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Inhibitive effects of anti-oxidative vitamins on mannitol-induced apoptosis of vascular endothelial cells 被引量:12
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作者 PAN Kai-yu SHEN Mei-ping +2 位作者 YE Zhi-hong DAI Xiao-na SHANG Shi-qiang 《Journal of Zhejiang University-Science B(Biomedicine & Biotechnology)》 SCIE CAS CSCD 2006年第10期825-829,共5页
Objective: Study blood vessel injury and gene expression indicating vascular endothelial cell apoptosis induced by mannitol with and without administration of anti-oxidative vitamins. Methods: Healthy rabbits were ran... Objective: Study blood vessel injury and gene expression indicating vascular endothelial cell apoptosis induced by mannitol with and without administration of anti-oxidative vitamins. Methods: Healthy rabbits were randomly divided into four groups. Mannitol was injected into the vein of the rabbit ear in each animal. Pre-treatment prior to mannitol injection was per- formed with normal saline (group B), vitamin C (group C) and vitamin E (group D). Blood vessel injury was assessed under electron and light microscopy. In a second experiment, cell culture specimen of human umbilical vein endothelial cells were treated with mannitol. Pre-treatment was done with normal saline (sample B), vitamin C (sample C) and vitamin E (sample D). Total RNA was extracted with the original single step procedure, followed by hybridisation and analysis of gene expression. Results: In the animal experiment, serious blood vessel injury was seen in group A and group B. Group D showed light injury only, and normal tissue without pathological changes was seen in group C. Of all 330 apoptosis-related genes analysed in human cell culture specimen, no significant difference was seen after pre-treatment with normal saline, compared with the gene chip without pre-treatment. On the gene chip pre-treated with vitamin C, 45 apoptosis genes were down-regulated and 34 anti-apoptosis genes were up-regulated. Pre-treatment with vitamin E resulted in the down-regulation of 3 apoptosis genes. Conclusion: Vitamin C can protect vascular endothelial cells from mannitol-induced injury. 展开更多
关键词 Anti-oxidative vitamins inhibitive effects APOPTOSIS Vascular endothelial cells MANNITOL
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Synthesis, Characterization and Corrosion Inhibitive Properties of New Thiazole Based Polyamides Containing Diarylidenecyclohexanone Moiety 被引量:1
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作者 K.I.Aly M.A.Hussein 《Chinese Journal of Polymer Science》 SCIE CAS CSCD 2015年第1期1-13,共13页
The present work aimed to synthesize a new interesting series of thiazole based polyamides containing diarylidenecyclohexanone moiety 5a-5f using low temperature solution polycondensation technique. The new polymers w... The present work aimed to synthesize a new interesting series of thiazole based polyamides containing diarylidenecyclohexanone moiety 5a-5f using low temperature solution polycondensation technique. The new polymers were synthesized by the reaction of thiazole based monomer namely, bis(2-aminothiazol-4-ylbenzylidene)cyclohexanone 3 with different aliphatic and aromatic diacid chlorides using NMP, and in the presence of anhydrous Li Cl as catalyst. Adipoyl, sebacoyl, oxaloyl, terephthaloyl, isophthaloyl dichlorides and biphenyl dicarbonyl dichloride were used as diacid chlorides. The structure of the model compound 4 as well as the new polymers was confirmed by correct elemental and spectral analyses. The thermal properties of those polymers were evaluated by TGA and DTG measurements and correlated to their structural units, beside X-ray diffraction analysis, solubility and viscometry measurements. The inherent viscosities for the synthesized polymers were in the range 0.6–1.03 d L/g. On the other hand the corrosion inhibitive properties of monomer 3 as well as polyamides 5d and 5f as selected examples were carried out on carbon-steel in 0.5 mol/L H2SO4 at 40 °C. The calculated inhibition efficiency(IE%) for polymer 5d was in the range(82 ± 6)% in all selected concentrations. The best value of IE% was obtained at 1 mg/L to reach 98.24% for polymer 5d and at 0.5 mg/L to reach 87.75% for polymer 5f. 展开更多
关键词 Diarylidenecyclohexanone Polyamides Synthesis Characterization Thiazole Corrosion inhibitive properties.
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A novel indirect inhibitive immunoassay for sulfamethoxazole
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作者 Ping Ping Tang Zhao Feng Luo +1 位作者 Ji Bao Cai Qing De Su 《Chinese Chemical Letters》 SCIE CAS CSCD 2010年第8期955-958,共4页
A new indirect inhibitive immunoassay using surface plasmon resonance(SPR) coupled with molecularly imprinted polymer(MIP) was developed.A sulfamethoxazole(SMX) MIP coating capillary was produced and used as an ... A new indirect inhibitive immunoassay using surface plasmon resonance(SPR) coupled with molecularly imprinted polymer(MIP) was developed.A sulfamethoxazole(SMX) MIP coating capillary was produced and used as an in-tube solid phase extraction(SPE) device.The MIP coating formed a nanometer film on the inner wall of the capillary.The anti-SMX mono-antibody was inhibited by SMX extracted by the MIP coating in a dose-dependent manner.The calibration curve was generated by linear fit over the range of 0.04-10.00 ng/mL.The limit of detection was 0.01 ng/mL.This method has high sensitivity and can be performed automatically. 展开更多
关键词 SULFAMETHOXAZOLE Molecularly imprinted polymer Surface plasmon resonance Indirect inhibitive immunoassay
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INHIBITIVE ACTION OF INORGANIC COMPOUND ON CORROSION OF ALUMINIUM IN HYDROCHLORIC ACID
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作者 Qing Hai CAI Bin LU Ling Fei CUI Department of Chemistry,Harbin Normal University,Harbin 150080 《Chinese Chemical Letters》 SCIE CAS CSCD 1992年第1期75-76,共2页
The inhibitive action of CaSO_4 towards corrosion of aluminium in 1 mol/L HCl has been inveetigated by using fluorometrio and weight loss techniques.The results show that the inhibitor exhibits an outstanding function... The inhibitive action of CaSO_4 towards corrosion of aluminium in 1 mol/L HCl has been inveetigated by using fluorometrio and weight loss techniques.The results show that the inhibitor exhibits an outstanding function of inhibition,especially at higher tempe- ratures,and it was found to be predomiantly of cathodic rate control.Ths mechanism of inhibition and the effect of CdSO_4 on the corrosion kinetics are also discussed. 展开更多
关键词 ACTION inhibitive ACTION OF INORGANIC COMPOUND ON CORROSION OF ALUMINIUM IN HYDROCHLORIC ACID
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The inhibitive study of egg shell powder on uns n08904 austenitic stainless steel corrosion in chloride solution 被引量:1
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作者 O.Sanni A.P.I.Popoola O.S.I.Fayomi 《Defence Technology(防务技术)》 SCIE EI CAS CSCD 2018年第5期463-468,共6页
The effect of egg shell powder(ES) as an environmental friendly inhibitor was studied for its corrosion inhibitive tendency on N08904 austenitic stainless steel in simulated saline(3.5% NaCl) solution using potentiody... The effect of egg shell powder(ES) as an environmental friendly inhibitor was studied for its corrosion inhibitive tendency on N08904 austenitic stainless steel in simulated saline(3.5% NaCl) solution using potentiodynamic polarization, weight loss, and SEM/EDX at room temperature. The experimental data explained the effective performance of ES with values of 57%-100% inhibition efficiency, at 2 g-10 g inhibitor concentration from weight loss tests due to the inhibition of stainless steel. The electrochemical action was as a result of the ionized particles which inhibit the compound influencing the redox reaction mechanism causing surface corrosion. ES's best performance was achieved when 6 g of the inhibitor concentration was added to the saline medium. Corrosion rate value decreased progressively with the presence of inhibitor because of anions adsorption at the interface of the metal film. Corrosion potential(Ecorr) value was found to decrease from-0.3991 V to-0.3447 V in the presence of inhibitor at 2 g concentration, decreasing gradually to-0.2048 at 6 g inhibitor concentration. The compounds identified in the ES completely adsorbed onto the surface of stainless steel as observed from the EDX analysis. The ES adsorption on stainless steel surface obeyed Langmuir adsorption isotherm. A corroded morphology with pits was observed in the SEM results without ES which contrast the images obtained with the presence of ES. 展开更多
关键词 AUSTENITIC STAINLESS steel CORROSION Inhibition EGG shell Chloride LANGMUIR
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The Inhibitive Effect of para-Amino Benzoic Acid and Its Polymer on Corrosion of Iron in 1 mol/L HC1 Solution
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作者 P.Manivel G. Venkatachari 《Journal of Materials Science & Technology》 SCIE EI CAS CSCD 2006年第3期301-305,共5页
Poly p-aminobenzoic acid has been synthesized by chemical oxidation method. The inhibitive effect of poly p-aminobenzoic acid on iron in 1 mol/L HCI solution was investigated by polarization and electrochemical impeda... Poly p-aminobenzoic acid has been synthesized by chemical oxidation method. The inhibitive effect of poly p-aminobenzoic acid on iron in 1 mol/L HCI solution was investigated by polarization and electrochemical impedance spectroscopy and compared with that of monomer p-aminobenzoic acid. The effectiveness of poly p-aminobenzoic acid is very high in comparison with that of monomer. The results show that both cathodic and anodic processes were suppressed by p-aminobenzoic acid and poly p-aminobenzoic acid of iron dissolution in 1 mol/L HCI by their adsorption on the iron surface. The inhibition efficiency of both p-aminobenzoic acid and poly p-aminobenzoic acid were found to increase with the inhibitor concentrations. Ultraviolet (UV) reflectance studies of the iron surface after exposure to inhibitor acid show that poly p-aminobenzoic acid is strongly adsorbed on iron surface. 展开更多
关键词 p-aminobenzoic acid Poly p-aminobenzoic acid HCL INHIBITION CORROSION
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Bio-inhibitive effect of an algal symbiotic bacterium on corrosion of magnesium in marine environment
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作者 Yuqiao Dong Guang-Ling Song +1 位作者 Yuqing Xu Dajiang Zheng 《Journal of Magnesium and Alloys》 SCIE EI CAS CSCD 2023年第12期4603-4618,共16页
It is a longstanding and challenging task to develop sustainable environment-friendly and cost-effective corrosion-protection technologies for Mg alloys, especially under marine conditions in which corrosion can norma... It is a longstanding and challenging task to develop sustainable environment-friendly and cost-effective corrosion-protection technologies for Mg alloys, especially under marine conditions in which corrosion can normally be significantly accelerated by bacterial activity. However,this paper reports on the corrosion of highly active Mg interestingly inhibited by an algal-symbiotic bacterium Bacillus altitudinis. The corrosion of Mg in the presence of the bacterium drastically reduced by one order of magnitude after 14 days of immersion. This means that the algal-symbiotic bacterium widely available in natural ocean environments may be employed as a green and sustainable inhibitor in the marine industry. Based on electrochemical measurements, surface analyses and microbe experiments, a combined inhibition mechanism is proposed in the paper to interpret the interesting corrosion behavior of Mg. 展开更多
关键词 MAGNESIUM Corrosion inhibition Marine environment BIOFILM BACTERIUM
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Inhibitive effects of some treatments on the browning rate during the in vitro culture of Acacia karroo Hayne
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作者 Zhu Hong-lang Janusz Zwolinski +2 位作者 Yin Wei-lun Liu Yu-jun Wang Hua-fang 《Forestry Studies in China》 CAS 2006年第4期43-46,共4页
Acacia karroo Hayne is an arbor species widely distributed in South Africa with the characteristics of fast growth and drought resistance. The species was introduced to China recently. In vitro culture is an effective... Acacia karroo Hayne is an arbor species widely distributed in South Africa with the characteristics of fast growth and drought resistance. The species was introduced to China recently. In vitro culture is an effective method to rapidly produce plants and a strategy to minimize somaclonal variation among regenerated plants. Browning, however, is a problem in establishing the in vitro culture system. The present study diminished the problem by selecting explants, using different browning inhibitors and chilling treatment. Results showed that the use of embryos as explants reduced the browning ratio to 46.7%, whilst stem segment explants were browned up to 56.7%. The adventitious buds were successfully induced in the modified tissue culture medium supplemented with 5.0 mg·L^-1 6-BA and 0.1 mg·L^-1 NAA. The proliferation coefficient of adventitious buds is 2.8. 展开更多
关键词 Acacia karroo Hayne BROWNING INHIBITION PROLIFERATION
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Inhibitive Effect of Umbellatus Polyporus Polysaccharide on Cachexic Manifestation induced by toxohormone-L in Rats
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作者 吴耕书 张荔彦 奥田拓道 《Chinese Journal of Integrative Medicine》 SCIE CAS 1997年第3期173-173,共1页
Inhibitive Effect of Umbellatus Polyporus Polysaccharide on Cachexic Manifestation induced by toxohormone-L ... Inhibitive Effect of Umbellatus Polyporus Polysaccharide on Cachexic Manifestation induced by toxohormone-L in RatsWUGeng-shu... 展开更多
关键词 Polyporus MANIFESTATION INDUCED Cachexic EFFECT POLYSACCHARIDE Umbellatus by inhibitive of
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Secretase inhibition in Alzheimer's disease therapeutics reveals functional roles of amyloid-beta42
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作者 Timothy Daly Bruno P.Imbimbo 《Neural Regeneration Research》 2026年第5期2003-2004,共2页
In the words of the late Sir Colin Blakemore,neurologists have historically sought to infer brain functions in a manner akin to to king a hammer to a computeranalyzing localized anatomical lesions caused by trauma,tum... In the words of the late Sir Colin Blakemore,neurologists have historically sought to infer brain functions in a manner akin to to king a hammer to a computeranalyzing localized anatomical lesions caused by trauma,tumors,or strokes,noting deficits,and inferring what functions certain brain regions may be responsible for.This approach exemplifies a deletion heuristic,where the absence of a specific function reveals insights about the underlying structures or mechanisms responsible for it.By observing what is lost when a particular brain region is damaged,throughout the history of the field,neurologists have pieced together the intricate relationship between anatomy and function. 展开更多
关键词 infer brain functions secretase inhibition Alzheimers disease therapeutics king hammer deletion heuristic amyloid beta deletion heuristicwhere observing what l
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Corrigendum
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《Neural Regeneration Research》 2026年第4期1276-1276,共1页
In the article titled“Inhibiting SHP2 reduces glycolysis,promotes microglial M1 polarization,and alleviates secondary inflammation following spinal cord injury in a mouse model,”published in Neural Regeneration Rese... In the article titled“Inhibiting SHP2 reduces glycolysis,promotes microglial M1 polarization,and alleviates secondary inflammation following spinal cord injury in a mouse model,”published in Neural Regeneration Research(Ding et al.,2025),the title was incorrectly presented due to an error during the language polishing process. 展开更多
关键词 language polishing process spinal cord injury reduces neural regeneration research ding INHIBITING mouse model published microglial m polarizationand SHP
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Empowering the NSC-34 cell line as a motor neuron model: Cytosine arabinoside's action
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作者 Giuseppe Vitale Susanna Amadio +1 位作者 Francesco Liguori Cinzia Volonté 《Neural Regeneration Research》 2026年第1期357-364,共8页
The NSC-34 cell line is a widely recognized motor neuron model and various neuronal differentiation protocols have been exploited. Under previously reported experimental conditions, only part of the cells resemble dif... The NSC-34 cell line is a widely recognized motor neuron model and various neuronal differentiation protocols have been exploited. Under previously reported experimental conditions, only part of the cells resemble differentiated neurons;however, they do not exhibit extensive and time-prolonged neuritogenesis, and maintain their duplication capacity in culture. The aim of the present work was to facilitate long-term and more homogeneous neuronal differentiation in motor neuron–like NSC-34 cells. We found that the antimitotic drug cytosine arabinoside promoted robust and persistent neuronal differentiation in the entire cell population. Long and interconnecting neuronal processes with abundant growth cones were homogeneously induced and were durable for up to at least 6 weeks in culture. Moreover, cytosine arabinoside was permissive, dispensable, and mostly irreversible in priming NSC-34 cells for neurite initiation and regeneration after mechanical dislodgement. Finally, the expression of the cell proliferation antigen Ki67 was inhibited by cytosine arabinoside, whereas the expression levels of neuronal growth associated protein 43, vimentin, and motor neuron–specific p75, Islet2, homeobox 9 markers were upregulated, as confirmed by western blot and/or confocal immunofluorescence analysis. Overall, these findings support the use of NSC-34 cells as a motor neuron model for properly investigating neurodegenerative mechanisms and prospectively identifying neuroprotective strategies. 展开更多
关键词 cytosine arabinoside Islet2 Hb9 Ki67 mitosis inhibition neurite initiation neurite regeneration neuronal differentiation protocol NSC-34 P75
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Inhibitive effects of three compositae plants on Microcystis aeruginosa 被引量:4
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作者 Weihao ZHANG Fuqing XU +2 位作者 Wei HE Xing ZHENG Chen YANG 《Frontiers of Environmental Science & Engineering》 SCIE EI CSCD 2009年第1期48-55,共8页
Based on common phenomena of biochemical interaction between plants and microorganisms,the inhibitive effects of three common terrestrial compositae plants,namely Artemisia lavandulaefolia DC.,Conyza canadensis(L.)Cro... Based on common phenomena of biochemical interaction between plants and microorganisms,the inhibitive effects of three common terrestrial compositae plants,namely Artemisia lavandulaefolia DC.,Conyza canadensis(L.)Cronq.,and Kalimeris indica(L.)Sch.-Bip.on the blue algae Microcystis aeruginosa was studied.Live compositae plants are co-cultivated with algae in two different inoculation doses for 10 days in 5-pools incubators,in order to exclude the influence of bacteria and nutrients.The results show that Artemisia lavandulaefolia DC has the most inhibitive potential among the three plants as evidenced by the most drastic decrease in optical density(OD680)of the algae.The inhibition rate is 93.3%(with initial inoculation dose of 2.0×10^(6) Cells/mL)and 89.3%(with initial inoculation dose of 4.0×10^(6) Cells/mL)respectively on the 10th day of cultivation.The average inhibition rate during the later half of the experiment is 0.76(with initial inoculation dose of 2.0×10^(6) Cells/mL)and 0.71(with initial inoculation dose of 4.0×10^(6) Cells/mL),respectively.Logistic model analysis shows that compositae plants such as A.lavandulaefolia DC.causes the reduction of the habitat’s carrying capacity of algae.ANOVA analysis is used to determine the similarity and differences between every experimental group and an average inhibitive rate model is used to evaluate the inhibition effects.The results show that A.lavandulaefolia DC.,which grow well in the aquatic environment,may have a great potential in controlling algae bloom in eutrophic water. 展开更多
关键词 ALLELOPATHY compositae plants Microcystis aeruginosa inhibition rate logistic model analysis
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Discoidin domain receptor 2 is an important modulator of BMP signaling during heterotopic bone formation 被引量:1
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作者 Fashuai Wu Chunxi Ge +4 位作者 Haichun Pan Yuanyuan Han Yuji Mishina Vesa Kaartinen Renny T.Franceschi 《Bone Research》 2025年第1期121-138,共18页
Bone morphogenetic proteins are essential for bone regeneration/fracture healing but can also induce heterotopic ossification(HO).Understanding accessory factors modulating BMP signaling would provide both a means of ... Bone morphogenetic proteins are essential for bone regeneration/fracture healing but can also induce heterotopic ossification(HO).Understanding accessory factors modulating BMP signaling would provide both a means of enhancing BMP-dependent regeneration while preventing HO.This study focuses on the ability of the collagen receptor,discoidin domain receptor 2(DDR2),to regulate BMP activity.As will be shown,induction of bone formation by subcutaneous BMP2 implants is severely compromised in Ddr2-deficient mice.In addition,Ddr2 deficiency attenuates HO in mice expressing the ACVR1 mutation associated with human fibrodysplasia ossificans progressiva.In cells migrating into BMP2 implants,DDR2 is co-expressed with GLI1,a skeletal stem cell marker,and DDR2/GLI1-positive cells participate in BMP2-induced bone formation where they contribute to chondrogenic and osteogenic lineages.Consistent with this distribution,conditional knockout of Ddr2 in Gli1-expressing cells inhibited bone formation to the same extent seen in globally Ddr2-deficient animals.This response was explained by selective inhibition of Gli1+cell proliferation without changes in apoptosis.The basis for this DDR2 requirement was explored further using bone marrow stromal cells.Although Ddr2 deficiency inhibited BMP2-dependent chondrocyte and osteoblast differentiation and in vivo,bone formation,early BMP responses including SMAD phosphorylation remained largely intact.Instead,Ddr2 deficiency reduced the nuclear/cytoplasmic ratio of the Hippo pathway intermediates,YAP and TAZ.This suggests that DDR2 regulates Hippo pathway-mediated responses to the collagen matrix,which subsequently affect BMP responsiveness.In summary,DDR2 is an important modulator of BMP signaling and a potential therapeutic target both for enhancing regeneration and treating HO. 展开更多
关键词 inhibited HEALING MODULATOR
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A Novel Method for Enhancing Oil Recovery by Thickened Supercritical CO_(2) Flooding in High-Water-Cut Mature Reservoirs 被引量:1
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作者 Kaoping Song Daigang Wang +3 位作者 Fengyuan Zhang Hong Fu Mingxing Bai Hamid Emami-Meybodi 《Engineering》 2025年第5期59-69,共11页
High-water-cut mature reservoirs typically serve as the“ballast”for ensuring China’s annual crude oil production of 200 million tons.Despite the use of water flooding and chemical methods,over 40%of crude oil remai... High-water-cut mature reservoirs typically serve as the“ballast”for ensuring China’s annual crude oil production of 200 million tons.Despite the use of water flooding and chemical methods,over 40%of crude oil remains unexploited.It is critical to develop efficient revolutionary technologies to further enhance oil recovery(EOR)by a large percentage in high-water-cut mature reservoirs.To address this issue,the potential of vertical remaining oil in Daqing Oilfield is first analyzed from massive monitoring data.Using molecular dynamics simulation to design optimal synthetic routine,a copolymer without flu-orine or silicon is synthesized by modifying vinyl acetate(VAc)with maleic anhydride(MA)and styrene(St),and treated as a supercritical CO_(2)(scCO_(2))thickener.The underlying EOR mechanism of the scCO_(2) thickener is thereafter clarified by high-temperature,high-pressure oil displacement experiments.The EOR effect by thickened scCO_(2) flooding in a typical high-water-cut mature reservoir is predicted,and future technological advancements of the technique are ultimately discussed.Results show that the ver-tical remaining oil enriched in weakly swept zones is a primary target for further EOR in high-water-cut mature reservoirs.The copolymer typically exhibits good solubility,strong dispersion stability,and high thickening effect in scCO_(2).Under an ambient pressure of 10 MPa and a temperature of 50℃,the disso-lution of copolymer at a mass concentration of 0.2%can effectively increase the viscosity of scCO_(2) by 39.4 times.Due to the synergistic effect between expanding vertical swept volume and inhibiting gas channel-ing,crude oil recovery can be further enhanced by 23.1%for a typical high-water-cut mature reservoir when the scCO_(2) viscosity is increased by 50 times.Our understandings demonstrate that the thickened scCO_(2) flooding technology has significant technical advantages in high-water-cut mature reservoirs,with challenges and future development directions in field-scale applications also highlighted. 展开更多
关键词 High-water-cut mature reservoirs Supercritical CO_(2)thickener Thickening effect Enhance oil recovery Inhibit gas channeling Expand swept volume
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SBL-JP-0004:A promising dual inhibitor of JAK2 and PI3KCD against gastric cancer
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作者 HASSAN M.OTIFI 《Oncology Research》 SCIE 2025年第1期235-243,共9页
Background:Gastric cancer(GC)remains a global health burden and is often characterized by heterogeneous molecular profiles and resistance to conventional therapies.The phosphoinositide 3-kinase and PI3K and Janus kina... Background:Gastric cancer(GC)remains a global health burden and is often characterized by heterogeneous molecular profiles and resistance to conventional therapies.The phosphoinositide 3-kinase and PI3K and Janus kinase(JAK)signal transducer and activator of transcription(JAK-STAT)pathways play pivotal roles in GC progression,making them attractive targets for therapeutic interventions.Methods:This study applied a computational and molecular dynamics simulation approach to identify and characterize SBL-JP-0004 as a potential dual inhibitor of JAK2 and PI3KCD kinases.KATOIII and SNU-5 GC cells were used for in vitro evaluation.Results:SBL-JP-0004 exhibited a robust binding affinity for JAK2 and PI3KCD kinases,as evidenced by molecular docking scores and molecular dynamics simulations.Binding interactions and Gibbs binding free energy estimates confirmed stable and favorable interactions with target proteins.SBL-JP-0004 displayed an half-maximal inhibitory concentration(IC_(50))value of 118.9 nM against JAK2 kinase and 200.9 nM against PI3KCD enzymes.SBL-JP-0004 exhibited potent inhibition of cell proliferation in KATOIII and SNU-5 cells,with half-maximal growth inhibitory concentration(GI50)values of 250.8 and 516.3 nM,respectively.A significant elevation in the early phase apoptosis(28.53%in KATOIII cells and 26.85%in SNU-5 cells)and late phase apoptosis(17.37%in KATOIII cells and 10.05%in SNU-5 cells)were observed with SBL-JP-0004 treatment compared to 2.1%and 2.83%in their respective controls.Conclusion:The results highlight SBL-JP-0004 as a promising dual inhibitor targeting JAK2 and PI3KCD kinases for treating GC and warrant further preclinical and clinical investigations to validate its utility in clinical settings. 展开更多
关键词 Gastric cancer(GC) Dual inhibition JAK2 PI3KCD SBL-JP-0004 Molecular docking Molecular dynamics simulation
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Trichoderma vermifimicola strain TC467 possessing phytopathogen antagonism,plant growth promotion and fungicide resistance
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作者 WANG Hengxu ZENG Zhaoqing ZHUANG Wenying 《菌物学报》 北大核心 2025年第10期102-113,共12页
Trichoderma strains possessing biological control functions have been used in agriculture against phytopathogens.Currently,only very few species of the genus were applied to or involved in plant disease control.Discov... Trichoderma strains possessing biological control functions have been used in agriculture against phytopathogens.Currently,only very few species of the genus were applied to or involved in plant disease control.Discovery of additional useful resources is desperately needed.In this study,biocontrol effect of Trichoderma vermifimicola strain TC467 was evaluated by dual confrontation culture,cellophane and two-compartment culture,pot experiments,and resistance to chemical fungicides.The results demonstrated that TC467 produced substances essential to phytopathogen control(including siderophore,xylanase and chitinase)and plant growth promoters(producing indole-3-acetic acid and gibberellin).The strain displayed a high inhibition rate against Botrytis cinerea reaching 85.26%;and its non-volatile and volatile secondary metabolites showed the inhibition rates to Sclerotinia sclerotiorum and B.cinerea as high as 84.67%and 47.62%,respectively.In pot experiments,comparing with untreated plants TC467 significantly enhanced the height and fresh weight of lettuce(Lactuca sativa var.ramosa)by 46.69%and 15.33%,respectively.Its fermentation broth effectively minimized the lettuce disease caused by B.cinerea with inhibition rate of 87.76%.In addition,the strain showed higher tolerance to hymexazol water-dispersible granule than that to other tested fungicides;at the concentration of 0.42 mg/L the growth rate of TC467 can even approach 98.19%.T.vermifimicola strain TC467 has the potential for practical application in biocontrol especially plant diseases caused by B.cinerea,which extends our knowledge of nature beneficial resources. 展开更多
关键词 biological control TRICHODERMA Botrytis cinerea growth inhibition rate plant diseases
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Synthesis and Anti-acute Myeloid Leukemia Activity of Cyclopropane-1,1-diamide Derivatives Containing Imidazo[1,2-a]pyridine
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作者 Wu Lüjia Li Jiangdong +4 位作者 Shi Zhonghua Jin Xin Wang Xianheng Zhao Changkuo Huang Qiang 《有机化学》 北大核心 2025年第1期286-296,共11页
A series of cyclopropane-1,1-diamide derivatives containing imidazo[1,2-a]pyridine were synthesized.The inhibitory effects of these compounds on FLT3-ITD kinase and their anti-proliferative activities against two acut... A series of cyclopropane-1,1-diamide derivatives containing imidazo[1,2-a]pyridine were synthesized.The inhibitory effects of these compounds on FLT3-ITD kinase and their anti-proliferative activities against two acute myeloid leukemia cell lines expressing FLT3-ITD were evaluated.With focused on the different substitutions of imidazo[1,2-a]pyridine,a preliminary exploration of the structure-activity relationship was conducted for 22 compounds.The results revealed that most compounds exhibited certain inhibitory effects on FLT3-ITD kinase with IC_(50) values below 0.5μmol·L^(-1).Among them,N-(4-fluorophenyl)-N-(4-(7-((2-morpholinoethyl)carbamoyl)imidazo[1,2-a]pyridine-3-carbonyl)phenyl)cyclopropane-1,1-dicarboxamide(12a)demonstrated the most potent FLT3-ITD kinase inhibitory activity and the strongest anti-proliferative effect on the MV4-11 and MOLM-13 cell lines expressing FLT3-ITD with IC50 values of 0.06 and 0.2μmol·L^(-1),respectively.Moreover,compound 12a did not exhibit anti-proliferative activity against cell lines without FLT3 mutations,such as THP-1,HCT-116,A549,HepG2,K562,and MCF-7,and it displayed non-cytotoxicity towards normal human renal tubular epithelial cells(HK-2),human liver progenitor cells(HepaRG),and HEK293(human embryonic kidney cells).Although 12a exhibits inferior inhibitory activity against FLT3-ITD kinase and anti-tumor cell proliferation compared to C abozantinib in this study,it can provide a reference for further research into FLT3-ITD inhibitors. 展开更多
关键词 imidazole[1 2-a]pyridine antiproliferative activity INHIBITION FLT3 kinase acute myeloid leukemia
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Insights into rapid screening and molecular mechanism of novel Rosa roxburghii seeds pancreatic lipase/cholesterol esterase inhibitory peptides:a combined in silico and in vitro perspective
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作者 Hao Yin Jiangxiong Zhu +5 位作者 Yu Zhong Danfeng Wang Yun Deng Yongli Jiang Linnan Yang Lutao Gao 《Food Science and Human Wellness》 2025年第7期2680-2692,共13页
Rosa roxburghii seeds are by-products of R.roxburghii processing,and their protein hydrolysates(RTSPHs)were found to possess a variety of biological activities.This study aimed to rapidly identify pancreatic lipase(PL... Rosa roxburghii seeds are by-products of R.roxburghii processing,and their protein hydrolysates(RTSPHs)were found to possess a variety of biological activities.This study aimed to rapidly identify pancreatic lipase(PL)and cholesterol esterase(CE)inhibitory peptides in RTSPHs and to elucidate their molecular mechanisms by combining peptidomics and virtual screening.The simulated intestinal environment worsened the peptide’s inhibition of PL but catalyzed the inhibition of CE.The fraction less than 3 kDa in RTSPHs was found to have the highest PL/CE inhibitory activity,among which 17 promising inhibitory peptides were identified and screened by peptidomics and virtual screening.LFCMH,RIPAGSPF,and YFRPR showed good inhibitory abilities against both PL and CE.Molecular docking showed that peptides inhibited PL and CE mainly by hydrogen bonding and hydrophobic interactions with residues in the active site and surface loop.Inhibition kinetic revealed that the peptides were competitive and mixed-type inhibitors of PL/CE.Further,the three peptides,LFCMH,RIPAGSPF,and YFRPR,could effectively inhibit 3T3-L1 preadipocytes differentiation,increase high-density lipoprotein cholesterol content and decrease low-density lipoprotein cholesterol content.This study suggests that combining peptidomics with virtual screening is an effective strategy for rapid screening of PL/CE inhibitory peptides. 展开更多
关键词 Bioactive peptide Enzyme inhibiting Virtual screening Molecular docking Inhibition kinetics
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Correction to:Overexpression of Tau Rescues Nogo-66-Induced Neurite Outgrowth Inhibition In Vitro
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作者 Yu-Chao Zuo Hong-Lian Li +4 位作者 Nan-Xiang Xiong Jian-Ying Shen Yi-Zhi Huang Peng Fu Hong-Yang Zhao 《Neuroscience Bulletin》 2025年第9期1710-1710,共1页
Correction to:Neurosci.Bull.December,2016,32(6):577–584.https://doi.org/10.1007/s12264-016-0068-z In this article,in Fig 5A,the picture of the Vector+Nogo-66 group was incorrect and should have appeared as shown below.
关键词 VITRO OVEREXPRESSION neurite outgrowth TAU NOGO INHIBITION
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