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NIS - libdoc.who.int - World Health Organization

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Folium cum Flore Crataegi<br />

tract (containing 18.75% oligomeric procyanidins) displaced 3 H-ouabain<br />

bound to sodium- and potassium-activated adenosine triphosphatase (39).<br />

Anticontractile effects<br />

An aqueous extract of the flowers inhibited barium chloride-induced contractions<br />

in rabbit <strong>int</strong>estine in vitro (78). A flavonoid-enriched extract of<br />

the leaves with flowers inhibited both histamine- and nicotine-induced<br />

contractions in rabbit <strong>int</strong>estine in vitro and partially inhibited contractions<br />

induced by barium chloride, acetylcholine or serotonin (ED 50<br />

0.02 mg/ml)<br />

(52). Intravenous administration of a flavonoid-enriched extract of the<br />

leaves with flowers to cats (20 mg/kg body weight) inhibited contractions<br />

in <strong>int</strong>estinal smooth muscle, and <strong>int</strong>raperitoneal injection (400 mg/kg<br />

body weight) inhibited acetic acid-induced writhing in mice (52).<br />

Sedative effects<br />

Sedative effects have been observed in various animal models after <strong>int</strong>ragastric<br />

administration of leaf with flower extracts (79, 80). A 60% ethanol<br />

extract of the flowers increased hexobarbital-induced sleeping times, and<br />

decreased spontaneous motility and exploratory behaviour in female mice<br />

(800 mg/kg body weight) (80).<br />

Diuretic effects<br />

A flavonoid-enriched fraction of a flower extract had diuretic activity in<br />

dogs (50 mg/kg body weight) (81).<br />

Toxicology<br />

Single-dose toxicity studies have demonstrated that rats and mice tolerate<br />

3 g/kg body weight, by gastric lavage, of a standardized hydroalcoholic<br />

extract of the leaves with flowers (containing 18.75% oligomeric procyanidins)<br />

without any clinical symptoms of toxicity. The <strong>int</strong>raperitoneal<br />

median lethal dose (LD 50<br />

) was 1.17 g/kg body weight in rats and 750 mg/<br />

kg body weight in mice. No toxic effects were observed in a repeat-dose<br />

toxicity study in which rats and dogs were given a standardized extract<br />

(containing 18.75% oligomeric procyanidins) at doses of 30, 90 and<br />

300 mg/kg body weight daily by the <strong>int</strong>ragastric route for 26 weeks (82).<br />

Clinical pharmacology<br />

Cardiac insufficiency<br />

Review of the pharmacological and clinical data indicates that standardized<br />

extracts of Folium cum Flore Crataegi increase myocardial performance,<br />

improve myocardial circulatory perfusion and tolerance in cases of<br />

101

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