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RESEARCH ON CHEMICAL INTERMEDIATES · 2013 ·Vol. 40 ·期 4 ·1575-1581 · IF 0.88

Synthesis and biological evaluation of novel 2-(substituted isoxazol-4-yl)-5-arylamino-1,3,4-oxadiazoles

Liu Feng,Wang Meiyan,Teng Xinhuan,Zhang Peizhi,Jiang Lin

A series of 2-(5-methyl-3-(4-chloro/trifluoromethylphenyl)isoxazol-4-yl)-5-arylamino-1,3,4-oxadiazoles were synthesized from 4-chloro/trifluoromethyl benzaldehyde, ethyl acetoacetate, hydroxylamine hydrochloride, hydrazine hydrate, and aryl isocyanate by multi-step reactions. The structures of the target compounds were elucidated by IR, 1 H NMR, MS, and elemental analysis. All these compounds were tested for in vitro antifungal activities against Botrytis cinerea and Rhizoctonia cerealis by the mycelium growth rate method, and the results indicated that some compounds displayed high antifungal activity against Botrytis cinerea.

✓ 已验证 DOI 高影响因子
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JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY A-CHEMISTRY · 2020 · IF 3.306

Visible light catalyzed anti-markovnikov hydration of styrene to 2-phenylethanol: From batch to continuous

Yuhang Chen,Jie Zhang,Zhiyong Tang,Yuhan Sun

The 2-phenylethanol production by traditional chemical methods requires multi-step reactions, in which harsh conditions such as high temperature or strong acid/base are required and undesired by-products are easily produced. The visible light catalyzed anti-Markovnikov hydration of styrene is a single-step reaction using non-toxic catalyst under mild conditions. However, this reaction usually takes ten or even dozens of hours, facing the problem in scale up. The present work aims to intensify this reaction in continuous flow microreactor with comparison to traditional batch reactor. The effects of light source shape, reaction temperature, substrate concentration and catalyst concentration on the reaction were investigated. The continuous flow microreactor permitted to ensure more uniform light intensity and larger specific surface area, the reaction rate could thus be enhanced. The maximum productivity of 2-phenylethanol was 0.122 mol/(L.h), which was 2.5 times higher than that obtained in test tube under the same reaction conditions and 34 times higher than that reported in previous literature. The optimal photosensitizer concentration was 2 %. The increase of substrate concentration would lead to the addition reaction between styrene cationic intermediates with styrene, thereby decreasing the selectivity of 2-phenylethanol.

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INORGANIC CHEMISTRY · 2022 · IF 5.436

CsY(SO4)2·4H2O: A Deep-Ultraviolet Birefringent Crystal Induced by an Edge-Sharing Connection

Yaoguo Shen,Longjie Huang,Zhifeng Wang,Yingwu Zhou,XiaoLing Xue,Hong Lin,Renwen Yan,Sangen Zhao,Junhua Luo

SO4 tetrahedral groups have weak polarization anisotropy, which thus results in the small birefringence of sulfates. Here, we report new sulfate CsY(SO4)2·4H2O with unprecedented birefringence among deep-ultraviolet (deep-UV) sulfates. Its single crystal (10 mm × 3.5 mm × 1.5 mm) was simply grown by an aqueous solution evaporation technique, and it features a rare layered structure composed of YO9 polyhedra, SO4 tetrahedra, and H2O molecules. Interestingly, each SO4 group donates two oxygen atoms to edge-share with one adjacent YO9 polyhedron and thus causes severe distortion of these groups. The characteristic edge-sharing mode gives CsY(SO4)2·4H2O a large birefringence of ∼0.045@546 nm, which is the maximum among deep-UV sulfates and phosphates with similar non-π-conjugated anionic groups. The ultraviolet–visible-near-infrared diffuse reflection and transmission spectra, infrared spectrum, thermal stability, and theoretical calculations are also presented. The fascinating results will improve our understanding of sulfates and may provide useful insights into the exploration of deep-UV sulfates with large birefringence.

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Journal of Dental Sciences · 2026 ·Vol. 21 ·期 4 ·2375 · IF 3.6

Runt-related transcription factor 2 transcriptionally represses sirtuin 1 to regulate osteoclastogenesis and tooth eruption

Jie Li,Changqing Yan,Xinyi Sun,Chenying Zhang,Xiaozhe Wang,Yang Liu,Shuguo Zheng

Background/purpose Cleidocranial dysplasia (CCD), caused by Runt-related transcription factor 2 (RUNX2) haploinsufficiency, features delayed tooth eruption. Although impaired osteoclastogenesis contributes to eruption failure, the direct molecular mechanisms linking RUNX2 deficiency to osteoclast dysfunction remain elusive. Sirtuin 1 (SIRT1) is a critical regulator of osteoclastogenesis; however, whether it serves as a downstream effector of RUNX2 remains unexplored. This study aimed to elucidate the mechanistic link between RUNX2 and SIRT1 in regulating osteoclast differentiation and tooth eruption. Materials and methods Tooth eruption and osteoclast differentiation were assessed by microcomputed tomography and histological analysis in Runx2 +/− mice. Chromatin immunoprecipitation quantitative polymerase chain reaction and luciferase reporter assays confirmed RUNX2 binding to the Sirt1 promoter. Osteoclast marker expression was evaluated by reverse transcription quantitative polymerase chain reaction and western blotting. Bone marrow-derived macrophages from Runx2 +/− mice were transfected with small interfering RNA targeting SIRT1 for rescue experiments. Osteoclast differentiation and function were assessed by tartrate-resistant acid phosphatase (TRAP) staining and bone resorption assays. Results Runx2 +/− mice showed significantly reduced mandibular first molar eruption and decreased TRAP-positive osteoclasts, accompanied by SIRT1 upregulation. RUNX2 directly bound to the Sirt1 promoter and repressed its transcription. SIRT1 knockdown increased expression levels of osteoclast markers and elevated acetylation of NF-κB p65 at lysine 310. Importantly, SIRT1 knockdown rescued osteoclast formation and resorption to wild-type levels in Runx2 +/− cells. Conclusion RUNX2 haploinsufficiency impairs tooth eruption through transcriptional derepression of SIRT1, which inhibits osteoclastogenesis via NF-κB p65 deacetylation, highlighting the RUNX2-SIRT1 axis as a novel therapeutic target for CCD.

✓ 已验证 DOI PubMed 高影响因子
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JOURNAL OF APPLIED ENTOMOLOGY · 2022 ·Vol. 146 ·期 6 ·760-772 · IF 2.183

Molecular characterization and its binding properties of general odorant binding protein 2 in Dioryctria abietella

Ya Xing,Fang Niu,Xiao-Mei Wang,Huan-Wen Chen,De-Fu Chi

Dioryctria abietella is a major pest of conifer cones that can initiate specific behaviours (locating hosts, finding mates and selecting oviposition sites) through sensitive olfactory systems. General odorant-binding proteins are involved in the first step in odorant perception in insects, but their specific functional roles in D . abietella chemoreception have not been fully elucidated. In this study, quantitative real-time polymerase chain reaction (PCR) examinations showed that DabiGOBP2 is predominantly expressed in the antennae of female adults. Western blot experiments further confirmed that these proteins show biased expression in the tissues. Binding property analysis demonstrated that DabiGOBP2 exhibited ligand specificity to terpenes, especially myrcene ( K i = 8.19 ± 0.05). Electroantennogram (EAG) and Y-tube assays showed that three plant volatiles elicited high EAG responses, but only dodecanal showed a strong attraction to females. However, myrcene and isobutyl benzoate were significantly repellent to males at high doses in the behaviour test. In conclusion, exploring the functions of DabiGOBP2 can help in better understanding the mechanism of the olfactory system of D . abietella and developing novel strategies to control this pest.

✓ 已验证 DOI 高影响因子
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Experimental and Therapeutic Medicine · 2018 ·Vol. 15 ·期 4 ·3265-3272 · IF 1.41

Efficient delivery of recombinant human bone morphogenetic protein (rhBMP‑2) with dextran sulfate‑chitosan microspheres

Yuan‑Jun Xia,Hong Xia,Ling Chen,Qing‑Shui Ying,Xiang Yu,Li‑Hua Li,Jian‑Hua Wang,Ying Zhang

Bone morphogenetic protein‑2 (BMP‑2) serves an important role in the development of bone and cartilage. However, administration of BMP‑2 protein alone by intravenous delivery is not very effective. Sustained delivery of stabilized BMP‑2 by carriers has been proven necessary to improve the osteogenesis effect of BMP‑2. The present study constructed a novel drug delivery system using dextran sulfate (DS)‑chitosan (CS) microspheres and investigated the efficiency of the delivery system on recombinant human bone morphogenetic protein (rhBMP‑2). The microsphere morphology, optimal ratio of DS/CS/rhBMP‑2, and drug loading rate and entrapment efficiency of rhBMP‑2 CS nanoparticles were determined. L929 cells were used to evaluate the cytotoxicity and effect of DS/CS/rhBMP‑2 microspheres on cell proliferation. Differentiation study was conducted using bone marrow mesenchymal stem cells (BMSCs‑C57) cells treated with DS/CS/rhBMP‑2 microspheres or the control microspheres. The DS/CS/rhBMP‑2 microspheres delivery system was successfully established. Subsequent complexation of rhBMP‑2‑bound DS with polycations afforded well defined microspheres with a diameter of ~250 nm. High protein entrapment efficiency (85.6%) and loading ratio (47.245) µg/mg were achieved. Release of rhBMP‑2 from resultant microspheres persisted for over 20 days as determined by ELISA assay. The bioactivity of rhBMP‑2 encapsulated in the CS/DS microsphere was observed to be well preserved as evidenced by the alkaline phosphatase activity assay and calcium nodule formation of BMSCs‑C57 incubated with rhBMP‑2‑loaded microspheres. The results demonstrated that microspheres based on CS‑DS polyion complexes were a highly efficient vehicle for delivery of rhBMP‑2 protein. The present study may provide novel orientation for bone tissue engineering for repairing and regenerating bone defects.

✓ 已验证 DOI PubMed 高影响因子
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Journal of Environmental Chemical Engineering · 2021 · IF 5.909

Removal of chlorobenzene over LaMnO3 and OMS-2 catalysts in a dielectric barrier discharge reactor

Liying Jiang,Zhiwei Yao,Pengju Wang,Jianmeng Chen,Yufen Zhang,Wu Huang,Xiang Cao,Yufeng Xu

Plasma-catalytic removal of chlorobenzene (CB) was conducted in a dielectric barrier discharge (DBD) reactor over two manganese-based catalysts, LaMnO 3 and cryptomelane-type octahedral molecular sieve (OMS-2). The physicochemical properties of two catalysts were characterized by XRD , SEM, TEM , BET, XPS and H 2 -TPR. It was shown that OMS-2 catalyst had larger surface area, smaller particle size, better redox properties, higher ratio of Mn 4+ /Mn 3+ and higher content of surface-adsorbed oxygen (O ads ). The introduction of manganese-based catalysts enhanced CB removal, increased the CO 2 selectivity , and inhibited ozone (O 3 ) and NO x formation. OMS-2 exhibited a better degradation, mineralization and energy yield, with 89.5% of CB degradation, 57.6% of CO 2 selectivity and 0.54 g kWh −1 at discharge voltage of 6 kV, than LaMnO 3 in the NTP-catalytic reactor and this was ascribed to more active sites, more O ads , higher redox property and better O 3 decomposition ability on OMS catalyst surface. The two manganese-based catalysts were stable in the NTP-catalysis system although some intermediate byproducts were deposited on the catalyst surface during the 24-h activity cycling tests. Moreover, the intermediate byproducts were analyzed by GC/MS, and then the possible degradation pathways of CB decomposition in the plasma-catalysis system were suggested.

✓ 已验证 DOI 高影响因子
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RSC Advances · 2016 ·Vol. 6 ·期 54 ·48737-48744 · IF 3.289

Conversion of bis(2-hydroxyethylene terephthalate) into 1,4-cyclohexanedimethanol by selective hydrogenation using RuPtSn/Al2O3

Danfeng Hou,Jiayu Xin,Xingmei Lu,Xiaonan Guo,Huixian Dong,Baozeng Ren,Suojiang Zhang

1,4-Cyclohexanedimethanol (CHDM) is a highly valued and widely used monomer in the polymer industry. Bis(2-hydroxyethylene terephthalate) (BHET), the product of glycolysis of waste PET, is an excellent raw material for the preparation of CHDM. Herein, a series of monometallic, bimetallic and trimetallic supported catalysts were prepared for the one-pot conversion of BHET into CHDM by the impregnation method and good performance was found over trimetallic RuPtSn/Al2O3 catalysts containing various active sites to catalyze the hydrogenation of the phenyl and carbonyl groups. The influences of various reaction parameters including temperature, pressure and time on the hydrogenation reaction were studied, and 100% conversion and 87.1% yield of CHDM were obtained with the trimetallic supported catalyst with Ru/Sn 1.5. Moreover, through the comparison between various methods for the preparation of CHDM, the conversion of BHET into CHDM by the one-pot method is considered one of the most competitive methods.

✓ 已验证 DOI 高影响因子
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APPLIED SURFACE SCIENCE · 2019 · IF 5.155

Nanotribological properties of 2-D MoS2 on different substrates made by atomic layer deposition (ALD)

Junjie Yang,Lei Liu

The friction influence of 2-D molybdenum disulfide (MoS 2 ) films deposited on different substrates (Si, SiO 2 and Al 2 O 3 ) by atomic layer deposition (ALD) has been investigated. All of the three substrates showed a trend of decreasing friction with increasing number of layers of MoS 2 , but the friction leveled off for more than 6 layers samples. Comparing these 2-D MoS 2 films with each other, MoS 2 on the Al 2 O 3 possesses the lowest friction, while MoS 2 on the Si possesses the highest one, owing to effect of substrate on the specific self-limiting reaction in ALD process. At the same time, the friction of the monolayer MoS 2 is strongest affected by sulfur deficient. As the number of layers increases, the influence of the substrate on the friction of MoS 2 can be approximately characterized by the work of adhesion. Greater work of adhesion corresponds to a higher friction force. When the thickness is more than 6 layers, the substrate effect disappears gradually. Moreover, the friction of 2-D MoS 2 could be controlled near linearly by changing plasma treatment time within the range from 1 to 20 s, which suggests a possible way for the friction control of 2-D MoS 2 on different substrate quasi-qualitatively or even qualitatively.

✓ 已验证 DOI 高影响因子
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ANALYTICAL AND BIOANALYTICAL CHEMISTRY · 2025 · IF 3.8

Ratiometric surface-enhanced Raman scattering quantification of extracellular matrix metalloproteinase-2 activity for tumor diagnosis

Zhu Dan,Zhong Hanyan,Shi Jingzhan,Liu Qiang,Wang Yiping

As a precursor to cancer metastasis, the matrix metalloproteinase (MMP) family can degrade almost all protein components of the extracellular matrix, disrupting the histological barrier and promoting tumor invasion. Therefore, the sensitive and reliable detection of MMP activity in the tumor microenvironment is of great importance for the diagnosis and prognosis of malignant tumors. Here, a ratiometric surface-enhanced Raman scattering (SERS) sensing strategy based on interference-free internal standard was proposed for the accurate quantification of MMP-2 activity. A plasmonic substrate with core-satellite structure was constructed by self-assembly of silver nanoparticles on the gold core, which provided excellent SERS enhancement due to the coupling interaction. Besides, rhodamine B (RhB)-labelled substrate peptides and 4-mercaptobenzonitrile (MBN) were used as the MMP-2 recognizer and internal standard, respectively. MMP-2 specifically cleaved the peptides in half, leaving the RhB molecule free and the Raman signal at 1650 cm −1 weak. Benefitting from the synergistic normalization by MBN at 2223 cm −1 in the cell silent region, this ratio-type readout signal ( I 2223 / I 1650 ) was resistant to the endogenous and exogenous interference, contributing to the reproducibility and stability. The experimental results showed that the nanoprobe was capable of detecting MMP-2 activity at concentrations ranging from 10 to 100 ng/mL, and the limit of detection could be down to 0.715 ng/mL. Importantly, it was successfully used to differentiate the breast cancer cells from the normal cells based on the MMP-2 activity, which could have a great potential in the fields of tumor biology and accurate disease diagnosis. Graphical abstract

✓ 已验证 产品关联 DOI PubMed 高影响因子
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FITOTERAPIA · 2025 · IF 2.6

Screening bioactive compounds from Qianghuo (Notopterygium incisum) volatile oil via COX-2 magnetic ligand fishing

Li Zhang,Hui Wu,Xiaoyuan Li,Xiu Zhang,Hua Li,Huaqiao Tang,Daxuan Tang,Shijing Du,Ya’’ou Liu,Yangfan Tang,Xiaoming Bao,Guoqiang Cheng

Qianghuo (the rhizomes and radixes of Notopterygium incisum Ting ex H.T. chang) is a traditional Chinese medicine, and widely used as an anti-inflammatory, anodyne, antifebrile agent. Qianghuo volatile oil also exhibits the same properties, and the effects are probably related to the inhibition of cyclooxygenase (COX), but its bioactive components are not clear yet. To figure out the bioactive components of Qianghuo volatile oil target to cyclooxygenase-2 (COX-2), a ligand fishing method using immobilized COX-2 magnetic beads (COX-2-MB S ) and gas chromatography–mass spectrometry (GC–MS) were developed to identify the compounds that act on COX-2. Nine ligands, including 3-carene, β-caryophyllene, eucalyptol, α-terpinene, Limonene, δ-terpinene, α-pinene, β-pinene and γ-terpinene, were specifically captured by COX-2-MB S . Among them, 3-carene, β-caryophyllene, and eucalyptol in Qianghuo volatile oil were isolated and confirmed by in vitro inhibition and in vivo anti-inflammatory activity assays as selective inhibitor against COX-2. The IC 50 values were 13.5, 10.1, and 7.6 μM, respectively. Compared with the model, 3-carene, β-caryophyllene, and eucalyptol considerably reduced ear swelling and paw edema. Moreover, 3-carene and eucalyptol significantly decreased the changes of COX-2 expression in RAW264.7 cells activated by LPS. Our study validated that the developed ligand-fishing method using COX-2-MBs coupled with GC–MS can be applied to recognize COX-2 inhibitors in Qianghuo volatile oil. In vitro/vivo assay showed 3-carene and eucalyptol in Qianghuo volatile oil had strong inhibition against COX-2. This study may provide novel methods for discovering active components for volatile oil–based drug development or aromatherapy.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2025 · IF 6.2

Phytosterols Inhibit ACAT2-Catalyzed Cholesteryl Esterification in Caco-2 Cells without Affecting Cholesterol Transporter Genes

Zixing Chen,Chi Ho Jacky Chau,Andrew Erickson,Huafang Ding,Shouhe Huang,Wen-Sen He,Hanyue Zhu,Zhen-Yu Chen

Phytosterols have long been used to prevent hypercholesterolemia-related diseases, although their effects on intestinal cholesterol metabolism remain elusive. This study applied comparative proteomics to investigate the effects of various sterols on proteomic changes in differentiated Caco-2 cells. A total of 206, 231, 180, and 197 differentially expressed proteins were identified following treatment with cholesterol, β-sitosterol, stigmasterol, and campesterol, respectively. Functional enrichment analysis revealed that phytosterols significantly altered the proteome of Caco-2 cells, though their effect on cholesterol transport protein expression was negligible. Notably, while phytosterols did not regulate the expression of acyl-CoA:cholesterol acyltransferase 2 (ACAT2), β-sitosterol and stigmasterol significantly lowered the level of cholesterol oleate in Caco-2 cells by 57.1 ± 0.8% and 51.4 ± 3.9%, respectively, demonstrating that they inhibited ACAT2-catalyzed cholesteryl esterification activity. In view of the fact that cholesterol needs to be converted to cholesteryl esters before incorporation into chylomicrons, it was concluded that phytosterols primarily reduce intestinal cholesterol absorption by inhibiting ACAT2 enzyme activity rather than its gene expression. This study provides new insights into the regulation of cholesterol homeostasis by phytosterols in the small intestine.

CAS / MDL: 57-88-5
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