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11.
Maria Jos G. Fernandes Renato B. Pereira David M. Pereira A. Gil Fortes Elisabete M. S. Castanheira M. Sameiro T. Gonalves 《International journal of molecular sciences》2020,21(23)
Eugenol, the generic name of 4-allyl-2-methoxyphenol, is the major component of clove essential oil, and has demonstrated relevant biological potential with well-known antimicrobial and antioxidant actions. New O-alkylated eugenol derivatives, bearing a propyl chain with terminals like hydrogen, hydroxyl, ester, chlorine, and carboxylic acid, were synthesized in the present work. These compounds were later subjected to epoxidation conditions to give the corresponding oxiranes. All derivatives were evaluated against their effect upon the viability of insect cell line Sf9 (Spodoptera frugiperda), demonstrating that structural changes elicit marked effects in terms of potency. In addition, the most promising molecules were evaluated for their impact in cell morphology, caspase-like activity, and potential toxicity towards human cells. Some molecules stood out in terms of toxicity towards insect cells, with morphological assessment of treated cells showing chromatin condensation and fragmentation, which are compatible with the occurrence of programmed cell death, later confirmed by evaluation of caspase-like activity. These findings point out the potential use of eugenol derivatives as semisynthetic insecticides from plant natural products. 相似文献
12.
Dr. Jessica Ceramella Dr. Annaluisa Mariconda Dr. Camillo Rosano Dr. Domenico Iacopetta Dr. Anna Caruso Prof. Pasquale Longo Prof. Maria Stefania Sinicropi Prof. Carmela Saturnino 《ChemMedChem》2020,15(23):2306-2316
Cancer is going to be the first cause of mortality worldwide in the 21th century. It is considered a multifactorial disease that results from the combined influence of many genetic aberrations, leading to abnormal cell proliferation. As microtubules are strongly implicated in cellular growth, they represent an important target for cancer treatment. The well-known microtubule-targeting agents (MTAs) including paclitaxel, colchicine and vinca alkaloids are commonly used in the treatment of various cancers. However, adverse effects and drug resistance are major limitations in their clinical use. To find new candidates able to induce microtubule alteration with reduced toxic effects or drug resistance, we studied a small new series of derivatives that present imidazolinic, guanidinic, thioureidic and hydrazinic groups ( 1 – 9 ). All the compounds were tested for their antitumor activity against a panel of six tumoral cell models. In particular, compound 8 (nonane-1,9-diyl-bis-S-amidinothiourea dihydrobromide) showed the lowest IC50 value against HeLa cells, together with a low cytotoxicity for normal cells. This compound was able to induce the apoptotic mitochondrial pathway and inhibited tubulin polymerization with a similar efficacy to vinblastine and nocodazole. Taken together, these promising biological properties make compound 8 useful for the development of novel therapeutic approaches in cancer treatment. 相似文献
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针对三相整流负载产生的6k±1次谐波,提出静止坐标系下的改进型6k±1重复控制策略。同时将比例控制与改进型重复控制相结合,设计改进重复控制并联比例的复合控制结构。为减小改进重复控制中延时环节不为整数的影响,采用基于Lagrange插值近似的FIR滤波器逼近分数延时特性。最后对系统进行稳定性分析和详细设计方法进行推导。通过Matlab仿真验证改进重复控制策略能有效跟踪6k±1次谐波且具有良好的补偿效果,动态响应较快。 相似文献
14.
为提高飞机起落架载荷实测精度,以支柱式起落架结构为研究对象,探讨处理其载荷标定数据的工程方法。首先,对实际受载情况和单向加载工况标定数据的分析,挖掘出三向载荷、缓冲支柱压缩行程与应变码值间的数学关系,将预测的数学关系代入到多向工况的标定数据中,验证了它们的准确性;其次,根据两种标定数据回归方法,提出了对应使用的支柱式起落架载荷-应变标定方程的数学模型;最后,将两种标定方程代回到标定数据中,计算起落架三向载荷,所有反算载荷的误差均在可控范围内,表明标定方程满足精度要求。将标定方程代入实测数据中,实测曲线符合变化规律。该处理方法的应用能有力提高支柱式起落架的起飞-着陆载荷实测和载荷谱编制的准确度。 相似文献
15.
Isopimaric acid is a typical rosin compound and can account for 30% of the total mass of slash pine rosin. The molecular structure of isopimaric acid derivatives features an unsaturated double bond at the C13 position, opening up the possibility of their industrial polymerization. In this study, isopimaric acid (95.4%), methyl isopimarate (99.5%), and allyl isopimarate (95.1%) were prepared as highly pure monomers. New experimental results are presented and mechanisms based on the investigation of free-radical polymerization under UV irradiation are proposed. New rosin monomers for potential value-added utilization of woody biomass are also identified. © 2019 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2019 , 136, 47817. 相似文献
16.
This paper presents an efficient numerical method to solve fractional infinite-horizon optimal control problems, where the dynamic control system depends on Caputo fractional derivatives. First, by a suitable change of variable, we transform the fractional infinite-horizon optimal control problem to a finite-horizon one. Then, with the help of an approximation, we replace the Caputo derivative to integer order derivative. According to the Pontryagin minimum principle (PMP) for optimal control problems and by constructing an error function, we define an unconstrained minimization problem. In the optimization problem, we use trial solutions for state, costate and control functions where these trial solutions are constructed by using two-layered perceptron neural network. Some numerical results are introduced to explain our main results. 相似文献
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18.
探析如何让京津冀地区独特的校园文化衍生品得到创新性发展,让文创产品更容易达到共情的目的,并传递不同的校园文化价值,围绕校园文化衍生品进行创新性设计。基于对京津冀地区不同校园文化背景的调研,在文旅融合背景下分析校园文化产品的现状与发展,以及有代表性的校园文化品牌。以清华大学文创产品为例,设计出具有创新性的校园文化产品,将文化元素与产品设计相结合。运用校园特色建筑、色彩、文化背景,发挥其原创性、传播性、文化性等优势,传播学校的理念及文化,扩大校园文化传播途径。在文旅融合背景下,设计出独特的校园文化衍生产品,传承文化内涵与理念,并提高校园文化认同感与归属感,成为京津冀地区发展校园文化的趋势,从而推动文化旅游产业的发展。 相似文献
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20.
Madhab Chandra Tripathy Debasmita Mondal Karabi Biswas Siddhartha Sen 《International Journal of Circuit Theory and Applications》2015,43(6):776-792
The present work reports the realization of an analog fractional‐order phase‐locked loop (FPLL) using a fractional capacitor. The expressions for bandwidth, capture range, and lock range of the FPLL have been derived analytically and then compared with the experimental observations using LM565 IC. It has been observed that bandwidth and capture range can be extended by using FPLL. It has also been found that FPLL can provide faster response and lower phase error at the time of switching compared to its integer‐order counterpart. Copyright © 2014 John Wiley & Sons, Ltd. 相似文献