Xu Han, Zhang Yunyi, Zhang Jianwen, Chen Daofeng
School of Pharmacy, Fudan University, Shanghai, PR China.
Int Immunopharmacol. 2007 Feb;7(2):175-82. doi: 10.1016/j.intimp.2006.09.006. Epub 2006 Oct 5.
The preliminary data from hemolytic assays indicated that the hot-water extract of the roots of Bupleurum smithii had anti-complementary activity. Further bioactivity-guided fractionation led to the isolation of D3-S1, a homogeneous form of acidic polysaccharide. D3-S1 was a branched polysaccharide with average molecular weight about 2,000,000 Da, composed of Ara, Gal and GalA in the ratio of 2.6:1.0:1.2, along with trace of Rha, Glc, Xyl and Man. Methylation analysis and NMR identified the linkages of the residues of D3-S1. Functional analysis showed that D3-S1 inhibited complement activation on both the classic and alternative pathways with CH(50) value of 0.34+/-0.02 mg/ml and AP(50) value of 0.081+/-0.003 mg/ml, respectively. Preliminary mechanism studies by using complement component depleted-sera indicated that D3-S1 selectively interacts with C1s, C3 and C4, but not C1q, C1r, C2, C5 and C9. The results suggested that D3-S1 could be of potential benefits in treatment of the complement-associated diseases.
溶血试验的初步数据表明，太白柴胡根的热水提取物具有抗补体活性。进一步通过生物活性导向分离，得到了一种酸性多糖的纯化物D3-S1。D3-S1是一种支链多糖，平均分子量约为2,000,000 Da，由Ara、Gal和GalA以2.6:1.0:1.2的比例组成，还含有微量的Rha、Glc、Xyl和Man。甲基化分析和核磁共振确定了D3-S1残基的连接方式。功能分析表明，D3-S1对经典途径和替代途径的补体激活均有抑制作用，其CH(50)值分别为0.34±0.02 mg/ml和AP(50)值为0.081±0.003 mg/ml。使用补体成分缺失血清进行的初步机制研究表明，D3-S1选择性地与C1s、C3和C4相互作用，但不与C1q、C1r、C2、C5和C9相互作用。结果表明，D3-S1在治疗补体相关疾病方面可能具有潜在益处。
