检索结果-南通市图书馆

Synthesis and anti-tumor activity of Novel Glycyrrhetinic Acid Derivatives

在线全文

学校读者我要写书评

暂无评论

Chemical Research in Chinese Universities 2012年第2期28卷 214-219页

作者： MENG Yan-qiu DING Jia-qi LIU Yuan NIE Hui-hui GUAN Sai ZOU Chao ZHAO Na CHEN Hong CAO Bo Department of Pharmaceutical Engineering Shenyang University of Chemical TechnologyShenyang 110142P.R.China Department of Pharmacognosy Medical College of Chinese People's Armed Police ForcesTianjin 300162P R.China

Twenty-five derivatives of glycyrrhetinic acid（GA） modified on the A-ring,at C30 and C11 positions were *** in vitro cytotoxicity against various cancer cell lines[henrietta lacks strain of cancer cells（HeLa）,human hepatocellular liver carcinoma cells（HepG2） and human gastric carcinoma cells（BGC-823）] was evaluated by standard MTT[3-（4,5-dimethyl-2-thiazol-yl）-2,5-diphenyl-2H-tetrazolium bromide] *** the tested derivatives were found to have stronger cell growth inhibitory than their parent compound *** them,compounds 3a,5a,and 8d have similar activity on HeLa cell line,and compound 8a has similar activity on HeLa,HepG2 and BGC-823 cell lines as Gefitinib.

关键词： Glycyrrhetinic acid derivative anti-tumor activity Structure modification

Synthesis and anti-tumor activity of Novel Amide Derivatives of Ursolic Acid

在线全文

学校读者我要写书评

暂无评论

Chemical Research in Chinese Universities 2008年第1期24卷 42-46页

作者： LIU Dan MENG Yan-qiu ZHAO Juan CHEN Li-gong College of Pharmaceuticals ＆ Biotechnology Tianjin University Tianjin 300072 P. R. China Faculty of Pharmaceutical Engineering Shenyang Institute of Chemical Technology Shenyang 110142 P. R. China

Ursolic acid was modified at C3 and C28 position to obtain fourteen derivatives including twelve novel compounds, and their chemical structures were characterized by IR, ^1H NMR and MS. Cell growth inhibitory effects of the derivatives against Hela cell were evaluated by MTT assay. All these derivatives were found to have stronger cell growth inhibitory than their parent compound, ursolic acid. The derivatives with a substituted acetyl group at C3 hydroxyl group show better activities than those with an unsubstituted hydroxyl group.

关键词： Ursolic acid Amide derivatives anti-tumor activity

Characterization and anti-tumor activity of Glycopeptides from Ganoderma sinensis

在线全文

学校读者我要写书评

暂无评论

Chemical Research in Chinese Universities 2009年第1期25卷 47-51页

作者： GAO Yang JIANG Ru-zhi CHEN Ying-hong LUO Hao-ming XU Duo-duo GAO Qi-pin research and Development Center Changchun University of Traditional Chinese Medicine Changchun 130117 P R. China Academy of Traditional Chinese Medicine and Material Medica of Jilin Province Changchun 130012 P. R. China

The water-soluble part（GS） of Ganoderma sinense Zhao, Xu et Zhang was divided into high molecular（GS-H） and low molecular（GS-L） parts by Cellulose Super Filtration, and GS was also fractionated into four fractions, GS-1, 2, 3, and 4 by ethanol precipitation according to their molecular weights. Chemical analysis shows that GS and GS-1, 2, 3, 4 were complexes of polysaccharide and peptide. The fractions with molecular weights over 4000, GS-1, 2, 3, and GS-H show anti-tumor activities, however, the fractions with molecular weights lower than 4000, GS-4, and GS-L have no anti-tumor activity, indicating that the anti-tumor activity of Ganoderma Sinensis was caused by glucopeptides with molecular weight ranging from 4000 to 20000. Two purified glucopeptides, GS-6b and GS-7b were obtained from GS-H by ion-exchange and gel-permeation chromatography. Their molecular weights, glycosidic linkages, and configurations were detected by means of IR spectrum, sugar composition analysis, and methylation analysis. The polysaccharide parts of GS-6b and GS-7b had glucan backbone consisting of β-1→3 Glc, and side chain containing glucosyl, mannosyl, fucosyl, xylosyl, galactosyl, and glucuronic acid residues attached on 1-2, 1-4, 1-6 positions of the backbone of GS-6b, or 1-6, 1-4 positions of the backbone of GS-7b. The peptide parts in GS-6b and GS-7b were composed of 10 kinds of amino acids, including Asp, Ser, Arg, Gly, Thr, Pro, Ala, Val, Met, and Lys.

关键词： Ganoderma sinense Zhao, Xu et Zhang anti-tumor activity Glucopeptide β- 1→3 glucan

Synthesis,Crystal Structure and anti-tumor activity of Ethyl 3-(4-methoxyphenyl)-4-oxo-3,3a,4,6-tetrahydro-1H-furo[3,4-c]pyran-3a-carboxylate

在线全文

学校读者我要写书评

暂无评论

Chinese Journal of Structural Chemistry 2011年第12期30卷 1737-1741页

作者：钟涵宇王甜甜张一凯陈焕吕志良张明峰耿冬平牛春娟李科 Department of Medicinal Chemistry School of PharmacySecond Military Medical University

The title compound（ethyl 3-（4-methoxyphenyl）-4-oxo-3,3a,4,6-tetrahydro-1H-furo[3,4-c]pyran-3a-carboxylate） has been synthesized,and its crystal structure was characterized by X-ray single-crystal *** crystal belongs to monoclinic,space group P21/n,with a = 10.124（4）,b = 11.754（4）,c = 13.792（5） ,β = 111.533（3）o,V = 1526.6（10） 3,Z = 4,C17H19O6,Mr = 319.32,Dc = 1.389 g/cm3,F（000） = 676,λ（MoKα） = 0.71073 ,μ = 0.105 mm-1,R = 0.0660 and wR = 0.2027 for 2993 observed reflections（I 2σ（I））.The compound shows potent anti-tumor activity in vitro.

关键词： 3 3a-dihydro-1H-furo[3 4-c]pyran-4(6H)-one synthesis crystal structure anti-tumor activity

CoMFA Model of anti-tumor activity for Fluoroquinolon-3-yl s-Triazole Sulfide-ketone Derivatives and Implications for Molecular Design

在线全文

学校读者我要写书评

暂无评论

Chinese Journal of Structural Chemistry 2021年第6期40卷 703-710,683页

作者： FENG Hui FENG Chang-Jun School of Chemistry&Chemical Engineering Xuzhou University of TechnologyXuzhou 221018China

Comparative molecular field analysis(CoMFA)techniques were used to perform three-dimensional quantitative structure-activity relationship(3D-QSAR)studies on the anti-tumor activity(pIH and pIC)of 28 fluoroquinolon-3-yl s-triazole sulfide-ketone derivatives(FQTSDs)against two cancer cell lines,including human hepatoma Hep-3B cells and human pancreatic cancer Capan-1 cells.23 compounds were randomly selected as the training set to establish the prediction models,which were verified by the test set of 6 compounds containing template *** obtained cross-validation(Rcv2)and non-cross-validation correlation coefficients(R2)of the CoMFA models were 0.477 and 0.850 for pIH,and 0.421 and 0.836 for pIC,*** contributions of steric and electrostatic fields to pIH were determined to be 48.1%and 51.9%,and those to pIC were 49.4%and 50.6%,*** CoMFA models were then used to predict the activities of the compounds in the training and testing sets,and the models had a strong stability and good *** on the 3D contour maps,four novel FQTSDs with a higher anti-tumor activity were ***,the effectiveness of these novel FQTSDs is still needed to be verified by experimental results.

关键词： fluoroquinolon-3-yl s-triazole sulfide-ketone derivative anti-tumor activity 3D-QSAR comparative molecular field analysis molecular design

Cytochalasins Q and 19, 20-epoxycytochalasin C exhibit anti-tumor activity in B16 melanoma cells via creatine metabolic pathways

在线全文

学校读者我要写书评

暂无评论

中国药理学与毒理学杂志 2019年第10期 779-780页

作者： ZHANG Peng LU Yi CHEN Hong-dan WANG Jia TONG Qing-yi TIAN Cheng YANG Jian ZHANG Zi-jun WANG Bao-tian PENG Wen XIANG Ming Department of Pharmacology Hubei Key Laboratory of Natural Medicinal Chemistry and Resource EvaluationSchool of Pharmacy Tongji Medical College Department of Geriatrics Union Hospital Huazhong University of Science and Technology

OBJECTIVE To investigate the anti-tumor activity of cytochalasins, fungal metabolites, isolated from Xylaria sp. DO1801 in B16 melanoma cells and its potential microfilament targeting mechanism. METHODS The structural elucidation of secondary metabolites extracted from Xylaria sp. DO1801 was identified using NMR analysis. Cancer cells and normal cells were employed to evaluate the in vitro cytotoxicity and the in vivo anti-tumor activity. The effects of cytochalasin Q（CQ）and 19, 20-epoxycytochalasin C（ECC） on microfilament and cytoskeleton in B16 cells were observed. The overall profiling of differential metabolites treated with CQ(5 μmol · L;) and ECC(5 μmol · L;) in B16 cells were analyzed by LC-MS/MS. The levels of creatine, phosphocreatine and ATP; protein and mRNA levels of brain-type creatine kinase（CKB） and guanidinoacetate N-methyltransferase（GAMT）; proteins in AMPK pathway and Factin; and m RNA levels of glucose and lipid related metabolic genes were detected. The glyco-lipid metabolism in B16 cells was analyzed as well. RESULTS Four cytochalasins were isolated from Xylaria sp. DO1801, and identified as 19, 20-epoxycytochalasin Q（ECQ）, cytochalasin Q（CQ）, 21-O-deacetyl-19, 20-epoxycytochalasin Q（DEC）, and 19, 20-epoxycytochalasin C（ECC）. These cytochalasin displayed potent anti-proliferation on 8 different cancer cell lines in a dose-dependent manner, but not on 2 non-cancerous cell lines. Additionally, CQ and ECC showed preferential anti-tumor activity in B16 cells and LLC cells. Also, intraperitoneal administration of CQ or ECC significantly suppressed tumor growth in mice bearing transplanted B16 melanoma cells. Interestingly, the microfilament structure of B16 cells was depolymerized after CQ and ECC treatment. Metabolomics analysis exhibited that CQ or ECC mainly inhibited the arginine metabolic pathway, specifically the creatine metabolic pathway. In addition, CQ or ECC presented as potential ligands for CKB by both autodock deciphering and being auth

关键词： cytochalasins anti-tumor activity creatine brain-type creatine kinase microfilament

Expression,Purification and anti-tumor activity of Curcin

在线全文

同方期刊数据库

学校读者我要写书评

暂无评论

Acta Biochimica et Biophysica Sinica 2006年第9期38卷 663-668页

作者： Meng-Jun LUO~1 Xin-Yu YANG~1 Wei-Xin LIU~2 Ying XU~1 Ping HUANG~2 Fang YAN~1 Fang CHEN~1* 1 College of Life Sciences,Sichuan University,Chengdu 610041,China 2 Chengdu Institute for Family Planning,Chengdu 610031,China CollegeofLifeSciences SichuanUniversityChengdu610041China ChengduInstituteforFamilyPlanning Chengdu610031China

Curcin,purified from the seeds of Jatropha curcas,can be used as a cell-killing *** the anti-tumor activity of the recombinant protein of curcin is important for its application inclinical *** segment encoding the mature protein of curcin was inserted into Escherichia colistrain M 15,and the recombinant strain was induced to express by isopropyl-β-D-thiogalactopyranoside at aconcentration of 0.5 *** recombinant protein was expressed in the form of inclusion bodies andpurified by Ni-NTA affinity *** target protein was incubated with the tumor cells atdifferent concentrations for different times and the results demonstrated that the target protein could inhibitthe growth of tumor cells (NCL-H446,SGC-7901 and S180) at 5μg/ml.

关键词： curcin expression purification recombinant protein anti-tumor activity

Oral JS-38,a metabolite from Xenorhabdus sp.,has both anti-tumor activity and the ability to elevate peripheral neutrophils

在线全文

同方期刊数据库

学校读者我要写书评

暂无评论

Chinese Journal of Natural Medicines 2014年第10期12卷 768-776页

作者： LIU Min-Yu XIAO Lin CHEN Geng-Hui WANG Yong-Xiang XIONG Wei-Xia LI Fei LIU Ying HUANG Xiao-Ling DENG Yi-Fang ZHANG Zhen SUN Hai-Yan LIU Quan-Hai YIN Ming School of Pharmacy Shanghai Jiao Tong University Department of Pharmacology Shanghai Institute of Pharmaceutical Industry Beijing Wenfeng Tianji Pharmaceuticals Ltd.

AIM: JS-38(mitothiolore), a synthetic version of a metabolite isolated from Xenorhabdus sp., was evaluated for its anti-tumor and white blood cell(WBC) elevating activities. METHOD: These anti-proliferative activities were assessed in vitro using a panel of ten cell lines. The anti-tumor activities were tested in vivo using B16 allograft mouse models and xenograft models of A549 human lung carcinoma and QGY human hepatoma in nude mice. The anti-tumor interactions of JS-38 and cyclophosphamide(CTX) or 5-fluorouracil(5-Fu) were studied in a S180 sarcoma model in ICR mice. Specific stimulatory effects were determined on peripheral neutrophils in normal and CTX- and 5-Fu-induced neutropenic mice. RESULTS: The IC50 values ranged from 0.1 to 2.0 μmol·L-1. JS-38(1 μmol·L-1) caused an increase in A549 tumor cell apoptosis. Multi-daily gavage of JS-38(15, 30, and 60 mg?kg-1?d-1) inhibited in vivo tumor progression without a significant effect on body weight. JS-38 additively enhanced the in vivo anti-tumor effects of CTX or 5-Fu. JS-38 increased peripheral neutrophil counts and neutrophil rates in normal BALB/c mice almost as effectively as granulocyte colony-stimulating factor(G-CSF). In mice with neutropenia induced by CTX or 5-Fu, JS-38 rapidly restored neutrophil counts. CONCLUSION: These results suggest that JS-38 has anti-tumor activity, and also has the ability to increase peripheral blood neutrophils.

关键词： JS-38 (mitothiolore) Xenorhabdus sp. anti-tumor activity Neutrophils Apoptosis

Establishment of Quality Standard for Freeze-dried Tablets of Polygonatum sibiricum and Study on anti-tumor activity of Diosgenin

在线全文

学校读者我要写书评

暂无评论

Medicinal Plant 2022年第5期13卷 21-25,30页

作者： Jianguang ZENG Zhengyong YU Hao LI Yusheng XU College of Agronomy Hunan Agricultural UniversityChangsha 410128China Hunan University of Humanities Science and TechnologyLoudi 417000China Sanqi Medical College Wenshan UniversityWenshan 663000China

[Objectives]The paper was to establish the quality standard for freeze-dried tablets of Polygonatum sibiricum and to explore the antitumor activity of its extract diosgenin.[Methods]Taking freeze-dried powder samples of *** from 4 different producing areas as materials,and referring to the quality standard of *** in the Chinese Pharmacopoeia(2020 edition),the contents of total ash,moisture,extract,total sugar and diosgenin were determined by total ash determination method,drying method,hot dipping method,0.2%anthrone-sulfuric acid method and HPLC,*** antitumor activities of diosgenin against A431(human epidermal carcinoma cells),H1975(human lung adenocarcinoma cells)and Ramos(human B lymphoblastoma cells)were investigated by MTT assay.[Results]The moisture content of the samples was 2.8%-4.7%(not more than 18.0%);the total ash content was 1.9%-3.4%(not more than 4.0%);the ethanol-soluble extract content was 72.99%-78.99%(not less than 45.0%);and the total sugar content was 7.95%-9.94%(not less than 7.0%).The lowest content of diosgenin was 0.18%,and diosgenin was significantly resistant to A431.[Conclusions]The content determination method established in the study is simple,accurate and reproducible.

关键词： Polygonatum sibiricum HPLC Diosgenin Content determination Quality standard anti-tumor activity