We investigated the effects of four ginseng saponins, ginsenoside-Rb-1, -Rg
(2), -Rg(3) and -Ro, on the responses induced by receptor stimulation of va
rious stimuli. Ginsenoside-Rg(2) (1-100 mu M) reduced the secretions of cat
echolamines from bovine adrenal chromaffin cells stimulated by acetylcholin
e and gamma-aminobutyric acid but not by angiotensin II, bradykinin, histam
ine and neurotensin. In guinea-pig, the ginsenoside also diminished the nic
otine-induced secretion of catecholamines from the adrenal chromaffin cells
, but it did not affect the muscarine- and the histamine-induced ileum cont
ractions. On the other hand, ginsenoside-Rg(3) (1-100 mu M) reduced not onl
y the acetylcholine-, the gamma-aminobutyric acid- and the neurotensin-indu
ced secretions but also, at a higher concentration (100 mu M), the angioten
sin II-, the bradykinin- and the histamine-induced secretions from the bovi
ne chromaffin cells. Furthermore, the saponin (3-100 mu M) significantly in
hibited the muscarine- and the histamine-induced ileum contractions of the
guinea-pig. Ginsenoside-Rb-1 and -Ro had no marked effect on their response
s. These results strongly suggest that ginsenoside-ag, is a potent selectiv
e blocker of nicotinic acetylcholine and gamma-aminobutyric acid receptors
(ionotropic receptors) and ginsenoside-Rg3 is not only a blocker of ionotro
pic receptors but also an antagonist of muscarinic or histamine receptors.
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