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Preparation of optically pure 3-aminocyclohexanecarboxylic acid and cis-5-amino-3-cyclohexenecarboxylic acid

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Preparation of optically pure 3-aminocyclohexanecarboxylic a...

Trinuclear gold-catalyzed site-selective alkylation of peptides

中国化学会第四届有机化学学术会议

作者： HU, Yu YANG, Yu-jin YU, Sheng-Liang Huang, qing-fei ZHU jin DENG jin-Gen Key Laboratory of Asymmetric Synthesis & Chirotechnology of Sichuan Province, Union Laboratory of Asymmetric Synthesis, Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences, Chengdu 610041. Graduate School of Chinese Academy of Sciences, Beijing

＜正＞The importance of the inhibitory neurotransmitter γ-aminobutyric acid （GABA ） in certain neurological and psychiatric disorders has become generally accepted. The research of γ-peptide which is consisted with GABA is beneficial in the aspects of our understanding of life. The preparations of （1R,3S）-1 and （1S,3R）-1 were reported. However, practical methods for preparation of enantiopure trans-1 and cis-2 are very few. Here, we synthesized four enantiomers of optically pure 3-aminocyclohexanecarboxylic acid （1） and two enantiomers of optically pure cis-5-amino-3-cyclohexenecarboxylic acid （2） by the resolution.

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Science China Chemistry 2025年第1期 249-256页

作者： qing-Yun Fang Chengyihan Gu Yinghan Chen Wencheng Yan Yong Liang Weipeng Li Chengjian Zhu Jie Han jin Xie State Key Laboratory of Coordination Chemistry Jiangsu Key Laboratory of Advanced Organic Materials Chemistry and Biomedicine Innovation Center (Chem BIC) School of Chemistry and Chemical Engineering Nanjing University Green Catalysis Center College of Chemistry Zhengzhou University State Key Laboratory of Natural Medicines China Pharmaceutical University

Selective modification of peptides has always been a challenging issue. The selective alkylation of peptides can alter the biological activity and physical properties of molecules, and it has gained significant research interest. We herein disclose an intriguing gold-catalyzed alkylation of peptides using bench-stable unactivated alkyl bromides under photoredox catalysis. A wide range of structurally diverse primary, secondary and tertiary alkyl bromides serve as effective coupling partners to precisely connect with the α-C(sp3)–H in glycine residue of peptides. This protocol demonstrates an exceptionally broad scope for alkyl halides and excellent tolerance for a wide range of useful functional groups. A series of relay transformations to construct cyclic peptides, to proceed click reaction and to realize peptide fluorescence labeling further enhance its synthetic practicality. In addition, mechanistic studies and density functional theory(DFT) calculations reveal an inner-sphere and subsequent outersphere single electron transfer(SET) mechanism.

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Silica optical fiber integrated with two-dimensional materials:towards opto-electro-mechanical technology

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Light(Science & Applications) 2021年第5期10卷 767-784页

作者： jin-hui Chen Yi-feng Xiong fei Xu Yan-qing Lu Institute of Electromagnetics and Acoustics Xiamen UniversityXiamen 361005China College of Engineering and Applied Sciences National Laboratory of Solid State Microstructures and Collaborative Innovation Center of Advanced MicrostructuresNanjing UniversityNanjing 210093China

In recent years,the integration of graphene and related two-dimensional(2D)materials in optical fbers have stimulated signifcant advances in ll-fber photonics and *** conventional passive silia fiber devices with 2D materials are empowered for enhancing light-matter interactions and are applied for manipulating light beams in respect of their polarization,phase,intensity and frequency,and even realizing the active photo-electric conversion and electro-optic modulation,which paves a new route to the integrated multifunctional ll-fber optoelectronic *** article reviews the fast-progress field of hybrid 2D-materials-optical fiber for the opto-electro-mechanical *** challenges and opportunities in this field for future development are discussed.

关键词： fiber optical polarization

Deciphering the molecular mechanisms of Simiaowan in the treatment of hyperuricemia: in vivo and in silico approaches

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Traditional Medicine Research 2025年第2期10卷 37-54页

作者： Yong-Chang Zeng Jun-Hong Wu Dan-Dan Xu Kang He Chang-qing Liu Li-fei Song Zheng-Zhi Wu Qian-Qian Jiang Shao-Yu Liang Department of Neurology The First Affiliated Hospital of Shenzhen UniversityShenzhen 518020China Pharmaceutical Department The Affiliated TCM Hospital of Guangzhou Medical UniversityGuangzhou 510000China School of Pharmacy Guizhou University of Traditional Chinese MedicineGuiyang 550025China Guangzhou Zeli Medical Technology Co. Ltd.Guangzhou 510700China

Background:Simiaowan(SMW),a well-known traditional Chinese medicine,has been employed to treat hyperuricemia(HUA)and gout for ***,the bioactive components and underlying mechanisms have not been *** objective of this study was to identify the active components and potential mechanisms of SMW by integrating pharmacological experimentation,serum pharmacochemistry,network pharmacology and molecular ***:HUA rats modelling by high-fat/high-sugar diet and potassium oxonate/adenine oral administration were used to evaluate the pharmacodynamic effects of ***-Q-Exactive-MS/MS was employed to detect the bioactive components present in SMW-containing *** pharmacology and molecular docking were utilized to elucidate the potential targets and underlying ***:SMW effectively ameliorated HUA rats via the inhibition of uric acid(UA)production,promotion of UA excretion,improvement of lipid and glucose metabolic abnormalities,antioxidant,anti-inflammatory and anti-insulin resistance effects.A total of 73 compounds detected in SMW-containing serum were identified as potential active components,with alkaloids,flavonoids,organic acids,and terpenoids emerging as the primary active *** 203 corresponding targets were obtained as SMW anti-HUA/gout targets,which mainly participated in apoptosis,insulin resistance,TNF,PI3K-Akt,HIF-1,NF-κB,MAPK,IL-17 and TLR signaling *** docking indicated that active compounds(***,phellodendrine,quercetin,formononetin,ferulic acid)had superior binding abilities to the key targets(*** carrier family 22 member 12(URAT1),solute carrier family 22 member 6(OAT1),ATP-binding cassette sub-family G member 2(ABCG2),solute carrier family 2,facilitated glucose transporter member 9(GLUT9),xanthine dehydrogenase/oxidase(XDH),transcription factor p65(RELA),toll-like receptor 4(TLR4),prostaglandin G/H synthase 2(PTGS2),caspase-3(CASP3),insulin(INS)).Conclusion:S

关键词： hyperuricemia network pharmacology serum pharmacochemistry Simiaowan UPLC-Q-Exactive-MS/MS

山姜素调节cAMP/PKA/CREB信号通路促进骨质疏松性骨折大鼠骨折愈合

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中国组织工程研究 2025年第12期29卷 2438-2443页

作者：陆飞周静金涛连云港市第一人民医院康复医学科江苏省连云港市222000 南京医科大学康达学院康复医学部江苏省连云港市222000 中国人民解放军东部战区总医院健康医学科江苏省南京市210018

背景:山姜素具有抗炎、抗肿瘤、抗菌等作用,已被证实能够缓解骨质疏松症,但山姜素对骨质疏松性骨折的影响及机制仍不清楚。目的:探讨山姜素调节环磷酸腺苷/蛋白激酶A/环磷酸腺苷反应元件结合蛋白信号通路对骨质疏松性骨折大鼠的改善作... 详细信息

背景:山姜素具有抗炎、抗肿瘤、抗菌等作用,已被证实能够缓解骨质疏松症,但山姜素对骨质疏松性骨折的影响及机制仍不清楚。目的:探讨山姜素调节环磷酸腺苷/蛋白激酶A/环磷酸腺苷反应元件结合蛋白信号通路对骨质疏松性骨折大鼠的改善作用。方法:采用双侧卵巢切除手术构建骨质疏松症骨折大鼠模型,将成功造模大鼠依据随机数字表法分为山姜素低、中、高剂量组、抑制剂组和模型组,另选12只大鼠作为假手术组。骨折造模当天,山姜素低、中、高剂量组大鼠灌胃7.5,15,30 mg/kg的山姜素+腹腔注射等量的生理盐水,抑制剂组灌胃30 mg/kg的山姜素+腹腔注射5 mg/kg的H-89(通路抑制剂),模型组与假手术组给予(灌胃+腹腔注射)等量生理盐水,1次/d,连续8周。放射性检查评估大鼠骨折愈合情况并进行愈合评分;骨密度扫描仪测定骨折处骨密度;通过三点弯曲实验和压缩实验评估大鼠股骨生物力学状况;苏木精-伊红染色观察大鼠骨折处病理损伤;酶联免疫吸附(ELISA)法检测血清碱性磷酸酶、骨钙素和Ⅰ型胶原交联C-末端肽、环磷酸腺苷水平的变化;Western blot检测股骨组织中骨形态发生蛋白2和环磷酸腺苷/蛋白激酶A/环磷酸腺苷反应元件结合蛋白通路蛋白表达。结果与结论:①相较于假手术组,模型组大鼠骨折愈合评分、骨密度、最大负荷、最大应力、碱性磷酸酶、骨钙素、环磷酸腺苷水平、骨形态发生蛋白2、磷酸化蛋白激酶A/蛋白激酶A、磷酸化环磷酸腺苷反应元件结合蛋白/环磷酸腺苷反应元件结合蛋白表达下降,Ⅰ型胶原交联羧基末端肽水平增加(P<0.05);与模型组比较,山姜素各剂量组大鼠上述各项指标呈现相反的变化(P<0.05);与山姜素高剂量组比较,抑制剂组大鼠上述指标变化均被逆转(P<0.05)。②结论:山姜素可能通过激活环磷酸腺苷/蛋白激酶A/环磷酸腺苷反应元件结合蛋白信号通路加速骨质疏松症骨折大鼠的骨折愈合。

关键词：山姜素环磷酸腺苷/蛋白激酶A/环磷酸腺苷反应元件结合蛋白骨质疏松骨折愈合大鼠

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Insight into relationship between composition,thickness and electrochemistry behavior of oxide film formed on TA15under different potentials in 0.5 mol·L^(-1)H_(2)SO_(4)

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Rare Metals 2023年第5期42卷 1760-1772页

作者： fei-fei Huang Yi Qin qing-Rui Wang Hiroaki Yoshida Lei Wen Hai Chang Ying jin National Center for Materials Service Safety University of Science and Technology BeijingBeijing100083China Innovation Group of Marine Engineering Materials and Corrosion Control Southern Marine Science and Engineering Guangdong LaboratoryZhuhai519080China Department of Physical Science Hiroshima UniversityHigashi-Hiroshima739-8526Japan

The oxide film formed on TA15 alloy in0.5 mol·L^(-1)H_(2)SO_(4)at different applied potentials is investigated by evaluating the film formation current density,film thickness,surface film composition,valence state,and the electrochemical *** relative quantitative spectral analysis revealed by X-ray photoelectron spectroscopy(XPS)and X-ray absorption spectra(XAS)shows that the increasing applied potential promotes the formation of thick and high-valence state *** contrasting with XAS of the reference titanium oxides,it is found that TiO_(2)within the oxide film changes from anatase type to rutile type with the potential increases to 2.00 *** oxide film formed at passive region has better protection performance,and with the increase of applied potential,the corrosion resistance of passive film increases,whereas the ND(donor density)values obtained from the Mott-Schottky(MS)results decrease with the increasing applied potential,indicating a better uniformity and protective effect of the oxide *** on above facts,the model of the oxide films formed on TA15 at different applied potentials in passive region and dissolve region is ***,the existence forms of all the TA15alloying elements under the most corrosion resistant condition are confirmed.

关键词： TA15 Electrochemical passivation Corrosion behavior Surface compositions and structures

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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

Increased CAP37 Expression in Stable Chronic Obstructive Pulmonary Disease

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Current Medical Science 2022年第5期42卷 949-957页

作者： jin-qing CHEN Yi-fei DUAN Jian-miao WANG Department of Respiratory and Critical Care Medicine Tongji HospitalTongji Medical CollegeHuazhong University of Science and TechnologyWuhan 430030China

Objective Cationic antimicrobial protein of 37 kDa(CAP37),a neutrophil-derived protein originally identified for its antimicrobial activity,is now known to have many regulatory effects on host ***,its role in the pathogenesis of chronic obstructive pulmonary disease(COPD)has not been *** therefore investigated the expression of CAP37 in COPD and its effects on airway structural cells,including bronchial epithelial cells,smooth muscle cells,and *** CAP37 was detected in the lung tissue,sputum,and plasma of COPD patients and the control subjects,as well as in the neutrophils stimulated by cigarette smoke extract(CSE).BEAS-2B cells,human bronchial smooth muscle cells(HBSMCs),and MRC-5 cells were treated with CAP37 or an anti-CAP37 antibody plus ***(IL)-6 and IL-8 were detected in the BEAS-2B *** cell proliferation was analyzed in the *** were also detected in the MRC-5 *** The expression of CAP37 was increased in the lung tissue and sputum supernatant of the COPD patients compared with the control *** sputum supernatant CAP37 levels were inversely correlated with the forced expiratory volume in the first second percentage predicted in ***37 was induced by CSE stimulation in the peripheral blood neutrophils from healthy ***37 induced expression of IL-6 and IL-8 in BEAS-2B cells,and collagen expression of lung fibroblasts(MRC-5 cells).However,CAP37 did not significantly alter the proliferation of the *** Our findings indicated that neutrophil-derived CAP37 may be involved in airway inflammation and fibrosis in COPD via affecting the bronchial epithelial cells,and fibroblasts,thus suggesting a possible role of CAP37 in the development and progression of COPD.

关键词： cationic antimicrobial protein of 37 kDa chronic obstructive pulmonary disease fibrosis inflammation neutrophil

Tunable and enhanced light emission in hybrid WS_(2)-optical-fiber-nanowire structures

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Light(Science & Applications) 2019年第1期8卷 1091-1098页

作者： jin-hui Chen Jun Tan Guang-xing Wu Xue-jin Zhang fei Xu Yan-qing Lu Key Laboratory of Intelligent Optical Sensing and Manipulation(Ministry of Education) College of Engineering and Applied SciencesNational Laboratory of Solid State Microstructures and Collaborative Innovation Center of Advanced MicrostructuresNanjing UniversityNanjing 210093People’s Republic of China School of Physics Nanjing UniversityNanjing 210093People’s Republic of China

In recent years,the two-dimensional(2D)transition metal dichalcogenides(TMDCs)have attracted renewed interest owing to their remarkable physical and chemical *** to that of graphene,the atomic thickness of TMDCs significantly limits their optoelectronic *** this study,we report a hybrid WS_(2)-optical-fibernanowire(WOFN)structure for broadband enhancement of the light-matter interactions,i.e.,light absorption,photoluminescence(PL)and second-harmonic generation(SHG),through evanescent field *** interactions between the anisotropic light field of an optical fiber nanowire(OFN)and the anisotropic second-order susceptibility tensor of WS_(2) are systematically studied theoretically and *** particular,an efficient SHG in the WOFN appears to be 20 times larger than that in the same OFN before the WS_(2) integration under the same ***,we show that strain can efficiently manipulate the PL and SHG in the WOFN owing to the large configurability of the silica *** results demonstrate the potential applications of waveguide-coupled TMDCs structures for tunable high-performance photonic devices.

关键词： fiber optical waveguide