TOXICOLOGY
·
2017
·
IF 3.582
Juanli Fu,Xiaomin Xia,Zixuan Liu,Yawen Wang,Yuxin Wang,Qiong Shi,Xiufang Song,Erqun Song,Yang Song
This study is aimed to investigate the inflammation and neurological dysfunction induced by tetrachloro- p -benzoquinone (TCBQ) through Toll-like receptor 4 (TLR4) signaling. We also investigated the protective role of melatonin as an antioxidant and anti-inflammatory agent. In vitro model was established by rat pheochromocytoma PC12 cells, meanwhile, TLR4 wild-type (C57BL/6) and knockout mice (C57BL/10ScNJ TLR4 −/− ) were used as in vivo model. In vitro study showed TCBQ exposure enhanced the expression of TLR4, myeloid differentiation factor 88 (MyD88) at both transcriptional and post-transcriptional levels. By contrast, melatonin decreased TLR4 and MyD88 expressions. Moreover, our result indicated that melatonin disrupted the formation of TLR4/MyD88/MD2/CD14 complex. In addition, melatonin terminated TCBQ-mediated phosphorylation of c-Jun N-terminal kinase (JNK), p38, and extracellular regulated protein kinase (ERK) signaling and hampered its downstream pro-inflammatory cytokine releases. In vivo result also indicated TLR4 deficiency partially protected against TCBQ-induced morphological and neuropathological changes in mice brain, suggested the role of TLR4. In conclusion, melatonin modulates TCBQ-mediated inflammatory genes through TLR4/MyD88-dependent signaling pathway. Our current study, to the best of our knowledge, is the first time show melatonin not only disrupt the binding of TLR4 and MyD88, but also restricted the formation of TLR4/MD2/CD14 complex, suggesting that melatonin supplementary may represent a valuable therapeutic strategy for inflammatory neurological dysfunction.
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JOURNAL OF NANOBIOTECHNOLOGY
·
2020
·Vol. 18
·期 1
·1-19
·
IF 6.518
Li Mingxin,Liu Guohao,Wang Kaixuan,Wang Lingfeng,Fu Xiang,Lim Lee Yong,Chen Wei,Mo Jingxin
Primary intracerebral hemorrhage (ICH) is a leading cause of long-term disability and death worldwide. Drug delivery vehicles to treat ICH are less than satisfactory because of their short circulation lives, lack of specific targeting to the hemorrhagic site, and poor control of drug release. To exploit the fact that metal ions such as Fe2+ are more abundant in peri-hematomal tissue than in healthy tissue because of red blood cell lysis, we developed a metal ion-responsive nanocarrier based on a phosphonated calix[4]arene derivative in order to deliver the neuroprotective agent dauricine (DRC) specifically to sites of primary and secondary brain injury. The potential of the dauricine-loaded nanocarriers for ICH therapy was systematically evaluated in vitro and in mouse models of autologous whole blood double infusion. The nanocarriers significantly reduced brain water content, restored blood-brain barrier integrity and attenuated neurological deficits by inhibiting the activation of glial cells, infiltration by neutrophils as well as production of pro-inflammatory factors (IL-1β, IL-6, TNF-α) and matrix-metalloprotease-9. These results suggest that our dauricine-loaded nanocarriers can improve neurological outcomes in an animal model of ICH by reducing inflammatory injury and inhibiting apoptosis and ferroptosis.
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DRUG METABOLISM AND DISPOSITION
·
2022
·Vol. 50
·期 4
·341-350
·
IF 3.579
Yingqiong Zhang,Yujia Chen,Binxin Dai,Mengru Bai,Shuanghui Lu,Nengming Lin,Hui Zhou,Huidi Jiang
Estrogen biosynthesis in human placental trophoblasts requires the human organic anion transporter 4 (hOAT4)-mediated uptake of fetal derived precursors such as dehydroepiandrosterone-3-sulfate (DHEAS) and 16α-hydroxy-DHEA-S (16α-OH-DHEAS). Scant information is available concerning the contribution of fetal metabolites on the impact of placental estrogen precursor transport and the followed estrogen synthesis. This study substantiated the roles of bilirubin as well as bile acids (taurochenodeoxycholic acid, taurocholic acid, glycochenodeoxycholic acid, chenodeoxycholic acid) on the inhibition of hOAT4-mediated uptake of probe substrate 6-carboxylfluorescein and DHEAS in stably transfected hOAT4-Chinese hamster ovary cells, with the IC50 of 1.53 and 0.98 μM on 6-carboxylfluorescein and DHEAS, respectively, for bilirubin, and 90.2, 129, 16.4, and 12.3 μM on 6-CF for taurochenodeoxycholic acid, glycochenodeoxycholic acid, taurocholic acid, and chenodeoxycholic acid. Bilirubin (2.5–10 μM) concentration-dependently inhibited the accumulation of estradiol precursor DHEAS in human choriocarcinoma JEG-3 cells (reduced by 60% at 10 μM) and primary human trophoblast cells (reduced by 80% at 10 μM). Further study confirmed that bilirubin (0.625–2.5 μM) concentration-dependently reduced the synthesis and secretion of estradiol in primary human trophoblast cells, among which 2.5 μM of bilirubin reduced the synthesis of estradiol by 30% and secretion by 35%. In addition, immunostaining and Western blot results revealed a distinct downregulation of hOAT4 protein expression in primary human trophoblast cells pretreated with 2.5 μM of bilirubin. In conclusion, this study demonstrated that bilirubin reduced the uptake of estrogen precursors and the followed synthesis of estradiol in human placenta via inhibition and downregulation of organic anion transporter 4.
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JOURNAL OF CHROMATOGRAPHY A
·
2017
·
IF 3.981
Jingtang Li,Tao Yu,Guangfu Xu,Yingxiang Du,Zongran Liu,Zijie Feng,Xuan Yang,Ying Xi,Jie Liu
Recently,ionic liquids (ILs) functionalized cyclodextrins (CDs) have attracted more and more attention in the fields of enantioseparation. In this study, a novel IL amino triazolium functionalized β-CD derivative, mono-6-deoxy-6-(4-amino-1,2,4-triazolium)-β-cyclodextrin chloride (4-ATMCDCl), was synthesized for the first time and managed to separate dansyl amino acids and naproxen by capillary electrophoresis (CE). Compared with native β-CD, the new selector exhibited good water solubility and enhanced enantioselectivity. Several crucial parameters such as selector concentration, buffer pH, and applied voltage were systematically investigated. The molecular docking program Autodock was applied to further demonstrate the mechanism of chiral recognition and the enhanced enantioselectivity of 4-ATMCDCl, which showed good agreement with our experimental results.
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INDUSTRIAL & ENGINEERING CHEMISTRY RESEARCH
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2020
·
IF 3.573
Xingjie Yang,Xubao Jiang,Muhammad Sohail Bashir,Xiang Zheng Kong
Polyurethanes (PUNs) have been widely used in many fields. However, there are few reports on their microsphere preparation through precipitation polymerization. Herein, uniform PUN microspheres are prepared by precipitation polymerization of toluene diisocyanate and trimethylolpropane, without any surfactant and stabilizer. Under optimized conditions, monomers are fully polymerized within 2 h at a monomer concentration as high as 25.0 wt %, with a high yield of the microspheres (96.9%). By loading Pd on their surface, composite microspheres Pd@PUN are obtained and used as catalysts. 4-Nitrophenol is completely reduced within 1 min, with a kinetic constant of 4.96 min–1, significantly higher than many reported Pd-loaded catalysts, and with comparable reusability. Used in degradation of dye molecules, the catalytic performance is practically unchanged after 20 recycled uses. This work provides a simple method for the preparation of highly uniform PUN microspheres with a high yield and their Pd-loaded catalysts, both of great potential for various applications.
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ADSORPTION SCIENCE & TECHNOLOGY
·
2013
·
IF 0.559
Ping Yu,Qilong Sun,Jianming Pan,Zhenjiang Tan,Jiangdong Dai,Yongsheng Yan,Feng Cheng
Poly(styrene–divinylbenzene)/Fe3O4 (Fe3O4@St–DVB) magnetic porous polymer microspheres based on suspension polymerization were prepared for adsorption of 2, 4-dichlorophenol (2, 4-DCP) and 2, 6-dichlorophenol (2, 6-DCP) from aqueous solution. The as-prepared product was characterized by Fourier transform infrared spectroscopy, Raman, X-ray diffraction, scanning electron microscopy, thermogravimetric analysis, differential thermal analysis and elemental analysis. The results showed that the composite material has both porous and magnetic characteristics, which aid in faster separation and increase in adsorption capacity. The adsorption performance of the Fe3O4@(St–DVB) magnetic porous microspheres was manifested by batch mode adsorption experiments with respect to pH, initial concentration, contact time and temperature. The adsorbent was found to be sensitive to changes in pH, and the adsorption capacity of 2, 4-DCP is higher than that of 2, 6-DCP. The kinetics experimental data fitted well with the pseudo-second-order model, as three steps belonged to the pseudo-second-order adsorption process. The adsorption isotherms were also described by the Langmuir and Freundlich isotherm models, respectively. It was found that the Langmuir isotherm model fitted the equilibrium data superior to the Freundlich model. Thermodynamic parameters were calculated by the Gibbs free energy function, confirming that adsorption process was spontaneous and endothermic. In addition, the reusability performance of the Fe3O4@(St–DVB) magnetic porous microspheres was demonstrated by four repeated cycles.
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TALANTA
·
2020
·
IF 5.339
Huadong Zhang,Huasheng Lai,Gongke Li,Yufei Hu
Halloysite nanotubes loaded with 4-aminothiophenol capped silver nanoparticles (mHNTs-AgNPs 4−ATP ) composite was synthesized as a sensitive surface-enhanced Raman scattering (SERS) probe for the determination of nitrite ions in sausage and pork luncheon meat . The as-prepared composite was characterized by transmission electron microscope, X-ray diffraction spectroscopy and Fourier transform infrared spectroscopy . The as-synthesized mHNTs-AgNPs 4−ATP composite with evenly distribution of AgNPs can provide in-situ derivatization site for sensitive and selective SERS detection of nitrite ions. Under acid condition, the 4-ATP capped on the AgNPs can be transformed into p , p ’-dimercaptoazobenzene (DMAB) through nitrite-triggered diazo reaction. This efficient nitrite-triggered reaction can be used to detect nitrite via the characteristic peaks of DMAB at 1143 cm −1 , 1392 cm −1 , and 1434 cm −1 . This SERS method has a wide logarithmic range of 0.0069–6.9 mg L −1 , with detection limit of 0.78, 3.4, 0.51 μg L −1 at the peak of 1143 cm −1 , 1392 cm −1 , and 1434 cm −1 , respectively. Besides, this method can be applied to detect nitrite ions in sausage and pork luncheon meat with relative standard deviation less than 10.3%, and the results were consistent with that analyzed by UV–Vis method. This method has good potential in efficient detection of meat product in food safety.
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SURFACE AND INTERFACE ANALYSIS
·
2016
·Vol. 48
·期 9
·990-994
·
IF 1.018
Yuanjie Teng,Guocheng Ding,Wenhan Liu,Jiangmei Liu,Yonghui Nie,Pan Li
Column electrodes pretreated through oxidation–reduction cycles were traditionally used in electrochemical surface-enhanced Raman scattering (SERS). In this study, a disposable screen-printed carbon electrode was introduced into in situ electrochemical SERS through the electrodeposition of dendritic gold/silver nanoparticles (Au/AgNPs) onto the surface of the carbon working electrode to induce the SERS enhancement effect on the electrode. Scanning electron microscopy images showed that dendritic Au/AgNPs nanostructures could be fabricated under appropriate electrodeposition conditions and could present a minimum SERS factor of 4.25 × 10 5 . Furthermore, the absorbed behavior of 4-mercaptopyridine was investigated under different potentials. The adsorption configuration was inferred to transform from ‘vertical’ to ‘lying-flat’. The proposed new electrode combined with a portable Raman spectrometer could be useful in the identifying products or intermediates during electrochemical synthesis or electrochemical catalysis in in situ electrochemical SERS. Copyright © 2016 John Wiley & Sons, Ltd.
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ACTA CHIMICA SLOVENICA
·
2017
·Vol. 64
·期 4
·825-831
·
IF 0.983
Ren YJ,Zhu JL,Zhang LX,Xu YX,Qian SS.
Three new complexes derived from 2-(4-(pyridin-2-yl)piperazin-1-yl)acetic acid (HL), [M(L)2(H2O)2] where M = CuII (1), ZnII (2) and CdII (3), have been synthesized and characterized by IR spectroscopy, elemental analysis and X-ray crystallography. The inhibitory activity of these three complexes against MAO-B was tested in vitro, and the molecular docking experiments were also carried out to rationalize their binding models. Both the experimental and docking simulation results indicated that complex 1 has the best inhibitory activity with IC50 value being 6.5 ± 0.31 μM.
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ORGANIC PROCESS RESEARCH & DEVELOPMENT
·
2020
·
IF 3.023
Zeyu Yang,Wenjie Ye,Youyu Xie,Qinghai Liu,Rong Chen,Hualei Wang,Dongzhi Wei
Bioreductions catalyzed by alcohol dehydrogenases (ADHs) play an important role in the synthesis of chiral alcohols. However, the synthesis of ethyl (S)-4-chloro-3-hydroxybutyrate [(S)-CHBE], an important drug intermediate, has significant challenges concerning high substrate or product inhibition toward ADHs, which complicates its production. Herein, we evaluated a novel ADH, SmADH31, obtained from the Stenotrophomonas maltophilia genome, which can tolerate extremely high concentrations (6 M) of both substrate and product. The coexpression of SmADH31 and glucose dehydrogenase from Bacillus subtilis in Escherichia coli meant that as much as 660 g L–1 (4.0 M) ethyl 4-chloroacetoacetate was completely converted into (S)-CHBE in a monophasic aqueous system with a >99.9% ee value and a high space-time yield (2664 g L–1 d–1). Molecular dynamics simulation shed light on the high activity and stereoselectivity of SmADH31. Moreover, five other optically pure chiral alcohols were synthesized at high concentrations (100–462 g L–1) as a result of the broad substrate spectrum of SmADH31. All these compounds act as important drug intermediates, demonstrating the industrial potential of SmADH31-mediated bioreductions.
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2021
·
IF 5.279
Hao-Min Song,Li-Xia Zhao,Shuai-Qi Zhang,Tong Ye,Ying Fu,Fei Ye
Cinnamic acid, isolated from cinnamon bark, is a natural product with excellent bioactivity, and it effectively binds with cyclohexanedione to form novel 4-hydroxyphenylpyruvate dioxygenase (HPPD) inhibitors. According to the active sub-structure combination principle, a series of novel 3-hydroxy-2-cinnamoyl-2-en-1-one derivatives were designed and synthesized. The title compounds were characterized by infrared, 1H NMR, 13C NMR, and HRMS. The in vitro inhibitory activity of AtHPPD verified that compound II-13 showed the most activity with a half-maximal inhibitory concentration (IC50) value of 0.180 μM, which was superior to that of mesotrione (0.206 μM) in vitro. The preliminary herbicidal activity tests demonstrated that some compounds had good herbicidal activity especially compound II-13 at a concentration of 150 g ai/ha. The binding mode of AtHPPD through molecular docking indicated that two oxygens of compounds II-13 formed bidentate interactions with metal ions, and the benzene ring formed π-π accumulation effects with Phe-381 and Phe-424. The results of molecular dynamics simulations showed that compound II-13 exhibited a more stable binding ability with AtHPPD than mesotrione. This study provided insights into the development of natural and efficient herbicides in the future.
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EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
·
2023
·
IF 6.7
Changjun Zhang,Yi Lu,Jingqi Zhang,Anjie Zang,Jinhui Ren,Zhiyuan Zheng,Miaoliang Fan,Yuanyuan Xie
Recent advances in understanding the role of iron and ROS in cell death suggest new therapeutic avenues to treat organ damage including acute kidney injury (AKI). Inhibiting ferroptosis was expected to have great potential for the treatment of this disease. Ferroptosis is characterized by iron-dependent lipid peroxidation and currently, a majority of reported ferroptosis inhibitors belong to either radical-trapping antioxidants or iron chelators . However, clinically used iron chelators such as deferoxamine and deferiprone have limited efficacy against ferroptosis (generally with EC 50 > 100 μM), despite their proven safety. Herein, we present the rational design of novel ferroptosis inhibitors by incorporating the naturally occurring cinnamic acid scaffold and the 3-hydroxypyridin-4(1 H )-one iron-chelating pharmacophore . Through ABTS ˙ + radical-scavenging assay, oxygen radical absorbance capacity (ORAC) measurement, Fe 3+ affinity evaluation, and anti-erastin-induced HT22 cell ferroptosis assays, we identified compound 9c as the most prospective ferroptosis inhibitor (ABTS ˙ + , IC 50 = 4.35 ± 0.05 μM; ORCA = 23.79 ± 0.56 TE; pFe 3+ = 18.59; EC 50 = 14.89 ± 0.08 μM, respectively). Notably, 9c dose-dependently alleviated cell death in cisplatin-induced AKI model. Our results provide insight into the development of new ferroptosis inhibitors through rational incorporation of pharmacophores from existing ferroptosis inhibitors, and compound 9c could be a promising lead compound worth further investigation.
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