Asian Journal of Pharmaceutical Sciences
·
2018
·
IF 4.56
Shu Han,Ruiyang Sun,Hong Su,Jing Lv,Huan Xu,Di Zhang,Yuanshan Fu
This study aimed to investigate the ability of the novel materials D -α-tocopheryl poly(2-ethyl-2-oxazoline) succinate (TPOS) to construct pH-sensitive liposomes. TPOS was initially synthesized and characterized by TLC, FTIR, and 1 H-NMR. The buffering capacity of polyethylene glycol- distearoyl phosphatidylethanolamine (PEG-DSPE) and TPOS was determined by acid-base titration, and TPOS displayed a slower downtrend and gentler slope of titration curve than PEG-DSPE within pH 7.4–5.0. Studies on the in vitro drug release demonstrated that TPOS modified docetaxel (DOC) liposomes (TPOS-DOC-L) had a slower drug-release rate at pH 7.4 similar to PEGylated-DOC liposomes (PEG-DOC-L), whereas the release rate reached approximately 86.92% ± 1.69% at pH 6.4. In vitro cellular uptake assays by microplate reader, and flow cytometry revealed that TPOS modified coumarin 6 liposomes (TPOS-C6-L) had stronger cellular uptake at pH 6.4 than that at pH 7.4 ( P < 0.01). Conversely, for PEGylated C6 liposomes (PEG-C6-L) and conventional C6 liposomes (C6-L), very similar cellular uptakes were exhibited at different pH values. Confocal laser scanning microscopy images showed that PEG-C6-L and C6-L were mainly located in lysosomes. By contrast, TPOS-C6-L showed broader cytoplasmic release and distribution at 4 h. MTT assay showed that the cytotoxicity of TPOS-DOC-L was similar to that of PEG-DOC-L and conventional DOC liposomes (DOC-L) at the same DOC concentration and at pH 7.4, but was much lower than those at pH 6.4 after 48 h of incubation. The apoptosis of PEG-DOC-L and DOC-L had no remarkable improvement with decreased pH from 7.4 to 6.4. Meanwhile, TPOS-DOC-L significantly induced the apoptosis of HeLa cells with decreased pH. Therefore, TPOS can be a biomaterial for the construction of a pH-sensitive drug delivery system.
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高影响因子
MECHANISMS OF AGEING AND DEVELOPMENT
·
2017
·
IF 3.087
Jiming Chen,Yifan Li,Qiangqiang Zhu,Tong Li,Hao Lu,Nan Wei,Yewei Huang,Ruoyu Shi,Xiao Ma,Xuanjun Wang,Jun Sheng
Epigallocatechin gallate(EGCG) is a monomer separated from tea catechins, as an well-known antioxidant, which helps fight wrinkles and rejuvenate skin cells. In this study, we investigated the anti-aging effect of EGCG, and to clarify underlying mechanism of skin aging in a d -galactose-induced aging mouse model. Forty-five male mice were divided into 5 groups and treated with different dose of EGCG, Vitamin C (Vit C) to mice as a positive control. All groups except vehicle were established aging model induced by d -galactose (200 mg/kg/day) that was subcutaneously injected to mice for 8 weeks. Two weeks after injection of d -galactose, EGCG and Vit C groups were simultaneously administered once a day by subcutaneously inject after 5 h for injecting d -galactose. The results show that EGCG can be absorbed by the skin. Overall, the conditions of the skin of EGCG-treatment groups were improved, the whole structure of skin were better than control groups, and the levels of oxidative stress and the expression of relate with EGFR proteins were significantly higher than control group after EGCG treatment. All these findings suggest that EGCG can resist skin senility effectively. And the EGFR with relate of downstream proteins are implicated in the skin aging.
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高影响因子
DRUG DEVELOPMENT RESEARCH
·
2018
·Vol. 79
·期 6
·307-312
·
IF 2.646
Zi-Li Ren,Hao Liu,Di Jiao,Hao-Tian Hu,Wei Wang,Jie-Xiu Gong,Ai-Li Wang,Hai-Qun Cao,Xian-Hai Lv
Hit, Lead & Candidate Discovery To discover succinate dehydrogenase inhibitors with a novel structure, we introduced cinnamic acid structure to optimize the lead structure 1 and synthesized four series of cinnamon–pyrazole carboxamide derivatives. The bioassay data showed that compounds (E)-N-(1-[4-chlorophenyl]-4-cyano-1H-pyrazol-5-yl)-3-(2-fluorophenyl) acrylamide ( 5III-d) and (E)-3-(2-chlorophenyl)-N-(1-[4-chlorophenyl]-4-cyano-1H-pyrazol-5-yl) acrylamide ( 5III-f) showed the significant antifungal activity against three fungi. In addition, 5III-d and 5III-f exhibited the excellent inhibitory effect against succinate dehydrogenase (SDH) enzymes with IC 50 values ranging from 19.4 to 28.7 μM. The study demonstrates that the chlorine substituent group is present on both the phenyl and pyrazole rings that have a very good effect on the antifungal effect, and the compounds 5III-d and 5III-f can act as potential SDH inhibitors (SDHI) and throw a sprat for a new generation of SDHI.
研究领域:
药物化学
·
微生物学
·
植物保护学
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APPLIED SURFACE SCIENCE
·
2021
·
IF 6.707
Wenwei He,Peng-Gang Ren,Zhong Dai,Xin Hou,Fang Ren,Yan-Ling Jin
In recent years, biomass-derived carbon electrode materials for energy storage have attracted intensive attention in terms of their natural unique structure, widespread availability and low cost. Herein, a unique hierarchical porous carbon composite material (CGCM@GNS&CNT) was facilely constructed on 3-D carbon skeleton by anchoring 2-D graphene nanosheet (GNS) and 1-D carbon nanotube (CNT) through self-assembling method. The CGs with abundant macroscopic pores were utilized as 3D carbon skeleton, CNT and GNS anchored on them were applied to enhance the specific surface area (SSA) and electrical conductivity. The composite material exhibits large SSA of 460 m 2 g −1 , interconnected conductive network and inherent N, O doping. The CGCM@GNS&CNT electrode achieves a high areal capacitance of 441 mF cm −2 and volumetric capacitance of 90 F cm −3 at 1 mA cm −2 in 1.5 M Na 2 SO 4 electrolyte. More importantly, the CGCM@GNS&CNT-based symmetric supercapacitor affords a remarkable energy density of 31 μWh cm −2 at a power density of 800 μW cm −2 in 1.5 M Na 2 SO 4 . The capacitance retention and coulombic efficiency can retain 102.5% and 100.5% over 2000 cycles, respectively, confirming its superb charge/discharge stability and long-term reversibility. These signify that CGCM@GNS&CNT material holds a considerable promise for electrode application in high-performance supercapacitor.
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APPLIED ORGANOMETALLIC CHEMISTRY
·
2020
·Vol. 34
·期 4
·e5451
·
IF 3.14
Shuang Huang,Xi Hong,Yong Sun,He-Zhen Cui,Quan Zhou,Yue-Jian Lin,Xiu-Feng Hou
Six tridentate NNN ligand precursors derived from 2-(pyridin-2-yl)benzo[d]thiazole(PBT) with different linkers, PBT NN X N (X = NH, NMe, O, S) ( 1a – 1f ), have been successfully prepared. The electronic properties of PBT NN X N ligands are well tunable by differing linkers between PBT skeleton and the pyridine ring, and/or by introducing electron-donating/withdrawing groups on the pyridine ring (R = OMe or F). The ligand precursors and representative complexes Ru ( PBT NN NH N )Cl 2 (PPh 3 ) ( 2a ), Ru ( PBT NN NMe N )Cl 2 (PPh 3 ) ( 2b ), and Ru ( PBT NN S N )Cl 2 (PPh 3 ) ( 2f ) have been characterized by NMR spectroscopy, high-resolution mass spectroscopy, and Fourier transform infrared (FT-IR). The molecular structures of 1f , 2a , and 2f have been determined by X-ray diffraction study. The results indicate that PBT NN NH N ligand in the complex presented coplanar with two five-membered chelating rings. It should be noted that 2a featuring a NH group exhibits superior performance compared to those with other linkers (such as NMe, O, or S). A variety of heterocyclic and aromatic nitriles with aromatic and aliphatic alcohols have been explored in α -alkylation for good to excellent yields. Based on kinetic experiments and mechanistic studies, a proposed mechanism was put forward. Ru-H species and benzaldehyde, which was oxidized from benzyl alcohol, were detected in the catalytic cycle.
研究领域:
无机化学
·
有机化学
·
催化
·
材料科学
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RARE METALS
·
2026
·Vol. 45
·期 10
·e70671
·
IF 12.1
Zhidan Wang,Rui Li,Yawen Wang,Yunfang Wang,Caimei Fan,Jianxin Liu,Shan Gao,Jiancheng Wang
en This link goes to a English section zh This link goes to a Chinese section Photocatalytic acetylene (C 2 H 2 ) semihydrogenation is a green route for ethylene (C 2 H 4 ) production, yet the activity–selectivity trade-off caused by imbalanced adsorption/activation of reactants and products remains a core challenge. Herein, we realize precise regulation of Pd oxidation states (Pd 0 , Pd δ + , and Pd 2+ ) on anatase TiO 2 nanocubes via a mild reduction strategy, fabricating a Pd δ + /TiO 2 photocatalyst with intermediate valence of Pd sites. Systematic characterizations and theoretical calculations reveal that Pd δ + optimizes the d-π/d-π* orbital interactions between Pd and C 2 H 2 /C 2 H 4 , achieving a moderate adsorption strength that balances efficient C 2 H 2 activation and rapid C 2 H 4 desorption. Pd 0 causes overadsorption/overhydrogenation, whereas Pd 2+ leads to weak substrate activation. Consequently, Pd δ + /TiO 2 achieves nearly 100% C 2 H 2 conversion and ∼90% C 2 H 4 selectivity, with a record-high turnover number (TON) of ∼4.1 × 10 4 and excellent cycling stability. This work clarifies the electronic mechanism of Pd valence engineering in carrier dynamics and modulating orbital hybridization, providing a new strategy for the rational design of C 2 H 2 semihydrogenation photocatalysts. 摘要 en This link goes to a English section zh This link goes to a Chinese section 光催化乙炔(C 2 H 2 )半加氢是一种制备乙烯(C 2 H 4 )的绿色路径,但反应物与产物吸附与活化不均衡引发的活性-选择性权衡问题仍是核心难题。本文通过温和还原策略,在锐钛矿二氧化钛纳米立方体上实现钯氧化态(Pd 0 、Pd δ + 、Pd 2+ )的精准调控,制备出活性位点为中间价态钯的 Pd δ + /TiO 2 光催化剂。系统表征与理论计算结果表明,Pd δ + 能够优化钯与C 2 H 2 /C 2 H 4 之间的d-π/d-π* 轨道相互作用,形成适中的吸附强度,兼顾高效活化乙炔与乙烯快速脱附, Pd 0 会造成吸附过强并引发过度加氢,而Pd 2+ 对底物活化能力较弱。因此,Pd δ + /TiO 2 可实现接近 100% 的乙炔转化率和约 90% 的乙烯选择性,周转数(TON)高达4.1 × 10 4 ,同时具备优异的循环稳定性。该研究阐明了调控钯价态对载流子动力学及轨道杂化进行调控的电子作用机制,为乙炔半加氢光催化剂的合理设计提供了新思路。
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JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE
·
2022
·Vol. 103
·期 2
·779-791
·
IF 4.125
Huanhuan Teng,Yi Zhang,Chuanshan Jin,Tongsheng Wang,Shengzhuo Huang,Lei Li,Songzi Xie,Deling Wu,Fengqing Xu
BACKGROUND Polygonatum cyrtonema Hua is cultivated for its edible and medical value. The steam-processed rhizome of P. cyrtonema is the main form for daily consumption and it has been used traditionally in tonics for treating various age-related disorders. The aim of our study was to compare the physicochemical properties and antioxidant activity of polysaccharides respectively extracted from crude P. Cyrtonema (PCPC), and steam-processed P. cyrtonema (PCPS), and to explore a possible underlying antioxidant mechanism. RESULTS The PCPC with a molecular weight of 4.35 × 10 3 Da mainly consisted of fructose and trace amounts of glucose, whereas PCPS with 4.24 × 10 4 Da was composed of fructose, arabinose, glucose, xylose, mannose, galacturonic acid and glucuronic acid. The PCPC had a triple-helical conformation whereas PCPS was a random coil. Both exhibited free radicals- scavenging activity in vitro . In a mouse model of oxidative damage, PCPC or PCPS treatment significantly reversed histopathological alterations, reactive oxygen species (ROS) accumulation and the reduction of antioxidant enzyme activity. They both also promoted Nrf2 nuclear transport by decreasing Keap-1 expression and increasing HO-1 expression. Both in vitro and in vivo , PCPS exhibited more potent antioxidant activity than PCPC. CONCLUSION Overall, the results suggest that PCPS has a stronger effect on the prevention of oxidative damage by activating Nrf2/HO-1 antioxidant signaling. This study demonstrates the role of steam-processed P. cyrtonema rhizome and provides valuable perspective for PCPS as a functional agent. © 2022 Society of Chemical Industry.
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高影响因子
FOOD CHEMISTRY
·
2021
·
IF 7.514
Dan Bu,Zong-cai Tu,Hui Wang,Yue-ming Hu,Qing Sun,Guang-xian Liu
The mechanism of d -allose in reducing the allergenicity and digestibility of ultrasound-pretreated α-lactalbumin (α-LA) was studied. The intensity reduction and peak red shift occurred in fluorescence spectra of glycated samples. Enzyme-linked immunosorbent assay and basophil degranulation analysis showed that d -allose significantly reduced the allergenicity of α-LA, and ultrasound-pretreated α-LA showed the lowest allergenicity after glycation. Compared with α-LA, the degree of hydrolysis decreased in glycated samples. Size-exclusion high-performance liquid chromatography showed that the glycated α-LA was resistant to digestive enzymes. The glycated sites and average degree of substitution per peptide molecule were determined using LC Orbitrap MS/MS. These results suggested that the masking of linear allergenic epitopes by glycation could reduce the allergenicity. Therefore, the combination of ultrasound pretreatment and glycation is a potential method to reduce protein allergenicity in food processing and provides a useful approach for the application of rare sugars in food processing.
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Advanced Healthcare Materials
·
2023
·
IF 10
Pengfei Sun,Wan Yang,Jiarong He,Liuliang He,Pengfei Chen,Wenjuan Xu,Qingming Shen,Daifeng Li,Quli Fan
Cancer seriously affects the quality of life of patients with the disease. Synergistic chemotherapy and photothermal therapy (PTT) have emerged as a promising anticancer paradigm to achieve expected therapeutic effects while mitigating side effects. However, the chemo/PTT combination therapy suffers from limited penetration depth, thermo-resistance performance of tumor cells, and low drug bioavailability. Herein, we developed multifunctional nanoparticles (BTP/DOX/2DG NPs) coloaded with near-infrared region II (NIR-II) light excitation donor–acceptor–donor (D-A-D) small molecules, doxorubicin (DOX), and 2-deoxy-D-glucose (2-DG) for reinforced starvation/chemo/NIR-II PTT combination therapy. Our synthesized phenylboronic acid (PBA)-modified water-soluble D-A-D molecule (BBT-TF-PBA) not only exhibits high binding ability to DOX and 2-DG through donor–acceptor coordination interactions PBA-diol bonds but also serve as a photoactive agent for NIR-II fluorescence imaging, NIR-II photoacoustic imaging, and NIR-II PTT. Under the acidic and oxidizing conditions in the tumor microenvironment, donor–acceptor coordination interactions and PBA-diol bond are decomposed, simultaneously releasing DOX and 2-DG from BTP/DOX/2DG NPs to achieve effective chemotherapy and starvation therapy. 2-DG also effectively inhibits the expression of heat shock protein and further enhances NIR-II PTT and chemotherapy efficiency. In vitro and in vivo experiments demonstrated the combination effect of BTP/DOX/2DG NPs for chemotherapy, NIR-II PTT, and starvation therapy. This article is protected by copyright. All rights reserved
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Advanced Healthcare Materials
·
2024
·
IF 10
Yixuan Xu,Huiping Dang,Changchang Teng,Dalong Yin,Lifeng Yan
Rapid propagation of tumor cells requires plenty of energy, which is adenosine triphosphate (ATP) dependent. ATP inhibition in tumors not only results in the starvation of tumor cells but also down-regulation of the level of heat shock proteins (HSPs), which usually increase during traditional photothermal therapy (PTT), especially when the temperature is up 50 °C. 2-deoxy-D-glucose (2DG) is an anti-glycolytic reagent and can be used as an efficient agent for ATP inhibition in tumors. Compared with typical PTT, low-temperature mild photothermal therapy (MPTT) is receiving more and more attention because it avoids the high temperatures causing damage to the normal tissue, and the increase of HSPs which decrease PTT. Here, multifunctional polypeptide nanoparticles pDG@Ahx conjugating both a NIR probe Ahx-BDP and 2DG into the side chain of the amphiphilic polypeptide have been prepared. In vitro and in vivo studies reveal that the as-prepared nanoparticles achieve a synergistic effect of starvation/MPTT/PDT (photodynamic therapy), and it provides a new strategy to NIR-I/II fluorescence imaging-guided starvation/MPTT/PDT synergy therapy for tumors.
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Materials
·
2016
·Vol. 9
·期 11
·913
·
IF 2.728
Guihua Cui,Zhengguo Gao,Nannan Qiu,Toshifumi Satoh,Toyoji Kakuchi,Qian Duan
Regioselective modification ofd-glucosamine (2-amino-2-deoxy-d-glucopyranose, GA) through C-1 and C-2 positions to synthesized thermo-responsive D-Glucosamine-poly(N-iso-propylacrylamide) (PNIPAM) via atom transfer radical polymerization (ATRP) was investigated for the first time. Two different schemes of the synthesis for GA derivatives (GA-PNIPAM (i) and (ii)) with well-defined structures using 3,4,6-tri-o-acetyl-2-deoxy-2-phthalimido-β-d-glucopyranose and 1,3,4,6-tetra-o-acetyl-2-amino-2-deoxy-β-d-glucopyranose intermediates were examined. The GA-PNIPAM (ii) had an amino at C-2 position, while there was a hydroxyl in GA-PNIPAM (i) at this position. Both the resulting oligomers (i) and (ii) had a narrow dispersity, and no significant cytotoxic response of copolymers (i) and (ii) was observed in the cell line over the concentration range from 0.1 μg/mL to 1000 μg/mL at any of the exposure times. In addition, it was discovered that GA-PNIPAM (i) and (ii) inhibited the proliferation of Human Hepatocellular Carcinoma Cells HepG2 as the concentration and the time changed, and the inhibitory activity of polymer (ii) was higher than that of he (i). The results suggest that the GA-PNIPAM polymers show excellent biocompatibility in vitro.Keywords:poly(N-isopropylacrylamide) (PNIPAM);d-glucosamine (GA);atom transfer radical polymerization (ATRP);lower critical solution temperature (LCST)
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ACTA PHYSICO-CHIMICA SINICA
·
2026
·
IF 13.5
Baogang Fu,Nan Su,Jianmin Luo,Yun Wang,Bo Hu,Liang Cheng,Hongjun Dong,Chunmei Li
SCN-AP with a D-π-A network was synthesized via sulfur doping and pyridine grafting. • SCN-AP achieves integrated design of 1 O 2 generation and kinetic matching of ORR/WOR. • SCN-AP boosts ·O 2 - / 1 O 2 generation, with a H 2 O 2 yield of 1030 μmol g -1 within 2 h. • Antibacterial assays verify the photoactivated antibacterial potential of SCN-AP. • In-situ XPS and DRIFTS characterize photogenerated electron flow and reaction intermediates. Photocatalytic H 2 O 2 synthesis is commonly dominated by the oxygen reduction reaction (ORR), whereas simultaneously enabling water oxidation reaction (WOR) and directional charge separation through band-structure regulation remains challenging. Herein, sulfur doping and pyridine modification were integrated to construct an intramolecular donor- π -acceptor (D- π -A) network within the carbon nitride framework. The resulting electronic polarization promotes directional separation of photogenerated charge carriers and optimizes the band structure to thermodynamically enable both ORR and WOR pathways. Consequently, the as-synthesized SCN-AP photocatalyst achieves an H 2 O 2 yield of 1030 μmol g -1 within 2 h in pure water, 3.73 times that of pristine PCN, and exhibits effective antibacterial activity against clinically relevant pathogens including Acinetobacter beijerinckii and Klebsiella variicola . The in-situ electron paramagnetic resonance (EPR) spectroscopy and in-situ diffuse reflectance infrared Fourier transform spectroscopy (DRIFTS) collectively support the coexistence of ORR and WOR pathways. The ORR serves as the predominant route and involves a ·O 2 - -mediated stepwise reduction pathway together with a 1 O 2 -associated pathway, while WOR provides a complementary hole-driven contribution to H 2 O 2 formation. This work demonstrates a feasible band-engineering strategy for constructing polymeric photocatalysts with directional charge transfer and dual-pathway H 2 O 2 photosynthesis. This work demonstrates a D-π-A-mediated electronic polarization strategy that directs charge migration in carbon nitride, enabling dual-pathway H 2 O 2 photosynthesis through coupled ORR and WOR processes. Download: Download high-res image (411KB) Download: Download full-size image
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