BIOMEDICAL MICRODEVICES
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2024
·Vol. 26
·期 4
·1-17
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IF 3
Zhou Su,Li Rui,Sun Jie,Gu Minyang,Gao Dan,Tang Liming,Zhu Jiangbo
The utilization of existing Skin-on-a-Chip (SoC) is constrained by the complex structures, the multiplicity of auxiliary devices, and the inability to evaluate exogenous chemicals that are hepatotoxic after percutaneous metabolism. In this study, a gravity-driven SoC without any auxiliary devices was constructed for the hepatocytotoxicity study of exogenous chemicals. The SoC possesses 3 layers of culture chambers, from top to bottom, for human skin equivalent (HSE), Human Umbilical Vein Endothelial Cells (HUVEC) and hepatocytes (HepG2), and the maintenance and expression capacity of the corresponding cells on the SoC were verified by specificity parameters. The reactivity of the SoC to exogenous chemicals was verified by 2-aminofluorene (2-AF). The SoC can realistically simulate the in vivo exposure process of exogenous chemicals that are percutaneously exposed and metabolized into the bloodstream and then to the liver to produce toxicity, and it can achieve the same effects on transcriptome as those of animal tests at lower exposure levels while examining multiple toxicological targets of the skin, vascular endothelial cells, and hepatocytes. Both in terms of species similarity, the principles of reduction, replacement and refinement (3R), or the level of exposure suggest that the present SoC has a degree of replacement for animal models in assessing exogenous chemicals, especially those that are hepatotoxic after percutaneous metabolism.
研究领域:
生物医学工程
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毒理学
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药理学
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细胞生物学
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PROGRESS IN ORGANIC COATINGS
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2025
·
IF 7.3
Shiyue Zhang,Xiaoqing Song,Wangjun Liu,Xiangxiang Zhai,Hongxin Gao,Qianhui Chong,Zhonglin Luo,Biaobing Wang
Polymer-based materials integrating high-performance flame retardancy with ultralong room-temperature phosphorescence (URTP) are highly desirable yet rarely achieved, especially for applications under harsh environmental conditions. In this work, a multifunctional small molecule (AFDOPO) was synthesized via a straightforward Atherton–Todd reaction between 2-aminofluorene and 9,10-dihydro-9-oxa-10-phosphaphenanthrene-10-oxide (DOPO), and its influence on the comprehensive properties of epoxy resin (EP) was systematically investigated. With only 1.5 wt% AFDOPO loading (phosphorus content: 0.38 wt%), the EP/AFDOPO-1.5 composite exhibits outstanding fire safety, achieving a limiting oxygen index of 31.2 % and a UL-94V-0 rating along with significant reductions in heat release rate (18.6 %), total heat release (4.1 %), and total smoke production (15.4 %) relative to pristine EP. Remarkably, the composite also displays bright ultralong room-temperature phosphorescence, maintaining a visible afterglow for over 20 s. Even after 31 days of immersion in strong acid/base or 5 days of UV aging, the afterglow durations remain as long as 9 s and 7 s, respectively. This study offers a feasible strategy for designing high-performance URTP materials capable of functioning reliably in demanding environments.
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REGULATORY TOXICOLOGY AND PHARMACOLOGY
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2015
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IF 2.031
Dan Wan,Xihong Zhou,Chunyan Xie,Xugang Shu,Xin Wu,Yulong Yin
Iron is an essential trace element that is vital important in various biological process. A deficiency in iron could induce public health problem e.g. anaemia, while an overload could induce ROS production, lipid peroxidation and DNA bases modifications. In the present study, a new iron fortifier was synthesized, and its acute/sub-acute toxicity was investigated. According to the improved Karber's method, the median lethal dose (LD 50 ) of the ferrous N-carbamylglycinate in SD rat was 3.02 g/kg and the 95% confidence intervals were between 2.78 and 3.31 g/kg. No biologically significant or test substance-related differences were observed in body weights, feed consumption, clinical signs, organ weights, histopathology , ophthalmology, hematology, and clinical chemistry parameters in any of the treatment groups of ferrous N-carbamylglycinate at target concentrations corresponding to 150, 300, and 600 mg/kg/day for 28 days. The no observed adverse effect level (NOAEL) for ferrous N-carbamylglycinate was at least 600 mg/kg b.w. day in rats. In addition, no evidence of mutagenicity was found, either in vitro in bacterial reverse mutation assay or in vivo in mice bone marrow micronucleus assay and sperm shape abnormality assay. On the basis of our findings, we conclude that ferrous N-carbamylglycinate is a low-toxic substance with no genotoxicity .
研究领域:
营养学
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毒理学
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分子生物学
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JOURNAL OF SEPARATION SCIENCE
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2019
·Vol. 42
·期 7
·1332-1340
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IF 2.516
Yan Wang,Shujuan Ma,Luwei Zhang,Na Zhang,Yanan Li,Junjie Ou,Yehua Shen,Mingliang Ye
Three monomers, octakis (3-mercaptopropyl) octasilsesquioxane, 1,2,4-trivinylcyclohexane and isophytol were employed to synthesize a novel monolithic stationary phase via photo-initiated thiol-ene click polymerization for reversed-phase liquid chromatography. Several factors such as porogenic system, reaction time and the molar ratio of functional groups were investigated in detail. The resulting poly(POSS- co -TVCH- co -isophytol) monolithic column exhibited suitable permeability for fast separation and outstanding thermal stability. Five alkylbenzenes were employed to evaluate the ability of chromatographic separation of the resulting monolithic columns at different flow rates, and showed the highest column efficiencies of 90,200–93,100 N/m (corresponding to 10.4–10.6 μm of plate height) at a velocity of 0.41 mm/s. The baseline separations of five anilines and eight phenols further proved the applicability of poly(POSS- co -TVCH- co -isophytol) monolithic column in the separation of small molecules.
研究领域:
分析化学
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材料科学
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RSC Advances
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2024
·Vol. 14
·期 30
·21432-21438
·
IF 3.9
Yunkai Sun,Xiaoxia Wu,Pei Zuo,Zhao Liu,Xuepei Miao,Jian Liu,Hairuo Wen
In the technical route for the synthesis of avanafil, 1-ethyl-(3-dimethylaminopropyl)carbamyldiimide hydrochloride (EDCI) and 1-hydroxybenzotriazole (HOBT) are used as reactive acid–amine binding agents. HOBT contains trace amounts of hydrazine residue, and there is a risk of introducing potentially mutagenic impurities with hydrazide-containing structures. The potentially genotoxic impurities E (Imp-E) and F (Imp-F) of avanafil with altering hydrazide-structure were synthesized by chemical method; subsequently, the impurities were evaluated and classified according to ICH M7 guidelines. Two complementary quantitative structure–activity relationship (QSAR) evaluation systems (Derek and Sarah) based on expert rules and statistics were used to preliminarily predict the genotoxicity of Imp-E and Imp-F, and the prediction result of E was suspected to be positive. In the Ames test of Imp-E and Imp-F, in the dose range of 62.5–1000 μg per plate, with or without the presence of metabolic activation system S9, the number of revertant colonies did not exceed 2 times the number of colonies in the solvent control group and did not show a dose–response relationship, and the test results were negative. Imp-E and Imp-F were determined to be negative for genotoxicity, which could be controlled as class 5 in ICH M7, that is, non mutagenic impurity.
研究领域:
药物化学
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毒理学
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制药工程
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Materials
·
2016
·Vol. 9
·期 7
·541
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IF 2.728
Lexin Zhang,Tifeng Jiao,Kai Ma,Ruirui Xing,Yamei Liu,Yong Xiao,Jingxin Zhou,Qingrui Zhang,Qiuming Peng
In this work, some amide compounds with different aromatic substituent headgroups were synthesized and their gelation self-assembly behaviors in 22 solvents were characterized as new gelators. The obtained results indicated that the size of aromatic substituent headgroups in molecular skeletons in gelators showed crucial effect in the gel formation and self-assembly behavior of all compounds in the solvents used. Larger aromatic headgroups in molecular structures in the synthesized gelator molecules are helpful to form various gel nanostructures. Morphological investigations showed that the gelator molecules can self-assembly and stack into various organized aggregates with solvent change, such as wrinkle, belt, rod, and lamella-like structures. Spectral characterizations suggested that there existed various weak interactions including π-π stacking, hydrogen bonding, and hydrophobic forces due to aromatic substituent headgroups and alkyl substituent chains in molecular structures. In addition, the drug release capacities experiments demonstrated that the drug release rate in present obtained gels can be tuned by adjusting the concentrations of dye. The present work would open up enormous insight to design and investigate new kind of soft materials with designed molecular structures and tunable drug release performance.Keywords:nanostructure;self-assembly;organogel;amide derivative;substituent headgroup;drug release
研究领域:
材料科学
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药学
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Frontiers in Microbiology
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2021
·
IF 5.64
Liu Xinning,Liu Yuanchang,Zhao Guangjian,Zhang Yidan,Liu Lu,Wang Juan,Wang Yifan,Zhang Siyu,Li Xin,Guo Dongliang,Wang Peng,Xu Ximing
Vibrio vulnificus is a zoonotic bacterium that is capable of causing highly lethal diseases in humans; this pathogen is responsible for 95% of all seafood-related deaths in the United States. Arylamine N-acetyltransferases (NAT, E.C. 2.3.1.5) is a major family of xenobiotic-metabolizing enzymes that can biotransform aromatic amine chemicals. In this research, to evaluate the effect of NAT on acetyl group transformation in arylamine antibiotics, we first used sequence alignment to study the structure of V. vulnificus NAT [(VIBVN)NAT]. The nat gene encodes a protein of 260 amino acids, which has an approximate molecular mass of 30 kDa. Then we purified recombinant (VIBVN)NAT and determined the enzyme activity by PNPA and DTNB methods. The DTNB method indicates that this prokaryotic NAT has a particular substrate specificity towards aromatic substrates. However, (VIBVN)NAT lost most of its activity after treatment with high concentrations of urea and H2O2. In addition, we also explored the stability of the enzyme at different temperatures and pH values. In analyzing the influence of metal ions, the enzyme activity was significantly inhibited by Zn2+ and Cu2+. The kinetic parameters Km and Vmax were determined using hydralazine, isoniazid, 4-amino salicylic acid, and 4-chloro-3-methylaniline as substrates, and the Tm, Tagg and size distribution of (VIBVN)NAT were observed. In particular, a molecular docking study on the structure of (VIBVN)NAT was conducted to understand its biochemical traits. These results showed that (VIBVN)NAT could acetylate various aromatic amine substrates and contribute to arylamine antibiotic resistance in V. vulnificus.
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RSC Advances
·
2020
·Vol. 10
·期 30
·17816-17828
·
IF 3.119
Wenchang Wei,Zheng Liu,Chuxin Liang,Guo-Cheng Han,Jiaxing Han,Shufen Zhang
In this work, two new bis-Schiff bases, namely 2-bromoisophthalaldehyde-2-aminofluorene (M1) and glutaraldehyde 2-aminofluorene (M2), were synthesized, and their structures were characterized and confirmed by infrared spectroscopy, Fourier transform mass spectrometry and UV-visible spectroscopy. Their corrosion inhibition performance on carbon steel in simulated circulating cooling water was investigated by weight loss measurements and electrochemical measurements. The potentiodynamic polarization curves confirmed that two bis-Schiff bases are anode-type inhibitors; electrochemical impedance spectroscopy tests showed that M1 and M2 possess the best inhibition efficiencies of 96.25% and 99.15% at the optimal concentration of 2.50 mmol L−1, respectively. The weight loss results showed that M1 and M2 exhibit maximum ηw values of 92.62% and 96.31%, respectively. Scanning electron microscopy showed that the inhibitors inhibited carbon steel corrosion. The adsorption isotherm measurements indicated that the two inhibitors exhibited physicochemisorption mechanisms and followed Langmuir adsorption isotherms. The relationships between the molecular structure and inhibition behavior of the inhibitors were explored by density functional theory, frontier molecular orbital studies, and Fukui index analysis, which affirmed that M2 possesses higher corrosion inhibition efficiency than M1.
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JOURNAL OF MOLECULAR LIQUIDS
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2018
·
IF 4.513
Chuxin Liang,Zheng Liu,Qiuqun Liang,Guo-Cheng Han,Jiaxing Han,Shufen Zhang,Xiao-Zhen Feng
Three new bis-Schiff bases, including bis(2-aminofluorene) glyoxal(L1), bis(2-aminofluorene) p-phthalaldehyde (L2) and bis(2-aminofluorene) 4,4′-biphenyldicarboxaldehyde (L3), were synthesized and characterized by Fourier transform infrared spectroscopy (FT-IR) and mass spectrometry (MS). Weight loss methods indicated that all these inhibitors have good resistance to 1.0 mol·L −1 hydrochloric acid corrosion , and the highest inhibition efficiency was 98.2% at 65 °C for L3. Polarization curves and electrochemical impedance spectroscopy (EIS) indicated that L3 exhibited excellent inhibition effect when concentration was 1.0 mmol·L −1 . Moreover, the L3 was adsorbed spontaneously onto the surface by both physisorption and chemisorption , which followed the Langmuir adsorption isotherm . The relationship between molecular structure and quantum chemical structure parameters of three bis-Schiff base corrosion inhibitors was studied by Quantum chemistry calculation performed by density function theory (DFT) method. Results showed that L3 had excellent inhibition performance, which was consistent with experimental results.
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