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1、硬士學(xué)垃論文摘要虎杖(PolygonumCuspidatunSieb.etZUCC)為蓼科(Polygonceae)蓼屬(Polgohum)多年生灌木狀草本植物虎杖(P0190numcuspidatum)的根及根莖。篩選抗癌中藥時(shí)發(fā)現(xiàn)中藥虎杖在體外顯示抗腫瘤作用。通過查找文獻(xiàn)和初步抗癌實(shí)驗(yàn)表明其主要成分是蒽醌類化合物。為了進(jìn)一步研究虎杖的抗癌活性成分和構(gòu)效關(guān)系,從中篩選結(jié)構(gòu)新穎且具有顯著抗癌活性的先導(dǎo)化合物,對虎杖進(jìn)行了系統(tǒng)的研究。本研究以乳腺癌(MCF一7)體外細(xì)胞毒活性為檢測手段,對虎杖進(jìn)行活性成分的追蹤分離和結(jié)構(gòu)鑒定。應(yīng)用正相硅膠柱層析、反復(fù)柱層析分離
2、技術(shù),從虎杖中分離得到7個(gè)化合物,應(yīng)用現(xiàn)代波譜技術(shù)(IR,EIMS,1H-NIIW,,”C-NMR,DEPT,COSY,HSQc)和多種化學(xué)方法鑒定了7個(gè)化合物的結(jié)構(gòu):①大黃素甲醚(physcion)、②大黃素(emodin)、③黃葵內(nèi)酯(Ambrettolide)、④B.谷甾醇(B.sitoster01)、⑤齊墩果酸(oleanolicacid)、⑥香豆素(coumarin)、⑦、2一乙氧基一8一乙?;?,4一萘醌(2一ethoxy一8一acetyl一1,4naphthoquinone)。體外細(xì)胞毒性篩選實(shí)驗(yàn)表明,虎杖的乙醚提取物和從中分離得到的化合物①
3、、②、③、⑦均對乳腺癌細(xì)胞MCF一7具有細(xì)胞毒活性。本論文首次對虎杖的乙醚提取物進(jìn)行了系統(tǒng)的抗癌活性評價(jià),為今后進(jìn)一步研究虎杖資源提供參考數(shù)據(jù)。本課題不僅豐富了對虎杖化學(xué)成分及其抗癌活性的了解,而且為進(jìn)一步研究開發(fā)新的抗癌活性藥物提供了科學(xué)依據(jù)。關(guān)鍵詞:虎杖;化學(xué)成分;抗癌;細(xì)胞毒性碩士學(xué)位論文虎杖抗癌活蛙成分匏研§0摘要ABSTRACTPolygonumCuspidatumSieb.etZuccbelongstothegenusofPolygonceae,familyofPolgohum.PolygonumCuspidatumSieb.etZuccwere
4、foundtOshowsignificantbioactivitiesinvitroagainsthumantumorcelllines.Theexperimentagainsthumantumorandconsultingliteratureindicatethatt11eiIbasisarethecompoundsofanthraquinone.Inordertostudymanyconstituentsconcerningwithanticancerandstructureactivityanddiscovernaturalproductswithne
5、wstructuresandbioactiveactivities,wehaveinvestigatedthePolygonumCuspidatumSieb.etZuec.a(chǎn)MCF-7bioassay-guidedfractionationledtotheisolationoftheactiveconstituents.Sevencompoundshavebeenisolatedfromtheethan61icextractofPolygonumCuspidatumSieb.etZuccbyrepeatedlychromatographyonnormal.B
6、ydetailedanalysisofthespectraldata(IR,EIMS,1H-NMR,”C-NMR,DEPT,COSY)andchemicalmethods.Thecompoundswerecharacterizedelucidatedasfollowing:physcion、emodin、Ambrettolide,13一sitosterol、Oleanolicacid,coumarin,2-ethoxy一8一acetyl一1,4naphthoquinone。Someofthemwerefoundtoshowsignificantbioacti
7、vitiesinvitroagainsthumantumorcelllines.Suchas,thequantitiesofdistillinginaetherandcompounds①、②、③、⑦againstthehumantumorcellsMCF一7.Weevaluatedtheactivityofthecompoundsofanthraquinonesystematicallyforthefirsttime;TheresultscanbethereferencedataforthefurtherresearchinganticancerofPoly
8、gonumCuspidatumSieb.etZucc