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10 个结果
  • 简介:Natureisarichsourceofmedicinalplantsandtheirproductsthatareusefulfortreatmentofvariousdiseasesanddisorders.Momordicacharantia,commonlyknownasbittermelonorbittergourd,isoneofsuchplantsknownforitsbiologicalactivitiesusedintraditionalsystemofmedicines.Thisplantiscultivatedinallovertheworld,includingtropicalareasofAsia,Amazon,eastAfrica,andtheCaribbeanandusedasavegetableaswellasfolkmedicine.Allpartsoftheplant,includingthefruit,arecommonlyconsumedandcookedwithdifferentvegetables,stir-fried,stuffedorusedinsmallquantitiesinsoupsorbeanstogiveaslightlybitterflavorandtaste.Theplantisreportedtopossessanti-oxidant,anti-inflammatory,anti-cancer,anti-diabetic,anti-bacterial,anti-obesity,andimmunomodulatoryactivities.Theplantextractinhibitscancercellgrowthbyinducingapoptosis,cellcyclearrest,autophagyandinhibitingcancerstemcells.Theplantisrichinbioactivechemicalconstituentslikecucurbitanetypetriterpenoids,triterpeneglycosides,phenolicacids,flavonoids,essentialoils,saponins,fattyacids,andproteins.Someoftheisolatedcompounds(KuguacinJ,KaravilosideXI,KuguaglycosideC,MomordicosideQ-U,Charantin,α-eleostearicacid)andproteins(α-Momorcharin,RNaseMC2,MAP30)possesspotentbiologicalactivity.Inthepresentreview,wearesummarizingtheanti-oxidant,anti-inflammatory,andanti-canceractivitiesofMomordicacharantiaalongwithashortaccountofimportantchemicalconstituents,providingabasisforestablishingdetailbiologicalactivitiesoftheplantanddevelopingnoveldrugmoleculesbasedontheactivechemicalconstituents.

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  • 简介:Cancerisgenerallyregardedastheresultofabnormalgrowthofcells.AccordingtoWorldHealthOrganization,canceristheleadingcauseofmortalityworldwide.Mothernatureprovidesalargesourceofbioactivecompoundswithexcellenttherapeuticefficacy.Numerousphytochemicalsfromnaturehavebeeninvestigatedforanticancerproperties.Inthisreviewarticle,wediscussseveralnaturalcompounds,whichhaveshownanti-canceractivity.Naturalcompoundsinducecellcyclearrest,activateintrinsicandextrinsicapoptosispathways,generateReactiveOxygenSpecies(ROS),anddown-regulateactivatedsignalingpathways,resultingininhibitionofcellproliferation,progressionandmetastasisofcancer.Severalpreclinicalstudieshavesuggestedthatnaturalcompoundscanalsoincreasethesensitivityofresistantcancerstoavailablechemotherapyagents.Furthermore,combiningFDAapprovedanti-cancerdrugswithnaturalcompoundsresultsinimprovedefficacy.Onthebasisoftheseexcitingoutcomesofnaturalcompoundsagainstseveralcancertypes,severalagentshavealreadyadvancedtoclinicaltrials.Inconclusion,preclinicalresultsandclinicaloutcomesagainstcancersuggestpromisinganticancerefficacyofagentsfromnaturalsources.

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  • 简介:目的这研究被设计评估tanshinone的反癌症行动我和tanshinoneIIA,和正常、癌的冒号房间上的tanshinoneIIA的六衍生物。结构活动关系(SAR)分析被进行描出为改进反癌症的tanshinones的结构的修正的意义行动。方法Tanshinone衍生物根据文学被设计并且综合。结肠癌房间上的不同混合物的cytotoxicity被MTT试金决定。tanshinones的Apoptotic活动被流动cytometry(FCM)测量。结果Tanshinone我和tanshinoneIIA两个都在结肠癌房间上展出了重要cytotoxicity。他们在p53+/+结肠癌房间线是更有效的。这也被注意我是的tanshinone的反癌症活动更多的有势力并且选择。tanshinoneIIA(N1和N2)的二衍生物也在结肠癌房间上展出了cytotoxicity。结论tanshinone的反冒号癌症活动我是更多的有势力并且比tanshinoneIIA选择,并且p53依赖者。tanshinoneIIA的结构的修正获得的衍生物在正常和结肠癌房间上展出了更低的cytotoxicity。从位、电子的特征观点,戒指A和呋喃或dihydrofuran的结构的修正在tanshinones影响的基本结构上包围D,这被结束这项活动。A和B戒指的delocalization的增加能提高如此的混合物的cytotoxicity,当一个非平面、小的大小的D戒指区域将提供改进反癌症活动时。

  • 标签: 药理学 性质 药物 药品
  • 简介:预防和治疗,而是他们的低水的溶解度,差的稳定性,相反的bioavailability,和低目标特性使在治疗学的剂量管理他们不现实的在癌症的许多phytochemicals表演诺言。这是特别地真的为(−)-epigallocatechingallate,curcumin,橡黄素,resveratrol,和genistein。对为这些自然产品开发新奇交货策略有增加的兴趣。Liposomes,微粒,nanoemulsions,稳固的类脂化合物nanoparticles,nanostructured类脂化合物搬运人并且poly(lactide-co-glycolide)nanoparticles是biocompatible和可被细菌破坏的nanoparticles。那些nanoparticles能增加phytochemicals的稳定性和溶解度,展出一个持续版本性质,提高他们的吸收和bioavailability,保护他们免受早熟的酶的降级或新陈代谢的伤害,延长他们的发行量时间,经由被动或指向的交货改进他们的目标特性到癌症房间或肿瘤,通过阻止他们过早地与生物环境交往降低毒性或副作用到正常房间或纸巾,并且提高纳米技术为为癌症的预防和治疗开发装载phytochemical的nanoparticles打开一扇门。

  • 标签: 药学 药剂学 调剂学 剂型
  • 简介:MicroRNAs(miRNAs)areasetofnon-codingsmallRNAmoleculesthatplayacriticalroleinregulationofproteincodinggenesincells.MiRNAshavebeenextensivelystudiedasnovelbiomarkers,therapeutictargets,andnewdrugsinvarioushumandiseases.Breastcancerisaoneoftheleadingtumortypessignificantlyaffectingwomenhealthworldwide.Overthepastdecade,anumberofnaturalagents,suchaspaclitaxelandcurcumin,havebeenappliedfortreatmentandpreventionofbreastcancerduetotheirrelativelylowtoxicity.However,themechanismsofactionhavenotbeencompletelyunderstood.InvestigationonmiRNAsisabletopotentiallyprovideanovelinsightintobetterunderstandingtheanticanceractivitiesofthesenaturalproducts.GiventhatasinglemiRNAcantargetmultiplegenes,theoretically,thosegenesinvolvedinacertainphenotypecanbeclusteredwithoneorafewmiRNAs.Therefore,pleiotropicactivitiesofnaturalagentsshouldbeinterpretedbyinteractionsbetweenselectedmiRNAsandtheirtargets.Inthisreview,wesummarizethelatestpublicationsrelatedtothealterationsofmiRNAsbytwonaturalagents(paclitaxelandcurcumin)thatarecurrentlyusedininterventionofbreastcancer,andconcludethatthemechanisminvolvingtheregulationofmiRNAexpressionisoneofthekeystounderstandpleiotropicactivitiesofnaturalagents.

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  • 简介:Cisplatinandotherplatinum-baseddrugsareusedfrequentlyfortreatmentoflungcancer.However,theirclinicalperformanceareusuallylimitedbydrugresistanceortoxiceffects.Carnosicacid,apolyphenolicditerpeneisolatedfromRosemary(Rosemarinusofficinalis),hasbeenreportedtohaveseveralpharmacologicalandbiologicalactivities.Inthepresentstudy,thecombinationeffectofcisplatinpluscarnosicacidonmouseLLC(Lewislungcancer)xenograftsandpossibleunderlyingmechanismofactionwereexamined.LLC-bearingmiceweretreatedwithintraperitonealinjectionwithcisplatin,oralgavagewithcarnosicacid,orcombinationwithcisplatinandcarnosicacid,respectively.Combinationofcarnosicacidandcisplatinyieldedsignificantlybetteranti-growthandpro-apoptoticeffectsonLLCxenograftsthandrugsalone.MechanisticstudyshowedthatcarnosicacidtreatmentboostedthefunctionofCD8~+TcellsasevidencedbyhigherIFN-γsecretionandhigherexpressionofFasL,perforinaswellasgranzymeB.Inthemeantime,theproportionofMDSC(myeloid-derivedsuppressorcells)intumortissueswerereducedbycarnosicacidtreatmentandthemRNAlevelsofiNOS2,Arg-1,andMMP9,whicharethefunctionalmarkersforMDSC,werereduced.Inconclusion,ourstudyprovedthatthefunctionalsuppressionofMDSCbycarnosicacidpromotedthelethalityofCD8~+Tcells,whichcontributedtotheenhancementofanti-lungcancereffectofcisplatin.

  • 标签: LUNG cancer Carnosic acid CISPLATIN MDSC
  • 简介:EuphorbiakansuiisacommonlyusedtraditionalChinesemedicineforthetreatmentofedema,pleuraleffusion,andasthma,etc.Accordingtothepreviousresearches,terpenoidsinE.kansuipossessvariousbiologicalactivities,e.g.,anti-virus,anti-allergy,antitumoreffects.Inthiswork,twentyfiveterpenoidswereisolatedfromE.kansui,includingthirteeningenane-andeightjatrophane-typediterpenoids(withtwonewcompounds,kansuininPandQ)andfourtriterpenoids.EighteenofthemwereanalyzedbyMTSassayforinvitroanticanceractivityinfivehumancancercelllines.Structure-activityrelationshipfor12ingenane-typediterpenoidsincolorectalcancerColo205cellswerepreliminarystudied.Significantanti-proliferationactivitieswereobservedinhumanmelanomacellsbreastcancerMDA-MB-435cellsandColo205cells.Morethanhalfoftheisolatedingenane-typediterpenoidsshowedinhibitoryactivitiesinMDA-MB-435cells.Eightingenane-andonejatrophane-typediterpenoidspossessedmuchlowerIC_(50)valuesinMDA-MB-435cellsthanpositivecontrolstaurosporine.Preliminarystructure-activityrelationshipanalysisshowedthatsubstituentonposition20wasimportantfortheactivityofingenane-typediterpenoidsinColo205cellsandsubstituentonposition3contributedmoresignificantbiologicalactivityofthecompoundsthanthatonposition5inbothMDA-MB-435andColo205cells.

  • 标签: TERPENOIDS ANTI-PROLIFERATION ACTIVITY Human cancer cells
  • 简介:Resistancetocisplatin(DDP)-basedchemotherapyisamajorcauseoftreatmentfailureinhumangastriccancer(GC).Itisnecessarytoidentifythedrugstore-sensitizeGCcellstoDDP.Inourpreviousresearch,ZuoJinWanFormula(ZJW)hasbeenprovedcouldincreasethemitochondrialapoptosisviacofilin-1inaimmortalizedcellline,SGC-7901/DDP.Duetotheimmortalizedcellsmaystilldifficulthighlyrecapitulatetheimportantmoleculareventsinvivo,primaryGCcellsmodelderivedfromclinicalpatientwasconstructedinthepresentstudytofurtherevaluatetheeffectofZJWandtheunderlyingmolecularmechanism.ImmunofluorescentstainingwasusedtoindentifyprimaryculturedhumanGCcells.Westernblottingwascarriedouttodetecttheproteinexpression.CellCountingKit-8(CCK-8)wasusedtoevaluatecellproliferation.Flowcytometryanalysiswasperformedtoassesscellapoptosis.ZJWinhibitedproliferationandinducedapoptosisinprimaryDDP-resistantGCcells.Notably,theapoptosisinGCcellswasmediatedbyinducingcofilin-1mitochondrialtranslocation,down-regulatingBcl-2andup-regulatingBaxexpression.Surprisingly,thelevelofp-AKTproteinwashigherinDDP-resistantGCcellsthanthatoftheDDP-sensitiveGCcells,andtheactivationofAKTcouldattenuateZJW-inducedsensitivitytoDDP.ThesedatarevealedthatZJWcanincreasethechemosensitivityinDDP-resistantprimaryGCcellsbyinducingmitochondrialapoptosisandAKTinactivation.ThecombiningchemotherapywithZJWmaybeaneffectivetherapeuticstrategyforGCchemoresistancepatients.

  • 标签: PRIMARY GC cells ZJW AKT CHEMORESISTANCE
  • 简介:Chemokine12(CXCL12),也作为stromal知道房间导出factor-1(SDF-1)和CXCchemokine亚科的一个成员,无所不在地在许多纸巾和房间类型被表示。它为transmembraneG联合蛋白质的受体CXCR4和CXCR7与ligand明确地交往。CXCL12/CXCR4轴参加一系列生理、生物化学、病理学的过程,例如发炎和白血球trafficking,导致癌症的骨头疼痛,和postsurgical伤害,并且也是在在肿瘤房间和他们的微型环境之间的cross-talking的一个关键因素。CXCR4的异常overexpression为肿瘤幸存,增长,angiogenesis,homing和转移是批评的。在这评论,我们在癌症,在临床的学习下面的CXCR4禁止者,和自然产品CXCR4对手总结了CXCL12/CXCR4的角色。在结论,发信号的CXCL12/CXCR4为肿瘤开发是重要的并且指向小径可能代表一条有效途径到在癌症治疗开发新奇治疗。

  • 标签: CXCL12/CXCR4 肿瘤 指向的治疗 PLERIXAFOR