JOURNAL OF MEDICINAL CHEMISTRY
·
2021
·
IF 7.446
Yi-You Huang,Jinhui Deng,Yi-Jing Tian,Jinhao Liang,Xi Xie,Yue Huang,Jiaqi Zhu,Ziran Zhu,Qian Zhou,Xixin He,Hai-Bin Luo
Idiopathic pulmonary fibrosis (IPF) is a progressive lung disease, and its incidence rate is rapidly rising. However, effective therapies for the treatment of IPF are still lacking. Phosphodiesterase 4 (PDE4) inhibitors were reported to be potential anti-fibrotic agents, but their clinical use was hampered by side effects like emesis and nausea. Herein, structure-based hit-to-lead optimizations of natural mangostanin resulted in the novel and orally active PDE4 inhibitor 18a with potent inhibitory affinity (IC50 = 4.2 nM), favorable physico-chemical properties, and a different binding pattern from roflumilast. Emetic activity tests on dogs demonstrated that 18a cannot cause emesis even at an oral dose of 10 mg/kg, whereas rolipram had severe emetic effects at an oral dose of 1 mg/kg. Finally, the oral administration of 18a (10 mg/kg) exhibited comparable anti-pulmonary fibrosis effects with pirfenidone (150 mg/kg) in a bleomycin-induced IPF rat model, indicating its potential as a novel anti-IPF agent with improved safety.
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JOURNAL OF ORGANIC CHEMISTRY
·
2024
·
IF 3.3
Wenhao Wang,Daming Feng,Ping Zhang,Peng Huang,Chunhua Ge
A novel method for synthesizing substituted 4-chloroquinolines has been devised, utilizing a cascade reaction of N-aryl enaminones promoted by bis(trichloromethyl) carbonate (BTC) and triphenylphosphine oxide (TPPO). This approach features accessible starting materials, a broad substrate range, extensive functional group compatibility, gentle reaction conditions, and straightforward operation. Its versatility is evidenced by its facile scalability and suitability for late-stage derivatization. A plausible mechanism involving α-carbonylation, 6π-azaelectrocyclization, and dehydroxychlorination sequence is proposed.
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FISH & SHELLFISH IMMUNOLOGY
·
2023
·
IF 4.7
Pei-Hua Zheng,Yao-Peng Lu,Xiu-Xia Zhang,Ke-Er Luan,Ze-Long Zhang,Jia-Jun Li,Tong Xu,Jun-Tao Li,Jian-An Xian,Hui Guo,An-Li Wang
4-Nonylphenol (4-NP) is one of the common endocrine-disrupting chemicals (EDCs) in estuaries and coastal zones, which can exert detrimental effects on the physiological function of aquatic organisms . However, the molecular response triggered by 4-NP remains largely unknown in Pacific white shrimp ( Litopenaeus vannamei ). In this study, transcriptomic analysis was performed to investigate the underlying mechanisms of 4-NP toxicity in the hepatopancreas of L. vannamei . Nine RNA-Seq libraries were generated from L. vannamei at 0 h, 24 h, and 48 h following exposure to 4-NP. Compared with 0 h vs 24 h, 962 up- and 463 down-regulated differentially expressed genes (DEGs) were identified, indicating that many genes in L. vannamei were induced to resist adverse circumstances by 4-NP exposure. In contrast, 902 up- and 1027 down-regulated DEGs were revealed in the comparison of 0 h vs 48 h, demonstrating that prolonged exposure to the stress from 4-NP resulted in more inhibited genes. To validate the accuracy of the transcriptome data, eight DEGs were selected for quantitative real-time polymerase chain reaction (qRT-PCR), which were consistent with the RNA-Seq results. Through KEGG pathway enrichment analysis, three specific pathways related to hormonal effects and endocrine function of L. vannamei were enriched significantly, including tyrosine metabolism, insect hormone biosynthesis , and melanogenesis . After 4-NP stress, genes involved in tyrosine metabolism (Tyr) and melanogenesis pathway (AC, CBP , Wnt, Frizzled, Tcf, and Ras) were induced to promote melanin pigment to help shrimp resist adverse environments. In the insect hormone biosynthesis, ALDH , CYP15A1, CYP15A1/C1, and JHE genes were activated to synthesize juvenile hormone (JH), while Spook, Phm, Sad, and CYP18A1 were induced to generate molting hormone. There is an enhanced interaction between the molting hormone and JH, with JH playing a dominant role and maintaining its “classic status quo action”. Our study demonstrated that 4-NP exposure led to impairments of biological functions in L. vannamei hepatopancreas. The genes and pathways identified provide novel insights into the molecular mechanisms underlying 4-NP toxicity effects in prawns and enrich the information on the toxicity mechanism of crustaceans in response to EDCs exposure.
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Journal of Materials Research and Technology-JMR&T
·
2023
·
IF 6.4
Yufei Liu,Xiaojin Wang,Lulu He,Min He,Changlei Yang,Jie Yu
The poor heat resistance of acrylonitrile-butadiene-styrene copolymer (ABS) is a significant limitation that restricts its application in various fields, including automotive, electronic devices and other fields. To address this issue, we employed a strategy involving the crosslinking of a macromolecular heat-resistant agent to enhance the heat resistance of ABS. Poly(N-(4-fluorophenyl) maleimide-alt-triallyl isocyanurate) (PFT), a reactive heat-resistant agent known for its rigid and reactive structures, was selected for this purpose. ABS/PFT composites were prepared by subjecting them to γ-ray irradiation, resulting in crosslinking through a solid-state interfacial reaction (SSIR) between PFT and ABS. The results show that the heat distortion temperature ( HDT ), glass transition temperature ( T g ), tensile strength and bending strength of the irradiated ABS/PFT (i-ABS/PFT) composites increased by 23.86%, 23.35%, 20.0% and 9.0%, respectively compared to pure ABS. Furthermore, ABS/PFT composites with SSIR exhibit the highest heat resistance, T g and HDT compared to non-SSIR ABS. The work presented in this paper provides a new direction for the heat-resistant modification of ABS and will expand its application in new fields.
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RSC Advances
·
2015
·Vol. 6
·期 1
·730-739
·
IF 3.84
Qianli Wang,Yiwei Zhang,Yuming Zhou,Zewu Zhang,Jinjuan Xue,Yuanmei Xu,Chao Zhang,Xiaoli Sheng,Naishu Kui
Ordered mesoporous ceria (meso-CeO2) was fabricated by nanocasting employing Ia3d mesoporous silica KIT-6 as the template. For comparison, ceria nanoparticles (nano-CeO2) with non-ordered mesoporous were also synthesized via a sol–gel method. Polyamidoamine (PAMAM) dendrimers were used as stabilizing agents to prepare a dispersed Pt nanoparticle colloidal solution. Afterward, the obtained well-dispersed Pt nanoparticles were immobilized on meso-CeO2 and nano-CeO2, respectively. The prepared samples were characterized through several techniques, such as X-ray diffraction (XRD), nitrogen adsorption–desorption isotherms, transmission electron microscopy (TEM), scanning electron microscopy (SEM), X-ray photoelectron spectroscopy (XPS), and energy dispersion X-ray analysis (EDX) with mapping. The results revealed that the as-prepared meso-CeO2 has high crystallinity, a relatively small crystalline size, a well-ordered mesoporous structure and high surface area of 115.3 m2 g−1. In addition, the Pt/meso-CeO2 catalyst showed relatively uniform distribution of Pt nanoparticles with small sizes (∼4 nm). The catalytic performances of the as-synthesized catalysts were evaluated relying on the reduction of 4-nitrophenol monitored by UV-vis spectra. It was found that Pt/meso-CeO2 exhibited better catalytic activity compared with Pt/nano-CeO2. Besides, Pt/meso-CeO2 possessed good reusability and maintained a conversion of no less than 90% even after five cycles.
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Sustainable Energy & Fuels
·
2023
·Vol. 8
·期 3
·604-609
·
IF 5.6
Jinhui Zhang,Chuanhe Ma,Haixuan Gao,Jinchun Jiang,Hailong Wang
An over-thick MoSe2 layer and numerous voids at the absorbing layer inside and backside lead to a relatively low Jsc and PCE of CZTSSe solar cells. In previous studies, MoO2 and MoO3 sacrificial layers have been commonly used to eliminate those voids and reduce the thickness of MoSe2 layers. However, there is still no clarity about which one is more effective. In this work, we prepared MoO2 and MoO3 sacrificial layers on the surface of Mo-coated SLG substrates by air annealing and ammonia (NH3·H2O) etching, respectively. J–V testing shows that both MoO2 and MoO3 can effectively improve the Jsc and PCE of CZTSSe solar cells, wherein MoO3 is more effective. Comparative analysis shows that the electrical mechanism of Jsc and PCE improvement lies in the significant reduction of device series resistance (Rs). SEM images and XRD pattern results indicate that the reason for Rs decreasing is void elimination and MoSe2 layer thickness reduction from 600 nm to 270 nm after applying MoO3. With the aid of the MoO3 sacrificial layer, the PCE of the CZTSSe device increases from 7.51% to 9.58% (total area 0.21 cm2) without the MgF2 anti-reflection layer.
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Advanced Science
·
2023
·
IF 15.1
Quanzhen Sun,Chen Shi,Weihao Xie,Yifan Li,Caixia Zhang,Jionghua Wu,Qiao Zheng,Hui Deng,Shuying Cheng
Ion doping is an effective strategy for achieving high-performance flexible Cu 2 ZnSn(S,Se) 4 (CZTSSe) solar cells by defect regulations. Here, a Li&Na co-doped strategy is applied to synergistically regulate defects in CZTSSe bulks. The quality absorbers with the uniformly distributed Li and Na elements are obtained using the solution method, where the acetates (LiAc and NaAc) are as additives. The concentration of the harmful Cu Zn anti-site defects is decreased by 8.13% after Li incorporation, and that of the benign Na Zn defects is increased by 36.91% after Na incorporation. Synergistic Li&Na co-doping enhances the carrier concentration and reduces the interfacial defects concentration by one order of magnitude. As a result, the flexible CZTSSe solar cell achieves a power conversion efficiency ( PCE ) of 10.53% with certified 10.12%. Because of the high PCE and the homogeneous property, the Li&Na co-doped device is fabricated to a large area (2.38 cm 2 ) and obtains 9.41% PCE . The co-doping investigation to synergistically regulate defects provides a new perspective for efficient flexible CZTSSe solar cells.
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SEPARATION AND PURIFICATION TECHNOLOGY
·
2023
·
IF 8.6
Feidong Yang,Lei Li,Junyuan Hua,Jintao He,Xiaohua Ma,Jianxin Li
To meet the growing demand for lithium resources, it is ideal to develop a green and efficient approach for recovering lithium resources from discarded lithium-ion batteries. In this work, nanofiber membranes of 14-crown-4-ether polyimide (14C4PI) (M n = 33 kDa) with the crown ether loading of 1.38 mmol g −1 in the main chain were fabricated by electrospinning and the structure of the nanofiber membrane was regulated by tuning the electrospinning parameters. The selectivity adsorption of 14C4PI nanofiber membrane was investigated in the simulated extract of discarded lithium-ion batteries. The results showed that the 14C4PI-12 nanofiber membrane with a high specific surface area of 41.27 m 2 /g and a diameter of 122.7 nm was successfully prepared under the operating conditions (polymer concentration of 12 wt%, voltage of 30 kV, flow speed of 1 mL h −1 , tip-to-collector of 100 mm). The 14C4PI-12 nanofiber membrane displayed a high equilibrium adsorption capacity for Li + (Q m = 40.17 mg g −1 ). The adsorption of Li + onto the membrane was proven to be monolayer chemical adsorption confirmed by adsorption kinetics and isotherm models. The calculated equilibrium adsorption rate (EAR) was up to 70 % and the complex-ratio of crown ether in 14C4PI to Li + was 1.46:1, whose theoretical value is 1:1. Meanwhile, the selective separation factor of Li + to Na + , K + , Mn 2+ , Co 2+ , and Ni 2+ were up to 52.3, 54.97, 48.82, 41.05 and 35.04, respectively, which were much higher than that obtained from other selective adsorption method reported in literatures. The density functional theory (DFT) calculations confirm that the superior selectivity of 14C4PI to Li + is attributed to the higher Gibbs free energy change of 14C4PI-Li + complexation (−113.99 kcal mol −1 ). To sum up, this work provides an efficient method to fabricate crown ether functional polymer nanofiber membrane for recycling lithium resources.
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DALTON TRANSACTIONS
·
2023
·Vol. 52
·期 21
·7119-7128
·
IF 4
Zhengguo Zhang,Hongxiao Lv,Kun Yang,Xiutang Zhang
Developing materials with excellent properties has become the norm in the field of basic research, prompting us to explore highly robust hybrid materials based on electron-rich POMs and electron-deficient MOFs. Herein, a θ-[Mo8O26]4−-based hybrid material of [Cu2(BPPP)2]{θ-[Mo8O26]} (NUC-62) with excellent physicochemical stability was self-assembled under acidic solvothermal conditions from Na2MoO4 and CuCl2 in the presence of a designed chelated ligand of 1,3-bis(3-(2-pyridyl)pyrazol-1-yl)propane (BPPP), which has sufficient coordination sites, spatial self-regulation and great deformation ability. In NUC-62, each of two tetra-coordinated CuII ions and two BPPP are unified into one dinuclear unit serving as the cation, which is interactively linked to θ-[Mo8O26]4− anions via rich hydrogen bonds of C–H⋯O. Because of the unsaturated Lewis acidic CuII sites, NUC-62 exhibits high catalytic performance on the cycloaddition reactions of CO2 with epoxides under mild conditions with a high turnover number and turnover frequency. Furthermore, NUC-62, as a recyclable heterogeneous catalyst, shows high catalytic activity for the esterification of aromatic acid under refluxing, which is much better than the inorganic acid catalyst of H2SO4 in terms of turnover number and turnover frequency. Moreover, because of open metal sites and rich terminal oxygen atoms, NUC-62 shows high catalytic activity for Knoevenagel condensation reactions of aldehydes and malononitrile. Hence, this study lays the groundwork for constructing heterometallic cluster-based microporous MOFs with excellent Lewis acidic catalysis and chemical stability. Therefore, this study lays a foundation for the construction of functional polyoxometalate complexes.
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SEPARATION AND PURIFICATION TECHNOLOGY
·
2023
·
IF 8.6
Kuixin Cui,Nan Duan,Shengming Jin
A novel collector 2-(4-Butoxyphenyl)acetohydroxamic acid (BAHA) was actively considered in the flotation of rhodochrosite. Flotation behaviors and BAHA adsorption concerning rhodochrosite, calcite and dolomite were systematacially investigated through microflotation tests, adsorption experiments, zeta potential measurements, FTIR and XPS analyses. Microflotation results showed that rhodochrosite performed a better floatability than calcite and dolomite at pH 8.0–10.0. Also, the adsorption amounts of BAHA collector on the rhodochrosite surface were obviously greater than those of calcite and dolomite. The results of zeta potential, FTIR and XPS analyses indicated that BAHA adsorbed onto rhodochrosite surfaces through chemisorption, electrostatic attraction and intermolecular hydrogen bonding, chemisorption and electrostatic attraction for calcite, and only chemisorption for dolomite. The interaction mechanisms between BAHA collector and mineral surfaces were responsible for the differences in the BAHA adsorption and floatability between rhodochrosite and two gangues. The flotation separation tests of three minerals confirmed that the rhodochrosite concentrate with Mn grade of 24.64% and recovery of 87.94% could be obtained. BAHA is a high selective collector and can realize the flotation separation of rhodochrosite against dolomite and calcite.
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MOLECULES
·
2023
·Vol. 28
·期 6
·2442
·
IF 4.6
Hongwu Liu,Shan Yang,Ting Li,Siyue Ma,Peiyi Wang,Guoqing Wang,Shanshan Su,Yue Ding,Linli Yang,Xiang Zhou,Song Yang
Imidazole alkaloids, a common class of five-membered aromatic heterocyclic compounds, exist widely in plants, animals and marine organisms. Because of imidazole’s extensive and excellent biological and pharmacological activities, it has always been a topic of major interest for researchers and has been widely used as an active moiety in search of bioactive molecules. To find more efficient antibacterial compounds, a series of novel imidazole-fragment-decorated 2-(pyrazol-4-yl)-1,3,4-oxadiazoles were designed and synthesized based on our previous works via the active substructure splicing principle, and their bioactivities were systematically evaluated both in vitro and in vivo. The bioassays showed that some of the target compounds displayed excellent in vitro antibacterial activity toward three virulent phytopathogenic bacteria, includingXanthomonas oryzaepv.oryzae(Xoo),Xanthomonas axonopodispv.citri(Xac) andPseudomonas syringaepv.actinidiae(Psa), affording the lowest EC50values of 7.40 (7c), 5.44 (9a) and 12.85 (9a) μg/mL, respectively. Meanwhile, compound7cpossessed good in vivo protective and curative activities to manage rice bacterial leaf blight at 200 μg/mL, with control efficacies of 47.34% and 41.18%, respectively. Furthermore, compound9ashowed commendable in vivo protective and curative activities to manage kiwifruit bacterial canker at 200 μg/mL, with control efficacies of 46.05% and 32.89%, respectively, which were much better than those of the commercial bactericideTC(31.58% and 17.11%, respectively). In addition, the antibacterial mechanism suggested that these new types of title compounds could negatively impact the cell membranes of phytopathogenic bacteria cells and cause the leakage of the intracellular component, thereby leading to the killing of bacteria. All these findings confirm that novel 2-(pyrazol-4-yl)-1,3,4-oxadiazoles containing an imidazole fragment are promising lead compounds for discovering new bactericidal agents.
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ACS Applied Polymer Materials
·
2022
·
IF 4.855
Xu Yang,Hong Zhao,Chunyang Li,Xindong Zhao,Jiaming Yang,Xuan Wang
Polypropylene (PP), as a recyclable thermoplastic polymer, is a promising insulating material for application as an environmentally friendly insulation layer in high-voltage-direct-current (HVDC) cables. However, the lack of toughness and the poor wide-temperature-range electrical properties under a DC electric field seriously restrict its development and application. Herein, a block polypropylene with a low elastic modulus is selected and grafted with organic molecules of maleic anhydride (MAH) and 4-tert-butylstyrene (St*) as a masterbatch (PP-g-(St*-co-MAH)) by an ultraviolet-irradiated radical reaction. The modified b-PP with different grafting contents was prepared by diluting the masterbatch through melt blending, and their DC electrical properties at a wide temperature range of 40–100 °C were tested. The results indicate that the introduction of a comonomer St* significantly improves the grafting rate of MAH and suppresses the degradation of PP chains during the grafting reaction; thus, the PP-g-(St*-co-MAH) possesses improved thermogravimetric performance and maintains the original mechanical properties and workability. The grafted functional groups introduce deep charge traps into the matrix and thus effectively suppress the space charge injection and accumulation, significantly reduce the conductivity, and enhance the breakdown strength of PP at wide temperature ranges. Among the tested materials, the PP grafted with 0.57 wt % St*-co-MAH exhibits the best electrical properties, while inadequate or excessive grafting content of St*-co-MAH relatively weakens the positive effects of grafting modification. The mechanism is analyzed based on calculation of the trap level and the three-dimensional (3D) electric potential.
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危险品化学品经营许可证（带存储）