Frontiers in Pharmacology
·
2022
·
IF 5.988
Wu Meng,Cui Jingyi,Hou Huimin,Li Ying,Liu Shengjie,Wan Li,Zhang Lili,Huang Wei,Sun Gaoyuan,Liu Jingchao,Jin Pengfei,He Shunmin,Liu Ming
Background: The inactivation of tumor-suppressor p53 plays an important role in second generation anti-androgens (SGAs) drug resistance and neuroendocrine differentiation in castration-resistant prostate cancer (CRPC). The reactivation of p53 by blocking the MDM2–p53 interaction represents an attractive therapeutic remedy in cancers with wild-type or functional p53. Whether MDM2-p53 inhibitor could overcome SGAs drug resistance in CRPC is still needed further research. Here, we investigated the anti-tumor efficacy and mechanisms of a novel MDM2-p53 inhibitor XR-2 in CRPC.Methods: To investigate the functions and mechanisms of XR-2 in prostate cancer, in vitro and in vivo biofunctional assays were performed. Western blot and qRT-PCR assay were performed to detect the protein and mRNA expression levels of indicated genes. CCK8, colony formation, flow cytometry and senescence assays were performed for cell function identifications. RNA-sequencing and bioinformatics analysis were mainly used to identify the influence of XR-2 on prostate cancer cells transcriptome. Subcutaneous 22Rv1 derived xenografts mice model was used to investigate the in vivo anti-tumor activity of XR-2. In addition, the broad-spectrum anti-tumor activities in vivo of XR-2 were evaluated by different xenografts mice models.Results: XR-2 could directly bind to MDM2, potently reactivate the p53 pathway and thus induce cell cycle arrest and apoptosis in wild-type p53 CRPC cell lines. XR-2 also suppresses the AR pathway as p53 regulates AR transcription inhibition and MDM2 participates in AR degradation. As a result, XR-2 efficiently inhibited CRPC cell viability, showed a synergistic effect with enzalutamide and overcame enzalutamide resistance both in vitro and in vivo. Moreover, results illustrated that XR-2 possesses broad-spectrum anti-tumor activities in vivo with favourable safety.Conclusion: MDM2-p53 inhibitor (XR-2) possesses potently prostate cancer progresses inhibition activity both in vitro and in vivo. XR-2 shows a synergistic effect with enzalutamide and overcomes enzalutamide resistance.
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高影响因子
BIOORGANIC CHEMISTRY
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2020
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IF 4.831
Li Yang,Shengzhang Liu,Ronghua Liu,Junwei He
The root of Dendropanax dentiger (Harms) Merr. is a traditional Chinese medicine that has been used to treat inflammation-related diseases with little scientific validation. In this study, a bioassay-guided phytochemical investigation of D. dentiger led to the isolation of 19 phenylpropanoid derivatives including one new compound ( 1 ) and 18 known ones ( 2 – 19 ). Their structures were elucidated by NMR and HRMS as well as comparison with literature data. The ability of cyclooxygenase-2 (COX-2) inhibition and antioxidant of all isolated compounds were measured in vitro . Chlorogenic acid derivatives ( 14 – 19 ) exhibited outstanding COX-2 inhibitory (IC 50 = 5.1–93.4 μM) and antioxidant (IC 50 = 13.2–31.9 μM) activities. Moreover, the tight structure-activities relationships were proposed. This is the first report on the COX-2 inhibitory activity of phenylpropanoids and D. dentiger .
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高影响因子
ENVIRONMENTAL TOXICOLOGY AND PHARMACOLOGY
·
2017
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IF 2.313
Nan Xiang,Chunfeng Zhao,Xiaoping Diao,Qian Han,Hailong Zhou
Di(2-ethylhexyl) phthalate (DEHP) is recognized as one of the most ubiquitous contaminants in marine environments and causes adverse effects on the health of marine organisms. The purpose of this study was to investigate the toxic effects of DEHP on the pearl oyster Pinctada martensii . The Pinctada martensii was exposed to 0.0, 0.5, 2, 8, or 32 mg L −1 DEHP for 7 and 10 days using parameters of antioxidant. Antioxidant indicators included levels of superoxide dismutase (SOD), catalase (CAT), glutathione (GSH), peroxidase (POD), and total antioxidant capacity (T-AOC) in the gills and hepatopancreas of Pinctada martensii for 7 and 10 days. Besides, we used the lowest observed effect concentration (LOEC) of five enzyme activities in different tissues of Pinctada martensii for 7 and 10 days to compare sensitivity. The results showed that the gills were more sensitive than the hepatopancreas of Pinctada martensii and that GSH activity in the gills and CAT activity in the hepatopancreas might be suitable biomarkers after 7 days of DEHP exposure. After 10 days of DEHP exposure, the GSH activity and CAT activity in the gills and SOD activity in the hepatopancreas could be regarded as biomarkers. Compared to the LOEC, GSH activity in the gills and CAT activity in the hepatopancreas after 7 days of DEHP exposure were more sensitive than any other biomarkers. In addition, after 10 days of DEHP exposure, GSH activity in the gills and hepatopancreas were much more sensitive than other activities. In conclusion, GSH activity demonstrated its potential to be used as a biomarker for the monitoring of DEHP pollution in the marine environment.
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高影响因子
FUEL
·
2025
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IF 7.5
Yali Niu,Rui Yao,Shuhui Fan,Jinping Li,Guang Liu
Anion-exchange membrane water electrolyzers (AEMWE) are promising for clean hydrogen production. However, the high energy barriers associated with water adsorption and dissociation combined with the high adsorption energy of hydrogen intermediates (H*) in alkaline environment result in slow kinetics for the hydrogen evolution reaction (HER). To tackle this, we report a catalyst comprising Pt nanoparticles loaded on Co(OH) 2 /PTI nanosheets (Pt/Co(OH) 2 /PTI) for efficient alkaline HER at high current densities. Operando characterization indicates that Co(OH) 2 promotes H 2 O adsorption and dissociation, while the Pt nanoparticles optimize H* adsorption energy, enabling preferential H* adsorption at the Pt site to facilitate H 2 generation and desorption. Furthermore, the ultra-thin poly (triazine imide) (PTI) support prevents the Pt nanoparticles aggregation, thereby enhancing catalyst stability. As a result, the synergistic Pt/Co(OH) 2 /PTI achieves superior HER performance, demanding an overpotential of merely 7 mV to achieve a current density of 10 mA cm −2 and just 220 mV to drive 1 A cm −2 , and it maintains stable for over 220 h under the condition of 1 A cm −2 . Additionally, the electrolyzer assembled using Pt/Co(OH) 2 /PTI as the cathode demonstrates stable operation for 200 h at 0.5 A cm −2 under 70 °C, highlighting its strong potential for industrial applications.
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SOLID STATE SCIENCES
·
2025
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IF 3.3
Wenyue Zhao,Zipeng Jin,Kunting Li,Huimin Feng,Lei Xu,Yiming Zhang
Efficiently harnessing solar energy for hydrogen production remains a significant challenge, primarily dependent on the rational design of photocatalysts. In this work, an S-scheme heterojunction was constructed by integrating TiO 2 with a biphenyl-bridged covalent triazine framework (CTF-2). The extended π-conjugation in CTF-2 significantly enhances visible-light absorption and generates abundant delocalized electrons. The heterostructure was confirmed by characterizations, which revealed an increased specific surface area and enhanced redox capacity. Photoelectrochemical tests indicated a significant reduction in charge recombination, attributed to the newly formed Ti-N bonds that promote electron transfer from TiO 2 to CTF-2. The active species capture experiment and band structure analysis corroborated the S-scheme charge transfer route. The optimal 1.0 wt% CTF-2/TiO 2 achieved an H 2 evolution rate of 2.975 mmol·g -1 ·h -1 , 4.92 times higher than pristine TiO 2 , and retained 83% of its activity after five cycles. This study provides a practical approach to designing high-performance, stable heterostructures for solar energy conversion.
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高影响因子
APPLIED PHYSICS A-MATERIALS SCIENCE & PROCESSING
·
2025
·Vol. 131
·期 7
·583
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IF 2.8
Zou Wenqian,Zhang Mengyu,Liu Xichen,Ding Shoujun J.,Zou Yong
Developing highly efficient and stable inorganic narrow-band green-emitting phosphor is crucial for phosphor converted backlighting devices. In this study, trivalent Tb 3+ ions self-actived NaTb(MoO 4 ) 2 (NTM) narrow-band green-emitting phosphor was prepared by a conventional high-temperature solid-state reaction method. The electronic structure, luminescence properties and luminescence thermal stability of NTM were studied through experiments and theoretical calculations. The structure of NTM was determined to be a tetragonal phase with the space group of I41/a (88). Besides, the NTM was confirmed with direct bandgap characteristics with bandgap width of 3.1231 eV. Upon 266 nm and 355 nm ultraviolet (UV) excitation, the narrow-band green-emitting properties of the phosphor were investigated. Importantly, the phosphor was confirmed with well luminescence thermal stability and the thermal activation energy ( E a ) was fitted to be 0.32 eV. The work demonstrates that trivalent Tb 3+ ions self-actived NTM is promising as high luminescence stable narrow-band green-emitting phosphor for backlighting display applications.
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MICROCHEMICAL JOURNAL
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2025
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IF 5.1
Weiqiang Li,Dandan Wei,Qian Xu,Luyu Yang,Yang Liu,Hengyi Xu
Foodborne pathogens pose serious risks to environmental protection and food safety. The low abundance of foodborne pathogens during the early stage of pollution makes the detection of them a challenge, and combining efficient bacterial enrichment with powerful signal release is a potential proposal. In this study, wulff-type boronate functionalized magnetic nanoparticles (MNPs) (B-N/APBA@MNPs) was designed, the binding pH and affinity of the original boronic acid were improved by teamed boronate affinity strategy. Characterization and capacity performance assessment ensure its successful synthesis and excellent capture performance for 2 bacteria. Meanwhile, controlled explosive release of carbon dots (CDs) nanocapsule was prepared by encapsulating CDs with characterized its successful synthesis and evaluate its fluorescence performance. The nanocapsule encapsulating strategy can effectively enhanced the fluorescent signal and avoided the interference of magnetic nanoparticles (MNPs) on CDs. Taking Listeria monocytogenes and Escherichia coli O157:H7 as a proof of concept, a dual-signal amplification platform based on Wulff-type boronate acids combined with controlled explosive release nanocapsule was established. Results showed an impressively low limit of detection (10 1 CFU/mL) and high recovery rates (84.95 % ∼ 116.27 %). Notably, the proposed dual-signal amplification strategy provides a design template for the detection of low concentration of bacteria in environmental detection and food safety.
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JOURNAL OF COLLOID AND INTERFACE SCIENCE
·
2025
·
IF 9.7
Zhuo Wang,Meiting Wang,Luan Fang,Zihan Li,Ping Nie,Yuting Gao,Juan Jian,Limin Chang
Hydrogen produced through self-powered water-splitting can effectively meet the demand for miniaturized devices. However, the design of an efficient catalyst that integrates a zinc-air battery (ZAB) with a water-splitting cell is crucial for the development of such devices. In this study, we synthesized Pt/Ni 3 (PO 4 ) 2 on nickel foam (NF) via a two-step process. The resulting Pt/Ni 3 (PO 4 ) 2 /NF exhibited significantly enhanced trifunctional properties (hydrogen evolution reaction, HER; oxygen evolution reaction, OER; oxygen reduction reaction, ORR) compared to the Ni 3 (PO 4 ) 2 /NF precursor. Additionally, the ZAB assembled using Pt/Ni 3 (PO 4 ) 2 /NF as the air-cathode demonstrated superior rechargeable performance compared to the Ni 3 (PO 4 ) 2 /NF-based counterpart. Moreover, when Pt/Ni 3 (PO 4 ) 2 /NF was directly used as both the cathode/anode for the water-splitting device and the air-cathode for the ZAB, the self-powered hydrolysis device exhibited excellent hydrogen production performance. Upon investigating the influence of in-situ decorated Pt nanoparticles, we found that these Pt nanoparticles: 1) facilitate the morphological reconstruction of Ni 3 (PO 4 ) 2 , thus increasing the electrochemical surface area of the catalyst; 2) lower the hydrogen adsorption free energy of Pt/Ni 3 (PO 4 ) 2 , and the associated OER theorical potential; 3) shift the d-band center of Pt/Ni 3 (PO 4 ) 2 closer to the Fermi level, ultimately enhancing its intrinsic catalytic activity. This work is expected to provide a foundation for experimental, theoretical, and practical applications of other Ni 3 (PO 4 ) 2 -based multifunctional materials.
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JOURNAL OF ORGANIC CHEMISTRY
·
2024
·
IF 3.3
Nan Wang,Yuanyuan Huang,You Zi,Mengke Wang,Weichun Huang
A practical and regioselective direct N-alkylation of 2-pyridones is enabled by use of α-keto esters in the P(NMe2)3-mediated deoxygenation process. The reaction proceeds under mild conditions to produce N-alkylated 2-pyridones with high selectivity and generality, and the protocol is shown to be applicable for the scale-up synthesis, which makes it promising for practical applications.
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高影响因子
INTERNATIONAL DAIRY JOURNAL
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2022
·
IF 3.572
Yaqi Tu,Lei Guan,Fazheng Ren,Hao Zhang
This study sought to research the antigenicity and functional characteristics of Maillard reaction products (MRPs) arising from the human breast milk oligosaccharide , 2′-fucosyllactose (2′-FL), and β-lactoglobulin (β-LG). The MRPs were prepared at 60 °C, 96 h and 79% relative humidity. During the Maillard reaction, the content of ultraviolet-absorbing and fluorescence compounds, and browning products increased. The free amino groups content decreased by 61.5% during the first 48 h then did not change significantly. The results of sodium dodecylsulphate polyacrylamide gel electrophoresis showed that high molecular mass MRPs were generated and the intrinsic fluorescence spectra suggested a masking effect of 2′-FL. The surface hydrophobicity of β-LG-2′-FL increased and the antigenicity of the MRPs reduced significantly compared with the control β-LG, with the inhibition rate reaching 49.09%. The 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity and ferric reducing/antioxidant power assay revealed significant increases in the antioxidant activity of the MRPs.
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高影响因子
Cell Reports
·
2023
·Vol. 42
·期 11
·113349-113349
·
IF 8.8
Shao Q,Wijaya CS,Wang S,Meng X,Yuan C,Ma C,Xu S
Maintaining cellular viability relies on the integrity of the plasma membrane, which must be repaired upon damage. Soluble N-ethylmaleimide-sensitive factor attachment protein receptor (SNARE)-mediated membrane fusion is a crucial mechanism involved in membrane repair. In C. elegans epidermal cell hyp 7, syntaxin-2 (SYX-2) facilitates large membrane wound repair; however, the underlying molecular mechanism remains unclear. Here, we found that SNAP-25 protein RIC-4 and synaptobrevin protein SEC-22 are required for SYX-2 recruitment at the wound site. They interact to form a SNARE complex to promote membrane repair in vivo and fusion in vitro. Moreover, we found that SEC-22 localized in multiple intracellular compartments, including endosomes and the trans-Golgi network, which recruited to the wounds. Furthermore, inhibition of RAB-5 disrupted SEC-22 localization and prevented its interaction with SYX-2. Our findings suggest that RAB-5 facilitates the formation of the RIC-4/SEC-22/SYX-2 SNARE complex and provides valuable insights into the molecular mechanism of how cells repair large membrane wounds.
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高影响因子
SYNTHESIS-STUTTGART
·
2019
·Vol. 51
·期 21
·4048-4065
·
IF 2.867
Rui-Xiang Wang,Zhuang Fang,Guanyinsheng Qiu,Wenlin Xie,Jin-Biao Liu
The copper-catalyzed synthesis of 3-vinylisocoumarin-1-imine is reported. The transformation proceeds smoothly with good yields in THF and the regioselectivity was determined by a O-nucleophilic 6-endo cyclization. Studies on the mechanism indicate that copper trifluoroacetate serves as a Lewis acid, and the use of vinyl-connected 2-alkynylbenzamide is important for this O-nucleophilic 6-endo cyclization.
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危险品化学品经营许可证（带存储）