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Preparation of kakkatin derivatives and their anti-tumor activity
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作者 Yu-Ying Jiang Hui-Hua Dong +3 位作者 Wen-Ting Zhou Jia-Zi Luo Xian Wei Yan-Qiang Huang 《World Journal of Clinical Oncology》 2024年第8期1078-1091,共14页
BACKGROUND Modern pharmacological studies have confirmed that plant-derived compounds from Puerariae flos(PF)has significant biological activities against liver damage,tumors and inflammation.Kakkatin is an isoflavone... BACKGROUND Modern pharmacological studies have confirmed that plant-derived compounds from Puerariae flos(PF)has significant biological activities against liver damage,tumors and inflammation.Kakkatin is an isoflavone polyphenolic compound isolated from PF flower.However,the effect of kakkatin and its derivatives on anti-tumor has not been well explored.AIM To design and synthesize a kakkatin derivative[6-(hept-6-yn-1-yloxy)-3-(4-hydroxyphenyl)-7-methoxy-4H-chromen-4-one(HK)]to explore its anti-tumor biological activity.METHODS Hept-6-yn-1-yl ethanesulfonate was introduced to replace hydrogen at the hydroxyl position of kakkatin phenol,and the derivative of kakkatin was prepared;the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide was used to detect cell viability,a clone formation assay was adopted to detect cell proliferation,apoptosis,necrosis,and cell cycles were analyzed by Annexin V/propidium iodide staining and flow cytometry.Cell migration and invasion ability were evaluated by cell scratch assay and transwell assay.The potential mechanism of HK on hepatocellular carcinoma(HCC)SMMC-7721 cells was explored through network pharmacology and molecular docking,and finally real-time PCR assays was used to verify the potential targets and evaluate the biological activity of HK.RESULTS Compared with kakkatin,the modified HK did not significantly increase the inhibitory activity of gastric cancer MGC803 cells,but the inhibitory activity of HCC SMMC-7721 cells was increased by about 30 times,with an IC50 value of 2.5μM,and the tumor inhibition effect was better than cisplatin,which could significantly inhibit the cloning,invasion and metastasis of HCC SMMC-7721 cells,and induce apoptosis and G2/M cycle arrest.Its mechanism of action is mainly related to the upregulation of PDE3B and NFKB1 target proteins in the cAMP pathway.CONCLUSION HK have a significant inhibitory effect on HCC SMMC-7721 cells,and the targets of their action may be PDE3B and NFKB1 proteins in the cAMP pathway,making it a good lead drug for the treatment of HCC. 展开更多
关键词 Kakkatin DERIVATIVE Hepatocellular carcinoma anti-tumor Biological activity
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Screening for Anti-tumor Activity of Fractions from Buddleja officinalis Maxim
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作者 Tong LI Xin XIE +9 位作者 Liyuan LI Aipeng LI Zhidong LEI Tingting HE Sirui MO Shangfeng HUANG Yao LIN Suoyi HUANG Lixiang LU Shiyou ZHOU 《Medicinal Plant》 2024年第2期48-50,56,共4页
[Objectives]The anti-tumor activity of fractions from Buddleja officinalis Maxim.by petroleum ether,ethyl acetate,n-butanol and water solvent was studied.[Methods]The ethanol extract from B.officinalis Maxim.was extra... [Objectives]The anti-tumor activity of fractions from Buddleja officinalis Maxim.by petroleum ether,ethyl acetate,n-butanol and water solvent was studied.[Methods]The ethanol extract from B.officinalis Maxim.was extracted and then concentrated with petroleum ether,ethyl acetate,n-butanol and water,respectively,and the extracts were obtained.The inhibitory effects of the four different fractions on the growth of three tumor cell lines in vitro were detected by CCK-8 method,and the median inhibitory concentration(IC 50 value)was calculated.[Results]The four fractions inhibited the growth of the three tumor cell lines in vitro,among which the n-butanol fraction had the best anti-tumor activity.The IC 50 values of the n-butanol fraction on human gastric cancer(SGC-7901),human breast cancer(MCF-7)and human liver cancer(BEL-7404)cell lines were 0.08,1.58 and 0.12 mg/mL,respectively.[Conclusions]Petroleum ether,ethyl acetate,n-butanol and water fractions from the ethanol extract of B.officinalis Maxim.had certain anti-tumor effects,and the n-butanol fraction had the best anti-tumor activity. 展开更多
关键词 Buddleja officinalis Maxim. Tumor cells anti-tumor activity screening
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Anti-tumor Activity of Isovanillin and Its Molecular Mechanism
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作者 Jingchao WANG Mingxinzhi WANG Chenghao JIN 《Medicinal Plant》 CAS 2023年第1期100-102,105,共4页
Taking isovanillin and the important products synthesized from raw materials of isovanillin as objects,this paper reviews its pharmacological effects and molecular mechanisms,including inhibiting tumor angiogenesis,bl... Taking isovanillin and the important products synthesized from raw materials of isovanillin as objects,this paper reviews its pharmacological effects and molecular mechanisms,including inhibiting tumor angiogenesis,blocking cancer cell self-repair,inducing cancer cell DNA fragmentation,cytotoxicity,inhibiting tumor growth,regulating brain nerves,inhibiting renin and other pharmacological effects,etc.,which provide new ideas for the in-depth research and development of isovanillin. 展开更多
关键词 Isovanillin Biological activity Pharmaceutical intermediates anti-tumor
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Synthesis and Anti-tumor Activity of Novel Amide Derivatives of Ursolic Acid 被引量:8
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作者 LIU Dan MENG Yan-qiu +1 位作者 ZHAO Juan CHEN Li-gong 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2008年第1期42-46,共5页
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 ... 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. 展开更多
关键词 Ursolic acid Amide derivatives anti-tumor activity
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Characterization and Anti-tumor Activity of Glycopeptides from Ganoderma sinensis 被引量:5
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作者 GAO Yang JIANG Ru-zhi +3 位作者 CHEN Ying-hong LUO Hao-ming XU Duo-duo GAO Qi-pin 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2009年第1期47-51,共5页
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 fractio... 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. 展开更多
关键词 Ganoderma sinense Zhao Xu et Zhang anti-tumor activity Glucopeptide β- 1→3 glucan
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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
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作者 钟涵宇 王甜甜 +6 位作者 张一凯 陈焕 吕志良 张明峰 耿冬平 牛春娟 李科 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2011年第12期1737-1741,共5页
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 diffraction.The c... 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 diffraction.The 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. 展开更多
关键词 3 3a-dihydro-1H-furo[3 4-c]pyran-4(6H)-one SYNTHESIS crystal structure anti-tumor activity
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Synthesis and Anti-tumor Activity of Novel Glycyrrhetinic Acid Derivatives
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作者 MENG Yan-qiu DING Jia-qi +6 位作者 LIU Yuan NIE Hui-hui GUAN Sai ZOU Chao ZHAO Na CHEN Hong CAO Bo 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2012年第2期214-219,共6页
Twenty-five derivatives of glycyrrhetinic acid(GA) modified on the A-ring,at C30 and C11 positions were synthesized.Their in vitro cytotoxicity against various cancer cell lines[henrietta lacks strain of cancer cell... Twenty-five derivatives of glycyrrhetinic acid(GA) modified on the A-ring,at C30 and C11 positions were synthesized.Their 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] assay.All the tested derivatives were found to have stronger cell growth inhibitory than their parent compound GA.Among 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. 展开更多
关键词 Glycyrrhetinic acid derivative anti-tumor activity Structure modification
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Establishment of Quality Standard for Freeze-dried Tablets of Polygonatum sibiricum and Study on Anti-tumor Activity of Diosgenin
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作者 Jianguang ZENG Zhengyong YU +1 位作者 Hao LI Yusheng XU 《Medicinal Plant》 CAS 2022年第5期21-25,30,共6页
[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 ... [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 P.sibiricum from 4 different producing areas as materials,and referring to the quality standard of P.sibiricum 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,respectively.The 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. 展开更多
关键词 Polygonatum sibiricum HPLC DIOSGENIN Content determination Quality standard anti-tumor activity
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Synthesis and Anti-tumor Activity Study of Shogaol Analogues
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作者 Song Lei Duan Yu +1 位作者 Xu Da Mao Yu 《Journal of Pharmacy and Pharmacology》 2018年第10期907-919,共13页
As one of the largest global public health problems, cancer greatly endangers human health. Researchers have been committed to discovering anticancer drugs with high efficiency and low toxicity. Shogaol, a kind of ing... As one of the largest global public health problems, cancer greatly endangers human health. Researchers have been committed to discovering anticancer drugs with high efficiency and low toxicity. Shogaol, a kind of ingredient from ginger with high anti-tumor activity, has attracted our attention. This study was an investigation on the composition and structure-activity relationship of different analogues of shogaol, with the purpose to screen for shogaol compounds which had higher anti-tumor activity and could be easily synthesized. We chose zingerone as the starting material to synthesize shogaol through four-step reactions without protective group, as a result, 31 analogues were synthesized for anti-tumor activity detect. The biological test results showed that: the missing of the unsaturated ketone and the phenolic hydroxyl group reduced the anti-tumor activity of shogaol; the site of phenolic hydroxyl had no significant influence on the anti-tumor activity, the indicating that the larger the steric hindrance of substituent, the lower the activity, but the higher the activity of cyclobutyl substituted derivatives. 展开更多
关键词 SHOGAOL SYNTHESIS ANALOGUES anti-tumor activity.
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3D-QSAR Studies on the Anti-tumor Activity of N-Aryl-salicylamide Derivatives 被引量:23
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作者 FENG Hui FENG Chang-Jun 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2019年第11期1874-1880,共7页
In the present work,comparative molecular field analysis(CoMFA)techniques were used to perform three-dimensional quantitative structure-activity relationship(3D-QSAR)studies on the anti-tumor activity(pHi,i=1,2,3,4)of... In the present work,comparative molecular field analysis(CoMFA)techniques were used to perform three-dimensional quantitative structure-activity relationship(3D-QSAR)studies on the anti-tumor activity(pHi,i=1,2,3,4)of N-aryl-salicylamide derivatives against four cancer cell lines,including A549,MCF-7,SGC-7901,and Bel-7402.12 compounds were randomly selected as the training set to establish the prediction models,which were verified by the test set of 5 compounds containing template molecule.The contributions of steric and electrostatic fields to pH1,pH2,pH3,and pH4 were 23.8% and 76.2%,20.1% and 79.9%,18.7% and 81.3%,and 14.3%and 85.7%,respectively.The cross-validation(Rcv 2)and non-cross-validation coefficients(R2)were 0.826 and 0.963 for pH1,0.867 and 0.974 for pH2,0.941 and 0.989 for pH3,and 0.797 and 0.961 for pH4,respectively.The CoMFA models were then used to predict the activities of the compounds,and it was found that the models had strong stability and good predictability.Based on the CoMFA contour maps,some key structural factors responsible for the anticancer activity of the series of compounds were revealed.The results provide some useful theoretical references for understanding the mechanism of action,designing new N-aryl-salicylamide derivatives with high anti-tumor activity,and predicting their activities. 展开更多
关键词 N-aryl-salicylamide derivatives anti-tumor activity 3D-QSAR COMFA
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Extraction, Purification and Anti-tumor Activity of Polysaccharide from Mycelium of Mutant Cordyceps Militaris 被引量:7
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作者 ZHANG Ai-li LU Jia-hui ZHANG Na ZHENG Dan ZHANG Gui-rong TENG Li-rong 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2010年第5期798-802,共5页
A water-soluble polysaccharide(named MCMP) was isolated from the mycelium with high yield mutation Cordyceps militaris by hot-water extraction, deproteinization by sevage, alcohol precipitation, anion-exchange and g... A water-soluble polysaccharide(named MCMP) was isolated from the mycelium with high yield mutation Cordyceps militaris by hot-water extraction, deproteinization by sevage, alcohol precipitation, anion-exchange and gel filtration chromatography CL-6B. The polysaccharide contained mannose, rhamnose, galactose and glucose in a molar ratio of 59.36:1:8.31:39.50, of which the average molecular weight is 8100. In our research, Hep-G2 cells, Hela cells and mesangial cells were chosen to determine the anti-tumor activity of the polysaccharide. The results of MTT assay show that polysaccharides of the mutant strain presented inhibitory activity on the cells proliferation after 48 h incubation. 展开更多
关键词 Cordyceps militaris POLYSACCHARIDE anti-tumor
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Evaluation of cytotoxic and anti-tumor activity of partially purified serine protease isolate from the Indian earthworm Pheretima posthuma 被引量:3
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作者 Mahendra Kumar Verma Francies Xavier +1 位作者 Yogendra Kumar Verma Kota Sobha 《Asian Pacific Journal of Tropical Biomedicine》 SCIE CAS 2013年第11期896-901,共6页
Objective:To isolate,partially purify and evaluate the cytotoxic and antitumor activity of a serine protease from the chosen Indian earthworm Pheretima posthuma.Methods:Whole animal extract was prepared and purified i... Objective:To isolate,partially purify and evaluate the cytotoxic and antitumor activity of a serine protease from the chosen Indian earthworm Pheretima posthuma.Methods:Whole animal extract was prepared and purified its protein constituents by size and charge based chromatographic separation techniques using Sephadex G-50 and DEAE-Cellulose resin respectively.Average molecular weight of the protein isolate was determined and analyzed for its cytotoxic property against Vero cells in different dilutions(1:20 and 1:40)and anti-tumor activity by MTT assay(a colorimetric assay)using breast cancer cell line MCF-7,with tamoxifen as standard.Results:One of the protein constituents after purification was characterized as serine protease by Caseinolytic plate diffusion assay.Average molecular weight of this purified isolate was determined,by SDS-PAGE analysis with standard protein ladder,as of 15 kDa.The performed tests suggested that the 15kDa fraction has potent cytotoxic activity and satisfactory antitumor activity as well in vitro.Conclusions:Exact molecular mechanism of the cytotoxic and antitumor activities is yet to be explored and currently we are working on ultra-purification and biophysical characterization of this fraction.Further investigation into the mechanism(s)of cytotoxic and antitumor activities at molecular level would be useful in treatment of various classes of cancer and viral infections in future. 展开更多
关键词 EARTHWORM FIBRINOLYTIC enzyme Cytotoxicity Antitumor activity SERINE PROTEASE Minimum inhibitory concentration
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Synthesis,Crystal Structure,Thermal Stability and Anti-tumor Activity In Vitro of Bis(tricyclohexyltin) Pimelicarboxylate 被引量:2
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作者 朱小明 邝代治 +4 位作者 冯泳兰 张复兴 庾江喜 蒋伍玖 张志坚 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2015年第11期1652-1658,共7页
Bis(tricyclohexyltin) pimelicarboxylate, [(CH2)5(CO2SnCy3)2] (1), has been synthesized by the reaction of tricyclohexyltin hydroxide with pimelic acid and characterized by means of 1R, 1H and 13C NMR, elementa... Bis(tricyclohexyltin) pimelicarboxylate, [(CH2)5(CO2SnCy3)2] (1), has been synthesized by the reaction of tricyclohexyltin hydroxide with pimelic acid and characterized by means of 1R, 1H and 13C NMR, elemental analysis and X-ray diffraction. Complex 1 crystallizes in triclinic space group Pi with a = 11.569(3), b = 12.0419(2), c = 17.3988(4) A, α = 81.4310(10), β = 79.8270(10), ), = 69.7060(10)°, V = 2227.60(9) A3, Z = 2, C43H7604Sn2, Mr = 894.42, Dc = 1.333 g.cm-3, μ = 1.157 mm-1, F(000) = 932, GOOF = 1.339, the final R = 0.0452 and wR = 0.1333 for 6709 observed reflections (1〉 2σ(I). Complex 1 shows discrete dimeric structures and the tin atoms have a distorted tetrahedral geometry. The 1D chain structure of complex 1 is formed by intermolecular Sn…O interactions. Complex 1 displays good thermal stability under 553 K and has selective antibacterial property. Complex 1 is strong in vitro anti-tumor activity against five human tumor cell lines, Colo205, HepG2, MCF-7, Hela and NCI-H460, and is significantly higher than that in the clinical use of carboplatin. 展开更多
关键词 tricyciohexyltin pimelicarboxylate synthesis crystal structure biological activity
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Study on Anti-tumor Activity and Mechanism of Isoorientin
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作者 Tong ZHANG Yu ZHANG +3 位作者 Shinong WANG Jiaru WANG Yinghua LUO Chenghao JIN 《Medicinal Plant》 CAS 2019年第1期7-9,共3页
Isoorientin can play an anti-tumor effect through interfering with tumor cell proliferation, inducing tumor cell apoptosis, regulating reactive oxygen species level, inducing tumor cell autophagy, blocking tumor cell ... Isoorientin can play an anti-tumor effect through interfering with tumor cell proliferation, inducing tumor cell apoptosis, regulating reactive oxygen species level, inducing tumor cell autophagy, blocking tumor cell infiltration and metastasis, inhibiting tumor neovascularization and other pathways. This paper reviews the research progress of anti-tumor activity and mechanism of isoorientin in recent years. 展开更多
关键词 Isoorientin anti-tumor APOPTOSIS AUTOPHAGY CELL PROLIFERATION
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Effect of anti-asthma Chinese medicine Chuankezhi on the anti-tumor activity of cytokine-induced killer cells 被引量:5
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作者 Jing-Jing Zhao Ke Pan +5 位作者 Qi-Jing Wang Zheng-Di Xu De-Sheng Weng Jian-Jun Li Yong-Qiang Li Jian-Chuan Xia 《Chinese Journal of Cancer》 SCIE CAS CSCD 2013年第10期553-560,共8页
Chuankezhi(CKZ),a new Chinese medicine,plays an important role in immunoregulation.Cytokineinduced killer(CIK)cells have been commonly used for immunotherapy in recent years.In this study,we aimed to investigate the i... Chuankezhi(CKZ),a new Chinese medicine,plays an important role in immunoregulation.Cytokineinduced killer(CIK)cells have been commonly used for immunotherapy in recent years.In this study,we aimed to investigate the immunoregulatory effect of CKZ on CIK cells.Peripheral blood monocytes were isolated from healthy donors,and CIK cells were generated by culturing monocytes with interferon-gamma(IFN-γ)and interleukin 2.Different concentrations of CKZ were added on day 2.After incubation for 14days in culture,the antitumor effects of CIK cells were measured by cytotoxicity assay.Flow cytometry was used to explore the effect of CKZ on CIK cell immunophenotype,intracellular cytokine production,and apoptosis.The effect of CKZ on the antitumor activity of CIK cells in nude mice was also investigated.CKZ increased the percentage of CD3+CD56+CIK cells but did not significantly change the percentage of CD4+,CD8+,or CD4+CD25+CIK cells.CKZ-conditioned CIK cells showed a greater ability to kill tumor cells,as well as a higher frequency of IFN-γand TNF-αproduction,compared with the CIK cells in the control group.CKZ also suppressed the apoptosis of CIK cells in vitro.Furthermore,CKZ combined with CIK cells had a stronger suppressive effect on tumor growth in vivo than the CIK,CKZ,or normal saline control groups.Our results indicate that CKZ enhances the antitumor activity of CIK cells and is a potential medicine for tumor immunotherapy. 展开更多
关键词 抗肿瘤活性 杀伤细胞 中国医药 细胞因子 外周血单核细胞 抗哮喘 免疫调节作用 IFN-γ
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Preparation and Photodynamic Anti-tumor Activity of Magnetic Polylactic Acid Nanoparticles Loaded with Photosensitizer
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作者 杨晓霞 黄慧 +3 位作者 陈志龙 黄鹏 孙筠 周兴平 《Journal of Donghua University(English Edition)》 EI CAS 2010年第3期306-311,共6页
A novel magnetic nanocarrier was strategically designed and successfully prepared.Photosensitizer 2,7,12,18-tetramethyl-3,8-di-(1-propoxyethyl)-13,17-bis-(3-hydroxypropyl)porphyrin(PHPP)was encapsulated into polylacti... A novel magnetic nanocarrier was strategically designed and successfully prepared.Photosensitizer 2,7,12,18-tetramethyl-3,8-di-(1-propoxyethyl)-13,17-bis-(3-hydroxypropyl)porphyrin(PHPP)was encapsulated into polylactic acid(PLA)-coated Fe3O4 nanoparticles.The diameter of nanocarrier is 30-50 nm by transmission electron micrograph(TEM).The encapsulation efficiency of photosensitizer is 27.98% calculated from UV-vis absorption spectra.The nanocarrier shows obvious photocytotoxic activity to Hela299 tumor cells in vitro. 展开更多
关键词 photocytotoxic activity PHOTOSENSITIZER polylactic acid(PLA) magnetic nanocarriers TUMOR
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Compound Astragalus and Salvia miltiorrhiza extract exerts anti-tumor activity by intervening the interaction of microRNA-145/microRNA-21 and Smad3C/3L phos-phorylation in hepatocellular carcinoma
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作者 Chao WU Meng FANG Yan YANG 《中国药理学与毒理学杂志》 CAS CSCD 北大核心 2018年第4期312-313,共2页
OBJECTIVBE To investigate the intervention of compound Astragalus and Salvia miltiorrhiza extract(CASE) consisted of astragalosides,astragalus polysaccharides and salvianolic acids on the interaction of microRNA-145/m... OBJECTIVBE To investigate the intervention of compound Astragalus and Salvia miltiorrhiza extract(CASE) consisted of astragalosides,astragalus polysaccharides and salvianolic acids on the interaction of microRNA-145/microRNA-21(miR-145/miR-21) and Smad3 C/3 L phosphorylation(pSmad3 C/pSmad3 L) down-stream of transforming growth factor-β(TGF-β)/mitogen activated protein kinase(MAPK) signaling in hepatocellular carcinoma(HCC) progression by in vitro and in vivo experi.ments.METHODS In HepG2 cells and xenografts of nude mice,antagomir/agomir and plasmids of Smad3 C/3 L phosphorylation site mutation(Smad3 3 S-A/Smad3 EPSM) were used to intervene miR-145/miR-21 and pSmad3 C/pSmad3 L expression respectively,then incorporative CASE treatment.Cell proliferation,migration,apoptosis,tumor growth and histopathologic characteristics of xenografts,relevant proteins of TGF-β/Smad pathway and miR-145/miR-21 were evaluated.RESULTS CASE up-regulated miR-145 while down-regulated miR-21,inhibited cell proliferation,migration and tumor growth,accelerated cell apoptosis in HepG2 cells respectively transfected with Smad3 WT,Smad3 EPSM,Smad3 3 S-A plasmids in cultured dishes and xenografts of nude mice,the above effects were more evident in HepG2 cells with increased pSmad3 C.In TGF-β1-stimulated HepG2 cells and xenografts of nude mice,CASE antagonized the facilitating effects of miR-145 antagomir/miR-21 agomir on cell migration,proliferation,tumor growth and inhibiting effects of miR-145 antagomir/miR-21 agomir on cell apoptosis;CASE increased miR-145 down-regulated by miR-145 antagomir and decreased miR-21 up-regulated by miR-21 agomir,reduced protein level of pSmad3 L and their proteins including TβRⅡ,pERK1/2,pJNK1/2 and pp38 while elevated pSmad3 C expression.CONCLUSION These results suggest that pSmad3 C/pSmad3 L maybe interact with miR-145/miR-21 in HCC progression,which may be one of important molecular mechanisms of CASE's anti-HCC effects. 展开更多
关键词 黄芪丹参 蛋白酶 治疗方法 中医
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Immunomodulatory Function of Pien Tze Huang in T Cell-Mediated Anti-tumor Activity against B16-F10,MC38 and Hep1-6 Tumor Models 被引量:1
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作者 FU Yu-bing LIU Chen-feng +8 位作者 WANG Jin-jia JI Xiao-lin TANG Rong-han LIAO Kun-yu CHEN Ling-yue HONG Ya-zhen FAN Bin-bin WANG Shi-cong LIU Wen-Hsien 《Chinese Journal of Integrative Medicine》 SCIE CAS CSCD 2024年第4期348-358,共11页
Objective To investigate the anti-tumor effects of Pien Tze Huang(PZH)in mouse models of B16–F10 melanoma,MC38 colorectal cancer,Hep1-6 hepatocellular carcinoma and chemically induced hepatocellular carcinoma model.M... Objective To investigate the anti-tumor effects of Pien Tze Huang(PZH)in mouse models of B16–F10 melanoma,MC38 colorectal cancer,Hep1-6 hepatocellular carcinoma and chemically induced hepatocellular carcinoma model.Methods Various tumor models,including B16–F10,MC38 and Hep1-6 tumor hypodermic inoculation models,B16–F10 and Hep1-6 pulmonary metastasis models,Hep1-6 orthotopic implantation model,and chemically induced hepatocellular carcinoma model,were utilized to evaluate the anti-tumor function of PZH.Tumor growth was assessed by measuring tumor size and weight of solid tumors isolated from C57BL/6 mice.For cell proliferation and death of tumor cells in vitro,as well as T cell activation markers,cytokine production and immune checkpoints analysis,single-cell suspensions were prepared from mouse spleen,lymph nodes,and tumors after PZH treatment.Results PZH demonstrated significant therapeutic efficacy in inhibiting tumor growth(P<0.01).Treatment with PZH resulted in a reduction in tumor size in subcutaneous MC38 colon adenocarcinoma and B16–F10 melanoma models,and decreased pulmonary metastasis of B16–F10 melanoma and Hep1-6 hepatoma(P<0.01).However,in vitro experiments showed that PZH only had slight impact on the cell proliferation and survival of tumor cells(P>0.05).Nevertheless,PZH exhibited a remarkable ability to enhance T cell activation and the production of interferon gamma,tumor necrosis factor alpha,and interleukin 2 in CD4^(+)T cells in vitro(P<0.01 or P<0.05).Importantly,PZH substantially inhibited T cell exhaustion and boosted cytokine production by tumor-infiltrating CD8^(+)T cells(P<0.01 or P<0.05).Conclusion This study has confirmed a novel immunomodulatory function of PZH in T cell-mediated anti-tumor immunity,indicating that PZH holds promise as a potential therapeutic agent for cancer treatment. 展开更多
关键词 Pien Tze Huang METASTASIS anti-tumor immunity T cell activation T cell exhaustion immune checkpoints Chinese medicine
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Association between physical activity and risk of gastroesophageal reflux disease:A systematic review and meta-analysis 被引量:2
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作者 Chuting Yu Tinglu Wang +7 位作者 Ye Gao Yunfei Jiao Huishan Jiang Yan Bian Wei Wang Han Lin Lei Xin Luowei Wang 《Journal of Sport and Health Science》 SCIE CAS CSCD 2024年第5期687-698,共12页
Background:Lifestyle plays an important role in preventing and managing gastroesophageal reflux disease(GERD).In response to the conflicting results in previous studies,we performed a systematic review and meta-analys... Background:Lifestyle plays an important role in preventing and managing gastroesophageal reflux disease(GERD).In response to the conflicting results in previous studies,we performed a systematic review and meta-analysis to investigate this association.Methods:Relevant studies published until January 2023 were retrieved from 6 databases,and the prevalence of symptomatic gastroesophageal reflux(GER)or GERD was determined from the original studies.A random effects model was employed to meta-analyze the association by computing the pooled relative risk(RR)with 95%confidence intervals(95%CIs).Furthermore,subgroup and dose-response analyses were performed to explore subgroup differences and the association between cumulative physical activity(PA)time and GERD.Results:This meta-analysis included 33 studies comprising 242,850 participants.A significant negative association was observed between PA and the prevalence of symptomatic GER(RR=0.74,95%CI:0.66-0.83;p<0.01)or GERD(RR=0.80,95%CI:0.76-0.84;p<0.01),suggesting that engaging in PA might confer a protective benefit against GERD.Subgroup analyses consistently indicated the presence of this association across nearly all subgroups,particularly among the older individuals(RR_(<40 years):RR_(≥40 years)=0.85:0.69,p<0.01)and smokers(RR_(smoker):RR_(non-smoker)=0.67:0.82,p=0.03).Furthermore,a dose-response analysis revealed that individuals who engaged in 150 min of PA per week had a 72.09%lower risk of developing GERD.Conclusion:Maintaining high levels of PA decreased the risk of GERD,particularly among older adults and smokers.Meeting the recommended PA level of 150 min per week may significantly decrease the prevalence of GERD. 展开更多
关键词 Physical activity Gastroesophageal reflux disease PREVALENCE Systematic review
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Association of accelerometer-measured sleep duration and different intensities of physical activity with incident type 2 diabetes in a population-based cohort study 被引量:2
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作者 Xinyi Jin Yilin Chen +8 位作者 Hongliang Feng Mingqing Zhou Joey W.Y.Chang Yaping Liu Alice Pik Shan Kong Xiao Tan Yun-Kwok Wing Yannis Yan Liang Jihui Zhang 《Journal of Sport and Health Science》 SCIE CAS CSCD 2024年第2期222-232,共11页
Purpose:The aim of the current study was to investigate the association of accelerometer-measured sleep duration and different intensities of physical activity(PA)with the risk of incident type 2 diabetes in a populat... Purpose:The aim of the current study was to investigate the association of accelerometer-measured sleep duration and different intensities of physical activity(PA)with the risk of incident type 2 diabetes in a population-based prospective cohort study.Methods:Altogether,88,000 participants(mean age=62.2±7.9 years,mean±SD)were included from the UK Biobank.Sleep duration(short:<6 h/day;normal:6-8 h/day;long:>8 h/day)and PA of different intensities were measured using a wrist-won accelerometer over a 7-day period between 2013 and 2015.PA was classified according to the median or World Health Organization-recommendation:total volume of PA(high,low),moderate-to-vigorous PA(MVPA)(recommended,not recommended),and light-intensity PA(high,low).Incidence of type 2diabetes was ascertained using hospital records or death registries.Results:During a median follow-up of 7.0 years,1615 incident type 2 diabetes cases were documented.Compared with normal sleep duration,short(hazard ratio(HR)=1.21,95%confidence interval(95%CI):1.03-1.41)but not long sleep duration(HR=1.01,95%CI:0.89-1.15)was associated with excessive type 2 diabetes risk.This increased risk among short sleepers seems to be protected against by PA.Compared with normal sleepers with high or recommended PA,short sleepers with low volume of PA(HR=1.81,95%CI:1.46-2.25),not recommended(below the World Health Organization-recommended level of)MVPA(HR=1.92,95%CI:1.55-2.36),or low light-intensity PA(HR=1.49,95%CI:1.13-1.90)had a higher risk of type 2 diabetes,while short sleepers with a high volume of PA(HR=1.14,95%CI:0.88-1.49),recommended MVPA(HR=1.02,95%CI:0.71-1.48),or high light-intensity PA(HR=1.14,95%CI:0.92-1.41)did not.Conclusion:Accelerometer-measured short but not long sleep duration was associated with a higher risk of incident type 2 diabetes.A higher level of PA,regardless of intensity,potentially ameliorates this excessive risk. 展开更多
关键词 Light physical activity Sleep duration Triaxial accelerometer Type 2 diabetes UK Biobank
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