer), and OVCAR-4 (Ovarian cancer) cell lines. Selectivity indexes of azepanoerythrodiol 3 at TGI level ranged from 5.93 (CNS cancer cell lines SF-539, SNB-19 and SNB-75) to 14.89 for HCT-116 (colon cancer) with SI 9.56 at GI₅₀ level for the leukemia cell line K-562. The present study highlighted the importance of A-azepano-ring in the triterpenic core for the development of novel antitumor agents, and a future aim to increase the selectivity profile will thus lie in the area of modifications of azepano-triterpenic acids at their carboxyl group.     

梯度铝蜂窝夹芯板的力学行为

梯度分层铝合金蜂窝板是一种有效的吸能结构,本工作在梯度铝蜂窝结构的基础上根据梯度率的概念,通过改变蜂窝芯层的胞壁长度,设计了4种质量相同、梯度率不同的铝蜂窝夹芯结构。通过准静态压缩实验,并结合非线性有限元模拟准静态及冲击态下梯度铝蜂窝夹芯结构的变形情况及其力学性能,分析对比了相同质量下梯度铝蜂窝夹芯结构在准静态下的变形模式以及冲击载荷下分层均质蜂窝结构和不同梯度率的分层梯度蜂窝结构的动态响应和能量吸收特性。结果表明:在准静态压缩过程中,铝蜂窝梯度夹芯板的变形具有明显的局部化特征,蜂窝芯的变形为低密度优先变形直至密实,层级之间的密实化应变差随芯层密度的增大而逐渐减小;在高速冲击下,梯度蜂窝板并非严格按照准静态过程中逐级变形直至密实,而是在锤头冲击惯性及芯层密度的相互作用下整体发生的线弹性变形、弹性屈曲、塑性坍塌及密实化;另外,在本工作所设计的梯度率中,当梯度率为γ₁=0.0276时,梯度蜂窝夹芯板的吸能性达到最好,相较于同等质量下的均质蜂窝夹芯板,能量吸收提高了10.63%。     

一类分数阶微积分的中值定理及应用

Riemann-Liouville分数阶微积分算子是一类带有一个函数的分数阶微积分算子的特殊情形，以Riemann-Liouville分数阶微积分算子的积分中值定理和微分中值定理为基础，我们得到了一类带有一个函数的分数阶微积分算子的积分中值定理和微分中值定理，并给出其在计算方面的一些应用。     

Fracture toughness of high strength seamless pipe steel from SE(T) and SE(B) specimens evaluated by different standards

Recently released, BS 8571:2014 standard offers an alternative for the experimental determination of fracture toughness and resistance curves of metallic materials from SE(T) specimens. Similar in stress conditions and constraint to cracked tubes, specimens in SE(T) geometry should yield less conservative toughness values than conventional high‐constraint specimens, such as SE(B) geometry. However, the convention to determine the J‐integral fracture toughness proposed in the new BS standard is different from ASTM standards. In this work, SE(T) and SE(B) specimens of similar dimensions of a tough high‐strength seamless pipe steel were tested following the BS 8571:2014 and ASTM E1820‐16 standards, respectively. Because of the different standardized definitions, SE(T) specimens yield lower fracture toughness than SE(B) specimens, which could lead to more conservative results in structural integrity analysis. This investigation also suggests the introduction of the blunting line concept in the BS 8571:2014 standard in order to minimize this problem.     

On the numerical solution of Fredholm integral equations utilizing the local radial basis function method

The current investigation describes a computational technique to solve one- and two-dimensional Fredholm integral equations of the second kind. The method estimates the solution using the discrete collocation method by combining locally supported radial basis functions (RBFs) constructed on a small set of nodes instead of all points over the analysed domain. In this work, we employ the Gauss–Legendre integration rule on the influence domains of shape functions to approximate the local integrals appearing in the method. In comparison with the globally supported RBFs for solving integral equations, the proposed method is stable and uses much less computer memory. The scheme does not require any cell structures, so it is meshless. We also obtain the error analysis of the proposed method and demonstrate that the convergence rate of the approach is high. Illustrative examples clearly show the reliability and efficiency of the new method.     

定向长钻孔整体水力压裂增透技术在赵固二矿的应用

针对赵固二矿煤层透气性低、钻孔有效影响半径小，实施定向长钻孔代替底板岩巷进行区域瓦斯治理期间钻孔工程量大、瓦斯抽采效果不理想的问题。结合煤层赋存特征及钻孔施工情况，采用定向长钻孔整体水力压裂增透技术，理论分析了合理坐封位置、压裂参数，完成200 m煤巷条带一次整体压裂，最大泵注压力24.3 MPa、累计注水量1 613 m³。并基于煤层全水分变化，考察确定了单个钻孔压裂影响范围达到巷道两帮30 m，有效改善了煤体储层特性，提高了煤层瓦斯抽采效率。在实现定向钻孔对预抽煤巷条带可靠控制的同时，最大程度降低了钻孔工程量、缩短了瓦斯治理周期，为实现矿区“以孔代巷”及高效安全开采提供了技术支撑。     

A simplified approach for the thermoelastic large deflection in the thin clamped annular sector plate

The present article is concerned with analysis of large deflection of a heated thin annular sector plate with clamped edges under transient temperature distribution using Berger’s approximate methods. The prescribed surface temperature is at the top face of the plate whereas the bottom face is kept at zero temperature. In this study, the Laplace transform as well as the classical method have been used for the solution of heat conduction equation. The thermal moment is derived on the basis of temperature distribution, and its stresses are obtained using resultant bending moment and resultant forces per unit length. The calculations are obtained for the aluminium plate in the form of an infinite series involving Bessel functions, and the numerical results for temperature, deflection, resultant bending moments, and thermal stresses have been illustrated by graphs.     

镁合金网格壁板压弯成形数值模拟及实验研究

为探索镁合金整体壁板压弯成形的可行性,以及镁合金壁板压弯成形过程中金属的流动规律,对AZ31镁合金网格壁板压弯成形进行了数值模拟和实验研究。建立了有限元数值模拟的几何模型,采用有限元计算软件对AZ31镁合金网格壁板压弯成形过程进行了数值模拟研究,分析了镁合金网格壁板压弯成形中的温度场、应变场、应力场、破坏系数等的分布规律。确定了合适的AZ31镁合金壁板压弯成形工艺参数,并对镁合金网格壁板压弯成形进行了实验研究,获得了合格的镁合金网格壁板弯曲件,并分析了镁合金网格壁板成形件尺寸精度,模拟结果与实验结果相吻合,最大相对误差为16.7%。     

基于微观孔隙结构的特低渗储层分类评价方法——以大庆油田古龙南地区为例

为了搞清研究区不同区块油井产能差异,针对研究区属于低孔￣特低渗储层的特点,将表征储层微观孔隙结构特征的平均孔喉半径作为参数引入储层分类评价中,建立了基于测井曲线的平均孔喉半径解释模型。选取孔隙度、渗透率、平均孔喉半径及有效厚度作为储层评价参数,在单因素储层分类评价的基础上,采用模糊综合评判方法对研究区储层进行综合分类。将研究区各单元储层分为Ⅰ,Ⅱ,Ⅲ类,利用单井产能情况对储层分类结果进行检验。1类井初期日产油量为3.06 t,2类井初期日产油量为1.71 t,3类井初期日产油量仅为0.36 t。初期日产油量是由不同类型单井Ⅰ,Ⅱ类储层所占比例决定的,Ⅰ,Ⅱ类储层所占比例越大,油井初期产油能力越强。该储层分类方法为研究区后期各区块开发调整提供了重要依据。     

长周期扰动应力下盘区柱内巷道锚杆支护动态响应规律

长周期扰动应力下盘区柱内巷道稳定及盘区柱整体稳定是大规模开采的关注重点。采用数值模拟方法,构建了大规模、多中段、长周期强烈开采扰动下的数值模型,建立了锚杆支护的拉伸破断、剪切破断数值力学模型,研究了不同水平、不同阶段回采过程中盘区柱内巷道锚杆支护的受力特性和盘区柱围岩的应力和塑性区发展特征。研究结果表明:不同开采阶段不同开采水平的锚杆轴力和巷道顶板变形响应明显,锚杆剪力由于变形监测部位的限制响应程度甚微,盘区柱内巷道稳定性好。盘区柱内巷道围岩偏应力场与塑性区动态演化仅在前两个中段开采时反应强烈,大规模开采结束时盘区柱仍然能够保持正常稳定。分析方法及分析结果能够对盘区柱内巷道稳定及盘区柱整体稳定做出提前预判,为盘区柱的正常使用提供安全保障。