Commercial dry extract of Hedera helix L., is used for the treatment o
f disorders of the respiratory tract; it is standardized towards papav
erine (papaverine equivalent value, PE, activity of 1 g test substance
equivalent to the activity of x mg papaverine) by in vitro antispasmo
dic activity on isolated guinea-pig ileum with acetylcholine as spasmo
gen. In order to determine the phytochemical basis for the antispasmod
ic activity, bioassay guided fractionation and subsequent isolation of
phenolic compounds (flavonols, caffeoylquinic acids) and saponins (he
deracoside C, alpha-hederin, hederagenin) was carried out. Fractions a
nd isolates obtained were investigated for antispasmodic activity and
their contribution to the activity of the extract was calculated. Sign
ificant activity was found for both saponins and phenolic compounds, t
he PE values being approx. 55 and 49 for alpha-hederin and hederagenin
, 54 and 143 for quercetin and kaempferol, and 22 for 3,5-dicaffeoylqu
inic acid, respectively. In view of their relative high concentration
the saponins contribute most to the antispasmodic activity, followed b
y dicaffeoylquinic acids and the flavonol derivatives. The results ind
icate that the summed PE value of the compounds mentioned is an accept
able agreement with the PE value of the whole extract determined biolo
gically.