Naturally occurring somatostatin and vasoactive intestinal peptide inhibitors. Isolation of alkaloids from two marine sponges
1996
Vassas, A. | Bourdy, G. | Paillard, J.J. | Lavayre, J. | Pais, M. | Quirion, J.C. | Debitus, C. (Faculte de Pharmacie, Montpellier (France). Lab. de Botanique. Phytochimie et Mycologie)
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 (SRlF). Xestospongine B 1., sceptrine 2., and ageliferine 3., three alkaloids isolated from Xesto-spongia 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/VlP receptors, these three alkaloids could be promising agents in the research on natural non-peptidic compounds for therapeutical interventions.
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