紫丁香苷及类似天然产物的全合成、结构改造与生物活性研究
批准号:
82003619
项目类别:
青年科学基金项目
资助金额:
24.0 万元
负责人:
董宏波
依托单位:
学科分类:
天然药物化学
结题年份:
2023
批准年份:
2020
项目状态:
已结题
项目参与者:
董宏波
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中文摘要
基于天然活性分子的先导化合物发现与研究,是创制新药最重要途径,是天然药物化学研究的热点。紫丁香苷(syringin)是一种广泛存在于维管植物中的苯丙素苷,生物活性丰富,为众多中药材的主要有效成分。自然界中还存在一些与紫丁香苷化学结构类似的天然产物,它们在抗氧化、抗炎、抗肿瘤三方面的活性十分突出。但由于其在自然界中丰度低、提取难度大,目前缺乏构效关系、作用机制以及作用靶点等系统性研究。为解决这些问题,本项目拟对含有紫丁香苷骨架的25个已报道的天然产物进行全合成(其中22个为首次全合成),并对其进行合理化衍生,系统的测试它们在抗氧化、抗炎、抗肿瘤三方面的活性,以阐明这类分子的构效关系,发现活性更好的先导化合物。这对于促进这类分子最终成药,推动来源植物的研究与开发都有着重要的意义。
英文摘要
Adopting natural products as the leading components and modifying the structure to improve pharmacological activity is one of the most important approaches to develop new drugs, which has been a popular field in recent years. Syringin, a phenylpropanoid glycoside which was identified in several vascular plants, is the main active ingredient of many traditional Chinese medicines. Although syringin and its natural analogues have the pharmacological properties including anti-inflammatory, antioxidant and antitumor activities, detailed pharmacological study of which so far has been minimal due to the low yield isolated from natural sources. As a result, the potential of these natural actives as leading compounds has been hampered by the lack of appropriate synthetic methodology. .In this project, we will synthesize 25 natural products with similar chemical structure of syringin and we also will obtain 100 derivatives of syringin. The anti-inflammatory, antioxidant and antitumor activities of them will be tested to establish the structure-activity relationship of this kind of compounds. Therefore this study will facilitate the final drugs developed from syringin and its analogues, and to promote research and development of the source plants.
期刊论文列表
专著列表
科研奖励列表
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专利列表
DOI:10.1021/acs.jnatprod.2c00021
发表时间:2022-04-22
期刊:JOURNAL OF NATURAL PRODUCTS
影响因子:5.1
作者:Dong, Hongbo;Wu, Min;Shi, Zheng
通讯作者:Shi, Zheng
DOI:10.1016/j.bioorg.2023.106764
发表时间:2023-08
期刊:Bioorganic chemistry
影响因子:5.1
作者:Hongbo Dong;Lihong Liao;P. Yu;Bin Long;Yufei Che;Lan Lu;Bing Xu
通讯作者:Hongbo Dong;Lihong Liao;P. Yu;Bin Long;Yufei Che;Lan Lu;Bing Xu
DOI:10.1691/ph.2021.1366
发表时间:2021-09-01
期刊:PHARMAZIE
影响因子:1.6
作者:He, Yujiao;Liu, Xiao;Liu, Deming
通讯作者:Liu, Deming
DOI:10.2174/1570178619666220111115718
发表时间:2022
期刊:Letters in Organic Chemistry
影响因子:--
作者:Min Wu;Lijia Xu;Mingwei Song;Ying Li;Yingying Wang;Hongbo Dong
通讯作者:Hongbo Dong
DOI:10.1021/acs.jnatprod.4c00008
发表时间:2024-02-19
期刊:JOURNAL OF NATURAL PRODUCTS
影响因子:5.1
作者:Dong,Hongbo;Liao,Li;Xu,Bing
通讯作者:Xu,Bing
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