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Blocking action of berberine on various receptors in rat anococcygeus muscle

Die blockierende Wirkung von Berberin auf verschiedene Rezeptoren im M. anococcygeus der Ratte

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Summary

The contractile responses of rat anococcygeus muscle to phenylephrine, acetylcholine and 5-hydroxytryptamine in relation to berberine and to their specific antagonists were studied separately.

The effects of phenylephrine and acetylcholine were blocked by berberine as well as by atropine. But the α-blocking action of atropine was exhibited only at high concentration.

The anococcygeus muscle response to phenylephrine was competitively inhibited by berberine with a PA2 value of 6.4. The contraction induced by acetylcholine was competitively inhibited by atropine (PA2=8.7), whereas berberine, which differs basically from atropine, shifted the dose-response curve for acetylcholine non-parallelly to the right with its maximal response reduced concomitantly. Its pD2 value was 4.6. This suggests that the antagonistic action of berberine may be exerted non-specifically through a site beyond the M-cholinergic receptor.

Berberine also relaxed the contraction of anococcygeus muscle induced by 5-hydroxytryptamine.

The contractile responses to histamine and isoprenaline were seen only at high concentration. In addition, the response to isoprenaline was little affected by propranolol in our experiment.

Zusammenfassung

Die kontraktile Antwort des M. anococcygeus der Ratte auf Phenylephrin, Azetylcholin und 5-Hydroxytryptamin bei gleichzeitiger Anwendung von Berberin und von deren spezifischen Antagonisten wurde getrennt untersucht.

Die Wirkung von Phenylephrin und von Azetylcholin wurde durch Berberin bzw. Atropin blockiert, jedoch zeigte sich die α-blockierende Wirkung von Atropin nur bei hoher Konzentration.

Die Reaktion des M. anococcygeus auf Phenylephrin wurde durch Berberin kompetitiv gehemmt (pA2 = 6.4); die durch Azetylcholin induzierte Kontraktion wurde durch Atropin kompetittv gehemmt (pA2 = 8.7). Berberin, das sich grundsätzlich von Atropin unterscheidet, verschob die Dosiswirkungskurve für Azetylcholin nichtparallel nach rechts mit gleichzeitiger Reduktion der maximalen Reizantwort (pD1,-wert = 4.6). Das läßt darauf schließen, daß die antagonistische Wirkung von Berberin unspezifisch auf eine Stelle außerhalb des M-cholinergen Rezeptors ausgeübt wird.

Auf Berberin ließ auch die durch 5-Hydroxytryptamin induzierte Kontraktion des M. anococcygeus nach.

Kontraktile Antworten auf Histarnin und Isoprenalin wurden nur bei hohen Konzentrationen beobachtet. Die Wirkung von Isoprenalin wurde in unserem Experiment durch Propianolol nur wenig beeinträchtigt.

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Authors and Affiliations

  1. Department of Pharmacology, Tongji Medical University, Wuhan

    Yao Wei-xing, Fang Da-chao, Xia Guo-jin & Jiang Ming-xing

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  1. Yao Wei-xing
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  2. Fang Da-chao
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  3. Xia Guo-jin
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  4. Jiang Ming-xing
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Wei-xing, Y., Da-chao, F., Guo-jin, X. et al. Blocking action of berberine on various receptors in rat anococcygeus muscle. Journal of Tongji Medical University 9, 86–90 (1989). https://doi.org/10.1007/BF02908932

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