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WHO monographs on selected medicinal plants - travolekar.ru

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Cortex Salicis<br />

Pharmacology<br />

Experimental pharmacology<br />

Anti-inflammatory activity<br />

Similar to salicylates, such as acetylsalicylic acid, extracts of the c<strong>ru</strong>de d<strong>ru</strong>g<br />

are thought to act by inhibiting the activity of cyclooxygenase and thereby<br />

inhibiting the synthesis of prostaglandins, which play a role in inflammati<strong>on</strong>,<br />

fever and pain. Acetylsalicylic acid inhibits the synthesis of prostaglandins<br />

through the acetylati<strong>on</strong> of the enzyme cyclooxygenase. Salicylic<br />

acid, and the salicylates that lack an acetyl group, reduce prostaglandin<br />

synthesis via inhibiti<strong>on</strong> of the activity of cyclooxygenase II (1, 21).<br />

Intragastric administrati<strong>on</strong> of 100.0 mg/kg body weight (bw) of tremulacin,<br />

a c<strong>on</strong>stituent of the bark, significantly inhibited carrageenaninduced<br />

hind paw oedema in rats (p < 0.001) (22). Intragastric administrati<strong>on</strong><br />

of 0.5 ml/kg bw of a 30% ethanol extract of the bark to rats reduced<br />

carrageenan-induced hind paw oedema, but was not effective in the adjuvant-induced<br />

arthritis or dextran-induced pedal oedema models (23).<br />

Antipyretic activity<br />

Intragastric administrati<strong>on</strong> of 0.8 ml/kg bw of a 30% ethanol extract to<br />

rats, suppressed yeast-induced pyrexia (23). The antipyretic effects of<br />

salicin, saligenin (an aglyc<strong>on</strong>e of salicin) and salicylic acid (an active metabolite<br />

of salicin) were assessed in rats (24). After intragastric administrati<strong>on</strong><br />

of salicin to rats, the metabolite salicylic acid appeared slowly in the<br />

plasma and c<strong>on</strong>centrati<strong>on</strong>s increased gradually, in c<strong>on</strong>trast to the rapid<br />

appearance observed after oral administrati<strong>on</strong> of sodium salicylate or saligenin.<br />

At a dose of 5 mM/kg bw, orally administered salicin did not affect<br />

the rectal temperature of afebrile rats while at the same dose, sodium salicylate<br />

and saligenin lowered body temperature significantly. However,<br />

salicin significantly reduced yeast-induced fever (p < 0.01), producing a<br />

normal body temperature, and completely prevented fever when administered<br />

simultaneously with yeast. Salicin did not induce gastric lesi<strong>on</strong>s<br />

even at a dose of 5 mM/kg bw; c<strong>on</strong>versely, sodium salicylate and saligenin<br />

induced severe gastric lesi<strong>on</strong>s in a dose-dependent manner when administered<br />

at doses of 1, 2.5 and 5 mM/kg bw (24).<br />

Pharmacokinetics<br />

The pharmacokinetics of salicin, saligenin (an aglyc<strong>on</strong>e of salicin) and<br />

salicylic acid (an active metabolite of salicin) were determined in rats (24).<br />

Poor absorpti<strong>on</strong> of salicin and rapid absorpti<strong>on</strong> of salicylic acid and saligenin<br />

were c<strong>on</strong>firmed in this animal model. Only small amounts of salicylic<br />

acid and saligenin were detected in the intestinal tracts of rats 1 h<br />

313

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