Lima C C, Criddle D N, Coelho-de-Souza A N, Monte F J, Jaffar M, Leal-Cardoso J H
Departamento de Ciências Fisiológicas, CCS, Universidade Estadual do Ceará, Fortaleza, Brazil.
Planta Med. 2000 Jun;66(5):408-11. doi: 10.1055/s-2000-8594.
The effects of methyleugenol (ME) on guinea-pig isolated ileum were studied. ME reversibly relaxed basal tonus (EC50 of 52.2 +/- 18.3 microM), an action unaltered by 0.5 microM tetrodotoxin or 0.5 mM hexamethonium, and relaxed the ileum pre-contracted with 60 mM KCl. ME slightly hyperpolarized the ileum from -57.3 to -62.8 mV but had no effect in depolarised tissues. ME inhibited contractions induced by ACh, histamine and KCl with IC50 values of approximately 82, 124, and 65 microM, respectively. Our results suggest that ME induces relaxation of guinea-pig ileum by a direct action on smooth muscle via a mechanism largely independent of alterations of membrane potential (Em).
研究了甲基丁香酚(ME)对豚鼠离体回肠的作用。ME可逆性地松弛基础张力(半数有效浓度[EC50]为52.2±18.3微摩尔),0.5微摩尔河豚毒素或0.5毫摩尔六甲铵不改变该作用,且ME可松弛用60毫摩尔氯化钾预收缩的回肠。ME使回肠轻微超极化,从-57.3毫伏变为-62.8毫伏,但对去极化组织无作用。ME抑制由乙酰胆碱、组胺和氯化钾诱导的收缩,其半数抑制浓度[IC50]值分别约为82、124和65微摩尔。我们的结果表明,ME通过主要独立于膜电位(Em)改变的机制直接作用于平滑肌,从而诱导豚鼠回肠松弛。