EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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2022
·
IF 7.088
Qidong Tang,Ting Peng,Jie Hu,Tao Zhang,Pengqin Chen,Daoxing Chen,Yunjie Wang,Lingfeng Chen,Linjiang Tong,Yi Chen,Hua Xie,Guang Liang
Pan-HER inhibitors exhibit extensive biological activity and offer unique advantages and usually bind to targets in an irreversible manner. Owing to the off-target toxicity of irreversible inhibitors, reversible pan-HER inhibitors are desirable. Herein, we describe the process of N -(ring structure fused phenyl)quinazoline-4-amine-based design, synthesis, and biological evaluation of pan-HER inhibitors in vitro and in vivo . Compound C5 , with the molecular skeleton of N -(3-bromo-1 H -indol-5-yl)-quinazolin-4-amine, displayed irreversible binding just like other effective pan-HER inhibitors. To our surprise, compound C6, which possessed the same skeleton, was found to be a high-strength reversible pan-HER inhibitor. This compound was capable of inhibiting HER1s (such as EGFR T790M/L858R and WT), HER2, and HER4 and can be considered as a breakthrough in the development of pan-HER inhibitors. Altogether, N -(3-bromo-1 H -indol-5-yl)-quinazolin-4-amine can serve as an effective molecular skeleton for developing both reversible and irreversible pan-HER inhibitors in the following discovery of antitumor drugs .
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高影响因子
MICROCHEMICAL JOURNAL
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2023
·
IF 4.8
Xiaoqi Chen,Aiyou Huang,Peng Ju
The integration of sterilization capabilities into sensing platforms is a crucial step in mitigating the significant health risks associated with the persistence of pathogenic bacteria. In this study, we developed a photoelectrochemical (PEC) pathogenic bacteria sensing platform integrated with sterilization function. The platform was based on the g-C 3 N 4 nanosheets decorated with AuNPs and Poly(3-thiophene boronic acid) (PTBA). The incorporation of AuNPs and PTBA proved highly beneficial for enhancing the PEC and photocatalytic performance of bulk g-C 3 N 4 . Leveraging the boronic acid group of PTBA, we achieved the selective capture of pathogenic bacteria on the surface of the electrode. The platform showed a high detection sensitivity towards Escherichia coli ( E. coli ) with a low limit detection (30.5 cfu/mL). Furthermore, the sensing platform demonstrated an exceptional antibacterial rate (99.9 %) resulting from the photoelectrocatalytic effect of PTBA/AuNPs/g-C 3 N 4 . This research presents a potential application of the platform as a self-cleaning biosensor for pathogenic diagnosis.
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2023
·
IF 6.1
Teng Wei,Dengfeng Tan,Shengyue Zhong,Hong Zhang,Zeyuan Deng,Jing Li
This study investigated differences in absorption and metabolism between 1,3-oleate-2-palmitate glycerol (OPO) and 1-oleate-2-palmitate-3-linoleate glycerol (OPL) using C57BL/6J mice. OPL was associated with higher postprandial plasma total triacylglycerol (TG), low-density lipoprotein cholesterol (LDL-C) concentrations, and the ratio of LDL-C to high-density lipoprotein cholesterol (HDL-C) compared to those of OPO (p > 0.05). OPO significantly increased postprandial oleic acid (OA) concentrations compared to OPL over the entire monitoring period (p < 0.05), while OPL significantly elevated linoleic acid (LA) levels compared to OPO (p < 0.05). After 1 month of feeding, the mice in both OPO and OPL groups showed lower final weight, weight gain, and liver TG, LDL-C, and LDL/HDL concentrations compared to the control (soybean oil) group. Lipidomics results showed that OPO increased the biosynthesis of very long-chain fatty acids and decreased the abundance of AcCa (16:1), AcCa (18:2), AcCa (18:1), AcCa (16:0), CarE (16:0), and CarE (16:1) relative to OPL. These lipid metabolites were positively correlated with liver TG, LDL-C, and LDL/HDL levels and negatively related to peroxisome proliferator-activated receptors α (PPARα) and acyl-CoA oxidase (ACOX1) expression. This study showed differences in physiologic functions between OPO and OPL and provided support for the future application of OPL in infant formula.
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高影响因子
Journal of Materiomics
·
2023
·
IF 9.4
Ying Zhang,Meng-Han Yan,Zhi-Fei Zhang,Hai-Rui Bai,Peng Li,Wei-Fang Han,Ji-Gong Hao,Wei Li,Yu-Chao Li,Chun-Ming Wang,Peng Fu
The increase in energy consumption and its collateral damage on the environment has encouraged the development of environment-friendly ceramic materials with good energy storage properties. In this work, (1– x )Na 0.5 Bi 0.5 TiO 3 - x Ca(Mg 1/3 Nb 2/3 )O 3 ceramics were synthesized by the solid-state reaction method. The 0.88Na 0.5 Bi 0.5 TiO 3 -0.12Ca(Mg 1/3 Nb 2/3 )O 3 ceramic exhibited a high recoverable energy storage density of 8.1 J/cm 3 and energy storage efficiency of 82.4% at 550 kV/cm. The introduction of Ca(Mg 1/3 Nb 2/3 )O 3 reduced the grain size and increased the band gap, thereby enhancing the breakdown field strength of the ceramic materials. The method also resulted in good temperature stability (20–140 °C), frequency stability (1–200 Hz), and fatigue stability over 10 6 cycles. In addition, an ultrahigh power density of 187 MW/cm 3 and a fast charge-discharge rate ( t 0.9 = 57.2 ns) can be obtained simultaneously. Finite element method analysis revealed that the decrease of grain size was beneficial to the increase of breakdown field strength. Therefore, the 0.88Na 0.5 Bi 0.5 TiO 3 -0.12Ca(Mg 1/3 Nb 2/3 )O 3 ceramics resulted in high energy storage properties with good stability and were promising environment-friendly materials for advanced pulsed power systems applications.
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Small
·
2023
·
IF 13.3
Wei Yang,Qi Liu,Lijuan Hou,Qiang Yang,Daobin Mu,Guoqiang Tan,Li Li,Renjie Chen,Feng Wu
Iron-based sulfate cathodes of alluaudite Na 2+2 δ Fe 2− δ (SO 4 ) 3 (NFS) in sodium-ion batteries with low cost, steady cycling performance, and high voltage are promising for grid-scale energy storage systems. However, the poor electronic conductivity and the limited understanding of the phase-evolution of precursors hinder obtaining high-rate capacity and the pure phase. Distinctive NFS@C@ n %CNTs ( n = 1, 2, 5, 10) sphere-shell conductive networks composite cathode materials are constructed creatively, which exhibit superior reversible capacity and rate performance. In detail, the designed NFS@C@2%CNTs cathode delivers an initial discharge capacity of 95.9 mAh g −1 at 0.05 C and up to 60 mAh g −1 at a high rate of 10 C. The full NFS@C@2%CNTs//HC cell delivers a practical operating voltage of 3.5 V and mass-energy density of 140 Wh kg −1 at 0.1 C, and it can also retain 67.37 mAh g −1 with a capacity retention rate of 96.4% after 200 cycles at 2 C. On the other hand, a novel combination reaction mechanism is first revealed for forming NFS from the mixtures of Na 2 Fe(SO 4 ) 2 · n H 2 O ( n = 2, 4) and FeSO 4 ·H 2 O during the sintering process. The inspiring results would provide a novel perspective to synthesize high-performance alluaudite sulfate and analogs by aqueous methods.
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TOXICOLOGY
·
2021
·
IF 4.221
Bobo Yang,Wenjun Zhao,Changsheng Yin,Yu Bai,Suhua Wang,Guangwei Xing,Fang Li,Jinsong Bian,Michael Aschner,Jiyang Cai,Haifeng Shi,Rongzhu Lu
Hydrogen sulfide (H 2 S) as the third gasotransmitter molecule serves various biological regulatory roles in health and disease. Acrylonitrile (AN) is a common occupational toxicant and environmental pollutant, causing brain and liver damage in mammals. The biotransformation of AN is dependent-upon reduced glutathione (GSH), cysteine and other sulfur-containing compounds. However, the effects of AN on the endogenous H 2 S biosynthesis pathway have yet to be determined. Herein, we demonstrated that a single exposure to AN (at 25, 50, or 75 mg/kg for 1, 6 or 24 h) decreased the endogenous H 2 S content and H 2 S-producing capacity in a dose-dependent manner, both in the cerebral cortex and liver of rats in vivo . In addition, the inhibitory effects of AN (1, 2.5, 5, 10 mM for 12 h) on the H 2 S content and/or the expression of H 2 S-producing enzymes were also found both in primary rat astrocytes and rat liver cell line (BRL cells). Impairment in the H 2 S biosynthesis pathway was also assessed in primary rat astrocytes treated with AN. It was found that inhibition of the cystathionine-β-synthase (CBS)/3-mercaptopyruvate sulfurtransferase (3-MPST)-H 2 S pathway with the CBS inhibitor or 3-MPST-targeted siRNA significantly increased the AN-induced (5 mM for 12 h) cytotoxicity in astrocytes. In turn, CBS activation or 3-MPST overexpression as well as exogenous NaHS supplementation significantly attenuated AN-induced cytotoxicity. Taken together, endogenous H 2 S biosynthesis pathway was disrupted in rats acutely exposed to AN, which contributes to acute AN neurotoxicity in primary rat astrocytes.
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DRUG DEVELOPMENT RESEARCH
·
2020
·Vol. 82
·期 3
·404-411
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IF 1.902
Xiaolong Sun,Xu Wang,Zhenyu Zhao,Jing Chen,Cheng Li,Gang Zhao
Diabetic foot ulcer (DFU) is an invariably common complication of diabetes, characterized by delayed wound healing process and increased inflammation. Evidence has indicated that paeoniflorin exerts an anti-inflammatory effect in diabetic retinopathy. The current work was aimed to investigate the effect of paeoniflorin on inflammation and wound healing in DFU. DFU rat models by streptozotocin and skin biopsy punch, as well as high glucose-treated human immortalized keratinocytes (HaCaT) were established. Levels of blood glucose, wound contraction and proinflammatory cytokine were detected after paeoniflorin administration. Several essential targets associated with the NF-κB and Nod-like receptor protein-3 (NLRP3) signaling pathways were examined. Results showed markedly down-regulation of interleukin (IL)-1β, IL-18 and tumor necrosis factor-alpha in paeoniflorin-treated DFU rats. Paeoniflorin decreased the expression levels of chemokine receptor CXCR2, nuclear NF-κB and p-IκB (Ser36), as well as increased IκB level. Histological analysis and immunostaining showed lower inflammatory cells with decreased NLRP3 and cleaved caspase-1 levels following paeoniflorin treatment. Further in vitro evidence confirmed that paeoniflorin efficiently inhibited NLRP3 and NF-κB-mediated inflammation in DFU by inhibiting CXCR2. These findings are suggestive of greatly attenuated wound inflammation and better wound healing in paeoniflorin-treated DFU rats. Our study demonstrates that paeoniflorin is a potential therapeutic agent for DFU.
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JOURNAL OF ALLOYS AND COMPOUNDS
·
2020
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IF 4.65
Tong Zou,Xinxin Xing,Yue Yang,Zhezhe Wang,Zidong Wang,Rongjun Zhao,Xu Zhang,Yude Wang
Copper, as an essential element in human body, can have adverse impact on environment and healthy individuals if it is excessive. So it is necessary to establish a rapid and effective method for detecting Cu 2+ . In this work, we describe a method for determination of Cu 2+ based on water-soluble ZnO quantum dots (QDs) modified with (3-aminopropyl)triethoxysilane (APTEs). The ZnO QDs functionalized with APTEs (NH 2 –ZnO QDs) synthesized by a simple sol-gel method and displayed strong yellow-green fluorescence with a peak at 535 nm under 350 nm excitation. High-resolution transmission electron microscopy, Fourier transform infrared spectroscopy , luminescence, and UV–visible absorption spectroscopy were used to characterize the NH 2 –ZnO QDs. In addition, the emission from NH 2 –ZnO QDs was selectively quenched upon addition of Cu 2+ . Therefore, this finding was used to design a fluorescent probe based on NH 2 –ZnO QDs to detect Cu 2+ in water solution, and the linear relationships were 2–20 nM and 1–100 μM respectively, with detection limit for Cu 2+ at 1.72 nM (on the basis of 3σ/slope criterion). This fluorescent probe had also been applied in real water sample to testify its availability in drinking water. Furthermore, the quenching mechanism was studied by measurements of UV–visible absorption spectra and fluorescent lifetime of ZnO QDs, which may be attributed to the aggregation induced by Cu 2+ and the dynamic quenching existing energy transfer between QDs and Cu 2+ .
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RAPID COMMUNICATIONS IN MASS SPECTROMETRY
·
2021
·Vol. 35
·期 19
·e9169
·
IF 2.419
Zhang-Na Qin,Jun Ding,Qiong-Wei Yu,Ping Zhou,Yu-Qi Feng
Rationale 3-Monochloropropane-1,2-diol (3-MCPD) is a well-known contaminant formed in food thermal processing, which could be found in a variety of foodstuffs. Due to its potential carcinogenicity, it was essential to quickly develop a rapid and high-throughput analytical method to monitor 3-MCPD in foodstuffs, which is described in this study. Methods 3-MCPD was extracted from foodstuffs and then was derivatized with a boronic acid–modified C 60 (B-C 60 ) through the boronic acid-diol reaction. Microwave heating was used to accelerate the derivatization reaction. Mass spectrometry (MS) analysis was conducted using matrix-assisted laser desorption/ionization-MS (MALDI-MS). The application of the method was validated using various smoked food samples. Results The chemical derivatization of 3-MCPD with B-C 60 enabled the addition of a C 60 -tag to 3-MCPD. High-throughput analysis of the sample within 0.5 h was realized. A good linear range from 0.02 to 1.5 μg mL −1 for 3-MCPD was obtained, with a detection limit of 0.005 μg mL −1 . The recoveries in spiked foodstuffs ranged from 85.4% to 115.1% with relative standard deviations of 2.0%–14.2%. This method was successfully applied to detect 3-MCPD in smoked foodstuffs. Conclusions A quantitative method was developed for the detection of 3-MCPD in foodstuffs using B-C 60 derivatization combined with MALDI-MS strategy. This proposed method may serve as a potential platform for the rapid and high-throughput analysis of 3-MCPD in foodstuffs for the purpose of food safety control.
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JOURNAL OF MOLECULAR LIQUIDS
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2021
·
IF 6.165
Tingting Guo,Xiaojuan Wang,Yang Shu,Jianhua Wang
In this study, the behavior of 1-alkyl-3-methylimidazolium dicyanamide ionic liquids (ILs) with ethyl, butyl, hexyl, octyl, and decyl side-chains was evaluated to gain a deeper insight into the potential hazards posed by ILs to the environment and organisms. The effects of the alkyl side-chain length on the interactions between the ILs and bovine serum albumin (BSA), the cytotoxicity and antibacterial performance of the ILs was evaluated. The BSA binding ability of the ILs increased with increasing alkyl side-chain length, and the binding constants of the ILs increased from 1.80 L/mol for 1-ethyl-3-methylimidazolium dicyanamide to 196 L/mol for 1-decyl-3-methylimidazolium dicyanamide. IL binding with BSA was a spontaneous process initiated by hydrophobic forces. This was confirmed using circular dichroism spectra, dynamic light scattering measurements and molecular docking simulations. The results of the cytotoxicity and antimicrobial activity of ILs demonstrated that the increase in alkyl side-chain length increased IL toxicity. The effects of the alkyl side-chain length of 1-alkyl-3-methylimidazolium tetrafluoroborate ILs on the interactions between ILs and BSA and cytotoxicity of the ILs were also evaluated. Furthermore, we demonstrated that tetrafluoroborate-based ILs were more toxic than dicyanamide-based ILs. Herein, we thoroughly describe the effects of the alkyl side-chain length on the properties of ILs and provide background information for future studies on the properties of carbon dots fabricated using ILs as precursors.
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JOURNAL OF MATERIALS SCIENCE & TECHNOLOGY
·
2021
·
IF 8.067
Xudong Qi,Kai Li,Enwei Sun,Bingqian Song,Da Huo,Jiaming Li,Xianjie Wang,Rui Zhang,Bin Yang,Wenwu Cao
Recently, the anomalous photovoltaic effect of ferroelectric materials has attracted considerable attention in the construction of efficient solar cells owing to the above-bandgap photovoltage of these materials. In this study, we investigate the anomalous photovoltaic effect of relaxor-based ferroelectric Pb(In 1/2 Nb 1/2 )O 3 -Pb(Mg 1/3 Nb 2/3 )O 3 -PbTiO 3 (PIMN-PT) ceramics with large remnant polarization and a narrow optical bandgap. Excellent photovoltaic performance with an ultrahigh open-circuit voltage of 23 V (575 V/cm) is achieved, which is higher than the open-circuit voltages of all reported polycrystalline materials with similar thickness. The phase structure, microstructure morphology, domain structure, ferroelectric and optical characteristics are analyzed, which could provide clues to the origin of the ultrahigh open-circuit voltage of PIMN-PT ceramics. The results suggest that the relaxor-based ferroelectric PIMN-PT system is a potential candidate for photovoltaic solar energy conversion devices.
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JOURNAL OF LIQUID CHROMATOGRAPHY & RELATED TECHNOLOGIES
·
2021
·
IF 1.312
Yan Du,Jinhua Hu,Zhixiong Hu,Weinong Zhang,Yutang Qi,Yanpeng Zhang,Xiaomin Li,Yi Liu
In this paper, a sensitive method for the determination of 3-chloro-1,2-propanediol (3-MCPD) by high performance liquid chromatography-fluorescence detection (HPLC-FLD) was established, in which 9-(2-Hydroxypropyl) adenine (HP-Ade) was selected as the fluorescent derivatization reagent because of its good water solubility and hydrophobicity. The principle of the method lies in the origination of chloroacetaldehyde with the periodate oxidation of 3-MCPD and its' fluorescence derivatization by HP-Ade to produce a strong fluorescent substance, name as 1-N6-vinylidene-9-(2-hydroxypropyl)adenine (ε-HP-Ade), used for quantitative determination of 3-MCPD by HPLC-FLD. Some mobile phase conditions and incubation parameters related with the method features were studied and optimized. Under the optimal conditions, the method shows high sensitivity, good linearity (r2 = 0.999) and good repeatability (RSD% between 1.04% and 2.55%), the detection limit (LOD) and quantification limit (LOQ) were 0.02 ng/mL and 0.06 ng/mL respectively. It has been successfully applied for the determination of various edible vegetable oil samples, the chromatogram shows symmetrical peak shape, perfect separation and very “clean” profiles. In comparison with gas chromatography-mass spectrum (GC-MS), the pretreatment process of the proposed method was totally operated in aqueous phase, the instrument requirements and cost are relatively lower, thus it will provide another choice for the routine analysis of 3-MCPD.
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