课题基金基金详情
基于HPLC-DAD-Q-TOF/MS技术的桃金娘科瑶药中新颖结构C-甲基化黄酮的发现及其抗炎活性研究
结题报告
批准号:
81303162
项目类别:
青年科学基金项目
资助金额:
23.0 万元
负责人:
贾贝西
依托单位:
学科分类:
H3201.中药资源
结题年份:
2016
批准年份:
2013
项目状态:
已结题
项目参与者:
贾陆、柳继锋、宋旭、曾华金、符玲、徐寅鹏、周勇辉、蔡元元
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中文摘要
瑶族医药以疗效取胜,但系统性深入研究较少。桃金娘科常用瑶药用于多种炎症的治疗,其效果得到长期临床验证和认可,并且均含有黄酮类化合物,是主要抗炎活性成分。对岗松前期研究表明,C-甲基化黄酮是桃金娘科植物特征性的化学成分,具有良好的生物活性;由岗松中C-甲基化黄酮化学结构新颖多样性,以及类似酚酸偶合反应的生源途径推测,桃金娘科瑶药中依然存在结构新颖的活性C-甲基化黄酮类衍生物。本课题拟在前期工作基础上,基于HPLC-DAD-Q-TOF/MS技术,快速定向分离鉴定桃金娘科瑶药中新颖结构C-甲基化黄酮类成分;并结合药物功效及临床应用特点,采用现代药理模型与方法,从细胞/分子/动物水平探讨其抗炎作用及机制。该研究成果在丰富C-甲基化黄酮天然产物化学结构多样性,发掘具有潜在药用价值全新化合物的同时,阐明桃金娘科瑶药抗炎作用物质基础,这对我国民族医药资源开发和具有自主知识产权新药研发具有重要意义。
英文摘要
As an important part of Traditional Chinese Medicine, Yao medicines are famous for their mysterious curative effects on difficult miscellaneous diseases, but are lack of systematic and in-depth studies. Myrtaceae Yao medicines are used for the treatments of various inflammatory and their efficacies are validated by long-term clinical applications. To our knowledge, flavonoids are the main bioactive constituents of Myrtaceae medicinal plants. Our previous investigations of Baeckea frutescens L. revealed that C-methylated flavonoids might be distinctive of the family Myrtaceae and exhibited a variety of biological functions. The diversities of novel chemical structures and biosynthetic pathways (phenolic coupling reaction) of isolated C-methylated flavonoids suggested that novel and bioactive C-methylated flavonoids derivatives must exist in all species of Myrtaceae Yao medicines. This project is proposed on the basis of our preliminary work and focused on novel C-methylated flavonoids and their anti-inflammatory activity. From the points of time consuming and accurate mass measurement capability, HPLC-DAD-Q-TOF/MS is employed for screening and guiding target separation of new compounds in herbal extract. Considering traditional efficacy and clinical characteristics, modern pharmacological models and methods are used to investigate anti-inflammatory effects and mechanisms at cells, molecules and animal levels respectively. The results of current project will discover novel C-methylated flavonoids with potential medicinal value and elucidate the anti-inflammatory therapeutic material basis for Myrtaceae Yao medicines. Furthermore it is of great significance for esearch and development of new drugs with independent intellectual property rights and resource development of traditional minority medicine.
C-甲基化黄酮类天然产物结构新颖多样,是桃金娘科植物特征性的化学成分,也是桃金娘科常用瑶药中主要的抗炎活性成分。本项目在前期工作基础上,以6-甲基槲皮素为例,总结C-甲基化黄酮类成分的质谱裂解规律,采用HPLC-DAD-Q-TOF/MS技术,快速靶向从桃金娘科瑶药岗松中分离鉴定11个新颖结构的C-甲基化黄酮类化合物,并通过量子化学计算圆二色谱(CD)的方法确定其绝对构型;建立脂多糖(LPS)诱导小鼠单核巨噬细胞RAW 264.7模型,对所得化合物进行抗炎活性筛选,结构表明岗松中C-甲基化黄酮类成分均能显著抑制LPS诱导RAW 264.7细胞一氧化氮(NO)的分泌,具有良好的抗炎作用;以岗松化学分离所得化合物为对照品,采用HPLC-DAD-Q-TOF/MS方法,对岗松不同药用部位和不同采收期药材进行定性定量分析,结果表明岗松地上部分和地下部分药材所含化学成分的种类基本一致,但各成分相对含量差异较大,并通过各指标性成分在不同采收时间的含量变化曲线,确定了岗松不同入药部位的最佳采收期;建立佐剂性关节炎(AA)大鼠模型,进行岗松抗类风湿性关节炎(RA)的初步药理学评价与验证,结果表明岗松提取物具有良好的抗炎免疫作用,其对AA大鼠的治疗作用与阳性药雷公藤多苷相当;总之,以上针对瑶药岗松开展的系统化学成分成分、质量分析、及初步药理学评价等系列性研究工作,为后续瑶药岗松抗RA药效物质基础及作用机制的深入性研究奠定基础,并为我国桃金娘科植物岗松药用资源的开发利用提供科学依据。
期刊论文列表
专著列表
科研奖励列表
会议论文列表
专利列表
Baeckeins J and K, Two Novel C-Methylated Biflavonoids from the Roots of Baeckea frutescens and Their Cytoprotective Activities
Baeckeins J 和 K,来自 Baeckea frutescens 根的两种新型 C-甲基化双黄酮类化合物及其细胞保护活性
DOI:--
发表时间:2016
期刊:Helvetica Chimica Acta
影响因子:1.8
作者:Hui-Qin Zhao;Feng-Xiao Ren;Hong-Min Liu;Qiang Wang
通讯作者:Qiang Wang
Identification and quantification of flavonoids and chromes in Baeckea frutescens by using HPLC coupled with diode-array detection and quadruple time-of-flight mass spectrometry
使用 HPLC 结合二极管阵列检测和四重飞行时间质谱法对 Baeckea frutescens 中的类黄酮和铬进行鉴定和定量
DOI:10.1080/14786419.2014.987144
发表时间:2015-05
期刊:Natural Product Research
影响因子:2.2
作者:Yan-Bing Zhang;Hong-Min Liu;Jie Yang;Qiang Wang
通讯作者:Qiang Wang
Baeckeins F-I, four novel C-methylated biflavonoids from the roots of Baeckea frutescens and their anti-inflammatory activities
Baeckeins F-I,来自 Baeckea frutescens 根的四种新型 C-甲基化双黄酮类化合物及其抗炎活性
DOI:10.1016/j.foodchem.2014.01.022
发表时间:2014-07-15
期刊:FOOD CHEMISTRY
影响因子:8.8
作者:Jia, Bei-Xi;Zeng, Xian-Lei;Wang, Qiang
通讯作者:Wang, Qiang
国内基金
海外基金