Effects of a labdane diterpene isolated from Brickellia paniculata on intracellular Ca2+ deposit of guinea-pig ileal longitudinal muscle.
The labdane diterpene 3alpha-angeloyloxy-2alpha-hydroxy-13,14Z-dehydrocativic acid (AAHDD) isolated from Brickellia paniculata leaves, produces relaxation of the guinea-pig ileum in vitro by Ca2+ antagonistic effects. In the longitudinal ileal muscle the compound inhibited the tonic contractions induced with 60 mM K+(IC50 = 15.52 +/- 1.93 microM) with half the potency than that of papaverine (IC50 = 6.70 +/- 1.31 MM). Phasic response to high K+ was also blocked by AAHDD, with the ratio IC50 phasic/IC50 to-nic = 7.11. In Ca2+-free, high K+ (60 mM) solution, AAHDD inhibited the contractions induced with 2 mM Ca2+ and pretreatment of the tissues with 10 uM cyclopiazonic acid or 30 pM ryanodine failed to influence the blockade of AAHDD on Ca2+ induced contractions. In muscles loaded with 45Ca, after washing the preparations with AAHDD in high K+ (60 mM) solution, determined 45Ca efflux was similar to that of the control without the diterpene. As the relaxant effect of AAHDD was not influenced by cyclopiazonic acid and by ryanodine, two agents which have been described as modulators of Ca2+ uptake and Ca2+ release from intracellular stores, the obtained results suggest that tension inhibitory effects produced by AAHDD do not involve the mobilization of Ca2+ at intracellular deposits.
Meckes
Mariana
M
U.I.M Farmacología de Productos Naturales. Hospital de Pediatría, CMN Siglo XXI, IMSS. Col. Doctores, México DF. meck7707@prodigy.net.mx
Román-Ramos
Rubén
R
Pérez
Salud
S
Calzada
Fernando
F
Ponce-Monter
Héctor
H
D000818:Animals; D019659:Asteraceae / Q000737:chemistry*; D002118:Calcium / Q000378:metabolism*; D004224:Diterpenes / Q000494:pharmacology*; D004347:Drug Interactions; D006168:Guinea Pigs; D007082:Ileum / Q000166:cytology; D007211:Indoles / Q000494:pharmacology; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects* / Q000378:metabolism / Q000502:physiology; D011188:Potassium / Q000502:physiology; D012433:Ryanodine / Q000494:pharmacology; D014665:Vasodilator Agents / Q000494:pharmacology
D004224:Diterpenes; D007211:Indoles; D014665:Vasodilator Agents; C433017:labdane; D012433:Ryanodine; D011188:Potassium; D002118:Calcium; C000543:cyclopiazonic acid