Xanthohumol for Human Malignancies: Chemistry,Pharmacokinetics and Molecular Targets

Xanthohumol (XH) is an important prenylated flavonoid that is found within the inflorescence of Humulus lupulus L. (Hop plant). XH is an important ingredient in beer and is considered a significant bioactive agent due to its diverse medicinal applications, which include anti-inflammatory, antimicrobial, antioxidant, immunomodulatory, antiviral, antifungal, antigenotoxic, antiangiogenic, and antimalarial effects as well as strong anticancer activity towards various types of cancer cells. XH acts as a wide ranging chemopreventive and anticancer agent, and its isomer, 8-prenylnaringenin, is a phytoestrogen with strong estrogenic activity. The present review focuses on the bioactivity of XH on various types of cancers and its pharmacokinetics. In this paper, we first highlight, in brief, the history and use of hops and then the chemistry and structure–activity relationship of XH. Lastly, we focus on its prominent effects and mechanisms of action on various cancers and its possible use in cancer prevention and treatment. Considering the limited number of available reviews on this subject, our goal is to provide a complete and detailed understanding of the anticancer effects of XH against different cancers.     

Osteosarcoma Pathogenesis Leads the Way to New Target Treatments

Osteosarcoma (OS) is a rare condition with very poor prognosis in a metastatic setting. Basic research has enabled a better understanding of OS pathogenesis and the discovery of new potential therapeutic targets. Phase I and II clinical trials are already ongoing, with some promising results for these patients. This article reviews OS pathogenesis and new potential therapeutic targets.     

The (Poly)Pharmacology of Cannabidiol in Neurological and Neuropsychiatric Disorders: Molecular Mechanisms and Targets

Cannabidiol (CBD), the major nonpsychoactive Cannabis constituent, has been proposed for the treatment of a wide panel of neurological and neuropsychiatric disorders, including anxiety, schizophrenia, epilepsy and drug addiction due to the ability of its versatile scaffold to interact with diverse molecular targets that are not restricted to the endocannabinoid system. Albeit the molecular mechanisms responsible for the therapeutic effects of CBD have yet to be fully elucidated, many efforts have been devoted in the last decades to shed light on its complex pharmacological profile. In particular, an ever-increasing number of molecular targets linked to those disorders have been identified for this phytocannabinoid, along with the modulatory effects of CBD on their cascade signaling. In this view, here we will try to provide a comprehensive and up-to-date overview of the molecular basis underlying the therapeutic effects of CBD involved in the treatment of neurological and neuropsychiatric disorders.     

Aminoacyl-tRNA Synthetases as Valuable Targets for Antimicrobial Drug Discovery

Aminoacyl-tRNA synthetases (aaRSs) catalyze the esterification of tRNA with a cognate amino acid and are essential enzymes in all three kingdoms of life. Due to their important role in the translation of the genetic code, aaRSs have been recognized as suitable targets for the development of small molecule anti-infectives. In this review, following a concise discussion of aaRS catalytic and proof-reading activities, the various inhibitory mechanisms of reported natural and synthetic aaRS inhibitors are discussed. Using the expanding repository of ligand-bound X-ray crystal structures, we classified these compounds based on their binding sites, focusing on their ability to compete with the association of one, or more of the canonical aaRS substrates. In parallel, we examined the determinants of species-selectivity and discuss potential resistance mechanisms of some of the inhibitor classes. Combined, this structural perspective highlights the opportunities for further exploration of the aaRS enzyme family as antimicrobial targets.     

应用膨胀算法提取目标的直接定位算法

为了解决被动雷达系统中的多发射源定位问题，提出了一种基于多重信号分类(MUSIC)算法和图像膨胀(IE)算法的直接定位方法。该方法结合了谱分析中的MUSIC思想，通过对接收量测协方差矩阵进行特征分析求解目标的位置。首先，在目标个数未知的前提下，利用Akaike信息准则(AIC)来确定模型阶数；然后，推导了基于MUSIC的定位代价函数；之后，利用图像膨胀算法处理得到的代价函数平面；最后，膨胀处理后的输出为目标个数及目标位置的估计值。提出的算法有效地解决了目标检测及提取的问题，能够确定多个目标的位置坐标，为后续的定位性能分析提供可能性，也保证了算法的完整性。进一步地分析了多个临近目标情况下影响目标提取性能的主要因素。     

Vibration analysis and identification of breathing cracks in beams subjected to single or multiple moving mass using online sequential extreme learning machine

In this paper, a novel approach was presented to vibration analysis and identification of breathing cracks in Timoshenko beam under single or multiple moving mass. Dynamic strain energies (DSEs) and translational accelerations in beam structures under moving mass were used as forward problem and application of an emergent learning algorithm called the online sequential extreme learning machine algorithm as inverse problem to predict crack depths and locations. To demonstrate the potential of the proposed vibration analysis over existing ones, two validation studies have been done. To evaluate the proposed method to identify breathing cracks, two examples, namely, clamped–clamped beam and two span continuous beams have been studied. Also, the effect of the discrepancy in stiffness between the finite-element model and the actual tested dynamic system has been investigated. Another examination has been performed in which moving mass with different speeds are utilized. Also, the effect of multi mass passing through the beam has been studied. The obtained results indicated that the proposed method could identify the breathing cracks existence and severity in the beam under moving mass using DSE and accelerations, which may be noisy or noise free.     

基于时空的弱点状运动目标检测技术

如何在复杂背景下持续有效地检测目标位置,一直是研究者们需要面对的主要挑战。本文在研究红外点状移动目标特征的基础上,根据目标无纹理,无形状的特性,提出一种改进的形态学目标增强算法,并利用目标连续时空不变性检测目标。首先,建立多尺度的图像金字塔,在每层上采用改进的形态学算法快速、粗糙定位小目标。然后进一步的根据目标在时空上的位置相关性,提出基于目标运动特征分析的精确检测方法。得到精确稳定的检测结果。最后实验结果表明与经典的形态学检测算法及其他算法相比,该技术能更有效地检测弱小目标,具有更高的鲁棒性。     

雷电通道水平电场影响因素分析

影响雷电通道产生的水平电场因素众多,分析其影响因素对电力系统的雷电防护具有重要意义。文中利用运动电荷电磁场方程求解得到闪电回击通道的水平电场和方位磁场,并结合C-R 算法,得到了有限电导率地面上方的水平电场。依据运动电荷电磁场方程的特征分析了不同回击速度、不同距离、不同电导率对雷击产生的水平电场的影响。得出以下结论:水平电场随回击速度增大而减小;水平电场波形呈双极性特征且水平距离越大或电导率越小负向偏移越明显。这些研究结论为输电线路雷电过电压计算打下良好的基础。与其他方法相比,本文方法可以避免远距离电磁场计算中的震荡问题和积分方程的奇异问题。     

深埋矿体移动带三维圈定方法及应用

针对深埋矿山开采移动带二维圈定方法工作量大、精度低且难以满足日益增长的经济效益需求的问题，提出了一种深埋复杂矿体移动范围三维确定方法。结合沙岭金矿千米深井工程实例，在移动范围确定过程中，借助先进的3D建模技术获得三维矿山模型。该模型可以实现各类地质体的可视化，直观地展示其形态与产状，清晰地反映各构成因素间的相互关系。在3D模型中截取的特征剖面与经典移动带圈定岩移参数获取方法相结合，能轻松获得各特征剖面上的岩移参数值。通过给定的岩移参数值进而确定各特征剖面上的地表移动边界点，将各移动边界点连接即可实现矿山移动范围的圈定。研究结果表明，基于三维地质建模技术的移动带圈定方法合理可行，确定的纱岭金矿地表移动带能够兼顾安全生产与经济效益，为矿山生产开发奠定了有益基础，为类似矿山提供了有益借鉴。