欢迎来到人人文库网! | 帮助中心 人人文库renrendoc.com美如初恋!
人人文库网
首页 人人文库网 > 资源分类 > PDF文档下载

外文翻译-- Relationships between Inhibition Constants, Types of.PDF

  • 资源大小:244.44KB        全文页数:4页
  • 资源格式: PDF        下载权限:游客/注册会员/VIP会员    下载费用:1
游客快捷下载 游客一键下载
会员登录下载
下载资源需要1

邮箱/手机号:
您支付成功后,系统会自动为您创建此邮箱/手机号的账号,密码跟您输入的邮箱/手机号一致,以方便您下次登录下载和查看订单。注:支付完成后需要自己下载文件,并不会自动发送文件哦!

支付方式: 微信支付    支付宝   
验证码:   换一换

友情提示
2、本站资源不支持迅雷下载,请使用浏览器直接下载(不支持QQ浏览器)
3、本站资源下载后的文档和图纸-无水印,预览文档经过压缩,下载后原文更清晰   

外文翻译-- Relationships between Inhibition Constants, Types of.PDF

RELATIONSHIPSBETWEENINHIBITIONCONSTANTS,TYPESOFINHIBITIONANDIC50CALCULATIONANDCOMPARISONONIC50OFTWOMODELTYROSINASEINHIBITORSHAIRONGMAO1,JIANGANGXIE1,QIMENGZHANG2,XINYUL3,SHUBAILI2,1DEPARTMENTOFCHEMISTRY,ZHENGZHOUTEACHERSCOLLEGE,ZHENGZHOU,CHINA2DEPARTMENTOFCHEMICALENGINEERINGTECHNOLOGY,CHANGZHOUINSTITUTEOFENGINEERINGTECHNOLOGY,CHANGZHOU,CHINA3INSTITUTEOFFINECHEMICALS,JIANGSUPOLYTECHNICUNIVERSITY,CHANGZHOU,CHINACORRESPONDINGAUTHOREMAILSBLIEMAILCZIENETABSTRACTCALCULATINGMETHODSFORINHIBITORCONCENTRATIONIC50LEADINGTO50ACTIVITYLOSTFORDIPHENOLASEACTIVITYOFANOVELPARABOLICCOMPETITIVEINHIBITORTHETRIFLUOROMETHYLCONTAINING1,2,3TRIAZOLE,TFTAANDANOVELMIXEDINHIBITORE41IMIDAZOYLMETHYLCINNAMICACIDOZAGRELWEREDERIVEDONTHEBASISOFKINETICSOFTYROSINASEINHIBITIONTHESEMETHODSWEREAPPLIEDTOCALCULATEIC50VALUESOFTHETWOTYROSINASEINHIBITINGCOMPOUNDSTHEEXPERIMENTALIC50VALUESOFTFTAANDOZAGRELWERE419ΜMAND345MM,RESPECTIVIELYMOREOVER,THECALCULATEDIC50VALUEOFTFTAANDOZAGRELWERE828ΜMAND315MM,RESPECTIVELYTHECALCULATIONRESULTOFOZAGRELISCLOSERTOEXPERIMENTALDATAKEYWORDSTYROSINASE;IC50;TRIFLUOROMETHYLCONTAINING1,2,3TRIAZOLETFTA;E41IMIDAZOYLMETHYLCINNAMICACIDOZAGRELIINTRODUCTIONTHEREGULATIONOFENZYMEACTIVITYISOFGREATINTERESTFORBIOCHEMICALRESEARCHPURPOSESANDFORANUMBEROFAPPLICATIONSINMEDICINE,PHYSIOLOGY,ANDPHARMACOLOGYINHIBITIONOFENZYMESFROMANYBIOLOGICALSOURCECANBEACHIEVEDBYSEVERALAGENTS,SUCHASSELFINACTIVATINGSUBSTRATESANDREVERSIBLEORIRREVERSIBLEINHIBITORSTYROSINASEEC114181ISACOPPERCONTAININGENZYMEWITHRESPONSIBILITIESFORSKIN,HAIR,MELANIZATIONANDENZYMATICBROWNINGINFRUITSANDVEGETABLES13ITCATALYZESTHEHYDROXYLATIONOFMONOPHENOLSMONOPHENOLASEACTIVITYANDTHEOXIDATIONOFODIPHENOLSTOOQUINONESDIPHENOLASEACTIVITY,BOTHDEPENDINGONMOLECULAROXYGEN4,5THEBROWNINGISRESPONSIBLEFORLOSSINNUTRITIONALQUALITY,ANDTHEREFOREBECOMESAMAJORPROBLEMINTHEFOODINDUSTRYTHEREFORE,THECONTROLOFTHETYROSINASEACTIVITYISOFIMPORTANCEINPREVENTINGTHESYNTHESISOFMELANININTHEBROWNINGOFMUSHROOMSANDOTHERVEGETABLESANDFRUITSMANYEFFORTSHAVEBEENPUTINTHESEARCHFORFEASIBLEANDEFFECTIVETYROSINASEINHIBITORS69INOURSEARCHFORTYROSINASENOVELINHIBITORS,TRIFLUOROMETHYLCONTAINING1,2,3TRIAZOLES10,ANDOZAGRELANALOGUES11,WEREFOUNDTOHAVEOBVIOUSINHIBITORYEFFECTSONTHEMONOPHENOLASEACTIVITYANDTHEDIPHENOLASEACTIVITYOFMUSHROOMTYROSINASETHEIC50INHIBITORCONCENTRATIONLEADINGTO50ACTIVITYLOSTISAMEASUREOFTHEEFFECTIVENESSOFACOMPOUNDININHIBITINGBIOLOGICALORBIOCHEMICALFUNCTIONOFTEN,THECOMPOUNDINQUESTIONISADRUGCANDIDATETHISQUANTITATIVEMEASUREINDICATESHOWMUCHOFAPARTICULARDRUGOROTHERINHIBITORSNEEDEDTOINHIBITAGIVENBIOLOGICALPROCESSBYHALFITISCOMMONLYUSEDASAMEASUREOFANTAGONISTDRUGPOTENCYINPHARMACOLOGICALRESEARCHHOWEVER,ITAPPEARSNOTTOHAVEBEENNOTICEDPREVIOUSLYTHATTHEREISAVERYSIMPLERELATIONSHIPBETWEENIC50WITHINHIBITIONCONSTANTSANDTYPESOFINHIBITIONTYPETHEREFORE,THEAIMOFTHEPRESENTWORKWASTODEVELOPAMETHODTOCALCULATEIC50OFTWONOVELTYROSINASEINHIBITORSIICALCULATIONANDCOMPARISONONIC50ACALCULATIONOFIC50FORTHEPARABOLICCOMPETITIVEINHIBITORTHETRIFLUOROMETHYLCONTAINING1,2,3TRIAZOLESEXHIBITANTIMICROBIAL,ANTIVIRALANDANTITUMORACTIVITIESANDHAVEARANGEOFIMPORTANTAPPLICATIONSINPHARMACEUTICALANDAGROCHEMICALINDUSTRIES12NNNF3COHFIG1STRUCTUREOFTHETRIFLUOROMETHYLCONTAINING1,2,3TRIAZOLETFTAWEFOUNDANOVELTRIFLUOROMETHYLCONTAINING1,2,3TRIAZOLETFTA,SEESTRUCTUREINFIG1CANINHIBITMUSHROOMTYROSINASEACTIVITYIC50419ΜMWITHITSINCREASINGCONCENTRATIONSTHEINHIBITIONKINETICS,ANALYZEDBYLINEWEAVERBURKPLOTS,INDICATEDTFTATOBEAPARABOLICCOMPETITIVEINHIBITOROFDIPHENOLASEWHENLDOPAWASUSEDASSUBSTRATEITISSUGGESTEDTHATTWOTFTAMOLECULESCANCOMBINEWITHFREETYROSINASETOFORMADEADENDCOMPLEXATENZYMEACTIVESITETHEINHIBITIONCONSTANTSKI1FORINHIBITORENZYMECOMPLEXANDKI2FORINHIBITORENZYMEINHIBITOR9781424447138/10/25002010IEEECOMPLEXWEREESTIMATEDTOBE929MMAND136MM,RESPECTIVELYTHEMECHANISMREPRESENTINGPARABOLICCOMPETITIVEINHIBITIONFORTHETYROSINASECATALYZEDREACTIONISASFOLLOWSESESEPK1K2K1K3K3K4IIEIK4EI2IIE,S,I,PDENOTEENZYMEMUSHROOMTYROSINASE,SUBSTRATELDOPA,INHIBITORTFTA,ANDPRODUCTDOPACHROME,RESPECTIVELY;ES,EI,ANDEI2ARETHERESPECTIVECOMPOUNDSASITISUSUALLYTHECASETHATSETANDIETINTHESTEADYSTATE,THERATEOFFORMATIONANDDISAPPEARANCEOFTHECOMPLEXESAREIDENTICALESES211KKK−1133IEEIKK−12EIIEI244−KK13THEEXPRESSIONSFORTHETOTALENZYMECONCENTRATIONANDTHEREACTIONRATEEIEIESEE2T14ES2KV15INSERTIONOFTHEEXPRESSIONSFORE,EI,ANDEI2INTERMOFES,INTOTHEEXPRESSIONFORTHETOTALENZYMECONCENTRATIONGIVESESI1IS1SE4433121121T⎥⎦⎤⎢⎣⎡⋅−−−−KKKKKKKKKK16I1ISSE4433121121T2−−−−⋅KKKKKKKKKKKV17BECAUSEK1K2/K1ISTHEMICHAELISCONSTANTKMFORTHEREACTIONINTHEABSENCEOFINHIBITOR,K3/K3ISTHEEQUILIBRIUMCONSTANTKI1FORTHEDISSOCIATIONOFTHECOMPLEXEIINTOEANDI,ANDK4/K4ISTHEEQUILIBRIUMCONSTANTKI2FORTHEDISSOCIATIONOFTHECOMPLEXEI2INTOEIANDI,THERATEEQUATIONMAYBEWRITTENINTHEFORMII1SSI2I12I1MMAXKKKKVV18WHICHINRECIPROCALFORBECOMESMAXI2I12I1MAXM1II1S1VKKKVKV⋅19ITISEVIDENTFROMEQ19THATTHESLOPEOFLINEWEAVERBURKLINESISINFLUENCEDBYTHECHANGINGIANDI2ACCORDINGTOEQ18,INTHEABSENCEOFTFTZ,THEKINETICFUNCTIONISSSMMAX0KVV110THEINHIBITIONRATIO01100VIV−SSII1SS1MMAXI2I12I1MMAX−KVKKKKV111WHENIREACHES50,IIC50,SO,II1SS21I2I12I1MMKKKKK112THEIC50VALUETHENEGATIVEVALUESHOULDBEREMOVEDISMM2MMI1I1I1I250MI1I24SIC2KKKKKKKKKKK113ACCORDINGTOTHEEXPERIMENTCONDITIONSANDEQ113KM0117MM,KI1929MM,KI2136MM,ANDS10MM,SOTHECALCULATEDIC50VALUEOFISTOBE828ΜMTHEN,ACCORDINGTOFIG5,THEEXPERIMENTALIC50VALUEIS419ΜMINTHISINVESTIGATION,THECALCULATEDIC50VALUEISABOUTTWOTIMESTHATOFTHEEXPERIMENTALONEBCALCULATIONOFIC50FORTHEMIXEDINHIBITOROZAGRELE41IMIDAZOYLMETHYLCINNAMICACID,SEESTRUCTUREINFIG2,ASASELECTIVEINHIBITOROFTHROMBOXANESYNTHASETXASINHUMANPLATELETSESPECIALLY,ISUSEDINTHETREATMENTANDPREVENTIONOFVARIOUSTHROMBOTICDISEASES13WEFOUNDTHATOZAGRELINHIBITEDMUSHROOMTYROSINASEACTIVITYTHEIC50VALUEWAS345MMOZAGRELWASESTIMATEDTOBEAREVERSIBLEMIXEDTYPEINHIBITOROFDIPHENOLASEACTIVITYWHENLDOPAWASUSEDASSUBSTRATEWITHTHECONSTANTSKS1,KS2,KI1,ANDKI2DETERMINEDTOBE221,389,0454,0799MM,REPECTIVELYTHEINHIBITIONKINETICS,ANALYZEDBYLINEWEAVERBURKPLOTS,INDICATEDOZAGRELTOBEAMIXEDINHIBITOROFDIPHENOLASEWHENLDOPAWASUSEDASSUBSTRATEITDEMONSTRATEDTHATOZAGRELBOUNDTHEENZYMEATASITEDISTINCTEDFROMTHESUBSTRATEACTIVESITE,BUTITBOUNDTOEITHEREORESFIG2STRUCTUREOFE41IMIDAZOYLMETHYLCINNAMICACIDOZAGRELINTHISTYPEOFREVERSIBLEINHIBITION,OZAGRELCANINTERACTWITHBOTHTHEFREEENZYMETYROSINASEANDTHEENZYMESUBSTRATECOMPLEXATASITEOTHERTHANTHEACTIVESITEWITHACLASSICALMICHAELISMENTENREACTIONMECHANISMESESEPKCATEISIIESIKI1KS1KS2KI2HERE,E,S,I,PDENOTEENZYMEMUSHROOMTYROSINASE,SUBSTRATELDOPA,INHIBITOROZAGREL,ANDPRODUCTDOPACHROME,RESPECTIVELY;ES,EI,ANDESIARETHERESPECTIVECOMPOUNDSASITISUSUALLYTHECASETHATSE0ANDIE0ITISASSUMEDTHATTHEEFFECTISNOTONLYONAFFINITYBUTALSOONTHERATEOFTHEBREAKDOWNOFTHEESCOMPLEX;THUSOZAGRELWOULDINFLUENCETHEENZYMEACTIVITYINTWOWAYS,AFFECTINGVMASWELLASKMITISFORMALLYCONVENIENTTOREGARDKS1,KS2,KI1ANDKI2ASTHEDISSOCIATIONCONSTANTSOFTHERESPECTIVECOMPLEXESESINTOEANDS,ESIINTOEIANDS,EIINTOEANDI,ANDESIINTOESANDI,RESPECTIVELYINTHEMICHAELISMENTENSTATE,THESUBSTRATEBINDINGSTEPANDFORMATIONOFTHEESCOMPLEXAREFASTRELATIVETOTHEBREAKDOWNRATEASISTHEUSUALLYTHECASE,THEEQUILIBRIUMEQUATIONSOFTHEENZYME,SUBSTRATE,INHIBITOR,PRODUCT,ANDTHEIRRESPECTIVECOMPOUNDSES,EI,ESIAREGIVENS1ESESK21I1EIEIK22S2EISESIK23I2ESIESIK24ACCORDINGTOEQ21TOEQ24,THERELATIONSHIPWITHKS1,KS2,KI1ANDKI2ISGIVENS1I1S2I2KKKK25THEEXPRESSIONSFORTHETOTALENZYMECONCENTRATIONANDTHEREACTIONRATETEEESEIESI26THEOVERALLVELOCITYWILLBEGIVENASFOLLOWSCATESVK27INSERTIONOFTHEEXPRESSIONSFORE,EI,ANDESIINTERMOFES,INTOTHEEXPRESSIONFORTHETOTALENZYMECONCENTRATIONGIVESS1S1TI1I2IIE1ESSSKKKK28CATTS1I1I2ESII1S1KVKKK29THERATEEQUATIONMAYBEWRITTENINTHEFORMMAXS1I1I2SII1S1VVKKK210WHICHINRECIPROCALFORMBECOMESS1I1I2MAXMAXII1111SKKKVVV⋅211ITISEVIDENTFROMEQUATION11THATTHEMIXEDTYPEINHIBITIONAFFECTSBOTHKMANDVMAXITSSPECIALCASEISNONCOMPETITIVEINHIBITIONWHICHWOULDAFFECTTHEVMAXBUTNOTTHEKMSO,THESLOPEANDINTERCEPTOFEQUATION11AREGIVENASTHEFOLLOWINGFORMS1I1MAXI1SLOPEKKV212I2MAXI1INTERCEPTKV213FORTHESTEADYSTATEMODEL,SUBSTRATEBINDINGOCCURSFASTERTHANTHEBREAKDOWNOFTHEESCOMPLEX,SOTHEKINETICFUNCTIONINTHEABSENCEOFINHIBITORISMAX0S1SSVVK214THEINHIBITIONRATIO01100VIV−MAXS1I1I2MAXS1SII1S11SSVKKKVK−215WHENIREACHES50,IIC50,SO,S15050S1I1I2S11ICIC21S1KKKK−216THEIC50VALUEISS150S1I2I1SICSKKKK217ACCORDINGTOEQ217ANDKS1,KS2,KI1,ANDKI2,THECALCULATEDIC50IS315MM,ITISVERYCLOSETOTHEEXPERIMENTALDATAOFIC50345MMIIICONCLUSIONTHEIC50VALUESOFTWONOVELTYROSINASEINHIBITORSWERECALCULATEDANDCOMPAREDTHECALCULATEDIC50VALUEOFOZAGRELISCLOSERTHANITSEXPERIMENTALDATATHERESULTSSOFAROBTAINEDINDICATEDTHATTHEFURTHERASSAYISNEEDED,FROMNOTONLYONEASPECT,BUTFROMAWHOLEPERSPECTIVEREFERENCES1LYU,“INHIBITORYEFFECTSOFSANDR6HYDROXY2,5,7,8TETRAMETHYLCHROMAN2CARBOXYLICACIDONTYROSINASEACTIVITY,”JAGRFOODCHEMVOL51,PP23442347,20032YJKIM,JECHUNG,MKURISAWA,HUYAMA,ANDSKOBAYASHI,“NEWTYROSINASEINHIBITORS,CATECHINALDEHYDEPOLYCONDENSATES,”BIOMACROMOLECULESVOL5,PP474479,20043MJIMNEZ,SCHAZARRA,JESCRIBANO,JCABANES,ANDFGARCACARMONA,“COMPETITIVEINHIBITIONOFTYROSINASEBY4SUBSTITUTEDBENZALDEHYDES,”JAGRFOODCHEMVOL49,PP40604063,20014FGMOLINA,JLMUŇOZ,RVARN,JNRODRGUEZLPEZ,FGARCACNOVAS,ANDJTUDELA,“ANAPPROXIMATEANALYTICALSOLUTIONTOTHELAGPERIODOFMONOPHENOLASEACTIVITYOFTYROSINASE,”INTJBIOCHEMCELLBIOLVOL39,PP238252,20075LGFENOLL,MJPEŇALVER,JNRODRGUEZLPEZ,RVARN,FGARCACNOVAS,JTUDELA,“TYROSINASEKINETICSDISCRIMINATIONBETWEENTWOMODELSTOEXPLAINTHEOXIDATIONMECHANISMOFMONOPHENOLANDDIPHENOLSUBSTRATES,”INTJBIOCHEMCELLBIOLVOL36,PP235246,20046JCESPNANDHJWICHERS,“KINETICSOFACTIVATIONOFLATENTMUSHROOMAGARICUSBISPORUSTYROSINASEBYBENZYLALCOHOL,”JAGRFOODCHEMVOL47,PP35033508,19997IKUBO,IKINSTHORI,YKUBO,YYAMAGIWA,TKAMIKAWA,ANDHHARAGUCHI,“MOLECULARDESIGNOFANTIBROWNINGAGENTS,”JAGRFOODCHEMVOL48,PP13931399,20008LGFENOLL,PAGARCRUIZ,RVARN,ANDFGARCACNOVAS,“KINETICSSTUDYOFOXIDATIONOFQUERCETINBYMUSHROOMTYROSINASE,”JAGRFOODCHEMVOL51,PP77817787,20039JJXIE,KKSONG,LQIU,QHE,HHUANG,ANDQXCHEN,“INHIBITORYEFFECTSOFSUBSTRATEANALOGUESONENZYMEACTIVITYANDSUBSTRATESPECIFICITIESOFMUSHROOMTYROSINASE,”FOODCHEMVOL103,PP10751079,200710SBLI,HLNIE,YXUE,HTZHANG,CTZHANG,ANDLZHU,“KINETICSOFMUSHROOMTYROSINASEINHIBITIONBYANOVELTRIFLUOROMETHYLCONTAINING1,2,3TRIAZOLECOMPOUND,”

注意事项

本文(外文翻译-- Relationships between Inhibition Constants, Types of.PDF)为本站会员(tuzhidiguo)主动上传,人人文库网仅提供信息存储空间,仅对用户上传内容的表现方式做保护处理,对上载内容本身不做任何修改或编辑。 若此文所含内容侵犯了您的版权或隐私,请立即通知人人文库网(发送邮件至[email protected]或直接QQ联系客服),我们立即给予删除!

温馨提示:如果因为网速或其他原因下载失败请重新下载,重复下载不扣分。

关于我们 - 网站声明 - 网站地图 - 资源地图 - 友情链接 - 网站客服客服 - 联系我们

网站客服QQ:2846424093    人人文库上传用户QQ群:460291265   

[email protected] 2016-2018  renrendoc.com 网站版权所有   南天在线技术支持

经营许可证编号:苏ICP备12009002号-5