千日红和细梗美登木的化学成分与抗菌活性研究

	千日红和细梗美登木的化学成分与抗菌活性研究
	徐祥娟
导师	罗晓东
关键词	千日红、细梗美登木、抗铜绿假单胞菌、抗MRSA Gomphrena globosa, Maytenus graciliramula, Anti-Pseudomonas aeruginosa activities, Anti-MRSA activity
摘要	本论文主要由两章组成：第一章通过活性导向分离，对传统药食两用植物千日红 (Gomphrena globosa) 花序部分的化学成分进行分离和结构鉴定，并进一步对分离出的化合物进行体内体外的抗铜绿假单胞菌 (Pseudomonas aeruginosa) 活性研究；第二章对细梗美登木 (Maytenus graciliramula) 的茎枝部分进行了化学成分分离、结构鉴定和抗MRSA (Methicillin-resistant Staphylococcus aureus, 耐甲氧西林金葡菌) 活性评价。通过半制备高效液相色谱、Sephadex LH-20凝胶色谱、正反相硅胶柱色谱等各种分离手段和UV、IR、MS、NMR等各种波谱技术，对千日红和细梗美登木进行系统分离，从中分离到化合物30个，其中新化合物2个，类型涉及萜类、黄酮类和酚类化合物。同时，对分离的化合物进行一系列的抗菌活性评价。 1 千日红的化学成分及抗菌活性研究千日红 (G. globosa) 为苋科 (Amaranthaceae) 千日红属 (Gomphrena) 植物。《中华本草》记载，千日红花序入药，可用于治疗痢疾、痈肿、溃疡等疾病。本研究通过活性导向的手段，选取临床上常见的致病菌铜绿假单胞菌作为研究对象，从千日红的活性段中分离出15个化合物，其中2个为新的黄酮醇苷类化合物，化合物3、5-9、11为首次从千日红属中分离得到，化合物12、13为首次从千日红中分离得到。通过基本抗菌活性评价（MIC、时间杀菌曲线）发现，化合物4-7具有较好的抗铜绿假单胞菌活性。进一步，通过扫描电子显微镜SEM观察和动物实验发现，化合物4 (kaempferol) 具有显著的抗铜绿假单胞菌活性，强于阳性药物头孢曲松钠 (ceftriaxone sodium)。 2 细梗美登木的化学成分及抗菌活性研究细梗美登木 (M. graciliramula) 为卫矛科 (Celastraceae) 美登木属 (Maytenus) 植物。据文献记载，其茎枝入药，具有调补风塔和清火解毒的功效。本研究对细梗美登木进行化学成分和抗菌活性研究，从其茎枝部分的乙醇提取物的乙酸乙酯可溶物中得到15个化合物，化合物类型涉及到三萜类、倍半萜类、黄酮类，其中化合物10、12-14为首次从美登木属中分离得到，化合物11、15为首次从细梗美登木中分离得到；选取MRSA作为研究对象，对分离到的化合物进行抗菌活性评价发现，仅化合物8和11显示微弱的抗MRSA活性。; This dissertation is mainly composed of two chapters, in which chapter 1 included the isolation and identification of chemical constituents of Gomphrena globosa inflorescence with aid of bioguided isolation and anti-Pseudomonas aeruginosa activities of isolated compounds were studied in vitro and in vivo and chapter 2 described the isolation, identification, and anti-MRSA (Methicillin-resistant Staphylococcus aureus) activities evaluation of chemical constituents from the stems and branches of Maytenus graciliramula. With diverse separation methods (semi-preparative high-performance liquid chromatography, Sephadex LH-20 gel chromatography, normal and reversed phase silica gel column chromatography) and spectrum technologies (UV, IR, MS, and NMR), 30 compounds including 2 new flavonol glycosides were isolated and identified from two plants, among which the types of compounds involve terpenoids, flavonoids and phenols. Meanwhile, a series of antibacterial activities evaluation of isolated compounds were conducted. 1 Chemical constituents and anti-bacterial activities from Gomphrena globosa G. globosa belongs to the genus Gomphrena of the family Amaranthaceae. “Chinese Materia Medica” records, the inflorescence of G. globosa can be used to treat dysentery, carbuncle, sore, ulcer, etc. With aid of bioguided isolation, 15 compounds including 2 new flavonol glycosides were isolated from the fraction that showed potent anti-P. aeruginosa activity, among which compounds 3, 5?9, 11 were firstly isolated from the genus Gomphrena and compounds 12, 13 were firstly isolated from G. globosa. Based on MIC (Minimum inhibitory concentration) and time-kill curves studies, compounds 4-7 showed medium anti-P. aeruginosa activity. Furthermore, combined SEM (scanning electron microscope) observation and animal experiments, compound 4 (kaempferol) showed potent anti-P. aeruginosa activity in vitro and in vivo, which is better than that of positive control drug Ceftriaxone sodium. 2 Structures and anti-bacterial activities from Maytenus graciliramula M. graciliramula belongs to the genus Maytenus of the family Celastraceae. According to the literature, its stems and branches can be used as “Dai medicine” in china, and has the efficacy of clearing away heat and toxic material, pain killing and subsidence of swelling. The research studied the chemical constituents and anti-MRSA activity of M. graciliramula. 15 compounds including triterpenes, sesquiterpenoids, and flavonoids were isolated from the ethyl acetate soluble substance of ethanol extract from stems and branches of M. graciliramula, among which compounds 10, 12-14 were firstly isolated from the genus Maytenus and compounds 11, 15 were firstly isolated from M. graciliramula. Biological activity evaluation showed that compounds 8 and 11 showed weak anti-MRSA activity.
语种	中文
	2022-05
学位授予单位	中国科学院大学
文献类型	学位论文
条目标识符	http://ir.kib.ac.cn/handle/151853/75108
专题	昆明植物所硕博研究生毕业学位论文
推荐引用方式 GB/T 7714	徐祥娟. 千日红和细梗美登木的化学成分与抗菌活性研究[D]. 中国科学院大学,2022.

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