WHO monographs on selected medicinal plants - travolekar.ru
WHO monographs on selected medicinal plants - travolekar.ru WHO monographs on selected medicinal plants - travolekar.ru
Fructus Myrtilli oxidant activity of the berries of various Vaccinium cultivars (including the crude drug) was performed (24). Total antioxidant capacity, measured as oxygen radical absorbance capacity, ranged from 13.9 to 45.9 μmol/g of fresh berries in the extract. Bilberry and the lowbush blueberries from Nova Scotia had the highest antioxidant activity (44.6 and 45.9 μmol/g, respectively). Radical scavenging properties of an extract or tea of the fruit containing anthocyanins was tested on the 1,1-diphenyl-2-picrylhydryl radical using electron spin resonance spectroscopy. Both the extract and the tea were effective 1,1-diphenyl-2-picrylhydryl radical scavengers. No direct correlation was found between the scavenging activity and the content of anthocyanosides and flavonoids in the extract, suggesting that the catechins and ascorbic acid may also play a role (25). Pharmacokinetics Administration to rats of a fruit extract containing anthocyanins, at a dose of 20–40 mg/kg bw (intravenous) or 25.0 mg/kg bw (intraperitoneal) underwent rapid body distribution. Elimination occurred primarily in the urine and bile, following a three-compartment pharmacokinetic model. After 4 hours, 20% of the dose was eliminated in the urine, regardless of route of administration, while at 24 hours, 15% and 18% of the dose was eliminated in the bile after intravenous and intraperitoneal administration, respectively. The anthocyanins possessed a greater affinity for some tissues, namely kidneys (79.0 μg/g tissue) and skin (27.4 μg/g tissue) than for plasma (19.0 μg/g) (26). The pharmacokinetics were assessed after intravenous administration of anthocyanosides (20.0–40.0 mg/kg bw) or oral administration to rats (400.0 mg/kg bw). The results of the intravenous dose were the same as those reported by Lietti and Forni (26). After a single oral administration, the plasma concentrations of anthocyanins reached a peak after 15 minutes and then rapidly declined within 2 hours. The extent of cumulative urinary and biliary elimination, together with the gastrointestinal recovery, demonstrated an absorption rate of approximately 5%. No hepatic first-pass effect was observed. Despite the modest gastrointestinal absorption and the low absolute bioavailability (1.2% of the administered dose), the peak levels in plasma (2.0–3.0 μg/ml) measured after the oral treatment are in the range of biological activity reported for these substances (27). Vascular permeability The anthocyanins contained in the fruit are thought to have “vitamin P” activity in that they increase the levels of intracellular vitamin C and de- 215
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<str<strong>on</strong>g>WHO</str<strong>on</strong>g> <str<strong>on</strong>g>m<strong>on</strong>ographs</str<strong>on</strong>g> <strong>on</strong> <strong>selected</strong> <strong>medicinal</strong> <strong>plants</strong><br />
Pharmacology<br />
Experimental pharmacology<br />
Anti-inflammatory activity<br />
An extract of the f<strong>ru</strong>it c<strong>on</strong>taining 25% anthocyanidins had vasoprotective<br />
and anti-oedema (anti-inflammatory) activities in experimental animals<br />
(21). In rabbits, chloroform-induced skin capillary permeability was reduced<br />
after intraperit<strong>on</strong>eal administrati<strong>on</strong> of the extract at a dose of 25.0–<br />
100.0 mg/kg body weight (bw) or intragastric administrati<strong>on</strong> at a dose of<br />
200.0–400.0 mg/kg bw of anthocyanosides. The anti-inflammatory effect<br />
of the extract lasted l<strong>on</strong>ger than that of the comparis<strong>on</strong> treatments <strong>ru</strong>tin<br />
or mepyramine. Intragastric administrati<strong>on</strong> of the anthocyanins to rats, at<br />
a dose of 25.0 to 100.0 mg/kg bw was effective treatment both in the skin<br />
capillary permeability test and <strong>on</strong> vascular resistance of animals fed a vitamin<br />
P-deficient diet. In both the animal models (rats and rabbits), the<br />
anthocyanins were twice as effective as the flav<strong>on</strong>oid, <strong>ru</strong>tin. Furthermore,<br />
intragastric administrati<strong>on</strong> of the anthocyanins (dose not stated) inhibited<br />
carrageenan-induced paw oedema in rats after intravenous injecti<strong>on</strong> or<br />
topical applicati<strong>on</strong> (21).<br />
Antioxidant activity<br />
An aqueous extract of the f<strong>ru</strong>it inhibited copper-induced oxidati<strong>on</strong> of human<br />
low-density lipoprotein in vitro. Results were obtained by measurement<br />
of oxidative resistance as determined by the lag-phase preceding<br />
c<strong>on</strong>jugated diene formati<strong>on</strong>; quantificati<strong>on</strong> of the amount of lipoperoxides,<br />
as well as thiobarbituric acid-reactive substances generated, and<br />
measurement of the modificati<strong>on</strong> in the net negative electrical charge of<br />
the lipoproteins, over a 7-hour time course experiment. Trace amounts of<br />
the extract, at c<strong>on</strong>centrati<strong>on</strong>s of 15 to 20 μg/ml induced statistically significant<br />
changes in the oxidati<strong>on</strong> behaviour of low-density lipoprotein,<br />
which included: prol<strong>on</strong>gati<strong>on</strong> of the lag-phase of c<strong>on</strong>jugated diene producti<strong>on</strong><br />
(p < 0.01); reducti<strong>on</strong> in the formati<strong>on</strong> of lipoperoxides and of<br />
thiobarbituric acid-reactive substances up to 7 hours and especially between<br />
1 and 5 hours (p < 0.01); and inhibiti<strong>on</strong> of modificati<strong>on</strong> in the net<br />
negative charge of low-density lipoprotein. These results dem<strong>on</strong>strate<br />
that the extract exerts potent protective acti<strong>on</strong> <strong>on</strong> low-density lipoprotein<br />
particles during in vitro copper-mediated oxidati<strong>on</strong> (22). An anthocyanin-c<strong>on</strong>taining<br />
extract of the f<strong>ru</strong>it inhibited lipid peroxidati<strong>on</strong> and hydroxyl<br />
radical formati<strong>on</strong> with a median inhibitory c<strong>on</strong>centrati<strong>on</strong> of<br />
50.3 μg/ml in rat liver microsomes (p < 0.01). The extract also exhibited<br />
superoxide scavenging activity (25.0 μg/ml, p < 0.01) (23). A study to<br />
compare the c<strong>on</strong>centrati<strong>on</strong> of phenolics and anthocyanins and the anti-<br />
214