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ACS Sustainable Chemistry & Engineering · 2020 · IF 7.632

Highly Selective Conversion of Furfural to Furfural Alcohol or Levulinate Ester in One Pot over ZrO2@SBA-15 and Its Kinetic Behavior

Junhua Zhang,Yao Liu,Shibo Yang,Junnan Wei,Liang He,Lincai Peng,Xing Tang,Yonghao Ni

Biorefinery for the purpose of producing biofuels, chemicals, and materials has received much attention. Furfural alcohol (FOL) and levulinate ester (LE) are important biomass-derived platform chemicals, and they are produced from sugar-based furfural (FAL). Unfortunately, the two products are often obtained separately in different reaction systems, which is undesirable; furthermore, it is of significant practical interest to control their selectivity so that the desired product can be accumulated in high yields. Herein, we present an efficient method for the highly selective conversion of FAL to FOL or isopropyl levulinate (IPL) in a one pot system using isopropanol as the hydrogen source and ZrO2@SBA-15 as a bifunctional catalyst with both Lewis acid and Brønsted acid sites. Under optimized reaction conditions, high yields of FOL and IPL in up to 90.4% and 87.2%, respectively, were obtained. Based on the experimental results, a kinetic model describing the catalytic conversion of FAL into FOL and IPL process has been established, which has a good correlation (R2 > 0.92) between the measured and predicted data. The developed kinetics can provide an effective tool to monitor the process and tailor the process conditions to obtain the desired product.

CAS / MDL: 7789-75-5 59-30-3
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MICROCHEMICAL JOURNAL · 2020 · IF 3.594

A novel water pollution monitoring and treatment agent: Ag doped carbon nanoparticles for sensing dichromate, morphological analysis of Cr and sterilization

Bo Hu,Yong Ma,Ning Wang

Drinking water shortage is a worldwide issue, so that the quality control and treatment of industrial sewage is very important. In this present work, Ag doped carbon nanoparticles (Ag-CDs) were prepared by a simple hydrothermal method, which could be used as an antibacterial and simultaneous detection of dichromate (Cr 2 O 7 2− ). The prepared Ag-CDs were characterized through high resolution transmission electron microscopy (HRTEM), fourier transform infrared spectroscopy (FTIR), X-ray photoelectron spectroscopy (XPS), X-ray diffraction (XRD) and thermogravimetric analysis (TGA). The characterization results indicated that the diameter of Ag-CDs were distributed in a range of 2.6–6.0 nm (ca. 4.25 nm) with the functional groups such as OH, NH 2 and CONH in the structure. Cr 3+ and Cr 2 O 7 2− could be distinguished under 365 nm UV light or fluorospectrophotometer. The Ag-CDs nanoparticles was also applied to the detection of Cr 2 O 7 2- in real water samples. There exhibits excellent antibacterial performance to both Escherichia coli O157:H7 ( E. coli O157:H7) and Staphylococcus aureus ( S. aureus ) for Ag-CDs nanoparticles. E. coli O157:H7 or S. aureus was deal with 2 μg mL −1 of Ag-CDs nanoparticles under 5 min with a killing rate of 100%, respectively. As a novel dichromate-sensitive antibacterial, the Ag-CDs nanoparticles hold great promise to broaden application in the environment pollution and water purification.

CAS / MDL: 59-30-3
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ACS Applied Bio Materials · 2020 · IF 0

MRI Enhancement and Tumor Targeted Drug Delivery Using Zn2+-Doped Fe3O4 Core/Mesoporous Silica Shell Nanocomposites

Weijun Fang,Wenjuan Zhu,Hu Chen,Hanyuan Zhang,Shi Hong,Wenmei Wei,Tingting Zhao

Developing of multifunctional nanoplateforms for simultaneous accurate cancer detection and target therapy is essential in cancer treatment. Herein, we present a facile synthesis of DOX/MNPs-FA nanocomposites for high-performance MRI and tumor-targeted drug delivery. In such core–shell structured DOX/MNPs-FA nanocomposite, the high magnetism of iron oxide core can be tuned and achieved by controlling the Zn2+ dopant amount, making them suitable as excellent contrasts in T2-weighted MR imaging. The outer porous silica shell with large pores about 5.4 nm in diameter possesses high surface area and pore volume. Anticancer drug (DOX molecules) can be stored in the large pore channels and is triggered to be released under acidic condition (pH 4–6). Importantly, the presence of folic acid on the surface of DOX/MNPs-FA allows the targeted delivery of the DOX to tumor cells, and therefore improves tumor chemotherapy efficiency. Our in vitro studies also demonstrated that DOX/MNPs-FA could be efficiently internalized into HeLa cells via the folate receptor-mediated endocytosis, and generate a greater cytotoxicity toward cancer cells compared to free DOX and DOX/MNPs. Therefore, these DOX/MNPs-FA multifunctional nanocomposites have great potential applications for simultaneous tumor diagnosis and targeted chemotherapy.

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Journal of Materials Chemistry B · 2020 ·Vol. 8 ·期 11 ·2307-2320 · IF 5.344

Novel β-1,3-D-glucan porous microcapsule enveloped folate-functionalized liposomes as a Trojan horse for facilitated oral tumor-targeted co-delivery of chemotherapeutic drugs and quantum dots

Xiaonan Li,Ziming Zhao,Yihua Yang,Zhaorong Liu,Jinglei Wang,Yalu Xu,Yanzhuo Zhang

In this study, a new type of β-1,3-D-glucan porous microcapsule (GPM)-enveloped and folate conjugated chitosan-functional liposome (FCL), FCL@GPM, was developed for the potential oral co-delivery of chemotherapeutic drugs and quantum dots (QDs) with facilitated drug absorption and antitumor efficacy. In this dual-particulate system, multiple FCLs serve as the cores for effective loading, folate-mediated tumor-targeting, facilitated intracellular accumulation, and pH-responsive controlled release of chemotherapeutic agents, while a GPM acts as the shell for affording macrophage-mediated tumor selectivity. Gefitinib (GEF) was selected as a chemotherapeutic agent, while acid degradable ZnO QDs were selected due to their dual role as an anticancer agent for synergistic chemotherapy and as a fluorescent probe for potential cancer cellular imaging. The GEF and ZnO QD co-loaded FCL@GPMs (GEF/ZnO-FCL@GPMs) exhibited a prolonged release manner with limited release before uptake by intestinal cells. Furthermore, Peyer's patch uptake, macrophage uptake, cytotoxicity, and biodistribution of FCL@GPMs were tested. In addition, GEF and ZnO QD co-loaded FCLs (GEF/ZnO-FCLs) not only have a tumor acidity responsive release property, but also induce a superior cytotoxicity on cancer cells as compared to GEF. Moreover, a 1.75-fold increase in the bioavailability of GEF delivered from GEF/ZnO-FCL@GPMs as compared to its trademarked drug (Iressa®). As a result, GEF/ZnO-FCL@GPMs exerted a superior antitumor efficacy (1.47-fold) as compared to the trademarked drug in mice. Considered together, the developed FCL@GPMs, combining the unique physicochemical and biological benefits of FCLs and GPMs, possess great potential as an efficient delivery system for the co-delivery of chemotherapeutic agents and quantum dots.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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MOLECULAR PHARMACEUTICS · 2020 · IF 4.321

Folic Acid-Modified Nanoerythrocyte for Codelivery of Paclitaxel and Tariquidar to Overcome Breast Cancer Multidrug Resistance

Ping Zhong,Xuehong Chen,Rishuo Guo,Xiaomei Chen,Zhihao Chen,Cui Wei,Yusheng Li,Wanting Wang,Yi Zhou,Linghao Qin

The efflux of anticancer agents mediated by P-glycoprotein (P-gp) is one of the main causes of multidrug resistance (MDR) and eventually leads to chemotherapy failure. To overcome this problem, the delivery of anticancer agents in combination with a P-gp inhibitor using nanocarrier systems is considered an effective strategy. On the basis of the physiological compatibility and excellent drug loading ability of erythrocytes, we hypothesized that nanoerythrocytes could be used for the codelivery of an anticancer agent and a P-gp inhibitor to overcome MDR in breast cancer. Herein, a folic acid-modified nanoerythrocyte system (PTX/TQR NPs@NanoRBC-PEG/FA) was prepared to simultaneously transport paclitaxel and tariquidar, and the in vitro and in vivo characteristics of this delivery system were evaluated through several experiments. The results indicated that the average diameter and surface potential of this nanocarrier system were 159.8 ± 1.4 nm and −10.98 mV, respectively. Within 120 h, sustained release of paclitaxel was observed in both pH 6.5 media and pH 7.4 media. Tariquidar release from this nanocarrier suppressed the P-gp function of MCF-7/Taxol cells and significantly increased the intracellular paclitaxel level (p < 0.01 versus the PTX group). The results of the MTT assay indicated that the simultaneous transportation of paclitaxel and tariquidar could significantly inhibit the growth of MCF-7 cells or MCF-7/Taxol cells. After 48 h of incubation with PTX/TQR NPs@NanoRBC-PEG/FA, the viability of MCF-7 cells and MCF-7/Taxol cells decreased to 7.37% and 30.2%, respectively, and the IC50 values were 2.49 μM and 6.30 μM. Pharmacokinetic results illustrated that, compared with free paclitaxel, all test paclitaxel nanoformulations prolonged the drug release time and showed similar plasma concentration–time profiles. The peak concentration (Cmax), area under the curve (AUC0–∞), and half-life (t1/2) of PTX/TQR NPs@NanoRBC-PEG/FA were 3.33 mg/L, 6.02 mg/L·h, and 5.84 h, respectively. Moreover, this active targeting nanocarrier dramatically increased the paclitaxel level in tumor tissues. Furthermore, compared with those of the other paclitaxel formulations, the cellular reactive oxygen species (ROS) and malondialdehyde (MDA) levels of the PTX/TQR NPs@NanoRBC-PEG/FA group increased by 1.38-fold (p < 0.01) and 1.36-fold (p < 0.01), respectively, and the activities of superoxide dismutase (SOD) and catalase (CAT) decreased to 67.8% (p < 0.01) and 65.4% (p < 0.001), respectively. More importantly, in vivo antitumor efficacy results proved that the PTX/TQR NPs@NanoRBC-PEG/FA group exerted an outstanding tumor inhibition effect with no marked body weight loss and fewer adverse effects. In conclusion, by utilizing the inherent and advantageous properties of erythrocytes and surface modification strategies, this biomimetic targeted drug delivery system provides a promising platform for the codelivery of an anticancer agent and a P-gp inhibitor to treat MDR in breast cancer.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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CHEMICAL ENGINEERING JOURNAL · 2020 · IF 10.652

Polyamide@Ag coralloid nanoarrays with 3D high-density hot spots for ultrasensitive SERS sensing

Yi Li,Lu Yu,Jiansheng Li,Lianjun Wang,Rui Lu

The preparation of surface-enhanced Raman scattering (SERS) substrate with both structural stability and SERS activity under extreme pH conditions faces several problems, including tedious preparation, time consuming processes, high cost, and the need for professional equipment and personnel. Herein, a facile preparation protocol for a large-scale nanoarray film substrate was developed for multi-purpose SERS sensing. Through a simple self-assembly process under specific conditions, well-ordered, highly sensitive, structurally tunable, acid-alkali resistant and disposable “polyamide@Ag” coralloid nanoarrays were fabricated. Due to the dense distribution of AgNPs on the top and side surfaces of the nanoarrays and optimized geometric construction, a large number of controllable Raman “hotspots” formed in the space, resulting in excellent Raman signal uniformity and SERS performance for Rhodamine 6G. To evaluate the potential application of this flexible substrate, it was implemented in the label-free trace determination of folic acid with a limit of detection as low as 5.24 × 10 −12 M. Importantly, the as-prepared polyamide@Ag nanoarrays exhibited high structural stability over a wide pH range from 1.25 to 12.00, which is beneficial for the detection of non-pH-neutral samples. The results demonstrated that this hybrid substrate has broad application prospects in fields as diverse as biosensing and environmental monitoring.

CAS / MDL: 58-61-7 59-30-3 298-00-0
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International Journal of Nanomedicine · 2020 · IF 5.115

Folate-Mediated Targeted Delivery of siPLK1 by Leucine-Bearing Polyethylenimine

Lu Hou,Zheyu Song,Zhonghang Xu,Yuanyu Wu,Wei Shi

Background siRNA-mediated polo-like kinase 1 (PLK1) silencing has been proposed as a promising therapeutic method for multiple cancers. However, the clinic application of this method is still hindered by the low specific delivery of siPLK1 to desired tumor lesions. Herein, folate (FA)-modified and leucine-bearing polyethylenimine was successfully synthesized and showed excellent targeted silencing to folate receptor overexpressed cells. Materials and Methods The condensation of siPLK1 by FA-N-Ac-L-Leu-PEI (NPF) was detected by the gel retardation assay. The targeted and silencing efficiency was evaluated by flow cytometry and confocal laser scanning microscope. The PLK1 expressions at gene or protein levels were detected by quantitative real-time PCR and Western blotting assay. Further impacts of the PLK1 silencing on cell viability, cell cycle, migration, and invasion were studied by MTT, colony formation, wound healing and transwell assays. Results The NPF and siPLK1 could efficiently assemble to stable nanoparticles at a weight ratio of 3.0 and showed excellent condensation and protection effect. Owing to the FA-mediated targeted delivery, the uptake and silencing efficiency of NPF/siPLK1 to SGC-7901 cells was higher than that without FA modification. Moreover, NPF-mediated PLK1 silencing showed significant antitumor activity in vitro. The anti-proliferation effect of PLK1 silencing was induced via the mitochondrial-dependent apoptosis pathway with the cell cycle arrest of 45% at G2 phase and the apoptotic ratio of 28.3%. Conclusion FA-N-Ac-L-Leu-PEI (NPF) could generate targeted delivery siPLK1 to FA receptor overexpressed cells and dramatically downregulate the expression of PLK1 expression.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2020 · IF 5.162

Biochemical characterization and evolutionary analysis of a novel pectate lyase from Aspergillus parasiticus

Guojun Yang,Wei Chen,Haidong Tan,Kuikui Li,Junyan Li,Heng Yin

In this study, a novel pectate lyase ( Ap Pel1) was identified and characterized from Aspergillus parasiticus . The Ap Pel1 hydrolysed oligogalacturonides (OGs) effectively and produced 4,5-unsaturated OGs from low-methoxyl (LM) pectin, with DP 2 to DP 5 as the major products. Furthermore, the multiple sequence alignments , structure model and phylogenetic analyses of the Ap Pel1 indicated that its catalytic active sites were highly conserved with other pectin lyases (PLs) and the Ca 2+ binding amino acid residues are different compared with pectate lyases (Pels). N187D, N191D and N187D/N191D mutants were constructed to test for both Ca 2+ binding properties and the effects on catalytic ability. The three mutations sharply decreased the activity of Ap Pel1 and Ca 2+ tolerance, indicating that the Ca 2+ binding amino acid residues are different from the other Pels. Based on the sequence and structure comparison between PLs and Pels, and mutation analysis, the Ap Pel1 may be direct evolution from PLs. Thus, this enzyme has potential for use in producing unsaturated OGs for biological activity study, and contributes to an improved understanding of the evolutionary relationships between PLs and Pels.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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BIOMATERIALS · 2020 · IF 10.317

A multifunctional anti-inflammatory drug that can specifically target activated macrophages, massively deplete intracellular H2O2, and produce large amounts CO for a highly efficient treatment of osteoarthritis

Guangzhen Yang,Mengni Fan,Jingwu Zhu,Chen Ling,Lihuang Wu,Xin Zhang,Ming Zhang,Jiayi Li,Qingqiang Yao,Zhongwei Gu,Xiaojun Cai

Specifically inhibiting the proliferation of activated macrophages and clearing the high levels of reactive oxygen species (ROS) secreted by macrophages is crucial for osteoarthritis (OA) treatment. Moreover, if the clearance of these high levels of ROS can be simultaneously used to induce oxidation-responsive release of anti-inflammatory drugs, the therapeutic effect of OA may be further improved. Here, a multifunctional anti-inflammatory drug (CPHs) based on a peptide dendrimer nanogel was constructed by physically encapsulating CORM-401 and wrapping its surface with folic acid (FA)-modified hyaluronic acid (HA). CPHs is capable of efficiently entering activated macrophages via FA- and HA-mediated specific targeting effects and then rapidly release large amounts of CO by massive consumption of H 2 O 2 . The generated CO effectively suppresses the secretion of interleukin (IL)-1β, IL-6, and tumor necrosis factor (TNF)-α by inhibiting cell proliferation ; inducing the activation of heme oxygenase (HO-1), and downregulating the expression of p38 MAPK , NF-kB (p50/p65) and TLR-2. In vivo experiments further confirmed that CPHs can massively deplete ROS in OA joints and effectively suppress the degradation of articular cartilage and their extracellular matrix. More importantly, CPHs is non-toxic to normal macrophages, and the high levels of CO generated in the joints do not result in notable changes in the HbCO levels in blood. Together, these results show that CPHs is an effective and safe anti-inflammatory drug and has essential application prospects in OA treatment.

CAS / MDL: 59-30-3 305-53-3
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npj Biofilms and Microbiomes · 2020 ·Vol. 6 ·期 1 ·1-12 · IF 7.067

IolR, a negative regulator of the myo-inositol metabolic pathway, inhibits cell autoaggregation and biofilm formation by downregulating RpmA in Aeromonas hydrophila

Dong Yuhao,Li Shougang,Zhao Dan,Liu Jin,Ma Shuiyan,Geng Jinzhu,Lu Chengping,Liu Yongjie

Aeromonas hydrophila is the causative agent of motile Aeromonad septicemia in fish. Previous studies have shown that the myo -inositol metabolism is essential for the virulence of this bacterium. IolR is a transcription inhibitor that negatively regulates myo -inositol metabolic activity. While in the process of studying the inositol catabolism in A. hydrophila Chinese epidemic strain NJ-35, we incidentally found that ΔiolR mutant exhibited obvious autoaggregation and increased biofilm formation compared to the wild type. The role of surface proteins in A. hydrophila autoaggregation was confirmed by different degradation treatments. Furthermore, calcium promotes the formation of aggregates, which disappear in the presence of the calcium chelator EGTA. Transcriptome analysis, followed by targeted gene deletion, demonstrated that biofilm formation and autoaggregation caused by the inactivation of iolR was due to the increased transcription of a RTX-family adhesion gene, rmpA . Further, IolR was determined to directly regulate the transcription of rmpA . These results indicated that iolR is negatively involved in autoaggregation and biofilm formation in A. hydrophila , and this involvement was associated with its inhibition on the expression of rmpA .

CAS / MDL: 59-30-3 2682-20-4
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS · 2020 · IF 3.99

A pH-sensitive drug delivery system based on folic acid-targeted HBP-modified mesoporous silica nanoparticles for cancer therapy

Yan Li,Shuai Wang,Fang Xiang Song,Li Zhang,Wei Yang,Hong Xia Wang,Qian Lin Chen

Mesoporous silica nanoparticles with folic acid (MSN−COOH-Tet-HBP-FA) are able to mediate targeting and have a pH stimulation response character, and therefore have been successfully synthesized as vectors for antitumor drug delivery. The model drug is tetrandrine (Tet). The chemical structure and properties of these NPs were characterized through systematic characterization analyses. Their drug loading capacity was significantly improved through carboxy modification (26.86 % in max), and they exhibited pH-dependent drug release profiles("zero pre-release" within 20 h in a normal physiological environment). In vitro cytotoxicity and cell uptake of the as-synthesized NPs in Hela and A549 cells were also evaluated, and exhibited high cytotoxicity and cell-targeted uptake capacity. It was concluded that MSN−COOH-Tet-HBP-FA could be used as a promising drug delivery system for cancer therapy.

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NEW JOURNAL OF CHEMISTRY · 2020 ·Vol. 44 ·期 6 ·2578-2586 · IF 3.288

Tumor microenvironment responsive mesoporous silica nanoparticles for dual delivery of doxorubicin and chemodynamic therapy (CDT) agent

Yuan Zhang,Omer Eltayeb,Yating Meng,Guomei Zhang,Yan Zhang,Shaomin Shuang,Chuan Dong

Chemodynamic therapy is a new antitumor strategy triggered by transition metal as chemodynamic agent via the in situ catalytic Fenton reaction. Herein, we engineer a smart nanocarrier activated by tumor microenvironment-specific weak acidic pH and high glutathione conditions for chemo/chemodynamic processes. This unique architecture orderly consists of mesosilica-encapsulated doxorubicin, self-polymerization of polydopamine Fe3+ clathrate, further bonding the targeting polymer MnO2 disguised albumin–folic acid. Polydopamine and albumin as intelligent nanovalves shield doxorubicin from premature leaking. Folic acid improves the targeting capability for folate receptor (FR) overexpressing cancer cells. After intake of the nanocarrier by tumor cells, the nanocarrier nanovalves are first biodegraded by native glutathione and pH, enabling on-demand anticancer drug escape, and also generate and release Fe3+ and Mn2+ (reduced by MnO2via glutathione depletion). Subsequently, the ions interact with H2O2, generating highly toxic hydroxyl radicals (˙OH) via a Fenton-like reaction to enhance the anticancer cell efficacy. This result proves that the designed nanocarrier more likely devours into FR-positive cancer cells and illustrates a high intracellular ˙OH generation, leading to the desired specific killing efficacy. We believe this innovative strategy will exhibit a new avenue for the potential of accurate chemo/chemodynamic co-therapy in cancer cells.

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