| 李昕茹,孙继芹,仇会鑫,等.绿藻鼠李聚糖模拟物的制备与抗EV71病毒活性评价[J].中国海洋药物,2022,41(3):1-9. |
| 绿藻鼠李聚糖模拟物的制备与抗EV71病毒活性评价 |
| Efficient synthesis and anti-EV71 activity study of green alga rhamnan glycomimetics |
| 投稿时间：2021-04-16 修订日期：2021-05-13 |
| DOI： |
| 中文关键词: 鼠李糖 聚酰胺胺 树枝状-星型糖聚合物 烯烃复分解开环聚合反应，抗病毒活性 |
| English Keywords:rhamnose PAMAM dendrimer-star glycopolymers ROMP antiviral activity |
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| 中文摘要: |
| 目的 海洋绿藻中含有丰富的硫酸化鼠李聚糖,具有抗病毒、抗肿瘤等多样生物活性。然而由于天然提取的鼠李聚糖结构复杂,限制了其构效关系的深入研究,设计开发结构均一、质量可控的天然鼠李聚糖模拟物,对于推动其作为药物开发具有重要意义。方法 以α-L-鼠李单糖为起始原料,通过衍生修饰和烯烃复分解开环聚合(ROMP)反应,首先制备了线性鼠李糖聚合物；然后以聚酰胺-胺(PAMAM)为骨架,基于“先臂后核”的设计思路,制备树枝状-星型鼠李糖聚合物。对制备的鼠李糖聚合物进行硫酸化修饰,模拟天然硫酸化绿藻多糖,并对其抗病毒活性开展研究。结果 通过烯烃复分解开环聚合反应成功制备了线性鼠李糖聚合物,并开发了一种以树枝状大分子PAMAM为骨架制备星型鼠李糖聚合物的高效方法。结论 通过单体聚合和末端枝接聚合法成功制备线性及树枝状-星型的天然绿藻鼠李聚糖模拟物,并证明该系列模拟物具有抗EV71病毒活性。 |
| English Summary: |
| Objective Marine green alga contain abundant sulfated rhamnose plysaccharides, which possess various biological activities including antiviral and antitumor, etc. However, due to the complexity of the structure of natural rhamnose polysaccharide, few studies reported its structure-activity relationship. How to design and develop natural rhamnose mimics with uniform structure and controllable quality is of great significance to promote its drug development. Methods By using rhamnose monosaccharide as starting material, linear rhamnose-based polymer was synthesized by derivatization and ring-opening metathesis polymerization (ROMP). Meanwhile, a series of dendrimer-star rhamnose polymers were prepared based on the idea of "arm first" with polyamide amine (PAMAM) as skeleton. The rhamnose polymers were sulfated to simulate the natural sulfated polysaccharides from green alga, and their antiviral activities were studied. Results Based on the ROMP polymerization of linear rhamnose polymers, the efficient end grafting polymerization of PAMAM was developed for the synthesis of dendrimer-star rhamnose-based polymers. Conclusion In this study, the linear and dendrimer-star like rhamnan mimetics of green alga were successfully prepared by monomer polymerization and end grafting polymerization, which were proved to possess anti-EV71 virus activities. |
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