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Journal of Chemistry · 2017 · IF 1.3

Synthesis and Biological Evaluation of Novel Jatrorrhizine Derivatives with Amino Groups Linked at the 3-Position as Inhibitors of Acetylcholinesterase

Xiaofei Jiang,Nengling Zhang,Nanqian Xiong,Yi Liu,Jianfeng Cao,ShengXiang Qiu

Jatrorrhizine was considered as one of the active constituents of Coptis chinensis Franch. Herein, jatrorrhizine derivatives with substituted amino groups linked at the 3-position were designed, synthesized, and biologically evaluated as inhibitors of acetylcholinesterase. Jatrorrhizine derivatives inhibited the activity of acetylcholinesterase (AChE) to a greater extent than the lead compound jatrorrhizine. All these jatrorrhizine derivatives were proved to be potent inhibitors of acetylcholinesterase (AChE) with submicromolar IC50 values, but less sensitive to butyrylcholinesterase (BuChE), which suggests that these jatrorrhizine derivatives are selective for AChE/BuChE. Compound 3g gave the most potent inhibitor activity for AChE (IC50 = 0.301 μM), which is greater than the lead compound jatrorrhizine. All these results demonstrated that these jatrorrhizine derivatives are potential inhibitors for AChE.

研究领域: 药理学 · 有机化学 · 神经科学
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MACROMOLECULAR BIOSCIENCE · 2018 ·Vol. 18 ·期 8 ·1800093 · IF 3.392

Preparation, Post-Modification, and Antibacterial Application of Gelatin Electrospun Membranes

Xi Yu,Liang Wang,Pengfei Yang,Jinku Xu,Mark G. Moloney,Lian Liu,Yunlin Pan,Yongqing Wang

Two bis(diaryldiazomethane)s substituted with amino groups are synthesized and used for the surface modification of membranes electrospun from gelatin. These membranes are then reacted with tolylene-2,4-diisocyanate to give urea-functionalized materials, so that hydrogen peroxide can be reversibly bound onto their surface. These membranes are characterized by scanning electron microscopy, XPS, differential scanning calorimeter, and tensile test to show their surface properties and bulk properties. The surface modification with amino-substituted diazomethanes and the subsequent cross-linking reaction with diisocyanates contribute to high loadings of hydrogen peroxide, and greatly increase the antibacterial activity of gelatin-derived membranes, which open a new horizon in the preparation of high loading antiseptic/antibacterial biomacromolecular surfaces and interfaces.

CAS / MDL: 9000-70-8
研究领域: 生物材料 · 医学工程 · 高分子化学
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Nature Communications · 2024 ·Vol. 15 ·期 1 ·1-10 · IF 14.7

Ligand engineering towards electrocatalytic urea synthesis on a molecular catalyst

Li Han,Xu Leitao,Bo Shuowen,Wang Yujie,Xu Han,Chen Chen,Miao Ruping,Chen Dawei,Zhang Kefan,Liu Qinghua,Shen Jingjun,Shao Huaiyu,Jia Jianfeng,Wang Shuangyin

Electrocatalytic C-N coupling from carbon dioxide and nitrate provides a sustainable alternative to the conventional energy-intensive urea synthetic protocol, enabling wastes upgrading and value-added products synthesis. The design of efficient and stable electrocatalysts is vital to promote the development of electrocatalytic urea synthesis. In this work, copper phthalocyanine (CuPc) is adopted as a modeling catalyst toward urea synthesis owing to its accurate and adjustable active configurations. Combining experimental and theoretical studies, it can be observed that the intramolecular Cu-N coordination can be strengthened with optimization in electronic structure by amino substitution (CuPc-Amino) and the electrochemically induced demetallation is efficiently suppressed, serving as the origination of its excellent activity and stability. Compared to that of CuPc (the maximum urea yield rate of 39.9 ± 1.9 mmol h −1 g −1 with 67.4% of decay in 10 test cycles), a high rate of 103.1 ± 5.3 mmol h −1 g −1 and remarkable catalytic durability have been achieved on CuPc-Amino. Isotope-labelling operando electrochemical spectroscopy measurements are performed to disclose reaction mechanisms and validate the C-N coupling processes. This work proposes a unique scheme for the rational design of molecular electrocatalysts for urea synthesis.

研究领域: 电化学 · 催化 · 材料科学 · 化学工程
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mBio · 2023 · IF 6.4

Gallic acid ameliorates colitis by trapping deleterious metabolite ammonia and improving gut microbiota dysbiosis

Jie Peng,Tong Liu,Pengfei Meng,Yue Luo,Siyue Zhu,Yanxin Wang,Mingxia Ma,Jiaojiao Han,Jun Zhou,Xiurong Su,Shiming Li,Chi-Tang Ho,Chenyang Lu

Gut microbiota dysbiosis is causally related to inflammatory bowel disease (IBD), and increased levels of the gut metabolite ammonia have been proposed to contribute to IBD development. In this study, we aimed to clarify the anti-colitis mechanism of gallic acid (GA) based on its ability to trap the deleterious metabolite ammonia and improve gut microbiota. Aminated product was detected in the fecal samples of mice after oral gavage of gallic acid (GA) and identified as 4-amino-substituted gallic acid (4-NH2-GA), thus confirming the ability of GA to trap ammonia in vivo. Then, we compared the beneficial effects of GA and 4-NH2-GA on dextran sulfate sodium (DSS)-induced colitis mouse and found that both compounds managed to alleviate colitis phenotypes, indicating ammonia trapping had no adverse effect on the original anti-colitis activity of GA. In addition, both GA and 4-NH2-GA improved the gut microbiota dysbiosis induced by DSS, and fecal microbiota transplantation was subsequently performed, which further revealed that the gut microbiota mediated the anti-colitis activity of both GA and 4-NH2-GA. In summary, this study clarified that GA alleviated colitis by targeting both the symptoms and root causes: it directly reduced the deleterious metabolite ammonia by forming aminated metabolites without compromising the original anti-colitis activity, and it also improved gut microbiota dysbiosis, which in turn contributed to the alleviation of colitis. Since the GA structure is presented in various polyphenols as a common building block, the novel anti-colitis mechanism obtained from GA may also apply to other complex polyphenols.

CAS / MDL: 119-90-4
研究领域: 药理学 · 胃肠病学 · 微生物学
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JOURNAL OF MOLECULAR STRUCTURE · 2021 · IF 3.196

Two novel mono-hydroxyl pyranoanthocyanidins bearing dimethylamino substituent(s) for dye-sensitized solar cell

Xiaolong Shi,Yuanzuo Li,Lihai Wang

Two novel analogues (AF3-1 and AF3-2) of natural pigments that were originally found in wine product, pyranoanthocyanidins, were designed based on pyrano-4′-dimethylamino-10-phenyl-flavylium (AF3) by respectively introducing another electron donor(s), dimethylamino and two methoxyl groups, to the phenyl moiety. They were synthesized and then successfully applied as sensitizers in DSSC to study effect of the additional donor(s) on the DSSC performance for such pyranoanthocyanidin. The introduced second dimethylamino substituent of AF3-1 slightly red shifts the absorption spectrum. Both title dyes show relatively strong ability to shield the photoanode surface from electrolyte and to restrain the electron recapture process. Yet it is difficulty for them to adsorb on the semiconductor surface effectively and to avoid undesirable dye aggregation. DSSCs based on the designed pyranoanthocyanidin turn out to have much higher V oc but decreased J sc compared to AF3. PCE of DSSC assembled with the better of the two pyranoanthocyanidins, AF3-1, is 1.79%, on the same level as that of the reference sensitizer.

研究领域: 化学 · 材料科学 · 太阳能
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TRANSACTIONS OF THE INDIAN INSTITUTE OF METALS · 2018 ·Vol. 71 ·期 5 ·1113-1126 · IF 0.91

Phosphorous Phthalocyanine Analogues as Degradable Corrosion Inhibitor of Mild Steel in 1 mol/L HCl

Chen Jin-ping,Zhang Xue-song

Four hydrosoluble macroazacyclic compounds, phosphorus phthalocyanine and substituent phosphorus triaza tetrabenzo corrole substituted with amino or sulfonate groups respectively, were investigated as corrosion inhibitors for mild steel in 1 mol/L HCl. The results obtained from weight loss test showed that the inhibitive efficiency of phosphorus phthalocyanine was higher than the phosphorus triaza tetrabenzo corrole; while the amino substituent phosphorus phthalocyanine showed the strongest inhibitive ability among them. The potentiodynamic tests illustrated that these inhibitors protected steel according to the mixed type mechanism on electrochemistry; while the impedance spectra revealed the increasing of charge transfer resistance and the decreasing of double layer capacitor caused by the adsorption of inhibitors. The surface analysis (XPS and SEM) proved the protection of steel surface by the adsorbed inhibitors. The molecular dynamic simulation indicated the advantages of phosphorus phthalocyanine as inhibitors associating with highly binding stability and stable adsorption configuration. The unique degradation properties of these inhibitors under visible light made them useful with environmental advantage in application.

CAS / MDL: 574-93-6
研究领域: 材料科学 · 腐蚀工程 · 化学工程 · 表面科学
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POLYMER · 2011 · IF 3.829

A readily modified polyethersulfone with amino-substituted groups: Its amphiphilic copolymer synthesis and membrane application

Zhuan Yi,Liping Zhu,Liang Cheng,Baoku Zhu,Youyi Xu

An amino-substituted polyethersulfone (PES) was synthesized by the polycondensation of a functional monomer bis(3-amino-4-hydroxyphenyl) sulfone with bis(4-fluorophenyl) sulfone. The amine groups incorporated into PES were employed as anchors to immobilize the chain transfer agents of reversible addition-fragmentation polymerization (RAFT). The resultant macro chain transfer agent was used to initiate the polymerization of the hydrophilic monomers N -isopropyl acrylamino (NIPAAm) and N, N -dimethylamino-2-ethyl methacrylate (DMAEMA), respectively. The gel permeation chromatography (GPC) results confirmed the successful synthesis of the amphiphilic copolymers PES- g -PNIPAAm and PES- g -PDMAEMA, and these two copolymers were perhaps the few examples of amphiphilic copolymer synthesized via a radical polymerization from PES main chains. The amino-substituted PES seemed a versatile precursor that showed a potential of functionalization via various strategies including click chemistry, atom transfer radical polymerization and RAFT polymerization. The synthesized amphiphilic copolymers were finally used as additives to improve the hydrophilicity and the filtration performances of PES membranes.

CAS / MDL: 5407-87-4 538-75-0
研究领域: 高分子化学 · 材料科学 · 膜技术
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