Medicinal Chemistry
·
2017
·Vol. 13
·期 8
·753-760
·
IF 2.331
Guo Ping,Xie Zixin,Zhang Huan,Zhang Zaikui,Han Chao,Cheng Donghua,Lin Dan,Zhang Yuan,Wang Xuebao,Guo Xin,Ye Faqing
Background: Thienopyrimidinone is a newly designed, selective fibroblast growth factor receptor 1 (FGFR1) inhibitor with an excellent anticancer effect. Objective: The goal of the present study was to design and synthesize better FGFR1 inhibitors through modifications of the lead
compound thienopyrimidinone. Methods: In the present study, a series of C-2 substituted derivatives of thienopyrimidinone, namely L1-L16, were synthesized, and their inhibitory effects on FGFR1 were evaluated. The anti-proliferative activities of these compounds were assessed by MTT assay.
Results: Among the novel derivatives, L11 was found to exert remarkable FGFR1 inhibitory activity (79.93% at 10 μM) and anti-proliferative activity, with IC50 values of 2.1, 2.5, and 3.5 µM in the FGFR1-overexpressing cell lines, H460, HT-1197, and B16F10, respectively.
Conclusion: Our newly synthesized thienopyrimidinone derivatives may be candidate FGFR1 inhibitors for future development as novel anticancer agents.
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PubMed
高影响因子
Biomaterials Science
·
2019
·Vol. 8
·期 3
·830-836
·
IF 5.251
Chengjun Wang,Ying Qian
A novel photosensitizer carbazolyl-BODIPY (Cz-BODIPY) with an orthogonal donor–acceptor structure was developed for photodynamic therapy (PDT). The photosensitizer Cz-BODIPY showed strong singlet oxygen sensitizing capability (ΦΔ = 0.68 in MeOH), excellent water solubility in dilute solution, and high photostability. The photosensitizer Cz-BODIPY exhibited negligible dark cytotoxicity and high phototoxicity (IC50 0.45 μM). Cz-BODIPY could induce cell apoptosis upon light illumination. Three cell states including living cells, apoptotic cells, and dead cells in the PDT process of Cz-BODIPY were determined via the Hoechst 33342/PI dual staining assays. The ROS (reactive oxygen species) generation in living cells during the PDT process of Cz-BODIPY was captured by the ROS detector, dihydroethidium (DHE). The photosensitizer Cz-BODIPY could be assimilated by zebrafish to generate ROS and diminish the integrity of zebrafish tissue upon light illumination. Tumor cell growth could be inhibited by Cz-BODIPY upon light illumination. The photosensitizer Cz-BODIPY displayed potential in real PDT application.
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高影响因子
JOURNAL OF BIOTECHNOLOGY
·
2015
·
IF 2.871
Xia Yi,Peng Zhang,Jiaoe Sun,Yi Tu,Qiuqiang Gao,Jian Zhang,Jie Bao
Pediococcus acidilactici TY112 producing l -lactic acid and P. acidilactici ZP26 producing d -lactic acid, were engineered from the wild-type P. acidilactici DQ2 by ldhD or ldh gene disruption , and the robustness of the wild-type strain to the inhibitors derived from lignocellulose pretreatment was maintained well. In simultaneous saccharification and fermentation (SSF), 77.66 g L −1 of l -lactic acid and 76.76 g L −1 of d -lactic acid were obtained at 25% (w/w) solids content of dry dilute acid pretreated and biodetoxified corn stover feedstock. l - and d -Lactic acid yield and productivity were highly dependent on the inhibitor removal extent due to the significant down-regulation on the expressions of ldh and ldhD encoding lactate dehydrogenase by inhibitor, especially syringaldehyde and vanillin at the low concentrations. This study provided a prototype of industrial process for high titer l - and d -lactic acid production from lignocellulose feedstock.
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高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2023
·
IF 8.2
Yanan Sun,Xiangze Jia,Chin Ping Tan,Bin Zhang,Xiong Fu,Qiang Huang
The formation of inclusion complexes (ICs) between V-type starch and flavors is traditionally conducted in an aqueous system. In this study, limonene was solid encapsulated into V6-starch under ambient pressure (AP) and high hydrostatic pressure (HHP). The maximum loading capacity reached 639.0 mg/g after HHP treatment, and the highest encapsulation efficiency was 79.9 %. X-ray Diffraction (XRD) results showed that the ordered structure of V6-starch was ameliorated with limonene, which avoided the reduction of the space between adjacent helices within V6-starch generated by HHP treatment. Notably, HHP treatment may force molecular permeation of limonene from amorphous regions into inter-crystalline amorphous regions and crystalline regions as the Small-angle X-ray scattering (SAXS) patterns indicated, leading to better controlled-release behavior. Thermogravimetry analysis (TGA) revealed that the solid encapsulation of V-type starch improved the thermal stability of limonene. Further, the release kinetics study showed that a complex prepared with a mass ratio of 2:1 under HHP treatment sustainably released limonene over 96 h and exhibited a preferable antimicrobial effect, which could extend the shelf life of strawberries.
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DOI
PubMed
高影响因子
JOURNAL OF COLLOID AND INTERFACE SCIENCE
·
2022
·
IF 9.965
Zuyang Luo,Qimin Peng,Zhiyang Huang,Lixia Wang,Yuting Yang,Jiaxin Dong,Tayirjan Taylor Isimjan,Xiulin Yang
Developing high-activity, long-durability, and noble metal-free oxygen evolution (OER) and hydrogen evolution (HER) cocatalysts are the bottlenecks for efficient overall water splitting (OWS). Here, novel cobalt vanadium oxides doped by nitrogen were synthesized by nitriding Co 2 V 2 O 7 @NF precursor at 300–450 °C for OER and HER reactions. N-Co 2 V 2 O 7 @NF (350 °C) and N-Co 2 VO 4 /VO 2 @NF (400 °C) show remarkable OER and HER performance with overpotentials of 310 mV and 224 mV at high current density (100 mA cm −2 ). Besides, they also revealed long-term solid stability even after 170 h and 700 h of continuous performance. Furthermore, the N-Co 2 V 2 O 7 @NF (+) ||N-Co 2 VO 4 /VO 2 @NF (–) OWS device possesses a cell voltage of 1.93 V at 500 mA cm −2 better than RuO 2 @NF (+) ||Pt/C@NF (–) (2.02 V) and can operate for 60 h with almost no degradation. This extraordinary performance can be attributed to the nanosheet structure, which can maximize the exposure of active sites and accelerate the mass transfer. Moreover, density functional theory (DFT) calculations suggest that N -doping can fine-tune the d-band center and band gap to facilitate intermediate adsorption and electron motion. The method presented here can be applied in other novel N -doped electrocatalysts for the energy field.
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高影响因子
JOURNAL OF MOLECULAR STRUCTURE
·
2021
·
IF 3.196
Jiancheng Zhao,Rui Liu,Zhenzhou Zhang,Qianqian Xing,Honghong Chang,Xianglin Hou,Yingxiong Wang
The tautomer structure of monosaccharides plays an important role in its conversion and utilization, which is mainly manifested in the selectivity of the product and the reaction mechanism. The tautomer distributions of N -acetyl- D -glucosamine (GlcNAc), a natural nitrogen-containing monosaccharide were investigated by quantitative 1 H NMR ( 1 H qNMR) and 13 C NMR ( 13 C qNMR) at 298 K under the condition commonly utilized for biorefinery. Catalysts used for biorefinery, i.e. BaCl 2 , KCl, ZnCl 2 , MgCl 2 , B(OH) 3 , SnCl 4 ·5H 2 O and amino acid ionic liquid were introduced into D 2 O or DMSO‑ d 6 to explore the tautomer distributions of GlcNAc. The introduction of ZnCl 2 and SnCl 4 ·5H 2 O promoted the conversion of α-pyranose to β-pyranose. The introduction of amino acid ionic liquid has little effect on the percentage of tautomers in D 2 O. However, when the amino acid ionic liquid, such as [Thr]Cl, was introduced into DMSO‑ d 6 , the proportion of β-pyranose increased to 29.06%, compared with no catalyst introduced. Besides, we also studied the tautomer distributions of GlcNAc in commonly utilized reaction solvents for biorefinery, such as N,N -dimethylformamide, N , N -dimethylacetamide, N -methyl-2-pyrrolidinone, ethylene and glycerol. In these solvents, the proportion of β-pyranose in N,N -dimethylformamide and glycerol was reduced to 25.84% and 38.38%, respectively. This study provides the basic experimental data of tautomer distributions of GlcNAc, and guided the conversion and utilization of GlcNAc in the future.
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高影响因子
Biomedical Physics & Engineering Express
·
2022
·Vol. 8
·期 3
·035002
·
IF 0
Siqi Li,Xiaoling Yu,Yuan Li,Tian Zhang
For nerve tissue engineering (NTE), scaffolds with the ability to release drugs under control and support the rapid proliferation of cells are very important for the repair of nerve defects. This study aimed to fabricate a conductive drug-loaded fiber mat by electrospinning and assess its potential as a scaffold for Schwann cells proliferation. The conductive polypyrrole (PPy) was coated on an electrospun poly (D, L-lactide) (PLA) fibrous mat, which was simultaneously embedded with protein-loaded chitosan nanoparticles and ibuprofen as a model small molecule drug. The fibrous mat shows suitable conductivity, mechanical properties, and hydrophilicity for NTE. For drug release and degradation studies, the fibrous mat can achieve sustained release of bovine serum albumin (BSA) and ibuprofen, and the PPy coating can increase the surface wettability and conductivity while slowing down the degradation of the fibrous mat. The application of electrical stimulation (ES) to the fibrous mat can accelerate the release of ibuprofen, but there was no significant effect on the release rate of the protein. The fibrous mat showed no cytotoxicity in vitro, and Schwann cells (SCs) can adhere, grow, and proliferate well on mats. At the 120th hour of culture in vitro, the relative growth rate of SCs on the conductive drug-loaded fibrous mat reached 198.22 ± 2.34%, which was an increase of 37.93% compared to the SCs on the drug-loaded fibrous mat with ES. The density and elongation of SCs on the conductive drug-loaded fibrous mat were greater than those on the PLA fibrous mat, indicating that the conductive polypyrrole-coated electrospun chitosan nanoparticles/PLA fibrous mat has good potential for application in nerve regeneration.
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CRYSTENGCOMM
·
2021
·Vol. 23
·期 22
·3989-3994
·
IF 3.545
Anqi Li,Xiaofan Ma,Jie Ma,Qingyi Yuan,Jun Zhang,Xiaopeng Xuan
Herein we reported a simple and economical method for fabricating a portable separation device based on exfoliated 2D-metal–organic framework (2D-MOF) nanosheets. This device is composed of a layered Cu-MOF as a filter and a syringe filter as the holder. Benefiting from the structural characteristic of the 2D-MOF nanosheets, the separation experiment reveals that this strategy can exhibit high efficiency and selectivity for dyes with different sizes. This device can be used disposably for a special purpose due to the low cost, simple manufacturing process in an emergency.
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高影响因子
POLYMER SCIENCE SERIES A
·
2021
·Vol. 63
·期 3
·267-274
·
IF 1.206
Jun Shao,Tang Juan,Pu Shouzhi,Hou Haoqing
Abstract Blending of poly( L -lactic acid)/poly( D -lactic acid) (PLLA/PDLA) leads to the formation of poly(lactide) stereocomplexation (PLA SC), which exhibits higher melting temperature and faster crystallization rate. The crystallization behavior of PLA homochiral crystallization (HC) under the existence of PLA SC was also widely investigated. During the variable processing, the SC with different morphologies would produce, and these SC could exert different influences on the subsequent formation of HC. However, the effects of SC developed in various conditions on the formation of HC are not compared yet and are also not clear until now, and which is important for the application of PLLA/PDLA blends. In this paper, the PDLAs with different molecular weights were blended with PLLA at a weight ratio of PLLA/PDLA 90/10, and the crystallization behaviors of PLLA HC from different conditions were investigated by differential scanning calorimetry (DSC). Results indicated that, incorporating a small amount of PDLA accelerated the formation of PLLA HC significantly regardless of the SC developed from the solution evaporation or the melt. The higher crystallization rate of HC was received in the PLLA/PDLA specimens with lower molecular weight of PDLA. For the specimens crystallized from the partially melting (most of SC developed during solution evaporation), the crystallization rate was higher than that corresponding specimens crystallized from the completely melting state (the SC were produced from the melt). This discrepancy would be due to variable SC morphologies produced during diverse processing.
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高影响因子
FUEL
·
2024
·
IF 6.7
Fengrui Li,Xiao Dai,Linfeng Zhang,Huadong Wu,Jianding Li,Jia Guo,Qun Yi
Conjugated microporous polymers (CMPs) with a donor–acceptor (D-A) molecular structure usually express the properties of well light-induced electron/hole separation efficacy and high photocatalytic activity. The triphenylamine (TPA) with a special three-dimensional propeller structure was chose as the electron donor, and the dibenzothiophene sulfone (BTDO) groups as the chain scaffold and electron acceptor to construct and prepare a unique “macrocyclic structure” D-A type CMPs photocatalyst (TPA-BTDO) for photocatalytic hydrogen production (PHP). In order to further improve the conjugation degree of the CMPs and enhance the electron transfer capacity and light absorption, the thiophene units was introduced as “π-bridge” to form a macrocyclic D-π-A type CMPs photocatalyst (TPA-T-BTDO). The results show that the addition of thiophene greatly improves the coplanarity between the donor–acceptor units, and the prepared TPA-T-BTDO-1 exhibited an amazing PHP efficiency of 65.41 mmol h −1 g −1 in the visible light region. More importantly, the PHP efficiency also reaches up to 39.63 mmol h −1 g −1 under the natural light conditions. Both the characterizations and DFT simulation results prove that the twisted structure of the TPA donor decreases the dihedral angle between the benzene rings of BTDO and TPA, which improves the coplanarity of polymer skeleton and then prevents the charges transfer along the polymer chain for recombination. This study highlights the significant influence of the geometry of the electron donor on the photocatalytic activity, as well as the strategy of the structure adjusting by adding suitable bridges between the donor–acceptor units.
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高影响因子
JOURNAL OF CHROMATOGRAPHY A
·
2018
·
IF 3.716
Liping Zhao,Juan Qiao,Ke Zhang,Dan Li,Hongyi Zhang,Li Qi
A chiral ligand exchange capillary electrochromatography (CLE-CEC) protocol was designed and implemented for d , l -amino acids enantioseparation with poly(maleic anhydride-styrene-methacryloyl- l -arginine methyl ester) as the coating. The block copolymer was synthesized through the reversible addition fragmentation chain transfer reaction. In the constructed CLE-CEC system, poly (methacryloyl- l -arginine methyl ester) moiety of the block copolymer played the role as the immobilized chiral ligand and Zn (II) was used as the central ion. Key factors, including pH of buffer solution, ratio of Zn (II) to ligands, the mass ratio of monomers in the block copolymer, which affect the enantioresolution were investigated. Comparing with the bare capillary, the CLE-CEC enantioresolution was enhanced greatly with the coating one. 5 Pairs of d , l -amino acids enantiomers obtained baseline separation with 5 pairs partly separated. The mechanism of enhancement enantioresolution of the developed CLE-CEC system was explored briefly. Further, good linearities were achieved in the range of 25.0 μM–5.0 mM for quantitative analysis of d -glutamine (r 2 = 0.997) and l -glutamine (r 2 = 0.991). Moreover, the proposed CLE-CEC assay was successfully applied in the kinetics study of glutaminase by using l -glutamine as the substrate.
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高影响因子
Chemical & Biomedical Imaging
·
2023
·
IF 0
Baoling Li,E Pang,Shaojing Zhao,Guowei Deng,Shuodong Wang,Benhua Wang,Jieyun Wu,Guangle Niu,Xiangzhi Song,Minhuan Lan
Near-infrared (NIR)-II fluorescence and photoacoustic (PA) dual-model imaging-guided photothermal therapy (PTT) can precisely diagnose and treat tumors and evaluate the therapeutic efficacy in real-time. Herein, we utilized a donor-π-acceptor (D-π-A) structured hemicyanine dye (named M1) with a large conjugated structure and strong intramolecular charge transfer effect and demonstrated that the aggregation of M1 could significantly enhance its photophysical performance by improving its photostability and photothermal conversion capability as compared with M1 in a single molecular state. Furthermore, we prepared water-dispersible NIR-II fluorescent nanoparticles (M1 NPs) by wrapping M1 with DSPE-PEG2000-NH2. The obtained M1 NPs exhibit strong NIR-I absorption and NIR-II fluorescence with their maxima at 734 and 1040 nm, respectively, with a fluorescence quantum yield of 2.84%. Moreover, M1 NPs also exhibit excellent biocompatibility, good photostability, and high photothermal conversion efficiency of 77.5%. In vitro and in vivo experiments reveal that M1 NPs can effectively image tumors through NIR-II fluorescence and PA signals, inhibit DNA replication, trigger cytoskeleton collapse, and eventually induce tumor cell apoptosis under 808 nm laser irradiation. Based on these outstanding properties, the application of M1 NPs in PA and NIR-II fluorescence imaging-guided PTT of tumors is demonstrated.
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