Identification of CB1/CB2 Ligands from Zanthoxylum bungeanum

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• 作者：Katina S. S. Dossou ; Krishna P. Devkota ; Cynthia Morton ; Josephine M. Egan ; Guanghua Lu ; John A. Beutler ; Ruin Moaddel
• 刊名：Journal of Natural Products
• 出版年：2013
• 出版时间：November 22, 2013
• 年：2013
• 卷：76
• 期：11
• 页码：2060-2064
• 全文大小：221K
• 年卷期：v.76,no.11(November 22, 2013)
• ISSN：1520-6025

文摘

In order to study cannabinoid receptor ligands, a novel plate-based assay was developed previously to measure internalization of CB1/CB2 receptors by determining the change in the intracellular levels of the radiolabeled agonists. This plate-based assay was also used for screening against complex matrices, specifically, in the present study screening for CB1/CB2 receptor activity of extracts for several species of the plant genus Zanthoxylum. The objective of this screen was to identify novel antagonists of the CB1 receptor, which simultaneously displayed agonist activity against the CB2 receptor, since compounds matching this criterion could be potential candidates for the treatment of type-1 diabetes. As a result, two Z. bungeanum extracts were deemed active, leading to the identification of eight compounds, of which compound 7 [(2E,4E,8E,10E,12E)-N-isobutyl-2,4,8,10,12-tetradecapentaenamide, 纬-sanshool] was obtained as a promising lead compound.