三株海洋来源真菌次级代谢产物及其活性的分析-analysis of secondary metabolites and their activities of three marine fungi.docx

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2018-07-30 发布于上海
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三株海洋来源真菌次级代谢产物及其活性的分析-analysis of secondary metabolites and their activities of three marine fungi.docx

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三株海洋来源真菌次级代谢产物及其活性的分析-analysis of secondary metabolites and their activities of three marine fungi

StructuresofthecompoundsStudiesonSecondaryMetabolitesofthreeMarine-derivedFungusandtheirbioactivitiesAbstractDuetotheuniquelivingconditions,marine-derivedfungipossessuniqueandrichvarietyofbiosyntheticpathwayinthelong-termofthenaturalselection,thusthesecondarymetabolitesofthemhavethenoveltyoftheskeletonsanddiversityofbiologicalactivity,andhavebeendiscoveredasanimportantsourceforleadcompounds.61fungalstrainswereisolatedfrom13spongesamplesfromtheSouthChinaSea.Byantitumorbioassayscreening,17activestrainswerechosen.CombinedwithTLCandHPLC,chemicalanalyseswereperformedfortheactivesecondarycompoundsofthese17strains,and2fungiofMXH-99（Metarhiziumanisopliae）andKXL-157（Apiosporamontaqnei）wereselectedforfurtherstudy.What’smore,thesecondarymetabolitesofthefungusGWQ-143（Penicilliumsolitum）isolatedbypreviousworkwerealsostudied.Ninenewcompounds,includingtwonaphtho-γ-pyronesglycosides、twolactones、twobenzamides、twomeroterpenoidsandonehexaketide,aswellastwonewnaturalproducts(benzamides),togetherwith17knownoneswereisolatedfromtheEtOACextractsofthefermentationsfromthreetargetstrains,MXH-99、GWQ-143andKXL-157,chromatographedbyrepeatedTLC,silicagelcolumn,SephadexLH-20andsemi-preparativeHPLC.Theirstructureswereestablishedonthebasisofchemicalandspectroscopicevidence.Theabilitiesof1-8toinhibitthegrowthofM.phleiweremeasuredbythefilterpaperdiskdiffusionmethod,theknownisochaetochrominB2(6)andustilaginoidinD(7)exhibitedthehighestactivitywithMICs50μg/mL;theantitumoractivitiesagainstseveralcancercelllinesofthesecompoundswereassayedwiththeresultsthatonlycompound23-25showedweekcytotoxicity.Theinhibitionratesofcompound24(ataconcentrationof50μM)againstP388andA549celllineswere73.8%and51.9%,respectively;andcompound23and25showedmoderateinhibitionratesof43.8%and36.6%againstP388celllineataconcentrationof25μM,respectively.Insummary,28compoundsincluding9newcompoundsand2newnaturalproductswereisolatefromthefermentationsofthreemarine-derivedfungi.Twoofthem(compounds6-7)exhibitedthehighestactivitywithMICs50μg/mL,t