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Investigation on the Interaction of Palmatine and Jatrorrhizine with β2-Adrenoceptor by High-performance Affinity Chromatography

  • HE Yuan ,
  • YAO Su-Yang ,
  • ZHENG Xiao-Hui ,
  • WEI Yin-Mao
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  • a Key Laboratory of Synthetic and Natural Function Molecule Chemistry of Ministry of Education, College of Chemistry & Material Science, Northwest University, Xi'an 710069;
    b College of Life Sciences, Northwest University, Xi'an 710069

Received date: 2011-09-14

  Revised date: 2011-11-20

  Online published: 2012-02-25

Supported by

Project supported by the National Natural Science Foundation of China (Nos.20975080 and 20875074);Program for New Century Excellent Talents in University (No.NCET-08-0892) and Chinese National Science Foundation for Talent Training (No.J0830417).

Abstract

The interaction of two bioactive components of Chinese traditional herb, palmatine (Pa) and jatrorrhizine (Ja), with β2-adrenoceptor (β2-AR) was investigated by high-performance affinity chromatography. The binding isotherms of two drugs were determined by frontal analysis, and the results showed that Pa had one kind of binding site, and Ja had two kinds of binding sites on β2-AR molecular. The association constants and binding sites were determined by zonal elution, at pH 7.4 and 25 ℃. The association constant for Pa was 2.93×104 L·mol-1, and the concentration of the binding sites was 1.13×10-4 mol·L-1. The association constants for Ja at the low and high binding sites were 1.93×104 and 1.56×105 L·mol-1, and the concentration of the two binding sites were 1.25×10-4 and 1.00×10-5 mol·L-1, respectively. The ratio of two binding sites was 93:7. It was further proved that Pa and Ja competed the low binding site on β2-AR. Thermodynamic results indicated that the interaction between the two drugs and β2-AR was mainly drived by electrostatic force.

Cite this article

HE Yuan , YAO Su-Yang , ZHENG Xiao-Hui , WEI Yin-Mao . Investigation on the Interaction of Palmatine and Jatrorrhizine with β2-Adrenoceptor by High-performance Affinity Chromatography[J]. Acta Chimica Sinica, 2012 , 70(02) : 121 -127 . DOI: 10.6023/A1109141

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