EXPERIMENTAL CELL RESEARCH
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2023
·
IF 3.7
Hong Liu,Yang Huang,Jing Yang,Xuejiao Xu,Qiaomei Dai,Yuwei Zhang,Li Zhao,Mengdi Zhang,Jing Zhang,Tonghui Liu,Lili Zhong
Estrogens have been demonstrated to inhibit age-related cognitive decline via binding to estrogen receptors (ERs). As a natural flavonoid component of Cuscuta Chinensis Lam. , Kaempferol-3- O -glucoside (K-3-G) not only possesses anti-neuroinflammatory potential but also functions as an agonist for ERα and ERβ. This study aimed to determine whether K-3-G improved cognition during the aging process, with an emphasis on its effect on microglial inflammation. In vivo , K-3-G (5 or 10 mg/kg/day) was orally given to the senescence-accelerated mouse prone 8 (SAMP8) mice from six to eight-month old. In addition to mitigating the memory and learning deficits of SAMP8 mice, K-3-G upregulated the expression of ERα and ERβ in their hippocampal CA1 region, with the higher dose being more effective. Less Iba-1 + microglial cells presented in SAMP8 mice treated with K-3-G. The formation of NLR Family Pyrin Domain Containing 3 (NLRP3) complex, production of pro-inflammatory cytokines and oxidative stress-related markers, as well as expression of pro-apoptotic proteins were reduced by K-3-G. In vitro , BV2 microglial cells exposed to oligomeric amyloid beta (Aβ) 1-42 were treated with 100 μM K-3-G. K-3-G showed similar anti-inflammatory effects on BV2 cells as in vivo . K-3-G-induced alterations were partly diminished by fulvestrant, an ER antagonist. Moreover, dual-luciferase reporter system demonstrated that K-3-G induced ER expression by activating the transcription of estrogen-response elements (EREs). Collectively, these findings demonstrate that K-3-G may be a novel therapeutic agent for senescence-related cognitive impairment by inhibiting microglial inflammation through its action on ERs.
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JOURNAL OF MEDICINAL CHEMISTRY
·
2021
·
IF 7.446
Hong Yao,Giuseppe Uras,Pengfei Zhang,Shengtao Xu,Ying Yin,Jie Liu,Shuai Qin,Xinuo Li,Stephanie Allen,Renren Bai,Qi Gong,Haiyan Zhang,Zheying Zhu,Jinyi Xu
Based on a multitarget strategy, a series of novel tacrine–pyrimidone hybrids were identified for the potential treatment of Alzheimer’s disease (AD). Biological evaluation results demonstrated that these hybrids exhibited significant inhibitory activities toward acetylcholinesterase (AChE) and glycogen synthase kinase 3 (GSK-3). The optimal compound 27g possessed excellent dual AChE/GSK-3 inhibition both in terms of potency and equilibrium (AChE: IC50 = 51.1 nM; GSK-3β: IC50 = 89.3 nM) and displayed significant amelioration on cognitive deficits in scopolamine-induced amnesia mice and efficient reduction against phosphorylation of tau protein on Ser-199 and Ser-396 sites in glyceraldehyde (GA)-stimulated differentiated SH-SY5Y cells. Furthermore, compound 27g exhibited eligible pharmacokinetic properties, good kinase selectivity, and moderate neuroprotection against GA-induced reduction in cell viability and neurite damage in SH-SY5Y-derived neurons. The multifunctional profiles of compound 27g suggest that it deserves further investigation as a promising lead for the prospective treatment of AD.
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高影响因子
MOLECULES
·
2023
·Vol. 28
·期 23
·7823
·
IF 4.6
Ke Deng,Yafei Wang,Lei Wang,Xianli Fan,Zhenyu Wu,Xue Wen,Wen Xie,Hong Wang,Zheng Zhou,Pengfei Chen,Xianggui Chen
Phase transition behaviors of poly(N-isopropylacrylamide) nanogels with different compositions induced by (−)-epigallocatechin-3-gallate (EGCG) and ethyl gallate (EG) has been investigated systematically. Monodisperse poly(N-isopropylacrylamide-co-N-hydroxymethyl acrylamide) (P(NIPAM-co-NMAM)) and poly(N-isopropylacrylamide-co-2-hydroxyethyl methacrylate) (P(NIPAM-co-HEMA)) nanogels with different feeding monomer ratios were prepared by emulsion polymerization. P(NIPAM-co-NMAM) nanogels exhibit rapid isothermal phase transition behavior in EGCG solutions with low concentration (10−3mol/L) in less than 10 minutes. The thermosensitive phase transition behaviors of nanogels are affected not only by the copolymerized monomers but also by the concentrations of EGCG and EG in aqueous solutions. Nanogels remain in a shrunken state and do not exhibit thermosensitive phase transition behaviors in EGCG solutions (≥5 mmol/L), whereas they display thermo-responsive phase transition behaviors in EG solutions. The volume phase transition temperature (VPTT) shifts to lower temperatures with increasing EG concentration. The diameters of P(NIPAM-co-NMAM) nanogels decrease with increasing EG concentration at temperatures between 29 and 33 °C. In contrast, the diameters of P(NIPAM-co-HEMA) nanogels increase with increasing EGCG concentration at temperatures between 37 and 45 °C. The results demonstrate the potential of nanogels for simple detection of EG and EGCG concentrations in aqueous solutions over a wide temperature range, and EGCG can serve as a signal for the burst-release of drugs from the P(NIPAM-co-NMAM)-based carriers at physiological temperature.Keywords:thermo-responsive nanogel;poly(N-isopropylacrylamide-co-N-hydroxymethyl acrylamide);poly(N-isopropylacrylamide-co-2-hydroxyethyl methacrylate);(−)-epigallocatechin-3-gallate;phase transition
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CERAMICS INTERNATIONAL
·
2023
·
IF 5.2
Teng Su,Huanle Chen,Zhiyang Wei,Mingyuan Hao,Xiaodong Wang,Yufeng Liu,Chao Ma,Yang Miao,Feng Gao
In this study, based on the highly disordered multi-component system with high-entropy and traditional perovskite with high dielectric constant, a series of the Al 3+ -doped high-entropy perovskite (Zn 1/6 Ba 1/6 Ca 1/6 Sr 1/6 La 1/3 )Ti 1-x Al x O 3 (0 ≤ x ≤ 0.1) ceramics was designed and synthesized by using a solid state reaction method to explore the effects of different doping amounts on microwave dielectric characteristics together with the microstructures. The single-phase structure in space group Pm-3m was determined in the sintering temperature range of 1325 °C–1400 °C and both had high dielectric constant (from 74.46 to 93.44). With the increase of Al doping amount, the variation trend of dielectric constant was closely related to the density and ionic polarizability. The Q × f value of doped samples was higher than that of undoped samples, which was mainly due to the interaction of oxygen vacancy content and grain size. Due to the high-entropy effect resulting in [Ti-O6] octahedral torsion, the τ f value was greatly reduced compared with traditional perovskite, which exhibited outstanding microwave dielectric properties (ε r = 74.46, Q × f = 4108 GHz at 4.31 GHz, and τ f = +184 ppm/°C). The present work provided an effective approach to improve the properties of microwave dielectric ceramics .
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ANALYST
·
2023
·
IF 4.2
Yueyuan Zhuang,Han Dong,Tianqing Liu,Yongmei Zhao,Yan Xu,Xiaojuan Zhao,Dan Sun
Caspase-3 is an important biomarker for the process of apoptosis, which is a key target for cancer treatment. Due to its low concentration in single cells and the structural similarity of caspase family proteins, it is exceedingly challenging to accurately determine the intracellular caspase-3 during apoptosis in situ. Herein, a biosensing strategy based on the target-induced SERS “hot spot” formation has been developed for the simultaneous highly sensitive and selective detection of intracellular caspase-3 level. The nanosensor is composed of gold nanoparticles modified with the probe molecule 4-mercaptophenylboronic acid (4-MPBA) and a peptide chain. The well-designed peptide chain contains two distinct functional domains, one with a sulfhydryl group for bonding to the gold nanoparticles and the other a fragment specifically recognized by caspase-3. When caspase-3 is present, the negatively charged segment (NH2–Asp–Asp–Asp–Glu–Val–Asp–OH) of the peptide chain is specifically hydrolyzed, leaving a positively charged fragment coated on the surface of the gold nanoparticles. At this time, the golden nanoparticles undergo significant coupling aggregation due to the electrostatic interaction, resulting in a large number of SERS “hot spot” formation. The SERS signal of the 4-MPBA located at the nano-gap is significantly boosted because of the local plasma enhancement effect. The highly sensitive determination of caspase-3 can be achieved according to the altered SERS signal intensity of 4-MPBA. The turn-on of the SERS signal-induced target contributes to the excellent selectivity and the formation of the SERS “hot spot” effect that further improves the sensitivity of caspase-3 detection. The advantages of this biosensing technique allow for the precise in situ monitoring of the dynamic changes in caspase-3 levels during apoptosis. In addition, the differences in caspase-3 levels during the apoptosis of various cell types were compared. Monitoring the caspase-3 levels can be used to track the cellular apoptosis process, evaluate the effect of drugs on cancer cells in real time, and provide guidance for the selection of the appropriate drug dosage.
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APPLIED CATALYSIS B-ENVIRONMENTAL
·
2023
·
IF 22.1
Xinlei Ji,Jia Kou,Gökalp Gözaydın,Xi Chen
Chitin biorefinery offers a unique opportunity to sustainably produce highly-valued organonitrogen compounds such as the versatile pharmaceutical precursor 3-acetamido-5-acetylfuran (3A5AF), bypassing the Haber process and mitigating the consumption of fossil feedstocks. However, the reported protocols engaged large quantities of toxic organic solvents and required harsh conditions. In this work, a highly efficient catalytic system has been developed in the nontoxic, biobased γ-valerolactone (GVL) solvent under relatively mild conditions. 3A5AF was selectively obtained with an unprecedent yield of 75.3% at 140 °C for 2 h by adding NH 4 SCN and HCl. The high yielding was exclusively promoted by a dissolution-dehydration effect. Based on the UPLC-TOF-MS and NMR analyses, the presence of NH 4 SCN has induced a very rapid NAG conversion possibly by coordinating with the acetamido group and the hydroxyl groups, and the 3A5AF product was obtained in a subsequent dehydration pathway from NAG with the Chromogen I and Chromogen III as the intermediates.
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ACS Central Science
·
2023
·
IF 18.2
Ruoxi Wang,Yu Wang,Yuting Niu,Danqing He,Shanshan Jin,Zixin Li,Lisha Zhu,Liyuan Chen,Xiaolan Wu,Chengye Ding,Tianhao Wu,Xinmeng Shi,He Zhang,Chang Li,Xin Wang,Zhengwei Xie,Weiran Li,Yan Liu
Maintaining the stemness of bone marrow mesenchymal stem cells (BMMSCs) is crucial for bone homeostasis and regeneration. However, in vitro expansion and bone diseases impair BMMSC stemness, limiting its functionality in bone tissue engineering. Using a deep learning-based efficacy prediction system and bone tissue sequencing, we identify a natural small-molecule compound, dihydroartemisinin (DHA), that maintains BMMSC stemness and enhances bone regeneration. During long-term in vitro expansion, DHA preserves BMMSC stemness characteristics, including its self-renewal ability and unbiased differentiation. In an osteoporosis mouse model, oral administration of DHA restores the femur trabecular structure, bone density, and BMMSC stemness in situ. Mechanistically, DHA maintains BMMSC stemness by promoting histone 3 lysine 9 acetylation via GCN5 activation both in vivo and in vitro. Furthermore, the bone-targeted delivery of DHA by mesoporous silica nanoparticles improves its therapeutic efficacy in osteoporosis. Collectively, DHA could be a promising therapeutic agent for treating osteoporosis by maintaining BMMSC stemness.
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ACS Applied Materials & Interfaces
·
2023
·
IF 9.5
Nitong Bu,Lin Wang,Di Zhang,Huimin Xiao,Xiaoman Liu,Xianrui Chen,Jie Pang,Chen Ma,Ruojun Mu
Biodegradable gelatin (G) food packaging films are in increasing demand as the substitution of petroleum-based preservative materials. However, G packaging films universally suffer from weak hydrophobicity in practical applications. Constructing a hydrophobic micro/nanocoating with low surface energy is an effective countermeasure. However, the poor compatibility with the hydrophilic G substrate often leads to the weak interfacial adhesion and poor durability of the hydrophobic coating. To overcome this obstacle, we used (3-aminopropyl) triethoxysilane (APS) as an interfacial bridging agent to prepare a highly hydrophobic, versatile G nanocomposite film. Specifically, tannic acid (TA)-modified nanohydroxyapatite (n-HA) particles (THA) were introduced in G matrix (G-THA) to improve the mechanical properties. Micro/nanostructure with low surface energy composed of nanozinc oxide (Nano-ZnO)/APS/stearic acid (SA) (NAS) was constructed on the surface of G-THA film (G-THA/NAS) through one-step spray treatment. Consequently, as-prepared G-THA/NAS film presented excellent mechanics (tensile strength: 7.6 MPa, elongation at break: 292.7%), water resistance ability (water contact angle: 150.4°), high UV-shielding (0% transmittance at 200 nm), degradability (100% degradation rate after buried in the natural soil for 15 days), antioxidant (78.8% of 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity), and antimicrobial (inhibition zone against Escherichia coli: 15.0 mm and Staphylococcus aureus: 16.5 mm) properties. It should be emphasized that the bridging function of APS significantly improves the interfacial adhesion ability of the NAS coating with more than 95% remaining area after the cross-cut adhesion test. Meanwhile, the G-THA/NAS film could maintain stable and long-lasting hydrophobic surfaces against UV radiation, high temperature, and abrasion. Based on these multifunctional properties, the G-THA/NAS film was successfully applied as a liquid packaging material. To sum up, we provide a feasible and effective method to prepare high-performance green packaging films.
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ORGANIC PROCESS RESEARCH & DEVELOPMENT
·
2023
·
IF 3.4
Junjie Li,Wei Feng,Shichun Weng,Zichao Guo,Wanghua Chen
3,4-bis(4-Aminofurazano-3-yl) furoxan (DATF) is a key precursor for the high-energy explosive 3,4-bis(4-nitrofurazano-3-yl) furoxan (DNTF), and it is also a high-nitrogen content energetic material. In this paper, the synthesis process of DATF was characterized using the HPLC technique, and the effects of four reaction parameters have been thoroughly studied. The thermal risk analysis for DATF synthesis was conducted with a reaction calorimeter (RC1) and an accelerating rate calorimeter. It was found that extracting the intermediate 3-amino-4-oxycyanofurazan from the aqueous to organic phases was an important way to improve the yield of DATF. Therefore, hydrophobic ethyl acetate was selected as one reaction solvent. The higher yield of DTAF obtained was about 60%. In addition, HPLC monitoring and reaction calorimetry results indicated that the rate of diazotization and decomposition of diazonium salt was feeding-controlled, and the cycloaddition reaction was a slow process. Most of the reaction heat has been released by the diazotization and decomposition of diazonium salt, while the heat effect of cycloaddition was not significant. Thermal stability analysis supported the conclusion that the decomposition of the reaction mixture was hardly possible to be triggered by the reaction heat. The thermal risk of DATF synthesis was low.
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Journal of Analysis and Testing
·
2021
·Vol. 5
·期 4
·387-395
·
IF 0
Zhou Yufeng,Duan Liguang,Huang Yixin,Liu Yaqi,Wang Lijuan,Qiao Xiaoqiang
The amino acids post-modified ionic liquids-based hybrid monolithic columns were successfully developed. For the first step, using 1-vinyl-3-dodecylimidazole bromide (VDI·Br) and polyhedral oligomeric silsesquioxane methacryl substituted (POSS-MA) as monomer and crosslinking agent, the monolithic POSS-VDI matrix material was polymerized in 100 μm capillary. The prepared POSS-VDI column is of ion-exchange/reverse-phase mixed-mode retention characteristics. The column efficiency reached 137,000 N/m for thioureas. The POSS-VDI column has also been successfully applied to recognize and analyze the effective components of Traditional Chinese Medicines Fangji and the Root of Kudzu Vine. Furthermore, based on its good chromatographic performances, in the second step, amino acids l -Proline ( l -Pro), Glycine (Gly) or DL-Phenylalanine (DL-Phe) were further exploited as the anion exchangers to post-modify the POSS-VDI column. The new POSS-VDI-Pro, POSS-VDI-Gly and POSS-VDI-Phe columns exhibited different separation selectivity for the complex egg white protein sample. The present work provides a good route to fabricate versatile amino acids and ionic liquids modified monolithic columns with good separation selectivity.
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Food Additives and Contaminants Part A-Chemistry Analysis Control Exposure & Risk Assessment
·
2021
·
IF 3.057
Qinqin Xu,Zikai Liu,Chen Yan,Runhua Lu,Wenfeng Zhou
In this study, a novel sorbent, 1-octyl-3-methylimidazolium hexafluorophosphate functionalised magnetic poly β-cyclodextrin, was successfully synthesised and applied to magnetic solid-phase extraction for the determination of pyrethroids in tea infusions. The sorbent was characterised by transmission electron microscopy, energy-dispersive spectroscopy, Fourier transform infrared spectroscopy, X-ray photoelectron spectroscopy, vibrating sample magnetometer and Brunauer–Emmett–Teller measurement. All factors affecting extraction efficiency, such as sorbent amount, extraction time, ionic strength and desorption conditions, were optimised individually. Under the chosen conditions, wide linearity (2.5–500 μg L−1) with determination coefficients ranging from 0.9995 to 0.9999, low limits of detection of 0.32–0.54 μg L−1 and good precision (intra-day: 2.6–7.0%; inter-day: 3.5–7.6%) were achieved for four pyrethroids in tea infusions. The relative recoveries of target analytes in real tea infusion samples were from 70% to 101% with relative standard deviations lower than 9.1%. We conclude that the proposed method is promising in the detection of pyrethroids in tea infusions.
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TOXICOLOGY LETTERS
·
2021
·
IF 4.374
Shanqi Guo,Yangyi Zhang,Shuo Wang,Tong Yang,Baojie Ma,Xiaojiang Li,Yizhuo Zhang,Xingkang Jiang
Antimony is a common environmental contaminant that causes biological toxicity in exposed populations worldwide. Previous studies have revealed that antimony promotes prostate cancer growth by stabilizing the c-Myc protein and mimicking androgen activity. However, the role of lncRNAs in the regulation of antimony-induced carcinogenesis remains unknown, and the precise mechanisms need to be explored. In the present study, we found that chronic exposure to antimony promoted cell growth and lipid metabolic disequilibrium in prostate cancer. Mechanistically, we identified a long noncoding RNA molecule, PCA3, that was substantially upregulated in LNCaP cells in response to long-term antimony exposure. Functional studies indicated that abnormal PCA3 expression modulated antimony-induced proliferation and cellular triglyceride and cholesterol levels. In addition, PCA3 levels were found to be inversely correlated with MIR-132-3 P levels by acting as a decoy for MIR-132-3P. Besides, SREBP1 directly interacted with MIR-132-3 P to increase cell growth and disrupt lipid metabolism by targeting its 3’UTR regions. Taken together, our results revealed that lncRNA PCA3 promotes antimony-induced lipid metabolic disorder in prostate cancer by targeting MIR-132-3 P/SREBP1 signaling.
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