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Analytical Methods · 2023 ·Vol. 15 ·期 27 ·3318-3324 · IF 3.1

Stability and spectroscopic analysis of CsPbBr3 quantum dots modified with 2-n-octyl-1-dodecanol

Hongyu Chen,Mingshuo Liu,Jianing Wang,Yunfei Wang,Yajuan Wang,Wenyan Liu

Due to their excellent optical and electrical properties, all-inorganic metal halide perovskite CsPbBr3 quantum dots (QDs) have become one of the most promising materials in the field of optoelectronics during recent years. However, the stability of CsPbBr3 QDs limits their practical application and further development to a certain extent. In order to improve their stability, CsPbBr3 QDs were modified with 2-n-octyl-1-dodecanol for the first time in this paper. The 2-n-octyl-1-dodecanol-modified CsPbBr3 QDs were prepared by the ligand-assisted reprecipitation (LARP) method at room temperature in an air environment. Then the stability of the samples was tested at different temperatures and humidity. When the humidity was 80%, the photoluminescence (PL) intensity of both unmodified and modified CsPbBr3 QDs increased to different degrees because the appropriate amount of water changed the crystallization environment. The PL intensity of the modified QDs increased, and the peak positions were basically not shifted, proving that they did not agglomerate. Thermal stability test results showed that the PL intensity of the 2-n-octyl-1-dodecanol-modified QDs could still maintain 65% of the original intensity at 90 °C, which is 4.6 times that of the unmodified CsPbBr3 QDs. Experimental results show that the stability of CsPbBr3 QDs is significantly improved after 2-n-octyl-1-dodecanol modification, which demonstrates the excellent surface passivation of CsPbBr3 QDs by 2-n-octyl-1-dodecanol.

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IET Nanobiotechnology · 2023 ·Vol. 17 ·期 4 ·387-395 · IF 2.3

Neutrophil membrane biomimetic delivery system (Ptdser-NM-Lipo/Fer-1) designed for targeting atherosclerosis therapy

Wei Li,Chang Liu,Sichuan Wang,Naifeng Liu

Atherosclerosis is a progressive inflammatory disease characterised by excessive lipid accumulation and inflammatory cell infiltration and is the basis of most cardiovascular diseases and peripheral arterial diseases. Therefore, an effectively targeted delivery system is urgently needed to deliver ferroptosis-specific inhibitors to the site of arterial plaque and the inflammatory microenvironment. Inspired by the fact that neutrophils can be recruited to arterial plaques under the action of adhesion molecules and chemokines, the authors developed a neutrophil membrane hybrid liposome nano-mimetic system (Ptdser-NM-Lipo/Fer-1) that delivers Ferrostatin-1 (Fer-1) to the atherosclerotic plaque effectively, which is composed of Fer-1-loaded Ptdser-modified liposomes core and neutrophils shell. Fer-1 was released at the AS plaque site to remove reactive oxygen species (ROS) and improve the inflammatory microenvironment. In vitro ROS clearance experiments have shown that 50 μmol/ml Fer-1 can significantly remove ROS produced by H 2 O 2 -induced MOVAS cells and Ptdser-NM-Lipo/Fer-1 revealed a 3-fold increase in the inhibition rate of ROS than free Fer-1 in induced-RAW264.7, demonstrating its superior ROS-cleaning effect. Based on the interaction of adhesion molecules, such as vascular cell adhesion molecule 1, ICAM-1, P-selectin, E-selectin, and chemokines released in the inflamed site, the aorta in NM-Lipo-treated mice displayed 1.3-fold greater radiant efficiency than platelet membrane-Lipo-treated mice. Meanwhile, due to the modification of the Ptdser, the aorta in Ptdser-NM-Lipo/Fer-1-treated mice exhibited the highest fluorescence intensity, demonstrating its excellent targeting ability for atherosclerosis. Therefore, we present a specific formulation for the treatment of atherosclerosis with the potential for novel therapeutic uses.

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European Journal of Integrative Medicine · 2023 · IF 2.5

Curcumol targets glutaminase 1 to regulate glutamine metabolism and induce senescence of hepatic stellate cells

Xuelin Duan,Tiejian Zhao,Jiaru Wang,Jiahui Wang,Yang Zheng

Introduction : Curcuma is used as an herbal remedy for the treatment of chronic liver diseases, and its main active ingredient is curcumol. This study explored the molecular mechanism of curcumol in regulating glutamine metabolism. Methods : The current investigation used lipopolysaccharide(LPS) to activate hepatic stellate cells (HSCs) and then analyzed the effects of curcumol on glutamine metabolism and cell proliferation. The effects of curcumol on glutaminase 1 (GLS1), senescence-related proteins, and extracellular matrix (ECM) expression were examined by western blotting and reverse transcription-quantitative polymerase chain reaction(RT-PCR). The effect of curcumol on the cell cycle was detected by flow cytometry. Furthermore, after overexpression of GLS1, we observed the effects of curcumol on glutamine metabolism, the expression of related molecules, and the cell cycle. Results : Curcumol significantly inhibited cell proliferation, glutamine metabolism, and GLS1 and ECM expression, and also significantly promoted cell senescence. With GLS1 overexpression, the inhibitory effects of curcumol on glutamine metabolism and on promoting cell senescence were rescued. Conclusion : Curcumol targets GLS1, inhibits glutamine metabolism, and induces senescence in HSCs. GLS1 may be an important target for the pharmacological effects of curcumol.

CAS / MDL: 4871-97-0
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CHEMICAL ENGINEERING JOURNAL · 2023 · IF 15.1

Physical UV-blocker TiO2 nanocomposites elevated toxicity of chemical sunscreen BP-1 under UV irradiation

Qiaorong Guo,Dongbin Wei,Chuanfang Zhao,Cuiping Wang,Haijun Ma,Yuguo Du

Physical UV-blocker TiO 2 nanocomposites and chemical sunscreen benzophenones (BPs) have been frequently detected in the aquatic environment, their combined fates and potential risk should be concerned. In this study, the typical cosmetic grade UV-blocker TiO 2 nanocomposites (labeled as CG-TiO 2 ) and 2,4-dihydroxy benzophenone (BP-1) were targeted, and the effects of CG-TiO 2 on the transformation of BP-1 during UV irradiation were explored. It was found that CG-TiO 2 destruction did not form toxic products, while they could promote the chemical reactions of BP-1 that will lead to highly toxic products during UV irradiation. More importantly, UV irradiation could break the organic coatings on CG-TiO 2 , the broken CG-TiO 2 exhibited stronger catalytic activity on BP-1 and form highly toxic products during UV irradiation. Total of 24 transformation products were tentatively identified, including hydroxyl BPs, hydroxyl dibenzo-p-dioxins, hydroxyl benzoyl benzoquinones, etc. The main transforamtion mechanisms of BP-1 included hydroxylation, radical coupling, oxidation, decarboxylation, Norrish type I reaction, and ring closure through electrophilic substitution. This study highlighted that physical UV-blocker CG-TiO 2 promoted the transformation of chemical sunscreen BP-1 and generated higher toxicity during UV irradiation. It was expected that these results would provide scientific data for evaluating the fates and potential risk of sunscreens in the environment.

CAS / MDL: 13463-67-7
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2023 · IF 8.2

Fractionation and characterization of poly(β-L-malic acid) produced by Aureobasidium melanogenum ipe-1

Changsheng Qiao,Guohang Sun,Hongbao Li,Weifeng Cao,Fei Shen,Rong Fan,Yinhua Wan

Poly (β-L-malic acid) (PMLA) is attracting industrial interest for its potential application in medicine and other industries, whose functions primarily depend upon its molecular size and chemical structure. Up to now, the fractionation and characterization of PMLA produced by Aureobasidium spp. were still unclear. In this study, the product from A. melanogenum ipe-1 was effectively fractionated using 300 and 50 kDa membranes. During the filtration, the mechanisms of membrane fouling were illegible since the PMLA can both reject and permeate the membrane, while the main fouling mechanism varied between standard blocking and complete blocking during the diafiltration . After fractionation, 14.0, 8.4 and 77.6 % of the PMLAs with M w s of 75,134, 21,344 and 10,056 Da were distributed in the 300 kDa retentate after diafiltrating, 50 kDa retentate after diafiltrating, and the 50 kDa permeate, respectively. The M w /M n s of the PMLAs were 4.12, 1.92, and 1.12 in the three fractions. Based on characteristic spectra of NMR, HPLC and FTIR, the product was not usual L-malic acid monomers, but glucose-terminated PMLA. The glucose was located at the terminal hydroxyl of PMLA. These results would serve as a valuable guide for process design and practical operation in subsequent industrial application.

CAS / MDL: 9057-02-7
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Nature Communications · 2023 ·Vol. 14 ·期 1 ·1-25 · IF 16.6

Nanoparticle-mediated TRPV1 channel blockade amplifies cancer thermo-immunotherapy via heat shock factor 1 modulation

Li Ting,Jiang Shuhui,Zhang Ying,Luo Jie,Li Ming,Ke Hengte,Deng Yibin,Yang Tao,Sun Xiaohui,Chen Huabing

The survival of malignant tumors is highly dependent on their intrinsic self-defense pathways such as heat shock protein (HSP) during cancer therapy. However, precisely dismantling self-defenses to amplify antitumor potency remains unexplored. Herein, we demonstrate that nanoparticle-mediated transient receptor potential vanilloid member 1 (TRPV1) channel blockade potentiates thermo-immunotherapy via suppressing heat shock factor 1 (HSF1)-mediated dual self-defense pathways. TRPV1 blockade inhibits hyperthermia-induced calcium influx and subsequent nuclear translocation of HSF1, which selectively suppresses stressfully overexpressed HSP70 for enhancing thermotherapeutic efficacy against a variety of primary, metastatic and recurrent tumor models. Particularly, the suppression of HSF1 translocation further restrains the transforming growth factor β (TGFβ) pathway to degrade the tumor stroma, which improves the infiltration of antitumor therapeutics (e.g. anti-PD-L1 antibody) and immune cells into highly fibrotic and immunosuppressive pancreatic cancers. As a result, TRPV1 blockade retrieves thermo-immunotherapy with tumor-eradicable and immune memory effects. The nanoparticle-mediated TRPV1 blockade represents as an effective approach to dismantle self-defenses for potent cancer therapy.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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Journal of Orthopaedic Surgery and Research · 2021 ·Vol. 16 ·期 1 ·1-9 · IF 2.359

Expression of STOML2 promotes proliferation and glycolysis of multiple myeloma cells via upregulating PAI-1

Zhang Hongxia,Wu Guangsheng,Feng Junjian,Lu Xiaohong,Liu Ping

Background This study aimed to investigate the effects of STOML2 and the relationship between STOML2 and PAI-1 in the development of multiple myeloma (MM). Methods Cell proliferation was tested using CCK-8 assay and cell colony formation assay. Glucose consumption, lactate production and ATP level were measured using commercial kits. The mRNA and protein expression were assessed using quantitative real-time polymerase chain reaction (qRT-PCR) and western blotting, respectively. Results Both mRNA and protein expression of STOML2 were upregulated in MM patients compared to healthy volunteers. CCK-8 and colony formation assays demonstrated that STOML2 silencing inhibited cell proliferation in MM cells. Knockdown of STOML2 reduced glucose consumption, lactate production and ATP/ADP ratios. STOML2 silencing by shSTOML2 led to reduced PAI-1 expression. Overexpression of PAI-1 reversed the inhibitory effects of shSTOML2 on MM cell growth. Conclusion Results from this study demonstrated that STOML2 silencing inhibits cell proliferation and glycolysis through downregulation of PAI-1 expression, suggesting a new therapeutic target for MM.

CAS / MDL: 30525-89-4
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FUEL · 2022 · IF 8.035

Viscosity measurement and correlation research of one biodiesel component (methyl octanoate) with five 1-alcohols

Xiaojie Wang,Yingjie Ma,Jianing Huo,Jidong Liu,Shizhao Wang,Lide Fang,Zhiyue Zhao

Alcohols are commonly used as additives in biodiesel to improve its viscous and dense properties for better applicability in the industrial field. In this work, experimental investigations are conducted on the dynamic viscosities for the binary mixture of methyl octanoate (one component of biodiesel) with one 1-alcohol containing 1-propanol, 1-butanol, 1-pentanol, 1-hexanol, and 1-heptanol from 293.15 to 333.15 K at atmospheric pressure. The excessive viscosity shows negative deviation from the ideal solution for each binary system and is fitted with the Redlich-Kister equation. The McAllister three-body model is used for the kinematic viscosity correlation of binary mixtures. To acquire dynamic viscosity, the experimental density is measured and correlated as a function of temperature and mole fraction of methyl octanoate. Meanwhile, the McAllister three-body model, Heric's model, Frenkel model, and Grunberg-Nissan model are used to correlate the viscosities of the mixtures. Furthermore, some research has also been done on the improvement of the prediction performance for McAllister three-body model based on the studied systems.

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Frontiers in Pharmacology · 2023 · IF 5.6

Fibroblast growth factor 1 ameliorates thin endometrium in rats through activation of the autophagic pathway

Jing Zhu,Zhenyao Li,Fengli Yin,Xiaoting Yu,Yuanfan Lu,Tong Zhou,Fanghua Gong,Zhangye Xu

Background : Thin endometrium is a reproductive disorder that affects embryo implantation. There are several therapies available for this disease, however they are not so effective. Fibroblast growth factor 1 (FGF1) is a member of fibroblast growth factor superfamily (FGFs), and it has been demonstrated that FGF1 expression was altered in samples collected from patients with thin endometrium. However, it is unclear if FGF1 could improve thin endometrium. The aim of this study was to investigate whether FGF1 have a therapeutic effect on thin endometrium. Methods: A model of thin endometrium induced by ethanol was constructed to investigate the effect and mechanism of action of FGF1 in thin endometrium. In the characterization experiments, 6–8 weeks female rats (n = 40) were divided into four groups: i) Control group; ii) Sham group; iii) Injured group; (iv) FGF1 therapy group. Endometrial tissues would be removed after three sexuel cycles after molding. Morphology and histology of the endometrium were evaluated by visual and hematoxylin and eosin staining. Masson staining and expression of α-SMA in endometrium showed the degree of endometrial fibrosis. Western blotting (PCNA、vWF and Vim) and immunohistochemistry (CK19 and MUC-1) demonstrated the effect of FGF1 on cell proliferation and angiogenesis. Moreover, immunohistochemistry (ER and PR) was used to explore the function of endometrium. The remaining rats (n = 36) were divided into three groups: i) Injured group; ii) FGF1 therapy group; and iii) 3-methyladenine. Western blotting (p38、p-p38、PI3K 、SQSTM1/p62、beclin-1 and LC3) was used to explore the mechanisms of FGF1. Results: In FGF1 therapy group, the morphology and histology of endometrium improved compared with the model group. Masson staining and the expression level of α-SMA showed that FGF1 could decrease the fibrotic area of endometrium. Besides, changes in ER and PR expression in the endometrium suggested that FGF1 could restore endometrium-related functions. Western blotting and immunohistochemistry revealed that PCNA, vWF, Vim, CK19 and MUC-1 were significantly increased after FGF1 treatment compared with the thin endometrium. In addition, Western blotting showed that p38, p-p38, PI3K, SQSTM1/p62, beclin-1 and LC3 levels were higher in FGF1 group than in the injured group. Conclusion: FGF1 application cured the thin endometrium caused by ethanol through autophagy mechanism.

CAS / MDL: 5142-23-4
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BIOORGANIC & MEDICINAL CHEMISTRY · 2017 · IF 2.93

Identification of nitroimidazole-oxime derivatives targeting the polo-box domain of polo-like kinase 1

Juan Sun,Han-Yu Liu,Ruo-Fei Xu,Hai-Liang Zhu

Recent progress in the development of small molecular skeleton-derived polo-like kinase (PLK1) catalytic domain (K D ) inhibitors has led to the synthesis of multiple ligands with high binding affinity. However, few systematic analyses have been conducted to identify key PLK1-PBD domain and characterize their interactions with potent PLK1 inhibitors. Therefore, we designed a series of PLK1-PBD inhibitors with an in silico scaffold modification strategy. A docking simulation combined with a primary screen in vitro were performed to filter for the lead compound, which was then substituted, synthesized and evaluated by a variety of bioassays. The biological profile of 4v suggests that this compound may be developed as a potential anticancer agent.

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EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY · 2022 · IF 7.088

Development of 5-hydroxyl-1-azabenzanthrone derivatives as dual binding site and selective acetylcholinesterase inhibitors

Xiaona Sun,Yujin Wang,Zhichao Lei,Shasha Yue,Li Chen,Jianbo Sun

A series of novel 5-hydroxyl-1-azabenzanthrone derivatives were designed, synthesized and evaluated as dual binding site acetylcholinesterase inhibitors for the treatment of Alzheimer's disease (AD). The most effective Compound 16 showed selective inhibition of acetylcholinesterase ( ee AChE IC 50  = 0.045 μM; ee BuChE IC 50  = 19.68 μM; SI = 437.33). Most of the compounds showed cytoprotective effects on PC12 cells damaged by hydrogen peroxide, which might be related to their antioxidant activity . Further experiments confirmed that 16 exhibited anti-apoptotic effects at low concentrations and reduced the relative level of ROS generation in PC12 cells. The expression level of proteins related to antioxidant stress pathway in PC12 cells was relatively increased after administrated with 16 , which may be beneficial to delay the progression of the disease. Moreover, 16 was evaluated to be safe in vivo and in vitro, and showed good overall pharmacokinetic performance and high bioavailability (Foral = 55.5%). Besides, 16 showed comparable performance in ameliorating the scopolamine-induced cognition impairment to donepezil . In addition, in vitro BBB permeability experiments confirmed that 16 had high BBB permeability.

CAS / MDL: 51-34-3
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EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY · 2019 · IF 4.833

Synthesis and bioevaluation of 1-phenylimidazole-4-carboxylic acid derivatives as novel xanthine oxidoreductase inhibitors

Haiyan Zhou,Xiaolei Li,Yuanyuan Li,Xinying Zhu,Lei Zhang,Jing Li

As part of a continuing study, we designed and synthesized four series of 1-phenylimidazole-4-carboxylic acid derivatives as xanthine oxidoreductase (XOR) inhibitors, evaluated their in vitro inhibitory potencies against XOR and hypouricemic effects in mice, and determined their structure-activity relationships (SARs). Most of the compounds exhibited in vitro XOR inhibition at the nanomolar level. In comparison to febuxostat (half-maximal inhibitory concentration [IC 50 ] value of 7.0 nM), compounds Ie and IVa exhibited the most promising XOR inhibitory effects with IC 50 values of 8.0 and 7.2 nM, respectively. In the potassium oxonate/hypoxanthine-induced acute and long-term hyperuricemia mouse models, compounds Ie and IVa displayed significant hypouricemic potencies ( P  < 0.05), that were slightly weaker than and similar to febuxostat, respectively. More interestingly, both compounds showed a capacity to improve kidney damage by decreasing creatinine and urea nitrogen levels compared to the long-term hyperuricemia mouse group ( P  < 0.05), while febuxostat showed no significant effect.

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