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云南植物研究~ 2007,29(4):486488 ActaBotanicaYunnanica 黑蕊虎耳草中岩白菜素没食子酸酯类及其对 丙型肝炎丝氨酸蛋白酶的抑制作用 左国营1,2,李正全1,陈丽蓉1,何红平3,徐筱杰1 (1北京大学化学与分子工程学院,养生堂天然药物实验室,北京100871;2昆明总医院,云南昆明650032; 3中国科学院昆明植物研究所西部植物化学与植物资源国家重点实验室,云南昆明650204) 摘要:研究了黑蕊虎耳草(Saxifragamelanocentra)中岩白菜素衍生物的化学和生物活性,从其地上部分分 离纯化得到一个新的岩白菜素没食子酸酯,主要通过1维和2维核磁共振波谱鉴定结构为11-氧-(4-氧甲基 没食子酰)岩白菜素[11-O-(4-O-methylgalloyl)bergenin(1)],该化合物对丙型肝炎丝氨酸蛋白酶(HCV NS3serineprotease)具有抑制活性,其IC50为0.32mgmL。 IC 关键词:抗丙型肝炎;黑蕊虎耳草;11-氧-(4-氧甲基没食子酰)岩白菜素;50 中图分类号:Q946文献标识码:A文章编号:0253-2700(2007)04-486-03 GallicAcidEstersofBergeninfromSaxifragamelanocentra (Saxifragaceae)andTheirInhibitionAgainst HCVNS3Protease 1,21131** ZUOGuo-Ying,LIZheng-Quan,ChenLi-Rong,HEHong-Ping,XUXiao-Jie (1CollegeofChemistryandMolecularEngineering,YangshengtangNatureMedicineLaboratory,PekingUniversity, Beijing100871,China;2KunmingGeneralHospital,Kunming650032,China;3TheStateKeyLaboratory ofPhytochemistryandPlantResourcesinWestChina,KunmingInstituteofBotany, ChineseAcademyofSciences,Kunming650204,China) Abstract:TostudythechemicalandbioactivecharacteristicsofbergeninderivativeswhichwerepurifiedfromSaxifraga melanocentraFranch.,anewgallicacidesterofbergenin,11-O-(4-O-methylgalloyl)bergenin(1)wasisolatedfromthe aerialpartsofSaxifragamelanocentraFranch.,anditsstructurewasestablishedmainlyonthebasisof1Dand2DNMR spectroscopicanalysis.ItshowedweakinhibitoryactivityagainstHCVNS3serineproteasewithIC50of0.32mgml. Keywords:HCVNS3serineprotease;Saxifragamelanocentra;11-O-(4-O-methylgalloyl)-bergenin;IC50 Bergenin(Chinesenamedyan-baicai-su),afa-1996).Inthecourseofourscreeningnaturalproducts mousantitussiveagentwhichhasbeenusedclinicallyasHepatisCvirus(HCV)inhibitors,westudiedthe formanyyears,isamajorconstituentfromthegenusofactiveconstituentsofSaxifragamelanocentraFranch BergeniaandSaxifraga(Saxifragaceae)andtheotherpreviously(Zuoetal.2005a).Furtherinvestigation plantspecies.Itshowedavarietyofbiologicalactivi-ofitsactiveconstitutionledustoisolateanewberge- ties,includingantioxidant,h