Pharmacological effects of Eugenia punicifolia (Myrtaceae) in cholinergic nicotinic neurotransmission.
The effects of the aqueous crude extract (5%) of Eugenia punicifolia on cholinergic nicotinic neurotransmission were investigated. Actions of aqueous crude extract over the inhibitory effect of the cholinergic nicotinic antagonists gallamine or pancuronium, on contractions induced by electrical stimulation of phrenic nerve of rat diaphragm, were studied. Tissues were mounted as for isotonic contractions and stimulation was delivered at submaximal voltage. Addition of Eugenia punicifolia did not alter the amplitude of twitch contraction. Gallamine (IC(50): 28.8+/-0.51 microM) or pancuronium (IC(50): 3.16+/-0.11 microM) completely inhibited twitch contractions. After the maximum effect of the antagonists was achieved, addition of the aqueous crude extract (0.5-1.0 mL) totally recovered the responses to electrical stimulation. Neostigmine, a reversible acethylcholinesterase inhibitor, partially recovered responses (49.70+/-6.90% at 1 microM). In another series of experiments, previous incubation of the extract (0.5 mL) shifted to the right inhibitory concentration-response curves for the antagonists gallamine (IC(50) before E. punicifolia: 35.8+/-1.61 microM; IC(50), after E. punicifolia: 2.24+/-0.04 mM) and pancuronium (IC(50), before E. punicifolia: 3.55+/-0.13 microM; IC(50), after E. punicifolia: 0.39+/-0.01 mM). Our results show that the aqueous extract of E. punicifolia recovered the action of competitive nicotinic antagonists at the neuromuscular junction. A receptor-mediated mechanism or the possibilities of interactions of the extract with the enzyme acethylcholinesterase, however, remain to be investigated.
Grangeiro
Marcielli Silva
MS
Departamento de Ciências Fisiológicas, ICB, UFAM, Manaus, AM, Brasil.
Calheiros-Lima
Ana Paula
AP
Martins
Manoel Francisco
MF
Arruda
Luis Frederico
LF
Garcez-do-Carmo
Lúcia
L
Santos
Wilson C
WC
D000818:Animals; D018678:Cholinergic Agents / Q000737:chemistry / Q000494:pharmacology*; D008297:Male; D009469:Neuromuscular Junction / Q000187:drug effects; D018515:Plant Leaves / Q000737:chemistry; D028321:Plant Preparations / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D011978:Receptors, Nicotinic / Q000378:metabolism*; D009435:Synaptic Transmission / Q000187:drug effects* / Q000502:physiology; D027842:Syzygium / Q000737:chemistry*
D018678:Cholinergic Agents; D028321:Plant Preparations; D011978:Receptors, Nicotinic