ARCHIV DER PHARMAZIE
·
2025
·Vol. 358
·期 9
·e70089
·
IF 3.6
Leyao Chen,Xinluan Lv,Xiaoyu Chang,Ruiyong Wang
The SARS-CoV-2 pandemic has spurred global efforts to develop therapeutic approaches. The main protease (Mpro) of SARS-CoV-2 is crucial for viral replication and a key target for therapeutic development. In this study, 22 thiosemicarbazone derivatives were synthesized. Enzyme activity assays showed compound 3c exhibited obvious inhibition of Mpro, with an IC 50 value of 3.89 μM. The interaction mechanisms between thiosemicarbazone derivatives and Mpro were investigated using synchronous fluorescence, three-dimensional fluorescence, and circular dichroism spectroscopy. The fluorescence results indicate that static quenching is predominant. The equilibrium dissociation constant ( K d ) of 2.3 μM between 3c and Mpro was obtained by microscale thermophoresis. This K d value demonstrates the binding affinity of 3c for Mpro, consistent with the spectral results. Meanwhile, the binding modes and stability of thiosemicarbazone derivatives with Mpro were evaluated through molecular docking and molecular dynamics simulations, which also confirmed the stable binding between compound 3c and Mpro. This study provides valuable insights into the interaction mechanism between thiosemicarbazone derivatives and Mpro and provides clues for the design of Mpro inhibitors.
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DOI
PubMed
高影响因子
Polymer Chemistry
·
2019
·Vol. 10
·期 34
·4718-4731
·
IF 4.76
Xian Yang,Junyi Ruan,Chen Ma,Bingjie Hao,Xiaoyu Huang,Guolin Lu,Chun Feng
Self-seeding of living crystallization-driven self-assembly (CDSA) has been considered to be one of the most attractive strategies to fabricate well-defined fiber-like nanostructures with excellent control over their length and composition. To extend the scope of self-seeding of oligo(p-phenylene vinylene) (OPV)-based copolymers, the poly(N-(2-hydroxypropyl) methacrylamide) (PHPMA) segment with proven biocompatibility, synthetic flexibility and well-developed conjugation chemistry, which was synthesized by reversible addition–fragmentation chain transfer (RAFT) polymerization using an azide-containing chain transfer agent, was coupled with the alkyne-terminated OPV block by a copper-catalyzed alkyne–azide cycloaddition reaction. All OPV5-b-PHPMA (OPV5-b-PHPMA36, OPV5-b-PHPMA71 and OPV5-b-PHPMA100, the subscripts represent the number of repeat units of each block) with the same crystallizable core-forming OPV segment but different corona-forming PHPMA blocks of various chain lengths can self-assemble in ethanol to form fiber-like micelles with a length of several micrometers by a direct heating and cooling process. Uniform fiber-like micelles with a length up to ∼1 μm can be easily prepared by temperature-induced self-seeding of OPV5-b-PHPMA71. However, for self-seeding of OPV5-b-PHPMA36, ribbon-like nanostructures with a uniform and controllable length were formed, whereas relatively short fiber-like micelles with broad length distributions were formed under similar conditions for OPV5-b-PHPMA100. These results indicated that the length of the PHPMA segment played an important role in determining the self-seeding behavior of OPV5-b-PHPMA.
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高影响因子
Acupuncture in Medicine
·
2025
·
IF 2.6
Xiao-xiao Liu,Hai-hua Zhang,Jian Sun,Xiao-zhuan Chen,Yang-yang Ye,Jing-yi Quan,Lu Zhang,Lin-lin Nie,Min Li,Zhi-xing Li
Objective:To evaluate the effects of electroacupuncture (EA) on myocardial insulin resistance (IR) in Zucker diabetic fatty (ZDF) rats, an established model for type 2 diabetes mellitus (T2DM).Methods:Twenty-four ZDF-Leprfa/fa rats were randomized to: (1) ZDF group (n = 8); (2) ZDF + PIO (pioglitazone) group (n = 8); and (3) ZDF + EA group (n = 8). An additional control group of eight healthy ZDF+/fa rats was included (Lean group). We examined protein and mRNA expression levels of critical insulin signaling pathway intermediates including insulin receptor substrate (IRS)-1, phosphoinositide 3-kinase (PI3K), protein kinase B (Akt), adenosine monophosphate (AMP)-activated protein kinase (AMPK), ribosomal protein S6 kinase (p70S6K), glycogen synthase kinase 3β (GSK3β) and glucose transporter type 4 (GLUT4), as well as serum levels of interleukin (IL)-6, tumor necrosis factor (TNF)-α and C-reactive protein. Echocardiography and cardiac histology were performed.Results:Significant improvements in glucose metabolism, reflected in reduced fasting insulin levels and fasting blood glucose levels, were demonstrated after EA and PIO treatment. EA treatment also led to a notable decrease in inflammatory cytokine levels. In addition, there were marked improvements in myocardial structural integrity, as evidenced by histological analyses. Moreover, increased GLUT4 expression in myocardial tissue suggested improved insulin signaling, further supported by reductions in markers of myocardial injury such as serum troponin T type 2 (TNNT2) and B-type natriuretic peptide (BNP).Conclusion:EA ameliorated myocardial IR in a rat model of T2DM and positively impacted TNNT2 and BNP levels, as well as phosphorylation status and mRNA expression of several genes involved in the insulin signaling pathway. Our findings underscore the potential of EA to modulate multiple therapeutic targets in the treatment of myocardial IR. If these effects can be replicated clinically, EA may represent a promising non-pharmacological option for the management of cardiometabolic risks associated with diabetes.
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PubMed
高影响因子
RESEARCH ON CHEMICAL INTERMEDIATES
·
2012
·Vol. 38
·期 8
·1839-1846
·
IF 0.697
Yan Tingfeng,Hong Mei,Niu Lei,Jiang Feng,Xiao Guomin
Oxidation of 2-methylnaphthalene (2-MN) with aqueous hydrogen peroxide was conducted in acetic acid. The epoxidation pathway was investigated by increasing the CH 3 CO 3 H content and adding manganese(II) naphthenate (MnPc) as catalyst. 2-Methyl-1,4-naphthoquinone was obtained in 75.6% conversion and with 80.0% selectivity under the latter conditions. A probable mechanism in which MnPc catalyzes the oxidation of 2-MN by hydrogen peroxide in acetic acid is proposed.
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高影响因子
POLYMER
·
2013
·Vol. 54
·期 18
·4902-4908
·
IF 3.379
Peng Liu,Wang Tang,Hailiang Zhang
A series of water-soluble thermoresponsive copolymers , i.e., poly[( N -isopropylacrylamide- co -bis( N -hydroxyisopropyl pyrrolidone) 2-vinylterephthalate] [P(NIPAm- co -HIPPVTA)], with well-defined comonomer content have been synthesized via conventional free-radical copolymerization at low conversion. The liquid crystalline behavior of the copolymers was investigated using polarized light microscope and differential scanning calorimetry . The results revealed that the P(NIPAm- co -HIPPVTA) exhibit liquid crystallinity when the NIPAm content is lower than 52.2 mol%, which was obviously different from that of previous papers. In addition, thermo-responsive behaviors of copolymer also demonstrated by dynamic light scattering . The cloud points of these copolymers can be tuned over a broad range (i.e., 9.9–81.2 °C) by simply altering the molar content of the HIPPVTA. It is noted that the cloud point of the copolymers showed unexpected trend (i.e., parabolicaly other than linearly or exponentially) with the increasing of HIPPVTA content. That is, with an increase of HIPPVTA molar content, the cloud point of copolymer decreases at first and then increases.
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高影响因子
Journal of Energy Storage
·
2023
·
IF 9.4
Xiaowei Wu,Xin Dong,Ziqin Liu,Xinyi Wang,Pu Hu,Chaoqun Shang
Although the Li metal anode has a high theoretical capacity and low potential, the uncontrolled growth of Li dendrites and the significant volume variation of the Li anode prevent the practical deployment of lithium metal batteries (LMBs). To effectively control the Li dendrite growth with suppression, in this contribution, the Ni(OH) 2 nanosheets modified Prussian blue tubes (PBT/Ni(OH) 2 ) are employed to construct a three-dimensional framework (3D) on the surface of Li. The PBT can homogenize the Li + flux, while the Ni(OH) 2 nanosheets provide sufficient space to accommodate the volume change of Li. Thus, the growth of Li dendrites is largely suppressed compared to pristine Li. In detail, with the introduction of PBT/Ni(OH) 2 , the Li||Li cells provide 500 h of consistent cycling performance at 1 mA cm −2 , while the Li||Li 4 Ti 5 O 12 (LTO) cells also exhibit superior cycle reversibility over 450 cycles at 175 mAh g −1 .
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高影响因子
JOURNAL OF ALLOYS AND COMPOUNDS
·
2016
·
IF 3.014
Yan Yuan,Junxiang Wang,Zongqian Hu,Haiping Lei,Donghua Tian,Shuqiang Jiao
A Prussian blue analogue, Na 2 Co 3 [Fe(CN) 6 ] 2 , has been fabricated by a facile co-precipitation method at room temperature as a potential cathode material for both lithium-ion and sodium-ion batteries. It found that the Na 2 Co 3 [Fe(CN) 6 ] 2 nanoparticles with a primary particle size of 30–40 nm have been synthesized, and exhibited an excellent electrochemical performance , including a long cycling behavior in lithium-ion batteries and a good rate performance in sodium-ion batteries. In lithium-ion batteries, the Na 2 Co 3 [Fe(CN) 6 ] 2 nanoparticles cathode can deliver an excellent cyclic performance with 73.0% retention of initial capacity after 50 cycles at 50 mA g −1 . Moreover, when Na 2 Co 3 [Fe(CN) 6 ] 2 is used as cathode material of sodium-ion batteries, it exhibits an outstanding rate performance exceeding 75.2% retention of initial capacity after 50 cycles at 200 mA g −1 . Therefore, the Na 2 Co 3 [Fe(CN) 6 ] 2 nanoparticles can be a potential cathode candidate for the application of lithium-ion and sodium-ion batteries due to its excellent electrochemical performance, easy preparation, low cost and environment benefits.
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高影响因子
JOURNAL OF ALLOYS AND COMPOUNDS
·
2018
·
IF 3.779
Zan Jiang,Jianguang Yuan,Huanqing Han,Ying Wu
As an important member of complex hydrides , Mg(BH 4 ) 2 has a high gravimetric capacity (14.9 wt%). In this study, the Mg(BH 4 ) 2 was synthesized by the ion exchange method. Afterwards, the Mg(BH 4 ) 2 composites with different amounts (2, 5, 10, 25 and 50 wt%) of carbon nanotubes (CNTs) were prepared by mechanical milling. Effects of the CNTs on the microstructural evolution and hydrogen storage properties were investigated. The onset desorption temperature of the Mg(BH 4 ) 2 -5 wt% CNTs is decreased to lower temperature around 120 °C from 275 °C. The desorption plateau of Mg(BH 4 ) 2 -5 wt% CNTs is the highest, which ascribes that CNTs causes the reaction pathway change. Additionally, the Mg(BH 4 ) 2 -5 wt% CNTs shows the best dehydriding kinetics properties, and can desorb 6.04 wt% hydrogen within 2000 s at 300 °C. The dehydrogenation activation energy of the Mg(BH 4 ) 2 -5 wt% CNTs is decreased to 130.2 kJ/mol H 2 , which is much lower than that of pure Mg(BH 4 ) 2 .
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高影响因子
ACTA MATERIALIA
·
2023
·
IF 9.4
Weijia Guo,Yutian Lu,Zhiyu Ma,Haitao Wu,Zhenxing Yue
Dielectric ceramics with low dielectric loss in the microwave bands are key materials used in fifth/sixth-generation (5G/6G) telecommunication. Exploring the defect behavior and the broadband dielectric response of ceramics is helpful to understand the loss mechanism and develop novel low-loss microwave dielectric ceramics. In this work, Al/Nb was co-substituted for Ti 4+ in Na 1/2 Sm 1/2 TiO 3 (NST) ceramics with a perovskite structure, and the low frequency, microwave and terahertz (THz) dielectric responses were investigated. In different frequency bands, the variations of dielectric loss with substitution amount are inconsistent. The Al/Nb-substitution increases the dielectric loss in the low frequency and microwave bands, while the dielectric loss in the THz band decreases. The changes in dielectric loss are closely related to the lattice defects in Na 1/2 Sm 1/2 Ti 1– z (Al 1/2 Nb 1/2 ) z O 3 (NST- z AN, 0 ≤ z ≤ 0.1) ceramics, which are studied by thermally stimulated depolarization current (TSDC) technique. The dielectric relaxation of the defects including oxygen vacancies ( V O · · ) and defect dipoles leads to the dielectric loss in the low-frequency and microwave bands. The dielectric loss in the THz band is mainly affected by the damping of lattice vibration , which is associate with the defect concentration. This work might provide a considerable reference for the development of low-loss dielectric materials.
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高影响因子
ChemElectroChem
·
2017
·Vol. 4
·期 9
·2314-2320
·
IF 4.136
Cong Zhou,Lina Lin,Yuzhu Ma,Liyan Huang,Jun Li,Zhengping Liu,Zhaoxia Dong
The amorphous mesoporous Ni(OH) 2 hollow spheres (Ni(OH) 2 -HSs) with waxberry-like morphology were fabricated by using a facile hydrothermal method with poly(styrene-acrylic acid) spheres as the template, followed by extraction of the template. In the hydrothermal process, Ni(NO 3 ) 2 ⋅6H 2 O was employed as the precursor of Ni(OH) 2 . SEM, TEM, XPS, XRD, and N 2 adsorption-desorption isotherm techniques were used to characterize the structure and morphology of Ni(OH) 2 -HSs. The obtained Ni(OH) 2 -HSs have a uniform morphology with an average diameter of 300 nm and shell thickness of about 25 nm. The mesoporous shells of the Ni(OH) 2 -HSs are composed of amorphous Ni(OH) 2 particles. When used as an electrode, the as-prepared Ni(OH) 2 -HSs exhibit pseudocapacitive behavior with a high specific capacitance of 2559 F g −1 at a scan rate of 1 mV s −1 and a good capacitance retention of 91.8% after 1000 cycles at a current density of 5 A g −1 . These results suggest promising applications of the waxberry-like amorphous Ni(OH) 2 hollow spheres in electrode materials for supercapacitors. Graphical Caps off : Amorphous mesoporous Ni-(OH) 2 hollow spheres (Ni-(OH) 2 -HSs) with a waxberry-like morphology are fabricated through a facile hydrothermal method by using poly-(styrene-acrylic acid) spheres as a template, followed by extraction of the template. When used as an electrode, the as-prepared Ni-(OH) 2 -HSs exhibit pseudocapacitive performances with a high specific capacitance and a good capacitance retention. These results suggest promising applications of the waxberry-like amorphous Ni-(OH) 2 hollow spheres in electrode materials for supercapacitors.
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高影响因子
EUROPEAN JOURNAL OF INORGANIC CHEMISTRY
·
2019
·Vol. 2019
·期 9
·1273-1278
·
IF 2.578
Wenqiang Chen,Qun Jing,Qiaoqiao Zhang,Ming-Hsien Lee,Xuefang Lu,Ping Wei,Zhaohui Chen
Introduction transition metal with d 10 electrons and lone pair cations with large radius into phosphate systems are helpful to get new crystal structure configuration. Guided by the above method, the first lead cadmium phosphate, Pb 2 Cd 3 (PO 4 ) 2 (P 2 O 7 ), was synthesized. Pb 2 Cd 3 (PO 4 ) 2 (P 2 O 7 ) features a three-dimensional (3D) structure, in which Pb(1) 2 O 8 dimer and Pb(2)O 5 polyhedra are filled between the two-dimensional (2D) layers, which are composed of unique [Cd 6 P 8 O 30 ] groups. In the Pb II M II PO (M II = without or divalent metal ions) systems, the title compound is the first phosphate containing two different P–O groups simultaneously. The ratios of cation/phosphorus (C/P) and polymerization modes of P–O anions have a close relationship by many structural comparisons. Thermal analysis shows that Pb 2 Cd 3 (PO 4 ) 2 (P 2 O 7 ) melts congruently and is thermally stable. In addition, the UV/Vis-IR diffuse reflectance spectrum and infrared (IR) spectrum have been reported. The relationship between electronic structure and optical properties was clarified by first-principles studies. Graphical The crystal structure of a new cadmium-based compound Pb 2 Cd 3 (PO 4 ) 2 (P 2 O 7 ), containing two kinds of P–O groups, exhibits unique [Cd 6 P 8 O 30 ] ∞ layers.
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高影响因子
CHINESE JOURNAL OF ANALYTICAL CHEMISTRY
·
2016
·Vol. 44
·期 8
·1286-1290
·
IF 0.566
Li-Hua DENG,Jin-Bo DAI,Zhen-Lin XU,Jin-Yi YANG,Hong WANG,Zhi-Li XIAO,Hong-Tao LEI,Yuan-Ming SUN,Yu-Dong SHEN
To detect furaltadone metabolite 3-amino-5-morpholinomethyl-2-oxazolidinone (AMOZ) in fish sample, a Eu 3+ labeling time-resolved fluoroimmunoassay (TRFIA) was developed. The experimental conditions were optimized as follows: the AMOZA-OVA concentration was 0.25 μg mL −1 ; the antibody was diluted by 50000 folds, and the competitive reaction time was 50 min. Under the optimal conditions, the method showed a detection limit of 0.01 ng mL −1 , an IC 50 of 0.26 ng mL −1 and a linear range (IC 20 −IC 80 ) of 0.025−2.83 ng mL −1 . The spiked recoveries of AMOZ in fish at three spiked levels ranged from 78.0% to 86.0%, and the relative standard deviations were less than 15%. Good correlation between ic-TRFIA and high performance liquid chromatography-tandem mass spectrometry was obtained for spiked food samples. The proposed ic-TRFIA method was suitable for the determination of AMOZ residue in food samples.
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高影响因子
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