Antispasmodic and Relaxant Activity of Chelidonine, Protopine, Coptisine, andChelidonium majusExtracts on Isolated Guinea-Pig lleum

Abstract

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(-4) g/ml.

Chelidonium majus L. (Greater celandine) – A Review on its Phytochemical and Therapeutic Perspectives

“…The alkaloids, chelidonine and protopine at concentrations of 1x10 -5 g/ml organ bath were markedly induced the relaxation (68.8% and 54.8%, respectively) of barium-chloride induced guinea-pig ileums contraction [74] . Another study also revealed the significant contribution of coptisine and (+)-caffeoylmalic acid to the total antispasmodic activity of C. majus extract [73] .…”

“…The hydro-alcoholic extract of C. majus and its active constituents were found to induce relaxation of acetylcholine and barium-chloride induced contraction of guinea-pig ileums [73,74] . The alkaloids, chelidonine and protopine at concentrations of 1x10 -5 g/ml organ bath were markedly induced the relaxation (68.8% and 54.8%, respectively) of barium-chloride induced guinea-pig ileums contraction [74] .…”

“…Recently four caffeic acid esters such as 2-(-)-caffeoyl-D-glyceric acid (61), 4-(-)-caffeoyl-Lthreonic acid (62), (+)-caffeoyl-L-malic acid (63) and 2-(-)-caffeoyl-L-threonic acid lactone (64) have been identified [13] . Besides, it contains lesser amount of phytosterols [α-spinasterol (65) (72), tyramine (73), histamine (74) and saponosides [12,[14][15][16] . In addition to these organic compounds, 24 essential macro-and microelements including Al, As, B, Ba, Ca, Cd, Co, Cr, Cu, Fe, Hg, K, Li, Mg, Mn, Mo, Na, Ni, P, Pb, S, Ti, V and Zn have been identified in root and herb.…”

Coptisine from Coptis chinensis inhibits production of inflammatory mediators in lipopolysaccharide-stimulated RAW 264.7 murine macrophage cells

“…This finding suggests that berberine, palmatine and coptisine are the active constituents in C. chinensis responsible for the use of this plant in inflammatory diseases. Coptisine has been found to exhibit antispasmodic (Hiller et al, 1998), anti-fungal ( Kong et al, 2009) and anti-oxidative (Gong et al, 2012) activities, as well as protection of gastric-mucous membranes (Hirano et al, 2001), however, its effect and mechanism for anti-inflammation are still unknown. In the present study, we, for the first time report that coptisine exhibits potent anti-inflammatory effects by inhibition of LPS-stimulated inflammatory mediators production in macrophages.…”

Plant defense responses against viral and bacterial pathogen infections. Focus on RNA-binding proteins (RBPs)

“…In traditional Chinese medicine the plant is used as an antitussive, to treat whooping cough and bronchitis. Greater Celandine is also attributed to have antiviral, anti-microbial, and anti-inflammatory properties [21][22][23]. Alkaloids of C. majus are implied to be responsible for the aforementioned activities and are the major reason of the medicinal and pharmaceutical interest in this plant [24].…”