Materials Express
·
2023
·Vol. 13
·期 8
·1339-1345
·
IF 0.7
Liao Wanrong,Fang Wang,Xu Juan
Lung cancer is a common malignancy of the respiratory system with a high morbidity and mortality. We intended to identify the apoptosis-promoting role of tripterine in lung cancer. Lung cancer SPC-A-1 cells were exposed to low, moderate, and high dosage of tripterine (2, 5 and 10 μmol/L)
with the model group not being intervened. After treatment, the role of tripterine in SPC-A-1 cell apoptosis was observed. In addition, lung cancer cells were transfected with TNF-α mimic (pc-TNF-α group) and TNF-α inhibitor (si-TNF-α group).
Tripterine +pc-TNF-α group was set up to determine the interaction between tripterine and TNF-α. The cell survival rate, TNF-α and Caspase-3 expression levels then were detected by MTT and flow cytometry. Tripteryglide treatment dose-dependently decreased
lung cancer cell viability and induced cell apoptosis, resulting in an increase of TNF-α expression. However, when TNF-α expression was inhibited upon transfection, SPC-A-1 cell apoptosis was suppressed. TNF-α mimics activated apoptosis and up-regulated
Caspase-3 expression. Combination of tripteryglide and TNF-α mimics more significantly elevated apoptotic rate of lung cancer cells when elevating the content of Caspase-3. SPC-A-1 cells are highly sensitive to TNF-α and TNF-α significantly increases
the activity and expression of Caspase-3. Tripteryglide can up-regulate TNF-α expression to facilitate lung cancer cell apoptosis and increase Caspase-3 expression.
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EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
·
2021
·
IF 4.384
Wenyan Li,Zheng Jiao,Yanhui Liu,Jiacheng Yao,Guodong Li,Jing Dong
Biapenem is a carbapenem antibiotic. It is excreted predominantly through the kidney as unchanged forms. However, the molecular mechanism of renal excretion of biapenem and potential drug-drug interactions (DDIs) were still unknown. In the present study, the role of organic anion transporters (OAT) 1/3 and organic cation transporters (OCT) 2 in the renal excretion of biapenem, and the potential DDIs between biapenem and six clinical commonly prescribed antibiotics and antiviral drugs that acted as substrates or inhibitors of OAT3 were evaluated in vitro . Further, the effect of probenecid on the pharmacokinetics of biapenem was explored in the rats. We observed that biapenem could not inhibit the transport activities of OAT1 or OCT2, while mildly inhibited OAT3 (IC 50 >500 μM). Among the tested antibiotics and antiviral drugs, the relatively high DDI index values (maximal unbound plasma concentration over IC 50 , I max,u /IC 50 ) were found for piperacillin, linezolid and benzylpenicillin, which were 2.84, 1.7 and 0.62, respectively. Although probenecid had the highest DDI index (27.1) in vitro , no significant impact of it on the pharmacokinetics of biapenem was observed in the rats. Our results indicated that biapenem was primarily eliminated by the glomerular filtration, while OAT3-mediated renal tubular secretion was a minor route. Biapenem is not a clinically relevant substrate or inhibitor because of its low affinity to OAT3. According to current results, it would be safe to use biapenem with other antibiotics and antiviral drugs that acted as substrates or inhibitors of OAT3.
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CELLULAR AND MOLECULAR BIOLOGY
·
2023
·Vol. 69
·期 9
·
IF 1.6
Aili Xuan,Mei Yang,Qun Xia,Qian Sun
Asthma is a respiratory inflammatory disease, and nicotinamide adenine dinucleotide phosphate oxidase 4 (NOX4) is involved in the progression of respiratory diseases. However, the role of NOX4 in asthma remains unclear. In the present study, we aimed to explore the effects of NOX4 on airway remodeling and inflammation. NOX4 expression was measured using immunocytochemistry (IHC), western blot, and real-time PCR (qPCR). Lung tissues were stained using the H&E assay. ELISA was used to examine the levels of airway remodeling-related indicators, and qPCR was used to detect airway inflammatory factors. The results indicated that NOX4 is highly expressed in lung tissues, bronchoalveolar lavage fluid (BALF), and serum of OVA-treated mice. Inhibition of NOX4 alleviated OVA-induced airway remodeling and inflammation. Similarly, TGF-β1 was also upregulated in BALF and serum OVA-induced mice. Inhibition of TGF-β1 signaling also improved airway remodeling and inflammation induced by OVA. Moreover, the downregulation of NOX4 inactivated the TGF-β1-Smad2/3 pathway, and TGF-β1 decreased Smad2/3 expression. Moreover, inhibition of the TGF-β1 was enhanced, while TGF-β1 reversed the effects on airway remodeling and inflammation induced by NOX4 inhibition. Taken together, the downregulation of NOX4 improves airway remodeling and inflammation via inactivation of the TGF-β1-Smad2/3 pathway in asthma mice, suggesting that NOX4 may be a therapeutic target for asthma.
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Algal Research-Biomass Biofuels and Bioproducts
·
2020
·
IF 4.008
Xiaodan Wang,Yanan Song,Baoling Liu,Wei Hang,Renjian Li,Hongli Cui,Runzhi Li,Xiaoyun Jia
The objective of this study is to characterize effects of autophagy inhibition by 3-methyladenine on astaxanthin and fatty acid accumulation in Haematococcus pluvialis cultivated under high light condition. The present data show that 0.02 mM 3-methyladenine treatment effectively inhibited autophagosome formation but no impact on the cell growth and biomass of H. pluvialis , leading to a large increase in cellular reactive oxygen species (ROS), astaxanthin and fatty acid accumulation as well as palmitic acid enrichment under high light of 700 μmol·m −2 ·s −1 . Furthermore, the key genes such as phytoene synthase ( PSY ), β-carotene ketolase ( CRTO ), and β-carotene hydroxylase ( CRTR-b ) in astaxanthin pathway are upregulated significantly whereas the expressions of the lipid-related genes biotin carboxylase ( BC ) and diacylglycerol acyltransferase ( HpDGAT2D ) just increased slightly in the 3-methyladenine-treated cells. Astaxanthin accumulation is not perfectly linear with fatty acid biosynthesis in H. pluvialis treated by 3-methyladenine under high light. Overall, autophagy might function importantly in astaxanthin and lipid enrichment in H. pluvialis under stress condition. The findings provide new insights to further investigation on the metabolic regulation in microalgae .
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Anti-Cancer Agents in Medicinal Chemistry
·
2022
·Vol. 22
·期 17
·3009-3024
·
IF 2.527
Zhu Yuting,Wang Huai,Yu Mingjun,Li Chao,Meng Xiaoming,He Meng,Yao Risheng
Background: GRPR is over-expressed in cancer cells and is a potential drug target for the treatment of cancer. PD176252, as the most representative non-peptide inhibitor of GRPR, can inhibit the growth of cancer cells, but its low selectivity to cancer cells and normal cells limits
its further application. Objective: The aim of this study was to design and synthesize novel GRPR inhibitor with stronger anti-cancer activity and higher affinity with GRPR than the lead compound PD176252. Methods: A series of 1, 3, 4-oxadiazole derivatives as PD176252 analogues
(4a-4j, 6a-6q) were synthesized and their cytotoxic activity was investigated on four cancer lines with high expression of GRPR (gastric (HGC-27), colon (HCT- 116), prostate (PC-3), and lung (A549)) and one human cell line (gastric mucosal epithelial (GES-1)) by MTT assay. Flow cytometry analysis
and Western Blot were used to determine whether the compound induced programmed apoptosis of cancer cells. Competitive binding experiment was used to verify the affinity between GRPR and the optimal compound. Results: Compound 6m exhibited significant growth inhibition on all tested cancer
cell lines, especially gastric cancer cells (HGC-27 cellular IC50 0.37 ± 0.04μM). Also, the selectivity of 6m to HGC-27 was much higher than that of PD176252. Flow cytometric analysis and Western Blot proved that 6m significantly promoted the apoptosis of HGC-
27 cells. Moreover, competitive binding experiment confirmed the close binding of 6m with GRPR, which indicated 6m with a higher affinity than lead compound PD176252. Conclusion: Our results suggested that 6m, as a novel GRPR inhibitor, had a higher affinity with GRPR and potential anti-cancer
effect than PD176252, which can be used as a template for further optimization.
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CHEMICAL ENGINEERING JOURNAL
·
2018
·
IF 6.735
Daoyan Feng,Hui Yang,Xingzhong Guo
3-Dimensional hierarchically porous ZnFe 2 O 4 /C composites with interconnected macropores and co-continuous hollow skeletons are facilely synthesized and used as anode materials for Li-ion batteries. The interconnected macropores impede the agglomeration of primary particles and buffer the volumetric variations, hollow mesoporous skeletons not only improve the interfacial contact area between electrode and electrolyte but also facilitate lithium ions transfer rate. Moreover, N-doped carbon layer further enhances the conductivity and mechanical strength of skeletons, as well as accelerates electron transfer during repeated discharge and charge process. The as-prepared 3-dimensional hierarchically porous ZnFe 2 O 4 /C composites possess excellent Li-ion storage properties, delivering a high reversible capacity of 972 mAh g −1 at 200 mA g −1 after 100 cycles and a decent specific capacity of 711 mAh g −1 even at a large current density of 1000 mA g −1 after 400 cycles. These values are among the highest reported for ZnFe 2 O 4 -based materials with different morphologies and nanostructures. The resultant ZnFe 2 O 4 /C composites display the potential practical application for high-performance Li-ion batteries.
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ChemSusChem
·
2022
·Vol. 15
·期 19
·e202201121
·
IF 9.14
Dong Yan,Shuhao Xiao,Xinyan Li,Rui Wu,Jinxia Jiang,Xiaobin Niu,Jun Song Chen
Graphical Balancing act : Boron-doped Na 3 V 2 (PO 4 ) 3 is synthesized through a facile electrospinning method. NVP@carbon with a balanced content of BCO 2 and BC 2 O exhibits the best sodium storage properties. BC 2 O mainly improves the sodium diffusion and BCO 2 enhances the structural stability. Na 3 V 2 (PO 4 ) 3 (NVP) is a widely studied cathode material for sodium-ion batteries because of its high ionic conductivity and attractive charge/discharge plateau (3.4 V vs. Na/Na + ). However, its poor electronic conductivity and severe volume expansion during sodium storage need to be addressed before its intensive application could be realized. Herein, boron-doped NVP was synthesized through a facile electrospinning method. By adding boric acid into the reaction mixture during electrospinning followed by carbonization, boron could be directly inserted into the carbon matrix, giving rise to B-doped carbon nanofiber wrapped NVP. By tuning the doping amount, the boron-containing configurations could be facilely manipulated, playing different roles in promoting the sodium storage properties of the composite. Based on the calculation results, BC 2 O enhanced sodium diffusion by lowering the energy barrier, while BCO 2 improved the structural stability. Due to these specific functionalities of the configurations, the as-prepared composite with a balanced amount of BC 2 O and BCO 2 demonstrated superior sodium storage capacity of 113 mAh g −1 at 1 C, outstanding long cycling performance of 103 mAh g −1 at 10 C, and retained 91 mAh g −1 after 1500 cycles. This gave rise to a capacity loss of only 0.08‰ per cycle, much better than the undoped counterpart.
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ADVANCED POWDER TECHNOLOGY
·
2020
·
IF 4.217
Weiwen Meng,Cong Li,Meng Yao,Zhangxing He,Xianwen Wu,Zhen Jiang,Lei Dai,Ling Wang
Aqueous lithium ion batteries (ALIBs) exhibit great application prospects in energy storage system, and the anode materials is the key to the extensive development of ALIBs. In this study, Li 1+x Ti 2−x Fe x (PO 4 ) 3 /C (x = 0, 0.05, 0.10, 0.30) composites as anode for ALIBs were synthesized via sol-gel method. The effect of Fe doping on LiTi 2 (PO 4 ) 3 /C properties was assessed by electrochemical measurements. In all of these composites, Li 1.1 Ti 1.9 Fe 0.1 (PO 4 ) 3 /C (LCF-10) presents the best electrochemical properties. LCF-10 exhibits discharge capacity with 120.0 and 80.2 mAh g −1 at 0.5 and 15C, severally, increasing by 1.2 and 1.3 times compared with the original LiTi 2 (PO 4 ) 3 /C. Besides, LCF-10 demonstrates remarkable cycling performance, whose discharge capacity retention can keep 70.2% at 5 C for 1000 cycles. Our study demonstrates that Fe doping for LiTi 2 (PO 4 ) 3 lattice can efficiently enhance electrochemical properties of LiTi 2 (PO 4 ) 3 /C composite.
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JOURNAL OF ALLOYS AND COMPOUNDS
·
2022
·
IF 6.371
Xiangchao Zhao,Yuansong Luo,Xiujian Zhao
NASICON-type solid electrolyte Li 1.3 Al 0.3 Ti 1.7 (PO 4 ) 3 (LATP) has become an excellent substitute for organic liquid electrolytes due to its high ionic conductivity and exceptional air stability. However, its application is limited by its poor sintering characteristics and high grain boundary resistance. In this study, TeO 2 was introduced into LATP as a sintering aid to promote its sintering, and its properties were measured by XRD , SEM, XPS, EIS and dilatometry . The results show that the addition of TeO 2 can form eutectic liquid phase in LATP ceramic pellets during sintering, thus effectively promoting particle sintering. Not only the grain size was greatly increased, but also grain boundary and pore defects were reduced. With the help of TeO 2 , the performance of LATP is greatly improved when sintered at only 750 °C, the relative density and total ionic conductivity reached 90.64% and 0.207 mS/cm, respectively. The highest total ionic conductivity of 0.279 mS/cm and the highest relative density of 93.81% were obtained when sintered at 800 ℃ and 950 ℃, respectively. However, due to the volatilization of Li and Te at high temperature, the relative density and total ionic conductivity of LATP with TeO 2 added sintered at high temperature have only a small increase compared to that without addition. In conclusion, this study provides a feasible scheme for improving LATP performance.
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ACS Applied Materials & Interfaces
·
2012
·
IF 4.525
Bo Yuan,Qiang Chen,Wen-Quan Ding,Ping-Sheng Liu,Shi-Shan Wu,Si-Cong Lin,Jian Shen,Yue Gai
AB diblock copolymers comprised of poly(2-methacryloyloxyethyl phosphorylcholine) (PMPC) and poly(3-methacryloxypropyl trimethoxysilane) (PMTSi) segments, which are used for biocompatible coatings, were investigated. Block copolymers with various compositions were synthesized by atomic transfer radical polymerization (ATRP). The obtained copolymers were dissolved in an ethanol solution, and dynamic light scattering showed that all block copolymers were capable of existing as micelles. After a convenient “one-step” reaction, the cellulose membranes could be covalently modified by these copolymers with stable chemical bonds (C–O–Si and Si–O–Si). Block copolymers with different PMPC chain length were applied to surface modification to find the most suitable copolymer. The functional MPC density can be controlled by adjusting the ratio of the two monomers (MPC and MTSi), which also affect surface properties, including the surface contact angle, surface morphology, and number of functional PC groups. The low-fouling properties were measured by protein adsorption, platelet adhesion and activation, and cell adhesion. Protein adsorption of bovine serum albumin (BSA), fibrinogen, and human plasma were also tested and a moderate monomer composite was attained. The protein adsorption behavior on the novel interfaces depends both on MPC density and PMPC chain length. Platelet adhesion and activation were reduced on all the modified surfaces. The adhesion of Human Embryonic Kidney 293 (293T) cells on the coated surfaces also decreased.
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mSystems
·
2020
·
IF 6.633
Yougui Li,Wenyi Xu,Fang Zhang,Shi Zhong,Yuqing Sun,Jinxi Huo,Jianxun Zhu,Chongming Wu
Hyperlipidemia is a worldwide epidemic with an obvious gender disparity in incidence. Modulations on gut microbiota by traditional Chinese medicines (TCM) are emerging as a potential rationale governing the profitable effects of drugs on hyperlipidemia. However, it is unclear how gut microbes regulate the progression of hyperlipidemia. Here, we found that mulberry leaf extract (MLE) and its active component 1-deoxynojirimycin (DNJ) diminished hyperglycemia and hypertriglyceridemia with similar efficacy in male and female mice but preferentially alleviated hypercholesterolemia in female mice. Further investigations showed that DNJ sex-specifically downregulated the expression of lipogenic genes, especially cholesterol-biosynthetic genes. Oral administration of DNJ imposed more profound modulation on gut microbiota in female mice than in male ones, as estimated by 16S rRNA metatranscriptomic analysis. DNJ markedly enriched Akkermansia and Clostridium group XIVa and promoted the production of indole-3-propionic acid (IPA) in a sexually dimorphic way. Importantly, IPA tightly associates with the antihyperlipidemic effect of DNJ and exhibited a potent lipid-lowering effect both in vitro and in vivo. Together, our results have established a regulatory mechanism by which DNJ sex-specifically improves hyperlipidemia, offering an in-depth theoretical basis for therapeutic exploitation of DNJ as a sex-specific intervention against hyperlipidemia.IMPORTANCE Hyperlipidemia has been intensively focused on by researchers around the world owing to its major contribution to cardiovascular diseases. Various evidence reveals that women are more susceptible than male counterparts to dyslipidemia, making sex-dependent therapeutic strategies and drugs urgently needed. In the present work, we demonstrate that DNJ, the main active component of mulberry leaves, exerts an obvious female-preferential antihyperlipidemic effect through specifically enriching Akkermansia and Clostridium XIVa and elevating an active microbial metabolite, indole-3-propionic acid (IPA), in female mice. Moreover, we have corroborated the potent lipid-lowering efficacy of IPA both in vitro and in vivo. These findings not only indicate a potential mechanism by which gut microbes and their metabolites confer the beneficial role of DNJ in ameliorating hyperlipidemia but also provide an in-depth theoretical basis for therapeutic exploitation of DNJ as a female-specific intervention against hyperlipidemia.
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ANALYTICAL CHEMISTRY
·
2014
·
IF 5.825
Rui Li,Kangbing Wu,Changxian Liu,Yin Huang,Yanying Wang,Huaifang Fang,Huijuan Zhang,Chunya Li
A novel ionic liquid, 4-amino-1-(3-mercapto-propyl)-pyridine hexafluorophosphate (AMPPH), was successfully synthesized and characterized. Subsequently, AMPPH was used as a functional monomer to fabricate AMPPH-modified gold nanoparticles (AMPPH–AuNPs) via a one-pot synthesis method. The as-prepared AMPPH–AuNPs were confirmed with transmission electron microscopy and X-ray photoelectron spectroscopy. AMPPH–AuNPs were used to construct a biocompatible interface to immobilize rabbit anti-human IgG (anti-HIgG) onto a glassy carbon electrode (GCE) surface, followed by a cross-linking step with glutaraldehyde to fabricate an anti-HIgG–AMPPH–AuNPs/GCE. The nonspecific binding sites were enclosed with bovine serum albumin (BSA) to develop an immunosensor for human IgG. Electrochemical impedance spectroscopy, cyclic voltammetry and differential pulse voltammetry were used to investigate the electrochemical properties of the developed immunosensor. The results indicate that AMPPH–AuNPs can improve the immunosensing performance. The current response of the immunosensor was found linearly related to human IgG concentration in the range of 0.1–5.0 ng mL–1 and 5.0–100.0 ng mL–1. The detection limit is estimated to be 0.08 ng mL–1 (S/N = 3). The obtained immunosensor was successfully applied to the analysis human IgG immunoglobulin in human serum, and the results were well consistent with ELISA method.
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