Wang Xuelian, Li Yeling, Liu Wenhui, Shen Yongye, Lin Zhen, Nakajima Akira, Xu Jing, Guo Yuanqiang
State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300350, People's Republic of China.
Department of Applied Biology and Food Sciences, Faculty of Agriculture and Life Science, Hirosaki University, 3 Bunkyo-cho, Hirosaki 036-8561, Japan.
Int J Biol Macromol. 2023 Aug 15;246:125555. doi: 10.1016/j.ijbiomac.2023.125555. Epub 2023 Jun 24.
Polysaccharides, an important class of carbohydrate polymers, are considered as one of the sources of drug molecules. To discover bioactive polysaccharides as potential agents against cancer, a homogeneous polysaccharide (IJP70-1) has been purified from the flowers of Inula japonica, which is a traditional medicinal plant used for various medical indications. IJP70-1 with a molecular weight of 1.019 × 10 Da was mainly composed of →5)-α-l-Araf-(1→, →2,5)-α-l-Araf-(1→, →3,5)-α-l-Araf-(1→, →2,3,5)-α-l-Araf-(1→, →6)-α-d-Glcp-(1→, →3,6)-α-d-Galp-(1→, and t-α-l-Araf. Apart from the characteristics and structure elucidated by various techniques, the in vivo antitumor activity of IJP70-1 was assayed using zebrafish models. In the subsequent mechanism investigation, it was found that the in vivo antitumor activity of IJP70-1 was not cytotoxic mechanism caused, but related to the activation of the immune system and inhibition of angiogenesis by interacting with the proteins toll-like receptor-4 (TLR-4), programmed death receptor-1 (PD-1), and vascular endothelial growth factor (VEGF). The chemical and biological studies have shown that the homogeneous polysaccharide IJP70-1 has the potential to be developed into an anticancer agent.
多糖是一类重要的碳水化合物聚合物，被认为是药物分子的来源之一。为了发现具有生物活性的多糖作为潜在的抗癌药物，从旋覆花（一种用于多种医学适应症的传统药用植物）的花朵中纯化出了一种均一多糖（IJP70-1）。分子量为1.019×10 Da的IJP70-1主要由→5)-α-L-阿拉伯呋喃糖-(1→、→2,5)-α-L-阿拉伯呋喃糖-(1→、→3,5)-α-L-阿拉伯呋喃糖-(1→、→2,3,5)-α-L-阿拉伯呋喃糖-(1→、→6)-α-D-葡萄糖吡喃糖-(1→、→3,6)-α-D-半乳糖吡喃糖-(1→和t-α-L-阿拉伯呋喃糖组成。除了通过各种技术阐明的特性和结构外，还使用斑马鱼模型测定了IJP70-1的体内抗肿瘤活性。在随后的机制研究中发现，IJP70-1的体内抗肿瘤活性不是由细胞毒性机制引起的，而是与通过与Toll样受体4（TLR-4）、程序性死亡受体1（PD-1）和血管内皮生长因子（VEGF）相互作用激活免疫系统和抑制血管生成有关。化学和生物学研究表明，均一多糖IJP70-1有潜力被开发成为一种抗癌药物。
