| 玉竹中高异黄酮类化合物生物活性研究 |
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| 引用本文： | 李丽红,任风芝,郑智慧,陈书红,高月麒,朱秀良.玉竹中高异黄酮类化合物生物活性研究[J].河北师范大学学报(自然科学版),2012,36(5):509-511. |
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| 作者姓名： | 李丽红 任风芝 郑智慧 陈书红 高月麒 朱秀良 |
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| 作者单位： | 华北制药集团新药研究开发有限责任公司微生物药物国家研究工程中心,河北石家庄,050015 |
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| 基金项目： | 国家重大新药创制专项(2010ZX09401-403) |
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| 摘 要： | 采用四唑盐(MTT)比色法、白细胞弹性蛋白酶抑制剂筛选模型及二氢乳清酸脱氢酶抑制剂筛选模型对从玉竹中分离出的4个高异黄酮类化合物进行生物活性评价,探讨化合物结构与其活性之间的构效关系.高异黄酮类化合物1～4对肿瘤细胞K562,A549和HCT-15具有细胞毒性,IC50为7～35μg/mL;化合物1～4对人白细胞弹性蛋白酶有抑制作用,IC50分别为13.1,70.4,13.8,55.2μg/mL;化合物2,4对二氢乳清酸脱氢酶有一定的抑制作用,IC50分别为10.0,11.1μg/mL.高异黄酮类化合物的生物活性与其取代基的类型及位置有关.
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| 关 键 词： | 玉竹 高异黄酮类化合物 抗肿瘤活性 人白细胞弹性蛋白酶 二氢乳清酸脱氢酶 |
Studies on Biological Activity of Homoisoflavanones from Polygonatum odoratum(Mill.) Druce |
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| LI Lihong
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REN Fengzhi
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ZHENG Zhihui
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CHEN Shuhong
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GAO Yueqi
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ZHU Xiuliang.Studies on Biological Activity of Homoisoflavanones from Polygonatum odoratum(Mill.) Druce[J].Journal of Hebei Normal University,2012,36(5):509-511. |
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| Authors: | LI Lihong REN Fengzhi ZHENG Zhihui CHEN Shuhong GAO Yueqi ZHU Xiuliang |
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| Institution: | (New Drug Research and Development Center of North China Pharmaceutical Group Corporation, National Microbial Medicine Engineering and Research Center,Hebei Shijiazhuang 050015,China) |
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| Abstract: | MTT assays were used to explore the inhibiting effect of the homoisoflavanones on cancer cell.Two high throughput screening modeles were established,one for screening human leukocyte elastase(HLE) inhibitor and the other for dihydroorotate dehydrogenase(DHODH) inhibitor from nature product.Compound 1~4 showed inhibitory activity on K562,A549 and HCT-15 cancer cell with IC50 from 7 to 35 μg/mL.Compound 1~4 showed inhibitory activity against HLE with IC50 of 13.1,70.4,13.8,55.2 μg/mL,respectively.Compound 2 and 4 showed inhibitory activity against DHODH with IC50 10.0,11.1 μg/mL,respectively.The location and type of substituent group affect biological activity of homoisoflavanones. |
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| Keywords: | Polygonatum odoratum homoisoflavanones anti-tumor activity human leukocyte elastase dihydroorotate dehydrogenase |
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