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WHO monographs on selected medicinal plants - travolekar.ru

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Ramulus cum Uncis Uncariae<br />

ti<strong>on</strong>s of the pure compounds and thus the applicability of these data to<br />

the c<strong>ru</strong>de d<strong>ru</strong>g and its preparati<strong>on</strong>s needs to be further investigated.<br />

Antiarrhythmic activity<br />

The effect of hirsutine, an indole alkaloid isolated from the c<strong>ru</strong>de d<strong>ru</strong>g, <strong>on</strong><br />

membrane potentials of rabbit sino-atrial node and guinea-pig right ventricle<br />

and left atrium was investigated. Hirsutine at c<strong>on</strong>centrati<strong>on</strong>s of<br />

0.1–30.0 μM decreased the maximum rate of rise and prol<strong>on</strong>ged acti<strong>on</strong><br />

potential durati<strong>on</strong> in sino-atrial node in vitro, as well as in atrial and ventricular<br />

preparati<strong>on</strong>s (18). Hirsutine, in c<strong>on</strong>centrati<strong>on</strong>s of 1.0–3.0 μM produced<br />

a dose-dependent relaxati<strong>on</strong> of the isolated rat aorta prec<strong>on</strong>tracted<br />

with either norepinephrine or potassium chloride soluti<strong>on</strong>, suggesting<br />

that the compound dilated blood vessels through the inhibiti<strong>on</strong> of voltage-dependent<br />

calcium channels (19). The compound, at a c<strong>on</strong>centrati<strong>on</strong><br />

of 30 μM, also decreased intracellular calcium c<strong>on</strong>centrati<strong>on</strong>s in isolated<br />

vascular smooth muscle cells through the inhibiti<strong>on</strong> of norepinephrineinduced<br />

calcium influx (20).<br />

Antic<strong>on</strong>vulsant activity<br />

Intragastric administrati<strong>on</strong> of a methanol extract of the c<strong>ru</strong>de d<strong>ru</strong>g to rats<br />

at a dose of 1.0 g/kg body weight (bw) inhibited kainic acid-induced epileptic<br />

seizures and reduced the levels of free radicals, as measured by lipid<br />

peroxidati<strong>on</strong> in the brain (21).<br />

Intraperit<strong>on</strong>eal administrati<strong>on</strong> of an ethyl acetate or methanol extract<br />

of the c<strong>ru</strong>de d<strong>ru</strong>g to mice at a dose of 70.0 mg/kg bw inhibited pentetrazole-induced<br />

c<strong>on</strong>vulsi<strong>on</strong>s (22). Hyperin, a chemical c<strong>on</strong>stituent isolated<br />

from the extract, decreased the elevated activities of -aminobutyric<br />

acid-T, xanthine oxidase and lipid peroxide induced by pentetrazole<br />

in mouse brain tissue in vitro at a c<strong>on</strong>centrati<strong>on</strong> of 25.0 mg/ml (23).<br />

Intragastric administrati<strong>on</strong> of an aqueous extract of the c<strong>ru</strong>de d<strong>ru</strong>g to<br />

mice, at a dose of 1.0–3.0 g/kg bw, inhibited glutamate-induced c<strong>on</strong>vulsi<strong>on</strong>s,<br />

but had no effect <strong>on</strong> c<strong>on</strong>vulsi<strong>on</strong>s induced by picrotoxin, strychnine<br />

or electroshock (24). The active c<strong>on</strong>stituents of the c<strong>ru</strong>de d<strong>ru</strong>g were isolated<br />

and identified as indole alkaloids, geissoschizine methyl ether and<br />

hirsutine. Intragastric administrati<strong>on</strong> of the alkaloids to mice at a dose of<br />

100.0 mg/kg bw also inhibited glutamate-induced c<strong>on</strong>vulsi<strong>on</strong>s in a dosedependent<br />

manner (24).<br />

An aqueous extract of the c<strong>ru</strong>de d<strong>ru</strong>g at a c<strong>on</strong>centrati<strong>on</strong> of 0.1 mg/ml<br />

prevented glutamate-induced neur<strong>on</strong>al death in cultured rat cerebellar<br />

granule cells through the inhibiti<strong>on</strong> of calcium influx into the cells (25). In<br />

cultured mouse cerebral neur<strong>on</strong>s, glucose oxidase-induced toxicity was reduced<br />

after treatment of the cells with 100 g/ml of the c<strong>ru</strong>de d<strong>ru</strong>g (26).<br />

357

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