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JOURNAL OF MEDICINAL CHEMISTRY · 2023 · IF 7.3

Identification of Novel Quinolin-2(1H)-ones as Phosphodiesterase 1 Inhibitors for the Treatment of Inflammatory Bowel Disease

Bei Zhang,Yi-Yi Yang,Zheng-Jiong Zhao,Run-Duo Liu,Ling-Ling Feng,Mei-Yan Jiang,Yijun Yuan,Shuheng Huang,Zhe Li,Quan Wang,Hai-Bin Luo,Yinuo Wu

Phosphodiesterase 1 (PDE1) is a subfamily of PDE super enzyme families that can hydrolyze cyclic adenosine monophosphate and cyclic guanosine monophosphate simultaneously. Currently, the number of PDE1 inhibitors is relatively few, significantly limiting their application. Herein, a novel series of quinolin-2(1H)-ones were designed rationally, leading to compound 10c with an IC50 of 15 nM against PDE1C, high selectivity across other PDEs, and remarkable safety properties. Furthermore, we used the lead compound 10c as a chemical tool to explore whether PDE1 could work as a novel potential target for the treatment of inflammatory bowel disease (IBD), a disease which is a chronic, relapsing disorder of the gastrointestinal tract inflammation lacking effective treatment. Our results showed that administration of 10c exerted significant anti-IBD effects in the dextran sodium sulfate-induced mice model and alleviated the inflammatory response, indicating that PDE1 could work as a potent target for IBD.

✓ 已验证 DOI PubMed 高影响因子
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ZEITSCHRIFT FUR NATURFORSCHUNG SECTION B-A JOURNAL OF CHEMICAL SCIENCES · 2017 ·Vol. 72 ·期 4 ·257-261 · IF 0.631

Two copper(II) coordination polymers constructed by bis(4-(1H-imidazol-1-yl)phenyl)methanone and dicarboxylate ligands

Gao-Feng Wang,Xiao Zhang,Shu-Wen Sun,Hong Sun,Hui Li,Hui-Xuan Ma,Yu-Peng Tang,Xiao-Na Gao,Lei Yang

Two new copper(II) complexes, {[Cu(bipmo)(npa)]} n ( 1 ) and {[Cu(bipmo)(pa)]} n ( 2 ) (bipmo=bis(4-(1 H -imidazol-1-yl)phenyl)methanone), were synthesized by solvothermal methods and structurally characterized by elemental analyses, infrared spectroscopy, and single-crystal X-ray diffraction. The results from single-crystal X-ray diffraction data indicate that the solid state structures of 1 and 2 consist of neutral metal aromatic carboxylate layers, which are pillared by the weak interactions to generate 3D architectures. The topological structures of 1 and 2 are uninodal nets based on 4-connected nodes with the Schläfli symbol of (6 5 ·8).

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Bioanalysis · 2015 ·Vol. 7 ·期 9 · IF 3.003

Simple and rapid determination of unsaturated fatty acids in 1 µl of rat plasma by LC–MS/MS

Shirui Zheng,Zhiyuan Ma,Feifeng Song,Jianfeng Ye,Ruwei Wang,Meijuan Tu,Liping Li,Hui Zhou,Su Zeng,Huidi Jiang

Background: Deficiency or imbalance of unsaturated fatty acids will promote the pathogenesis of many diseases. In order to monitor the exposure of unsaturated fatty acids, the method based on LC–MS/MS was developed. Results: Standard calibration curves for α-linolenic acid, linoleic acid, palmitoleic acid and oleic acid were linear (r ≥0.99). The intra-and interbatch accuracy (RE%) ranged from -4.5 to 8.6%, while the intra- and interbatch precisions (RSD%) were ≤8.7%. The extraction recovery varied from 85.4 to 99.6%, and no obvious matrix effect was observed. Conclusion: The method offers a simple approach for measuring 4 unsaturated fatty acids in 1 μl rat plasma within 3.95 min.

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JOURNAL OF CHEMICAL SCIENCES · 2020 ·Vol. 132 ·期 1 ·1-14 · IF 1.406

trans-4-[4-(Dimethylamino)styryl]-1-methylpyridinium iodide@cyclopentanocucurbit[6]uril as a fluorescent probe for anion recognition

Cheng Si Yuan,Yang Xi Nan,Tao Zhu,Wei Lian Tong,Zhao Wei Wei,Jiang Dao Fa,Jin Yan Mei,Gao Jie,Ma Pei Hua

Abstract The host–guest binding characteristics of cyclopentanocucurbit[6]uril (CyP 6 Q[6]) and cyanine dye trans -4-[4-(dimethylamino)styryl]-1-methylpyridinium iodide ( t -DSMI) have been studied. The results show that CyP 6 Q[6] and t -DSMI form a 1:1 inclusion system, generating strong fluorescence. On this basis, the fluorescent probe t -DSMI@CyP 6 Q[6] has been constructed, and its anion recognition ability has been investigated. In a neutral environment, BF 4 − , H 2 PO 4 − , and I − elicit obvious specific responses from the probe, since they have stronger binding forces. This probe shows greater sensitivity than the previously reported probe t -DSMI@HMeQ[6]. Graphic abstract Since the complex formed by CyP 6 Q[6] and t -DSMI can produce strong fluorescence at pH > 4.6, t -DSMI@CyP 6 Q[6] was constructed to recognize the anions at pH  ≅  5. The results show that in a near neutral environment, BF 4 − , H 2 PO 4 − , and I − elicit obvious specific responses from the probe.

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ACS Applied Materials & Interfaces · 2017 · IF 7.504

Self-Assembly of 1-Pyrenemethanol on ZnO Surface toward Combined Cathode Buffer Layers for Inverted Polymer Solar Cells

Xiang Cai,Tao Yuan,Xiangfu Liu,Guoli Tu

Solid alcohol 1-pyrenemethanol (PyM) was first introduced to modify the zinc oxide (ZnO) layer which is used in the inverted polymer solar cells (PSCs) as a cathode buffer layer (CBL). As a low-cost industrial product, the PyM can modify the surface defects and improve the electron mobility of ZnO CBL, which can be attributed to the self-assembly of PyM on the ZnO surface due to the hydrogen bonds and the conjugated structure in PyM. With a blend of PTB7:PC71BM as active layer, the device with ZnO/PyM CBL exhibited a notable power conversion efficiency (PCE) of 8.26%, which is better than that of control devices based on bare ZnO CBL (7.26%). With the addition of PyM, the device based on PTB7-Th:PC71BM showed a higher PCE of 9.10%, an obvious improvement from the 7.79% of control devices. There was no obvious change in device performance with the increase of PyM solution concentration, indicating that the device fabrications are thickness-insensitive. These results could be particularly useful in solution processing of buffer layer materials to high-efficiency organic solar cells.

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Journal of Materials Chemistry A · 2013 ·Vol. 1 ·期 35 ·10292-10299 · IF 0

A MOF/graphite oxide hybrid (MOF: HKUST-1) material for the adsorption of methylene blue from aqueous solution

Ling Li,Xiao Lan Liu,Hong Yun Geng,Bin Hu,Gong Wu Song,Zu Shun Xu

The adsorption of methylene blue (MB) from aqueous solution on a HKUST-1/GO (MOFs : HKUST-1) composite was studied in view of the adsorption isotherm, kinetics and regeneration of the sorbent. The adsorption isotherms of methylene blue (MB) on the HKUST-1/GO composite followed both the Freundlich isotherm and the Langmuir isotherm. Adsorption kinetics and thermodynamic parameters were determined from the experimental data. The used HKUST-1/GO could be regenerated by acetone, so it can be recycled for reuse. The high adsorption capacity and excellent reusability make HKUST-1/GO attractive for the removal of MB from aqueous solution.

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Biosensors-Basel · 2023 ·Vol. 13 ·期 7 ·723 · IF 5.4

Streptavidin-Conjugated DNA for the Boronate Affinity-Based Detection of Poly(ADP-Ribose) Polymerase-1 with Improved Sensitivity

Fengli Gao,Gang Liu,Yishu Qiao,Xiuwen Dong,Lin Liu

This work reports the development of a fluorescence method for the detection of poly(ADP-ribose) polymerase-1 (PARP1), in which a phenylboronic acid-modified fluorescein isothiocyanate dye (FITC-PBA) was used to recognize the formed poly(ADP-ribose) (PAR) polymer. The detection system was designed by conjugating recombinant streptavidin (rSA) with PARP1-specific double-stranded DNA (dsDNA) through streptavidin–biotin interaction. Capture of PARP1 via rSA–biotin–dsDNA allowed for the poly-ADP-ribosylation (PARylation) of both rSA and PARP1 in a homogeneous solution. The resulting rSA–biotin–dsDNA/PAR conjugates were then captured and separated via the commercialized nitrilotriacetic acid–nickel ion-modified magnetic bead (MB-NTA-Ni) through the interaction between NTA–Ni on MB surface and oligohistidine (His6) tag in rSA. The PAR polymer could capture the dye of FITC-PBA through the borate ester interaction between the boronic acid moiety in PBA and thecis-diol group in ribose, thus causing a decrease in fluorescence signal. The PARylation of streptavidin and the influence of steric hindrance on PARylation efficiency were confirmed using reasonable detection strategies. The method showed a wide linear range (0.01~20 U) and a low detection limit (0.01 U). This work should be valuable for the development of novel biosensors for the detection of poly(ADP-ribose) polymerases and diol-containing species.Keywords:streptavidin;nitrilotriacetic acid;magnetic bead;poly(ADP-ribose) polymerase;boronic acid;immobilization-free

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ENERGY & FUELS · 2018 · IF 3.024

Mechanism and Kinetic Study of Carbon Dioxide Absorption into a Methyldiethanolamine/1-Hydroxyethyl-3-methylimidazolium Lysine/Water System

Wei Li,Shujing Wen,Li Shen,Yuchi Zhang,Cheng Sun,Sujing Li

In this work, the aqueous solutions of 1-hydroxyethyl-3-methylimidazolium lysine ([C2OHmim][Lys]) and methyldiethanolamine (MDEA) were developed to obtain an efficient absorbent for CO2 capture. The absorption performance, regeneration performance, reaction mechanism, and kinetic study of the blends were investigated. It was found that, for the blended absorbents, a molar ratio of 8:2 of MDEA/[C2OHmim][Lys] was the optimum ratio based on the absorption rate, absorption capacity, and other factors. The CO2 absorption capacity of the blends is 0.75 mol of CO2/mol of ionic liquid, and the absorption rate was higher than that of the aqueous MDEA solution. The regeneration efficiency of the blends was 93% after the third absorption generation cycle, which was higher than the aqueous solutions of 1 mol/L MDEA (88%) or 1 mol/L [C2OHmim][Lys] (88%) under the same conditions, indicating a better regeneration performance of the blends. The reaction mechanism and kinetic study of the CO2 absorption into the blends were investigated by 13C nuclear magnetic resonance and a double stirred-cell absorber, respectively. [C2OHmim][Lys] in aqueous solution first formed carbamate with CO2, and the next step was hydrolysis of MDEA and partial carbamate, with the production of bicarbonate. It also found that the influence of the temperature in the CO2 absorption was different in the two steps. Also, [C2OHmim][Lys] could promote the hydration reaction of MDEA and CO2 according to the chemical mechanism and kinetic study. The kinetic region was considered to be a fast pseudo-first-order reaction, and the activation energy of the blends was 40.0 kJ mol–1.

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BIOMATERIALS · 2022 · IF 15.304

Enhancement of anti-PD-1/PD-L1 immunotherapy for osteosarcoma using an intelligent autophagy-controlling metal organic framework

Yu-Xiang Ge,Tai-Wei Zhang,Lei Zhou,Wang Ding,Hai-Feng Liang,Zhi-Chao Hu,Qin Chen,Jian Dong,Feng-Feng Xue,Xiao-Fan Yin,Li-Bo Jiang

Poor immunogenicity and compromised T cell infiltration impede the application of immune-checkpoint blockade (ICB) immunotherapy for osteosarcoma (OS). Although autophagy is involved in enhancing the immune response, the synergistic role of autophagy in ICB immunotherapy and the accurate control of autophagy levels in OS remain elusive and challenging. Here, we designed a pH-sensitive autophagy-controlling nanocarrier, [email protected] @PEG-FA (CBZP), loading a natural derivative, curcumin (CUR), to boost the immunotherapeutic response of PD-1/PD-L1 blockade by activating immunogenic cell death (ICD) via autophagic cell death, and BMS1166 to inhibit the PD-1/PD-L1 interaction simultaneously, enhancing the tumor immunogenicity and sensitizing the antitumor T cell immunity. After entering tumor cells, the pH-sensitive nanoparticles induced autophagy and decreased the intracellular pH , which in turn further facilitated the release of CUR to enhance autophagic activity. Transferring CBZP to orthotopic OS tumor-bearing mice showed powerful antitumor effects and established long-term immunity against tumor recurrence, accompanied by enhanced dendritic cell maturation and tumor infiltration of CD8 + T lymphocytes. Collectively, CBZP exhibited synergistic effects in treating OS by combining ICD induction with checkpoint blockade, thereby shedding light on the use of autophagy control as a potential clinical therapy for OS.

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ANALYTICA CHIMICA ACTA · 2019 · IF 5.256

A magnetic SERS immunosensor for highly sensitive and selective detection of human carboxylesterase 1 in human serum samples

Jun Feng,Yajuan Xu,Wenyi Huang,Hongxing Kong,Yanqing Li,Hao Cheng,Lijun Li

Hepatocellular carcinoma (HCC) is a common and lethal cancer. New serum markers for detecting HCC are urgently needed. Human carboxylesterase 1 (hCE1) is an important member of the serine hydrolase superfamily and is closely related to the occurrence of HCC. It can be used as a good serum marker for early diagnosis of HCC. Here, we developed a surface enhanced Raman scattering (SERS)- based magnetic immunosensor that specifically recognizes and detects trace amounts of hCE1 in human serum via a sandwich structure consisting of a SERS tags, magnetic supporting substrates, and target antigen (hCE1). The SERS tags are 4-mercaptobenzoic acid (4-MBA)-labeled AgNPs, and the SERS supporting substrates are composed of a raspberry-like morphology of Fe 3 O 4 @SiO 2 @AgNPs magnetic nanocomposites surface-functionalized with a hCE1 antibody. The prepared SERS magnetic immunosensor exhibits excellent selectivity and extremely high sensitivity for hCE1 detection. The SERS signal and logarithm of hCE1 concentration presented a wide linear response range of 0.1 ng mL −1 to 1.0 mg mL −1 , and the detection limit of hCE1 was 0.1 ng mL −1 . The results indicate that the immunosensor can be used for the rapid determination of hCE1 in human serum without a complicated sample pre-treatment. Furthermore, the immunosensor has good reproducibility and stability, and has a promising prospect for the quantitative detection of other tumor markers in early clinical diagnosis.

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CATALYSIS LETTERS · 2022 ·Vol. 153 ·期 2 ·348-363 · IF 2.936

Synthesis of Ti-MWW Zeolite by Refluxing and Implanting Titanium Method and Further Application in 1-Hexene Epoxidation

Chu Jidong,Ge Zhijin,Peng Jiahui,Hu Hui,Guo Shujuan,Chen Xiaohui

The efficient and economic heteroatom-implanting method for MWW-type zeolite has been the focus of attention and needs further exploration. Ti incorporated MWW zeolite was synthesized by sequential treatment of boron-containing zeolite precursor. The catalysts were applied to the epoxidation of 1-hexene. The implanting titanium process was conducted under a mild condition with Ti(SO 4 ) 2 /NH 4 HF 2 /HNO 3 solution, and the product Ti-MWW precursors have framework titanium alone, the novel method is named as refluxing and implanting titanium method which integrates acid treatment and titanium incorporation into one step and reduces the consumption of time of this process into 1 h. A density functional theory was conducted to explain the formation mechanism of interlayer-expanded structure of Ti-MWW zeolite. Subsequently, Ti-MWW precursors were treated in modified reagent solution to obtain larger pore structure, which increase the conversion of 1-hexene from 20.45 to 62.96%. The catalytic performance of Ti-MWW zeolite in this work are superior to Ti-MWW zeolite synthesized by traditional dry-gel conversion method the conversion of 1-hexene of which was 4.2%. This novel method is a promising approach for the synthesis of high catalytic performance heteroatomic zeolite. Graphical abstract

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BIOMATERIALS · 2016 · IF 8.387

Mild photothermal therapy/photodynamic therapy/chemotherapy of breast cancer by Lyp-1 modified Docetaxel/IR820 Co-loaded micelles

WenTing Li,JinRong Peng,LiWei Tan,Jing Wu,Kun Shi,Ying Qu,XiaWei Wei,ZhiYong Qian

Patients suffering from cancer have benefited from combination therapy. Nanocarriers are the ideal candidates for combination therapy. In this study, we constructed docetaxel (DTX) loaded micellar nanomedicines co-loaded with near infrared (NIR) dye-IR820 for photothermal therapy (PTT)/photodynamic therapy (PDT)/chemotherapy of breast cancer. Lyp-1, a tumor homing peptide, was introduced into the nanosystems to construct the active targeting nanomedicine. In order to deliver IR820 to the tumor site and overcome its short lifetime in vivo , a PEI derivative—PCL-g-PEI was introduced. IR820 with negative charge was formed stable static interaction with the amine groups, meanwhile, the absorption of IR820 in the NIR region was weakened. It indicated that the nanosystem constructed in this study may provide an alternative candidate for mild PTT. By the evaluation of the photothermal conversion in vivo , we can confirm that IR820 has been successfully delivered and effectively accumulated in the tumor site. Furthermore, the tumor cells targeting and anticancer performances of this nanosystem have been studied in vitro and in vivo . The results demonstrated Lyp-1 modification has enhanced the tumor targeting delivery of DTX and IR820. By combining PTT and PDT, DTX nanomedicine efficiently inhibited the growth and metastasis of breast cancer in mice. This nanosystem is a promising candidate for combination therapy of breast cancer.

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