MOLECULES
·
2025
·Vol. 30
·期 11
·2400
·
IF 4.6
Ming Yuan,Huai Wang,Mingjun Yu,Sen Yao,Risheng Yao
Cisplatin (CIS) is a widely used chemotherapeutic agent that is highly effective against various cancers. However, its clinical application is frequently limited by its substantial nephrotoxic side effects. The gastrin-releasing peptide receptor (GRPR), a critical regulator in inflammatory diseases, has been identified as a promising therapeutic target. Our previous studies have demonstrated that the GRPR antagonists PD176252 and RH-1402 can mitigate CIS-induced nephrotoxicity through anti-inflammatory mechanisms. Based on these findings, we designed and synthesized a series of 2-arylpropanoic acid-L-tryptophan derivatives to enhance the therapeutic effects. Among these compounds,3mexhibited superior renal protection by significantly improving mouse renal tubular epithelial cell (mRTEC) viability from 50.2 ± 2.6% to 80.5 ± 3.9%, surpassing PD176252 (70.8 ± 1.4%) and RH-1402 (73.9 ± 3.7%). Moreover, compound3mmarkedly reduced the expression of kidney injury molecule-1 (KIM-1) and inflammatory cytokines [Tumor Necrosis Factor-α (TNF-α), Interleukin-6 (IL-6), Monocyte Chemoattractant Protein-1 (MCP-1)]. Finally, molecular docking results revealed that3mexhibited a high binding affinity for GRPR. Computational predictions using SwissADME further indicated that3mpossesses favorable drug-like properties, thereby supporting its potential as a promising candidate for mitigating CIS-induced nephrotoxicity.
研究领域:
药理学
·
肿瘤学
·
毒理学
·
分子生物学
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DOI
PubMed
高影响因子
TALANTA
·
2021
·
IF 6.057
Huazheng Yu,Yanhong Li,Aisheng Huang
Sialic acid (SA) is a crucial component of glycoproteins and glycolipids on the cellular membrane, which is essential for maintaining the function of cell membranes, such as cell recognition and communication. Simultaneously, sialic acid plays a significant role in many physiological and pathological processes. Hence, it is urgent to develop a simple and sensitive strategy for determining sialic acid. In this work, a new metal-organic framework called UiO-66-NH 2 @B(OH) 2 has been designed and synthesized for the recognition and detection of sialic acid. The boronic acid functional group in UiO-66-NH 2 @B(OH) 2 can bind to a diol moiety of the glycerol side chain of sialic acid, which will attenuate or even quench the fluorescence of UiO-66-NH 2 @B(OH) 2 , thus opening a new road to detect sialic acid. Based on the measurement results, sialic acid can be quantitatively measured in a linear range of 0.05–2.5 mmoL/L with the UiO-66-NH 2 @B(OH) 2 probe. The detection limit of sialic acid is as low as 0.025 mmol/L. Furthermore, the boronic-acid functionalized probe UiO-66-NH 2 @B(OH) 2 displays high sensitivity and high selectivity to recognize the sialic acid in mouse serum samples. Therefore, the developed UiO-66-NH 2 @B(OH) 2 can be used as a promising probe to identify and detect sialic acid in the practical application.
研究领域:
分析化学
·
生物化学
·
材料科学
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DOI
高影响因子
CHROMATOGRAPHIA
·
2019
·Vol. 82
·期 10
·1579-1583
·
IF 1.552
Lou Chunli,Zheng Mengmeng,Xu Yao,Shen Yuting,Kang Jingwu
A sensitive method was developed for detecting 2,2′-azobis(2-amidinopropane) dihydrochloride in polyvinylpyrrolidone by capillary electrophoresis with indirect UV detection. The detection sensitivity was improved significantly using the field-amplified sample injection technique. The background electrolyte was composed of 25 mM imidazole-HCl solution (pH 4.0), in which imidazole acted as the cation probe for the indirect detection at UV 214 nm. Effects of the experimental parameters including pH, the concentration of imidazole as well as the sample injection time on sample preconcentration were investigated and optimized. Under the optimized conditions, baseline separation of 2,2′-azobis(2-amidinopropane) ion with other ions in the polyvinylpyrrolidone samples was achieved within 8 min. The RSD% for the repeatability of the migration time and the peak area were determined as 0.95% and 3.47%, respectively. The limit of detection (LOD, S / N = 3) and the limit of quantitation (LOQ, S / N = 10) were determined as 1.11 × 10 −5 M and 2.77 × 10 −5 M, respectively. The measured recovery at three concentration levels was in the range of 101–104%. This method was successfully applied to detect 2,2′-azobis(2-amidinopropane) in the commercial polyvinylpyrrolidone samples.
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产品关联
DOI
高影响因子
CELL BIOCHEMISTRY AND BIOPHYSICS
·
2024
·
IF 1.8
Tu Jia,Liu Qiaoling,Sun Huirong,Gan Luzhen
Diabetic cardiomyopathy (DCM) is a prevalent complication of diabetes mellitus characterized by cardiac dysfunction and myocardial remodeling. Farrerol (FA), an active ingredient in Rhododendron with various pharmacological activities, has an unclear specific role in DCM. Therefore, this study aims to investigate the effects of FA on DCM rats and elucidate its mechanism. The type 2 diabetes mellitus (T2DM) model was induced in adult male Sprague-Dawley rats by administering a high-fat diet for 8 weeks along with STZ injection. Subsequent to successful modeling, FA and the positive drug Dapagliflozin (Dapa) were orally administered via gavage for an additional 8-week period. After administration, the rats’ body weight, fasting blood glucose, fasting insulin, and blood lipid profiles were quantified. Cardiac function was assessed through evaluation of cardiac function parameters, histopathological examination and measurement of myocardial enzyme markers were conducted to assess myocardial injury and fibrosis, Oil red O staining was utilized to evaluate myocardial lipid accumulation, wheat germ agglutinin (WGA) staining was used for assessing cardiomyocyte hypertrophy, and Western blot analysis was used to detect the proteins expression level of AMP-activated protein kinase (AMPK) pathway. The rat cardiomyocyte H9c2 were induced with palmitic acid to establish an in vitro cell model of myocardial lipid toxicity. Subsequently, the cells were subjected to treatment with FA and AMPK inhibitor Compound C, followed by assessment of lipid formation and expression levels of proteins related to the AMPK signaling pathway. The findings demonstrated that both FA and Dapa exhibited efficacy in ameliorating diabetic symptoms, cardiac dysfunction, myocardial fibrosis, cardiomyocyte hypertrophy, and lipid accumulation in T2DM rats. Additionally, they were found to enhance AMPK phosphorylation and PPARα expression while down-regulating CD36. Similarly, FA was observed to inhibit lipid formation in H9c2 and activate the AMPK signaling pathway. However, the improved effect of FA on lipotoxic cardiomyocytes induced by palmitic acid was partially reversed by Compound C. Therefore, the activation of the AMPK signaling pathway by FA may enhance cardiac lipid metabolism, thereby improving cardiac dysfunction and myocardial fibrosis in DCM rats.
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产品关联
DOI
PubMed
高影响因子
Journal of Nanoelectronics and Optoelectronics
·
2021
·Vol. 16
·期 11
·1834-1843
·
IF 0.961
Yuan Wenfeng,Yang Jia,Yuan Mengmeng,Fan Jiacheng,Li Ke,Wang Libo,Zhou Aiguo
In this paper, a novel conductive hydrogel was made by a one-pot method at 60 °C for 12 hours in one step without any cross-linking agent. The hydrogel was composited of Ti3C2 MXene nano slices, poly(vinyl alcohol) (PVA) and poly-N-(2-hydroxyethyl acrylamide)
(PHEAA), named as MXene/PVA/PHEAA hydrogel. Compared with previous methods to make MXene hydrogel, this one-pot method was facile and fast. The as-prepared hydrogel was highly stretchable with the breaking elongation of 1300% and tensile strength of 1.1 MPa. MXene nano sheets dispersed in
the hydrogel formed a three-dimensional conductive network, which increased the strength and conductivity of the gels. The conductivity changed with the gel’s deformation and could be applied as strain sensors. The strain sensors made of the hydrogels were highly stretchable, bendable
and flexible with the response range of 1%–300% and a large gauge factor of 4.23. The sensors can be applied to detect human movements such as finger bending, leg bending, water drinking. The MXene/PVA/PHEAA hydrogel made by this facile one-pot method is promising to make strain sensors
for health detection.
研究领域:
材料科学
·
生物医学工程
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DOI
高影响因子
JOURNAL OF COLLOID AND INTERFACE SCIENCE
·
2021
·
IF 8.128
Lixia Wang,Rongfei Ye,Panming Jian,Jiangyong Liu
Metal-free catalysts with environmental friendless, cost-competitiveness and less susceptibility to leaching and poisoning over metal-based catalysts, have revolutionized in the catalysis domain. In this respect, we herein report the first application of cheap and abundant pumpkin-derived N -doped porous carbon for the reduction of 2-methyl-4-nitrophenol assisted by NaBH 4 . The obtained catalyst is cost-competitive, efficient and robust, with an attractive mass-normalized rate constant of 4.73 s −1 g −1 and good recycling performance. Systematical analyses demonstrate that the 2-methyl-4-nitrophenol reduction reaction catalyzed by the N -doped carbon proceeds through the Langmuir–Hinshelwood kinetics and the performance enhancement benefits from the strong adsorption and activation of the substrates induced by the electronic modulation in the carbon framework via N -doping. This study opens up new avenues for the high-value use of pumpkin as well as the development of metal-free strategy in more catalytic applications.
研究领域:
催化化学
·
环境科学
·
材料科学
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DOI
高影响因子
International Journal of Electrochemical Science
·
2023
·
IF 1.5
Jiao Chen,Hongye Qin,Yaping Pan,Jinli Wu,Jianan Liu,Wanying Lin,Jun Jiang,Enzuo Liu,Junwei Sha,Fang He,Liying Ma,Naiqin Zhao
It is necessary and challenging to develop platinum-based electrocatalysts with low Pt content and high performance for industrial development in a suitable strategy. Herein, ultralow Pt (0.35 wt%) loading Ni(OH) 2 nanosheets (named as 2-Pt/Ni(OH) 2 ) with cataphracted structure is synthesized on nickel foam by one-step hydrothermal process. It only needs an overpotential of 34 mV to achieve a current density of 10 mA cm -2 without any significant decrease for 40 hours. This excellent performance of hydrogen evolution reaction (HER) is attributed to the fact that the cataphracted structure not only has a larger active area and more active sites, but also effectively limits the size of Pt nanoparticles to 2~3 nm, which results in a higher active quality. In addition, the relatively simple and easily operational one-step method can reduce the Pt content to 0.35 wt% significantly. This facile strategy opens up new approaches in the rational design and synthesis of low loading Pt electrocatalysts with eminent electrocatalytic activity for industrial production.
研究领域:
材料科学
·
电化学
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DOI
高影响因子
iScience
·
2023
·
IF 5.8
Yao Li,Zi-Yu Liang,Hai-Lin Wang
Summary Red blood cells supply the oxygen required for all human cells and are in demand for emerging blood-loss therapy. Here we identified N6-methyl-2′-deoxyadenosine (6mdA) as an agonist that promotes the hyperproliferation of burst-forming unit erythroid (BFU-E) progenitor cells. In addition, 6mdA represses the apoptosis of erythroid progenitor cells (EPCs). Combined use of with SCF and EPO enabled cultures of isolated BFU-E to be expanded up to 5,000-fold. Transcriptome analysis showed that 6mdA upregulates the expression of the EPC-associated factors c-Kit, Myb, and Gata2 and downregulates that of the erythroid maturation-related transcription factors Gata1, Spi1, and Klf1. Mechanistic studies suggested that 6mdA enhances and prolongs the activation of erythropoiesis-associated master gene c-Kit and its downstream signaling, leading to expansion and accumulation of EPCs. Collectively, we demonstrate that 6mdA can efficiently stimulate the EPC hyperproliferation and provide a new regenerative medicine recipe to improve ex vivo generation of red blood cells.
研究领域:
血液学
·
分子生物学
·
再生医学
·
细胞生物学
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DOI
PubMed
高影响因子
ChemMedChem
·
2017
·Vol. 12
·期 4
·319-326
·
IF 3.225
Tingjunhong Ni,Ran Li,Fei Xie,Jing Zhao,Xin Huang,Maomao An,Chengxu Zang,Zhan Cai,Dazhi Zhang,Yuanying Jiang
Graphical Infections unanchored ! A series of novel 2-aminonicotinamide derivatives were designed, synthesized, and evaluated for in vitro antifungal activity. Compounds 11 g and 11 h have excellent activity against Candida albicans , with MIC 80 values of 0.0313 μg mL −1 , and exhibit broad-spectrum antifungal activity against fluconazole-resistant C. albicans , C. parapsilosis , C. glabrata , and Cryptococcus neoformans , with a MIC 80 range of 0.0313–2.0 μg mL −1 . Further investigation suggested that compound 11 g targets the cell wall and decreases glycosylphosphatidylinositol anchor content on the cell surface of C. albicans . Based on the structures of the reported compounds G884 [ N -(3-(pentan-2-yloxy)phenyl)nicotinamide], E1210 [3-(3-(4-((pyridin-2-yloxy)methyl)benzyl)isoxazol-5-yl)pyridin-2-amine], and 10 b [2-amino- N -((5-(3-fluorophenoxy)thiophen-2-yl)methyl)nicotinamide], which inhibit the biosynthesis of glycosylphosphatidylinositol (GPI)-anchored proteins in fungi, a series of novel 2-aminonicotinamide derivatives were designed, synthesized, and evaluated for in vitro antifungal activity. Most of these compounds were found to exhibit potent in vitro antifungal activity against Candida albicans , with MIC 80 values ranging from 0.0313 to 4.0 μg mL −1 . In particular, compounds 11 g [2-amino- N -((5-(((2-fluorophenyl)amino)methyl)thiophen-2-yl)methyl)nicotinamide] and 11 h [2-amino- N -((5-(((3-fluorophenyl)amino)methyl)thiophen-2-yl)methyl)nicotinamide] displayed excellent activity against C. albicans , with MIC 80 values of 0.0313 μg mL −1 , and exhibited broad-spectrum antifungal activity against fluconazole-resistant C. albicans , C. parapsilosis , C. glabrata , and Cryptococcus neoformans , with a MIC 80 range of 0.0313–2.0 μg mL −1 . Further studies by electron microscopy and laser confocal microscopy indicated that compound 11 g targets the cell wall and decreases GPI anchor content on the cell surface of C. albicans .
研究领域:
药理学
·
微生物学
·
化学
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DOI
PubMed
高影响因子
FITOTERAPIA
·
2019
·
IF 2.431
Yue Yang,Haihui Xie,Yueming Jiang,Xiaoyi Wei
Averrhoa carambola L. (Oxalidaceae) was widely cultivated for fruits (star fruit), whereas the value of leaves remains to be discovered. Our study on the leaves yielded five flavan-3-ols ( 1 – 5 ) and two 2-diglycosyloxybenzoates. Their structures were determined by spectroscopic and chemical methods. Epicatechin-(5,6-bc)-4β-( p -hydroxyphenyl)-dihydro-2(3 H )-pyranone ( 1 ) and benzyl 2-β- d -apiofuranosyl-(1 → 6)-β- d -glucopyranosyloxybenzoate ( 6 ) were new structures. 6-( S −2 -Pyrrolidinone-5-yl)epicatechin ( 4 ) and 6-( R -2-pyrrolidinone-5-yl)epicatechin ( 5 ) were obtained as monomeric diastereomer for the first time and their absolute configurations were determined by electronic circular dichroism (ECD) computation. Epicatechin-(7,8-bc)-4α-( p -hydroxyphenyl)-dihydro-2(3 H )-pyranone ( 2 ), epicatechin-(7,8-bc)-4β-( p -hydroxyphenyl)-dihydro-2(3 H )-pyranone ( 3 ), and methyl 2-β- d -apiofuranosyl-(1 → 6)-β- d -glucopyranosyloxybenzoate ( 7 ) were not previously reported from the genus Averrhoa . Compounds 1 – 5 showed more potent 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS) radical cation and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activities and ferric reducing antioxidant power (FRAP) than l -ascorbic acid. Meanwhile 1 and 3 exhibited lipase and α-glucosidase inhibitory activities, respectively. The results clarified the structures of flavan-3-ols and 2-diglycosyloxybenzoates in the leaves and their antioxidant, lipase, and α-glucosidase inhibitory activities.
研究领域:
植物化学
·
药理学
·
食品科学
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DOI
PubMed
高影响因子
TETRAHEDRON
·
2024
·
IF 2.1
Nan Wang,Yuanyuan Huang,Mengke Wang,Weichun Huang,You Zi
Herein, a new approach for the synthesis of ( Z )- N -alkenyl-2-pyridones from 2-pyridones and propiolates using phosphine catalysis under mild conditions is reported. This dual Z -diastereoselective and N -selective reaction demonstrates excellent selectivity, yielding sole ( Z )- N -alkenyl-2-pyridones. Furthermore, scale-up studies confirm its practical applicability, with consistent efficiencies observed.
研究领域:
有机化学
·
合成化学
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DOI
高影响因子
Catalysts
·
2025
·Vol. 15
·期 5
·416
·
IF 4
Jie Qin,Guohong Chen,Kaiqi Zheng,Jiajun Wu,Fanan Wang,Xueping Liu,Rengui Weng
2-Methyltetrahydrofuran (2-MTHF), a hydrogenated derivative of levulinic acid (LA), is a biomass-derived platform compound with diverse and significant applications as a biofuel, gasoline additive, green solvent, and pharmaceutical synthesis intermediate. This study investigates the preparation of a Cu1Ni2/Al2O3catalyst through the calcination–reduction of CuNiAl hydrotalcite as a precursor, which was subsequently utilized in the hydrogenation of LA to produce 2-MTHF. The calcination–reduction process applied to CuNiAl hydrotalcite results in a lattice confinement effect. This method not only disperses the active metal sites but also alters the bonding patterns of the active metals, thereby enhancing the activity and stability of the Cu1Ni2/Al2O3catalyst. The results indicate that complete conversion of LA and a 2-MTHF yield of 87.6% can be achieved under optimal conditions of 190 °C, 5 MPa hydrogen, and a reaction time of 5 h, demonstrating an efficient one-step conversion process. Additionally, the catalyst’s recyclability was assessed through multiple reuse tests, with a loss of activity of only 9.2% after six cycle experiments, suggesting its feasibility and reliability for industrial applications.
研究领域:
催化化学
·
生物质转化
·
绿色化学
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产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）