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The Pharmaceutical Society of Korea (대한약학회)
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Calcium Channel Blocking and $\alpha$-Adrenoceptor Blocking Action of Coptidis Rhizoma Extracts and their Alkaloid Components in Rat Aorta

  • Lee, Dong-Ung (Departemen of Biochemistry, College of Natural Science, Dongguk University) ;
  • Chang, Ki-Churl (Department of Pharmacology and Cardiovascular Research Institute, College of Medicine, Gyeongsang National University)
  • Published : 1996.12.01
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Abstract

Vascular relaxation action of crude extracts of two kinds of Coptidis rhizoma (Coptis chinensis and Coptis japonica, Ranunculaceae) was investigated and compared with that of berberine and palmatine, active alkaloid components of these plants. The results show that total extracts, berberine, and palmatine induced a concentration-dependent vasodilatation of rat thoracic aorta contracted with phenylephrine (PE). Palmatine, unlike to berberine, did not inhibit contraction induced by KCI. In calcium-free media, not only berberine but also crude extracts inhibited calcium-induced contraction. Furthermore, pretreatment of crude extracts inhibited contraction induced by PE noncompetitively. In PE-induced contraction, berberine was 2.5 times more potent than Coptis chinensis in the relaxation of rat aorta in terms of $IC_{50}$ values. Analysis of the effects of crude extracts on the Emax and $IC_{50}(PE)IC_{50}(KCI)$ ratios provides information on selectivity and indicates that extracts exhibit greater inhibition of the contrac tile response induced by PE than by KCI. We concluded that crude extracts have .alpha.-adrenoceptor blocking action and possesses inhibitory effect on calcium influx, which may be at least in part responsible for the antihypertensive action.

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