ANALYTICAL BIOCHEMISTRY
·
2021
·
IF 3.365
Haiyan Zhou,Guorui Zhong,Jing Bai,Xiaolei Li,Wen Peng,Lei Zhang,Jing Li
The urate transporter 1 (URAT1) inhibitors were considered a very promising class of uricosuric agents for the treatment of hyperuricemia and gout. In vitro activity testing of these compounds has been conducted by radio-labeling uric acid for a long time. However, relatively few offer the convenience and speed of fluorescence-based assays. Herein, we report the development of a non-radioactive cell-based method for the screening of URAT1 inhibitors using the human embryonic kidney 293T cells stably expressing human URAT1, and 6-carboxyfluorescein (6-CFL) as a substrate. The URAT1-mediated transport of 6-CFL was time dependent and saturable (Km = 239.5 μM, Vmax = 6.2 pmol/well/min, respectively). Molecules known to interact with organic anion transporters, including benzbromarone , probenecid , and lesinurad, demonstrated concentration-dependent inhibition of 6-CFL transport by URAT1. Moreover, we screened a small subset of compounds, and identified compound 4 as a promising URAT1 inhibitor. This in vitro assay may be employed to screen for novel URAT1 inhibitors, which are effective against hyperuricemia.
研究领域:
药理学
·
生物化学
✓ 已验证
DOI
PubMed
高影响因子
iScience
·
2021
·
IF 5.458
Mingwei Weng,Zihao Zhang,Francis Okejiri,Yue Yan,Yubing Lu,Jinshu Tian,Xiuyang Lu,Siyu Yao,Jie Fu
Catalytic transfer hydrogenation (CTH) of biomass-derived furfural (FAL) to furfuryl alcohol is recognized as one of the most versatile techniques for biomass valorization. However, the irreversible sintering of metal sites under the high-temperature reaction or during the coke removal regeneration process poses a serious concern. Herein, we present a silicalite-1-confined ultrasmall CuO structure (CuO@silicalite-1) and then compared its catalytic efficiency against conventional surface-supported CuO structure (CuO/silicalite-1) toward CTF of FAL with alcohols. Characterization results revealed that CuO nanoparticles encapsulated within the silicalite-1 matrix are ∼1.3 nm in size in CuO@silicalite-1, exhibiting better dispersion as compared to that in the CuO/silicalite-1. The CuO@silicalite-1, as a result, exhibited nearly 100-fold higher Cu-mass-based activity than the CuO/silicalite-1 counterpart. More importantly, the activity of the CuO@silicalite-1 catalyst can be regenerated via facile calcination to remove the surface-bound carbon deposits, unlike the CuO/silicalite-1 that suffered severe deactivation after use and cannot be effectively regenerated.
研究领域:
化学工程
·
材料科学
✓ 已验证
DOI
PubMed
高影响因子
AICHE JOURNAL
·
2020
·Vol. 66
·期 5
·e16917
·
IF 3.519
Bofeng Zhang,Yajie Tian,Dali Chen,Ling Li,Guozhu Li,Li Wang,Xiangwen Zhang,Guozhu Liu
Multimetallic nanocatalysts have attracted increasing attention for steam reforming owing to highly exposed active sites, but often suffering from severe sintering. Herein, we design subnanometric Ni-Pt bimetal clusters (ca. 1.7 nm) encapsulated in Silicalite-1 zeolite (2Ni0.5Pt@S-1) through ligand-stabilized method to prevent sintering by fixing the metal into microporous channels. In the steam reforming of n -dodecane test, 2Ni0.5Pt@S-1 gave an excellent activity and stability with a decrease of conversion only 4% at 600°C for 4 hr, which was about a quarter that of 2Ni0.5Pt/S-1 synthesized by co-impregnation method, ascribing to superior sinter-resistance of encapsulation structure. Moreover, 2Ni0.5Pt@S-1 exhibited a higher H 2 selectivity up to 69.9% than that of 2Ni0.5Pt/S-1 (64.4%), owing to suppressed methanation reaction based on subnanometric clusters. Shape-selective steam reforming of n -dodecane and ofm -xylene was also observed, because of m -xylene could hardly diffuse into the zeolite channels due to its bulky molecular size, further preventing potential deactivation by tars in reforming process.
研究领域:
催化化学
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材料科学
·
能源化学
✓ 已验证
DOI
高影响因子
Current Nanoscience
·
2024
·Vol. 21
·期 4
·757-765
·
IF 1.4
Zirui Liu,Dan Li,Baofeng Zhao,Xifan Mei
BackgroundGouty arthritis, characterized by excruciating pain and discomfort, poses a significant burden on patients. While nanomedicines have shown promise in addressing this ailment, their complicated synthesis processes often involve potentially toxic procedures, contributing to adverse side effects in disease management.MethodsIn this study, we introduce a straightforward and elegant solution by utilizing easily prepared gold platinum (AuPt) nanoparticles for the treatment of gouty arthritis. The synthesis of these nanoparticles involves the use of gold and platinum precursors in conjunction with NaBH4, simplifying the manufacturing process. Experimental models of gout were established in both in vivo and in vitro settings through lipopolysaccharide and monosodium urate crystal induction.ResultsOur findings revealed that AuPt nanoparticles exhibited potent anti-inflammatory effects against gout. This effect was attributed to their ability to activate the Nrf2/HO-1 pathway, resulting in pain alleviation and the inhibition of inflammation, ultimately leading to the reduction of joint edema. With their uncomplicated synthesis and promising therapeutic potential, these simply prepared AuPt nanoparticles emerge as a compelling candidate for pharmaceutical intervention in the treatment of gouty arthritis.ConclusionThis approach not only holds the promise of delivering effective relief to patients but also minimizes the risk of unwanted side effects associated with complex nanomedicine synthesis processes.
研究领域:
药理学
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纳米医学
·
炎症研究
✓ 已验证
DOI
高影响因子
BIOORGANIC CHEMISTRY
·
2020
·
IF 4.831
De-Yun Cui,Yi Yang,Meng-Meng Bai,Jiang-Xue Han,Cong-Cong Wang,Hong-Tao Kong,Bo-Yuan Shen,Da-Chao Yan,Chun-Ling Xiao,Yi-Shuang Liu,En Zhang
New Delhi Metallo-β-lactamase-1 (NDM-1), a Zn (II)-dependent enzyme, can catalyze the hydrolysis of almost all β-lactam antibiotics including carbapenems, resulting in bacterial antibiotic resistance, which threatens public health globally. Based on our finding that H 2 dedpa is as an efficient NDM-1 inhibitor, a series of H 2 dedpa derivatives was systematically prepared. These compounds exhibited significant activity against NDM-1, with IC 50 values 0.06–0.94 μM. In vitro , compounds 6k and 6n could restore the activity of meropenem against Klebsiella pneumoniae , Escherichia coli and Proteus mirabilis possessing either NDM or IMP. In particular, the activity of meropenem against E. coli producing NDM-4 could be improved up to 5333 times when these two compounds were used. Time–kill cell-based assays showed that 99.9% of P. mirabilis were killed when treated with meropenem in combination with compound 6k or 6n . Furthermore, compounds 6k and 6n were nonhemolytic (HC 50 > 1280 μg/mL) and showed low toxicity toward mammalian (HeLa) cells. Mechanistic studies indicated that compounds 6k and 6n inhibit NDM-1 by chelating the Zn 2+ ion of the enzyme.
研究领域:
微生物学
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药物化学
·
感染病学
✓ 已验证
DOI
高影响因子
FREE RADICAL BIOLOGY AND MEDICINE
·
2025
·
IF 8.2
Tongwang Luo,Shengzhe Song,Shujie Wang,Sheng Jiang,Bin Zhou,Quanjiang Song,Lingjun Shen,Xiaodu Wang,Houhui Song,Chunyan Shao
Cadmium (Cd), a pervasive environmental toxicant, poses significant threats to human and animal health through multi-organ toxicity. While ferroptosis has been implicated in Cd-induced pathologies, the molecular mechanisms underlying Cd-mediated nephrotoxicity remain poorly understood. This study elucidates the ferroptosis pathway in CdCl 2 -exposed PK-15 cells and murine kidney, characterized by iron overload, lipid peroxidation, and mitochondrial dysfunction, which were ameliorated by ferroptosis inhibitor ferrostatin-1. Transcriptomic analysis revealed substantial upregulation of heme oxygenase-1 (HO-1) following CdCl 2 exposure. Mechanistically, CdCl 2 triggered nuclear translocation of nuclear factor erythroid 2-related factor-2 (NRF2), subsequently activating HO-1 transcription. Over-activated HO-1 catalyzes the decomposition of heme and releases free iron, accompanied with the degradation of ferritin heavy chain 1 (FTH1) induced by CdCl 2 exposure, which leads to intracellular iron overload and excessive lipid peroxides production through Fenton reaction, resulting in ferroptosis ultimately. In vivo validation confirmed NRF2/HO-1-mediated ferroptosis in CdCl 2 -induced murine nephrotoxicity. Both pre-treatment with HO-1 competitive inhibitor Zinc protoporphyrin IX (ZnPP) and knockout of HO-1 gene remarkably alleviated PK-15 cells against ferroptosis induced by CdCl 2 treatment. Our findings demonstrate that Cd exposure initiates NRF2-mediated HO-1 overexpression, driving iron-dependent lipid peroxidation and subsequent ferroptosis. This mechanistic insight provides potential therapeutic targets for mitigating Cd-induced renal damage, advancing our understanding of heavy metal toxicity and its cellular consequences.
研究领域:
毒理学
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细胞生物学
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环境健康科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF ELECTROANALYTICAL CHEMISTRY
·
2019
·
IF 3.218
Wei Chen,Jiayue Dong,Sihan Zhou,Chunyong Zhang,Degang Fu
1-naphthol (1-NAP) and 2-naphthol (2-NAP) are both hazardous pollutants which pose great threat to our living environment. In the current work, a comparative investigation on the electrochemical mineralization of 1-NAP and 2-NAP using boron-doped diamond (BDD) anode was presented. Experiments were carried out using synthetic 1-NAP or 2-NAP solutions containing Na 2 SO 4 as supporting electrolyte . A two-level factorial design methodology was adopted to optimize the mineralization process, six mathematical models were thus constructed and used to explore the structure-property relation involved. The results obtained suggested that 1-NAP was easier and faster to break down than 2-NPA under the same oxidation conditions, which were in line with the outcome obtained from cyclic voltammetry , HPLC and TOC measurements. To understand the destruction mechanism, the electron structures of 1-NAP and 2-NAP were further examined by the quantum chemistry calculations with density functional theory. It was also found that the results from frontier orbital analysis could well explain the differing mineralization performances recorded in BDD anode cell. Finally, with the aid of LC/MS analysis, the oxidation pathways of 1-NAP or 2-NAP on BDD anodes were proposed.
研究领域:
环境科学
·
电化学
✓ 已验证
DOI
高影响因子
CHEMICAL ENGINEERING JOURNAL
·
2011
·
IF 3.074
Ting Wu,Xiang Cai,Shaozao Tan,Hongye Li,Jiesheng Liu,Weidong Yang
In order to explore the potential of graphene (G) in removal of hazardous chemicals in waste water, chemically reduced graphene oxide was employed as the adsorbent and the adsorption characteristics of graphene toward acrylonitrile (AN), p-toluenesulfonic acid (p-TA), 1-naphthalenesulfonic acid (1-NA) and methyl blue (MB) were evaluated under laboratory conditions. The results showed that the organic chemicals with larger molecule size and more benzene rings possessed a higher adsorption speed and a higher maximum adsorption capacity on G. The maximum adsorption capacities of p-TA, 1-NA and MB on G are ∼1.43 g/g G, ∼1.46 g/g G and ∼1.52 g/g G at 30 °C, respectively, which are the highest values of p-TA, 1-NA or MB adsorption on different kinds of today's nanomaterials. Under the maximum adsorption capacity, the absorption quantity of MB on G was dependent on the initial concentration of MB, and higher temperature could facilitate the adsorption process. The G efficiency remains almost constant during the first five cycles of the adsorption–desorption process. In addition, the fluorescence spectra implied that the adsorption of MB on G was a π–π stacking adsorption process. In conclusion, the G could serve as a promising adsorbent for the removal of chemicals containing benzene rings in waste water.
研究领域:
环境科学
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材料科学
✓ 已验证
DOI
高影响因子
APPLIED ORGANOMETALLIC CHEMISTRY
·
2021
·Vol. 35
·期 4
·e6147
·
IF 4.105
Sujuan Ge,Yuming Zhou,Xiaoli Sheng,Chunfeng Mao,Lina Zhao,Jianxing Xu,Lei Qiu
Piperidinium-based ionic liquids (ILs) were synthesized under mild conditions by coordinating N -alkyl- N -methylpiperidinium bromide ([Pip 1,x ]Br) with anhydrous AlCl 3 . The weak basicity of N -methylpiperidine had little impact on downstream problems from proton impurities and catalyst poisoning. The results of Fourier transform infrared (FT-IR), electrospray ionization mass spectrometry (ESI-MS), and nuclear magnetic resonance ( 27 Al NMR) confirmed that the active components in [Pip 1,x ]Br-2AlCl 3 ( χ = 0.67) were [Al 3 Cl 9 Br] − and [Al 2 Cl 6 Br] − . Besides, the reaction performance of [Pip 1,8 ]Br-2AlCl 3 under different conditions was carried out by single-factor experiment and further confirmed by orthogonal experimental method. Among these reaction conditions, the optimal combination was the reaction temperature of 40°C, ILs/O molar ratio of 0.2:1, px/O molar ratio of 12:1, and the reaction time of 30 min. Furthermore, [Pip 1,8 ]Br-2AlCl 3 had excellent stability and can be recycled 14 times. It was the high-efficiency catalytic activity and prominent recyclability that made continuous industrial production possible.
研究领域:
化学工程
·
催化科学
✓ 已验证
DOI
高影响因子
EUROPEAN JOURNAL OF PHARMACOLOGY
·
2025
·
IF 4.7
Ji-Ping Wei,Bo Zhao,Zi-Jian Jiang,Peng-Yu Wang,Yan Xu,Ning Ding,Yuan-Yuan Hu,Wei Wang,Bo-Tao Jiang
Renal ischemia/reperfusion (I/R) injury is the most common cause of acute kidney injury (AKI). It can progress to chronic injury and subsequently to chronic kidney disease (CKD) via the renal fibrosis pathway. Luteolin is one of the most commonly occurring flavonoids and exhibits potential therapeutic activity against various pathophysiological processes. In this study, we investigated the protective role of luteolin in counteracting renal I/R injury and its potential mechanisms through systematic network pharmacology, molecular docking, and in vivo experimental studies. Using network pharmacology, we constructed and analyzed a luteolin-renal I/R injury target network. We assessed the relationship between luteolin and renal I/R injury targets using molecular docking analysis. Subsequently, we established a rat model of AKI to CKD transition using unilateral ischemia/reperfusion injury (UIRI), and detected changes in the expression of related proteins using biochemical indices. Network pharmacological analysis and molecular docking showed that luteolin affected renal I/R injury through multiple targets and pathways. As demonstrated by in vivo experiments, luteolin significantly attenuated renal I/R-induced oxidative injury by inhibiting renal lipid peroxidation in rats through the modulation of the nuclear factor erythroid 2-related factor 2 (Nrf2)/heme oxygenase-1 (HO-1) pathway. Luteolin attenuated the levels of relevant inflammatory markers, significantly upregulated the synthesis of apoptosis-related proteins, and downregulated the expression of anti-apoptotic proteins. Our results suggest that luteolin effectively inhibited oxidative damage, inflammation, apoptosis, and fibrosis caused by renal I/R injury, thus exerting a nephroprotective effect. The antioxidant effects of luteolin may be related to the regulation of Nrf2/HO-1 signaling.
研究领域:
药理学
·
分子生物学
·
肾脏病学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2025
·Vol. 26
·期 6
·2727
·
IF 4.9
Kang Li,Xiaomei Ge,Wei Liu,Lei Huang,Xinye Lv,Yuhui Tang,Zhehao He,Yingxue Yang,Miaofen Chen,Jianguo Zeng,Pi Cheng
B-cell lymphoma-2 (Bcl-2) family proteins are fundamental regulators of intrinsic cell apoptosis, and overexpression of apoptotic proteins (Bcl-2 and Mcl-1) is a characteristic of many haematological malignancies. Thus, it is necessary to discover novel inhibitors to treat leukemia. In the current study, we synthesized a series of quercetagetin derivatives (compounds2a–2t,3a–3jand4a–4g) and evaluated their anticancer activities on four leukemia cells (U937, K562, K562R and KG-1). Among those synthesized derivatives, compounds2aexhibited the best antiproliferative activity (IC50= 0.276, 0.159, 0.312 and 0.271 µM to U937, K562, K562R and KG-1, respectively). In addition,2ainduced apoptosis in K562 and markedly arrested the cell cycle G2/M phase of K562. The Western blot assay showed that2ais a potential inhibitor that can effectively suppress the expression of Bcl-2 and Mcl-1. The molecular docking study predicted that2ahad firm interactions with the active pockets of Bcl-2 and Mcl-1. Finally, in silico pharmacokinetic evaluation of2aindicated its potential as an anti-leukemia drug lead in the future.
研究领域:
药理学
·
肿瘤学
·
分子生物学
✓ 已验证
DOI
PubMed
高影响因子
Journal of Saudi Chemical Society
·
2022
·
IF 4.712
Zeping Wang,Binjie Hu,George Zheng Chen
A hydrophobic ionic liquid (1-octyl-3-methylimidazolium hexafluorophosphate, C 8 mimPF 6 ) with a function of inhibiting corrosion was encapsulated at different concentrations in the copolymer of poly (methyl methacrylate) and poly (butyl acrylate) through miniemulsion polymerization. These latexes were coated on steel samples whose corrosion properties were evaluated by electrochemical techniques. It was found that increasing the C 8 mimPF 6 concentration from 0 wt% to 30 wt%, the corrosion inhibition efficiency was remarkably improved from 41% to 89% based on the charge transfer resistance and from 64% to 87% based on the corrosion current density, respectively. The ionic liquid did not attend the reaction during latex preparation but behaved as corrosion inhibitors on the steel surface. Such an anticorrosion effect could be ascribed to the physical adsorption of the C 8 mim + cation on the reaction sites and the hydrophobicity enhancement resulting from the hydrophobic PF 6 − anion.
研究领域:
材料科学
·
腐蚀与防护
·
电化学
✓ 已验证
DOI
高影响因子
危险品化学品经营许可证（带存储）