简介:
简介:Cytarabine(1-β-D-arabinofuranosylcytosine,Ara-C),isolatedfromaCaribbeanspongespeciesTethyacrypta,isthefirstantitumordrugfromamarineresource.In1980,theUSFoodandDrugAdministrationapprovedthisdrugforthetreatmentofdifferenttypesofleukemia.Thisdrughasashortplasmahalf-life,lowstability,limitedbioavailability,andseveresideeffects.Toimprovestabilityandbioavailability,wesynthesizedninenovelderivativesbyblockingthecytarabinemetabolicsitesandimprovinglipophilicity.ThecLogPvaluesofthenewlysynthesizedcompoundswerecalculated.Allthesynthesizedcompoundsweremorelipophilicthancytarabine,resultinginmembranepermeabilityandbioavailabilityimprovement.TheantitumoractivitiesagainstleukemiacelllineHL-60wereevaluatedbyusingtheMTTassay.ThebioassayresultsrevealedthattheIC50valuesofcompounds5,8and9were0.080,0.090and0.057μmolL-1,respectively,whichwassimilarwiththatofcytarabine(0.056μmolL-1).Incomparison,compound4withaphosphategroupatO5’wasinactive.Becausephosphoesterbondsareeasilyhydrolyzedbyalkalinephosphataseandarecommonlyusedinproducingprodrugstrategies,compound4mightalsobemetabolizedinvivoandgeneratecompound3orevencytarabinethroughamulti-stepreaction.Thus,compound4mightbeapromisingcompoundtobedevelopedasaprodrug.
简介:
简介:Amapoftheaverageatomicnumberoflunarrockandsoilcanbeusedtodifferentiatelithologyandsoiltypeonthelunarsurface.Thispaperestablishesalinearrelationshipbetweentheaverageatomicnumberoflunarrockorsoilandthefluxofpositionannihilationradiation(0.512-MeVgamma-ray)fromthelunarsurface.TherelationshipisconfirmedbyMonteCarlosimulationwithdatafromlunarrockorsoilsamplescollectedbyLuna(Russia)andApollo(USA)missions.AmapoftheaverageatomicnumberofthelunarrockandsoilonthelunarsurfacehasbeenderivedfromtheGamma-RaySpectrometerdatacollectedbyChang’e-1,anunmannedChineselunar-orbitingspacecraft.Inthemap,thehigheraverageatomicnumbers(ZA>12.5),whicharerelatedtodifferenttypesofbasalt,areinthemariaregion;thehighestZA(13.2)readingsareassociatedwithSinusAestuum.ThemiddleZA(~12.1)regions,intheshapeofirregularovalrings,areinWestOceanusProcellarumandMareFrigoris,whichseemstobeconsistentwiththedistributionofpotassium,rareearthelements,andphosphorusasauniquefeatureonthelunarsurface.Theloweraverageatomicnumbers(ZA<11.5)arefoundtobecorrelatedwiththeanorthositeonthefarsideoftheMoon.
简介:TheeffectsofBacillussubtilis2-1fromtheintestineofhealthyseacucumberonthegrowth,digestiveenzymeactivitiesandintestinalmicrobiotaofjuvenileseacucumber(Apostichopusjaponicus)weredeterminedinthepresentstudy.SeacucumberwasfedwithSargassumthunbergiipowdersupplementedwithB.subtilis2-1atdifferentconcentrationsvaryingamong0(control),105,107,and109CFUg-1for8weeks.ResultsshowedthatthegrowthperformanceandintestinalamylaseandtrypsinactivitiesweresignificantlyincreasedbydietaryB.subtilis2-1at109CFUg?1(P<0.05).However,dietaryB.subtilis2-1hadnosignificantinfluenceonthelipaseactivityinseacucumber(P>0.05).Thepolymerasechainreactiondenaturinggradientgelelectrophoresisand16SrRNAgenesequencinganalysisindicatedthatdietaryB.subtilis2-1at105and107CFUg-1inhibitedmostoftheProteobacteriaincludingthoseingenusVibrio.DietaryB.subtilis2-1at109CFUg-1notonlydecreasedtheabundanceandspeciesofgenusVibrio,butalsoincreasedtheintensityofgeneraPsychrobacterandBacillus.AspecificdosageofdietaryB.subtilis2-1couldincreasethegrowthandmodulatetheintestinalmicrobiotaofseacucumber;thusitmightbeanovelprobioticforkeepingthehealthofseacucumber.
简介:AbstractTheGartnerkofelboreholeisoneofthemostthoroughlystudiedanddescribedPermo-Triassicsectionsintheworld.Detailedbulkorganiccarbonisotopestudiesshowanegativebaseshiftfrom-24%0to-28%0intheLatestPermianwhichlattervaluepersistsintotheEarliestTriassicafterwhichitdecreasesslightlyto-26‰.Twostronglynegativepeaksof〉-38‰intheLatestPermianandalesserpeakof-31‰intheEarlyTriassicaretoonegativetobeduetoagreaterproportionofmorenegativeorganicmatterandmustbeduetoverynegativemethaneeffects.TheoverallchangetomorenegativevaluesacrosstheBulla/Teseroboundaryfitstherelativeriseinsealevelforthistransitionbasedonthefacieschanges.ApositiveshiftinorganiccarbonisotopevaluesattheLatePermianEventHorizonmaybeduetoanincreaseinland-derivedorganicdetritusatthislevel-afeatureshownbyallTethyanPermo-Triassicboundarysectionsthoughtheseothersectionsdonothavethesamevalues.Carbonatecarbonisotopetrendsaresimilarinallsectionsdroppingby2-3unitsacrossthePermo-Triassicboundary.Gart-nerkofelcarbonateoxygenvaluesaresurprisingly,con-sideringtheubiquitousdolomitization,compatiblewithvalueselsewhereandindicatereasonabletropicaltemper-aturesof60~CintheLatestPermiansabkhasto20-40℃intheoverlyingmarinetransitionbeds.Increasedland-derivedinputattheLatePermianEventHorizonmaybeduetooffshoretransportbytsunamiswhosedepositshavebeenrecognizedinIndiaatthislevel.
简介:为预测和评价贵州普安泥堡金矿床的成矿潜力,采用原生晕地球化学方法对10460勘探线所控制的Ⅲ-1号矿体进行原生晕轴向分带特征研究。采集了该勘探线上6个钻孔矿体附近的构造蚀变岩石样品进行ICP-AES分析。通过对各元素进行相关性分析及因子分析,选取原生晕地球化学特征研究的指示元素为Au、As、Ag、Cu、Hg、Mo、Co、Cd、Sb。综合原生晕分带图及指示元素分带序列分析,判断Ⅲ-1矿体原生晕出现了明显的分带异常,其由浅部到深部总体表现为:前缘晕元素+尾晕元素—近矿晕—前缘晕元素+近矿晕元素+尾晕元素的元素异常分布序列,指示在深部存在一个或多个隐伏矿体,是造成元素异常叠加共存与轴向分带序列异常的原因。
简介:凌源-宁城盆地是松辽盆地外围南部众多具良好油气勘探前景的小盆地之一,为研究其中的油气资源情况,在牛营子地区部署和实施了油气地质调查井——牛D1井。该钻井揭示侏罗系海房沟组可能为研究区重要的烃源岩发育层系之一。系统采集了海房沟组岩心,对其进行了岩石热解、镜质体反射率、气相色谱-质谱等分析及有机地球化学研究。结果表明,海房沟组浅部多为好-很好烃源岩,而深部多为差烃源岩和非烃源岩,有机质类型均主要为Ⅱ_2和Ⅲ型;浅部烃源岩的三环萜烷、升藿烷和甾烷系列丰度较高,规则甾烷呈不对称"V字型";而深部烃源岩的三环萜烷、升藿烷和甾烷系列丰度较低,规则甾烷多呈"反L型"。综合认为海房沟组浅部具有相对较强的生烃潜力,但牛D1井海房沟组烃源岩的成熟度较低,建议今后加强对海房沟组烃源岩展布和成熟度平面分布特征的研究。