川续断是川续断科植物川续断的干燥根,具有抗菌、消炎、抗氧化、抗肿瘤、神经保护等药理活性。川续断皂苷VI是川续断的主要活性成分,也是《中国药典》(2020版)规定的川续断的指标成分。自2007年以来,川续断皂苷VI的药理活性和临床用途吸引了国内外众多医药工作者的关注,据不完全统计,迄今已有相关专利20余项,研究论文近百篇。本期我们来一起认识川续断皂苷VI这个明星天然化合物吧!The traditional Chinese medicine Chuan-Xu-Duan, possesses pharmacological activities of antibacterial, anti-inflammatory, antioxidant, anticancer, and neuroprotective effects, is the dried root of the plant Dipsacus asper Wall. exHenry belonging to the Dipsacus family. Dipsacus asperoside VI is the principal active constituent of Chuan-Xu-Duan, and it is also the designated marker compound for Chuan-Xu-Duan as specified in the Pharmacopoeia of the People's Republic of China (2020 edition).Since 2007, the pharmacological activities and clinical applications of dipsacus asperoside VI have garnered significant attention from numerous domestic and international pharmaceutical researchers. According to incomplete statistics, there have been more than 20 related patents and nearly one hundred research papers published to date.川续断皂苷VI的化学结构 1 结构与命名如图所示,川续断皂苷VI,又称木通皂苷D,英文名为akebia saponin D,其骨架为齐墩果烷型五环三萜,在齐墩果烷母核的C-3位连接1个阿拉伯糖,C-28位连接1个龙胆二糖。1. Name and StructureDipsacus asperoside VI, as shown in above figure, is also named as akebia saponin D, belonging to the oleanane-type pentacyclic triterpenoid saponins. It features an arabinose moiety linked to the C-3 position of the oleanane nucleus and a gentiobiose moiety linked to the C-28 position. 2 理化性质川续断皂苷VI为白色粉末,可用氯仿/甲醇结晶。其分子式为C47H76O18,分子量为928.50,熔点为234-235℃,CAS号为39524-08-8。川续断皂苷VI可发生Liebermann-Burchard反应、Kahlenberg反应和Tschugaeff反应,其酸水解产物为三萜母核和阿拉伯糖、葡萄糖。2. Physical and Chemical PropertiesDipsacus asperoside VI presents as a white powder that can be crystallized using chloroform/methanol. Its molecular formula is C47H76O18, with a molecular weight of 928.50. It exhibits a melting point of 234-235℃ and is identified with CAS number 39524-08-8.Dipsacus asperoside VI can be identified by the Liebermann-Burchard reaction, Kahlenberg reaction, and Tschugaeff reaction. Upon acid hydrolysis, it yields triterpenoid nucleus, arabinose, and glucose as products. 3 药理活性现代药理学研究表明,作为续断的主要活性成分,川续断皂苷VI能有效透过血脑屏障,具有显著的抗骨质疏松、抗炎及神经保护等活性。3. Pharmacological ActivitiesDipsacus asperoside VI, as the primary active compound of Chuan-Xu-Duan, exhibits the capability to effectively penetrate the blood-brain barrier, and show significant activities in terms of anti-osteoporosis, anti-inflammatory, and neuroprotective effects, which has been revealed by modern pharmacological studies.3.1 治疗筋伤骨折张玮、Ishida K,Haudenschild D.R.等人在独立动物实验中均发现川续断皂苷VI能上调小鼠成肌细胞C2C12中Ocn、Runx2和Col1α1的mRNA和蛋白质水平;Oury J等研究发现川续断皂苷VI可以通过PI3K/AKT信号通路诱导骨髓基质细胞成骨分化,还可以通过BMP-2/MAPK/SMAD依赖的Runx2信号通路诱导成骨细胞分化。此外临床实验证明川续断皂苷VI能够抑制破骨细胞的形成,促进成骨细胞分化,提高成骨细胞的活性和数量,进而促进基质钙化、骨痂生长,从而防止骨质疏松、促进骨折的愈合,发挥川续断“强筋骨、续折伤”的功效。3.1 Activity on Treatment of Tendon Injury and Bone FracturesProfessors Zhang Wei, Ishida K, Haudenschild D.R. …