首页|三色旋花化学成分及抗炎活性研究

三色旋花化学成分及抗炎活性研究

扫码查看
目的:研究三色旋花种子的化学成分及单体化合物的抗炎活性.方法:采用硅胶、十八烷基硅烷键合硅胶填料(Octadecylsilyl,ODS)反相色谱和制备型HPLC等方法分离纯化,并利用核磁共振(nuclear magnetic resonance,NMR)、质谱(mass spectrometry,MS)等波谱学方法鉴定化合物的结构.利用脂多糖(lipopolysaccharide,LPS)诱导的RAW264.7 细胞模型及分子对接技术,初步探索所分离化合物的抗炎作用.结果:从三色旋花种子的二氯甲烷部位中分离得到 11 个化合物,分别是 α-亚油酸(1)、1-亚油酸甘油酯(2)、N-亚油酸乙醇胺(3)、咖啡酸乙酯(4)、5-hydroxy-3,4-dimethy-5-pentyl-2(5H)-furanone(5)、东莨菪素(6)、3-吲哚甲醛(7)、methyl dioxindole-3-acetate(8)、ethyl dioxindole-3-acetate(9)、coixspirolactam B(10)、coixspirolactam C(11).活性研究发现,化合物 4 能够显著抑制LPS诱导的一氧化氮生成,而且能显著抑制炎症因子诱导型一氧化氮合酶(inducible nitric oxide synthase,iNOS)和环氧合酶-2(cyclooxygenase-2,COX-2)的表达,并能与iNOS和COX-2 蛋白结合,进而发挥抗炎作用.结论:化合物 2~5 和 7~11 为首次从旋花属植物中分离得到,化合物 1 为首次从植物三色旋花中分离得到.其中,化合物 4 具有显著的抗炎活性,具有进一步研究开发的价值.
Chemical constituents from Convolvulus tricolor L.and their anti-inflammatory activities
Objective:To study the chemical constituents from Convolvulus tricolor L.(C.tricolor)and their anti-inflammatory activities.Methods:The chemical constituents were separated and purified by silica gel,Octadecylsilyl(ODS)reverse phase chromatography and preparative HPLC,and were identified by nuclear magnetic resonance(NMR)and mass spectrometry(MS)spectroscopic techniques.The lipopolysaccharide(LPS)-induced RAW264.7 cell model and molecular docking technology were used to evaluate the anti-inflammatory activities.Results:Eleven compounds were isolated from dichloromethane extract of C.tricolor seeds,and were identified as α-linoleic acid(1),1-monolinolein(2),N-linoleoylethanolamine(3),ethyl caffeate(4),5-hydroxy-3,4-dimethy-5-pentyl-2(5H)-furanone(5),scopoletin(6),3-indole formaldehyde(7),methyl dioxindole-3-acetate(8),ethyl dioxindole-3-acetate(9),coixspirolactam B(10),coixspirolactam C(11).The activity research found that compound 4 could significantly reduce LPS-induced nitric oxide generation,which can also significantly inhibit the expression of inducible nitric oxide synthase(iNOS) and cyclooxygenase-2(COX-2),and bind to iNOS and COX-2 proteins,thereby exerting anti-inflammatory effects. Conclusions:Compounds 2-5 and 7-11 were firstly isolated from genus Convolvulus,while compound 1 was isolated C. tricolor for the first time. Among them,compound 4 exhibited potent anti-inflammatory activity,and had value for further research and development.

Convolvulus tricolor L.chemical constituentsanti-inflammatory activitymolecular docking

李雨欣、祝东荣、张熙晗、祁天姿、顾金萍、林斌、陆天琦、王雯丽、范博义

展开 >

南通大学药学院,江苏 226019

天津理工大学化学化工学院

沈阳药科大学无涯创新学院

江苏浩丰生物科技有限公司

展开 >

三色旋花 化学成分 抗炎活性 分子对接

国家自然科学基金国家自然科学基金南通市科技计划江苏省研究生科研与实践创新计划国家级大学生创新创业训练计划

3237041932100317MSZ2022173KYCX22-3381202310304067Z

2024

南通大学学报(医学版)
南通大学

南通大学学报(医学版)

影响因子:0.637
ISSN:1674-7887
年,卷(期):2024.44(2)