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Herba Chelidonii
Intragastric administration of 12.5, 62.5 and 125 mg/kg body weight (bw)
of the extract twice weekly over 3 weeks resulted in a reduction in CCl 4
-
induced hepatotoxicity. Increased plasma activities of the enzymes alanine
aminotransferase, aspartate aminotransferase, alkaline phosphatase
and lactate dehydrogenase, as well as the increased bilirubin level, induced
by CCl 4
, were significantly decreased by the extract. The liver tissue appeared
free from fibrosis, and cholesterol, which first decreased as a result
of treatment with CCl 4
, significantly increased during the treatment with
the extract. Histopathological evaluation of the liver cells indicated a
marked reduction in the number of necrotic cells (61). However, it is difficult
to evaluate the clinical significance of these findings with regard to
hepatotoxic adverse reactions (see Adverse reactions).
Anti-inflammatory activity
An extract made from a tincture of crude drug, as well as the individual
alkaloids chelidonine, berberine, chelerythrine and sanguinarine, were
tested in an anti-inflammatory enzyme assay in vitro to determine their
ability to inhibit 5- and 12-lipoxygenases (5-LOX and 12-LOX), two enzymes
in the inflammatory cascade. The two most active inhibitors of
both enzymes were the quaternary alkaloids, sanguinarine (median inhibitory
concentration (IC 50
) = 0.4 µM for 5-LOX and 13 µM for 12-LOX)
and chelerythrine (IC 50
= 0.8 µM for 5-LOX and 33 µM for 12-LOX).
Chelidonine and berberine were inactive. An extract containing 0.68% total
alkaloids, calculated as chelidonine inhibited 5-LOX activity with an
IC 50
of 1.9 µM (based on the molecular weight of chelidonine) (62).
Antispasmodic activity
The effects of two dry ethanol extracts of the herb with a defined content of
the main alkaloids (chelidonine, protopine and coptisine), and the alkaloids
themselves were assessed in three different antispasmodic tests using ileum
isolated from guinea-pigs. When ileal contractions were stimulated by barium
chloride, both extracts reduced contractions, the more concentrated
extract by 53.5% and the less concentrated by 49%, when added to the bath
media at a concentration of 500 µg/ml. In addition, both chelidonine and
protopine exhibited papaverine-like musculotropic action, whereas coptisine
(in concentrations of up to 30 µg/ml) was ineffective in this model.
Both carbachol and electrical-field-stimulated contractions were also reduced
by all three alkaloids. The IC 50
of the crude drug extracts in carbachol-
and electrical-field-induced ileal spasms were in the range of 250–
500 µg/ml (63). An aqueous-ethanol extract of the herb containing 0.81%
total alkaloids, calculated as coptisine, as well as the individual compounds,
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