香榧叶的化学成分及生物活性研究  

Studies on chemical constituents and bioactivities of leaves of Torreya grandis

作　　者：段芳芳[1] 贾晓会[1] 贾姗姗[1] 徐润生[1,2] 袁珂[1,2] 童品璋 DUAN Fang-fang;JIA Xiao-hui;JIA Shan-shan;XU Run-sheng;YUAN Ke;TONG Pin-zhang(Zhejiang Agriculture and Forestry University,Lin＇an 311300,China;Zhuji Academy of Innovation and Development,Zhejiang Agricul~re and Forestry University,Zhuji 311800,China;The Forestry Bureau of Zhuji,Zhuji 311800,China)

机构地区：[1]浙江农林大学,浙江临安311300 [2]浙江农林大学诸暨创新发展研究院,浙江诸暨311800 [3]诸暨市林业局,浙江诸暨311800

出　　处：《中草药》2018年第20期4791-4797,共7页Chinese Traditional and Herbal Drugs

基　　金：浙江省自然科学基金资助项目(LY13H280011)

摘　　要：目的对香榧Torreya grandis叶进行化学成分和生物活性研究。方法采用MCI-Gel CHP-20、Diaion HP-20、Toyopearl HW-40、Sephadex LH-20、RP18及硅胶等柱色谱法对香榧叶中的化学成分进行分离纯化,根据理化性质和波谱技术(1H-NMR、13C-NMR、HR-ESI-MS)鉴定化合物的结构,采用海虾致死生物活性法和MTT法测定部分化合物的细胞毒活性和抗肿瘤活性。结果从香榧叶醋酸乙酯部位和正丁醇部位共分离鉴定了10个化合物,分别为香榧酯(1)、花柏酚(2)、4-epiagathadial(3)、3,4-二羟基苯甲酸3-O-β-D-葡萄糖苷(4)、脱氢松香酸(5)、反式璎珞柏酸(6)、顺式璎珞柏酸(7)、2-甲氧基-1,4-苯二甲醇(8)、松脂素(9)、β-谷甾醇(10)。其中化合物1～4具有一定的细胞毒活性,对海虾的半数致死浓度(LC50)值分别为7.7、8.0、8.8、4.2μg/m L;化合物4在10μg/m L时对人肝癌细胞Huh7和Hep G2的抑制率最显著,分别为67%和69%。结论以上化合物除化合物10外均为首次从该植物中分离得到。生物活性测定结果表明,化合物1～4具有一定的细胞毒活性;化合物4具有较强的Huh7和Hep G2细胞抑制活性。Objective To study the chemical constituents and bioactivities of leaves of Torreya grandis.Methods The chemical constituents were isolated by MCI-Gel CHP-20,Diaion HP-20,Toyopearl HW-40,Sephadex LH-20,RP-18 and silica gel column chromatographic methods.Their structures were identified on the basis of physicochemical and spectroscopic analysis.The cytotoxic activity and antitumor activity of compounds 1—4 were investigated by lethal-to-prawn larva bioactivity determining method and MTT assay.Results Ten compounds were isolated from Et OAc extract and n-Bu OH of leaves of T.grandis.Their structures were identified as torreyagrandate（1）,hinokiol（2）,4-epiagathadial（3）,3,4-dihydroxybenzoic acid 3-O-β-D-glucoside（4）,dehydroabietic acid（5）,trans-communic acid（6）,cis-communic acid（7）,（2-methoxy-1,4-phenylene） dimethanol（8）,pinoresinol（9）,and β-sitosterol（10）.The bioactivity experiment indicated that compounds 1—4 possessed certain cytotoxic activity towards brine shrimp,and LC50 value were 7.7,8.0,8.8,and 4.2 μg/m L,respectively.In addition,it was found that compound 4 presented remarkable inhibitory effect on two kinds of cells of human liver cancer cells of Huh7（67%） and Hep G2（69%） at a dose of 10 μg/m L.Conclusion All compounds are isolated from leaves of T.grandis for the first time expect compound 10.Compounds 1—4 exhibite certain cytotoxic activity,and compound 4 displays stronger antitumor activity towards Huh7 and Hep G2 liver cancer cells.

关 键 词：香榧 细胞毒活性 香榧酯 花柏酚 3 4-二羟基苯甲酸3-O-β-D-葡萄糖苷 

分 类 号：R284.1[医药卫生—中药学]