BRITISH JOURNAL OF PHARMACOLOGY
·
2015
·Vol. 172
·期 16
·4052-4065
·
IF 4.842
Lin Guo,Yanke Chen,Rui Zhao,Guanghui Wang,Eitan Friedman,Ao Zhang,Xuechu Zhen
Background and Purpose Application of orthosteric sigma-1 receptor agonists as anti-seizure drugs has been hindered by questionable efficacy and potential adverse effects. Here, we have investigated the anti-seizure effects of the novel and potent allosteric modulator of sigma-1 receptors, SKF83959 and its derivative SOMCL-668 (3-methyl-phenyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-ol). Experimental Approach The anti-seizure effects of SKF83959 were investigated in three mouse models, maximal electroshock seizures, pentylenetetrazole-induced convulsions and kainic acid-induced ‘status epilepticus’. Also, in rats, the cortical epileptiform activity induced by topical application of picrotoxin was recorded in electrocorticograms. In rat hippocampal brain slices, effects of the drugs on the high potassium-evoked epileptiform local field potentials were studied. Anti-seizure activities of SOMCL-668, a newly developed sigma-1 receptor selective allosteric modulator, were also investigated. Key Results SKF83959 (20, 40 mg·kg −1 ) exhibited anti –seizure actitity in the three mouse models and reduced the cortical epileptiform activity without alteration of spontaneous motor activity and motor coordination. These effects were blocked by the sigma-1 receptor antagonist BD1047, but not the dopamine D 1 receptor antagonist SCH23390. SKF83959 alone did not directly inhibit the epileptiform firing of CA3 neurons induced by high potassium in hippocampal slices, but did potentiate inhibition by the orthosteric sigma-1 receptor agonist SKF10047. Lastly, a selective sigma-1 receptor allosteric modulator SOMCL-668, which does not bind to dopamine receptors, exerted similar anti-seizure activities. Conclusions and Implications SKF83959 and SOMCL-668 displayed anti-seizure activities, indicating that allosteric modulation of sigma-1 receptors may provide a novel approach for discovering new anti-seizure drugs.
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MOLECULES
·
2025
·Vol. 30
·期 10
·2122
·
IF 4.6
Zhinan Wang,Xiaowei Li,Liang Zhao,Saiwa Liu,Jingjing Du,Xi Jia,Lirui Ge,Jian Xu,Kexin Cui,Yu Ga,Jinxiu Wang,Xi Xia
The emergence ofmcr-1-mediated colistin resistance has become a critical global health concern, highlighting the urgent need for innovative approaches to restore colistin’s therapeutic potential. In this study, we evaluated the antibacterial activity of four matrine-type alkaloids—namely, matrine, oxymatrine, sophocarpine, and sophoramine—againstmcr-1-positiveEscherichia coli. While these alkaloids showed limited efficacy when used alone, the combination of matrine with colistin exhibited remarkable synergistic effects, as demonstrated by checkerboard assays and time-kill curve analyses. The matrine–colistin combination caused minimal erythrocyte damage while effectively attenuating resistance development in vitro. This synergy was further corroborated in a murine infection model, where the combination significantly reduced bacterial loads in target tissues. Mechanistic studies revealed that the matrine–colistin combination enhances antimicrobial activity by disrupting bacterial membrane integrity, increasing intracellular colistin accumulation, and triggering reactive oxygen species-mediated oxidative damage. Collectively, these findings highlight the potential of matrine as a promising adjuvant to overcome colistin resistance, providing a novel therapeutic approach to address the challenge of infections cause by multidrug-resistant Gram-negative bacteria.
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JOURNAL OF NANOSCIENCE AND NANOTECHNOLOGY
·
2016
·Vol. 16
·期 1
·242-245
·
IF 1.338
Sun Ke Ke,Li Ling,He Yu Qi,Fan Lu,Wu Ya Qi,Liu Li
A hybrid HKUST-1/GO composite was synthesized and its drug loading and drug release abilities were investigated. The adsorption of IBU (ibuprofen) onto the surface of HKUST-1/GO and HKUST-1 composites was compared, and it was found that the addition of GO enhanced both IBU loading and
stability. The addition of GO also enhanced the specific surface area. Drug release experiments on IBU loaded HKUST-1 and HKUST-1/GO were conducted, and it was found that drug release of HKUST-1/GO was slower, which can be explained by the hydrogen bonding between GO and IBU. It can be concluded
that the addition of GO not only enhances drug loading, but can also achieve a more desirable slow-release of the drug.
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Heliyon
·
2023
·
IF 4
Liangliang Shi,Chenyue Jia,Jiangtao Feng,Weinong Zhang,Junbo He
1- O -alkylglycerols are a class of natural existing lipids with broad biological activities. However, their use in food or agricultural fields remains to be investigated, especially for their antimicrobial activity. In this work, three 1- O -alkylglycerols, 1- O -octanylglycerol (C 8 Gly 1 ), 1- O -dodecylglycerol (C 12 Gly 1 ), and 1- O -hexadecylglycerol (C 16 Gly 1 ), were synthesized in the isolated yields of 71.3–89.8 % and characterized by 1 H NMR, 13 C NMR, FITR, mass spectra, and HPLC-ESLD. The critical micelle concentration (CMC) of 1- O -alkylglycerols was determined to be 1.65 mmol/L (C 8 Gly 1 ), 0.33 mmol/L (C 12 Gly 1 ), and 0.23 mmol/L (C 16 Gly 1 ) using the pyrene method. C 12 Gly 1 and C 16 Gly 1 had similar surface tensions that are lower than C 8 Gly 1 . C 8 Gly 1 can form micelles in aqueous solution with excellent nano-dispersed uniformity and stability. Furthermore, C 8 Gly 1 and C 12 Gly 1 not only displayed good antibacterial activity against Staphylococcus aureus , but they also inhibited the growth of Botryosphaeria dothidea , Monilia fructigena , and Phytophthora capsicum at 400 μg/mL. Thus, the C 8 Gly 1 and C 12 Gly 1 can serve as novel antimicrobial agents in food preservation.
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JOURNAL OF MOLECULAR STRUCTURE
·
2013
·
IF 1.404
Yan Wang,Xihui Ge,Minqing Zhang,Huaigong Zhu,Zijian Zhang,Ming Wang
Growth characteristics of urea inclusion compounds with 1-decene, n-decane and mixture of 1-decene and n-decane (relative mass ratio = 1:1) were studied by CCD high-speed Camera. The present studies show that the speed of UICs growth in tunnel direction is faster than in vertical direction and the length of UICs with 1-decene is shorter than UICs with n-decane, and the length of UICs with mixture is between them due to the influence of the vinyl in 1-decene. The value of R = I (CH2)/ I (CH3) and M = I (CH CH2)/ I (CH3) in FTIR spectrum of UICs increasing with growth time demonstrates that urea prefers to include n-decane than 1-decene. 13 C CP/MAS NMR studies of UICs indicate that the arrangement of 1-decene in UICs is CH3⋯CH3 and CH CH2⋯CH2 CH. The arrangement of 1-decene in UICs leads to short chain of UICs with 1-decene in tunnel direction. The 13 C CP/MAS NMR spectra of UICs with MIX reveal that there are three different types of arrangement: CH3⋯CH3, CH CH2⋯CH3 and CH CH2⋯CH2 CH. The methods of FTIR and DSC were used to test the stability of UICs with different guests. The result shows that UICs with n-decane are stable than UICs with 1-decene. And the stability of UICs with mixture is in the middle.
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JOURNAL OF ELECTROANALYTICAL CHEMISTRY
·
2025
·
IF 4.1
Junling Meng,Wan Huang,Meijing Lu,Jingxuan Cao,Na Xu,Lina Zhao
In recent years, the in-situ exsolution of metal nanoparticles from the anodic oxide framework through reduction treatment has emerged as an effective strategy to boost electrochemical performance by increasing active sites and facilitating charge transfer. However, this approach is primarily restricted to simple perovskite structures. The development of novel and more efficient oxide matrices for the controlled desorption of high-density metal catalysts remains a significant challenge. In this study, Ruddlesden-Popper (RP) type layered oxides Pr 2 NiO 4 and Pr 3 Ni 2 O 7 were innovatively employed as new primary matrices with the objective of achieving controllable exsolution of nickel metal nanoparticles by leveraging their unique layered architecture. X-ray diffraction (XRD) and X-ray photoelectron spectroscopy (XPS) analyses confirmed that following reduction treatment, Ni nanoparticles were successfully exsolved in situ from the oxide surface, with a notably higher density of Ni nanoparticles observed for Pr 3 Ni 2 O 7 . Electrochemical tests show that after 3 h of reduction at 850 °C, the cell with Pr 3 Ni 2 O 7 anode can achieve a peak power density of 969.7 mW cm −2 . Furthermore, when employed the studied compounds as anode materials, they showed negligible performance degradation after 100-h operation at 700 °C under 300 mA cm −2 current density. Furthermore, SEM characterization provided additional verification of the experimental results. This research not only underscores the considerable potential of RP phase oxides as high-performance SOFC anode materials but also offers new insights into future developments in SOFC anodes by adjusting RP phase sequences to regulate nanoparticle density effectively.
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2023
·
IF 6.1
Tong Zhou,Xue Xia,Heping Cui,Yun Zhai,Foxin Zhang,Khizar Hayat,Xiaoming Zhang,Chi-Tang Ho
The influence of pH was studied on volatile flavor formation during thermal treatment of an Amadori rearrangement product (ARP) with or without the addition of cysteine (Cys). The formation of thiols and sulfides or 2-acetylthiazole and pyrazines induced by Cys during thermal degradation of ARP was pH-dependent. At low pH levels, the hydrolysis of Cys to hydrogen sulfide (H2S) was promoted, giving rise to the increase of thiols and sulfides with an obvious meaty aroma. However, alkaline conditions were beneficial for enhancing the cyclization or transformation of imine to the enol structure, which strengthened the formation of 2-acetylthiazole and pyrazines with a roasted and nutty aroma. The imine was derived from the nucleophilic addition of Cys and methylglyoxal (MGO) and subsequent decarboxylation. At pH 8, Cys-induced variation of the flavor profile was weakened during thermal degradation of ARP. Accordingly, the combinational effect of pH and added Cys could be beneficial for achieving the desirable flavors during thermal processing of ARP.
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Frontiers in Nutrition
·
2022
·
IF 6.59
Wu Yue,Yang Jingjuan,Xu Chengmei,Li Qiuqi,Ma Yage,Zhao Shenglan,Zhuang Jiachen,Shen Fei,Wang Qianqian,Feng Fengqin,Zhang Xi
The sea cucumber peptides (SCPs) from Acaudina leucoprocta were derived from the patented bio-enzyme digestion technology and the molecular weight of obtained SCPs was <10 kDa. In this study, we investigated the possible anti-aging effects of SCPs on the model of Caenorhabditis elegans and the underlying mechanisms. SCPs extend the average lifespan of nematodes by 31.46%. SCPs enhance the anti-stress capacity of C. elegans by improving heat resistance and mobility, Also, the accumulated potential oxidative stress inducers like lipofuscin and reactive oxygen species (ROS) were reduced to 40.84 and 71.43%. In addition, SCPs can increase the antioxidant capacity in nematodes by enhancing the activity of SOD and CAT and reducing MDA accumulation in nematodes to 32.44%. Mechanistically, SCPs could mediate DAF-16/DAF-2/SOD-3/OLD-1/PEPT-1 axis to improve antioxidant capacity and extend lifespan in nematodes. Taken together, these findings provide a direction for the anti-aging effects of sea cucumber peptides and new insights into the further purifications of SCPs and future research on aging.
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Food Bioscience
·
2022
·
IF 5.318
Caixing Pan,Heping Cui,Khizar Hayat,Xiaoming Zhang,Chi-Tang Ho
This research elucidated the reason of flavor deficiency during the thermal degradation of glutamic acid (Glu)-galactose (Gal) Amadori rearrangement product (GG-ARP) and the solution. The flavor formation from GG-ARP during the thermal degradation was investigated. Compared to the volatile compounds in Glu-Gal Maillard reaction products (GG-MRP), pyrazines in the volatile compounds derived from GG-ARP were restrained. The disadvantage in evolution asynchrony and content sufficiency of α -dicarbonyl compounds and Glu in the GG-ARP model limited the pyrazines formation. With the addition of Gal, the asynchronous effect was further exacerbated, and the furans in the GG-ARP-Gal model (956.81 μg/L, 120 °C, 60 min) were more significantly dominant among the volatile flavor compounds than in the GG-ARP model (454.98 μg/L, 120 °C, 60 min), while the pyrazines were still missing. Whereas, the extra-added Glu in the GG-ARP model could offset the deficiency of amino acids growth after α -dicarbonyl formation and promote the formation of pyrazines (74.47 μg/L, 120 °C, 60 min). Meanwhile, the formation of diketones (92.96 μg/L, 120 °C, 60 min) was promoted. The addition of Glu enhanced both milk-like and baking flavor of the GG-ARP system simultaneously. Formulated GG-ARP-Glu mixture was proposed to promisingly achieve the controlled formation of process flavors for baked foods with both desirable milk-like and baking scent.
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Biomed Research International
·
2022
·
IF 3.246
Aparna Vasudevan,Dinesh Kumar Kesavan,Liang Wu,Zhaoliang Su,Shengjun Wang,Mohan Kumar Ramasamy,Waheeta Hopper,Huaxi Xu
Antibiotic resistance is one of the significant problems globally; there is an increase in resistance with introducing every new class of antibiotics. Further, this has become one of the reasons for arising of new resistance mechanisms in Acinetobacter baumannii. In this study, we have screened natural compounds as a possible inhibitor against the NDM-1 β-lactamase enzyme from A. baumannii using a combination of in silico methods and in vitro evaluation. The database of natural compounds was screened against NDM-1 protein, using Glide docking, followed by QM-polarised ligand docking (QPLD). When the screened hits were validated in vitro, withaferin A and mangiferin had good IC50 values in reducing the activity of NDM-1 enzymes, and their fractional inhibitory concentration index (FICI) was ascertained in combination with imipenem. The withaferin A and mangiferin-NDM-1 docking complexes were analyzed for structural stability by molecular dynamic simulation analysis using GROMACS for 100 ns. The molecular properties of the natural compounds were then calculated using density functional theory (DFT). Withaferin A and mangiferin showed promising inhibitory activity and can be a natural compound candidate inhibitor synergistically used along with carbapenems against NDM-1 producing A. baumannii.
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JOURNAL OF MOLECULAR STRUCTURE
·
2022
·
IF 3.841
Rui Chen,Qiuyue Li,Kai Xu,Zhiwei Zhang,Tianhua Wang,Jinkang Ma,Yan Xi,Lifeng Cao,Bing Teng,Haitao Wu
In this present work, a chalcone derivative 1-(4-Chlorophenyl)-3-(4-ethoxyphenyl)-prop-2-en-1-one is investigated using the density functional theory. PES scan is used to find the most stable conformational structure of the title compound. The geometrical parameters, FT-IR and FT-Raman spectra are performed by the DFT method with B3LYP/6-311+G basis set, which are very comparable with the experimental results. UV-Vis spectrum, frontier molecular orbitals, global reactivity descriptors, molecular electrostatic potential surface, NLO parameters and Mulliken charge in the gas phase, various polar and non-polar solvents are performed to reveal solvents effect. Further, it is found that the electronic properties show a good correlation with the polarity of solvents. Hirshfeld Surface analysis demonstrates H···H contact is dominant in the crystal packing. By means of molecular reactivity descriptors such as natural bond orbital analysis, Fukui function and dual descriptor analysis, the chemical reactivity is theoretically estimated. ELF and LOL are used to access the energy density of electrons. Molecular docking illustrates ECC may be a potential inhibitor for 6R3K protein.
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Cureus Journal of Medical Science
·
2024
·
IF 1
Ye-Ran Mao,Ling-Yi Zhu,Ruo-Fei Du,Xiao-Yu Liu,Zhidan Liu,Li Li
Background and objectives: In ancient China, bee venom was widely used to treat various diseases. Although using bee venom is not currently a mainstream medical method, some have applied it to treat certain conditions, including idiopathic facial paralysis (IFP). Recently, melittin (Mel), the main active component of bee venom, has been shown strong anti-inflammatory and analgesic effects. However, how bee venom improves neurological dysfunction in facial paralysis remains unknown. This study aimed to investigate the anti-neurotraumatic effect of Mel on Schwann cells (SCs), the main cells of the neuron sheath, injured by oxidative stress. Methods: A model of hypoxic SCs was established, and CCK-8 assay, siRNA transfection, enzyme-linked immunosorbent assay, quantitative reverse transcription-polymerase chain reaction, western blot, immunofluorescence, and cell ultrastructure analyses were conducted to investigate the mitigation of hypoxia-induced damage to SCs in vitro, revealing the effects of Mel on oxidative stress injury in SCs. Results: The overexpression of HIF-1α in CoCl 2 -induced SCs (p < 0.05) indicated the establishment of an SCs hypoxia model. The proliferation and regeneration process of the hypoxic SCs enhanced in the Mel-treated group compared to the CoCl 2 group has been proven through the CCK-8 experiment (p < 0.0001) and S-100 mRNA expression detection (p < 0.0001). The increased level of reactive oxygen species (ROS) (p < 0.001) and decreased superoxide dismutase (SOD) levels (p < 0.05) in the CoCl 2 -induced SCs indicated that Mel can alleviate the oxidative stress damage to SCs induced by CoCl 2 . Mel alleviated oxidative stress and inflammation in hypoxic SCs by reducing pro-inflammatory cytokines IL-1β (p < 0.0001) and TNF-α (p < 0.0001). In addition, Mel augmented cellular vitality and regulated indicators related to oxygen metabolism, cell repair, neurometabolism, and vascular endothelial formation after hypoxia, such as C-JUN (p < 0.05), glial cell line-derived neurotrophic factor (GDNF; p < 0.001), vascular endothelial growth factor (VEGF; p < 0.05), hypoxia-inducible factor 1-alpha (HIF-1α; p < 0.05), interleukin-1 receptor type 1 (IL-1R1; p < 0.05), enolase1 (ENO1; p < 0.05), aldose reductase (AR; p < 0.01), SOD (p < 0.05), nerve growth factor (NGF; p < 0.05), and inducible nitric oxide synthase (iNOS; p < 0.05). In terms of its mechanism, Mel inhibited the expression of proteins associated with the NF-κB pathway such as IKK (p < 0.01), p65 (p < 0.05), p60 (p < 0.001), IRAK1 (p < 0.05), and increased IKB-α (p < 0.0001). Moreover, knocking out of IL-1R1 in the si-IL-1R1 group enhanced the therapeutic effect of Mel compared to the Mel-treated group (all of which p < 0.05). Conclusion: This research provided evidence of the substantial involvement of IL-1R1 in oxidative stress damage caused by hypoxia in SCs and proved that Mel alleviated oxidative stress injury in SCs by targeting IL-1R1 to downregulate the NF-κB-mediated inflammatory response. Mel could potentially serve as an innovative therapeutic approach for the treatment of IFP.
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