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NIS - libdoc.who.int - World Health Organization

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WHO monographs on medicinal plants commonly used in the Newly Independent States (<strong>NIS</strong>)<br />

leaves with flowers (equivalent to 6 mg of procyanidins/kg body weight)<br />

to anaesthetized normotensive dogs decreased norepinephrine-induced elevation<br />

of blood pressure. The extract (equivalent to 0.03 mg procyanidins/ml)<br />

also had β-blocking activity and inhibited epinephrine-induced<br />

tachycardia in isolated frog hearts (69). Hyperoside, isolated from an extract<br />

of the leaves and flowers, administered either <strong>int</strong>ravenously at a dose<br />

of 1 mg/kg body weight or by infusion at 0.1 mg/kg body weight/min for<br />

30 min, decreased blood pressure in anaesthetized dogs (68). Intravenous<br />

administration of an aqueous extract of the leaves (average dose 31 mg/kg<br />

body weight) decreased the systolic, diastolic and mean blood pressure in<br />

normotensive anaesthetized rats (66). Acute or chronic <strong>int</strong>ragastric administration<br />

of a fluidextract or a glycerol/ethanol extract reduced arterial<br />

blood pressure in normotensive rats and in rats with desoxycorticosterone<br />

acetate-induced hypertension (50). Intragastric administration of a standardized<br />

extract (300 mg/kg body weight daily) decreased blood pressure<br />

by 9 mm Hg (1.20 kPa) (67). Intravenous administration of a standardized<br />

extract (containing 18.75% oligomeric procyanidins) to anaesthetized rats<br />

(30 mg/kg body weight) or dogs (15 mg/kg body weight) decreased total<br />

peripheral resistance and arterial blood pressure (54).<br />

Anti-inflammatory effects<br />

Both free radical production and lipid peroxidation are involved in various<br />

pathological processes, including cardiac ischaemia. As determined<br />

by in vitro studies, Folium cum Flore Crataegi has free radical scavenging<br />

and antioxidant activities. A standardized extract (containing 18.75%<br />

oligomeric procyanidins) and an oligomeric procyanidin-fraction of the<br />

extract inhibited lipid peroxidation (IC 50<br />

0.48 µg/ml (extract), 0.3 µg/ml<br />

(fraction)), and the activity of human neutrophil elastase (IC 50<br />

4.75 µg/ml<br />

(extract), 0.84 µg/ml (fraction)) (56). A 70% methanol extract of the flower<br />

buds inhibited lipid peroxidation in rat liver microsomes (IC 50<br />

23 µg/l)<br />

(70, 71). Both phenolic and flavonoid-enriched fractions of extracts of the<br />

leaves and flowers had antioxidant activity in vitro (70–72).<br />

Effect on signal transduction<br />

An aqueous or methanol extract of the leaves with flowers, as well as hyperoside,<br />

vitexin and vitexin rhamnoside, inhibited the activity of cyclic AMPdependent<br />

phosphodiesterase isolated from guinea-pig or rat heart (73, 74).<br />

Both luteolin 7-glucoside and rutin were also active (75). Hydroalcoholic<br />

extracts of the flowers and flower heads inhibited the formation of thromboxane<br />

A 2<br />

and prostaglandin I 2<br />

in rabbit cardiac tissues in vitro, thus indicating<br />

an anti-inflammatory effect of the extracts (76, 77). A standardized ex-<br />

100

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