Brastianos Harry C, Vottero Eduardo, Patrick Brian O, Van Soest Rob, Matainaho Teatulohi, Mauk A Grant, Andersen Raymond J
Department of Chemistry, University of British Columbia, Vancouver, BC, Canada V6T 1Z1.
J Am Chem Soc. 2006 Dec 20;128(50):16046-7. doi: 10.1021/ja067211+.
Exiguamine A (1), a hexacyclic alkaloid with an unprecedented skeleton, has been isolated from the marine sponge Neopetrosia exigua collected in Papua New Guinea. The structure of exiguamine A (1) was elucidated by a combination of spectroscopic analysis and single-crystal X-ray diffraction analysis. Exiguamine A (1) has a Ki of 210 nM for inhibition of indoleamine-2,3-dioxygenase (IDO) in vitro, making it one of the most potent IDO inhibitors known to date. A putative biogenesis for the new exiguamine skeleton starts from DOPA, tryptophan, and N,N-dimethylhydantoin.
埃克西古胺A（1）是一种具有前所未有的骨架的六环生物碱，它是从在巴布亚新几内亚采集的海洋海绵微小新岩海绵中分离得到的。通过光谱分析和单晶X射线衍射分析相结合的方法阐明了埃克西古胺A（1）的结构。埃克西古胺A（1）在体外抑制吲哚胺-2,3-双加氧酶（IDO）的Ki值为210 nM，使其成为迄今为止已知的最有效的IDO抑制剂之一。新的埃克西古胺骨架的推测生物合成起始于多巴、色氨酸和N,N-二甲基乙内酰脲。
