摘要
目的本研究对忍冬花中均一多糖结构和抗新生血管生成活性进行研究,为忍冬的活性物质基础研究提供新的理论数据。方法水提醇沉并结合阴离子交换色谱和凝胶渗透色谱法获得忍冬均一多糖LF-02-2,并通过分子量检测、单糖组成分析、糖残基连接方式分析、部分酸水解、糖醛酸还原结合核磁共振数据推导出LF-02-2的结构。同时,运用人微血管内皮细胞管腔形成实验测定其体外抗新生血管活性。结果对LF-02-2的结构解析表明,均一多糖LF-02-2的重均分子量为74.1 kDa,其单糖组成由鼠李糖(Rha)、半乳糖(Gal)、半乳糖醛酸(GalA)和阿拉伯糖(Ara)组成,摩尔比分别为10.43∶14.94∶6.66∶67.97。其主链由1,4-连接的α-Galp A、1,2-连接的α-Rhap和1,2,4-连接的α-Rhap组成。分支由末端连接和1,4,6-连接的β-Galp,末端连接和1,5-连接的α-Araf连接,取代发生在1,2,4-连接的α-Rhap的O-4位。管腔形成实验结果表明LF-02-2能显著抑制人微血管内皮细胞(Human Microvascular Endothelial Cell,HMEC)的管腔形成。结论忍冬花中一种类RG-I型果胶多糖LF-02-2具有显著抗血管生成活性,具有开发为抗血管生成药物的潜力。
Objective This study aims to investigate the structure and anti-angiogenic activity of homogeneous polysaccharides in Honeysuckle flowers,constructing the theoretical basis for its widespread application.Methods Homogeneous Honeysuckle polysaccharide LF-02-2 was obtained through water extraction,alcohol precipitation,anion exchange chromatography,and gel permeation chromatography.The structure of LF-02-2 was deduced through molecular weight determination,monosaccharide composition analysis,sugar residue linkage analysis,partial acid hydrolysis,and sugar aldonic acid reduction combined with NMR data.Additionally,in vitro tube formation experiments using human microvascular endothelial cells(HMEC-1)were conducted to assess its anti-angiogenic activity.Results Structural analysis of LF-02-2 revealed a homogeneous polysaccharide with a weight-average molecular weight of 74.1 kDa.The monosaccharide composition included rhamnose(Rha),galactose(Gal),galacturonic acid(GalA),and arabinose(Ara)in molar ratios of 10.43:14.94:6.66:67.97.The main chain consisted of 1,4-linkedα-GalpA,1,2-linkedα-Rhap,and 1,2,4-linkedα-Rhap.Branches were connected to O-4 of 1,2,4-linkedα-Rhap and includedβ-Galp with terminal connections and 1,4,6-linkedβ-Galp andα-Araf with terminal and 1,5-linked connections.Tube formation experiments demonstrated that LF-02-2 significantly inhibited tube formation in human microvascular endothelial cells(HMEC).Conclusion LF-02-2,an RG-I pectic polysaccharide from Honeysuckle flowers,exhibited significant anti-angiogenic activity,suggesting its potential for development as an anti-angiogenic drug.
作者
靳灿
林黎艳
陈惠娴
丁侃
JIN Can;LIN Liyan;CHEN Huixian;DING Kan(Zhongshan Institute for Drug Discovery/Shanghai Institute of Materia Medica,Zhongshan 528400,China;Chinese Academy of Sciences Shanghai Institute of Materia Medica,Shanghai 201203,China;Southern Medical University,Guangzhou 510515,China;Lianyungang Higher Vocational Technical CollegeTraditional Chinese Medicine,Lianyungang 222007,China)
出处
《世界科学技术-中医药现代化》
CSCD
北大核心
2024年第5期1172-1181,共10页
Modernization of Traditional Chinese Medicine and Materia Medica-World Science and Technology
基金
国家自然科学基金委员会重点项目(31230022):抗肿瘤分子靶向性聚糖结构与功能机制研究,负责人:丁侃
作者简介
通讯作者:丁侃,研究员,博士研究生导师,主要研究方向:中药中多糖的结构与功能、构效关系、多糖的靶向性及其作用机理,细胞膜蛋白聚糖及其相关酶的功能机制以及糖类创新药物研究。
