Calcium channel blocking activity of calycosin, a major active component of Astragali Radix, on rat aorta (original) (raw)

Cardiovascular Pharmacology

Acta Pharmacologica Sinica volume 27, pages 1007–1012 (2006)Cite this article

Abstract

Aim:

To investigate the vasoactivity of calycosin, a major active component of Astragali Radix.

Methods:

Experiments were performed on isolated rat thoracic aortic rings pre-contracted with phenylephrine (PHE) or KCl.

Results:

Calycosin produced a concentration-dependent relaxation on the tissue pre-contracted using PHE with 4.46±0.13 of p_D_2 and 95.85%±2.67% of _E_max; or using KCl with 4.27±0.05 of pD2 and 99.06%±2.15% of _E_max, and displaced downwards the concentration-response curves of aortic rings to PHE or KCl. The relaxant effect of calycosin on denuded endothelium aortic rings was the same as on intact endothelium aortic rings, and its vasorelaxant effect was not influenced by _L_-NAME or indomethacin. In Ca2+-free solution, calycosin (30 μmol/L) did not have an effect on PHE (1 × 10−6 mol/L)-induced aortic ring contraction. The effects of calycosin and nifedipine where somewhat different; calycosin decreased aortic ring contractions induced by the two agonists, but nifedipine displayed a more potent inhibitory effect on KCl-induced contractions than on PHE-induced contractions, and the vascular relaxing effects of calycosin and nifidipine were additive on PHE-induced contraction but not KCl-induced.

Conclusion:

Calycosin is a vasorelaxant. Its action is endothelium-independent and is unrelated to intracellular Ca2+ release. It is a noncompetitive Ca2+ channel blocker. The effect of calycosin on Ca2+ channel blockade may be different from that of dihydropyridines. This study demonstrated a novel pharmacological activity of calycosin, and supplied a theoretic foundation for Astragali Radix application.

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Authors and Affiliations

  1. Department of Molecular and Cellular Pharmacology, School of Pharmaceutical Sciences, Peking University, Beijing, 100083, China
    Xiu-li Wu & Yin-ye Wang
  2. Department of Natural Medicinal Chemistry, School of Pharmaceutical Sciences, Peking University, Beijing, 100083, China
    Jun Cheng & Yu-ying Zhao

Authors

  1. Xiu-li Wu
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  2. Yin-ye Wang
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  3. Jun Cheng
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  4. Yu-ying Zhao
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Corresponding author

Correspondence toYin-ye Wang.

Additional information

Project supported by the National Natural Science Foundation of China (No 30371735).

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Wu, Xl., Wang, Yy., Cheng, J. et al. Calcium channel blocking activity of calycosin, a major active component of Astragali Radix, on rat aorta.Acta Pharmacol Sin 27, 1007–1012 (2006). https://doi.org/10.1111/j.1745-7254.2006.00349.x

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