title: Naturally occurring somatostatin and vasoactive intestinal peptide inhibitors. Isolation of alkaloids from two marine sponges.
abstract: The vasoactive intestinal peptide (VIP) and somatostatin (somatotropin release inhibiting factor, SRIF) are important neurotransmitters in a number of basic physiological events. Their disturbances have been reported in many diseases such as cystic fibrosis, impotent man (VIP), Alzheimer's disease, and some tumours (SRIF). Xestospongine B (1), sceptrine (2), and ageliferine (3), three alkaloids isolated from Xestospongia sp. and Agelas novaecaledoniae are reported as somatostatin and VIP inhibitors. The natural products 1, 2 and 3 exhibited a high affinity for somatostatin (IC50 = 12 microM, 0.27 microM, and 2.2 microM, respectively), 2 and 3 showed an affinity for VIP (19.8 microM and 19.2 microM, respectively). Due to the interaction between non-peptidic compounds and somatostatin/VIP receptors, these three alkaloids could be promising agents in the research on natural non-peptidic compounds for therapeutical interventions.
authors.affiliation: Laboratoire de Botanique, Phytochimie et Mycologie, Faculté de Pharmacie, Montpellier, France.
authors.forename: A
authors.initials: A
authors.lastname: Vassas
authors.forename: G
authors.initials: G
authors.lastname: Bourdy
authors.forename: J J
authors.initials: JJ
authors.lastname: Paillard
authors.forename: J
authors.initials: J
authors.lastname: Lavayre
authors.forename: M
authors.initials: M
authors.lastname: Païs
authors.forename: J C
authors.initials: JC
authors.lastname: Quirion
authors.forename: C
authors.initials: C
authors.lastname: Debitus
mesh_terms: D000470:Alkaloids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D000818:Animals; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D011161:Porifera / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013004:Somatostatin / Q000037:antagonists & inhibitors*; D014660:Vasoactive Intestinal Peptide / Q000037:antagonists & inhibitors*
chemical_list: D000470:Alkaloids; D014660:Vasoactive Intestinal Peptide; D013004:Somatostatin