DRUG DELIVERY
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2021
·
IF 6.419
Jianbo Li,Tiange Feng,Weijing Yang,Yaru Xu,Shuaishuai Wang,Huijie Cai,Zhilei Liu,Hong Qiang,Jinjie Zhang
Although Fraxinellone (Frax) isolated from Dictamnus albus L. possessed excellent anti-hepatic fibrosis activity, oral administration of Frax suffered from the inefficient therapeutic outcome in vivo due to negligible oral absorption. At present, the oral formulation of Frax is rarely exploited. For rational formulation design, we evaluated preabsorption risks of Frax and found that Frax was rather stable while poorly dissolved in the gastrointestinal tract (78.88 μg/mL), which predominantly limited its oral absorption. Further solubility test revealed the outstanding capacity of cyclodextrin derivatives (CDs) to solubilize Frax (6.8–12.8 mg/mL). This led us to study the inclusion complexes of Frax with a series of CDs and holistically explore their drug delivery performance. Characterization techniques involving 1H-NMR, FT-IR, DSC, PXRD, and molecular docking confirmed the most stable binding interactions when Frax complexed with 6-O-α-D-maltosyl-β-cyclodextrin (G2-β-CD-Frax). Notably, G2-β-CD-Frax exhibited the highest solubilizing capacity, fast dissolution rate, and superior Caco-2 cell internalization with no obvious toxicity. Pharmacokinetic studies demonstrated markedly higher oral bioavailability of G2-β-CD-Frax (5.8-fold that of free drug) than other Frax-CDs. Further, long-term administration of G2-β-CD-Frax (5 mg/kg) efficiently inhibited CCl4-induced hepatic fibrosis in the mouse without inducing any toxicity. Our results will inspire the continued advancement of optimal oral Frax formulations for anti-fibrotic therapy.
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高影响因子
NEW JOURNAL OF CHEMISTRY
·
2018
·Vol. 42
·期 12
·9757-9763
·
IF 3.201
Yalan Liu,Jiao Li,Gang Chang,Ruizhi Zhu,Hanping He,Xiuhua Zhang,Shengfu Wang
Electrochemical sensors have been highly developed and play an important role in the early diagnosis of different diseases. In this work, a simple and rapid electrochemical method was developed for the quantitative detection of a trinucleotide repeat (TNR) sequence d(CAG)n based on magnetic beads and screen-printed carbon electrodes. Their combination greatly simplified the operation process. The intensity of the electrochemical signal was linearly correlated against the concentration of the TNR sequence d(CAG)n in the range from 100 pM to 1 μM, with a limit of detection as low as 24 pM. Furthermore, the number of repeats of the TNR sequence d(CAG)n could be detected and also showed a good linear relationship. The proposed method provides a promising rapid and simple method for the detection of a CAG TNR sequence for point-of-care testing in clinical applications.
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CHEMICAL RESEARCH IN TOXICOLOGY
·
2018
·
IF 3.432
Xiaomin Xia,Bin Lu,Wenjing Dong,Bingwei Yang,Yawen Wang,Qi Qin,Zixuan Liu,Erqun Song,Yang Song
Our previous study showed that tetrachlorobenzoquinone (TCBQ) mediated the activation of Nod-like receptor protein 3 (NLRP3) inflammasome, which involves K+ efflux, reactive oxygen species (ROS) production, and mitochondrial DNA damage. In addition, TCBQ down-regulates NLRP3 ubiquitination and promotes the activation of NLRP3 inflammasome. However, the induction of NLRP3 inflammasome by atypical pathways has not yet been characterized. Using human umbilical vein endothelial cells (HUVEC), we discovered that TCBQ activates caspase 1/4/5 and cleaves gasdermin D (GSDMD) into N-terminal and C-terminal cleavage products. In parallel, TCBQ also activates receptor interacting protein kinase 3 (RIPK3)/mixed lineage kinase domain-like protein (MLKL) signaling pathways. The N-terminal fragments of GSDMD and MLKL translocate from cytoplasm to cell membrane and form oligomers and membrane pores on the cell membrane. The formation of membrane pores not only promotes the extracellular secretion of interleukin 1 beta (IL-1β) but also affects cellular ion homeostasis, in particular promotes K+ outflow, which further activates NLRP3 inflammasome and aggravates cellular inflammation. These results indicated that GSDMD and MLKL play important roles in TCBQ-induced endothelial pro-inflammatory responses, which may point to potential therapeutic approaches for TCBQ-mediated toxicity.
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JOURNAL OF CHEMICAL THERMODYNAMICS
·
2018
·
IF 2.631
Xiao Feng,Ali Farajtabar,Hu Lin,Gaoquan Chen,Zhiying Wang,Xinbao Li,Hongkun Zhao
The D-tryptophan solubility in aqueous solutions of methanol, ethanol, isopropanol and N , N -dimethylformamide (DMF) was measured by the saturation shake-flask method at temperatures ranging from 283.15 K to 333.15 K. The maximum solubility was found in water for alcohol (1) + water (2) mixtures, and in neat DMF for DMF (1) + water (2) mixture. When the same temperature and mass fraction of the water is given, the highest mole fraction solubility of D-tryptophan was found in (DMF + water). The solid phases were tested by X-ray powder diffraction (XPRD) showing no polymorphic transformation, solvate formation or crystal transition. Three solubility models, i.e. the Jouyban-Acree, van’t Hoff-Jouyban-Acree and Apelblat-Jouyban-Acree were employed to correlate the experimental solubility values so as to obtain thermodynamic parameters. The RAD and RMSD data were no more than 1.65% and 9.40 × 10 −5 , respectively. Linear solvation energy relationship analysis based on Kamlet-Taft parameters indicated that the variation of D-tryptophan solubility depended on π ∗ for methanol (ethanol, isopropanol) (1) + water (2), and cavity term for DMF (1) + water (2). The preferential solvation parameters ( δx 1,3 ) for methanol, ethanol, isopropanol and DMF derived by means of the inverse Kirkwood–Buff integrals were negative in the four solvent mixtures with intermediate and alcohol-rich compositions, which indicated that D-tryptophan was preferentially solvated by water. The higher solvation by water could be explained in terms of the higher acidic behaviour of the solvents interacting with the Lewis basic groups of the D-tryptophan. However D-tryptophan is preferentially solvated neither by water nor by DMF in DMF + water mixture.
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CATALYSIS TODAY
·
2014
·
IF 3.309
Huiling Li,Aojie Deng,Junli Ren,Changyu Liu,Wenju Wang,Feng Peng,Runcang Sun
One of the most promising strategies for furfural production is to extract continually the target product from the aqueous solution utilizing organic solvents. With the aim to develop an ecologically viable catalytic pathway for furfural production without the addition of mineral acids, we presented a modified biphasic system using a solid acid (SO 4 2− /TiO 2 -ZrO 2 /La 3+ ) as catalyst for producing furfural from xylose. Different kinds of aprotic organic solvents (DMSO, DMF and DMI) in water phase and 2-butanol in organic phase (MIBK) were investigated as reaction media. Furfural yield and xylose conversion efficiency were dependent on the amounts of aprotic organic solvents and 2-butanol, the solid/liquid ratio, and the volume ratio of the organic phase and the aqueous phase as well as the reaction temperature and time. As a result, DMI showed the best performance on improving furfural yield during the furfural production. 3563.3 μmol of furfural/g of xylose with 97.9% xylose conversion efficiency was obtained after 12 h at 180 °C when the volume ratios of water to DMI and MIBK to 2-butanol were 8:2 and 7:3, respectively.
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JOURNAL OF COLLOID AND INTERFACE SCIENCE
·
2014
·
IF 3.552
Juan Li,Xiaodan Yang,Chiyao Bai,Yin Tian,Bo Li,Shuang Zhang,Xiaoyu Yang,Songdong Ding,Chuanqin Xia,Xinyu Tan,Lijian Ma,Shoujian Li
A novel COF-based material (COF-COOH) containing large amounts of carboxylic groups was prepared for the first time by using a simple and effective one-step synthetic method, in which the cheap and commercially available raw materials, trimesoyl chloride and p -phenylenediamine, were used. The as-synthesized COF-COOH was modified with previously synthesized 2-(2,4-dihydroxyphenyl)-benzimidazole (HBI) by “grafting to” method, and a new solid-phase extractant (COF-HBI) with highly efficient sorption performance for uranium(VI) was consequently obtained. A series of characterizations demonstrated that COF-COOH and COF-HBI exhibited great thermostabilities and irradiation stabilities. Sorption behavior of the COF-based materials toward U(VI) was compared in simulated nuclear industrial effluent containing UO 2 2+ and 11 undesired ions, and the UO 2 2+ sorption amount of COF-HBI was 81 mg g −1 , accounting for approximately 58% of the total sorption amount, which was much higher than the sorption selectivity of COF-COOH to UO 2 2+ (39%). Batch sorption experiment results indicated that the uranium(VI) sorption on COF-HBI was a pH dependent, rapid (sorption equilibrium was reached in 30 min), endothermic and spontaneous process. In the most favorable conditions, the equilibrium sorption capacity of the adsorbent for uranium could reach 211 mg g −1 .
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Polymers
·
2024
·Vol. 16
·期 23
·3287
·
IF 4.7
Han Zhou,Zaitian Cheng,Guoxing Pan,Lin Hu,Fapei Zhang
The performance of organic field-effect transistors (OFETs) is highly dependent on the dielectric–semiconductor interface, especially in ion-gel-gated OFETs, where a significantly high carrier density is induced at the interface at a low gate voltage. This study investigates how altering the alkyl side chain length of donor–acceptor (D-A) copolymers impacts the electrical performance of ion-gel-gated OFETs. Two difluorobenzothiadiazole-based D-A copolymers, PffBT4T-2OD and PffBT4T-2DT, are compared, where the latter features longer alkyl side chains. Although PffBT4T-2DT shows a 2.4-fold enhancement of charge mobility in the SiO2-gated OFETs compared to its counterpart due to higher crystallinity in the film, PffBT4T-2OD outperforms PffBT4T-2DT in the ion-gel-gated OFETs, manifested by an extraordinarily high mobility of 17.7 cm2/V s. The smoother surface morphology, as well as stronger interfacial interaction between the ion-gel dielectric and PffBT4T-2OD, enhances interfacial charge accumulation, which leads to higher mobility. Furthermore, PffBT4T-2OD is blended with a polymeric elastomer SEBS to achieve ion-gel-gated flexible OFETs. The blend devices exhibit high mobility of 8.6 cm2/V s and high stretchability, retaining 45% of initial mobility under 100% tensile strain. This study demonstrates the importance of optimizing the chain structure of polymer semiconductors and the semiconductor–dielectric interface to develop low-voltage and high-performance flexible OFETs for wearable electronics applications.
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JOURNAL OF COLLOID AND INTERFACE SCIENCE
·
2024
·
IF 9.4
Jiaqi Li,Yuxi Zhang,Hanhao Liang,Jiaming Li,Xiao Yu,Jianglin Wang,Yini Long,Zhanhong Yang
Manganese oxide is a promising cathode material for rechargeable batteries due to its high theoretical specific capacity. However, its practical application is hindered by its poor conductivity and rapid capacity decay caused by Jahn-Teller distortion during charging and discharging. This work introduces Na 2 EDTA during the synthesis of Mn O 2 , and the amino group is introduced by adsorption to deposit to form N-doped Mn O 2 . Alkaline N-doped Mn O 2 battery upshifts the d-band center of Mn, improves the conductivity of Mn O 2 and the formation energy of O vacancies during the charge-discharge process, and suppresses Jahn Teller distortion. As a result, N-doped Mn O 2 achieves a high capacity of up to 197mAh g −1 and excellent capacity retention of 94.2% over 250 cycles with slower voltage decay. This strategy enables the material with high cycling performance for single-electron discharge secondary alkaline manganese batteries.
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INTERNATIONAL JOURNAL OF HYDROGEN ENERGY
·
2024
·
IF 8.1
Jiachen Zou,Guanying Song,Anguo Cui,Jinfeng Cui,Zhenjiang Li
The rational design of highly active electrocatalysts for water electrolysis remains challenging for green hydrogen utilization . Herein, guided by the correlation between the electroactivity and the d-band center (E d ), a novel hierarchical nanoarchitecture (Ni 2 P/NiFe 2 O 4 -V O @N-GTs) was fabricated, in which, Ni 2 P nanoparticles are grown on the oxygen vacancy-rich NiFe 2 O 4 nanosheet arrays anchoring on N-doping graphene tubes. The results reveal that the multiple strategies including the vacancies and heterogeneous interface construction effectively induce the charge redistribution, and further adjust the E d to the appropriate energy level, which endows the optimal balance between the adsorption and desorption ability of the catalyst to reaction intermediates, thus leading to the conspicuous electrocatalytic activity . Additionally, the hierarchical nanoarchitecture contributes to the exposure of more active sites, the efficiency of electron transfer , and the release of generated gas. Hence, Ni 2 P/NiFe 2 O 4 -V O @N-GTs presents superior bifunctional activity, especially a low overpotential of 194 mV at 10 mA cm −2 for OER . The corresponding overall water electrolyzer owns a lower cell voltage and long-term durability with continuously operating over 330 h at 100 mA cm −2 , outperforming the most reported bifunctional electrocatalysts . This work presents an effective pathway for regulating the E d through multiple strategies to improve the catalytic performance of catalysts.
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POLYMER INTERNATIONAL
·
2017
·Vol. 67
·期 3
·313-321
·
IF 2.07
Chunyan Luo,Minrui Yang,Wei Xiao,Jingjing Yang,Yan Wang,Weixing Chen,Xia Han
Poly( l -lactic acid) (PLLA) is a good biomedical polymer material with wide applications. The addition of poly(ethylene glycol) (PEG) as a plasticizer and the formation of stereocomplex crystals (SCs) have been proved to be effective methods for improving the crystallization of PLLA, which will promote its heat resistance. In this work, the crystallization behavior of PEG and PLLA/poly( d -lactic acid) (PDLA) in PLLA/PDLA/PEG and PEG- b -PLLA/PEG- b -PDLA blends has been investigated using differential scanning calorimetry, polarized optical microscopy and X-ray diffraction. Both SCs and homocrystals (HCs) were observed in blends with asymmetric mass ratio of PLLA/PDLA, while exclusively SCs were observed in blends with approximately equal mass ratio of PLLA/PDLA. The crystallization of PEG was only observed for the symmetric blends of PLLA 39k /PDLA 35k /PEG 2k , PLLA 39k /PDLA 35k /PEG 5k , PLLA 69k /PDLA 96k /PEG 5k and PEG- b -PLLA 31k /PEG- b -PDLA 27k , where the mass ratio of PLLA/PDLA was approximately 1/1. The results demonstrated that the formation of exclusively SCs would facilitate the crystallization of PEG, while the existence of both HCs and SCs could restrict the crystallization of PEG. The crystallization of PEG is related to the crystallinity of PLLA and PDLA, which will be promoted by the formation of SCs. © 2017 Society of Chemical Industry
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JOURNAL OF MEDICINAL CHEMISTRY
·
2024
·
IF 6.8
Ting Xu,Xiaoting Yan,Ayue Kang,Longhua Yang,Xinhui Li,Yue Tian,Ruige Yang,Shangshang Qin,Yong Guo
The escalation of multidrug-resistant bacterial infections, especially infections caused by methicillin-resistant Staphylococcus aureus (MRSA), underscores the urgent need for novel antimicrobial drugs. Here, we synthesized a series of amphiphilic 2-phenyl-1H-phenanthro[9,10-d]imidazole-antimicrobial peptide (AMP) mimic conjugates (III1–30). Among them, compound III13 exhibited excellent antibacterial activity against G+ bacteria and clinical MRSA isolates (MIC = 0.5–2 μg/mL), high membrane selectivity, and low toxicity. Additionally, compared with traditional clinical antibiotics, III13 demonstrated rapid bactericidal efficacy and was less susceptible to causing bacterial resistance. Mechanistic studies revealed that III13 targets phosphatidylglycerol (PG) on bacterial membranes to disrupt membrane integrity, leading to an increase in intracellular ROS and leakage of proteins and DNA, ultimately causing bacterial cell death. Furthermore, III13 possessed good fluorescence properties with potential for further dynamic monitoring of the antimicrobial process. Notably, III13 showed better in vivo efficacy against MRSA compared to vancomycin, suggesting its potential as a promising candidate for anti-MRSA medication.
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JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
·
2025
·
IF 3.1
Xiaolin Wu,Qiao Yu,Yuzhao Hou,Xuemei Zhang,Simon Sani Ocholi,Liming Wang,Ziping Yan,Jie Li,Lifeng Han
Cholestatic liver disease(CLD) is caused by impaired bile flow due to obstruction of the biliary tract, and long-term exposure to bile acids in the liver triggers inflammation, eventually leading to liver toxicity and liver fibrosis. Emodin-8- O-β -D-glucopyranoside(EG) is anthraquinone compound that is widely found in traditional Chinese medicine. It possessed antioxidative and anti-inflammatory activities. However, the effect of EG on cholestatic liver injury(CLI) has not been explored. In this study, Alpha-naphthyl isothiocyanate(ANIT)-induced CLI mice were used to investigate the anti-cholestasis and hepatoprotective effects of EG through serum biochemical index detection, non-targeted metabolomics, lipidomics, and intestinal flora 16S rRNA sequencing. The results suggested that EG restores homeostasis of the gut microbiome while regulating bile acids metabolism and lipid-related metabolic pathways to reduce liver damage in ANIT-induced cholestasis. This study provides a new perspective on the mechanism of EG, and help offer a more natural approach to managing liver damage.
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