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Antispasmodic and relaxant activity of chelidonine, protopine, coptisine, and Chelidonium majus extracts on isolated guinea-pig ileum

Two ethanolic dry extracts from the herb Chelidonium majus L. with a defined content of the main alkaloids (chelidonine, protopine, and coptisisine) and the alkaloids themselves were studied in three different antispasmodic test models on isolated ileum of guinea-pigs. In the BaCl2- stimulated ileum, chelidonine and protopine exhibited the known papaverine- like musculotropic action, whereas coptisine (up to 3.0 x 10-5 g/ml) was ineffective in this model. Both extracts were active with 53.5% and 49.0% relaxation at 5 x 10-4 g/ml. The carbachol and the electric field stimulated contractions were antagonized by all three alkaloids. Coptisine showed competitive antagonist behaviour with a pA2 value of 5.95. Chelidonine and protopine exhibited a certain degree of non-competitive antagonism. In the electric field the antagonist activities decreased in the order protopine > coptisine > chelidonine. The concentrations of the chelidonium herb extracts for 50% inhibition of the carbachol and electrical field induced spasms were in the range of 2.5 to 5 x 10-4g/ml.

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Reference£º
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem