[Screening test for calcium antagonist in natural products. The active principles of Uncariae ramulus et uncus].
We have previously reported on the Ca2+-blocking activity and active constituents of natural products. In the course of screening, Uncariae ramulus et uncus, a chinese herbal medicine, was found to possess such activity. In this paper, we attempted to characterize its active constituent which plays an important role in Ca2+-blocking activity. Its active principles were identified to be oxyindole-type alkaloids, rhynchophylline, corynoxeine, isorhynchophylline and isocorynoxeine, that showed inhibitory effects, similar to that of verapamil, on contractile response to high concentration of potassium ion (rats), CaCl2 (rats), norepinephrine in normal and Ca2+-free medium (rats and rabbits) and 45Ca2+-uptake (rats) in thoracic aorta with an activity two orders of magnitude less than the activity of verapamil.
Yamahara
J
J
Kyoto Pharmaceutical University, Japan.
Miki
S
S
Matsuda
H
H
Kobayashi
G
G
Fujimura
H
H
D000470:Alkaloids / Q000302:isolation & purification / Q000494:pharmacology*; D000818:Animals; D002118:Calcium / Q000378:metabolism; D002121:Calcium Channel Blockers / Q000302:isolation & purification / Q000494:pharmacology*; D004365:Drugs, Chinese Herbal / Q000032:analysis*; D026121:Indole Alkaloids; D009119:Muscle Contraction / Q000187:drug effects; D000078183:Oxindoles; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains
D000470:Alkaloids; D002121:Calcium Channel Blockers; D004365:Drugs, Chinese Herbal; D026121:Indole Alkaloids; D000078183:Oxindoles; C054799:corynoxeine; C052714:rhyncophylline; D002118:Calcium