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121 个结果
  • 简介:Objective:ToinvestigatetheeffectsofE7080andN5-(1-iminoethyl)-L-ornithinedihydrochloride(L-NIO)oncolorectalcanceraloneandincombination.Methods:HT29colorectalcancercelllinefromSapInstitutewasused.Real-timecellanalysis(xCELLigencesystem)wasperformedtodeterminetheeffectsofE7080andL-NIOoncolorectalcellproliferation.WhileapoptosiswasdeterminedwithAnnexinVstaining,andtheeffectofagentsonangiogenesiswasdeterminedwithchorioallantoicmembrane(CAM)model.Results:WefoundthatE7080hasastrongantiproliferativeeffectwithanhalfmaximuminhibitionofconcentration(IC50)valueof5.60×10–8mol/L.AlsoithasbeenobservedthatE7080showedantiangiogenicandapoptoticeffectsonHT29colorectalcancercells.AntiangiogenicscoresofE7080were1.2,1.0and0.6for100,10and1nmol/LE7080concentrations,respectively.Furthermore,apoptosishasbeendetectedin71%ofHT29colorectalcancercellsafteradministrationof100nmol/LE7080whichmayindicatestrongapoptoticeffect.MeanwhileadministrationofL-NIOalonedidnotshowanyeffect,butthecombinationofE7080withL-NIOincreasedtheantiproliferative,antiangiogenicandapoptoticeffectsofE7080.Conclusions:ResultsofthisstudyindicatethatE7080maybeagoodchoiceintreatmentofcolorectaltumors.FurthermoretheincreasedeffectsofE7080whencombinedwithL-NIOraisethepossibilitytousealowerdoseofE7080andthereforeavoid/minimizethesideeffectsobservedwithE7080.

  • 标签: 酪氨酸激酶抑制剂 结直肠癌 NOS抑制剂 结肠 抗血管生成 细胞凋亡
  • 简介:瞄准:在与clinicopathological特征和成纤维细胞生长因素受体1的表示(FGFR1)和ephrinligands的关系在胃的癌症澄清Ephrin受体A4(EphA4)的表示和角色。方法:十一根胃的癌房间线,胃的腺癌的24个配对的外科的新鲜标本并且邻近非,肿瘤组织,74个常规修理福尔马林的、嵌入石蜡的肿瘤标本,和55个标本在组织上看到微数组(TMA)被分析。反向的transcription-PCR(RT-PCR),即时RT-PCR,免疫组织化学,和房间生长试金被执行。结果:EphA4mRNA表示的Overexpression在8被观察(73%)11胃的癌症,房间排队并且10(42%)24胃的癌症纸巾。EphA4的Overexpression,由免疫组织化学分析了,在62被观察(48%)129胃的癌症纸巾。在蛋白质水平,在表示上的EphA4显著地与侵略和复发的深度被联系。在表示上的EphA4也在表示上与FGFR1被相关。有EphA4积极的癌症的病人比有显著地更短的全面幸存时期与EphA4否定的癌症做了那些(P=0.0008)。为ephrinligands的mRNAs是在在胃的癌症房间线和癌症纸巾的各种各样的联合的coexpressed。由在EphA4-overexpressing胃的癌症房间线的siRNA的EphA4表示的Downregulation在房间生长导致了重要减少。结论:我们的结果建议那在胃的癌症在EphA4的表示上起一个作用。

  • 标签: 胃癌 纤维原细胞生长因子受体1 酪氨酸激酶 预后
  • 简介:Cancerevadeshostimmunesurveillancebyusingimmunecheckpoints,whichareinhibitorypathwayscrucialformaintainingself-tolerance1.Tumorcellsexpressmultipleinhibitoryligands,andtumor-infiltratinglymphocytes(TIL)expressavarietyofinhibitoryreceptors.InhibitoryreceptorscytotoxicT-lymphocyte-associatedprotein4(CTLA-4)andprogrammeddeath-1

  • 标签: 酪氨酸激酶抑制剂 EGFR 细胞毒性T淋巴细胞 宿主免疫 肿瘤浸润 CTLA-4
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  • 简介:BACKGROUND:Ithasbeenshownthatginsenoside,theeffectivecomponentofginseng,canenhanceexpressionofcholineacetyltransferase,aswellasbrain-derivedneurotrophicfactor(BDNF)anditsreceptortyrosinekinaseB(TrkB),incholinergicneuronsofthebasalforebrain.OBJECTIVE:ToqualitativelyandquantitativelyverifytheinfluenceofginsenosideonexpressionofBDNFanditsreceptor,TrkB,inthemedialseptumofagedrats,andtoprovideamolecularbasisforclinicalapplication.DESIGN,TIMEANDSETTING:Acontraststudy,whichwasperformedintheDepartmentofAnatomy,ChinaMedicalUniversity,andtheDepartmentofAnatomy,ShenyangMedicalCollegebetweenDecember2005andMay2007.MATERIALS:Thirty-five,healthy,female,SpragueDawleyratswereselectedforthisstudy.Ginsenoside(81%purity)wasprovidedbyJilinJi’anWantaiChineseMedicineFactory;anti-BDNFantibody,anti-TrkBantibody,andtheirkitswereprovidedbyWuhanBosterCompany.METHODS:Atotalof35ratsweredividedintothreegroups:young(fourmonthsold),aging(26monthsold),andginsenoside.Ratsintheginsenosidegroupwereadministeredginsenoside(25mg/kg/d)between17monthsand26months.MAINOUTCOMEMEASURES:ImmunohistochemistryandinsituhybridizationwereusedtomeasureexpressionofBDNFandTrkBinthemedialseptumofagedrats,andthedetectedresultswereexpressedasgrayvalues.RESULTS:①Qualitativedetection:usingmicroscopy,degenerativeneuronswerevisibleinthemedialseptumintheaginggroup.However,neuronalmorphologyintheginsenosidegroupwassimilartoneuronsintheyounggroup.②Quantitativedetection:themeangrayvalueofBDNF-positiveandTrkB-positiveproductsintheaginggroupweresignificantlyhigherthanintheyounggroup(t=3.346,4.169,P<0.01);however,themeangrayvalueintheginsenosidegroupwassignificantlylowerthanintheaginggroup(t=2.432,2.651,P<0.01).CONCLUSION:GinsenosidecanincreaseexpressionofBDNFandTrkBinth

  • 标签: 人参皂甙 隔片 激酶 神经营养因子
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  • 简介:Objective:Tostudytheeffectofactivecompound6FandAfromPterissemipinnataL.(PsL)ontheactivitiesofDNAtopoisomerase(TOPO)IandII,activitiesofcytosolicandmembraneTPK,andexpressionofoncogenec-mycinlungadenocarcinomacells.Methods:Theeffectofcompound6FandAonactivitiesofcytosolicandmembraneTPKwasmeasuredbyscintillationcounting;theeffectofcompoundAonexpressionofoncogenec-mycwasdeterminedbyflowcytometryindirectfluorimetry.Results:compound6FandAcouldinhibittheactivitiesofTOPOI,andtheystronglyinhibitedtheTOPOIIin0.01mg/Land10.0mg/Lrespectively.CompoundAslightlyinhibitedtheactivitiesofmembraneTPK,butnotthecytosolicone.CompoundAcouldinhibittheexpressionofoncogenec-myc.Conclusion:Topoisomerasesaretargetofcompound6FandA.CompoundAcouldslightlyinhibittheactivitiesofTPK,andshowedaninhibitoryeffectontheexpressionofoncogenec-myc.

  • 标签: Pteris semipinnata L. DNA topoisomerase 酷氨酸蛋白质 kinase C-MYC
  • 简介:Thetitlecompoundchlorpropham(CASnumber:101-21-3,C10H12ClNO2,Mr=213.66)waspreparedbytheadditionreactionof3-chlorophenylisocyanatewithisopropanol.Spectraldata,IR,NMRandMS,werereported.ThispaperprovidessomerelatedinformationaboutRegulatoryStatus,ToxicologicalEffects,EcologicalEffectsandEnvironmentalFatealso.

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  • 简介:Ameloblastomaisabenignbutlocallyaggressiveodontogenieneoplasmthataccountsfor10%ofalltumorsarisinginthemandibleandmaxilla(1).Eightypercentofameloblastomasariseinthemandible,andtheyareusuallyfoundinyoungadults.Itfrequentlyrecursifnotadequatelyresected.Therefore,thestandardtherapyforthistumoriscompleteboneresectionwithanadequatemarginofsafety:marginalorsegmentalosteotomy.However,aestheticdeformities,functionalimpairmentsandpsychologicalimpairmentsafterradicalsurgeryforlargeameloblastoma,havebeenseriousissues(1).

  • 标签: BRAF INHIBITOR AMELOBLASTOMA Eighty PERCENT
  • 简介:Apotentialdualinhibitor(4)forexogenousabsorptionandendogenicsynthesisofcholesterolwasdesignedbasedontheconjugationoftheβ-lactampharmacophoreofezetimibeandtheδ-lactonepharmacophoreofstatins.Themergerofezetimibeandstatin4wassynthesizedfromp-hydroxybenzaldehydethroughaten-steproute.1HNMRanalysisshowedexistenceoffourpairsofenantiomers(5.7:5.7:1:1,molarratio).Andcompound4wasfoundtolowertotalglucose(TG)levelinratserumviaahigh-cholesterolandhigh-fatfeedingexperiment.

  • 标签: 他汀类药物 抑制剂 合并 NMR分析 胆固醇 内源性
  • 简介:BOUNDEDNESSANDBLOWUPFORTHEGENERALACTIVATOR-INHIBITORMODELLiMINGDE(李名德);CHENSHAOHUA(陈绍华);QINYUCHUN(秦禹春)(DepartmentofMathematic...

  • 标签: Activator-inhibitor MODEL BOUNDEDNESS blow up HOLOMORPHIC
  • 简介:AbstractPsoriatic arthritis (PsA) is a type of chronic inflammatory arthritis which is associated with psoriasis. The early recognition and treatment for PsA are of critical importance. Janus kinase (JAK) inhibitors, as a kind of orally small molecules, have emerged as an encouraging class of drug in PsA treatment. This review provides a discussion of the role and current status of JAK inhibitors in the control of PsA. There are three JAK inhibitors approved for use in autoimmune diseases, for example, tofacitinib, baricitinib, and upadacitinib, and only tofacitinib has been approved in PsA treatment. The clinical trials of upadacitinib and filgotinib in PsA patients are undergoing. The efficacy and safety of these agents were briefly discussed. Although there are still issues in terms of their efficacy and safety currently, JAK inhibitors are expected to benefit more PsA patients in future.

  • 标签: Janus kinase Janus kinase inhibitors Psoriatic arthritis Drug treatment Tofacitinib
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  • 简介:TheethanecrackeratasteamcrackerofYangziPetrochemicalCompany(YPC)hasbeensafelyoperatingformorethan100dayssinceapplicationofdomesticN360cokeinhibitorstartingAugust28,2004tosetanewrecordontheoperatingcycleofethanecracker,whichhasrevealedgreatsuccessincommercialapplicationofthisinhibitor.

  • 标签: 扬子江石化公司 乙烯 抑制剂 裂解炉 涂层