虎杖抗癌活性成分的研究

【作者】 裴莲花；

【导师】 吴学；

【作者基本信息】 延边大学 ， 有机化学， 2006， 硕士

【摘要】 虎杖（Polygonum Cuspidatum Sieb．et zucc）为蓼科（Polygonceae）蓼属（Polgohum）多年生灌木状草本植物虎杖（Polgonum cuspidatum）的根及根茎。筛选抗癌中药时发现中药虎杖在体外显示抗肿瘤作用。通过查找文献和初步抗癌实验表明其主要成分是蒽醌类化合物。为了进一步研究虎杖的抗癌活性成分和构效关系，从中筛选结构新颖且具有显著抗癌活性的先导化合物，对虎杖进行了系统的研究。本研究以乳腺癌（MCF-7）体外细胞毒活性为检测手段，对虎杖进行活性成分的追踪分离和结构鉴定。应用正相硅胶柱层析、反复柱层析分离技术，从虎杖中分离得到7个化合物，应用现代波谱技术(IR，EIMS，¹H-NMR，¹³C-NMR，DEPT，COSY，HSQC)和多种化学方法鉴定了7个化合物的结构：①大黄素甲醚（physcion）、②大黄素（emodin）、③黄葵内酯（Ambrettolide）、④β-谷甾醇（β-sitosterol）、⑤齐墩果酸（oleanolic acid）、⑥香豆素（coumarin）、⑦、2-乙氧基-8-乙酰基-1，4-萘醌（2-ethoxy-8-acetyl-1，4naphthoquinone）。 体外细胞毒性筛选实验表明，虎杖的乙醚提取物和从中分离得到的化合物①、②、③、⑦均对乳腺癌细胞MCF-7具有细胞毒活性。本论文首次对虎杖的乙醚提取物进行了系统的抗癌活性评价，为今后进一步研究虎杖资源提供参考数据。 本课题不仅丰富了对虎杖化学成分及其抗癌活性的了解，而且为进一步研究开发新的抗癌活性药物提供了科学依据。更多还原

【Abstract】 Polygonum Cuspidatum Sieb. et Zucc belongs to the genus of Polygonceae, family of Polgohum. Polygonum Cuspidatum Sieb. et Zucc were found to show significant bioactivities in vitro against human tumor cell lines. The experiment against human tumor and consulting literature indicate that their basis are the compounds of anthraquinone. In order to study many constituents concerning with anticancer and structure activity and discover natural products with new structures and bioactive activities, we have investigated the Polygonum Cuspidatum Sieb. et Zucc.a MCF-7 bioassay-guided fractionation led to the isolation of the active constituents. Seven compounds have been isolated from the ethanolic extract of Polygonum Cuspidatum Sieb. et Zucc by repeatedly chromatography on normal. By detailed analysis of the spectral data (IR, EIMS, ¹H-NMR, ¹³C-NMR, DEPT, COSY) and chemical methods. The compounds were characterized elucidated as following: physcion 、 emodin 、 Ambrettolide 、 β-sitosterol 、 Oleanolic acid 、 coumarin 、 2-ethoxy-8- acetyl-1, 4naphthoquinone。Some of them were found to show significant bioactivities in vitro against human tumor cell lines. Such as, the quantities of distilling in aether and compounds ①、 ②、 ③、 ⑦ against the human tumor cells MCF-7. We evaluated the activity of the compounds of anthraquinone systematically for the first time; The results can be the reference data for the further researching anticancer of Polygonum Cuspidatum Sieb. et Zucc for the future.These can help people to recognize the constituents of Polygonum Cuspidatum Sieb. et Zucc and also apply to science research of the new Antineoplastic Constituents.更多还原