Some Observations on the Cardiovascular Effects of 9-Substituted Berberines

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A comparative study of the effect of berberine and its 9-substituted compounds (I, R=OH ; II, berberine, R=OCH3 ; III, R=OC4H9 ; IV, R=OC5H11 ; V, R=OC8H17 ; VI, R=OC12H25) on blood pressure of rats showed that substitution of OC4H9 or OC5H11 for OCH3 of berberine prolonged the transient hypotensive activity of berberine, whereas substitution by OH caused a slight hypertension. The dose of III or IV, which caused hypotension, was found to inhibit cardiac function in rats, whereas II had no effect on it. II, III, and IV decreased the beating rate in isolated perfused toad heart. Only II was found to have acetylcholine-potentiating action in frog muscle as well as guinea-pig small intestine in vitro. In the same preparations III and IV, contrariwise, inhibited acetylcholine action. In spinal rats, any response in blood pressure was not observed after the injection of each of the test compounds. From these results, possible mechanism of action of the test compounds is discussed.

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