摘要
目的研究桦褐孔菌乙酸乙酯部位化学成分,初步筛选出具有抗肿瘤活性的单体化合物。方法用制备型高效液相、大孔树脂HPD100、Sephadex LH-20凝胶、小孔树脂MCI、硅胶等柱层析方法对桦褐孔菌乙酸乙酯部位进行分离纯化,综合应用光谱法(1HNMR、13CNMR、HRMS)鉴定结构。体外培养人胃癌SGC-7901、肝癌HepG2及神经胶质瘤U-87细胞,不同浓度(12. 5、25、50、100、200μmol/L)单体化合物刺激后,MTT法观察各单体化合物对肿瘤细胞增殖的影响。结果从乙酸乙酯部位分离鉴定12个成分(酚类、羊毛脂烷型三萜和甾醇),分别为:原儿茶醛(1)、4-(3,4-二羟苯基)-3-丁烯-2-酮(2)、大黄酚(3)、Coelarthenol(4)、1,2-Benzenedicarboxylic acid dibuty ester(5)、栓菌酸(6)、柠檬酸三乙酯(7)、(22E,24R)-麦角甾-7,22-二烯-3β,5α,6β-三醇(8)、Aquilarin A(9)、1,4-benzenedicarboxylic acid 1-butyl-4-(2-methylpropyl) ester(10)、3β-羟基-(22E,24R)-麦角甾-7,22-二烯(11)、(24S)-Ergost-7-en-3-ol (12)。结论化合物2、6、8具有较强的抗肿瘤作用,其中化合物2、9首次从桦褐孔菌中分离得到。
Objective To study the chemical constituents of the ethyl acetate extracts from Inonotus obliquus and preliminarily screen out the monomeric compounds with antitumor activity.Methods The constituents of the ethyl acetate extracts from Inonotus obliquus were isolated bypreparative high performance liquid chromatography(pHPLC),following by macroporous resin HPD100,Sephadex LH-20,MCI and silica gel column chromatography.The structures were identified by NMR.The SGC-7901 cells,HepG2 cells and U-87 cells were cultured and stimulated with the compounds with the concentrations ranging from 12.5 to 200μmol/L.The cell proliferation ability was detected using MTT method.Results Twelve compounds were identified as protocatechualdehyde(1),4-(3,4-dihydroxyphenyl)-3-butene-2-one(2),chrysophanol(3),coelarthenol(4),1,2-benzenedicarboxylic acid dibutyl ester(5),trametenolic acid B(6),triethyl citrate(7),(22E,24R)-ergosta-7,22-diene-3β,5α,6β-triol(8),aquilarin A(9),1,4-benzenedicarboxylic acid 1-butyl-4-(2-methylpropyl)ester(10),(22E,24R)-ergosta-7,22-dien-3β-ol(11),(24S)-ergost-7-en-3-ol(12).Conclusion Twelve compounds were obtained and indentified,among which compound 2 and compound 9 are firstly isolated from Inonotus obliquus.Compound 2,6 and 8 exhibits potent antitumor activities in vitro.
作者
吴泽华
程文明
张致勇
缪忆如
李春如
Wu Zehua;Cheng Wenming;Zhang Zhiyong(Anhui Provincial Key Laboratory on Bioactivity of Natural Product,School of Pharmacy, Anhui Medical University,Hefei 230022;State Key Laboratory of Natural Medicines,China Pharmaceutical University,Nanjing 210009;Zhejiang BIOASIA Institute of Life Science,Jiaxing 314200)
出处
《安徽医科大学学报》
CAS
北大核心
2018年第11期1757-1761,共5页
Acta Universitatis Medicinalis Anhui
基金
安徽省自然科学基金(编号:090413105)
天然药物活性组分与药效国家重点实验室(中国药科大学)资助项目(编号:SKLNMKF201416)
关键词
桦褐孔菌
乙酸乙酯部位
抗肿瘤
酚类
羊毛脂烷型三萜
甾醇
Inonotus obliquus
ethyl acetate extracts
antitumor
phenols
lanostane triterpenoids
steroids
