基于LC-DAD-MS技术为导向的两种中亚特色植物结构新颖二萜生物碱的发现及其生物活性研究
批准号:
32000277
项目类别:
青年科学基金项目
资助金额:
24.0 万元
负责人:
赵波
依托单位:
学科分类:
植物化学
结题年份:
2023
批准年份:
2020
项目状态:
已结题
项目参与者:
赵波
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中文摘要
二萜生物碱具有广泛的生物活性与药用价值,尤其在抗心律不齐和镇痛方面作用显著,目前已有4个二萜生物碱应用于临床。迄今,已报道的天然二萜生物碱已有千余个,主要来源于毛茛科翠雀属和乌头属植物。前期研究发现,以毛果船苞翠雀花和牛扁为代表的中亚地区特色翠雀属和乌头属植物中的二萜生物碱成分具有骨架类型多样、新颖度高和成药潜力大等特征,具有很好的深入研究和开发的价值。本项目在已有的研究基础上,以LC-DAD-MS技术为导向,结合现代化的分离纯化技术,从毛果船苞翠雀花和牛扁中分离结构新颖的二萜生物碱,采用多种波谱和光谱学方法和技术确定其结构,进行抗心律不齐、镇痛和肿瘤细胞毒等生物活性筛选,完善其构效关系,为进一步高效低毒的二萜生物碱先导化合物的发现奠定物质基础,也为自主知识产权的创新药物开发及中亚地区特色植物资源可持续利用提供科学依据,并在寻找有益于人类健康的新颖活性天然产物方面具有重要意义。
英文摘要
Diterpenoid alkaloids are a kind of nitrogen-containing organic compounds with wide range of biological activities and medicinal value, especially in the aspects of antiarrhythmic and analgesia. Four diterpenoid alkaloids have been used in clinical. At present, more than one thousand natural diterpenoid alkaloids have been found, which are mainly from genera Delphinium and Aconitum of Ranunculaceae family. It was found that the diterpenoid alkaloids from the characteristic Delphinium and Aconitum plants in Central Asia, represented by Delphinium naviculare var. lasiocarpum and Aconitum barbatum var. puberulum, have the characteristics of diverse skeleton types, high novelty and great potential for medicine, which have a great value for in-depth research and development. On the basis of the existing research, this project will guided by LC-DAD-MS and combined with modern separation and purification technologies, the diterpenoid alkaloids with new structure will be isolated from the Delphinium naviculare var. lasiocarpum and Aconitum barbatum var. puberulum, while their structures will identified by a variety of spectral and spectroscopic methods and technologies. The biological activities such as antiarrhythmic, analgesia and cytotoxicity of the isolations will be tested, and their structure-activity relationships will be improved. The results of this project will lay a material foundation for further discovery of high-efficiency and low-toxicity lead compounds of diterpenoid alkaloids, provide a scientific basis for the development of innovative drugs with independent intellectual property rights and the sustainable utilization of characteristic plant resources in Central Asia, as well as be of great significance in finding new active natural products beneficial to human health.
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DOI:DOI 10.1007/s10600-023-04010-x
发表时间:2023
期刊:Chemistry of Natural Compounds
影响因子:--
作者:N. Ablajan;W. J. Xue;J. Y. Zhao;D. R. Kodirova;Sh. Sh. Sagdullaev;B. Zhao;H. A. Aisa
通讯作者:H. A. Aisa
DOI:10.1002/cbdv.202200936
发表时间:2023-01
期刊:Chemistry & Biodiversity
影响因子:2.9
作者:N. Ablajan;W. Xue;Jiang-yu Zhao;Abdubakiev Sardorbek;Nurmirza Boymirzayevich Begmatov;S. Sagdullaev
通讯作者:N. Ablajan;W. Xue;Jiang-yu Zhao;Abdubakiev Sardorbek;Nurmirza Boymirzayevich Begmatov;S. Sagdullaev
DOI:10.1080/14786419.2021.2005050
发表时间:2021-11-10
期刊:NATURAL PRODUCT RESEARCH
影响因子:2.2
作者:Ablajan, Nurfida;Zhao, Bo;Aisa, Haji Akber
通讯作者:Aisa, Haji Akber
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