EUROPEAN JOURNAL OF PHARMACOLOGY
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2019
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IF 3.17
Qi-meng Liu,Qing Xiao,Xiang Zhu,Kai-feng Chen,Xia-wen Liu,Ru-chao Jiang,Dan Wu,Jun-min Shi,Li-jun Dai,Jun-jun Huang
Benign prostatic hyperplasia (BPH) is a common disorder of the urinary system in aging men. 2-(1H-indol-3-yl)-N-[3-(4-(2-methoxyphenyl) piperazinyl) propyl] acetamide (HJZ-3), which is derived from naftopidil , exhibited 97.7- and 64.6-fold greater inhibitory effects for a 1D adrenoceptor than for a 1B - and a 1A -adrenoceptors in vitro, respectively. To investigate the therapeutic potential for treating BPH, we evaluated the pharmacological activity of HJZ-3. Specifically, we evaluated through estrogen/androgen-induced rat benign prostatic hyperplasia model in vivo. HJZ-3 effectively prevented the progression of rat prostatic hyperplasia by suppressing the increase in prostate index and reducing the quantitative analysis of the relative acinus volume, relative stroma, epithelial volume and epithelial thickness and expression of proliferating cell nuclear antigen and α -smooth muscle actin. HJZ-3 decreased α 1A - and α 1D -adrenoceptor protein expressions in prostate tissue. HJZ-3 is a good alternative for α 1A - and α 1D -adrenoceptor blocker. It may relax smooth muscle tone and relieve symptoms of BPH.
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ChemPlusChem
·
2020
·Vol. 85
·期 1
·240-246
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IF 2.753
Sheng Tang,Xinyu Xiao,Jing Hu,Bo Gao,Hunglin Chen,Zongyang Peng,Jianchun Wen,Masanao Era,Dechun Zou
Graphical Solvent-free is best : Mixed halide hybrid perovskites (MHPs) are prepared through a solvent-free mechanochemical synthesis (MCS) route with superior control over halide compositions. The MCS route eliminates the problem in the preparation of MAPb(I x Br 1− x ) 3 with continuously varying x , while maintaining the material properties and suppressing phase segregation in solvent synthesis (SS) routes. Thus, the optical band gaps can be tuned easily by compositional control. Hybrid perovskites have recently received much attention in optoelectronic applications. However, hybrid perovskites are unstable in a humid environment. Mixed halide perovskites (MHPs) show enhanced stability and band-gap tunability upon engineering of their halide composition. Here, MHPs are prepared through a solvent-free mechanochemical synthesis (MCS) route that allows superior control over halide compositions than the solvent synthesis routes (SS). The MCS route eliminates the problem in the preparation of MAPb(I x Br 1− x ) 3 with continuously varying x , while maintaining the material properties and suppressing phase segregation present in SS routes. UV-vis absorption and X-ray diffraction patterns confirm the production of the desired pure-phase MHPs. For MAPb(I x Br 1− x ) 3 (0≤ x ≤1), with increased ratio of halide ( x ), the cubic phase gradually transforms into the tetragonal phase and band-gap tunability is accomplished. The MCS route for the preparation of MHPs is a very promising and efficient technique for superior control in optoelectronic properties, leading to improved control in fabrication approaches.
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International Journal of Nanomedicine
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2019
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IF 4.471
Dian Chen,Tonghe Zhu,Wei Fu,Haibo Zhang
Purpose A promising vascular scaffold must possess satisfying mechanical properties, great hemocompatibility, and favorable tissue regeneration. Combining natural with synthetic materials is a popular method of creating/enhancing such scaffolds. However, the effect of additional modification on the materials requires further exploration. Materials and methods We selected polycaprolactone (PCL), which has excellent mechanical properties and biocompatibility and can be combined with collagen. Electrospun fibers created using a PCL/collagen solution were used to fashion mixed nanofibers, while separate syringes of PCL and collagen were used to create separated nanofibers, resulting in different pore sizes. Mixed and separated nanofibers were cross-linked with glutaraldehyde (GA), 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide (EDC), and genipin; hence, we named them as mixed GA, mixed EDC (ME), mixed genipin (MG), separated GA, separated EDC (SE), and separated genipin (SG). Results Fourier transform infrared (FTIR) spectroscopy and X-ray diffraction showed that cross-linking did not affect the main functional groups of fibers in all groups. ME, MG, SE, and SG met the requisite mechanical properties, and they also resisted collagenase degradation. In hemocompatibility assays, only ME and MG demonstrated ideal safety. Furthermore, ME and MG presented the greatest cytocompatibility. For vascular scaffolds, rapid endothelialization helps to prevent thrombosis. According to human umbilical vein endothelial cell migration on different nanofibers, ME and MG are also successful in promoting cell migration. Conclusion ME and MG may be promising candidates for vascular tissue engineering. The study suggests that collagen cross-linked by EDC/ N -hydroxysuccinimide or genipin facilitates endothelial cell regeneration, which could be of great benefit in tissue engineering of vascular scaffolds.
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JOURNAL OF ORGANIC CHEMISTRY
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2019
·
IF 4.745
Yong-Long Zhao,Xing-Hai Fei,Yong-Qin Tang,Peng-Fei Xu,Fen-Fen Yang,Bin He,Xiao-Zhong Fu,Yuan-Yong Yang,Meng Zhou,Yuan-Hu Mao,Yong-Xi Dong,Chun Li
An organocatalytic asymmetric α-sulfenylation of 2-substituted indolin-3-ones with N-(alkylthio or arylthio)succinimides has been developed for the first time using Cinchona-derived squaramide as the catalyst. Various chiral 2,2-disubstituted indole-3-ones with S- and N-containing heteroquaternary carbon stereocenters were obtained with up to 98% yield and 99% ee.
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DRUG DEVELOPMENT RESEARCH
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2019
·Vol. 80
·期 6
·750-757
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IF 1.742
Chang Zheng,Wen Hou,Jun Liu,Xiao-Fang Xu,Jing Lin,Ping-Hua Sun,Wei-Min Chen
The prevalence of multidrug resistance among clinically significant bacterial pathogens underlines a critical need for the development of new classes of antibacterial agents with novel structural scaffolds. Cajaninstilbene acid (CSA), which is isolated from pigeonpea leaves, has shown potent antibacterial activity. In this study, a series of 2-hydroxyl-4-methoxyl-3-(3-methylbut-2-en-1-yl)-6-(4-phenylbenzoylamino)benzoic acid derivatives derived from CSA were designed and synthesized, and their antibacterial activities were evaluated. Several synthesized compounds exhibit better antibacterial activity than CSA against Staphylococcus aureus , Staphylococcus epidermidis , and two strains of methicillin-resistant S. aureus . Meanwhile, the results of 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide assays illustrate the good selectivity between bacteria and normal cells of the most active compounds 6u and 6v . Furthermore, well combinations with bacterial RNA polymerase of 6u arising from docking study imply the possible mechanism of antibacterial activity of these synthetic compounds.
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MOLECULAR NUTRITION & FOOD RESEARCH
·
2025
·Vol. 70
·期 1
·e70363
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IF 4.2
Shaoxuan Wang,Fei Pan,Xinyan Xu,Qian Fan,Yangyang Wang,Lei Zhao,Liang Zhao
Heterocyclic aromatic amines (HAAs), potential carcinogens formed in processed meats, have been linked to liver injury. This study evaluated whether cyanidin-3-O-glucoside (C3G, 100 mg/kg) protects against liver injury by the representative HAA 2-amino-3-methylimidazo[4,5-f]quinoline (IQ, 20 mg/kg) in mice, and explored mechanisms by integrated approaches: biochemical assays, histology, Western blot, and molecular dynamics (MD) simulations. Results demonstrated that C3G significantly ameliorated IQ-induced liver injury, as indicated by reduced serum AST and ALT and inflammatory cytokines (IL-6, IL-1β, TNF-α) levels. Additionally, C3G restored redox homeostasis by inhibiting lipid peroxidation and protein carbonylation, while enhancing antioxidant defenses (GSH, GSH-Px, and SOD). Mechanistically, C3G exerted its protective effects via multiple anti-apoptotic pathways. Specifically, it attenuated mitochondrial apoptosis by lowering the Bax/Bcl-2 ratio and inhibiting cytochrome c-caspase-9/3 activation. It also alleviated endoplasmic reticulum (ER) stress by downregulating GRP78/ATF4/CHOP and caspase-12. Furthermore, C3G interfered with death receptor signaling by reducing Fas/FasL/FADD activation and caspase-8, while upregulating CFLAR. MD simulations further demonstrated that C3G binds to the hydrophobic pocket of BAX and weakens BAX-BIM interactions. These results conclusively identify C3G as a multi-target agent against IQ-induced liver damage, highlighting its promise for development into a novel dietary strategy to counteract the toxicological risks of processed meat consumption.
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JOURNAL OF ORGANIC CHEMISTRY
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2025
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IF 3.6
Yang Zhu,Guisheng Deng
The I2-catalyzed reaction of 1-(2-hydroxyphenyl)-propargyl alcohols with indoles and subsequent treatment with K2CO3 provided (benzofuran-3-yl)-1H-indoles in good to excellent yields with high regioselectivity. This one-pot and two-step strategy proved to be suitable for a wide range of substrates except for aliphatic alkynyl alcohols as well as the indoles bearing N-protected groups such as the Ts group possessing strong electron-withdrawing feature. The reaction procedure involved a cross-coupling and the construction of a benzofuran framework via 5-exo-dig cyclization.
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Biomaterials Advances
·
2026
·
IF 6.7
Shuqi Li,Mengyuan Liu,Linglin Zhu,Jingxian Zhang,Min Ji,Huasong Gao,Yumin Yang,Luzhong Zhang
Indole-3-propionic acid loaded hydrogels were synthesized for spinal cord injury. • The synthesized hydrogels possessed good biocompatibility and alleviated oxidative stress. • The hydrogels significantly enhanced recovery of both motor and sensory functions. • The hydrogels provided a novel therapeutic strategy for SCI treatment. Spinal cord injury (SCI) is a devastating neurological condition with an exceptionally high disability rate. The clinical management of SCI remains suboptimal primarily owing to both the inhibitory characteristics of the post-injury microenvironment and inherently limited regenerative ability. In this study, we report an indole-3-propionic acid (IPA) loaded polyethylene glycol dimethacrylate (PEGDA)/lysine hydrogel for repairing spinal cord injury. Compressive Young's moduli of hydrogels can be precisely tuned by adjusting the compositional ratios. The IPA loaded hydrogels exhibits not only excellent biocompatibility but also possesses a remarkable ability to alleviate oxidative stress. In an established spinal cord injury model, 3.4 kPa IPA loaded hydrogels significantly enhanced functional recovery, promoted axonal regeneration, and supported the growth of newborn neurons. These findings indicate that the IPA loaded hydrogel offers a promising new therapeutic avenue for SCI treament.
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INORGANIC CHEMISTRY
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2026
·
IF 4.6
Bailin Chen,Yansheng Jiang,Hangwei Jia,Shuai An,Xueling Hou,Shilie Pan
Birefringent crystals, as core materials for polarization modulation, hold significant importance for the advancement of laser polarizing technology, high-precision instruments, and other optical communication fields today. However, balancing the deep ultraviolet (DUV) cutoff edge and birefringence remains a demanding challenge. Borophosphates have emerged as a promising research direction for optoelectronic functional materials, but the small birefringence of most borophosphates limits their applications. Here, a novel mixed-coordinated hydroxyborophosphate, NH4B3PO6(OH)3, has been successfully designed and obtained. This compound belongs to the triclinic space group P1 (No. 2), exhibiting pronounced birefringence (the experimental refractive index difference value is 0.057 at 546 nm) and a short DUV cutoff edge below 200 nm. These properties indicate that NH4B3PO6(OH)3 exhibits excellent potential as a DUV birefringent material.
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JOURNAL OF CHEMICAL TECHNOLOGY AND BIOTECHNOLOGY
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2026
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IF 2.7
Zhe Dong,Wei Xue,Jianhua Lv,Daolai Sun
BACKGROUND 3-Hydroxybutanal (3-HBA) is an important chemical product with a wide range of applications. This study investigated the liquid-phase condensation of acetaldehyde to produce 3-HBA over MgO-based catalysts, such as MgO–Y 2 O 3 , MgO–La 2 O 3 , and MgO–Al 2 O 3 . The influence of the Mg/Y ratio on the catalyst performance was thoroughly investigated, and the effects of the reaction conditions on the formation of 3-HBA were also studied. Furthermore, the relationship between the catalyst properties and the catalytic activity was investigated. RESULTS The MgO–Y 2 O 3 catalyst showed a high catalytic performance for the production of 3-HBA, and the optimal Mg/Y molar ratio was 1:1. The MgO–Y 2 O 3 catalyst with a molar ratio of 1:1 exhibited both weak acidic and weak basic properties, and its acid and base amounts were lower than those of MgO. Reaction temperature significantly affected the reaction, and increasing the temperature was detrimental to the formation of 3-HBA. In the reaction conducted using the MgO–Y 2 O 3 catalyst at 45 °C for 2.5 h, the conversion of acetaldehyde achieved was 52.5% with a 3-HBA selectivity of 82.4%. CONCLUSION The MgO–Y 2 O 3 catalyst with appropriate acid–base properties effectively promotes the formation of 3-HBA. An insufficient or excessive number of acidic or basic active sites is detrimental to 3-HBA yield. It is proposed that the acidic sites activate the CO bond via an electron-withdrawing effect, while the basic sites facilitate α -H elimination to generate a delocalized reactive intermediate. This intermediate subsequently undergoes nucleophilic addition to form 3-HBA. © 2026 Society of Chemical Industry (SCI).
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JOURNAL OF MEMBRANE SCIENCE
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2026
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IF 8.8
Wenyuan Qiu,Xiaoke Wei,Tao Wang,Hao-yan Yin,Haibing Wei
Anion exchange membranes (AEMs) are central to clean-energy electrochemical technologies, yet achieving high hydroxide conductivity together with dimensional and alkaline stability remains challenging. Here we implement a straightforward branching strategy in poly(arylene 3-piperidinium)s by incorporating two trifunctional units, i.e., triptycene and 1,3,5-triphenylbenzene, into the polymer backbone. This architecture suppresses water uptake and swelling without compromising the membrane's ion-transport efficiency and chemical durability. Compared to linear membranes, the branched membranes exhibit a 34−36% reduction in water absorption. Triptycene-based branched AEMs achieved superior performance, including suppressed swelling (<18% at 80 °C), high conductivity up to 191 mS cm −1 at 80 °C, and improved alkaline stability, remaining intact in 1 M NaOH for at least 2000 h. Importantly, a water electrolyzer based on B-PT3Pip-3%Trip demonstrated a current density of 6.9 A cm −2 at 2.0 V and 80 °C, and can operate stably under 1 A cm −2 at 60 °C for 1000 h with a voltage decay of only 81 μV h −1 . The synthetic simplicity of the branching strategy, together with the combination of suppressed swelling, high conductivity, and long-term durability, makes branched poly(arylene 3-piperidinium) AEMs highly promising for AEM water electrolysis applications.
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Nanoscale
·
2026
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IF 5.2
Le Luo,Xiaoming Mo,Yusheng Song,Zhentao Du,Sheng Cao,Jinju Zheng,Bingsuo Zou,Jialong Zhao
Quantum-confined CsPbBr3 nanoplatelets (NPLs) are appealing candidates for ultraviolet (UV)/blue photodetectors due to their strong excitonic binding energy and large absorption coefficient. However, the inherent soft lattice and surface defects of CsPbBr3 NPLs lead to poor operational stability, limiting their practical applications. Here, we report an A-site alloying strategy that enhances the structural rigidity and defect formation energy of CsPbBr3 NPLs. The strategy synergistically employs short-chain tetrolic acid (TLA) ligands to passivate uncoordinated Pb2+ ions and formamidinium (FA+) cations to compensate for Cs+ vacancies. This dual repair strategy enhanced both the conductivity and UV irradiation stability of CsPbBr3-based NPLs. As a result, the self-powered UV photodetectors based on Cs0.73FA0.27PbBr3-TLA NPLs exhibited a responsivity of 89 mA W-1, a specific detectivity of 3.99 × 1012 Jones, and an on/off ratio approaching 106 at 0 V bias. Even after 30 days of ambient storage, the device maintained excellent photoresponse and a high specific detectivity of 1.73 × 1012 Jones. Clear images obtained with a custom-built 2D imaging system corroborate the fast response and excellent stability of the device. These results underscore the efficacy of the combined lattice and surface engineering approach for realizing high-performance, durable perovskite NPL-based UV photodetectors.
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