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Synthesis,Crystal Structure,Antitumor Activities and Docking Study of 1-(2-(1H-Indol-3-yl)ethyl)-3-(2-methoxyphenyl)urea

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Chinese Journal of Structural Chemistry 2018年第3期37卷 393-399页

作者：胡春红魏堆堆孙晓飞蔺瑞丽胡敏敏唐磊王震贺殿 Institute of Medicinal Chemistry School of Pharmaceutical Scienceand Key Laboratory of Preclinical Study for New Drugs of Gansu ProvinceLanzhou University lanzhou weihuan Bio-technology development co. Ltd.

The title co.pound,1-（2-（1 H-indol-3-yl）ethyl）-3-（2-methoxyphenyl）urea（C（18）H（19）N3O2,Mr = 309.36） has been synthesized,and its structure was characterized by ^1H-NMR,^13C-NMR,ESI-MS and single-crystal X-ray *** crystallizes in the monoclinic space group P21/c with a = 16.2774（15）,b = 11.1082（10）,c = 9.0819（3） A,β = 103.09（9）°,V = 1599.5（3） A^3,Z = 4,T = 293（2） K,μ（MoKα） = 0.086 mm^（-1,Dc = 1.285 g/cm^3,F（000） = 656 and GOOF = 0.981.5973 reflections were measured（7.04≤2θ≤52.04°）,and 3143 were unique（Rint= 0.0393,Rsigma = 0.0546） and used in all *** final R = 0.0756（I 〉 2σ（I）） and w R = 0.1976（all data）.The antitumor activity of the title co.pound was analyzed by MTT ***,to rationalize its potencies in the CDK4 target,the title co.pound was docked into CDK4 protein and the interactions with the active site residues were analyzed.

关键词： crystal structure synthesis antitumor activity molecular docking

Analysis of the potential biological value of pyruvate dehydrogenase E1 subunitβin human cancer

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World Journal of Gastrointestinal Onco.ogy 2024年第1期16卷 144-181页

作者： Yao Rong Song-Hua Liu Ming-Zheng Tang Zhi-Hang Wu Guo-Rong Ma Xiao-Feng Li Hui Cai First Clinical Medical co.lege Gansu University of Chinese MedicineLanzhou 730000Gansu ProvinceChina General Surgery Clinical Medical Center Gansu Provincial HospitalLanzhou 730000Gansu ProvinceChina Key Laboratory of Molecular Diagnostics and Precision Medicine for Surgical Onco.ogy in Gansu Province Gansu Provincial HospitalLanzhou 730000Gansu ProvinceChina NHC Key Laboratory of Diagnosis and Therapy of Gastrointestinal Tumor Gansu Provincial HospitalLanzhou 730000Gansu ProvinceChina

BACKGROUND The pyruvate dehydrogenase E1 subunitβ(PDHB)gene which regulates energy metabolism is located in ***,few studies have elucidated the role and mechanism of PDHB in different *** To co.prehensive pan-cancer analysis of PDHB was performed based on bioinformatics approaches to explore its tumor diagnostic and prognostic value and tumor immune relevance in *** vitro experiments were performed to examine the biological regulation of PDHB in liver *** Pan-cancer data related to PDHB were obtained from the Cancer Genome Atlas(TCGA)*** of the gene expression profiles of PDHB was based on TCGA and Genotype Tissue Expression Dataset *** regression analysis and Kaplan-Meier methods were used to assess the co.relation between PDHB expression and survival prognosis in cancer *** co.relation between PDHB and receiver operating characteristic diagnostic curve,clinico.athological staging,somatic mutation,tumor mutation burden(TMB),microsatellite instability(MSI),DNA methylation,and drug susceptibility in pan-cancer was also *** algorithms were used to analyze the co.relation between PDHB and immune cell infiltration and tumor chemotaxis environment,as well as the co.expression analysis of PDHB and immune checkpoint(ICP)*** expression and functional phenotype of PDHB in single tumor cells were studied by single-cell sequencing,and the functional enrichment analysis of PDHB-related genes was *** study also validated the level of mRNA or protein expression of PDHB in several ***,in vitro experiments verified the regulatory effect of PDHB on the proliferation,migration,and invasion of liver *** PDHB was significantly and differently expressed in most *** was significantly associated with prognosis in patients with a wide range of cancers,including kidney renal clear cell carcinoma,kidney renal papillary cell carcinoma,breast invasive carcinom

关键词： Cuprotosis Pyruvate dehydrogenase E1 subunitβ Pan-cancer Prognosis Liver cancer

Bibliometric analysis of the status and trend of biological soil crusts research from 1912 to 2023

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Research in co.d and Arid Regions 2024年第2期16卷 98-108页

作者： XiaoJu Yang FaSi Wu Long Li QingLin Guo ZongRen Yu Songco.g Chen XueYong Zhao Naiman Desertification Research Station Northwest Institute of Eco-Environment and ResourcesChinese Academy of SciencesLanzhouGansu 730000China University of Chinese Academy of sciences Beijing 100049China National Research Center for co.servation of Ancient Wall Paintings and Earthen Sites Dunhuang AcademyDunhuangGansu 736200China Gansu Provincial Research Center for co.servation of Dunhuang Cultural Heritage DunhuangGansu 736200China Cultural Heritage co.servation and Design co.sulting co. Ltd.of Mogao GrottoesDunhuangGansu 736200China

biological soil crusts(BSCs)play an important role in soil development and eco.ogical function,and it is more important for quantitatively analyzing the processes and trends of BSCs to identify the advantages and disadvantages of BSCs research for the development and application of BSCs *** analysis of 2,186 BSCs literatures from Web of science showed an exponential growth trend,as China and the United States as the top 2 in terms of publication *** quality publications are mainly from European and American co.ntries,such as the United States,Germany and *** top 3 publishers are Journal of Arid Environments,Soil Biology&Biochemistry and Plant and Soil,and disciplines include eco.ogy,environmental science,and soil science,etc..Research institutions mainly affiliate to the Chinese Academy of sciences,United States Department of the Interior,United States Geological Survey,Hebrew University of Jerusalem,co.sejo Superior de Investigaciones Cientificas,and Universidad Rey Juan *** mainly co.e from United States,Israel,Spain and *** are mainly from the National Natural science Foundation of China,Spanish Government,Chinese Academy of sciences,and National science Foundation of the United *** soil crusts(biocrusts,cyanobacteria,lichens,moss crusts,bryophytes),drylands,climate change,photosynthesis and desert are high-frequency *** research will focus on the driving mechanisms of BSCs on global biogeochemical cycles,maintaining global biodiversity on important eco.ogical processes,global C,N,and P *** impact on biological invasion,sandstorms,and water balance,multifunctional and reciprocal mechanisms for maintaining the stability of desert and sandy eco.ystems,and impact on the formulation of management policies for arid eco.ystems,co.responding to global climate change,and the estimation of regional,local,and microscale distribution of BSCs based on machine deep learning modeling gradually fo

关键词： biological soil crusts Bibliometric analysis Web of science CiteSpace VOSviewer

Effects of medium fluid cavitation on fluctuation characteristics of magnetic fluid seal interface in agricultural centrifugal pump

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International Journal of Agricultural and biological Engineering 2021年第6期14卷 85-92页

作者： Zhenggui Li Wangxu Li Qifan Wang Ru Xiang Jie Cheng Wei Han Zhaoqiang Yan Key Laboratory of Fluid and Power Machinery Ministry of EducationXihua UniversityChengdu 610039China Huaneng Gansu Hydropower development co. LtdLanzhou 730000China School of Energy and Power Engineering Lanzhou University of TechnologyLanzhou 730050China Zigong Zhaoqiang Sealing Products Industrial co. LtdZigong 643000SichuanChina

The fluctuation law of magnetic fluid seal interface of an agricultural centrifugal pump is theoretically unknown;the pressure and velocity fluctuations are crucial factors that cause interface *** this study,the pressure and velocity fluctuations of the sealing interface on an agricultural centrifugal pump during cavitation were investigated based on the methods of Ansys CFX numerical calculation and experimental *** results demonstrated that at the same flow rate,the pressure fluctuation amplitude of the sealing interface decreased gradually from the shaft surface to the bottom of the polar *** different flow rates,the amplitude of the pressure fluctuation decreased with an increase in the flow *** cavitation of the medium aggravated the impact and water hammer of the liquid,leading to the occurrence of the jitter phenomenon in the sealing interface to accelerate the fluctuation frequency of the axial velocity of the sealing liquid,which accelerated the emulsification of the magnetic *** law can provide a reference for the design of magnetic fluid sealing devices for agricultural centrifugal pumps.

关键词： centrifugal pump magnetic liquid sealing device medium cavitation interface fluctuations

Rabdosia serra alleviates dextran sulfate sodium salt-induced co.itis in mice through anti-inflammation,regulating Th17/Treg balance,maintaining intestinal barrier integrity,and modulating gut microbiota

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Journal of Pharmaceutical Analysis 2022年第6期12卷 824-838页

作者： Hongyi Li Yi Wang Shumin Shao Hui Yu Deqin Wang Chuyuan Li Qin Yuan Wen Liu Jiliang Cao Xiaojuan Wang Haibiao Guo Xu Wu Shengpeng Wang State Key Laboratory of Quality Research in Chinese Medicine Institute of Chinese Medical SciencesUniversity of MacaoMacao999078China Laboratory of Molecular Pharmaco.ogy Department of PharmacologySchool of PharmacySouthwest Medical UniversityLuzhouSichuan646000China Hutchison Whampoa Guangzhou Baiyunshan Chinese Medicine co. Ltd.Guangzhou510000China co.lege of Pharmacy Shenzhen Technology UniversityShenzhenGuangdong518118China School of Pharmacy Lanzhou UniversityLanzhou730000China Macao Centre for Research and development in Chinese Medicine University of MacaoMacao999078China

Rabdosia serra(***),an important co.ponent of Chinese herbal tea,has traditionally been used to treat hepatitis,jaundice,cholecystitis,and ***,the chemical co.position of *** and its effect against co.itis remain *** this study,the chemical co.position of the water extract of *** was analyzed using ultra performance liquid chromatography co.pled with a hybrid linear ion trap quadrupole-orbitrap mass spectrometer(UPLC-LTQ-Orbitrap-MS).A total of 46 co.pounds,co.prising ent-kaurane diterpenoids,flavonoids,phenolic acids,and steroids,were identified in the water extract of ***,and the extract co.ld significantly alleviate dextran sulfate sodium salt-induced co.itis by improving co.on length,upregulating anti-inflammatory factors,downregulating proinflammatory factors,and restoring the balance of T helper 17/T regulatory *** also preserved intestinal barrier function by increasing the level of tight junction proteins(zonula occludens 1 and occludin)in mouse co.onic *** addition,*** modulated the gut microbiota co.position by increasing bacterial richness and diversity,increasing the abundance of beneficial bacteria(Muribaculaceae,Bacteroides,Lactobacillus,and Prevotellaceae_UCG-001),and decreasing the abundance of pathogenic bacteria(Turicibacter,Eubacterium_fissicatena_group,and Eubacterium_xylanophilum_group).Gut microbiota depletion by antibiotics further co.firmed that *** alleviated co.itis in a microbiota-dependent ***,our findings provide chemical and biological evidence for the potential application of *** in the management of co.itis.

关键词： Rabdosia serra Chemical profile co.itis Inflammation Gut microbiota

Design of a highly potent GLP-1R and GCGR dual-agonist for reco.ering hepatic fibrosis

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Acta Pharmaceutica Sinica B 2022年第5期12卷 2443-2461页

作者： Nazi Song Hongjiao Xu Jiahua Liu Qian Zhao Hui Chen Zhibin Yan Runling Yang Zhiteng Luo Qi Liu Jianmei Ouyang Shuohan Wu Suijia Luo Shuyin Ye Runfeng Lin Xi Sun Junqiu Xie Tian Lan Zhongdao Wu Rui Wang Xianxing Jiang School of Pharmaceutical sciences Guangdong Provincial Key Laboratory of Chiral Molecule and Drug DiscoverySun Yat-sen UniversityGuangzhou 510006China Department of Parasitology of Zhongshan School of Medicine Sun Yat-sen UniversityGuangzhou 510006China Key Laboratory of Tropical Disease co.trol Ministry of EducationSun Yat-sen UniversityGuangzhou 510006China Provincial Engineering technology Research Center for biological Vector co.trol Sun Yat-sen UniversityGuangzhou 510006China Research Unit of Peptide science Chinese Academy of Medical SciencesLanzhou 730000China Key Laboratory of Preclinical Study for New Drugs of Gansu Province School of Basic Medical SciencesLanzhou UniversityLanzhou 730000China Shenzhen Turier Biotech.co. Ltd.Shenzhen 518118China Guangdong Pharmaceutical University Guangzhou 510006China

Currently, there is still no effective curative treatment for the development of late-stage liver fibrosis. Here, we have illustrated that TB001, a dual glucagon-like peptide-1 receptor/glucagon receptor(GLP-1 R/GCGR) agonist with higher affinity towards GCGR, co.ld retard the progression of liver fibrosis in various rodent models, with remarkable potency, selectivity, extended half-life and low toxicity. Four types of liver fibrosis animal models which were induced by CCl_(4), a-naphthyl-isothiocyanate(ANIT), bile duct ligation(BDL) and Schistosoma japonicum were used in our study. We found that TB001 treatment dose-dependently significantly attenuated liver injury and co.lagen accumulation in these animal models. In addition to decreased levels of extracellular matrix(ECM) accumulation during hepatic injury, activation of hepatic stellate cells was also inhibited via suppression of TGF-β expression as well as downstream Smad signaling pathways particularly in CCl_(4)-and S. japonicum-induced liver fibrosis. Moreover, TB001 attenuated liver fibrosis through blocking downstream activation of proinflammatory nuclear factor kappa B/NF-kappa-B inhibitor alpha(NFκB/IKBa) pathways as well as cJun N-terminal kinase(JNK)-dependent induction of hepatocyte apoptosis. Furthermore, GLP-1 R and/or GCGR knock-down results represented GCGR played an important role in ameliorating CCl_(4)-induced hepatic fibrosis. Therefore, TB001 can be used as a promising therapeutic candidate for the treatment of multiple causes of hepatic fibrosis demonstrated by our extensive pre-clinical evaluation of TB001.

关键词： GLP-1R GCGR Liver fibrosis Inflammation Apoptosis Candidate peptides

PARK16 rs708730 Polymorphism Decreases Parkinson’s Disease Risk in European Ancestry Population:A Meta-analysis

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Journal of Geriatric Medicine 2019年第2期1卷 15-22页

作者： Zhijie Han Baochu Wei Chenghong Zhang Hongtian Zhu Lei Tang Ruili Lin Dian He Yang Zhang Pingrong Yang Junquan He Pingshun Song 无 Materia Medica development Group Institute of Medicinal ChemistryLanzhou University School of PharmacyLanzhou730000China Department of Bioinformatics School of Basic MedicineChongqing Medical UniversityChongqing400016China lanzhou Pulmonary Hospital Lanzhou730046China Gansu Institute for Drug co.trol Lanzhou730070China lanzhou weihuan biological science and technology development co. Ltd.Lanzhou730000China

Parkinson’s disease(PD)is a co.plex fatal chronic neurodegenerative disease most co.mon in elderly *** early genome-wide association studies(GWAS)found that the minor allele variant of PARK16 rs708730 polymorphism is a significant protective factor for PD in Caucasian ***,these results cannot be repeated by the following studies in Caucasian populations and other *** co.sidered that the inco.sistency of the findings may be caused by the small-scale samples or the heterogeneity among different ***,in this study,we synthesized the previous related GWAS studies through three authoritative sources,and used the large-scale samples(10,645 PD cases and 30,499 co.trols)to reevaluate the association between rs708730 polymorphism and *** results showed that there is no association between them in Asian ancestry ***,in European ancestry population,we found that the minor allele variant(G)of rs708730 polymorphism is significantly associated with a decreased risk of ***,our findings further verified the association of rs708730 with PD and show its genetic heterogeneity among different populations,which can help to develop a better understanding of the PD’s pathogenesis.

关键词： Parkinson’s disease Genome-wide association studies Meta-analysis PARK16 rs708730 polymorphism

Linking microbial carbon pump capacity and efficacy to soil organic carbon storage and stability under heavy metal pollution

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Soil Eco.ogy Letters 2023年第2期5卷 55-63页

作者： Xiao Liu Xia Xu Tian Ma Shiwei Zhou Xiaoli Bi Hongbo He Xudong Zhang weihuan Li co.lege of Agriculture Ludong UniversityYantai 264025China Department of Eco.ogy Co-Innovation Center for Sustainable Forestry in Southern ChinaNanjing Forestry UniversityNanjing 210037China State Key Laboratory of Grassland Agro-eco.ystems College of Pastoral Agriculture Science and TechnologyLanzhou UniversityLanzhou 730020China Yantai Institute of co.stal Zone Research Chinese Academy of SciencesYantai 264003China Institute of Applied Eco.ogy Chinese Academy of SciencesShenyang 110016China

Heavy metal pollution can lead to a great loss of soil organic carbon(SOC).However,the microbial mechanisms that link heavy metal pollution to SOC remain poorly ***,we investigated five apple-orchard soils at different distances from a Pb-Zn *** assessing the heavy metal pollution level based on Grade Ⅱ of the national soil environmental quality standard(China),we found SOC stocks and microbial carbon pump(MCP)capacity(i.e.,microbial residue carbon)under medium and heavy pollution levels were significantly lower than those under safe,co.don and light pollution *** structural equation model showed causality in the SOC variations linked to pollution level through MCP capacity,which co.ld co.tribute 77.8% of the variance in SOC *** verified MCP capacity can serve as a key parameter for evaluation of SOC storage under heavy metal *** MCP efficacy,i.e.,the proportion of microbial residue carbon to SOC,also decreased under medium and heavy *** suggested that,with a heavier pollution level,there was a higher rate of reduction of microbial residue carbon in soil than the rate of reduction of *** MCP efficacy can be a useful assessment of SOC stability,the significantly positive relationship between MCP efficacy and clay co.tent in co.relation analysis implied that lower MCP efficacy was co.related with SOC stability under the heavier pollution *** study provides valuable insights to identify the mechanisms of microbially mediated C transformation processes that are influenced by heavy metal pollution in agroeco.ystems.

关键词： Microbial residues Soil microbial carbon pump Carbonsequestration Heavy metals Agricultural soil

A pan-cancer analysis of the biological function and clinical value of BTLA in tumors

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BIOCELL 2023年第2期47卷 351-366页

作者： XIANGLAI JIANG JIN HE YONGFENG WANG JIAHUI LIU XIANGYANG LI XIANGUI HE HUI CAI Graduate School Ningxia Medical UniversityYinchuan750004China General Surgery Clinical Medical Center Gansu Provincial HospitalLanzhou730000China Key Laboratory of Molecular Diagnostics and Precision Medicine for Surgical Onco.ogy in Gansu Province Gansu Provincial HospitalLanzhou730000China NHC Key Laboratory of Diagnosis and Therapy of Gastrointestinal Tumor Gansu Provincial HospitalLanzhou730000China The First Clinical Medical co.lege of lanzhou University Lanzhou730000China

B and T-lymphocyte attenuator(BTLA)plays an immunosuppressive role by inhibiting T-and B-cell *** is associated with a variety of diseases,especially cancer ***,the function of BTLA in various cancers and its clinical prognostic value have still not been co.prehensively *** study aimed to identify the relationship between BTLA and cancer from the perspectives of differences in BTLA expression,its clinical value,immune infiltration,and the co.relation with immune-related genes in various *** regarding mRNA expression,miRNA expression,lncRNA expression,and clinical data of patients of 33 existing cancers were co.lected from the TCGA *** miRNA of BTLA and the lncRNA that interacts with the target miRNA were obtained from the StarBase *** on bioinformatics analysis methods,the relationship between various types of cancers and BTLA was thoroughly investigated,and a co.peting endogenous RNA network of BTLA,target miRNA,and interacting lncRNA was *** Kaplan-Meier(KM)prognostic analysis of BTLA and target miRNA(has-miR-137)in various types of cancers was co.pleted using the KM *** expression varied in different cancers,with statistical significance in nine cancer *** plotter to analyze the overall survival(OS)and regression-free survival prognosis of cancer patients revealed that the BTLA expression was statistically different in the OS of 11 types of cancers out of 21 types of cancers;the OS of 8 type of cancers was also statistically *** analysis of tumor immune genes revealed a positive co.relation of BTLA expression with immunosuppressive gene(CTLA4 and PDCD1)*** Set Enrichment Analysis showed that BTLA and its co.expressed genes mainly act through biological processes and pathways,including immune response regulation,cell surface receptor signaling pathway,antigen binding,antigen receptor-mediated signaling pathway,and leukocyte *** has t

关键词： Pan-cancer BTLA Tumor immunity Clinical value