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Journal of Coatings Technology and Research · 2019 ·Vol. 16 ·期 3 ·857-868 · IF 1.584

Polyelectrolytes fabrication on magnesium alloy surface by layer-by-layer assembly technique with antiplatelet adhesion and antibacterial activities

Peng Mengke,Zhang Xiaodan,Xiao Xiao,Dong Mengjin,Zhao Guowei,Liu Peng,Chen Yashao,Wang Changhao

Abstract Magnesium alloy (MgA) was widely used in biomedical field owing to its good biocompatibility and degradability. The surface of MgA was usually modified to improve its corrosion resistance, biocompatibility, and biological properties. Herein, we employed a layer-by-layer assembly technique to assemble both polyanionic and polycationic electrolytes onto the microarc oxidation-treated MgA surface to yield MgA-MgO-PEI-[Ge(HANPs)/Lzm] 50 , where the gelatin-conjugated hydroxyapatite nanoparticles [Ge(HANPs)] are the polyanionic electrolyte, lysozyme (Lzm) is the polycationic electrolyte, and polyethyleneimine (PEI) is the transition layer. The morphology and chemical composition of MgA-MgO-PEI-[Ge(HANPs)/Lzm] 50 were characterized by X-ray diffraction, scanning electron microscopy, and X-ray photoelectron spectroscopy, indicating that [Ge(HANPs)/Lzm] 50 were successfully fabricated on the surface of MgA-MgO. The surface of MgA-MgO-PEI-[Ge(HANPs)/Lzm] 50 exhibited good hydrophilicity as evidenced by the low water contact angle of 24.5°. Excellent corrosion resistance of MgA-MgO-PEI-[Ge(HANPs)/Lzm] 50 was obtained since it can decrease about four orders of magnitude of corrosive current ( I corr ) compared to pristine MgA. The biological assay for MgA-MgO-PEI-[Ge(HANPs)/Lzm] 50 showed good antiplatelet adhesion and excellent antibacterial activities against both E. coli and S. aureus. Graphical abstract

研究领域: 生物材料学 · 表面工程学
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CHEMICAL RESEARCH IN CHINESE UNIVERSITIES · 2016 ·Vol. 32 ·期 6 ·943-946 · IF 1.086

Studies on triterpenoid glycosides from rhizomes of Panacis majoris and their antiplatelet aggregation activity

Li Min,Jin Yongri,Wang Xiaozhong,Wu Qian,Liu Ying,Li Peng,Li Xuwen

A new triterpenoid glycoside( 1 ) and seven known triterpenoid glycosides, pseudoginsenoside RT 2 ( 2 ), yesanchinoside R 2 ( 3 ), vinaginsenoside R13( 4 ), vinaginsenoside R8( 5 ), notoginsenoside E( 6 ), 6′′′- O -acetylginsenoside Re( 7 ), 6″- O -acetylginsenoside Rb 1 ( 8 ), were isolated from the rhizomes of Panacis majoris . The new triterpenoid glycoside was elucidated as 3- O -[ β - D -glucopyranosyl-(1→2)- β - D -(6′- O -ethyl)-glucuronopyranosyl]-oleanolic acid-28- O - β - D -glucopyranoside by extensive spectroscopic and phytochemical methods. Compounds 2 ― 8 were obtained from the plant for the first time. Compounds 3 and 4 displayed good activities against adenosine diphosphate (ADP)-induced platelet aggregation, and compounds 1, 5, 6 and 8 showed moderate activities. Compound 6 exhibited moderate antiplatelet aggregation activity induced by arachidonic acid(AA).

研究领域: 天然产物化学 · 药用植物学 · 心血管药理学 · 药物代谢 · 分子药理学
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CHEMISTRY & BIODIVERSITY · 2024 · IF 2.3

Design, Synthesis, and Anti-Inflammatory Activity Evaluation of Novel Indanone Derivatives for the Treatment of Vascular Dementia

Xue-Song Tang,Lin-Yu He,Sheng-Nan Li,Wen-Cheng Zhang,Ze-Yu Wu,Ai-Ling Hui

Vascular dementia (VaD) is a neurodegenerative disease resulting from cerebral vascular obstruction, leading to cognitive impairment, and currently lacks effective treatment options. Due to its complex pathogenesis, multi-target drug design (MTDLs) strategies are considered among the most promising therapeutic approaches. In this study, we designed and synthesized a series of novel indanone derivatives targeting targets related to vascular health and dementia. The results indicated that compound C 5 exhibited excellent acetylcholinesterase inhibitory activity (IC 50 =1.16 0.41 μM) and anti-platelet aggregation activity (IC 50 =4.92±0.10 μM) within ranges of 0.1–1000 μM and 0.03–300 μM, respectively, possibly mediated by molecular docking interactions. Furthermore, compound C 5 demonstrated protective effects on cells at concentrations ≤50 μM, significantly reducing the release of nitric oxide (NO), tumor necrosis factor-alpha (TNF-α), and interleukin-1 beta (IL-1β) in a concentration-dependent manner, showcasing its potent neuroinflammatory inhibitory effects. Anti-inflammatory therapies are regarded as effective strategies for treating VaD. Therefore, compound C 5 holds promise as a novel candidate drug for further investigation into the treatment of vascular dementia. Graphical

研究领域: 神经病学 · 药理学 · 药物设计
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ARCHIV DER PHARMAZIE · 2019 ·Vol. 353 ·期 2 ·1900231 · IF 2.145

Design, synthesis, and biological evaluation of 4-methoxy-3-arylamido-N-(substitutedphenyl)benzamide derivatives as potential antiplatelet agents

Xiujie Liu,Xin Chen,Kai Qiu,Zhihao Zhang

A series of 4-methoxy-3-arylamido- N -(substitutedphenyl)benzamides 6a – u were designed according to the splicing principle of structural design in the medicinal chemistry theory and were synthesized in five steps: nitration, acylation, ammoniation, reduction, and secondary ammoniation. The structures of the target compounds were characterized and verified by infrared, 1 H nuclear magnetic resonance (NMR), 13 C NMR, and electron spray ionization spectroscopy. Their in vitro antiplatelet aggregation activities induced by adenosine diphosphate (ADP) or arachidonic acid (AA) were assessed by Born's method. The biological evaluation revealed that all compounds exhibited certain levels of activities in both of the antiplatelet aggregation assays; compounds 6c (IC 50 = 3.84 μM) and 6f (IC 50 = 3.12 μM) displayed the strongest antiplatelet aggregation activities in the ADP-induced and AA-induced assay, separately. Moreover, compounds that had stronger activities were chosen for cell toxicity testing via the cell counting kit-8 assay. The results indicated that none of the compounds had obvious cell toxicity against L929 cells at the doses of 10 and 20 μM. It is worth pointing out that compound 6c showed the highest antiplatelet activity and the lowest cell toxicity. In general, 4-methoxy-3-arylamido- N -(substitutedphenyl)benzamides have the potential to become a kind of safer and more effective antiplatelet agents.

研究领域: 药物化学 · 药理学
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Frontiers in Bioengineering and Biotechnology · 2022 · IF 6.064

Heparin/Collagen-REDV Modification of Expanded Polytetrafluoroethylene Improves Regional Anti-thrombosis and Reduces Foreign Body Reactions in Local Tissues.

Yaping Shan,Gang Chen,Qiqi Shi,Jiaxi Huang,Yaping Mi,Wenbo Zhang,Huifeng Zhang,Bing Jia

Prosthetic implants of expanded polytetrafluoroethylene (ePTFE) in the cardiovascular system have a high failure rate over the long term because of thrombosis and intimal hyperplasia. Although multiple surface modification methods have been applied to improve the anti-thrombotic and in situ endothelialization abilities of ePTFE, none have delivered outstanding results in vivo . Our previous study combined heparin/collagen multilayers and REDV peptides to modify ePTFE, and the in-vitro results showed that modification ePTFE with heparin/collagen-REDV can promote the cytocompatibility and antiplatelet property. This study illustrated the physical change, selective endothelial cells capture ability, and in vivo performance in further. The physical test demonstrated that this modification improved the hydrophilicity, flexibility and strength of ePTFE. A competition experiment of co-cultured endothelial cells and vascular smooth muscle cells verified that the heparin/collagen-REDV modification had high specificity for endothelial cell capture. A rabbit animal model was constructed to evaluate the in vivo performance of modified ePTFE implanted in the right ventricular outflow tract. The results showed that heparin/collagen-REDV modification was safe, promoted endothelialization, and successfully achieved regional anti-thrombosis without influencing body-wide coagulation function. The pathologic manifestations and mRNA expression pattern in tissues in contact with modified ePTFE indicated that this modification method may reduce M2-type macrophage infiltration and the expression of genes related to immune and inflammatory responses. The heparin/collagen-REDV modification may lower the incidence of complications related to ePTFE implantation and has good prospects for clinical use.

研究领域: 生物材料 · 心血管工程 · 组织工程 · 生物医学工程 · 免疫学
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