Chem. J. Chinese Universities ›› 2014, Vol. 35 ›› Issue (10): 2119.doi: 10.7503/cjcu20140089

• Organic Chemistry • Previous Articles     Next Articles

Structural Characterization of One Homogeneous Polysaccharide from Echinops latifolius Tausch. and Anti-complementary Activity of Its Sulfated Derivatives

BAO Bin, WANG Huijun, WANG Hongwei, SHI Songshan, WANG Shunchun*()   

  1. Key Laboratory for Standardization of Chinese Medicines, Ministry of Education, Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines of SATCM, Institute of Chinese, Institute of Chinese Materia Medica,Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China
  • Received:2014-01-27 Online:2014-10-10 Published:2014-09-15
  • Contact: WANG Shunchun E-mail:shunchunwang@126.com
  • Supported by:
    Supported by the National Natural Science Foundation of China(No.81373951) and the Key New Drug Creation and Manufacturing Program of China(No.2012ZX09301001-003)

Abstract:

To isolate and characterize the anti-complementary polysaccharide from the root of Echinops latifolius Tausch., bioactivity-guided fractionation and purification was used to obtain the anti-complementary polysaccharide from the hot-water extract of the root of Echinops latifolius Tausch. 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. A homogenous water-soluble polysaccharide(EPS-2A) was obtained from Echinops latifolius Tausch., which average molecular weight was estimated to be 118000. A combination of monosaccharide composition, methylation and configuration analysis, as well as NMR spectroscopy, indicated that EPS-2A was poly-(1-4)-α-D-galactopyranosyluronic acid in which (87.8±0.5)% of uronic acid existed as methylester. Two sulfated derivatives(Sul-2A-1 and Sul-2A-2) from EPS-2A were prepared after sulfation with 1∶1 and 2∶1 of chlorosulfonic acid and pyridine, respectively. The anti-complementary assay showed that Sul-2A-1 and Sul-2A-2 demonstrated a stronger inhibitory effect [CH50=(74.1±4.6) μg/mL for Sul-2A-1; CH50=(35.7±2.8) μg/mL for Sul-2A-2] on the complement activation through the classic pathway, compared to that of heparin [CH50=(103.0±9.0) μg/mL]. The results suggested that the sulfated derivatives Sul-2A-1 and Sul-2A-2 might be promising drug candidates in case of necessary therapeutic complement inhibition.

Key words: Echinops latifolius Tausch., Polysaccharide, Structure analysis, Sulfated derivative, Anti-complement

CLC Number: 

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