NEW LEUKOTRIENE-B4 RECEPTOR ANTAGONIST - LEUCETTAMINE-A AND RELATED IMIDAZOLE ALKALOIDS FROM THE MARINE SPONGE LEUCETTA-MICRORAPHIS
NEW LEUKOTRIENE-B4 RECEPTOR ANTAGONIST - LEUCETTAMINE-A AND RELATED IMIDAZOLE ALKALOIDS FROM THE MARINE SPONGE LEUCETTA-MICRORAPHIS
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DOI：
10.1021/np50091a016
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发表时间：
1993-01-01
影响因子：
5.1
通讯作者：
WESTLEY, JW
中科院分区：
文献类型：
--
作者：
CHAN, GW;MONG, S;WESTLEY, JW
从帕劳海绵Leucetta microraphis中分离得到三个新的咪唑生物碱：leucettamines A [1]和B [2]及leucettamidine [3]。它们的结构是建立在广泛的光谱分析的基础上。亮氨酰胺A显示出有效的白三烯B受体结合活性（K（i）= 1.3 μ M），而亮氨酰胺B基本上无活性（K（i）= 100 μ M），亮氨酰胺脒显示出显著的活性（K（i）= 5.3 μ M）。亮氨酸胺A被鉴定为一种纯的LTB 4受体拮抗剂，为炎症治疗提供了一种新的结构导向剂。
Three new imidazole alkaloids, leucettamines A [l] and B [2] and leucettamidine [3], have been isolated from the Palauan sponge Leucetta microraphis. Their structures were established on the basis of extensive spectral analyses. Leucettamine A showed potent leukotriene B, receptor binding activity (K(i) = 1.3 muM), while leucettamine B was essentially inactive (K(i) = 100 muM) and leucettamidine showed significant activity (K(i) = 5.3 muM). With leucettamine A identified as a pure LTB4 receptor antagonist, a new structure lead is presented to inflammation therapy.