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Screening and identification of Caulis Sinomenii bioactive ingredients with dual‐target NF‐κB inhibition and β2‐AR agonizing activities
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Dan Sun Yanqi Han Weiya Wang Zengyong Wang Xiaoyao Ma Yuanyuan Hou Gang Bai 《Biomedical chromatography : BMC》2016,30(11):1843-1853
Caulis Sinomenii (CS) is a valuable traditional medicine in China. Its extract can act as an anti‐inflammatory agent and a vascular smooth muscle relaxant. However, the underlying mechanisms remain unknown. In this study, we developed a simple dual‐target method based on ultra‐performance liquid chromatography/quadrupole time‐of‐flight mass spectrometry combined with a dual‐target bioactive screening assay for anti‐inflammatory and antispasmodic activities to characterize the chemical structure of various bioactive compounds of CS rapidly. Seven potential NF‐κB inhibitors were identified, including laudanosoline‐1‐O‐xylopyranose, 6‐O‐methyl‐laudanosoline‐1‐O‐glucopyranoside, menisperine, sinomenine, laurifoline, magnoflorine and norsinoacutin. Furthermore, IL‐6 and IL‐8 assays confirmed the anti‐inflammatory effects of these potential NF‐κB inhibitors, in which laudanosoline‐1‐O‐d ‐xylopyranose and menisperine were revealed as novel NF‐κB inhibitors. Among the seven identified alkaloids, three potential β2‐adrenergic receptor agonists, including sinomenine, magnoflorine and laurifoline, were characterized using a luciferase reporter system to measure for the activity of β2‐adrenergic receptor agonists. Finally, sinomenine, magnoflorine and laurifoline were identified not only as potential NF‐κB inhibitors but also as potential β2‐adrenegic receptor agonists, which is the first time this has been reported. Molecular dynamic simulation and docking results suggest that the three dual‐bioactive constituents could not only inhibit Pseudomonas aeruginosa PAK strain‐induced inflammatory responses via a negative regulation of the Braf protein that participates in MAPK signaling pathway but also activate the β2‐adrenegic receptor. These results suggest that CS extract has dual signaling activities with potential clinical application as a novel drug for asthma. 相似文献
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肝损伤是影响公众健康的重大问题之一, 已经引起了人们越来越多的关注. 而过表达的过氧化亚硝酸盐(ONOO?)在肝损伤等疾病的发病机制中起着重要作用, 被认为是一种与早期肝损伤密切相关的生物活性分子. 因此, 为了探究ONOO?在肝损伤过程中的作用, 开发可以实现肝损伤过程中ONOO?高选择性和实时检测的分析方法具有重要意义. 本文报道了一种具有大斯托克斯位移的远红光至近红外(FR-NIR)ONOO?荧光探针. 由于该探针具有大的斯托克斯位移, 可以有效消除光谱重叠和自吸收的干扰, 从而显著提高成像的信噪比. 此外, 该探针对ONOO?具有高的灵敏度(检出限为25.8 nmol/L)和良好的选择性, 被成功用于药物诱导肝损伤过程中ONOO?信号的成像检测. 相似文献
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This paper deals with the chemotaxis-growth system: , , in a smooth bounded domain with zero-flux boundary conditions, where μ, δ, and τ are given positive parameters. It is shown that the solution exponentially stabilizes to the constant stationary solution in the norm of as provided that and any given nonnegative and suitably smooth initial data fulfills , which extends the condition in [8]. 相似文献
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Acta Mathematicae Applicatae Sinica, English Series - For the variational inequality with symmetric cone constraints problem, we consider using the inexact modified Newton method to efficiently... 相似文献
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We present simple formulas for estimating the temperatures attained during absorption of radiation in a foil. The method proposed for selecting materials for bolometers makes it possible to substantially improve the temporal resolution of the instrument. 相似文献
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Xin Xiao Shangjin He Meihan Dan Yang Su Fei Huo Wangqing Zhang 《Journal of polymer science. Part A, Polymer chemistry》2013,51(15):3177-3190
Dispersion RAFT polymerization of styrene in the alcohol/water mixture mediated with the brush macro‐RAFT agent of poly[poly(ethylene oxide) methyl ether vinylphenyl‐co‐styrene] trithiocarbonate [P(mPEGV‐co‐St)‐TTC] with similar molecular weight but different chemical composition is investigated. Well‐controlled RAFT polymerization including an initial slow homogeneous polymerization and a subsequent fast heterogeneous polymerization at almost complete monomer conversion is achieved. The molecular weight of the synthesized block copolymer increases linearly with the monomer conversion, and the polydispersity is relatively narrow (PDI < 1.3). The RAFT polymerization kinetics is dependent on the chemical composition in the brush macro‐RAFT agents, and those with high content of hydrophobic segment lead to fast RAFT polymerization. The growth of the block copolymer nano‐objects during the RAFT polymerization is explored, and various block copolymer nano‐objects such as nanospheres, worms, vesicles and large‐compound‐micelle‐like particles are prepared. The parameters such as the chemical composition in the brush macro‐RAFT agent, the chain length of the solvatophobic block, the concentration of the feeding monomer and the solvent character affecting the size and morphology of the block copolymer nano‐objects are investigated. © 2013 Wiley Periodicals, Inc. J. Polym. Sci., Part A: Polym. Chem. 2013, 51, 3177–3190 相似文献