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CHEMISTRY & BIODIVERSITY · 2023 ·Vol. 20 ·期 5 ·e202300105 · IF 2.9

Synthesis and Antibacterial Activity Evaluation of Imidazole Derivatives Containing 6-Methylpyridine Moiety

Wen-Bo Xu,Yu-Qing Meng,Jingxin Sun,Yu-Xuan Yang,Wan-Xin Li,Man-Yu Wang,Ming-Guan Piao,Siqi Li,Jishan Quan,Cheng-Hua Jin

A series of 2-cyclopropyl-5-(5-(6-methylpyridin-2-yl)-2-substituted-1 H -imidazol-4-yl)-6-phenylimidazo[2,1- b ][1,3,4]thiadiazoles ( 15a – t and 16a – f ) were synthesized and their antibacterial activities were evaluated. More than half of the compounds showed moderate or strong antibacterial activity. Among them, compounds 15t (MIC=1–2 μg/mL) and 16d (MIC=0.5 μg/mL) showed the strongest antibacterial activities. Notably, compound 16d did not exhibit cytotoxicity in HepG2 cells and did not show hemolysis like the positive control compound Gatifloxacin. The results suggest that compound 16d should be further investigated as a candidate antibacterial agent. Graphical

研究领域: 药物化学 · 微生物学 · 药理学
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Environmental Science-Processes & Impacts · 2025 · IF 3.9

Comparative Cytotoxicity and Toxicological Mechanisms of 6:2 Cl-PFAES and PFOS on Pancreatic β Cells: Implications for Glucose Metabolism Disruption

Xiaomin Ren,Jianying Wang,Fenqing Zhao,Pingping Zhang,Huan He,Zhixiang Xu,Bin Huang,Xuejun Pan

Previous studies have indicated that 6:2 chlorinated polyfluoroalkyl ether sulfonate (6:2 Cl-PFAES), a substitute for perfluorooctane sulfonate (PFOS), caused disruptions in glucose metabolism, but its toxicological mechanisms remain unclear. Pancreatic β cells are responsible for regulating glucose metabolism. This study used mouse insulinoma β cells (β-TC-6) to study the toxic effects of 6:2 Cl-PFAES and elucidate its potential mechanisms. Through cell counting kit-8, trypan blue staining, and apoptosis assays, we found that 6:2 Cl-PFAES showed toxicity to β-TC-6 cells, even surpassing that of PFOS. Mechanistic studies demonstrated that 6:2 Cl-PFAES induced oxidative stress by ascendant levels of reactive oxygen species (ROS) and malondialdehyde (MDA), alongside increased superoxide dismutase (SOD) activity. The oxidative stress-inducing capability of 6:2 Cl-PFAES was stronger than PFOS. Co-exposure with N-acetyl-L-cysteine (NAC), as the ROS scavenger, which obviously reduced the degree of cell apoptosis and the production of ROS, highlighting oxidative stress as a crucial mechanism of 6:2 Cl-PFAES-induced cell death. Transcriptomic analysis further revealed that 6:2 Cl-PFAES affected genes association with the oxidative phosphorylation pathway, confirming the oxidative stress effect, and altered diabetes-related genes expression, suggesting a heightened risk of diabetes. This study provides insights into the toxicity of 6:2 Cl-PFAES on β cells and its potential risks on glucose metabolism disruption.

CAS / MDL: 67-68-5
研究领域: 毒理学 · 分子生物学 · 环境健康科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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CHIRALITY · 2013 ·Vol. 25 ·期 11 ·735-742 · IF 1.894

Use of Sulfated Cyclofructan 6 and Sulfated Cyclodextrins for the Chiral Separation of Four Basic Pharmaceuticals by Capillary Electrophoresis

Yi Jun Zhang,Ming Xian Huang,Yu Ping Zhang,Daniel Wayne Armstrong,Zachary S. Breitbach,Jae Jeong Ryoo

Sulfated cyclofructan 6 (S-CF6) and sulfated cyclodextrins (S-α-, β-, γ-CDs) are highly selective chiral selectors for the enantioseparation of basic solutes. In this study, S-CF6 was introduced for the enantiomeric separation of four basic pharmaceuticals (including tamsulosin, tiropramide, bupivacaine, and norephedrine) by capillary electrophoresis (CE), and the enantiomeric separation performance was compared with S-α-, β-, γ-CDs. The effects of the chiral selector type, chiral selector concentration, operating voltage, and column temperature were examined and optimized. Excellent resolutions were obtained for all solutes on these chiral selectors. Chirality 25:735–742, 2013 . © 2013 Wiley Periodicals, Inc.

CAS / MDL: 2180-92-9 61-12-1
研究领域: 分析化学 · 药学
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JOURNAL OF CHEMICAL AND ENGINEERING DATA · 2023 · IF 2.6

Study on 6-Bromo-2-methylquinoline in Ten Monosolvents and Four Binary Blends at 278.15–323.15 K: Solubility, Correlation, and Solvent Effect

Lingli Zhang,Chunjuan Huang

The equilibrium solubility of 6-bromo-2-methylquinoline in various binary blends [ethanol/isopropanol/N,N-dimethylformamide (DMF)/methanol + water] and ten monosolvents (methanol, ethanol, n-propanol, isopropanol, ethyl acetate, toluene, acetone, acetonitrile, DMF, and water) was studied by the isothermal method at 278.15–323.15 K under 101.2 kPa. Among the ten pure solvents, the maximum solubility in mole fraction was obtained in toluene (3.318 × 10–2), followed by ethyl acetate (2.991 × 10–2), acetone (2.764 × 10–2), acetonitrile (2.528 × 10–2), DMF (2.220 × 10–2), n-propanol (9.141 × 10–3), isopropanol (8.123 × 10–3), ethanol (3.896 × 10–3), methanol (9.981 × 10–4), and water (2.888 × 10–5) at 323.15 K. In four solvent mixtures, the maximum and minimum solubilities were obtained in the (DMF + water) and (methanol + water) blends. The solubility of 6-bromo-2-methylquinoline in pure solvents was only affected by temperature and calculated by the Apelblat, van’t Hoff, and NRTL models. The Jouyban–Acree (J–A), van’t Hoff–Jouyban–Acree (V–J–A), and modified Apelblat–Jouyban–Acree (A–J–A) models were used to evaluate the solubility data in mixed systems. The calculation of solvent effect deeply explored the dissolution behavior of 6-bromo-2-methylquinoline from the molecular point of view, and the results showed that the interaction between the solute and solvent was dominant. The apparent thermodynamic properties of 6-bromo-2-methylquinoline in pure solvents were obtained by van’t Hoff plots.

研究领域: 化学 · 物理化学
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SCIENCE OF THE TOTAL ENVIRONMENT · 2020 · IF 6.551

Preparation of porous antibacterial polyamide 6 (PA6) membrane with zinc oxide (ZnO) nanoparticles selectively localized at the pore walls via reactive extrusion

Qi Tang,Kang Wang,Xiaoming Ren,Qunchao Zhang,Weiwei Lei,Tao Jiang,Dean Shi

Antibacterial polymer membranes have been widely used in many fields of our daily life. In this study, porous PA6 membrane with ZnO nanoparticles attaching on to the surface of inner pore walls is prepared. Firstly, SMA (styrene maleic anhydride copolymer) is used to graft onto the surface of ZnO nanoparticle in DMF (dimethylformamide). Then the pre-treated ZnO nanoparticles (ZnO-SMA) are added into SEBS (Styrene-ethylene-butylene-styrene copolymer)/PA6 (60/40 wt/wt) blends with co-continuous morphology. The effects of SMA molecular structure (molecular weight and maleic anhydride content) used for ZnO-SMA nanoparticles on their dispersion states in SEBS/PA6/ZnO-SMA nanocomposites are investigated. When SMA3 (MAH = 8 wt%, Mn = 250,000 g mol −1 ), which has relatively higher molecular weight and lower MAH content, is used as the pre-treating agent, ZnO-SMA3 nanoparticles tend to be dispersed at the phase interface in SEBS/PA6/ZnO-SMA nanocomposites. However, when SMA2 (MAH = 23 wt%, Mn = 110,000 g mol −1 ) with relatively lower molecular weight and higher MAH content is used, no ZnO-SMA2 nanoparticles locate at the interface but stay within PA6 phase. Porous PA6 membranes are obtained by selectively etching SEBS phase out with xylene. It can be found that porous PA6 membrane containing ZnO-SMA3 nanoparticles still exhibits much better antibacterial property (R = 3.76) toward S. aureus even at a very low ZnO content (0.5 wt%). This result should be ascribed to almost all the ZnO-SMA3 nanoparticles being exposed to the surface of inner pore walls of PA6 membrane. This work proposes an effective method to prepare porous polymer membrane with functional nanoparticles selectively located at the inner pore walls.

研究领域: 材料科学 · 生物医学工程
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PLoS One · 2012 ·Vol. 7 ·期 9 ·e44754 · IF 4.092

Bisphenol A Alters n-6 Fatty Acid Composition and Decreases Antioxidant Enzyme Levels in Rat Testes: A LC-QTOF-Based Metabolomics Study

Minjian Chen,Bin Xu,Wenliang Ji,Shanlei Qiao,Nan Hu,Yanhui Hu,Wei Wu,Lianglin Qiu,Ruyang Zhang,Yubang Wang,Shoulin Wang,Zuomin Zhou,Yankai Xia,Xinru Wang

Background Male reproductive toxicity induced by exposure to bisphenol A (BPA) has been widely reported. The testes have proven to be a major target organ of BPA toxicity, so studying testicular metabolite variation holds promise for the discovery of mechanisms linked to the toxic effects of BPA on reproduction. Methodology/Principal Findings Male Sprague-Dawley rats were orally administered doses of BPA at the levels of 0, 50 mg/kg/d for 8 weeks. We used an unbiased liquid chromatography-quadrupole time-of-flight (LC-QTOF)-based metabolomics approach to discover, identify, and analyze the variation of testicular metabolites. Two n-6 fatty acids, linoleic acid (LA) and arachidonic acid (AA) were identified as potential testicular biomarkers. Decreased levels of LA and increased levels of AA as well as AA/LA ratio were observed in the testes of the exposed group. According to these suggestions, testicular antioxidant enzyme levels were detected. Testicular superoxide dismutase (SOD) declined significantly in the exposed group compared with that in the non-exposed group, and the glutathione peroxidase (GSH-Px) as well as catalase (CAT) also showed a decreasing trend in BPA treated group. Conclusions/Significance BPA caused testicular n-6 fatty acid composition variation and decreased antioxidant enzyme levels. This study emphasizes that metabolomics brings the promise of biomarkers identification for the discovery of mechanisms underlying reproductive toxicity.

CAS / MDL: 506-32-1 60-33-3
研究领域: 毒理学 · 生殖健康 · 分析化学
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LANGMUIR · 2024 · IF 3.7

Additive-Free, In Situ Rapid Repair of Vacancies in Fe[Fe(CN)6] Electrodes for Efficient Capacitive Deionization

Zewen Fan,Wannan Wang,Jing Ren,Shaofei Zhang,Ruipeng Ren,Yong-Kang Lv

Fe[Fe(CN)6] (FeHCF) is considered a promising material for capacitive deionization–desalination of saline wastewater due to its excellent structure. However, additives are usually introduced during the synthesis of FeHCF in order to avoid [Fe(CN)6]3– vacancy defects filled by ligand water, which can result in the appearance of harmful byproducts and additional water treatment costs. In this study, an additive-free in situ vacancy repair strategy is proposed for the rapid synthesis of high-quality FeHCF in a saturated K3Fe(CN)6 solution. During the process of synthesizing FeHCF in solution, a high concentration of [Fe(CN)6]3– is found to facilitate the binding of Fe3+ to [Fe(CN)6]3– and hinder the hydrolysis and coordination reaction of Fe3+. After undergoing repair, FeHCF4 demonstrates an increased capacity and highly reversible electrochemical performance due to the robust structure. When utilized as Faraday cathodes in hybrid capacitive deionization (HCDI) systems, FeHCF4 exhibits a higher salt removal capacity (65.67 mg g–1) and lower energy consumption (0.68 kWh kg–1-NaCl) compared to unrepaired FeHCF1, while still maintaining excellent cycling performance. This environmentally friendly approach of repairing vacancies serves as a source of inspiration for the advancement of high-performance Prussian Blue analogues as capacitive sodium-removing materials.

研究领域: 材料科学 · 环境工程 · 电化学
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SCIENCE OF THE TOTAL ENVIRONMENT · 2024 · IF 8.2

Eco-corona enhanced the interactive effects of nanoplastics and 6:2 chlorinated polyfluorinated ether sulfonate in zebrafish embryos

Shulin Liu,Muhammad Junaid,Chong Wang,Jun Wang

Nanoplastics (NPs, < 1000 nm) interact with chemicals and biomolecules to produce chemical−/eco-corona, altering the environmental destiny, bioavailability, and toxicity of plastic particles and co-occurring chemicals. This study employs exogenous (humic acid, HA) and endogenous (bovine serum albumin, BSA) natural organic matter (NOM) to investigate the eco-corona formation on NPs and explore the interfacial effects of eco-corona and 6:2 chlorinated polyfluorinated ether sulfonate (Cl-PFESA, commonly named as F-53B) on zebrafish ( Danio rerio ) after 7 days of exposure. Our results indicated significant changes in growth and developmental indices of zebrafish embryos among all eco-corona groups ( p  < 0.05). Additionally, NFB (BSA-corona, 1 mg/L NPs + 200 μg/L F-53B + 10 mg/L BSA), NFH (HA-corona, 1 mg/L NPs + 200 μg/L F-53B + 10 mg/L HA) and NFHB (BSA-HA-corona, 1 mg/L NPs + 200 μg/L F-53B + 10 mg/L BSA + 10 mg/L HA) showed elevated bioaccumulation of NPs, ROS generation and induction of apoptosis. Transcriptomic analysis showed the number of differentially expressed genes (DEGs) in the following order: BSA-HA-corona (NFHB (2953) > HA-corona (NFH (2797) > NH (2721) > F-53B (2292) > NF (2033) > BSA-corona (NFB (687) > NB (450)), and no DEGs were detected in the single NP compared to the control. Further, the PI3K-AKT, immune system, endocrine system, digestive system, infectious diseases, and neurovegetative disease pathways showed sensitive responses in the NFH/NFHB groups compared to those in the NFB group. Therefore, the interactive effects of NPs and F-53B on zebrafish embryos were lower in the presence of BSA-corona than those in HA- or HA-BSA-coronas, indicating a relationship between the formation of diverse eco-coronas on NPs by multiple NOM and an associated increase in the interfacial toxicological effects of plastic particles and F-35B in freshwater organisms.

CAS / MDL: 9048-46-8 68131-04-4
研究领域: 环境科学 · 毒理学
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ACS Omega · 2025 · IF 4.3

Mining Arylsulfatase from Genome-Scale Metabolic Pathways of Pseudoalteromonas sp. SR43-6 and Its Agar-Based Desulfurization Applications

Songzhi Li,Yang Guo,Hong Jiang,Huan Zhang,Jiayu Li,Yanli Chen,Jie Li,Xiangzhao Mao,Minxiao Wang

Arylsulfatase catalyzes the cleavage of sulfate ester bonds and plays a role in agar desulfation, thereby enhancing agar gel strength and quality. While studying the desulfurization pathway in Pseudoalteromonassp. SR43-6, a sequence encoding a potential arylsulfatase─Pseudoalteromonas Ars (Ps-Ars)─was found. The enzyme, with p-nitrophenyl sulfate as a substrate, exhibited optimal activity at 35 °C and pH 8.0. Its relative activity (206 U/mg) exceeded that of the recently identified arylsulfatases. Four hundred units of the enzyme removed 86.4% of sulfate groups from Gelidium amansii agar in 4 h, whereas 800 U of the enzyme removed 71.3% of sulfate groups from Gracilaria lemaneiformis agar in 8 h. After enzymatic treatment, G. amansii agar gel strength was enhanced by 32%, and a similar improvement was observed in G. lemaneiformis agar gel strength. Enzymatic agar desulfurization offers mild, quality-retaining, and environmentally friendly advantages, augmenting industrial application prospects.

研究领域: 生物化学 · 海洋微生物学 · 食品科学
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CHEMICAL ENGINEERING JOURNAL · 2025 · IF 13.2

Interleukin-6-taregeted dual-drug nanoparticles enhance glioblastoma chemotherapy by facilitating blood-brain barrier penetration and alleviating cardiotoxicity

Zesheng Sun,Jialiang Lin,Yue Huang,Qianqian Liu,Xucheng Zhu,Yu Yang,Ya Wen,Chunbin Shao,Weiquan Liao,Yan Song,Sharon Prince,Yi Wang,Rongqin Huang,Jinlong Shi

Overcoming the blood-brain barrier (BBB) to effectively deliver chemotherapeutics while minimizing systemic toxicity remains a formidable challenge in glioblastoma (GBM) treatment. Herein, amphiphilic liposomal nanoparticles are engineered to encapsulate hydrophobic ursolic acid (UA) and hydrophilic doxorubicin (DOX), surface-functionalized with an interleukin-6 (IL-6) receptor-targeting peptide (I 6 P 8 ) to enable glioma-specific targeting. The I 6 P 8 -modified nanoparticles facilitate BBB penetration and selective glioma accumulation, thereby potentiating the synergistic cytotoxicity of DOX and UA. Furthermore, the interaction between I 6 P 8 and IL-6 not only impairs IL-6-mediated glioma cell proliferation but also enhances therapeutic efficacy. Notably, the dual-drug nanoparticles mitigate DOX-induced cardiotoxicity by attenuating NADPH oxidase 4 (NOX4) expression and promoting nitric oxide (NO) release via UA, thereby preserving myocardial integrity. Comprehensive in vitro and in vivo evaluations confirm that the engineered nanoplatform significantly prolongs median survival of GBM-bearing mice while exhibiting excellent biocompatibility. This study introduces a targeted and low-toxic nanotherapeutic strategy for effective GBM management.

研究领域: 生物医学 · 肿瘤学 · 神经科学 · 药理学
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JOURNAL OF THE AMERICAN CERAMIC SOCIETY · 2024 ·Vol. 107 ·期 8 ·5400-5411 · IF 3.5

Vat photopolymerization 3D printing of Al2O3 ceramic cores with strip-shaped pores by using polyamide 6 fiber template

Xiaofei Zhai,Jingyi Chen,Ruyue Su,Xiong Gao,Xueqin Zhang,Rujie He

The complex ceramic core used for hollow turbine blades requires high porosity and flexural strength. This work combined vat photopolymerization 3D printing with sacrificial template method to prepare Al 2 O 3 ceramic cores with strip-shaped pores using polyamide 6 (PA6) fibers as templates. When the porosity was greater than 30%, the maximum flexural strength reached up to 110.48 MPa. The sacrificial templating method improved the porosity of Al 2 O 3 ceramic cores, forming an internal porous structure that combined strip-shaped large pores with irregularly shaped small pores. The influences of PA6 fiber content and diameter on the shrinkage, porosity, microstructure, and comprehensive properties of alumina ceramic cores were studied, revealing the mechanism of the coexistence of high porosity and high strength.

CAS / MDL: 15625-89-5
研究领域: 材料科学 · 制造工程
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JOURNAL OF RARE EARTHS · 2013 · IF 1.363

Crystal structures and fluorescence properties of lanthanide complexes prepared with 2,2′-biphenyldicarboxylic acid and 2,2′:6′,2″-terpyridine

Hongzhen XIE,Guanzhong LU

Five lanthanide complexes of Ln 2 (dpdc) 2 (tpy) 2 (NO 3 ) 2 (H 2 O) 2 [Ln=La ( 1 ), Ce ( 2 ), Pr ( 3 ), Sm ( 4 ), Gd ( 5 ), H 2 dpdc=2,2’-biphenyldicarboxylic acid and tpy=2,2′:6′,2″-terpyridine] were prepared at room temperature and characterized by X-ray diffraction, FT-IR and thermo-gravimetric analysis. The results showed that complexes 1–5 were isostructural and consisted of dinuclear units [Ln 2 (dpdc) 2 (tpy) 2 (NO 3 )(H 2 O) 2 ] bridged by two dpdc 2− ligands. The dinuclear units with strong intramolecular hydrogen bonds were assembled into 2D supramolecular layers by the weak π … π staking interactions between pyridine rings of tpy. The TG analysis showed that the complexes 1 – 5 behaved higher thermal stability with no mass loss at < 320 °C. The lanthanide contraction effect and the solid state luminescence properties of complexes 1 – 5 were also investigated. The luminescence emission spectra of complexes 1 – 5 exhibited ligands emission bands and complex 3 and 4 had no typical emission in the visible region.

CAS / MDL: 10277-43-7
研究领域: 化学 · 材料科学
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