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WHO monographs on selected medicinal plants - travolekar.ru

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Cortex Berberidis<br />

and Trichom<strong>on</strong>as vaginalis and induced morphological changes in the<br />

parasites (49).<br />

Cardiovascular effects<br />

Berberine has been reported to have protective effects against cardiac arrhythmias<br />

and severe c<strong>on</strong>gestive heart failure (50–52). This physiological<br />

effect is due to the ability of berberine to prol<strong>on</strong>g acti<strong>on</strong> potential durati<strong>on</strong><br />

and inhibit the inward rectifier potassium current and outward delayed<br />

rectifier potassium current (50–100 μM). Berberine has also been<br />

shown to inhibit the human ether-a-go-go-related channel expressi<strong>on</strong> in<br />

Xenopus oocytes (median effective dose was 95 μM). In rats, Langendorff<br />

perfusi<strong>on</strong> of an isolated heart was performed using verapamil to bring<br />

about acute heart failure. Treatment of the heart with berberine (10 μmol/l)<br />

before the use of verapamil significantly reduced the degree of heart failure<br />

as compared with the c<strong>on</strong>trol group (p < 0.001) (52).<br />

Effects <strong>on</strong> smooth muscle<br />

Berberine, at a c<strong>on</strong>centrati<strong>on</strong> of 1 μM, relaxed norepinephrine-prec<strong>on</strong>tracted<br />

isolated rat aorta strips (53). Berberine induced relaxati<strong>on</strong> in isolated<br />

prec<strong>on</strong>tracted rat mesenteric arteries at a c<strong>on</strong>centrati<strong>on</strong> of 10 -5 M<br />

(54, 55). At a c<strong>on</strong>centrati<strong>on</strong> of 0.1–100 μM, berberine suppressed basal<br />

t<strong>on</strong>e and induced a c<strong>on</strong>centrati<strong>on</strong>-dependent relaxati<strong>on</strong> of phenylephrine-prec<strong>on</strong>tracted<br />

rabbit corpus cavernosum in vitro (56). Intracavernous<br />

injecti<strong>on</strong> of berberine to anaesthetized rabbits at a dose of 5.0 mg/kg<br />

increased intracavernosal pressure from 12.7 to 63.4 mmHg, and the durati<strong>on</strong><br />

of tumescence ranged from 11.5 to 43.7 minutes (56). Berberine<br />

inhibited norepinephrine and phenylephrine-induced c<strong>on</strong>tracti<strong>on</strong>s in<br />

prostate strips isolated from rabbit (57).<br />

The effects and mechanism of berberine <strong>on</strong> the intracellular free calcium<br />

c<strong>on</strong>centrati<strong>on</strong> in the smooth muscle cells of guinea-pig col<strong>on</strong> were<br />

assessed in vitro using bi-wavelength spectrophotometry in suspensi<strong>on</strong>s<br />

of these cells. In the resting state, berberine had no significant effects <strong>on</strong><br />

free calcium c<strong>on</strong>centrati<strong>on</strong>, but inhibited the increase in free calcium levels<br />

induced by 60 mm potassium chloride in a c<strong>on</strong>centrati<strong>on</strong>-dependent<br />

manner. The median inhibitory c<strong>on</strong>centrati<strong>on</strong> was 34.09 μM. At c<strong>on</strong>centrati<strong>on</strong>s<br />

of 30 and 100 μM, berberine inhibited the elevati<strong>on</strong> of free calcium<br />

evoked by 10 μM of acetylcholine in the presence or absence of extracellular<br />

calcium. These data suggest that berberine inhibits the influx of<br />

extracellular calcium and calcium release from intracellular stores in the<br />

smooth muscle cells of col<strong>on</strong>, indicating that berberine may be a calcium<br />

channel blocker (58).<br />

37

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