Naturally Occurring Somatostatin and Vasoactive Intestinal Peptide Inhibitors. Isolation of Alkaloids from Two Marine Sponges

A. Vassas; G. Bourdy; J. J. Paillard; J. Lavayre; M. Païs; J. C. Quirion; C. Debitus

doi:10.1055/s-2006-957790

Planta Medica, Table of Contents

Planta Med 1996; 62(1): 28-30
DOI: 10.1055/s-2006-957790

Paper

Naturally Occurring Somatostatin and Vasoactive Intestinal Peptide Inhibitors. Isolation of Alkaloids from Two Marine Sponges

A. Vassas¹ , G. Bourdy² , J. J. Paillard³ , J. Lavayre³ , M. Païs⁴ , J. C. Quirion⁴ , C. Debitus⁵

¹Laboratoire de Botanique, Phytochimie et Mycologie, Faculté de Pharmacie, F-34060 Montpellier, France
²ORSTOM, CP 9214, La Paz, Bolivia
³Rhône-Poulenc Rorer S. A., CRVA, BP14, F-94403 Vitry/Seine Cedex, France
⁴CNRS, Institut de chimie des substances naturelles, F-91198 Gif sur Yvette Cedex, France
⁵ORSTOM, BP A5, Nouméa, Nouvelle-Calédonie

Abstract

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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 µM, 0.27 µM, and 2.2 µM, respectively), 2 and 3 showed an affinity for VIP (19.8 µM and 19.2 µM, 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.

Key words

Porifera - Nepheliospongida - Axinellida - ageliferine - sceptrine - xestospongine B - somatostatin receptor - vasoactive intestinal peptide receptor

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