EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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2016
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IF 3.902
Yu-Ou Teng,Hong-Ye Zhao,Jing Wang,Huan Liu,Mei-Le Gao,Yao Zhou,Kai-Lin Han,Zhen-Chuan Fan,Yong-Min Zhang,Hua Sun,Peng Yu
A series of novel di- or trisubstituted isatin derivatives were designed and synthesized in 5–6 steps in 25–45% overall yields. Their structures were confirmed by 1H NMR and 13C NMR as well as LC-MS. The anticancer activity of the fourty-three new isatin derivatives against human T lymphocyte cells Jurkat was evaluated by MTT assay in vitro . SAR study suggested that the combination of 1-benzyl and 5-[ trans -2-(methoxycarbonyl)ethen-1-yl] substitution greatly enhanced their cytotoxic activity. Among them, compound 2h was shown to have a significant cytotoxic activity with an IC50 value of 0.03 μM, more than 330-fold higher than that of it's mother molecule isatin. Investigation of the cell morphology changes and annexin-V/PI staining study demonstrated that compound 2h inhibited the proliferation of Jurkat cells by inducing apoptosis. Since compound 2h induced the dissipation of mitochondrial membrane potential and the activation of caspase-3, it was obvious that compound 2h inhibited the proliferation of Jurkat cells through the mitochondrial apoptotic pathway. Other than this, compound 2h exerted inhibition effect to many other tumor cells and only showed weak cytotoxic to human normal cells suggesting that compound 2h possessed a broad range of anticancer spectrum and high safety to normal cells.
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高影响因子
Frontiers in Bioscience-Landmark
·
2023
·Vol. 28
·期 11
·311
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IF 3.1
Qing Zhu,Yuanshan Han,Ying He,Yilan Fu,Hui Yang,Yun Chen,Yingrui Shi
Background: Breast cancer-related depression (BCRD) is strongly associated with BC and increases recurrence and mortality. This study investigated the role of kaempferol in the pathogenesis of BCRD and its underlying mechanism. Methods: 4T1 mouse BC cells were treated with corticosterone (Cort) in vitro to develop a neuronal injury model, and a BCRD mouse model was established by injecting 4T1 cells and Cort. The effects of kaempferol on 4T1 cells and BCRD models were measured by behavioral tests, Cell Counting Kit-8 assay, wound healing assay, colony formation assay, Western blot analysis, quantitative real-time PCR, hematoxylin and eosin staining, enzyme-linked immunosorbent assay, and immunofluorescence. BCRD cells were transfected with the cyclo-oxygenase-2 (COX-2) overexpression plasmid to study the role of the COX-2/prostaglandin E2 (PGE2) axis in the anti-BCRD activity of kaempferol. The connection between kaempferol and COX-2 was analyzed by molecular docking. Results: Kaempferol reduced the viability, migration, and clones of 4T1 cells and inhibited BC growth and depression-like behavior in mice. Kaempferol alleviated inflammation in BCRD, decreased interleukin 1 beta (IL-1β) and IL-6 levels, and increased transforming growth factor beta 1 (TGF-β1) and IL-10 levels. In addition, kaempferol elevated the levels of serotonin, dopamine, and norepinephrine and the amount of 5-Bromo-2′-deoxyuridine/neuronal nuclei-positive cells. Kaempferol downregulated COX-2 and PGE2, and kaempferol could dock with the protein structure of COX-2. Overexpression of COX-2 reduced BCRD viability, upregulated IL-1β and IL-6 levels, and downregulated TGF-β1 and IL-10 expression. Overexpression of COX-2 reversed the protective effects of kaempferol. Conclusion: Kaempferol exerted anti-BCRD effects, at least in part by inhibiting the COX-2/PGE2 pathway, which regulates neuroinflammation, neurotransmitter imbalance, and defective neurogenesis. Therefore, kaempferol may be a promising candidate active ingredient for treating BCRD.
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FUEL
·
2023
·
IF 7.4
Fangfang Shang,Zhuo Li,Hendao Quan,Xiaoxun Ma
Constructing electrode-electrolyte interphase and enhancing wettability between separator and electrolyte are vital to electrochemical performances of Lithium-metal batteries, especially for suppressing the growth of Li dendrites. In this work, 2-Trifluoroacetyl furan is developed as the multifunctional additive to inhibit Li dendrite growth, and then enhance the cycling time and rate performance of Li||LiNi 0.6 Co 0.2 Mn 0.2 O 2 (NCM622) cells. TFFE additive can enhance the Li ion flowing efficiency by improving wettability between separator and electrolyte and providing more channel of Li ions. Furthermore, TFFE can not only form solid electrolyte interphase (SEI) on the surface of Li anode, but also forms cathode electrolyte interphase (CEI) on the surface of NCM622 electrode. Finally, TFFE could stabilize the LiPF 6 -based electrolyte by removing hydrogen fluoride (HF) and H 2 O, protecting the generated SEI/CEI layer. As a result, introducing 1.0 wt% TFFE additive, the Li||Li symmetric cells could achieve stable cycling for 780 h at 0.5 mA cm −2 , which is higher than that in baseline electrolyte (350 h). And, Li||NCM622 cells in the 1.0 wt% TFFE-contained electrolyte displays remarkably enhanced capacity of 90 % almost after 200 cycles.
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BIOCHEMICAL PHARMACOLOGY
·
2023
·
IF 5.8
Luomin Lin,Yuwei Huang,Jinyi Wang,Xiaocao Guo,Fangjun Yu,Di He,Chuanbin Wu,Lianxia Guo,Baojian Wu
CYP2A5 , an enzyme responsible for metabolism of diverse drugs, displays circadian rhythms in its expression and activity. However, the underlying mechanisms are not fully established. Here we aimed to investigate a potential role of CRY1/2 (circadian clock modulators) in circadian regulation of hepatic CYP2A5. Regulatory effects of CRY1/2 on CYP2A5 were determined using Cry1 -null and Cry2 -null mice, and validated using AML-12, Hepa1-6 and HepG2 cells. CYP2A5 activities both in vivo and in vitro were assessed using coumarin 7-hydroxylation as a probe reaction. mRNA and protein levels were detected by qPCR and western blotting , respectively. Regulatory mechanism was studied using a combination of luciferase reporter assays, chromatin immunoprecipitation (ChIP) and co-immunoprecipitation (Co-IP). We found that ablation of Cry1 or Cry2 in mice reduced hepatic CYP2A5 expression (at both mRNA and protein levels) and blunted its diurnal rhythms. Consistently, these knockouts showed decreased CYP2A5 activity (characterised by coumarin 7-hydroxylation) and a loss of its time-dependency, as well as exacerbated coumarin-induced hepatotoxicity. Cell-based assays confirmed that CRY1/2 positively regulated CYP2A5 expression and rhythms. Based on combined luciferase reporter, ChIP and Co-IP assays, we unraveled that CRY1/2 interacted with E4BP4 protein to repress its inhibitory effect on Cyp2a5 transcription and expression . In conclusion, CRY1/2 regulate rhythmic CYP2A5 in mouse liver through repression of E4BP4. These findings advance our understanding of circadian regulation of drug metabolism and pharmacokinetics .
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MOLECULES
·
2023
·Vol. 28
·期 19
·6777
·
IF 4.6
Zhaoyu Zhang,Yurong Zhao,Zhang Hu,Zhenyu Si,Ziming Yang
The widespread prevalence of infectious bacteria is one of the greatest threats to public health, and consequently, there is an urgent need for efficient and broad-spectrum antibacterial materials that are antibiotic-free. In this study, 2-pyridinecarboxaldehyde (PCA) was grafted onto chitosan (CS) and the modified CS coordinated with silver ions to prepare PCA-CS-Ag complexes with antibacterial activity. To obtain complexes with a high silver content, the preparation process was optimized using single-factor experiments and response surface methodology. Under the optimal preparation conditions (an additional amount of silver nitrate (58 mg), a solution pH of 3.9, and a reaction temperature of 69 °C), the silver content of the PCA-CS-Ag complex reached 13.27 mg/g. The structure of the PCA-CS-Ag complex was subsequently verified using ultraviolet–visible spectroscopy, Fourier-transform infrared spectroscopy, proton nuclear magnetic resonance spectroscopy, and thermogravimetric analysis. Furthermore, three possible complexation modes of the PCA-CS-Ag complex were proposed using molecular mechanics calculations. The results of the antibacterial assay in vitro showed that the PCA-CS-Ag complex exhibited strong antibacterial activity against both Gram-positive and Gram-negative bacteria, exerting the synergistic antibacterial effect of modified chitosan and silver ions. Therefore, the PCA-CS-Ag complex is expected to be developed as an effective antibacterial material with promising applications in food films, packaging, medical dressings, and other fields.Keywords:modified chitosan;silver;complex;response surface methodology;antibacterial
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
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2023
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IF 5.2
Yin Xie,Xiaowei Xu,Yan Cui,Liang Qiao,Kebin Chi,Dejun Shi,Yang Bai,Zhijie Wu,Shengbao He
Solvent is vital in determining the colloidal chemistry of perovskite ink. A depth understanding on the colloidal chemistry is essential to fine-regulate the crystallization of perovskite film. A low-polar solvent, 2-methoxyethanol (2-Me), shows growing potential than the traditional high-polar solvents in scaling-up perovskite solar cells, owing to the fast evaporation rate and the ability to form perovskite films without anti-solvent. However, as a relatively new solvent, the colloidal chemistry has not been fully understood. Here, the colloidal chemistry of fresh and aged perovskite ink using 2-Me as the solvent is investigated. The as-composed perovskite ink is characteristic of weakly bonded I - ions and the existence of cluster complexes. In the fresh perovskite ink, the weakly bonded I - ions enhance the dissolution of methylammonium (MA + ), and also induce the formation of I 3 - ions in the diluted or aged solution. Both iodoplumbate species and cluster complexes are dispersed by MA + ions in the solution, however, the former transforms to clusters after aging. These changes results in increased crystal size and non-uniform coverage in the perovskite film. These findings provide valuable insights into the optimization of perovskite ink using 2-Me as the solvent.
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Molecular Catalysis
·
2021
·
IF 5.062
Yue Zhang,Zhiyong Pan,Nan Wang,Li Wang
Silica SBA-15 without removal of template P123 was calcined in an inert atmosphere and the carbon-modified SBA-15 thus obtained was used as the support of Pd catalyst for the hydrogenation of 2-ethylanthraquinone (EAQ). The effects of extraction times of P123 in SBA-15 with water prior to inert calcination and calcination temperature on the structure and catalytic performance of Pd catalyst were studied. The results of elemental analysis, X-ray diffraction, X-ray photoelectron spectroscopy, inductively coupled plasma, Fourier transform infrared spectroscopy, Raman spectra, water contact angle measurement, N 2 adsorption-desorption, transmission electron microscopy and energy dispersive X-ray mapping showed that carbon content of catalysts varied in the range of 3.4 % and 1.1 % with increasing extraction times from 0 to 6 due to the decrease in the residual amount of P123 in uncalcined SBA-15. With rising calcination temperature, the occurrence state of carbon in catalysts was converted from amorphism into graphite. The Pd catalyst supported on SBA-15 extracted for 3 times and calcined at 650 °C had 2.0 % carbon, and exhibited the highest activity (0.37 molH 2 ·gPd −1 ·min −1 ) and selectivity (98.9 %). This is due to the presence of appropriate amount of carbon, which provided a relatively high hydrophobicity without significantly reducing the specific surface area and pore size of SBA-15 support. The high hydrophobicity benefits the adsorption of EAQ from the working solution to the surface of catalyst.
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ELECTROCHIMICA ACTA
·
2021
·
IF 6.901
Xiaofei Miao,Xiangxin Zhang,Sujing Chen,Yongchuan Liu,Yuanqiang Chen,Junhong Lin,Qi Chen,Yining Zhang
For improving the energy density of carbon-based supercapacitors, the highly reversible redox mediators with giant pseudocapacitance have been studied extensively. In this work, the dual-redox combination of sodium anthraquinone-2-sulfonate (AQS) and potassium bromide (KBr) is introduced into the carbon-based supercapacitors to enhance the electrochemical performances. In the dual-redox enhanced supercapacitors (DRESc), the performances of negative and positive electrodes are improved by AQS and KBr, respectively. In order to use AQS and KBr rationally and effectively, two different approaches are studied: (I) redox mediators are adsorbed in the electrodes; (II) redox mediators are added into the electrolyte. The experimental results demonstrate that the combination of adsorbing AQS onto the negative electrode (the approach I) and adding KBr in the electrolyte (the approach II) is the best approach. Furthermore, electrochemical results prove that it is an optimal choice to adsorb 3 mg AQS for the negative electrode in this work. Meanwhile, to match the AQS-enhanced negative electrode, synchronous potential measurements indicate that the optimal choice for the positive electrode is adding 1.5 M KBr in the 1 M H 2 SO 4 electrolyte. Finally, the DRESc achieved a maximum gravimetric energy density (E G ) of 32.05 Wh kg −1 at 0.5 A g −1 and a maximum gravimetric power density (P G ) of 2200 W kg −1 at 8 A g −1 , implying that the AQS-Br dual-redox system is a promising candidate for energy storage and conversion.
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NANO LETTERS
·
2021
·
IF 11.189
Hua Kang,Xuejun Wang,Mingquan Guo,Changhao Dai,Renzhong Chen,Lei Yang,Yanling Wu,Tianlei Ying,Zhaoqin Zhu,Dapeng Wei,Yunqi Liu,Dacheng Wei
The fast spread of SARS-CoV-2 has severely threatened the public health. Establishing a sensitive method for SARS-CoV-2 detection is of great significance to contain the worldwide pandemic. Here, we develop a graphene field-effect transistor (g-FET) biosensor and realize ultrasensitive SARS-CoV-2 antibody detection with a limit of detection (LoD) down to 10–18 M (equivalent to 10–16 g mL–1) level. The g-FETs are modified with spike S1 proteins, and the SARS-CoV-2 antibody biorecognition events occur in the vicinity of the graphene surface, yielding an LoD of ∼150 antibodies in 100 μL full serum, which is the lowest LoD value of antibody detection. The diagnoses time is down to 2 min for detecting clinical serum samples. As such, the g-FETs leverage rapid and precise SARS-CoV-2 screening and also hold great promise in prevention and control of other epidemic outbreaks in the future.
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2021
·
IF 3.981
Xiuting He,Zhongcheng Cao,Nuannuan Li,Liuxiang Chu,Jiazhen Wang,Chunyan Zhang,Xiaoyan He,Xiaoyan Lu,Kaoxiang Sun,Qingguo Meng
7-Ethyl-10-hydroxycamptothecin (SN-38)-loaded polyethylene glycol-GPLGVRG-poly β-benzyl- l -aspartic acid (PEG-GPLGVRG-PBLA) self-assemblies were successfully prepared using a classical nanoprecipitation method to give an enzyme-responsive nano-drug delivery system. The PEG-GPLGVRG-PBLA/SN-38 self-assemblies were characterized by transmission electron microscopy , dynamic light scattering , and high-performance liquid chromatography. The encapsulation efficiency was 91.7 ± 1.21% and the drug loading was 16.6 ± 0.93%. The 12 h in vitro release of SN-38 from PEG-GPLGVRG-PBLA/SN-38 treated with MMP-2 was 73.2 ± 2.05%, which was significantly higher than that for the group without MMP-2, demonstrating the enzyme-responsiveness of the nano-drug delivery system. In addition, the cellular uptake and tumor accumulation of PEG-GPLGVRG-PBLA were better than those of PEG-PBLA, and the blank PEG-GPLGVRG-PBLA showed high biocompatibility . These findings indicate that the enzyme-responsive nano SN-38 delivery system could provide new opportunities in tumor therapy.
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SEPARATION AND PURIFICATION TECHNOLOGY
·
2021
·
IF 7.312
Jia Deng,Xiang Zhan,Feng Wu,Shuxian Gao,Li-Zhi Huang
Trichloroethylene (TCE), one of the most frequently detected chlorinated organic pollutants (COPs) in groundwater, has potential risks to human health. The bimetallic system consisting of zero-valent iron (ZVI) and a second catalytic metal has been widely investigated for reductive dechlorination of COPs. However, the passivation layer of ZVI inhibits the electron transfer causing a low dechlorination efficiency. In this work, we designed a novel bimetallic system using Fe(OH) 2 and Ni for fast dechlorination of TCE. The reduction efficiency of TCE reaches 94.8 % after 5 h of reaction in the Fe(OH) 2 /Ni system. TCE was completely dechlorinated to nontoxic gas products including ethylene and ethane, which was attributed to the generation of active hydrogen species (H*) in the system. The Ni 2+ cations undergo the process of hydroxylation and olation. Subsequently, electrons of Fe(OH) 2 were transferred to Ni(II) causing the formation of Ni(0). The catalytic Ni(0) sites generate H* for TCE dechlorination via catalytic reduction of H 2 O/H + . A part of Fe(II) in the Fe hydroxide layer of Fe(OH) 2 was oxidized to Fe(III) leading to the formation of green rust with a hexagonal structure. Our work demonstrates Fe(OH) 2 /Ni is a promising composite material for the remediation of TCE-contaminated groundwater.
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BIOSENSORS & BIOELECTRONICS
·
2021
·
IF 10.618
Ying Peng,Yanhong Pan,Zhaowei Sun,Jinlong Li,Yongxiang Yi,Jie Yang,Genxi Li
The pandemic of coronavirus disease 2019 (COVID-19) caused by the severe acute respiratory syndrome-coronavirus-2 (SARS-CoV-2) is continuously worsening globally, herein we have proposed an electrochemical biosensor for the sensitive monitoring of SARS-CoV-2 RNA. The presence of target RNA firstly triggers the catalytic hairpin assembly circuit and then initiates terminal deoxynucleotidyl transferase-mediated DNA polymerization. Consequently, a large number of long single-stranded DNA products can be produced, and these negatively charged DNA products will bind a massive of positively charged electroactive molecular of Ru(NH 3 ) 6 3+ due to the electrostatic adsorption. Therefore, significantly amplified electrochemical signals can be generated for sensitive analysis of SARS-CoV-2 RNA in the range of 0.1–1000 pM with the detection limit as low as 26 fM. Besides the excellent distinguishing ability for SARS-CoV-2 RNA against single-base mismatched RNA, the proposed biosensor can also be successfully applied to complex matrices, as well as clinical patient samples with high stability, which shows great prospects of clinical application.
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