Anti-Cancer Agents in Medicinal Chemistry
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2018
·Vol. 18
·期 3
·422-427
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IF 2.556
Kuang Shan,Sima Zhenhua,Liu Jiawei,Li Wuguo,Song Qiaoling,Zhang Qing,Yu Qiang
Background: 2-Methoxystypandrone (2-MS), isolated from the roots of Polygonum cuspidatum, is a potent dual inhibitor of the STAT3 and NF-ΚB pathways. Objective: To investigate the molecular targets and mechanisms of 2-MS. Method: A biotin-conjugated 2-MS analog, named
2-MS-Biotin, was designed and synthesized. The effects of 2-MS-Biotin on the STAT3 and NF-ΚB pathways were examined by Western blotting. The cytotoxicity of 2- MS-Biotin was evaluated using real-time cell analysis system. Proteins directly bound to 2-MS-Biotin were pulled down through
streptavidin agarose beads and were detected using Western blotting. Results: 2-MS-Biotin retained the inhibition activities of the parent compound 2-MS on the STAT3 and NF-ΚB pathways as well as on cancer cell growth. Also, JAK2 and IKK proteins can be effectively pulled down by
2- MS-Biotin. Conclusion: Using 2-MS-Biotin as a tool, both JAK2 and IKK were identified as the targets of 2-MS.
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高影响因子
JOURNAL OF INFECTION
·
2018
·
IF 4.603
Shuyi Wang,Juan Xue,Ping Lu,Chunshan Ni,Hao Cheng,Rui Han,Stijn van der Veen
Summary Objectives The rise in multidrug resistant Neisseria gonorrhoeae poses a threat to healthcare, while the development of an effective vaccine has remained elusive due to antigenic and phase variability of surface-expressed proteins. In the current study, we identified a fully conserved surface expressed protein and characterized its suitability as a vaccine antigen. Methods An in silico approach was used to predict surface-expressed proteins and analyze sequence conservation and phase variability. The most conserved protein and its surface-exposed Loop 2, which was displayed as both a structural and linear epitope on the oligomerization domain of C4b binding protein, were used to immunize mice. Immunogenicity was subsequently analyzed by determination of antibody titers and serum bactericidal activity. Results MtrE was identified as one of the most conserved surface-expressed proteins. Furthermore, MtrE and both Loop 2-containing fusion proteins elicited high protein-specific antibody titers and particularly the two Loop 2 fusion proteins showed high anti-Loop 2 titers. In addition, antibodies raised against all three proteins were able to recognize MtrE expressed on the surface of N. gonorrhoeae and showed high MtrE-dependent bactericidal activity. Conclusions Our results show that MtrE and Loop 2 are promising novel conserved surface-expressed antigens for vaccine development against N. gonorrhoeae .
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CHEMBIOCHEM
·
2023
·
IF 3.2
Xin Li,Changzheng Gao,Wanqing Wei,Wei Song,Weiwei Meng,Jia Liu,Xiulai Chen,Cong Gao,Liang Guo,Liming Liu,Jing Wu
Graphical We developed a pathway for the synthesis of L-ABA in a tri-enzymatic cascade in Escherichia coli BL21 (DE3) using L-Thr, and the expression of three enzymes was optimized by vector design. We solved the crystal structure of the key enzyme LDH and proposed protein engineering strategies based on the structure to improve the catalytic activity of the enzyme. L-2-aminobutyrate (L-ABA) is an important chiral drug intermediate with a key role in modern medicinal chemistry. Here, we describe the development of an efficient method for the asymmetric synthesis of L-ABA in a tri-enzymatic cascade in Escherichia coli BL21 (DE3) using a cost-effective L-Thr. Low activity of leucine dehydrogenase from Bacillus thuringiensis ( Bt LDH) and unbalanced expression of enzymes in the cascade were major challenges. Mechanism-based protein engineering generated the optimal triple variant Bt LDH M3 (A262S/V296C/P150M) with 20.7-fold increased specific activity and 9.6-fold increased k cat / K m compared with the wild type. Optimizing plasmids with different copy numbers regulated enzymatic expression, thereby increasing the activity ratio (0.3 : 1:0.6) of these enzymes in vivo close to the optimal ratio (0.4 : 1 : 1) in vitro . Importing the optimal triple mutant Bt LDH M3 into our constructed pathway in vivo and optimization of transformation conditions achieved one-pot conversion of L-Thr to 130.2 g/L L-ABA, with 95 % conversion, 99 % e.e . and 10.9 g L −1 h −1 productivity (the highest to date) in 12 h on a 500 mL scale. These results describe a potential biosynthesis approach for the industrial production of L-ABA.
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ACS Applied Materials & Interfaces
·
2022
·
IF 10.383
Xiaoyi Ma,Shiyu Guo,Shuangrong Ruan,Yao Liu,Jie Zang,Yushan Yang,Haiqing Dong,Yan Li,Tianbin Ren,Maomao An,Yongyong Li
Corona Virus Disease 2019 (COVID-19) pandemic, caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), is seriously threatening human health. Following SARS-CoV-2 infection, immune cell infiltration creates an inflammatory and oxidative microenvironment, which can cause pneumonia, severe acute respiratory syndrome, kidney failure, and even death. Clinically, a safe and effective treatment strategy remains to be established. Herein, a nano-bait strategy for inhibition of SARS-CoV-2 infection by redirecting viral attack while simultaneously relieving inflammation is developed. Specifically, the nano-bait was based on the exosome-sheathed polydopamine (PDA@Exosome) nanoparticles, which were generated by exocytosis of the PDA nanoparticles from H293T cells. In this approach, PDA@Exosome inherits from the source cells of H293T cells a surface display of ACE2 through pre-engineered expression. The resulting PDA@Exosome can compete with ACE2-expressing epithelial cells for S protein binding, in either the pre-exposure or post-exposure route. Moreover, relying on the ability of PDA to intercept and deactivate radical species, the PDA@Exosome can significantly attenuate the level of inflammatory cytokines by mediating oxidative stress, a major cause of organ injury. Due to its high trapping, multiple antioxidant ability, and good biocompatibility, the HACE2-exosome based nano-bait is a promising robust antiviral nanotherapeutics for the ongoing COVID-19 pandemic.
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2018
·
IF 3.909
Qiang Chu,Meng Chen,Dongxiao Song,Xixi Li,Yunyun Yang,Zihuan Zheng,Yonglu Li,Yangyang Liu,Lushuang Yu,Zheng Hua,Xiaodong Zheng
Oxidative stress is a critical cause for the progression of neurodegenerative diseases, indicating that screening natural antioxidant and pharmacological targeting of mechanism need more attention. Natural plant polysaccharides are the primary group of natural antioxidants showing mighty antioxidant activity. Therefore, a polysaccharide (AFP-2) from flowers of Apios americana Medik was isolated, purified and characterized. Then, a H 2 O 2 -induced PC12 cells oxidative stress model was established to investigate the neuroprotective role of AFP-2 and to clarify the potential mechanism of action against H 2 O 2 -induced neurotoxicity. It was found that AFP-2 reduced ROS production and mitochondrial damage caused by hydrogen peroxide in PC12 cells. In addition, data from transmission electron microscope and western blot displayed that AFP-2 significantly activated autophagy in PC12 cells via Akt-mTOR pathway. These results together qualify AFP-2 as an interesting natural polysaccharide worth further investigation as a neuroprotective agent.
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JOURNAL OF POWER SOURCES
·
2020
·
IF 8.247
Zhenhua Ge,Bin Fu,Xing Li,Jinping Zhao,Bo Ma,Zhiqiang Luo,Yantao Chen
Electrochemical water splitting is a very prospective technique to obtain the green hydrogen fuel . The oxygen evolution reaction becomes a limitation owing to the multiple electron transfer process. Thereby, a lot of attention is paid on the development of noble-metal free electrocatalysts for boosting the water oxidation process . The heterostructure of Mn 3 O 4 nanoparticles on Cu(OH) 2 nanowire arrays is fabricated, which exhibits an electrocatalytic activity close to RuO 2 . Compared with the single (hydro)oxides, the largely improved performance of the heterostructure towards water oxidation can be attributed to the enhanced charge transfer by the electronic interaction across the interface and the increased active sites for the rational combination of different active species . This work can be valuable for highlighting the role of heterostructure in the design and development of novel transition metal-based electrocatalysts for water oxidation.
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Scientific African
·
2023
·
IF 2.9
Berlanty A. Zayed,Ahmed N. Ali,Alaa A. Elgebaly,Nourhan M. Talaia,Mahmoud Hamed,Fotouh R. Mansour
The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) virus's worldwide pandemic has highlighted the urgent need for reliable, quick, and affordable diagnostic tests for comprehending and controlling the epidemic by tracking the world population. Given how crucial it is to monitor and manage the pandemic, researchers have recently concentrated on creating quick detection techniques. Although PCR is still the preferred clinical diagnostic test, there is a pressing need for substitutes that are sufficiently rapid and cost-effective to provide a diagnosis at the time of use. The creation of a quick and simple POC equipment is necessary for home testing. Our review's goal is to provide an overview of the many methods utilized to identify SARS-CoV 2 in various samples utilizing portable devices, as well as any potential applications for smartphones in epidemiological research and detection. The point of care (POC) employs a range of microfluidic biosensors based on smartphones, including molecular sensors, immunological biosensors, hybrid biosensors, and imaging biosensors. For example, a number of tools have been created for the diagnosis of COVID-19, based on various theories. Integrated portable devices can be created using loop-mediated isothermal amplification, which combines isothermal amplification methods with colorimetric detection. Electrochemical approaches have been regarded as a potential substitute for optical sensing techniques that utilize fluorescence for detection and as being more beneficial to the Minimizing and simplicity of the tools used for detection, together with techniques that can amplify DNA or RNA under constant temperature conditions, without the need for repeated heating and cooling cycles. Many research have used smartphones for virus detection and data visualization, making these techniques more user-friendly and broadly distributed throughout nations. Overall, our research provides a review of different novel, non-invasive, affordable, and efficient methods for identifying COVID-19 contagious infected people and halting the disease's transmission.
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JOURNAL OF MATERIALS SCIENCE-MATERIALS IN ELECTRONICS
·
2021
·Vol. 32
·期 10
·13941-13947
·
IF 2.478
Liu Ying,Cao Bo,Zhang Xu,Luo Rong,Luo Chunhua,Lin Hechun,Peng Hui
Layered Co(OH) 2 has been regarded as a potential candidate for pseudocapacitor electrode material, but it is limited by its poor conductivity and low surface area. Herein, carbonated multi-walled carbon nanotubes (MWCNTs-COOH) were used to improve the conductivity of α-Co(OH) 2 nanocomposites. α-Co(OH) 2 nanoflowers were successfully grown and tangled with MWCNTs-COOH to form a randomly oriented network structure mediated by ammonia using water-methanol as co-solvent at room temperature. The capacitance performances of the obtained α-Co(OH) 2 @MWCNT-COOH composites were investigated to find that MWCNT-COOH improved the specific capacitance efficiently. Especially, in the presence of 20% in mole of MWCNT-COOH, the composite gave rise to the high specific capacitance of 1027 F/g at the current density of 2 A/g with good cycle stability, whose specific capacitance remained 78% of its original even after 5000 cycles at 30 A/g current. The large surface area and strengthening the conductivity of the composites lead to the improvement of efficiency in charge/discharge process.
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JOURNAL OF THE AMERICAN CERAMIC SOCIETY
·
2020
·Vol. 103
·期 9
·5013-5027
·
IF 3.502
Yongbao Xiao,Yao Ji,Yichen Ye,Shujing Huang,Weichao Wang
Alkali-earth-metaphosphate-based fluoro-sulfo-phosphate M(PO 3 ) 2 –AlF 3 –MSO 4 (MPFS, M = Ca, Sr, Ba) glasses have been developed via simultaneously incorporating fluoride and sulfate into metaphosphate glass. Their glass-forming regions were efficiently determined under the guidance of thermodynamic calculation method. The physical and structural properties of BaPFS glass were investigated in detail. Furthermore, near-infrared spectroscopic properties of Er 3+ -doped BaPFS (Er–BaPFS) glass were studied. Physical parameters, such as Abbe's number ν d (55-75) and nonlinear refractive index n 2 (1.17-1.86 × 10 −13 esu), of BaPFS glass are strongly depended on P/F/S ratio. The structure of BaPFS glass gradually depolymerizes and tends to become multianionic when Ba(PO 3 ) 2 is substituted by AlF 3 and BaSO 4 . Anion-substitution strategy effectively modulates the property and structure of glass, providing a scheme to derive glass materials. In addition, enhanced emission at ~1.5 μm has been observed from Er–BaPFS glass along with large emission cross section (5.0-5.5 × 10 −21 cm 2 ) and long lifetime (6.7-7.3 ms), resulting in large figure of merit (3.46-3.84 × 10 −23 cm 2 ·s), which is a promising candidate for solid-state laser.
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Optical Materials Express
·
2019
·Vol. 9
·期 9
·3835-3842
·
IF 2.673
Xianshun Lv,Xianshun Lv,Xianshun Lv,Ping Wang,Huajian Yu,Huajian Yu,Yanyan Hu,Yanyan Hu,Huadi Zhang,Huadi Zhang,Chengcheng Qiu,Chengcheng Qiu,Jing Li,Jing Li,Jing Li,Xuping Wang,Xuping Wang,Bing Liu,Bing Liu,Yuanyuan Zhang,Yuanyuan Zhang,Yuanyuan Zhang
A colorless crystal of Ba2Mg(BO3)2 about 37 × 25 × 17 mm3 has been grown successfully by the Kyropoulos method. Thermal analyses results show that Ba2Mg(BO3)2 melts congruently. The phase purity of the raw materials and the grown crystals were confirmed by powder X-ray diffraction. Ba2Mg(BO3)2 exhibits a low UV cutoff of 187 nm and high transmittance below 3000 nm. The refractive indices of the crystal have been measured and the the least-squares fitting method was used to obtain the Sellmeier dispersion equations. The results indicate that Ba2Mg(BO3)2 is a potential birefringence crystal with large birefringence of 0.10422 at 546 nm.
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RSC Advances
·
2022
·Vol. 12
·期 21
·13251-13260
·
IF 4.036
Xinglong Li,Mingming Li,Yuxin Liu,Yisi Feng,Pan Pan
5-Hydroxymethylfurfural (HMF) is one of the most important platform molecules and could be transformed into a variety of fuel additives and high value-added chemicals. Multiple catalyst systems have been developed for the conversion of carbohydrates to HMF, but there are still unavoidable problems, including high temperature and pressure, difficult recovery of solvent, corrosion of equipment, poor catalyst circulation, etc. Herein, a new magnetic Fe3O4@SiO2@mSiO2-TaOPO4 catalyst for the preparation of HMF from fructose in 2-pentanol was developed. The structures of the catalysts were characterized by FT-IR, TSM, EDS, SEM, XRD and VSM. The 2-pentanol solvent is not only conducive to the production of HMF, but also enables the reaction to be carried out at a lower pressure. The highest yield of HMF (85.4%) was obtained using 20 wt% catalyst under 10% substrate concentration (0.5 g of fructose) at 120 °C for 3 h. The catalysts can be easily separated by magnetism. The slight decrease in catalyst activity after 7 cycles was mainly due to the loss of catalyst during the cycle operation. Simultaneously, the total yield of HMF was 51.3% after scale-up to 15 g of fructose, showing the possible industrial application potential of this catalyst system.
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JOURNAL OF CHEMICAL RESEARCH
·
2016
·
IF 0.661
Hui-Long Zhu,Yu-Wei Liu,Wei-Wei Liu,Fu-Jun Yin,Zhi-Ling Cao,Juan Bao,Meng Li,Ling-Yan Qin,Da-Hua Shi
Four 5-benzyl-1,3,4-thiadiazol-2-amine derivatives were synthesised from phenylacetic acid derivatives. The structures of the 5-benzyl-1,3,4-thiadiazole derivatives were characterised by NMR spectroscopy and X-ray crystallography. The acetylcholinesterase-inhibition activities were also tested. Among the four compounds, 5- (4-bromobenzyl)-1,3,4-thiadiazol-2-amine showed the best acetylcholinesterase-inhibition activity with an IC50 of 49.86 μM. The docking study performed with AUTODOCK demonstrated that this compound could interact with the catalytic active site of acetylcholinesterase.
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危险品化学品经营许可证（带存储）