Vassas A, Bourdy G, Paillard J J, Lavayre J, Païs M, Quirion J C, Debitus C
Laboratoire de Botanique, Phytochimie et Mycologie, Faculté de Pharmacie, Montpellier, France.
Planta Med. 1996 Feb;62(1):28-30. doi: 10.1055/s-2006-957790.
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.
血管活性肠肽（VIP）和生长抑素（促生长激素释放抑制因子，SRIF）是许多基本生理活动中的重要神经递质。在许多疾病中，如囊性纤维化、阳痿患者（VIP相关）、阿尔茨海默病和一些肿瘤（SRIF相关），都有它们紊乱的报道。从Xestospongia属和新喀里多尼亚海绵中分离出的三种生物碱，即西托斯海绵素B（1）、sceptrine（2）和ageliferine（3），被报道为生长抑素和VIP抑制剂。天然产物1、2和3对生长抑素表现出高亲和力（IC50分别为12 microM、0.27 microM和2.2 microM），2和3对VIP表现出亲和力（分别为19.8 microM和19.2 microM）。由于非肽类化合物与生长抑素/VIP受体之间的相互作用，这三种生物碱可能成为天然非肽类化合物治疗干预研究中的有前景的药物。
