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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 />

Glycyrrhizin reduces the toxic action of carbon tetrachloride- and galactosamine-induced<br />

cytotoxicity in cultured rat hepatocytes, through its<br />

antioxidant activity (9, 27). Glycyrrhizin inhibited histamine release from<br />

rat mast cells and prevented carbon tetrachloride-induced liver lesions and<br />

macrophage-mediated cytotoxicity (27). Intragastric administration of a<br />

flavonoid fraction isolated from Radix Glycyrrhizae to mice protected<br />

against carbon tetrachloride hepatotoxicity (39). Glycyrrhizin protected<br />

the liver apparently through its membrane stabilization effects (27).<br />

The anti-inflammatory and antiallergic actions of the drug have been<br />

attributed to the corticosteroid-like activity of glycyrrhizin and glycyrrhetic<br />

acid (enoxolone). These compounds act indirectly by potentiating<br />

the activity of corticosteroids. In vitro, glycyrrhetic acid inhibits<br />

Δ 4 β-reductase, an enzyme that competitively inactivates steroid hormones,<br />

and 11β-hydroxysteroid dehydrogenase, the enzyme that deactivates cortisol<br />

(27). Glycyrrhizin given <strong>int</strong>raperitoneally suppressed contact dermatitis<br />

in mice, and was more effective than prednisolone, but no effects<br />

were observed after oral administration (9).<br />

In vitro, the drug inhibits the growth of Bacillus subtilis (40), Mycobacterium<br />

tuberculosis (41), Aspergillus spp. (42), Staphylococcus aureus,<br />

Mycobacterium smegmatis, and Candida albicans (43).<br />

Clinical pharmacology<br />

Oral administration of Radix Glycyrrhizae to 15 patients with peptic ulcer<br />

reduced symptoms and improved healing in 75% of the cases (44).<br />

Glycyrrhetic acid (enoxolone), the active constituent, produced its antiulcer<br />

activity by inhibiting 15-hydroxyprostaglandin dehydrogenase and<br />

Δ 13 -prostaglandin reductase (45). Inhibition of these two enzymes stimulated<br />

an increase in the concentration of prostaglandins E and F 2α<br />

in the<br />

stomach, which promoted the healing of peptic ulcers owing to a cytoprotective<br />

effect on the gastric mucosa (45). Carbenoxolone, a derivative<br />

of glycyrrhetic acid, has been used clinically for years in the treatment of<br />

gastric and duodenal ulcers (46).<br />

Oral administration of deglycyrrhizinated liquorice (380 mg, 3 times<br />

daily) to 169 patients with chronic duodenal ulcers was as effective as<br />

antacid or cimetidine treatments (47). These results indicate that, in addition<br />

to glycyrrhetic acid, other unidentified constituents of Radix Glycyrrhizae<br />

contribute to its antiulcer activity.<br />

Reports on the usefulness of liquorice extracts on body fluid homeostasis<br />

in patients with Addison disease are contradictory. One study found<br />

no positive effects (48), while three other studies noted an increase in<br />

weight gain and sodium retention (49–51).<br />

168

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