南欧大戟中大戟二萜类成分及其自噬相关活性评价

	南欧大戟中大戟二萜类成分及其自噬相关活性评价
	李盈瑶
导师	邸迎彤
关键词	南欧大戟 Euphorbia peplus 大戟二萜 Euphorbia diterpenoids 自噬-溶酶体 autophagy-lysosomal
摘要	自噬(autophagy）是一种维持细胞稳态的多功能降解系统，用于循环利用细胞内容物，清除聚集的蛋白质、受损的细胞器和入侵的病原体(如病毒和细菌)。自噬障碍与人类多种疾病有关，包括神经退行性疾病、癌症和肌肉性病变等。因此，寻找与自噬相关的药物在当今社会显得愈发重要。天然产物是发现治疗重大疾病的药物或重要先导化合物的主要源泉之一，有望从天然产物中寻找到相关的活性成分。南欧大戟（Euphorbia peplus Linn.）为大戟科（Euphorbiaceae）、大戟属（Euphorbia）植物，是一种民间草药，被用于哮喘、皮肤病和癌症等的治疗。南欧大戟中的二萜类成分，其结构复杂，药理活性显著。本课题以南欧大戟（Euphorbia peplus）为研究对象，对其二萜类化学成分进行了研究，并对分离得到的二萜类化合物进行自噬相关活性评价，期望能从中寻找到与自噬相关的活性分子。本论文一共分为三章。第一章阐述南欧大戟的化学成分研究。综合采用了各种分离手段（如：MCI小孔树脂、正相硅胶、反相硅胶、聚苯乙烯凝胶、葡聚糖凝胶以及半制备HPLC等）以及现代谱学技术（如UV、IR、NMR、X-ray单晶衍射等）从采自云南周边的南欧大戟中分离鉴定了共40个化合物，包括二萜38个，其中新化合物8个。二萜类化合物主要包括：26个jatrophane型二萜，4个ingenane型二萜，1个lathyrane型二萜，2个paraliane型二萜，2个abietane型二萜，3个pepluane型二萜。第二章阐述南欧大戟中大戟二萜类成分自噬相关活性评价。对从南欧大戟中分离得到的二萜类化合物1-38，基于自噬-溶酶体系统，利用HM mCherry-GFP-LC3细胞自噬流进行活性评估。发现新化合物1和2具有一定增强细胞自噬流的作用，其活性与阳性对照雷帕霉素（rapamycin）作用相当，因此其可能成为治疗相关疾病的潜在活性分子。第三章阐述大戟属植物中大戟二萜类化合物研究现状。主要对大戟二萜类成分的骨架类型，以及生源途径等内容进行了简要介绍。关键词：南欧大戟；大戟二萜；自噬-溶酶体; Autophagy is a versatile degradation system for maintaining cellular homeostasis. It is used to recycling cytosolic materials to remove the aggregated protein, damaged organelle and invasive pathogens (such as viruses and bacteria). Auto-dysfunction is related to various diseases, including neurodegenerative diseases, cancer and muscle lesions. Therefore, looking for autophagy-related drugs is becoming more important in today's society. Natural products are one of the main sources of drugs that treat major diseases or important pilot compounds. It is expected to find relevant active ingredients from natural products. Euphorbia peplus Linn. belongs to Euphorbia plant, which is a folk herb for treating skin diseases, asthma and cancer. The diterpenoids ingredients in the Euphorbia peplus have a complex structure, and the pharmacological activity is remarkable. This subject is based on the Euphorbia Peplus, and the diterpene compounds were studied and evaluated against autophagy activity. It is expected to find relevant Active molecule. This paper is divided into three chapters. Chapter Ⅰ illustrates the chemical composition of Euphorbia peplus. Fouty compounds were isolated from the whole plant of Euphorbia peplus by various separation means (MCI, silica gel, polystyrene gel, glucan gel, and semi-prepared HPLC) and modern spectrum techniques (UV, IR, NMR, X-Ray single crystal diffraction). There are 38 diterpene, including 8 new compounds. The diterpenoids mainly include: 26 jatrophane diterpenoids, 4 ingenne diterpenoids, 1 lathyrane diterpenoid, 2 paraliane diterpenoids, 2 abietane diterpenoids, and 3 pepluane diterpenoids. Chapter II illustrates the activity evaluation related to autophagy of diterpenoids from Euphorbia peplus. Based on the autophagy-lysosomal system, the compound 1-38 performs an active assessment by HM mCherry-GFP-LC3 cells autophagy flow. It is found that new compounds 1 and 2 can enhance cell autophagy flow, and their activity is comparable to the positive control rapamycin. So compounds 1 and 2 may become a potential active molecule of the treatment of related diseases. Chapter III illustrates the current status of the study on Euphorbia diterpenoids of Euphorbia. Mainly introduce the skeleton type of Euphorbia diterpenoids, as well as the biosynthetic pathway. Keywords: Euphorbia peplus; Euphorbia diterpenoids; autophagy-lysosomal
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/151853/75167
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	李盈瑶. 南欧大戟中大戟二萜类成分及其自噬相关活性评价[D]. 中国科学院大学,2022.

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