Extracts from rhizomes of Cyperus articulatus (Cyperaceae) displace [3H]CGP39653 and [3H]glycine binding from cortical membranes and selectively inhibit NMDA receptor-mediated neurotransmission.
The marshland plant Cyperus articulatus (Cyperaceae) is commonly used in traditional medicine in Africa and Latin America to treat a wide variety of human diseases ranging from headache to epilepsy. We tested the hypothesis that the purported anti-epileptic effect of this plant might be due to a functional inhibition of excitatory amino acid receptors. One or several component(s) contained in the extracts inhibited the binding of [3H]CGP39653 to the NMDA recognition site and of [3H]glycine to the strychnine-insensitive glycine site of the NMDA receptor complex from rat neocortex. Water extracts from rhizomes of Cyperus articulatus dose-dependently reduced spontaneous epileptiform discharges and NMDA-induced depolarizations in the rat cortical wedge preparation at concentrations at which AMPA-induced depolarizations were not affected. We conclude that the purported beneficial effects of Cyperus articulatus might at least partially be due to inhibition of NMDA-mediated neurotransmission.
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Sandoz Research Institute Berne Ltd., Switzerland.
Meier
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CL
Urwyler
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Wang
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Herrling
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PL
D015763:2-Amino-5-phosphonovalerate / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D000818:Animals; D000927:Anticonvulsants / Q000378:metabolism / Q000494:pharmacology*; D001667:Binding, Competitive; D002540:Cerebral Cortex / Q000187:drug effects* / Q000502:physiology / Q000648:ultrastructure; D018691:Excitatory Amino Acid Antagonists / Q000378:metabolism* / Q000494:pharmacology; D005998:Glycine / Q000378:metabolism* / Q000494:pharmacology; D008297:Male; D008566:Membranes / Q000187:drug effects / Q000502:physiology / Q000648:ultrastructure; D010879:Piperazines / Q000378:metabolism / Q000494:pharmacology; D010936:Plant Extracts / Q000378:metabolism / Q000494:pharmacology*; D010946:Plants, Medicinal; D051381:Rats; D017207:Rats, Sprague-Dawley; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors* / Q000378:metabolism / Q000502:physiology; D009435:Synaptic Transmission / Q000187:drug effects*; D014316:Tritium
D000927:Anticonvulsants; D018691:Excitatory Amino Acid Antagonists; D010879:Piperazines; D010936:Plant Extracts; D016194:Receptors, N-Methyl-D-Aspartate; D014316:Tritium; C069052:CGP 39653; C065286:SDZ EAA 494; D015763:2-Amino-5-phosphonovalerate; D005998:Glycine