In vitro antispasmodic compounds of the dry extract obtained from Hedera helix.
Commercial dry extract of Hedera helix L. is used for the treatment of disorders of the respiratory tract; it is standardized towards papaverine (papaverine equivalent value, PE, activity of 1 g test substance equivalent to the activity of x mg papaverine) by in vitro antispasmodic activity on isolated guinea-pig ileum with acetylcholine as spasmogen. In order to determine the phytochemical basis for the antispasmodic activity, bioassay guided fractionation and subsequent isolation of phenolic compounds (flavonols, caffeoylquinic acids) and saponins (hederacoside C, alpha-hederin, hederagenin) was carried out. Fractions and isolates obtained were investigated for antispasmodic activity and their contribution to the activity of the extract was calculated. Significant activity was found for both saponins and phenolic compounds, the PE values being approx. 55 and 49 for alpha-hederin and hederagenin, 54 and 143 for quercetin and kaempferol, and 22 for 3,5-dicaffeoylquinic acid, respectively. In view of their relative high concentration the saponins contribute most to the anti-spasmodic activity, followed by dicaffeoylquinic acids and the flavonol derivatives. The results indicate that the summed PE value of the compounds mentioned is an acceptable agreement with the PE value of the whole extract determined biologically.
Trute
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A
Institut für Pharmazeutische Biologie und Phytochemie, Westf, Wilhelms-Universität, Münster, Germany.
Gross
J
J
Mutschler
E
E
Nahrstedt
A
A
D000818:Animals; D005260:Female; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects / Q000503:physiopathology; D066298:In Vitro Techniques; D008297:Male; D010276:Parasympatholytics / Q000494:pharmacology*; D010936:Plant Extracts / Q000494:pharmacology*; D010946:Plants, Medicinal / Q000737:chemistry*
D010276:Parasympatholytics; D010936:Plant Extracts