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Chinese Chemical Letters 2017年第6期28卷 1220-1227页

作者： Chao Ding Dan Li yan-Wei Wang Sai-Sai Han chun-Mei Gao chun-yan tan Yu-yang Jiang Department of Chemistry Tsinghua University Beijing 100084 China The State Key Laboratory Breeding Base-Shenzhen Key Laboratory of Chemical Biology The Graduate School at Shenzhen Tsinghua University Shenzhen518055 China Department of Pharmacology and Pharmaceutical Sciences School of Medicine Tsinghua University Beijing 100084 China

By combining the core pharmacophores of HDAC inhibitor vorinostat and kinase inhibitors vandetanib,BMS-690514,neratinib,and TAK-285 with 1,2,3-triazole as linker,eight novel 6-substituted-4-aminoquinazolin derivatives were synthesized and characterized by -1H NMR,-（13）C NMR,and high resolution mass *** inhibitory activities against five enzymes（VEGFR2,HER2,EGFR,HDAC1,and HDAC6） and five cancer cell lines（A549,BT-474,A431,SK-BR-3,and NCI-H1975） were *** bioassay results show that the introduction of triazole linked vorinostat-like segment dramatically changed the selectivity profiles of newly synthetic compounds relative to vandetanib,BMS-690514,neratinib,and *** them,compound 6b exerted outstanding enzymatic and cellular activities through its simultaneous and synergistic inhibitions on multiple pathways,which might have the great potential to confer the better benefits than single-targeted inhibitors in cancer therapy.

关键词： Anticancer Kinase HDAC Multitarget Selectivity

Novel synthetic acridine-based derivatives as topoisomerase Ⅰ inhibitors

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Chinese Chemical Letters 2014年第7期25卷 1021-1024页

作者： Bin Li chun-Mei Gao Qin-Sheng Sun Lu-Lu Li chun-yan tan Hong-Xia Liu Yu-yang Jiang Tsinghua University Department of Chemistry The Ministry-Province Jointly Constructed Base for State Key Lab-Shenzhen Key Laboratory of Chemical Biology Shenzhen Anti-Tumor Drug Development Engineering Laboratory the Graduate School at ShenzhenTsinghua University School of Medicine Tsinghua University

Novel DNA binding agents against topoisomerases are needed for effective treatment of cancers. A series of new acridine-based derivatives 7a-7d were synthesized and their antiproliferative activity against K562 and HepG-2 cell lines were evaluated. Compound 7c with pyridin-2-yl-methanamino group substituted at the C9 position of acridine showed good antitumor activity against both cell lines. The DNA-binding affinity of compound 7c was evaluated by UV-vis absorption spectra and fluorescence emission spectra. DNA topoisomerase I mediated relaxation of plasmid pBR322 DNA was also tested. Our results suggested that compound 7c with good antitumor activity and topoisomerase I inhibition activity can be developed as a prime candidate for further chemical optimization.

关键词： Acridine DNA binding agent Topoisomerase Anticancer

Discovery of novel dual inhibitors of VEGFR and PI3K kinases containing 2-ureidothiazole scaffold

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Chinese Chemical Letters 2016年第1期27卷 1-6页

作者： Lin Li Cun-Long Zhang Hong-Rui Song chun-yan tan Huai-Wei Ding Yu-yang Jiang Department of Chemistry Tsinghua University The Graduate School at Shenzhen Tsinghua University School of Pharmaceutical Engineering Shenyang Pharmaceutical University

A series of compounds possessing 2-（3-phenyl）ureidothiazol-4-formamide derivatives with a 2-ureidothiazole scaffold were designed and synthesized. Some compounds demonstrated inhibition of cell proliferation against both MDA-MB-231 and Hep G2 cell lines using Sorafenib as the positive *** 6i showed a good to moderate inhibition on VEGFR-2 and PI3Ka which was proved by further molecular docking study. This study suggests that compound 6i is a potential dual inhibitor of VEGFR-2 and PI3Ka and is applicable for further investigation.

关键词： 2-Aminothiazole VEGFR PI3 KAnticancer

Novel synthetic 9-benzyloxyacridine analogue as both tyrosine kinase and topoisomerase I inhibitor

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Chinese Chemical Letters 2013年第8期24卷 677-680页

作者： Xu-Liang Lang Qin-Sheng Sun Yu-Zong Chen Lu-Lu Li chun-yan tan Hong-Xia Liu chun-Mei Gao Yu-yang Jiang Department of Chemistry Tsinghua University The Ministry-Province Jointly Constructed Base for State Key Lab-Shenzhen Key Laboratory of Chemical Biology Bioinformatics and Drug Design Group.Department of Pharmacy Centre for Computational Science and Engineering Shenzhen Anti-Tumor Drug Development Engineering Laboratory The Graduate School at ShenzhenTsinghua University School of Medicine Tsinghua University

Multi-target agents against tyrosine kinases and topoisomerases are potentially useful for the effective treatment of *** of new multi-target scaffolds are important for developing such agents. A series of five novel acridine analogues,LXL 1-5,were synthesized and their antiproliferative activity against HepC-2 cell lines were evaluated,among which the 9-benzyloxyacridine analogue,LXL-5, showed inhibitory activity against tyrosine kinases,VEGFR-2 and *** results of UV-visible absorption spectra and fluorescence emission spectra,as well as DNA topoisomerase I inhibition assay, indicated topoisomerase I inhibitory *** study suggested that acridine scaffold,previously shown to have no multi-target kinase and topoisomerase inhibitory activity,might be potentially developed as a multi-target inhibitor of tyrosine kinases and topoisomerase I.

关键词： Acridine Topoisomerases Tyrosine kinases Antitumor DNA-binding

Identification of Lentinula edodes ‘135’ Strains Using a Sequence Characterized Amplified Region (SCAR) Marker

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食用菌学报 2006年第3期 8-11页

作者： SONG chun-yan, tan Qi, CHEN Ming-jie Institute of Edible Fungi, Shanghai Academy of Agricultural Sciences, Shanghai 201106, China

The accuracy of a specific Sequence Characterized Amplified Region (SCAR) marker for Lentinula edodes ‘135’ strains, obtained using primers based on RAPD methodology, was confirmed by using the marker to correctly identify nine ‘135’ strains from a test sample of 163 L. edodes strains. Antagonism tests and AFLP amplification were used to further analyze these nine ‘135’ strains, together with strains Qingyuan 135 (Q135) and Fujian 135 (F135), in order to better understand their genetic background. A total of seventeen antagonistic reactions were recorded although the degree of the antagonism observed was generally weak. AFLP analysis revealed a high similarity between the eleven ‘135’ strains, and the average similarity coefficient was 0.9271. Our data demonstrate the feasibility and reliability of the specific SCAR marker for distinguishing ‘135’ strains from other L. edodes strains.

关键词： Identification of Letinula edodes SCAR marker AFLP Antagonism

Deciphering Water Oxidation Catalysts:The Dominant Role of Surface Chemistry over Reconstruction Degree in Activity Promotion

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Nano-Micro Letters 2025年第3期17卷 340-354页

作者： Li An Jianyi Li Yuanmiao Sun Jiamin Zhu Justin Zhu Yeow Seow Hong Zhang Nan Zhang Pinxian Xi * Zhichuan JXu chun‑Hua yan State Key Laboratory of Applied Organic Chemistry Key Laboratory of Nonferrous Metal Chemistry and Resources Utilization of Gansu ProvinceFrontiers Science Center for Rare IsotopesCollege of Chemistry and Chemical EngineeringLanzhou UniversityLanzhou 730000People’s Republic of China School of Materials Science and Engineering Nanyang Technological UniversitySingapore 639798Singapore Faculty of Materials Science and Energy Engineering Institute of Technology for Carbon NeutralityShenzhen Institute of Advanced TechnologyChinese Academy of SciencesShenzhen 518055People’s Republic of China Key Laboratory of Electromagnetic Materials and Devices National Center for International Research On Photoelectric and Energy MaterialsSchool of Materials and EnergyElectron Microscopy CenterYunnan UniversityKunming 650091People’s Republic of China State Key Laboratory of Baiyunobo Rare Earth Resource Researches and Comprehensive Utilization Baotou Research Institute of Rare EarthsBaotou 014030People’s Republic of China Beijing National Laboratory for Molecular Sciences State Key Laboratory of Rare Earth Materials Chemistry and ApplicationsPKU‑HKU Joint Laboratory in Rare Earth Materials and Bioinorganic ChemistryPeking UniversityBeijing 100871People’s Republic of China

Water splitting hinges crucially on the availability of electrocatalysts for the oxygen evolution *** surface reconstruction has been widely observed in perovskite catalysts,and the reconstruction degree has been often correlated with the activity ***,a systematic study on the roles of Fe substitution in activation of perovskite LaNiO_(3)is *** substituting Fe content influences both current change tendency and surface reconstruction ***_(0.9)Fe_(0.1)O_(3)is found exhibiting a volcano-peak intrinsic activity in both pristine and reconstructed among all substituted perovskites in the LaNi_(1-x)Fe_(x)O_(3)(x=0.00,0.10,0.25,0.50,0.75,1.00)*** reconstructed LaNi_(0.9)Fe_(0.1)O_(3)shows a higher intrinsic activity than most reported NiFe-based ***,density functional theory calculations reveal that Fe substitution can lower the O 2p level,which thus stabilize lattice oxygen in LaNi0.9Fe0.1O3 and ensure its long-term ***,it is vital interesting that activity of the reconstructed catalysts relied more on the surface chemistry rather than the reconstruction *** effect of Fe on the degree of surface reconstruction of the perovskite is decoupled from that on its activity enhancement after surface *** finding showcases the importance to customize the surface chemistry of reconstructed catalysts for water oxidation.

关键词： Oxygen evolution reaction Perovskite oxides Doping Activation and reconstruction

大语言模型对批评隐喻分析中隐喻识别的应用性研究

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外语学刊 2025年第1期 47-56页

作者：于艳春黑龙江大学外文学院哈尔滨150080 哈尔滨学院外国语学院哈尔滨150080

批评隐喻分析(critical metaphor analysis,CMA)作为一种语篇的隐喻分析方法,意在揭示语言使用者的潜在意图,不但可深化我们对语言隐喻的理解,还能揭示隐喻在人类思维和交流中的重要作用。隐喻识别作为CMA分析框架中的一个关键步骤,为... 详细信息

批评隐喻分析(critical metaphor analysis,CMA)作为一种语篇的隐喻分析方法,意在揭示语言使用者的潜在意图,不但可深化我们对语言隐喻的理解,还能揭示隐喻在人类思维和交流中的重要作用。隐喻识别作为CMA分析框架中的一个关键步骤,为隐喻阐释和隐喻说明等后续研究工作提供了坚实基础,是CMA中极其重要且不可或缺的一部分。本研究首先对CMA中隐喻识别的融合性和枢纽性进行深入讨论,探究CMA中隐喻识别的发展特性,熟悉CMA的整个分析框架。同时,针对CMA在隐喻识别中存在的客观性不足问题,提出尝试结合大语言模型(ChatGPT)进行隐喻识别的方法,并基于真实研究案例了解该方法的具体实践操作。通过案例,本研究也对使用大语言模型(ChatGPT)进行隐喻识别过程中遇到的问题进行分析和总结,希望通过合理、恰当地应用技术手段,探索人机协作的最佳方式,以提升隐喻识别的客观性,完善CMA的分析框架,更深入地进行语篇的隐喻研究。

关键词：大语言模型 ChatGPT 批评隐喻分析隐喻识别隐喻阐释隐喻说明

Advances in ethnopharmacology,phytochemistry and pharmacology of Erigerontis Herba and its Chinese medicine prescriptions

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Traditional Medicine Research 2025年第1期10卷 44-61页

作者： yang Zhou Yuan-yan Huang Ding-Yue Shang Ying Chen Meng Tian Cheng-Yu Jin Xin Lu Bing-chun yan Han-Qing Pang Institute of Translational Medicine School of MedicineYangzhou UniversityYangzhou 225009China Jiangsu Key Laboratory of Integrated Traditional Chinese and Western Medicine for Prevention and Treatment of Senile Diseases Yangzhou UniversityYangzhou 225009China School of Medicine Nanjing University of Chinese MedicineNanjing 210023China State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources Guangxi Normal UniversityGuiling 541004China.

Erigerontis Herba(EH),the dried whole plant of Erigeron breviscapus,is well-known for circulating blood,activating meridians to alleviate pain,expelling wind,and clearing away *** has been extensively utilized in southern China for the treatment of stroke hemiplegia,chest stuffiness and pains,rheumatic arthralgia,headache,and *** review focuses on the botany,ethnopharmacology,phytochemistry,pharmacology and toxicity of EH and its related prescriptions to offer new insights for prospective research of *** information about EH was retrieved from ancient records and books,PubMed,China National Knowledge Infrastructure,Chinese Pharmacopoeia,Web of Science,Doctoral and Master’s Theses,and various electronic *** is a member of Compositae family and is mainly grown in southern *** Chinese medicine records that EH has the effects of circulating blood and removing blood stasis,expelling wind,and removing cold,as well as relieving rigidity of muscle and relieving *** now,nearly 200 ingredients have been characterized from EH,including flavonoids,caffeoyls,aromatic acids,coumarins,pentacyclic terpenoids,volatile oil and other *** extracts,EH related prescriptions(Dengzhan Xixin injection,Dengzhan Shengmai capsules,etc.)or compounds(scutellarin,scutellarein,etc.)possessed obvious therapeutic effects of ischemic stroke,cerebral hemorrhage,myocardial infarction,Alzheimer’s disease,diabetes and its complications,gastric cancer,bone,and joint degenerative ***,the major active compound of EH,has been used as a quality *** no obvious toxicity of EH has been *** to its traditional applications,ethnopharmacology,phytochemistry,pharmacology,and toxicity,EH was applied as a valuable herb for clinical application in food and medicine *** several compounds have been shown to possess diverse biological activities,the underlying mechanisms of their actions remain *** fully exploi

关键词： Erigeron breviscapus traditional applications ethnopharmacology phytochemistry pharmacology

小分子苦味淬灭剂应用于口服液体制剂的研究概况

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中国药学杂志 2017年第18期52卷 1569-1575页

作者：张婷张定堃林俊芝韩雪姜红许润春马鸿雁谭庆刍杨明韩丽成都中医药大学药学院中药材标准化教育部重点实验室中药资源系统研究与开发利用省部共建国家重点实验室培育基地成都611137 成都中医药大学附属医院中心实验室成都610072 江西中医药大学南昌330004

口服液体制剂中苦味药物多以分子态或胶体形式存在,分散度大,能瞬时形成广泛而强烈的刺激,使得传统掩味与矫味方法难以完全掩蔽苦味,严重制约患者服用的顺应性。近年来,小分子苦味淬灭剂的发现,为改善口服液体制剂的口感提供了新的选择... 详细信息

口服液体制剂中苦味药物多以分子态或胶体形式存在,分散度大,能瞬时形成广泛而强烈的刺激,使得传统掩味与矫味方法难以完全掩蔽苦味,严重制约患者服用的顺应性。近年来,小分子苦味淬灭剂的发现,为改善口服液体制剂的口感提供了新的选择,逐渐成为掩味技术研究的热点。基于此,笔者阐释了小分子苦味淬灭剂的概念与特点,归纳了苦味淬灭的作用机制与影响因素,介绍了常用的小分子苦味淬灭剂及其特点和应用,以期推动小分子苦味淬灭剂在口服液体制剂中的开发应用,为口服液体制剂的苦味掩蔽提供科学的理论指导与技术支持,对于推动口服液体制剂现实问题的解决、处方设计优化与产品品质提升具有重要理论价值与实践意义。

关键词：口服液抑苦结构特点小分子苦味淬灭剂

Cis-and Trans-Coordination Assembly of Nitrogen Heterocycle with Copper(Ⅱ) and Silver(Ⅰ)

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Chemical Research in Chinese Universities 2008年第6期24卷 661-667页

作者： tan Di tan Gui-ping HUANG Xiao-chun TONG Shan-ling yanG Ke-er yan yan Department of Light Industry and Chemical Engineering Guangdong University of Technology Guangzhou 510006 P. R. China Department of Chemistry Shantou University Shantou 515063 P. R. China

After the preparation of 1,4-bis（4,5-dihydro-lH-imidazol-2-yl）benzene（bdib）, a nitrogen heterocycle with potential coordination manners of both cis- and trans-configuration forms, three complexes, including cis-[Cuz（bdib ）2（/L-OCH3）2]Cl2·2MeOH（1）, trans-[Cu（bdib）（AcO）2]n（2）, and cis-[Ag2（bdib）2]（NO3）2.2H20（3）, were successfully self-assembled. Complexes 1 and 2 crystallized in the monoclinic system with P21/n space group and complex 3 in the triclinic system with P1 space group.

关键词： Nitrogen heterocycle Cis- and trans-coordination Copper Silver