Inhibitory effect of the norlignan 2-(2'-hydroxy-4',6'-dimethoxyphenyl)-5-[(E)-propenyl]benzofuran from Krameria tomentosa on acetylcholine-induced relaxation of the rat aorta.
In this work, we studied the effect of the norlignan 2-(2'-hydroxy-4',6'-dimethoxyphenyl)-5-[( E)-propenyl]benzofuran (DMPP) in the rat aorta. In aortic rings with intact endothelium, DMPP inhibited in a concentration-dependent manner the vasodilator effect produced by acetylcholine with an IC50 value of 31.2+/-6.3 microM. DMPP also inhibited basal nitric oxide production. In endothelium-denuded vessels DMPP was without effect whereas superoxide dismutase (SOD) was effective in potentiating responses to the NO donor SIN-1. Contractile effects of carbachol in guinea-pig ileum and trachea were unaffected by DMPP. It is concluded that DMPP inhibits the endothelium-dependent relaxation induced by acetylcholine in the rat aorta without affecting receptor or smooth muscle cells function. Decreased nitric oxide production by endothelial cells seems to be the mechanism involved in the inhibitory effect of DMPP.
Castro
Janiza C
JC
Laboratório de Tecnologia Farmacêutica, Universidade Federal da Paraíba, João Pessoa, PB, Brazil.
Silva
Marcelo S
MS
Cortes
Steyner F
SF
Lemos
Virgínia S
VS
D000109:Acetylcholine; D000818:Animals; D001011:Aorta / Q000187:drug effects*; D001572:Benzofurans / Q000494:pharmacology*; D002217:Carbachol / Q000494:pharmacology; D004727:Endothelium / Q000187:drug effects; D005260:Female; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D020128:Inhibitory Concentration 50; D031326:Krameriaceae / Q000737:chemistry*; D017705:Lignans / Q000494:pharmacology*; D008297:Male; D015394:Molecular Structure; D009119:Muscle Contraction / Q000187:drug effects; D009569:Nitric Oxide / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D014132:Trachea / Q000187:drug effects; D014664:Vasodilation / Q000187:drug effects*
C447283:2-(2'-hydroxy-4',6'-dimethoxyphenyl)-5-propenylbenzofuran; D001572:Benzofurans; D017705:Lignans; D009569:Nitric Oxide; D002217:Carbachol; D000109:Acetylcholine