中国中药杂志

2010, v.35(03) 315-322

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小花异裂菊中的萜类成分及其活性
Terpenoids of Heteroplexis micocephala and their bioactivities

樊晓娜;林生;朱承根;胡金凤;刘洋;陈晓光;陈乃宏;王文杰;石建功;
FAN Xiaona,LIN Sheng,ZHU Chenggen,HU Jinfeng,LIU Yang,CHEN Xiaoguang,CHEN Naihong,WANG Wenjie,SHI Jiangong (Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College (Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine,Ministry of Education,Beijing 100050,China)

摘要(Abstract):

目的:研究异裂菊属Heteroplexis植物小花异裂菊的化学成分及其活性。方法:用乙醇提取后通过醋酸乙酯萃取、反复硅胶柱色谱、PharmadexLH-20柱色谱以及反相HPLC柱色谱分离纯化;运用光谱数据解析鉴定化合物结构;采用人肿瘤细胞、MPP+诱导PC12细胞损伤和多形核白细胞β葡萄糖苷酸酶释放药理模型筛选其活性。结果:从乙醇提取物的醋酸乙酯萃取部位中分离鉴定了17个萜类化合物,其中2个单萜类:(-)-龙脑阿魏酸酯(1)和黑麦交酯(2)。7个倍半萜类:1β-羟基-α-莎草酮(3),α-莎草醇(4),10α-hydroxycadin-4-en-15-al(5),1-epi-10β-hydroxycadin-4-en-15-al(6),10α-hydroxyisodauc-3-en-15-al(7),大根香叶烯B(8)和mandassidione(9)。5个二萜类:12-epi-bacchotricuneatinA(10),1-hydroxy-12-epi-bacchotricuneatinA(11),cleroinermin(12),desoxyarticulin(13)和anhydroolearin(14)。3个三萜类:木栓酮(15),熊果酸(16)和obtusalin(17)。化合物1对人胃癌细胞(BGC-823)显示一定的生长抑制作用,IC50值为8.00×10-5mol·L-1,活性强度与阳性对照喜树碱接近;在1×10-5mol·L-1浓度下,化合物12对MPP+致PC12细胞损伤有保护作用,与模型组比较相对保护率为104.32%,有显著差异(P<0.001);在1×10-5mol·L-1浓度下,化合物2能抑制PAF刺激的多形核白细胞β葡萄糖苷酸酶释放,抑制率为52.7%(P<0.05)。结论:化合物1~17均为首次从异裂菊属植物中分离鉴定;化合物1对人胃癌细胞具有选择性生长抑制活性,化合物12有神经细胞保护活性,化合物2具有潜在抗炎作用,其他化合物在测试浓度下在以上筛选模型中未显示明显活性。
Objective:To investigate the chemical constituents of Heteroplexis micocephala. Method:The constituents were isolated by using a combination of various chromatographic techniques including column chromatography over silica gel,Pharmadex LH-20,and C-18,as well as reversed-phase HPLC. Structures of the isolates were identified by spectroscopic data analysis. In vitro cytotoxic,neuroprotective,and anti-inflammatory activities were screened by using cell-based models. Result:Seventeen terpenoids were isolated. The structures were identified as two monoterpenoids:(-)-bornyl ferulate(1) and loliolide(2). Seven sesquiterpenoids:1β-hydroxy-α-cyperone(3),α-rotunol(4),10α-hydroxycadin-4-en-15-al(5),1-epi-10β-hydroxycadin-4-en-15-al(6),10α-hydroxyisodauc-3-en-15-al(7),germacrene B(8),and mandassidione(9). Five diterpenoids:12-epi-bacchotricuneatin A(10),1-hydroxy-12-epi-bacchotricuneatin A(11),cleroinermin(12),desoxyarticulin(13),and anhydroolearin(14). And three triterpenoids:friedelin(15),ursolic acid(16),and obtusalin(17). In the in vitro assays,1 showed selective cytotoxic activity against BGC-823,with an IC50 value of 8.00×10-5 mol·L-1. At a concentration of 1×10-5 mol·L-1,12 showed neuroprotective activity against MPP+ induced PC12-syn cell damage,with a relative cell proliferation rate of 104.32%(P<0.001). 2 exhibited inhibitory activity against the release of β-glucuronidase from the polymorphous nuclear leukocytes induced by PAF,with an inhibitory rate of 52.7%(P<0.05) at the same concentration. Conclusion:Compounds 1-17 were obtained from the genus Heteroplexis for the first time. 1 showed selective cytotoxic activity against human gastric cancer cell lines(BGC-823),12 and 2 showed potent neuroprotective and anti-inflammatory activities,respectively.

关键词(KeyWords): 异裂菊属;小花异裂菊;萜类;细胞毒活性;神经保护活性;抗炎活性
Heteroplexis; Heteroplexis micocephala; terpenoids; bioactivities.

Abstract:

Keywords:

基金项目(Foundation): 国家自然科学基金项目(30825044,20432030);; 教育部长江学者和创新团队支持计划(IRT0514);; 国家重点基础研究发展(973)计划(2004CB13518906,2006CB504701)

作者(Authors): 樊晓娜;林生;朱承根;胡金凤;刘洋;陈晓光;陈乃宏;王文杰;石建功;
FAN Xiaona,LIN Sheng,ZHU Chenggen,HU Jinfeng,LIU Yang,CHEN Xiaoguang,CHEN Naihong,WANG Wenjie,SHI Jiangong (Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College (Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine,Ministry of Education,Beijing 100050,China)

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