Wise M L, Soderstrom K, Murray T F, Gerwick W H
Department of Biochemistry and Biophysics, Oregon State University, Corvallis 97331, USA.
Experientia. 1996 Jan 16;52(1):88-92. doi: 10.1007/BF01922423.
A polyenoic fatty-acid isomerase (PFI) from a red marine alga was used to convert anandamide (5Z,8Z,11Z,14Z-eicosatetraenoyl-N-ethan olamide) to the 5Z,7E,9E,14Z-eicosatetraenoyl-N-ethanol amide isomer. This novel eicosanoid, termed conjugated triene anandamide (CTA), was assessed for its ability to bind to the cannabinoid receptor in rat brain membrane preparations. CTA is a high affinity cannabimimetic substance whose novel structure provides new insight into structure-activity relationships of cannabinoid receptor ligands. These experiments illustrate the utility of enzymes isolated from marine organisms in the development of pharmacological probes.
一种来自红色海洋藻类的多烯脂肪酸异构酶（PFI）被用于将花生四烯乙醇胺（5Z,8Z,11Z,14Z-二十碳四烯酰-N-乙醇胺）转化为5Z,7E,9E,14Z-二十碳四烯酰-N-乙醇胺异构体。这种新型类二十烷酸，称为共轭三烯花生四烯乙醇胺（CTA），在大鼠脑膜制剂中被评估了其与大麻素受体结合的能力。CTA是一种高亲和力的大麻素模拟物质，其新颖的结构为大麻素受体配体的构效关系提供了新的见解。这些实验说明了从海洋生物中分离的酶在药理学探针开发中的实用性。
