MEDICINAL CHEMISTRY RESEARCH
·
2019
·Vol. 28
·期 9
·1388-1401
·
IF 1.72
Chen Xin,Liu Xiujie,Qiu kai,Xu Xiang,Li Caiwen,Wang Yan
According to the bio-isosterism theory, a series of N , N ’-disubstitutedphenyl-4-ethoxylbenzene-1, 3-disulfonamides ( 5a - p ) were designed and synthesized by two steps of reactions including chlorosulfonation and ammonolysis. The structures of all compounds have been confirmed by IR, 1 H-NMR, 13 C-NMR, and ESI-MS spectra. The in vitro anti-platelet aggregation activities were evaluated by Born’s test induced by adenosine diphosphate (ADP) and arachidonic acid (AA), respectively. The biological evaluation results revealed that compound 5h had the lowest IC 50 value (0.32 μM) and the highest inhibition rate (40.9 %) that of three positive control agents clopidogrel (0.41 μM, 23.5 %), aspirin (0.53 μM, 28.9 %), and picotamide (0.76 μM, 32.7 %). Afterwards, compounds with higher activities were selected to further study in vitro cytotoxicity via cell counting kit-8 (CCK-8) assay. The cytotoxicity results indicated that compound 5h had simultaneously the lowest cytotoxicity, while other compounds had no significant relationship between the anti-platelet activities and cytotoxicities. Based on above in vitro anti-platelet activity data, the SAR (Structure Activity Relationship) of the target compounds was preliminarily summarized. In general, N , N ’-disubstitutedphenyl-4-ethoxylbenzene-1, 3-disulfonamides have the potential of further study and very likely become safer and more effective anti-platelet agents.
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高影响因子
JOURNAL OF PHARMACEUTICAL SCIENCES
·
2015
·
IF 2.59
Hua Sun,Zhiguo Ma,Danyi Lu,Baojian Wu
ABSTRACT In th is study, we aimed to determine the glucuronidation potential of psoralidin in humans and to perform validation on use of psoralidin-3- O -glucuronidation as afunctional marker for UGT1A9. Glucuronidation kinetics was determined using human liver microsomes (HLMs), human intestine microsomes (HIM), and expressed UDP-glucuronosyltransferase (UGT) enzymes. The chemical structures of metabolites were determined by liquid chromatography-mass spectrometry and nuclear magnetic resonance spectroscopy analyses. Validation of psoralidin-3- O -glucuronidation as a UGT1A9 marker was performed using combined approaches including reaction phenotyping, chemical inhibition, activity correlation analysis, and determination of relative activity factor (RAF). HLM and UGT1A9 generated two monoglucuronides (9- O -glucuronide and 3- O -glucuronide) from psoralidin, whereas HIM, UGT1A1, UGT1A7, and UGT1A8 generated one only (9- O -glucuronide). Formation of 3- O -glucuronide in HLM was markedly inhibited by the UGT1A9-selective inhibitors magnolol and niflumic acid . Further, psoralidin-3- O -glucuronidation was strongly correlated with propofol-glucuronidation in a group of nine individual HLMs ( r = 0.978, p < 0.001). Strong correlation was also observed between psoralidin-3- O -glucuronidation and the UGT1A9 protein levels measured by Western blotting ( r = 0.944, p < 0.001). Moreover, UGT1A9 was responsible for 99.6% of psoralidin-3- O -glucuronidation in HLM based on the RAF approach. In conclusion, psoralidin was subjected to efficient glucuronidation, generating one or two monoglucuronides depending on UGT isozymes . Also, psoralidin-3- O -glucuronidation was an excellent in vitro marker for UGT1A9.
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PubMed
高影响因子
Environmental Science-Nano
·
2022
·Vol. 9
·期 7
·2572-2586
·
IF 9.473
Wen Chen,Xiang Ye,Qiong Tang,Ting Yu,Pengcheng Tu,Xiaodong Zheng
Nano-plastic pollution has been increasingly recognized as a key environmental issue. Nano-plastic exposure is linked to a multitude of environmental and health effects, and we have previously reported that cyanidin-3-O-glucoside (C3G) promoted discharge and reduced the biotoxicity of polystyrene (PS). This study further determines the impact of C3G on PS exposure, and investigates the role of energy metabolism in the ameliorative effects of C3G. Through a Caenorhabditis elegans (C. elegans) model, C3G was discovered to be capable of promoting discharge and alleviating biotoxicity induced by environment-relevant PS exposure. C3G was also found to restore PS-induced ATP reduction accompanied by improved mitochondrial dysfunction, suggesting involvement of energy metabolism. Using a Caco-2 cell model, we found that the molecular mechanism involves C3G protecting against PS-induced ATP reduction by activating the AMPK/SIRT1/PGC-1α signaling pathway. C3G-mediated ATP production and mitochondrial functions, which improve the activity of ABC transporters and cellular efflux of PS, may constitute the primary toxicity-alleviating mechanism through which C3G acts. Furthermore, in a mouse model administered with PS, it was discovered that C3G activates the AMPK/SIRT1/PGC-1α signaling pathway regulating the ATP level in colon tissue, in addition to the increased fecal PS discharge. These findings suggest that C3G protects against adverse effects of PS exposure on multiple organism models, and the underlying mechanism involves mitochondria-related energy metabolism and efflux.
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高影响因子
Food & Function
·
2021
·Vol. 12
·期 18
·8351-8365
·
IF 5.396
Yonglu Li,Xin Yu,Yaxuan Wang,Xiaodong Zheng,Qiang Chu
Lung cancer has been threatening human health worldwide for a long time. However, the clinic therapies remain unsatisfactory. In this study, the anti-adenocarcinoma lung cancer A549 cell line abilities of Tetrastigma hemsleyanum tuber flavonoids (THTF) were evaluated in vivo, and isobaric tags for relative and absolute quantification (iTRAQ)-based proteomic analysis was conducted to detect the protein alterations in THTF-treated solid tumors. The differentially expressed proteins were related to the cytoskeleton and mostly accumulated in the calcium signaling pathway. The in vitro study illustrated that 80 μg mL−1 THTF significantly suppressed cellular viability to approximately 75% of the control. Further results suggested that kaempferol-3-O-rutinoside (K3R), the major component of THTF, effectively triggered cytoskeleton collapse, mitochondrial dysfunction and consequent calcium overload to achieve apoptosis, which remained consistent with proteomic results. This study uncovers a new mechanism for THTF anti-tumor ability, and suggests THTF and K3R as promising anti-cancer agents, providing new ideas and possible strategies for future anti-lung cancer prevention and therapy.
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PubMed
高影响因子
JOURNAL OF THE AMERICAN CERAMIC SOCIETY
·
2024
·Vol. 107
·期 12
·8281-8290
·
IF 3.5
Shumin Duan,Zhenjun Qing,An Liu,Haiyan Li,Yan Xue
Ultra-low temperature sintered ceramics, Li 2 (Mg 1− x Ca x ) 2 (MoO 4 ) 3 ( x = 0.025–0.100), were synthesized using the solid-phase method. XRD analysis revealed that adding Ca 2+ increased the second-phase CaMoO 4 content. Particularly, Li 2 (Mg 0.975 Ca 0.025 ) 2 (MoO 4 ) 3 ceramics exhibited excellent properties: ε r = 9.31, Q × f = 55,400 GHz, and τ f = −38.9 ppm/°C. Incorporating Ca 2+ significantly improved the performance of ceramics. The microwave dielectric properties of Li 2 (Mg 0.9 Ca 0.1 ) 2 (MoO 4 ) 3 ceramics sintered at 650°C showed enhancements: ε r of 9.55, Q × f of 63,500 GHz, and τ f of −10.8 ppm/°C. The rise in ε r can be attributed to polarizability, while a higher packing fraction led to a larger Q × f value, and the reduced distortion of the [Li/Mg/CaO 6 ] octahedra enhanced the τ f value. Moreover, the increased of CaMoO 4 also positively influenced the ceramic's properties. Furthermore, in accordance with the principles of complex chemical bonding, the elevation of ionicity, lattice energy, and bond energy of the Mo–O bond contributed to the enhancement of ε r , Q × f , and τ f , respectively. Raman spectroscopy showed a positive correlation between dielectric loss and full width at half maximum of the Raman peak. Good chemical compatibility between silver and Li 2 (Mg 0.9 Ca 0.1 ) 2 (MoO 4 ) 3 ceramic was demonstrated through our co-firing experiment.
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高影响因子
JAPANESE JOURNAL OF APPLIED PHYSICS
·
2013
·
IF 1.067
Dali Wang,Zhaohua Jiang,Bin Yang,Shantao Zhang,Mingfu Zhang,Feifei Guo,Wenwu Cao
A novel xPb(Ni1/3Nb2/3)O3–(1-x)(0.30BiScO3–0.70PbTiO3) (PNN–BS–PT) ternary system was prepared by the columbite precursor method. The phase structure, microstructure, and electrical properties of ceramics of this system were investigated to identify the morphotropic phase boundary (MPB) composition of this system. The MPB with coexisting rhombohedral–tetragonal phases of PNN–BS–PT was located at approximately x=0.35, confirmed by their respective electric properties. With increasing PNN content, the coercive field EC, the Curie temperature TC, and the rhombohedral-to-tetragonal phase transition temperature TR–T were found to decrease and showed nearly linear dependences on their compositions. The enhanced properties were achieved in the MPB composition with x=0.35, which are as follows: dielectric constant εr=3160 (1 kHz), piezoelectric coefficient d33=490 pC/N, and electromechanical coupling factor kp=0.44. In addition, a large bipolar strain on the order of 0.6% was achieved for the composition when an electrical field E=40 kV/cm was applied.
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高影响因子
INORGANIC CHEMISTRY
·
2020
·
IF 4.825
Ji Wu,Ke Cao,Cai-Yan Zhang,Tao-Tao Xu,Xin-Yu Wen,Bo Li,Junxiao Yang
A palladium catalyzed selective B(3)–H activation/oxidative dehydrogenative coupling for the synthesis of bis(o-carborane)s connected with B(3)–B(3′) and B(3)–B(6′) bonds has been developed for the first time. A plausible mechanism involving stepwise activation of B(3)–H and B(3′/6′)–H bonds by PdII and PdIV was proposed. This work is the first example and the most efficient protocol for synthesis of bis(o-carborane)s connected with B(3)–B(3′) and B(3)–B(6′) bonds, which has important reference for design, synthesis, and application of bis(o-carborane)s in related fields.
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高影响因子
CERAMICS INTERNATIONAL
·
2024
·
IF 5.1
Qin Yu,Cheng Liu,Junxiao Liu,Da Huang,Tianlong Wen,Dainan Zhang,Huaiwu Zhang
In this study, NaMg 1- x Mn x (PO 3 ) 3 (0.00 ≤ x ≤ 0.0625) ceramics with low dielectric constant were prepared via the solid-state reaction method. The effects of Mn 2+ substitution on the microstructure and dielectric properties (at microwave and terahertz frequencies) of the NaMg(PO 3 ) 3 ceramics were studied by means of the Rietveld refinement, morphology, and ionic polarizability analysis. It is obtained that the NaMg 0.0975 Mn 0.025 (PO 3 ) 3 ceramic sintered at 880 °C for 4 h exhibited optimal dielectric properties at microwave frequencies, where ε r = 4.585, Q × f = 48,313 GHz (@17.228 GHz), and τ f = −40.83 ppm/°C. The Q × f and τ f values were changed by 74.2 % and 27.8 %, as compared to the values of 27,728 GHz and −56.52 ppm/°C for the pure NaMg(PO 3 ) 3 ceramic, respectively. For terahertz frequencies (0.2–1.0 THz), the ε r values were decreased to 3.79–3.98, and the tan δ values were between 0.0203 and 0.1152. All the experimental results indicate that this system exhibits great potentials both at microwave and terahertz frequencies.
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高影响因子
INDUSTRIAL CROPS AND PRODUCTS
·
2024
·
IF 5.6
Tao Zhang,Li-hong Ma,Qian-hao Zhu,Xin-yu Zhang,Chu-yi Nie,Jing-ya Zhou,Jie Sun,Feng Liu
Auxin (Indole-3-acetic acid, IAA) is essential for anther development and male fertility, but little is known about its homeostasis in developing anthers due to its complex and diverse synthesis pathways. Here, we employed transcriptomic, targeted metabolomic, and amino acid analyses on a wild type (WT) cotton ( Gossypium hirsutum ) line SD98–6 and its nearly-isogenic male sterile (MS) line SD98–6A, to delve into the relationship between IAA and anther fertility. In WT anthers, IAA homeostasis was achieved mainly through self-synthesis, conjugate hydrolysis, and polar transport, and accumulation of IAA exhibited an inverted "U" pattern with the highest content observed at the tetrad stage. In MS anthers, no IAA accumulation was observed after the meiosis stage and the IAA content remained constantly low, mainly due to reduction of the substrates (phenylalanine and tryptophan) for IAA synthesis, and significantly decreased expression of the genes involved in IAA synthesis. Meanwhile, carbohydrate metabolism pathways directly contributing to IAA synthesis and synthesis of amino acids were malfunctional in MS anthers based on the expression profile of the metabolic genes and content measurement. These results provide valuable insights into the IAA homeostasis in cotton anthers and imply that genes related to IAA homeostasis are potential targets for development of IAA-sensitive male sterile cotton lines.
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高影响因子
FOOD CHEMISTRY
·
2024
·
IF 8.5
Bohan Ma,Xiaopeng Zhu,Mohamed Aamer Abubaker,Jian Hu,Qin Shu,Yongfeng Liu
The effects of dairy sterilization techniques (65 °C/30 min, 72 °C/15 s, 85 °C/15 s, 100 °C/5 min, and 121 °C/5 s) on the epigallocatechin-3-gallate-casein (EGCG-CS) complexes were investigated through the structural and functional characteristics in this work. Fourier transform infrared spectroscopy (FT-IR) detection showed the r edshirting of the absorption peak suggested structural changes in the amide I area. Field emission scanning electron microscopy (FESEM) and viscosity measurements proved that treatments above 85 °C broke non-covalent bonds, leading to instability and low viscosity of EGCG-CS. Moreover, the values of surface hydrophobicity, solubility, and sulfhydryl group content appeared the same phenomenon of first rising then falling at higher temperatures, resulting from the CS protein exhibited obvious peptide chain stretch and hydrophobic residue exposure. Notably, the 15-s thermal treatment at 85 °C enhanced the structural stability, foaming, and emulsifying abilities of the EGCG-CS complexes, providing important technology information for industrial applications.
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PubMed
高影响因子
JOURNAL OF PORPHYRINS AND PHTHALOCYANINES
·
2021
·
IF 1.811
Safi Ullah,Keisuke Ogumi,Xuelin Zhen,Huan Wang,Yutaka Matsuo
A Suzuki–Miyaura coupling reaction was performed to synthesize 5,15- meso -bis(2-chlorothiophen-3-yl)porphyrins in order to obtain a building block for further functional porphyrins. Photophysical and electrochemical properties were investigated to understand the effect of 2-chloro substituted thiophenes which are connected at their 3-position to the meso -position of the porphyrin. A computational calculation with counterpoise method was demonstrated to estimate the relative intermolecular interaction in order to compare solubility. Installed chloro atoms at the 2-position of thiophen-3-yl decreased in intermolecular interaction which caused an increase in solubility.
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高影响因子
NANOTECHNOLOGY
·
2019
·Vol. 30
·期 16
·165402
·
IF 3.399
Xiaojie Ni,Lei Lei,Yu Yu,Junjie Xie,Ming Li,Songwang Yang,Mei Wang,Jiandang Liu,Hongjun Zhang,Bangjiao Ye
Pristine and Br-doped H2N = CHNH2Pb(I1−xBrx)3 (FAPb(I1−xBrx)3, Br content x = 0, 0.05, 0.15, 0.2, 0.3, and 0.4) films were prepared. The effect of Br-doping on phase stability, defect density, and performance of FAPb(I1−xBrx)3 was investigated by x-ray diffraction (XRD), scanning electron microscopy, ultraviolet–visible–near infrared absorbance spectroscopy, x-ray photoemission spectroscopy (XPS), Kelvin probe force microscopy (KPFM), positron annihilation spectroscopy, and current density–voltage (J–V) characteristics. The XRD measurements exhibit the enhancement of perovskite phase stability at x = 0.05. However, the phase stability decreases gradually with Br content (x) over 0.05. The increase of Br-doping content leads to the downshifting of both valence band (VB) position (indicated by XPS) and Fermi level (illustrated by KPFM). The energy level shifts are most probably due to the increase of Br 4p orbital content in VB and the change of self-doping levels. Doppler broadening spectra of positron annihilation radiation of the samples reveal that, the defect densities of Br-doped samples are much lower than that of pristine FAPbI3. For FAPb(I0.95Br0.05)3 sample, a high photoelectric conversion efficiency of 17.12% (25.7% higher than that of undoped sample) is successfully achieved. The significant enhancement of photoelectric conversion efficiency realized by Br-doping is attributed to the improvement of morphology, high phase stability, and low defect densities.
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高影响因子
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