Na+,K(+)-ATPase inhibiting activity of cardiac glycosides from Erysimum cheiranthoides.
We previously reported the isolation of eleven new cardiac glycosides called cheiranthosides I-XI together with two known ones (olitoriside and erysimoside) from the seeds of Erysimum cheiranthoides L. The glycosides were evaluated for their inhibitory activity against Na+,K(+)-ATPase by comparing with typical cardiac glycosides. Two of them, cheiranthoside III and VIII, showed high inhibiting activity which was equivalent to that of digitoxin. Cheiranthoside XI containing a rhamnopyranosyl digitoxopyranosyl moiety and a carboxyl group showed the lowest activity which was similar to that of the inactive aglycone, strophanthidin. Some characteristics in the structure-activity relationship are also discussed.
Lei
Z H
ZH
Kuniyasu
A
A
Tai
B S
BS
Nakayama
H
H
Nohara
T
T
D000818:Animals; D019607:Brassicaceae / Q000737:chemistry*; D002301:Cardiac Glycosides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D002316:Cardiotonic Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D002540:Cerebral Cortex / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D017506:H(+)-K(+)-Exchanging ATPase / Q000378:metabolism; D008516:Medicine, Chinese Traditional; D015394:Molecular Structure; D008517:Phytotherapy; D010946:Plants, Medicinal / Q000737:chemistry*; D054328:Proton Pump Inhibitors; D012639:Seeds / Q000737:chemistry*; D013329:Structure-Activity Relationship; D013552:Swine
D002301:Cardiac Glycosides; D002316:Cardiotonic Agents; D004365:Drugs, Chinese Herbal; D004791:Enzyme Inhibitors; D054328:Proton Pump Inhibitors; D017506:H(+)-K(+)-Exchanging ATPase