简介：Inviewoftheanti-HIVactivitiesofdelavirdineandresveratrol,anovelanti-AIDsdrugResdelasu,1-{3-[(1-methyl-ethyl)amino]-2-pyridinyl}-4-{[5-(4-{5[(1E)-2-(hydroxyphenyl)ethenyl]-1,3-benzenedioyl-carbonylbu-tanoyl}amino)-1H-indol-2-yl]carbonyl}-piperazinewassynthesizedbylinkingthedelavirdinederivativeandresveratrolwithsuccinicanhydrideastheconjugatedcompoundviatwodifferentroutes.Itsstructurewasconfirmedbymeansof1HNMR,13CNMR,IR,MS,andelementalanalysis.TherouteofesterificationfollowedbyamidationforsynthesizingResdelasuwassimplerandgaveahigheryield(46%)thanthatofamidationfollowedbyesterification.ItwasprovedthatthemethodwasefficientandconvenienttoprepareResdelasu.TheresultsofHIV-1ReverseTranscriptaseAssayandquantitativetitrationofHIV-1viaMAGIassayshowedthatanovelanti-AIDsdrug,Resdelasu,hadbeensynthesized.

简介：Theactivesiteof3CLproteinase(3CL^por)forcoronaviruswasidentifiedbycomparingthecrystalstructuresofhumanandporcinecoronavirus.Theinhibitorofthemainproteinofrhinovirus(Ag7088)couldbindwith3CL^proofhumancoronavirus,thenitwasselectedasthereferenceformoleculardockinganddatabasescreening.Theligandsfromtwodatabaseswereusedtosearchpotentialleadstructureswithmoleculardocking.SeveralstructuresfromnaturalproductsandACD-SCdatabaseswerefoundtohavelowerbindingfreeenergywith3CL^prothanthatofAg7088.ThesestructureshavesimilarhydrophobicitytoAg7088.Theyhavecomplementaryelectrostaticpotentialandhydrogenbondaeceptoranddonorwith3CL^pro,showingthatthestrategyofanti-SARSdrugdesignbasedonmoleculardockinganddatabasescreeningisfeasible.

简介：Adetectionofanthracyclineantitumordrugdaunomycin(DNR)reactingwithDNAinsimulatemetabolisminvitrohasbeenmade.ItwasfoundthatDNRcouldreactwithDNAtoformDNR-DNAadducts.TheadductcompositionsofDNRwithfishspermDNAandthermallydenaturatedDNAweredetermined.TheequilibriumassociationconstantKofDNRwithfishspermDNAis1.98×10^5L/molandthatofDNRwithdenaturatedDNAis2.29×10^4L/mol.Semiquinonefreeradicals,metabolicproductsofDNR,candestroybothfishspermDNAanditsthermallydenaturatedDNA.ItisverifiedbyhyperchromiceffectincreaseobservedinUVspectrumandAFMexperiments.ThemechanismofDNAdegradationhasalsobeeninvestigated.Resultsobtainedallowonetoexplainthereasonofsideeffectofanthracyclinedrugandgivethewaytodepress,whichwereofclinicalsignificance.

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简介：多保护是在安全管理的一个原则，并且反爆炸的使用和耐火的代理人是它的关键部分。在这份报纸，反爆炸的领域里的nano氧化物粒子的性质并且耐火被分析。纳米粒子的沉积速度是计算的。CH4作为一个例子被拿，并且它起始的阶段的燃烧机制被结束。反应系统的分子的精力上的15氧化物的效果与程序Hyperchem6被计算，并且在激进分子和氧化物之间的可能的接触方式被得到。氧化物例如ZrO2，能与激进分子结合，这被结束，并且因此阻止燃烧反应。nano-ZrO2暴发地产生了喷雾器，这被发现比在用作反爆炸和耐火的代理人的另外的对应物优异，因此，将在安全管理起一个日益重要的作用。

简介：EachofKeggintypeheteropolytungstosilicicandheteropolytungstogermanicacidsreactedwith8-quinolinol,p-aminodimethylanilineandpyridine,respectively,yieldingsixchargetransferheteropolycomplexes(CTHPCs),whichwerepurifiedandcharacterizedbyelementalanalysis,IR,UVand183WNMR.Theanti-HIV-1activitiesofCTHPCswereevaluatedbyELISAofHIV-P24antigen.ThetoxicityagainstMT-4cellswasmeasuredbyMTT.Theresultsshowthatmedianinhibitoryconcentration(IC50)foreachCTHPCtoinhibitHIV-P24antigenincellculturewaslowerthan5μg/mL,whilemediantoxicityconcentration(IC50)againstMT-4cellswashigherthan268μg/mL.Thefollowingmechanismsmightbeconsideredfortheiranti-HIV1activity,namely,(1)inhibitingthepenetrationofHIV-1virusintotargetcellsforitcanblockadeCD4receptorofMT-4cellsand(2)inhibitionofsyncytiumformation.

简介：电气化学的实验被执行测试铝锌的腐蚀率热剧降的涂层。5.3%铝锌合金(重量比率)有优异耐蚀性质，这被显示出。坚定的微观结构显示了由纳米组成的非结晶的结构系统的大小的粒子。分析显示了5.3%铝锌系统的吉布斯精力的大否定变化。分子的动力学模拟证明5.3%铝锌系统从另外的系统有很不同的行为。这个特别系统的阶段转变从模拟被观察。转变温度在400K附近被决定。模拟显示5.3%铝锌系统在从300～900K的温度范围上是非结晶的，支持从铝锌合金的非结晶的固体有的实验的推理特殊耐蚀特性。

简介：Bothenantiomersofdenopamineweresynthesizedusingmicrobial-chemicalapproachviabioreductionof1-(acetoxyphenyl)ketone4(R=CH2C1)and5(R=CO2Et)withfungusGeotrichumsp.G38.

简介：CardiactroponinI(cTnI)wasseparatedandpurifiedfromhumanleftventriculartissuebyaffinitychromatographicmethodandusedtoimmunizeBalb/cmicebyintraperitonealinjectionandfourhybridomacelllines,whichsecretedmonoclonalantibody(mAb)againsthumancTnI,wereobtainedbycellfusion,identificationandcloningtwice.ThreemAbs(9F5,2F11,8C12)wereproducedfromtheascitesofBalb/cmiceinjectedintraperitoneallythehybridomacellsandcharacterizedbymeansofasurfaceplasmonresonance(SPR)biosensor.AnoptimalandspecificsensingmembranefortroponinIwaspreparedwithstaphylococcalproteinA(SPA)astheintermediatelayerandmAbagainsthumancTnIasthecaptureantibody.Onthebasisofthesensingmembrane,twomodesofoperationoftheSPRbiosensorweredeveloped,i.e.,adirectdetectionofantigen-antibodyaffinityandasandwichassay.Inthesandwichassaydetectionmode,themAbscompetitionwasmeasuredbymonitoringwhetherthesecondaryantibodyhadbeenattachedtothecTnIalreadycapturedbythefirstantibodyonthesensorsurface.TheSPRbiosensorwasshowntobeabletodirectlydetecttheantigen-antibodyaffinityandtheorderoftheaffinitywasfoundtobe9F5＞2F11＞8C12.Inthesandwichdetectionmode,itwasfoundthatthedifferentepitopesonthecTnImoleculeswererecognizedbythethreemAbsrespectively,buttheasymmetricalcompetitionwasshownbetween2F11and8C12andnocompetitionwasfoundbetween9F5and2F11or8c12.Basedontheseresults,adoublemonoclonalsandwichimmunoassayforcTnIwasdevelopedbyusingtheoptimalantibodypairof9F5and2F11andtheSPRbiosensorwithSPAsubstratemembrane,whichshowedanexcellentsensitivityof0.8μg/LforboththebufferandtheserumsamplescomparedwiththedirectdetectionofcTnIforthebufferwiththelowestdetectionlimitof4μg/LandconventionalELISAwiththesensitivityof1.9μg/L.

简介：Aseriesofnewflavanonederivativesoffarrerolwasdesignedandsynthesizedasapotentinhibitorofvascularsmoothmusclecells(VSMCs)vegetationaccordingtoaconvenientmethod.Thestructuresofallthesynthesizedcompoundswereconfirmedby1HNMR,13CNMRandEIHR-MS.ThebiologicalactivitiesofthesecompoundsagainstVSMCsinvitrowereevaluated.Theassayresultsindicatethattwocompounds,5,7-dihydroxy-6,8-dimethyl-2-(2-nitrophenyl)chroman-4-one(7f)and2,3-dibromo-4,5-dihydroxydiphenylmethanone(7j)exhibitedhighactivityagainstVSMCsinvitrowithIC50valuesof9.9and6.7μmol/L,respectively,andthepreliminarystructure-activityrelationship(SAR)wasdescribed.

简介：Anewcerebroside,1-O-(β-D-glucopyranosyloxy)-(2S,3R,4E,8Z)-2-[(2′R)-2’-hydroxylignoceranoylamino]-4,8-tetradecene-3-diolwasisolatedfromthe60%EtOHextractoftraditionalChinesemedicalplantCyperusrotundusL.Itsstructurewasdeterminedonthebasisofspectroscopicdata.Thisnewcompoundshowedanti-proliferationeffectonvascularsmoothmusclecells(VSMCs).

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简介：Anovelaciddyeacidwassynthesizedbythecondensationreactionbetweenbromamineacidand2-amino-6-nitrobenzothiazoleanditsanti-UVprotectionpropertieswereevaluated.Theresultsshowedthatsilkdyedwiththisdyehadverygoodultravioletradiationprotectioncapabilityandexcellentdyeingperformance.TheUV-absorptionmechanismofthisdyewasalsodiscussed.

简介：ＳＹＮＴＨＥＳＩＳＡＮＤＡＮＴＩ－ＨＵＭＡＮＩＭＭＵＮＯＤＥＦＩＣＩＥＮＣＹＶＩＲＵＳ－１（ＨＩＶ－１）ＡＣＴＩＶＩＴＹＯＦ９－（２－ＰＨＯＳＰＨＯＮＹＬＭＥＴＨＯＸＹＥＴＨＹＬ）ＡＤＥＮＩＮＥ（１）ＡＮＤＩＴＳＲＥＧＩＯＩＳＯＭＥＲ３－（２－ＰＨＯ...