简介:Naturalproducts(NPs)arecompoundsthatarederivedfromnaturalsourcessuchasplants,animals,andmicroisms.Therapeuticshasbenefitedfromnumerousdrugclassesderivedfromnaturalproductsources.TheBiopharmaceuticsDrugpositionClassificationSystem(BDDCS)wasproposedtoserveasabasisforpredictingtheimportanceoftransportersandenzymesindeterminingdrugbioavailabilityanddisposition.Itcategorizesdrugsintooneoffourbiopharmaceuticalclassesaccordingtotheirwatersolubilityandextentofmetabolism.Thepresentpaperreviews109drugsfromnaturalproductsources:29%belongtoclass1(highsolubility,extensivemetabolism),22%toclass2(lowsolubility,extensivemetabolism),40%toclass3(highsolubility,poormetabolism),and9%toclass4(lowsolubility,poormetabolism).HereinweevaluatedthecharacteristicsofNPsintermsofBDDCSclassforall109drugsaswellsasforsubsetsofNPsdrugsderivedfromplantsourcesasantibiotics.Inthe109NPsdrugs,wepiled32drugsfromplants,50%(16)oftotalinclass1,22%(7)inclass2and28%(9)inclass3,nonefoundinclass4;Meantime,theantibioticswerefound5(16%)inclass2,22(71%)inclass3,and4(13%)inclass4;nodrugwasfoundinclass1.Basedonthisclassification,weanticipateBDDCStoserveasausefuladjunctinevaluatingthepotentialcharacteristicsofnewnaturalproducts.
简介:目的:观察针药并用治疗非特异性急性腰扭伤的临床疗效。方法:将69例患者按就诊川页序随机分为针药并用组、针刺组和药物组。针刺组24例,采用针刺治疗,每日1次,共治疗5次;药物组20例,采用口服双氯芬酸钠治疗,50mg每次,每日2次,连服5日;针药并用纽25例采用与针刺组、药物组相同的针刺和药物治疗。以疼痛量表和下腰痛量表评价临床疗效。结果:三组患者治疗后在疼痛,活动度方面均有一定改善,但针药并用组疗效最佳,与针刺组、药物组比较,差异有统计学意义(P〈0.01);针刺组与药物组比较,差异无统计学意义。结论:针药并用治疗急性腰扭伤疗效优于单纯针刺治疗或常规剂量双氯芬酸钠治疗。
简介:Glioblastoma(GBM)isoneofthemostlethalhumancancers.GenomicanalysesdefinethemoleculararchitectureofGBMandhighlightacentralfunctionformechanistictargetofrapamycin(mTOR)signaling.mTORkinaseexistsintwomultiproteincomplexes,namely,mTORC1andmTORC2.Thesecomplexesdifferintermsoffunction,regulationandrapamycinsensitivity.mTORC1iswellestablishedasacancerdrugtarget,whereasthefunctionsofmTORC2incancer,includingGBM,remainspoorlyunderstood.ThisstudyreviewstherecentfindingsthatdemonstrateacentralfunctionofmTORC2inregulatingtumorgrowth,metabolicreprogramming,andtargetedtherapyresistanceinGBM,whichmakesmTORC2asacriticalGBMdrugtarget.
简介:Thepaperdescribesdrugreleaseevaluationofabiodegradablelong-actingcon-traceptiveCapsule(CaproF)containinglevonorgestrel(LNG)invivo.Poly(E-Capro-lactone)(PCL)biodegradablematerial,suitableformanymedicalapplication,wasusedinthisstudy.Itwasextrudedintotubes.ThetubeswerethencutandloadedwithLNGpowderbeforemelting-sealedonbothendstogetdrugcapsules.Thissub-dernalimplanthasbeenfoundtobehighlyeffectiveinanimalexperiments.Twoad-
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简介:Wepresentherethedevelopmentofcholesterol(Chol)-modifieddendrimersystemfortargetedchemotherapyoffolate(FA)receptor-expressingcancercells.Inourstudy,poly(amidoamine)(PAMAM)dendrimersofgeneration5(G5)werefunctionalizedstepby-stepwithChol,fluoresceinisothiocyanate(FI),andFAviaapoly(ethyleneglycol)(PEG)spacer(PEG-FA),andthenacetamidetoshieldtheirremainingsurfaceamines.ThesynthesizedG5.NHAc-Chol-FI-PEG-FA(forshort,G5-CFPF)dendrimerswereutilizedtoencapsulate10-hydroxycamptothecin(HCP),ahydrophobicanticancerdrug.WefindthateachG5-CFPFdendrimercanencapsulate13.8HCPmolecules.ThecomplexesshowaslowerreleaseprofilesofHCPinapH-dependentmannerthanthecontrolcomplexesformedusingthesamedendrimerswithoutCholunderthesameconditions.ThankstothetargetingroleplayedbyFA,thecomplexesdisplayaspecificinhibitionefficacytoFAreceptor-expressingcervicalcancercells.ThedesignedChol-modifieddendrimersmaybeadoptedasapromisingcarrierforapplicationintargetedcancertherapy.
简介:Thepresentworkshowsdrug-carrierinteractions,releasebehaviorsandcellresponsesofhydroxyapatite(HA)containingsalvianolicacidB(SalB),astragaluspolysaccharide(APS),andnaringin.X-raydiffraction(XRD)showedthatthecrystallinityandcrystalsizeofHAdecreasedsignificantlywhenSalBwasadded(p<0.05).Transmissionelectronmicroscope(TEM)confirmedthatthenano-acicularcrystalsofHAcontainingSalBwerethemostfineamongallspecimens.ItwasconjecturedthatSalBpreferentiallyadsorbedonthepositivelychargedsurfaceofHAcrystalstoinhibittheirgrowth.InvitroreleaseofHAcontainingChinesemedicinesfollowedthefirst-orderequation.Thedrug-carrieraffinitybetweenHAandSalBmighthaveprolongedthereleaseofSalB.TheproliferationanddifferentiationofosteoblastswerepromotedbyChinesemedicinescontainingHAinthetimeanddosagedependentmanner.Theosteoblastsdisplayedapolygonalmorphologywithcell-celljunctionsinallcases.ItissuggestedthatthecontainedChinesemedicineswouldpromotetheactivitiesoftheosteoblasts.
简介:Weinvestigatedthepharmacokineticsofcaroverineintheperilymph,cerebrospinalfluidandplasmaaftersystemicandlocaladministrationsinguineapigsbyusinghigh-performanceliquidchromatography.Auditorybrainstemresponsesweremeasuredtoevaluateauditoryfunctionaleffect.Theresultsshowedthatlocalapplicationwasabothsafeandefficientmethod.Wefurtherreviewedliteratureandpinpointedthattheroundwindowiseffectivelylocaldrugdeliverymeansforfutureinnereartreatment.
简介:Bothenantiomersofdenopamineweresynthesizedusingmicrobial-chemicalapproachviabioreductionof1-(acetoxyphenyl)ketone4(R=CH2C1)and5(R=CO2Et)withfungusGeotrichumsp.G38.
简介:Inthefightagainstcancer,controlleddrugdeliverysystemshaveemergedtoenhancethetherapeuticefficacyandsafetyofanti-cancerdrugs.Amongthesesystems,mesoporoussilicananoparticles(MSNs)withafunctionalsurfacepossessobviousadvantagesandwerethusrapidlydevelopedforcancertreatment.Manystimuli-responsivematerials,suchasnanoparticles,polymers,andinorganicmaterials,havebeenappliedascapsandgatekeeperstocontroldrugreleasefromMSNs.ThisreviewpresentsanoverviewoftherecentprogressintheproductionofpH-responsiveMSNsbasedonthepHgradientbetweennormaltissuesandthetumormicroenvironment.Fourmaincategoriesofgatekeeperscanrespondtoacidicconditions.Thesecategorieswillbedescribedindetail.
简介:背景:训练的整个身体颤动(WBV)出现到豆子为在更老的个人训练的常规抵抗的有效选择。到目前为止,没有数据在心和肺的健康上关于振动效果存在。目的:这随机的ised控制了估计的试用在超过60岁的社区住所成年人在心和肺的健康和肌肉力量上训练的1年的WBV的效果。方法:220个成年人的一个总数(意味着年龄67.1年)随机被分到一个WBV组,健康组或控制组。在一个颤动平台上行使的TheWBV组,和健康组表演了心血管,抵抗,平衡和拉长的锻练。控制组没参予任何训练。心率在一个单个WBV会议期间被测量。山峰氧举起(VO2peak)和time-to-peak锻练(TPE)在进步自行车ergometry期间被测量。肌肉力量被一个测力计估计。结果:心率在WBV训练期间显著地增加了。在1年以后,VO2peak,TPE和肌肉力量在WBV和健康组显著地增加了。两个都训练的组在VO2peak和肌肉力量同样改善了。健康组比WBV组在TPE更显著地改善了。结论:WBV在社区住所训练老看起来有效改进心和肺的健康和肌肉力量。
简介:OpticalmethodsandMTTmethodareusedtocharacterizetheantiproliferationeffectofantitumordrug9-aminoacridine(9AA)withandwithoutsilvernanoparticles.IntracellularsurfaceenhancedRamanscattering(SERS)spectraandfluorescentspectraof9AAindicatetheformof9AAadsorbedonthesurfaceofsilvernanoparticles.AlthoughbothsilvernanoparticlesandantitumordrugcaninhibitthegrowthofHelacells,silvernanoparticlescanslowdowntheantiproliferationeffectonHelacellsatlowconcentrationofantitumordrugs.Ourexperimentalresultssuggestthatsilvernanoparticlesmayserveasslow-releasedrugcarriers,whichisimportantinantitumordrugdelivery.
简介:Objective:Toinvestigatetheeffectoftwoantisenseoligonucleotidesoncellsurviving,bcl-2expressionandapoptosisofleukemiacells.Methods:Theexperimentalassayswereperformedwithcellculture,immunochemistryandflowcytometry.Results:Thetwoantisenseoligodeoxynucleotides,combinedwithVp16orAra-corDNR,wereabletodeclinethesurvivalrateofmyeleukemiccells,downregulatebcl-2geneexpressionandinduceapoptosisofleukemiccellssignificantly,ascomparedwithVp16orAra-corDNRalone.Conclusion:Itispossibleforthetwonewbcl-2antisensestobedevelopedintoclinicaltrialsforleukemiaandtumorwithbcl-2geneoverexpression.
简介:Objective-TocomparetheconsistencyoftheresultsfromdetectingHIV-1antibodyinthepairedurineandserumspecimensfromdrugusersbyELISA.Methods:Thepairedurineandserumspecimensfrom273drugusersdetainedatadetoxificationunitwerecollected,andtheHIV-1antibodiesinthespecimensofthemwerescreenedbyurineandserumELISAkits,respectively.Results:Of273serumspecimens,94onesshowedpositivereactionandamong94counterparturinespecimens,93onesalsoappearedpositivereaction.Takingtheresultstogether,theconsistentrateofHIV-1antibodyscreenedbyurineandserumELISAkitswas99.6%.Conclusion:TheurineELISAkit,whichscreenedHIV-1antibodyofurineshowingalmostthesameresultstestedbyserumELISAkit,isreliable.ItisproposedthaturineELISAbeintroducedinmanyfields.
简介:Objective:TostudythedifferencesandsimilaritiesoftheantisensedrugswithdifferentstructuresonthebiologicalfunctionsofK562cells.Methods:Cytotoxiceffectsweremeasuredbyuseofacellviabilityassay.FlowcytometricanalysisandagarosegelelectrophoresisofDNAfragmentationwerealsoperformed.Theexpressionlevelofproteinwasassayedbyimmunofluorescenceusingfluoresceisothiocyanatelabel.Results:PNAtargetingthecodingregionoftheBcl-2messengerRNAcouldeffectivelyinhibitK562cellviability,down-regulatethesynthesisoftheBcl-2proteinandincreasecellapoptosis.By72haftertheBcl-2antisensePNAtreatment,K562cellsshowedmorereductioninthelevelofBcl-2proteincomparedwithcellstreatedwiththeantisenseODN.Aftertreatmentwith10μmol/LofBcl-2antisensePNAorantisenseODNfor72h,apoptoticratesofK562cellswere13.15±1.13and11.72±1.12,respectively.Furthermore,therewassignificantdifferenceinthepercentageofapoptoticcellsbetweenantisensePNAgroupandantisenseODNgroup.Conclusion:TheresultssuggestthatantisensePNAtargetingthecodingregionofBcl-2mRNAhasbetterantisenseeffectsthantheantisenseoligonucleotidesoninducingapoptosisofK562cells.
简介:AbstractObjectives:Polycystic ovary syndrome (PCOS) is a common endocrine disease in women of childbearing age. Although it is a leading cause of menstrual disorders, infertility, obesity, and other diseases, its molecular mechanism remains unclear. This study aimed to analyze the target genes, pathways, and potential drugs for PCOS through text mining.Methods:First, three different keywords ( "polycystic ovary syndrome", "obesity/adiposis", and "anovulation" ) were uploaded to GenCLiP3 to obtain three different gene sets. We then chose the common genes among these gene sets. Second, we performed gene ontology and signal pathway enrichment analyses of these common genes, followed by protein-protein interaction (PPI) network analysis. Third, the most significant gene module clustered in the protein-protein network was selected to identify potential drugs for PCOS via gene-drug analysis.Results:A total of 4291 genes related to three different keywords were obtained through text mining, 72 common genes were filtered among the three gene sets, and 69 genes participated in PPI network construction, of which 23 genes were clustered in the gene modules. Finally, six of the 23 genes were targeted by 30 existing drugs.Conclusions:The discovery of the six genes (CYP19A1, ESR1, IGF1R, PGR, PTGS2, and VEGFA) and 30 targeted drugs, which are associated with ovarian steroidogenesis (P <0.001), may be used in potential therapeutic strategies for PCOS.