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狄宏晔, 章蕴毅, 陈道峰. 补体抑制活性柴胡多糖及其作用靶点研究[J]. 中国天然药物, 2013, 11(2): 177-184.
引用本文: 狄宏晔, 章蕴毅, 陈道峰. 补体抑制活性柴胡多糖及其作用靶点研究[J]. 中国天然药物, 2013, 11(2): 177-184.
DI Hong-Ye, ZHANG Yun-Yi, CHEN Dao-Feng. Isolation of an anti-complementary polysaccharide from the root of Bupleurum chinense and identification of its targets in complement activation cascade[J]. Chinese Journal of Natural Medicines, 2013, 11(2): 177-184.
Citation: DI Hong-Ye, ZHANG Yun-Yi, CHEN Dao-Feng. Isolation of an anti-complementary polysaccharide from the root of Bupleurum chinense and identification of its targets in complement activation cascade[J]. Chinese Journal of Natural Medicines, 2013, 11(2): 177-184.

补体抑制活性柴胡多糖及其作用靶点研究

Isolation of an anti-complementary polysaccharide from the root of Bupleurum chinense and identification of its targets in complement activation cascade

  • 摘要: 目的:从北柴胡根中分离表征具有抗补体活性的多糖成分。方法:以抗补体活性为导向从北柴胡根水提物中分离纯化活性多糖;化学和谱学方法表征多糖的理化性质;采用体外细胞溶血试验法测定抗补体活性;并利用补体成分缺失血清鉴定补体激活过程中的作用靶点。结果:获得一个均一多糖BC-PS2,是一个具分支结构的杂多糖,平均分子量2 000 KDa,其单糖摩尔比为:葡萄糖/阿拉伯糖/半乳糖/甘露糖=3.5:2.4:2.0:1.0,并含有少量的鼠李糖和木糖以及蛋白(1.11%);单糖的主要连接方式包括:末端、1,3-、1,6-和1,3,6-连接的葡萄糖,末端、1,5-连接的阿拉伯糖,末端、1,4-、1,6-和1,4,6-连接的半乳糖,末端、1,4-和1,4,6-连接的甘露糖;BC-PS2对补体激活的经典和旁路途径均有抑制作用,CH50和AP50分别为(0.2220.013)和(0.3560.032)mgmL-1;靶点研究结果表明BC-PS2作用于补体成分C1q,C2和C9。结论:BC-PS2是一个具有抗补体活性的多糖成分,应该是柴胡治疗与补体过度激活相关疾病的药效成分之一。

     

    Abstract: AIM:To isolate and characterize the anti-complementary polysaccharide from the root of Bupleurum chinense.METHODS:Bioactivity-guided fractionation and purification was used to obtain the anti-complementary polysaccharide from the hot-water extract of the root of Bupleurum chinense.The polysaccharide was characterized by various chemical and spectral analyses.The anti-complementary activities were evaluated by hemolytic assay in vitro.The action targets were identified in the system with individual complement-depleted sera.RESULTS:A homogeneous polysaccharide BC-PS2 was isolated as an anti-complementary agent.It was identified as a branched polysaccharide with an average molecular weight about 2 000 KDa,composed of Glc,Ara,Gal,and Man in the ratio 3.5:2.4:2.0:1.0,respectively,along with a trace of Rha and Xyl,and only 1.11% of protein.The main linkages of the residues of BC-PS2 include terminal,1,6-linked,1,3-linked and 1,3,6-linked Glcp,terminal and 1,5-linked Araf,terminal,1,4-linked,1,6-linked and 1,4,6-linked Galp,terminal,and,1,4-linked and 1,4,6-linked Manp.The bioassay experiments revealed that BC-PS2 inhibited complement activation on both the classical and alternative pathways,with CH50 and AP50 of(0.2220.013) and(0.3560.032) mgmL-1,respectively.Preliminary mechanism studies indicated that BC-PS2 interacted with C1q,C2,and C9 components.CONCLUSION:The results demonstrated that BC-PS2 is an anti-complementary polysaccharide,and should be important constituent of the root of Bupleurum chinense for its application in the treatment of diseases associated with the excessive activation of complement system.

     

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