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对叶大戟中大环二萜类成分分离分析研究
陆东礼
Subtype硕士
Thesis Advisor阿吉艾克拜尔·艾萨
2013-05-28
Degree Grantor中国科学院大学
Place of Conferral北京
Degree Discipline有机化学
Keyword对叶大戟 大环二萜类化合物 生物活性 维吾尔药
Other Abstract

对叶大戟(Euphorbia sororiaA. Schrenk)是大戟科大戟属一年生草本植物,现主要分布于中亚与新疆田等地。对叶大戟是传统的维吾尔药材,具有利水消肿,镇咳平喘,燥湿开胃,健脑益智的作用。临床用于治疗腹胀胃弱,皮肤疾病和语言不利等疾病。

研究表明,大环二萜类化合物是其主要活性成分,具有抗肿瘤、抗HIV及抗菌等活性。我们课题组黄昀首次从对叶大戟中分到9个假白榄烷型大环二萜类化合物,为了进一步研究其物质基础,作者针对对叶大戟果实中的大环二萜类成分进行分离鉴定及活性筛选。

首先,通过硅胶柱、凝胶柱及制备反相柱等柱层析手段从对叶大戟果实中分到10个单体化合物,并通过核磁、质谱、X-单晶衍射等手段对其结构进行了鉴定。其中有6个新的大环二萜类化合物(化合物1-6)和2个已知的大环二萜类化合物(化合物7-8)首次从对叶大戟中分离得到。我们对化合物1-7进行了活性筛选,结果表明这些化合物虽然没有细胞毒性,但均具有一定的抗肿瘤多药耐药活性,其中化合物2有很强的多药耐药逆转活性。我们还对假白榄烷型化合物的多药耐药逆转活性的构效关系进行了初步的探讨。

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Euphorbia sororia A. Schrenk belongs to the euphorbia genus of the euphorbiaceae family, which is widely distributed in Central Asian and Hetian of Xinjiang Uighur Autonomous Regon. E. sororia, an annual herb, is traditional Uyghur medicinal herbs to cure abdominal pain, abdominal distention, skin disease, and paralysis. Macrocyclic diterpenes are the main bioactive constituents in the euphorbia genus. They exhibited multi-drug resistance reversal activity, antiproliferative activity, anti-HIV activity and so on. Previous phytochemical inveatigations on E. sororia yielded nine macrocyclic diterpenes. In the course of our investigation on this plant, ten compounds were isolated by different means, such as silica gel column, sephadex LH-20 and preparation HPLC. All the compounds were identified by MS and NMR spectral data. Among them, six new macrocyclic diterpenes (compounds 1-6) and two known macrocyclic diterpenes (compounds 7-8) were first isolated from this plant. Compounds 1-7 were assayed for their antiproferative activity in four human cancer cell lines, and they were inactive for all the cell lines. The multidrug-resistance-reversing activity was investigated on Kbv200 cells. Compound 2 displayed a strong multidrug-resistance-reversing activity. Preliminary structure activity relationship data are discussed. Key word: Euphorbia sororia, Macrocyclic Diterpene, Bioactivity, Uighur Medicine
Document Type学位论文
Identifierhttp://ir.xjipc.cas.cn/handle/365002/2497
Collection资源化学研究室
Affiliation中国科学院新疆理化技术研究所
Recommended Citation
GB/T 7714
陆东礼. 对叶大戟中大环二萜类成分分离分析研究[D]. 北京. 中国科学院大学,2013.
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