5alpha-cardenolides from Kanahia laniflora inhibit ionotropic acetylcholine receptors.
5alpha-cardenolides isolated from Kanahia laniflora are inhibitors of muscle-type nicotinic acetylcholine receptors expressed in TE671 cells with IC (50) values in the range of 27 - 60 microM, as determined by whole-cell patch-clamp electrophysiological experiments.
Clarkson
Cailean
C
Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, Copenhagen, Denmark.
Mellor
Ian R
IR
Lambert
Maja
M
Jaroszewski
Jerzy W
JW
D029062:Apocynaceae; D002298:Cardenolides / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use; D035264:Flowers; D006801:Humans; D020128:Inhibitory Concentration 50; D018733:Nicotinic Antagonists / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D018408:Patch-Clamp Techniques; D008517:Phytotherapy; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D018515:Plant Leaves; D011978:Receptors, Nicotinic / Q000187:drug effects* / Q000378:metabolism
D002298:Cardenolides; D018733:Nicotinic Antagonists; D010936:Plant Extracts; D011978:Receptors, Nicotinic