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NEW JOURNAL OF CHEMISTRY · 2022 ·Vol. 47 ·期 3 ·1256-1267 · IF 3.925

Continuous heterogeneous isomerization of 3/4-methyltetrahydrophthalic anhydride (3/4-MTHPA) with acid- and base-modified γ-Al2O3 catalysts

Lei Yin,Hui Yang Li,Tingting Ge,Yuchao Li,Cuncun Zuo,Ming Wang,GuangJun Cui,Haofei Huang,Lin Guo

A series of acid–base-loaded γ-Al2O3 catalysts was applied as the catalysts for the isomerization of 3/4-methyl-tetrahydro phthalic anhydride. With a basic metal (K or Na) as the basic source and phosphorus (P) as the acid source, γ-Al2O3 was modified by equal volume immersion. NH3/CO2-TPD, XRD, TEM/EDS, BET, and TGA were used to analyze the catalysts, and 15%-K/Al2O3 and 10%-P/Al2O3 were determined as the most appropriate catalysts. The isomers were qualitatively and quantitatively analyzed using nuclear magnetic resonance (1H-NMR) and infrared spectroscopy (IR), and the reaction mechanism for the isomer formation was proposed. With 3-MTHPA as the substrate, the acid/base reaction temperature was 165/150 °C, the reaction time was 3 h and the amount of the catalyst added was 3%. A new type of continuous isomeric fixed-bed reactor was designed. The stability of the catalyst was tested, and the activity loss was 4.6–6.6% after 10 hours of operation.

CAS / MDL: 1344-28-1 25155-30-0
研究领域: 化学工程 · 催化科学
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JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY · 2019 · IF 4.027

Synthesis and biological evaluation of 3–(4-aminophenyl)-coumarin derivatives as potential anti-Alzheimer’s disease agents

Yu-Heng Hu,Jie Yang,Yun Zhang,Ke-Chun Liu,Teng Liu,Jie Sun,Xiao-Jing Wang

The work is focused on the design of drugs that prevent and treat Alzheimer’s disease (AD) and its complications. A series of 3–(4-aminophenyl)-coumarin derivatives designed, synthesised, fully characterised and evaluated in vitro/vivo. The biological assay experiments showed that some compounds displayed a clearly selective inhibition for acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Among all compounds, compound 4m exhibited the highest AChE inhibition with an IC50 value of 0.091 ± 0.011 µM and compound 4k exhibited the highest BuChE inhibition with an IC50 value of 0.559 ± 0.017 µM. A zebrafish behaviour analyser (Zebrobox) was used to determine the behavioural effects of the active compound on the movement distance of the aluminium chloride-induced zebrafish. Compound 4m offered a potential drug design concept for the development of therapeutic or preventive agents for AD and its complications.

研究领域: 药理学 · 神经科学 · 药物设计
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PROCESS BIOCHEMISTRY · 2023 · IF 4.4

Rational immobilization of l-threonine aldolase from Bacillus nealsonii for efficiently synthesis of l-syn-3-[4-(methylsulfonyl)] phenylserine

Haidong Teng,Kaitong Chen,Lan Wang,Jianping Wu,Gang Xu

l -syn-3-[4-(methylsulfonyl)] phenylserine is a key industrial intermediate for the synthesis of florfenicol, thiamphenicol , and other products. l -Threonine aldolase can synthesize l -syn-3-[4-(methylsulfonyl)] phenylserine from glycine and 4-methylsulphonyl benzaldehyde directly. However, the selectivity of free l -threonine aldolase was difficult to meet the requirement of industrialization. Here, we selected the suitable site to insert His tag as immobilized site to improve the selectivity of l -threonine aldolase based on the molecular dynamics simulation and prior protein engineering. The phenanthroline was coupled to the surface of magnetic nanoparticles coated with silicon and thus enabled the selective and oriented immobilization of His-tagged l -threonine aldolase. Due to magnetic nanoparticles coated with silicon as supports, it was easy to separate the residual reactant and impurities from the immobilized enzyme by magnetic attraction. Moreover, the immobilization was combined with the purification of free enzymes through directional immobilization, which avoided heterozyme linking supports and improved the utilization efficiency of supports. Our study demonstrates an effective approach: how to analyze and select enzyme-targeted ligation sites in conjunction with previous modifications of engineered bacteria, and the immobilized enzyme obtained also provided a good candidate for the industrial production of l -syn-3-[4-(methylsulfonyl)] phenylserine.

研究领域: 生物化学 · 酶工程 · 纳米生物学
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JOURNAL OF ALLOYS AND COMPOUNDS · 2022 · IF 6.371

Low loss Ba3Ti4Nb4O21 microwave dielectric ceramics through (Mn1/3Nb2/3)4+ ion control engineering for LTCC applications

Xiaohui Wu,Qin Zhang,Fangyi Huang,Xingyu Huo,Fuyu Li,Yulan Jing,Yuanxun Li,Hua Su

In this work, a new low loss Ba 3 Ti 4- x (Mn 1/3 Nb 2/3 ) x Nb 4 O 21 (MN-BTN, 0 ≤  x  ≤ 12 mol%) ceramics configuration was presented through preparing by the solid-state route. The XRD patterns, Rietveld refinement , microstructure, and microwave properties were systematically analyzed. All the fabricated MN-BTN ceramics belonged to the hexagonal structure with a P 6 3 / mcm space group. More specifically, the 6MN-BTN ceramic exhibited a high relative density of ~92.3 %, homogeneous grains distribution with an average size of ~71.95 µm, and several excellent microwave dielectric properties : ε r = 59.67, Q× f = 16,226 GHz, τ f = +103.9 ppm/℃ sintered at 1220 ℃. The incorporation of 1.5  wt % BaCu(B 2 O 5 ) (BCB) compound within the 6MN-BTN ceramic not only effectively reduced the sintering temperature from 1220 ℃ to 950 ℃, but also the excellent microwave dielectric properties were maintained: ε r = 42.33, Q× f = 11,300 GHz, τ f = +24.7 ppm/℃. Interestingly, the 6MN-BTN + 1.5  wt % BCB ceramic showed better chemical compatibility with Ag. The proposed 6MN-BTN + 1.5  wt % BCB ceramic configuration could be regarded as a promising material for LTCC applications.

研究领域: 材料科学 · 陶瓷工程 · 微波工程
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International Journal of Electrochemical Science · 2023 · IF 1.5

Electrosynthesis and Characterization of a New Conducting Copolymer from 2’-aminomethyl-3, 4-ethylenedioxythiophene and 3, 4-ethylenedioxythiophene

Hui Sun,Baoyang Lu,Xuemin Duan,Jingkun Xu,Liqi Dong,Xiaofei Zhu,Kaixin Zhang,Dufen Hu,Shouli Ming

The copolymerization of 2’-aminomethyl-3, 4-ethylenedioxythiophene (EDOT-MeNH 2 ) and 3, 4-ethylenedioxythiophene (EDOT) was successfully performed electrochemically in acetonitrile (CH 3 CN) containing tetrabutylammonium hexafluorophosphate (Bu 4 NPF 6 ) as the supporting electrolyte by direct anodic oxidation of the monomer mixtures. A series of experiments with different monomer feed ratios were carried out to investigate the influence of monomer feed ratio on the electrochemical copolymerization and the overall properties of the copolymer films. As-formed novel copolymers owned both the advantages of poly(2’-aminomethyl-3, 4-ethylenedioxythiophene) (PEDOT-MeNH 2 ) and poly(3, 4-ethylenedioxythiophene) (PEDOT), i.e ., good electrochemical behavior, excellent electrochemical stability, and good thermal stability. Spectroelectrochemistry analysis of copolymer with the feed ratio of 1:1 reflected λ max due to the π–π* transition and polaron band formation was found to be 620 nm and the band gap ( E g ) was calculated as 1.67 eV. The structure, thermogravimetry and morphology of the copolymers were investigated by infrared spectroscopy, thermal analysis, and scanning electron microscopy, respectively.

研究领域: 材料科学 · 高分子化学 · 电化学 · 导电聚合物 · 有机电子学
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Frontiers in Pharmacology · 2021 · IF 5.811

Piperazine-Derived α1D/1A Antagonist 1- Benzyl-N- (3-(4- (2-Methoxyphenyl) Piperazine-1-yl) Propyl) -1H- Indole-2- Carboxamide Induces Apoptosis in Benign Prostatic Hyperplasia Independently of α1-Adrenoceptor Blocking

Xiao Qing,Liu Qi-Meng,Jiang Ru-Chao,Chen Kai-Feng,Zhu Xiang,Ma Lei,Li Wei-Xi,He Fei,Huang Jun-Jun

Previous studies have indicated that α1D/1A antagonist naftopidil (NAF) suppresses prostate growth by decreasing cell proliferation without affecting apoptosis and prostate volume in benign prostatic hyperplasia (BPH). A NAF-derived α1D/1A antagonist 1- benzyl-N-(3-(4-(2-methoxyphenyl) piperazine-1-yl) propyl)-1H-indole-2- carboxamide (HJZ-12) has been reported from our laboratory, which exhibits high subtype-selectivity to both α1D- and α1A- AR (47.9- and 19.1- fold, respectively) with respect to a1B-AR in vitro. However, no further study was conducted. In the present study, a pharmacological evaluation of HJZ-12 in BPH was performed on an estrogen/androgen-induced rat BPH model and human BPH-1 cell line. In vivo, HJZ-12 exhibited better performance than NAF in preventing the progression of rat prostatic hyperplasia by not only decreasing prostate weight and proliferation (similar to NAF) but also, shrinking prostate volume and inducing prostate apoptosis (different from NAF). In vitro, HJZ-12 exhibited significant cell viability inhibition and apoptotic induction in BPH-1 cell line, without presenting cell anti-proliferation properties. Intriguingly, the role of HJZ-12 on cell viability and apoptosis was an α1-independent action. Furthermore, RNA-Seq analysis was applied to screen out six anti-apoptotic genes (Bcl-3, B-lymphoma Mo-MLV insertion region 1 [Bmi-1], ITGA2, FGFR3, RRS1, and SGK1). Amongst them, Bmi-1 was involved in the apoptotic induction of HJZ-12 in BPH-1. Overall, HJZ-12 played a remarkable role in preventing the progression of prostatic hyperplasia through α1-independent apoptotic induction, indicating that it will be a multi-target effective candidate for BPH treatment.

CAS / MDL: 8001-25-0 50-50-0
研究领域: 药理学 · 泌尿学 · 分子生物学 · 细胞生物学
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JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS · 2024 · IF 3.1

Metabolic characteristics of prostate cancer cells with high metastatic potential revealed by (S)-ethyl 1-(3-(4-chlorophenoxy)-2-hydroxypropyl)-3-(4-methoxyphenyl)-1H-pyrazole-5-carboxylate inhibition

Baoyan Ding,Wei Meng,Xiaoling Zang,Zhihua Lv

A small molecule, (S)-ethyl 1-(3-(4-chlorophenoxy)-2-hydroxypropyl)-3-(4-methoxyphenyl)-1H-pyrazole-5-carboxylate (SEC), has been reported to be capable of suppressing metastasis of prostate cancer (PCa) cells. In this study, SEC was used to study the metabolic responses of PCa cell lines (LNCaP, PC3, and DU145) with different metastatic potential and the alterations of mTOR, p-mTOR, AMPK, and p-AMPK levels, when the PCa cells were inhibited. The ultra-high performance liquid chromatography-high resolution mass spectrometry (UHPLC-HRMS)-based analysis showed that SEC induced the decreases of intracellular metabolites including glutamic acid, glutamine, and histidine (LNCaP); creatinine, citric acid/isocitric acid, and aspartic acid (PC3); and spermidine, S-hydroxymethylglutathione, LPE (20:3), and palmitic amide (DU145), and the increases of intracellular LPC (18:0) (LNCaP); tyrosine, pyroglutamic acid/pyrroline hydroxycarboxylic acid (PC3); and tyrosine, phenylalanine, phenylacetylglycine, spermine, histidine, and choline (DU145). SEC also caused the decrease of extracellular N1-acetylspermidine (LNCaP), erythronic acid/threonic acid (PC3 and DU145), and nicotinic acid/picolinic acid (DU145), and the increase of extracellular 5’-methylthioadenosine (DU145). High metastatic PC3 and DU145 cells exhibited changes in aromatic amino acid metabolism including tyrosine metabolism, phenylalanine, tyrosine, and tryptophan metabolism, and phenylalanine metabolism (PC3 and DU145), TCA cycle (PC3), arginine and proline metabolism, and glycerophospholipid metabolism (DU145), different from the low metastatic LNCaP cells, which had changes in alanine, aspartate, and glutamate metabolism, and arginine biosynthesis. In addition, the levels of p-mTOR and p-AMPK were shown to be obviously downregulated and upregulated, respectively, in high metastatic PC3 and DU145 cells upon SEC inhibition, while this behavior was not detected in LNCaP cells.

研究领域: 肿瘤学 · 代谢组学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF COLLOID AND INTERFACE SCIENCE · 2019 · IF 6.361

Poly (3, 4-ethylenedioxythiophene) modified polyvinylidene fluoride membrane for visible photoelectrocatalysis and filtration

Jiadong Liu,Yijia Wang,Lei Wang

A polyvinylidene fluoride (PVDF) organic conductive membrane with photoelectric activity was successfully developed via printing of oxidant (FeCl 3 ·6H 2 O) layer by layer and then chemical vapor deposition (CVD) of Poly (3, 4-ethylenedioxythiophene) (PEDOT). Four kinds of membranes were prepared by changing the number of oxidant coatings layers. The structure and photoelectric properties of four membranes were well characterized. The photocurrent density of 3.7 × 10 −4 A indicated that the four-oxidant coating layers membrane achieved the best performance in photo-electricity activity. A comprehensive study of degradation efficiency under different photoelectric conditions was carried out. Results showed that the photoelectrocatalytic removal of tetracycline hydrochloride was 1.6 and 7.9 times higher than that of photocatalysis and photolysis, respectively, under a voltage of 3 V assisted with visible light irradiation. The anti-interference and stability tests in continuous filtration process demonstrated that the dissolved organic matters (DOMs) can result in a 30% fluctuation on removal rate. The streaming potential tests of DOMs adsorption on membrane surface indicated that the more obvious the adsorption phenomenon was, the degradation of tetracycline hydrochloride was weaker. The degradation intermediates were identified and pathways were proposed in this work. The photoelectrocatalysis of PEDOT modified PVDF membrane provided a new potential for water purification .

研究领域: 环境科学 · 材料科学
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Chinese Journal of Natural Medicines · 2014 · IF 0

Synthesis and cytotoxic activity of 3, 4, 11-trihydroxyl modified derivatives of bergenin

De-Biao YAN,Dong-Ping ZHANG,Ming LI,Wen-Yuan LIU,Feng FENG,Bin DI,Qing-Long GUO,Ning XIE

To synthesize a series of 3-, 4-, and/or 11-trihydroxy modified bergenin derivatives and evaluated their cytotoxic activity in vitro . The phenolic hydroxyl groups of bergenin were protected by benzyl groups with benzyl bromide. Treatment of dibenzyl bergenin with the corresponding acid in the presence of EDC·HCl and DMAP in CH 2 Cl 2 , followed by hydrogenation over Pd/C catalysts, afforded derivatives of bergenin esters. All of the target compounds were identified by IR, MS, and 1 H NMR. Twenty-six novel and three known derivatives of bergenin esters were synthesized. Their cytotoxicity values were evaluated by the MTT assay on the inhibition of DU-145 and BGC-823 cells in vitro . Several triply-substituted ( 3a, 4a, 5a, 6a, 7a ) and doubly-substituted ( 8b, 9b ) bergenin derivatives exhibited higher cytotoxic activity than bergenin. The result showed that the size of substituents and the lipophilicity of the bergenin esters displayed an important role on their cytotoxic activity.

研究领域: 药物化学 · 肿瘤学
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SYNTHETIC METALS · 2024 · IF 4

Multi-color electrochromic copolymer films based on 2,2′-thiophene and 3, 4-ethylenedioxythiophen

Hailan Zeng,Ruomei Wu,Yanan Li,Haiyun Jiang,Xiang Wang,Weili Zhang,Ziyu Li,Jun Zhang,Zhengrong Yan

In this work, the copolymers were successfully synthesized by electrochemical polymerization of two monomers, bithiophene (BT) and 3,4-ethylenedioxythiophene (EDOT), in a lithium perchlorate/propylene carbonate (LiClO 4 /PC) solution. The as-prepared were characterized with the aid of cyclic voltammetry, colorimetric analysis, Fourier transform infrared spectroscopy, and Ultraviolet-visible spectroscopy. The electrochromic and colorimetric properties of copolymers poly(2,2′-bithiophene-co-3,4-ethylenedioxythiophene) (P(BT-co-EDOT)) and homopolymer poly(2,2′-bithiophene) (PBT) in 0.1 M LiClO 4 /PC solution were investigated, and the coloring process based on the redox reaction of the film was observed. When an anodic potential is applied, the copolymer P(BT-co-EDOT) films show a color change from blue-purple to blue-gray changes, and the homopolymer PBT shows a color change from orange to brown. In addition, spectroelectrochemistry studies indicate that copolymer P(BT-co-EDOT) has a lower optical band gap (1.73–1.87 eV) than homopolymer PBT. The copolymers P(BT-co-EDOT) show a high optical contrast (36.65–42.62%) and coloration efficiency (215.8–296.6 cm 2 C −1 ). The copolymer P(BT1-co-EDOT1) demonstrates excellent redox cycling stability, with 90% of the original optical contrast maintained after 500 cycles, making it an ideal candidate for copolymers.

研究领域: 材料科学 · 电化学
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JOURNAL OF ELECTRONIC MATERIALS · 2019 ·Vol. 48 ·期 11 ·7068-7075 · IF 1.676

Thermoelectric Properties of In2O3(ZnO)k (k = 3, 4, 5, 7) Superlattice Ceramics

Li Shuhui,Zhou Ying,Cui Lijun,Ge Zhenhua,Feng Jing

In 2 O 3 (ZnO) k superlattice ceramics are promising oxide thermoelectric materials, as superlattice interfaces are effective in scattering phonons and filtering low-energy electrons to decrease thermal conductivity and improve the figure of merit ( ZT ) value. In this work, homologous compounds were prepared by solid-state reaction method using ZnO and In 2 O 3 as raw materials. Phase purity and crystal structure were characterized by x-ray diffraction, revealing that In 2 O 3 (ZnO) k crystallizes in an R3 m space group for odd k values and P6 3 /mmc for even k values. The study of thermoelectric (TE) properties showed that as k increased, the thickness of InO(ZnO) + 3 also increased, while the electrical conductivity, thermal conductivity, Seebeck coefficient, power factor and ZT value were all decreased. In 2 O 3 (ZnO) 3 samples obtained a maximum power factor of 651  μ W m −1  K −2 at 973 K, and also achieved a maximum ZT value of 0.24 at 973 K.

研究领域: 材料科学 · 凝聚态物理 · 能源转换技术
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JOURNAL OF APPLIED POLYMER SCIENCE · 2011 ·Vol. 124 ·期 1 ·109-115 · IF 1.24

Oxidative chemical polymerization of 3, 4-ethylenedioxythiophene and its applications in antistatic coatings

Jikui Wang,Guofeng Cai,Xudong Zhu,Xiaping Zhou

The oxidative chemical polymerization of 3, 4-ethylenedioxythiophene (EDOT) was conducted at room temperature in the presence of poly(styrene sulfonate) (PSS) as the doping agent, sodium supersulphate (Na 2 S 2 O 8 ) and ferric sulphate(Fe 2 (SO 4 ) 3 ) as the compound oxidant and deionized water as the solvent. In order to remove sodium ion (Na + ), ferric ion (Fe 3+ ), and sulfate ion (SO4 2− ), certain amount of ion exchanger was added after 24 h, the dark blue poly(3, 4-ethylenedioxythiophene) (PEDT)/PSS solution was obtained. The influence of different proportions of EDOT and PSS, different proportions of EDOT and the compound oxidant, different stirring rates on the morphology, and surface resistivity were discussed. The influence of pH value of the PEDT/PSS solution, the coating thickness, and soak time on the surface resistivity was investigated. Recipe and experimental conditions were optimized and the PEDT/PSS solution was obtained with excellent performance which has relatively low in surface resistance, good water tolerance, and light transmittance. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2012

CAS / MDL: 15244-10-7 7775-27-1
研究领域: 材料科学 · 化学工程
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