College of Biotechnology and Food Engineering, Hefei University of Technology, Hefei 230009, China.
Carbohydr Polym. 2013 Sep 12;97(2):690-4. doi: 10.1016/j.carbpol.2013.05.033. Epub 2013 May 23.
Phosphorylated polysaccharide PLEP-1a, with the PO₄³⁻ content of 6.39%, was prepared from LEP-1a by phosphorylation. IR, (13)C NMR and (31)P NMR results of PLEP-1a showed that the original basic structure of the polysaccharide was not changed, and the -H₂PO₃ group was linked at C₆ of LEP-1a. The results of anti-tumor experiments in vivo showed that 100 mg/kg and 400 mg/kg of LEP-1a could significantly improve the food consumption, body weight, tumor inhibition rate and thymus index of S180 sarcoma mice, and increase the levels of SOD, IL-2 and TNF-α in mice blood serum, indicating that LEP-1a had an excellent anti-tumor activity. Furthermore, PLEP-1a had a significantly enhanced inhibitory effect on S180 sarcoma mice than LEP-1a, suggesting that phosphorylation is an effective way of improving the biological activity of LEP-1a.
从 LEP-1a 制备得到的磷酸化多糖 PLEP-1a 的 PO₄³⁻含量为 6.39%。PLEP-1a 的 IR、(13)C NMR 和 (31)P NMR 结果表明，多糖的原始基本结构没有改变，-H₂PO₃基团连接在 LEP-1a 的 C₆上。体内抗肿瘤实验结果表明，100 mg/kg 和 400 mg/kg 的 LEP-1a 可显著提高 S180 肉瘤小鼠的食物摄入量、体重、肿瘤抑制率和胸腺指数，并增加小鼠血清中超氧化物歧化酶（SOD）、白细胞介素-2（IL-2）和肿瘤坏死因子-α（TNF-α）的水平，表明 LEP-1a 具有优异的抗肿瘤活性。此外，与 LEP-1a 相比，PLEP-1a 对 S180 肉瘤小鼠具有显著增强的抑制作用，表明磷酸化是提高 LEP-1a 生物活性的有效途径。
