【作者】 徐静；

【导师】 田瑄； 刘珍伶；

【作者基本信息】 兰州大学 ， 有机化学， 2011， 硕士

【摘要】 开唇兰属(Anoectochilus)系兰科(Orchidaceae)多年生草本植物。该属植物约有40余种,分布于亚洲热带地区至大洋洲。我国有20种,2个变种,产于西南部至南部,其中花叶开唇兰和台湾开唇兰最有价值,既是我国民间使用的一类珍贵中药材,同时又是室内观赏植物珍品。该属的部分种全草民间作药用,具有清热、凉血、祛风利湿以及降血压等功效。金线莲是开唇兰属中的一员,主要分布于云南、四川、贵州、广西、西藏、浙江、江西、广东、海南、福建以及台湾等省区,民间有“药王”之称。据报道,该属植物普遍含有黄酮及苷类化合物。本文对金线莲(Anoectochilus roxburghii)乙酸乙酯部分的主要化学成分进行了研究,应用硅胶柱层析(CC)、制备薄层层析(PTLC)、重结晶等方法分离得到31个化合物,并且应用UV、IR、MS、NMR等波谱技术及熔点、旋光等物理常数,结合相关文献以及与标样对照,鉴定了27个化合物的结构,主要为黄酮、苷类以及三萜类化合物,其中1个为新化合物,6个化合物为首次从该属植物中分离得到,同时也测定了其中一部分化合物的抗氧化活性。鬼臼毒素是一种天然的木脂素类化合物。鬼臼及其衍生物具有显著的生物活性,如抗病毒、抗肿瘤、杀虫等。其中,抗肿瘤活性最引人关注,常作为研究开发抗癌药物的先导化合物。我们对已合成的7个脱氧鬼臼自旋标记衍生物进行了体外抗肿瘤、抗氧化活性研究和脂水分配系数的测定,发现其中5个化合物对人肺癌细胞(A-549)的活性优于VP-16和母体化合物,3个化合物对白血病细胞(HL-60)也有较好的活性。同时发现这些化合物均有很好的水溶性,与VP-16和母体化合物相比,其抗氧化能力也明显增强。更多还原

【Abstract】 The genus Anoectochilus, belonging to Orchidaceae, is a perennial herb, which comprise more than 40 species that are widespread in the tropical regions, from Asia to Oceania. There are 20 species and 2 varieties in China, from southwest to the south. Among them, Anoectochilus roxburghii and Anoectochilus formosanus are most valuable, which have been used in Chinese folk medicines, and at the same time, they are all ornamental plants. Several species of this genus are used as folk medicines for febrifugation, detoxification, dispelling wind, eliminating dampness and hypertension. The Anoectochilus roxburghii, a member of genus Anoectochilus, which is called "King Medicine", mainly distributes in Yunnan, Sichuan, Guizhou, Guangxi, Tibet, Zhejiang, Jiangxi, Guangdong, Hainan, Fujian and Taiwan etc. It is common knowledge that this genus has been identified to contain flavones and glycosides.This dissertation studies on chemical constituents of the EtoAc part of Anoectochilus roxburghii. 31 compounds have been isolated by silica gel column chromatography (CC), preparative thin layer chromatography (PTLC) and recrystallization etc.. The structures of 27 compounds have been elucidated by spectroscopic methods:UV、IR、MS、NMR, physical constants:melting point and optical rotation, as well as comparison with authentic samples or the data from literature. The were identified as flavones, glycosides and triterpenes etc., one of them is new compound, six compounds are isolated from this genus for the first time. Meanwhile, the antioxidative activities of some of them were tested.Podophyllotoxin is a natural lignan compound. Podophyllotoxin as well as its congeners and derivatives exhibits pronounced biological activity mainly as antiviral, antineoplastic and insecticidal etc.. Among them, antitumor activity is the most attractive, making it as a lead compound for anticancer drug design and development. In this part of thesis,7 novel spin labeled derivatives of deoxypodophyllotoxin compounds which have been synthesized, we evaluated for their cytotoxic, antioxidative activities in vitro and lipid-water partition coefficient. As a result,5 compounds show higher inhibition activity against A-549 cells compared with the clinical drug VP-16 and parent compound,3 compounds show excellent inhibition activity against HL-60 cells. All these derivatives have a good aqueous solubility and significantly antioxidative activity compared with VP-16 and parent compound.更多还原