Jaimovich E., Mattei C., Liberona J. L., Cardenas C., Estrada M., Barbier J., Debitus Cécile, Laurent Dominique, Molgo J. (2005). Xestospongin B, a competitive inhibitor of IP3-mediated Ca2+ signalling in cultured rat myotubes, isolated myonuclei, and neuroblastoma (NG108-15) cells. Febs Letters, 579 (10), p. 2051-2057. ISSN 0014-5793.
Titre du document
Xestospongin B, a competitive inhibitor of IP3-mediated Ca2+ signalling in cultured rat myotubes, isolated myonuclei, and neuroblastoma (NG108-15) cells
Année de publication
2005
Auteurs
Jaimovich E., Mattei C., Liberona J. L., Cardenas C., Estrada M., Barbier J., Debitus Cécile, Laurent Dominique, Molgo J.
Source
Febs Letters, 2005,
579 (10), p. 2051-2057 ISSN 0014-5793
Xestospongin B, a macrocyclic bis-1-oxaquinolizidine alkaloid extracted from the marine sponge Xestospongia exigua, was highly purified and tested for its ability to block inositol 1,4,5-trisphosphate (IP3)-induced Ca2+ release. In a concentration-dependent manner xestospongin B displaced [H-3]IP3 from both rat cerebellar membranes and rat skeletal myotube homogenates with an EC50 of 44.6 +/- 1.1 mu M and 27.4 +/- 1.1 mu M, respectively. Xestospongin B, depending on the dose, suppressed bradykinin-induced Ca2+ signals in neuroblastoma (NG108-15) cells, and also selectively blocked the slow intracellular Ca2+ signal induced by membrane depolarization with high external K+ (47mM) in rat skeletal myotubes. This slow Ca2+ signal is unrelated to muscle contraction, and involves IP3 receptors. In highly purified isolated nuclei from rat skeletal myotubes, Xestospongin B reduced, or suppressed IP3-induced Ca2+ oscillations with an EC50 = 18.9 +/- 1.35 mu M. In rat my rotubes exposed to a Ca2+-free medium, Xestospongin B neither depleted sarcoplasmic reticulum Ca2+ stores, nor modified thapsigargin action and did not affect capacitative Ca2+ entry after thapsigargin-induced depletion of Ca2+ stores. Ca2+-ATPase activity measured in skeletal myrotube homogenates remained unaffected by Xestospongin B. It is concluded that xestospongin B is an effective cell-permeant. competitive inhibitor of IP3 receptors in cultured rat myotubes, isolated myonuclei, and neuroblastoma (NG108-15) cells. (c) 2005 Federation of European Biochemical Societies. Published by Elsevier B.V. All rights reserved.
Plan de classement
Activités biologiques [035SUBSAN02]
Descripteurs
INVERTEBRE AQUATIQUE ; SUBSTANCE NATURELLE ; ALCALOIDE ; STRUCTURE CHIMIQUE ; ACTIVITE BIOLOGIQUE ; INTERET PHARMACOLOGIQUE ; CULTURE CELLULAIRE ; TEST ; XESTOSPONGIN B ; EPONGE
Description Géographique
NOUVELLE CALEDONIE
Localisation
Fonds IRD [F B010038253]
Identifiant IRD
fdi:010038253
