Duan Yuanqi, Hu Zhengyu, Jin Long, Zong Tieqiang, Zhang Xiaohui, Liu Yanan, Yang Pengcheng, Sun Jinfeng, Zhou Wei, Li Gao
Key Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, Yanbian University College of Pharmacy, Yanji 133002, PR China.
Key Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, Yanbian University College of Pharmacy, Yanji 133002, PR China.
Int J Biol Macromol. 2024 Sep;276(Pt 1):134117. doi: 10.1016/j.ijbiomac.2024.134117. Epub 2024 Jul 31.
The degradation of Belamcanda chinensis (L.) DC. polysaccharides was carried out by five concentrations of trifluoroacetic acid (TFA) (1-5 mol/L), and their physicochemical properties, degradation kinetics and anticomplementary activity were investigated. The findings revealed a notable reduction in the molecular weight of BCP, from an initial value of 2.622 × 10 g/mol to a final value of 6.255 × 10 g/mol, and the water solubility index increased from 90.66 ± 0.42 % to 97.78 ± 0.43 %. The degraded polysaccharides of B. chinensis exhibited a comparable monosaccharide composition comprising Man, GalA, Glc, Gal, and Ara. As the concentration of TFA increased, the degradation rate constant increased from 1.468 × 10 to 5.943 × 10, and the process followed the first-order degradation kinetic model (R > 0.97) and the random fracture model (R > 0.96). Furthermore, the five degraded polysaccharides still exhibit good thermal stability. In vitro experiments showed that DBCP-3 exhibited more potent anticomplementary activity than the original polysaccharides and positive drugs, which was strongly correlated with its Mw (r = 0.6-0.8), inhibiting complement activation by blocking C2 and C4. These results indicated that TFA degradation has a positive effect on polysaccharides, of which DBCP-3 is expected to treat diseases involving hyperactivation of the complement system.
采用五种浓度(1 - 5 mol/L)的三氟乙酸(TFA)对射干多糖进行降解,并对其理化性质、降解动力学及抗补体活性进行研究。结果表明,射干多糖的分子量显著降低,从初始值2.622×10 g/mol降至最终值6.255×10 g/mol,且水溶性指数从90.66±0.42%增至97.78±0.43%。降解后的射干多糖具有相似的单糖组成,包括甘露糖、半乳糖醛酸、葡萄糖、半乳糖和阿拉伯糖。随着TFA浓度增加,降解速率常数从1.468×10增至5.943×10,降解过程符合一级降解动力学模型(R>0.97)和随机断裂模型(R>0.96)。此外,五种降解多糖仍具有良好的热稳定性。体外实验表明,DBCP - 3比原始多糖和阳性药物表现出更强的抗补体活性,这与其分子量密切相关(r = 0.6 - 0.8),通过阻断C2和C4抑制补体激活。这些结果表明,TFA降解对多糖有积极作用,其中DBCP - 3有望用于治疗涉及补体系统过度激活的疾病。