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张琬玥, 刘玮, 徐航, 高向东. 肿节风多糖SGP-2的高级结构解析及构效关系研究[J]. 中国药科大学学报, 2021, 52(5): 630-635. DOI: 10.11665/j.issn.1000-5048.20210517
引用本文: 张琬玥, 刘玮, 徐航, 高向东. 肿节风多糖SGP-2的高级结构解析及构效关系研究[J]. 中国药科大学学报, 2021, 52(5): 630-635. DOI: 10.11665/j.issn.1000-5048.20210517
ZHANG Wanyue, LIU Wei, XU Hang, GAO Xiangdong. Advanced structure analysis and structure-activity relationship of polysaccharide SGP-2 from Sarcandra glabra[J]. Journal of China Pharmaceutical University, 2021, 52(5): 630-635. DOI: 10.11665/j.issn.1000-5048.20210517
Citation: ZHANG Wanyue, LIU Wei, XU Hang, GAO Xiangdong. Advanced structure analysis and structure-activity relationship of polysaccharide SGP-2 from Sarcandra glabra[J]. Journal of China Pharmaceutical University, 2021, 52(5): 630-635. DOI: 10.11665/j.issn.1000-5048.20210517

肿节风多糖SGP-2的高级结构解析及构效关系研究

Advanced structure analysis and structure-activity relationship of polysaccharide SGP-2 from Sarcandra glabra

  • 摘要: 肿节风多糖SGP-2是前期研究中从肿节风全草中提取、分离纯化得到的一种具有良好降血糖活性的酸性多糖。采用激光粒度分析、透射电子显微镜(TEM)及原子力显微镜(AFM)分析技术进行结构表征,分别对SGP-2在纯水及盐溶液中的高级结构以及不同理化条件处理后SGP-2及其衍生物的高级结构进行分析,并探讨了上述各样品的体外α-葡萄糖苷酶抑制活性。在纯水中SGP-2以聚集体及高分支球体两种构象存在,AFM分析得到SGP-2球体平均直径为33 nm,平均高度为1.84 nm。而在0.05 mol/L Na2SO4溶液中SGP-2主要表现为具有高分支结构的紧密球体且粒径降低。SGP-2经0.5 mol/L尿素处理并透析后的球体结构在1 000 μg/mL下抑制率可达原型SGP-2抑制率的98.8%;140 ℃加热后的SGP-2呈现分支杆状结构,于1 000 μg/mL下抑制率高达83.3%,对α-葡萄糖苷酶抑制的活性高于同浓度下的原型SGP-2;而羧基还原后的衍生物呈缠结链结构,对于α-葡萄糖苷酶的抑制活性大大降低。因此,球状结构或分支杆状结构对于SGP-2的活性发挥具有重要的作用。本研究为深入探讨多糖分子的高级结构与活性间的构效关系提供了理论依据。

     

    Abstract: SGP-2 was an acidic polysaccharide with good hypoglycemic activity isolated from Sarcandra glabra (Thunb.) Nakai in the previous study. This study used the laser particle size analysis, transmission electron microscopy (TEM) and atomic force microscopy(AFM) analysis techniques to analyze the advanced structure of SGP-2 in the deionized water and Na2SO4 solution and discuss the structure-activity relationship between the advanced structural characterizations and the α-glucosidase inhibition activities of SGP-2 and its derivative in vitro.Results showed that SGP-2 presented aggregates and spheres in the deionized water.AFM analysis showed that the diameter of SGP-2 was 33 nm and the height was 1.84 nm, whereas compact spherical conformations with high degrees of branching were observed in 0.05 mol/L Na2SO4 solution and SGP-2 had smaller particle size in saline solution compared with that in water.SGP-2 treated by 0.5 mol/L urea and dialysis at the concentration of 1 000 μg/mL showed 98.8% inhibition activity of that from untreated SGP-2. The inhibition rate of short rod conformation with branches reached 83.3% when the temperature rose up to 140 °C, and the α-glucosidase inhibition activity was even higher than that of untreated SGP-2 under the same condition; while SGP-2 with the tangled glycan chains under the condition of carboxyl group reduced had much lower inhibition activity.Therefore, the spherical structure or the short rod conformation with branches played an important role in the activity of SGP-2. This research provides a theoretical basis for further study of structure-function relationship between the advanced structure and activity of polysaccharides.

     

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