考察花色苷及其苷元与大麻素受体的亲和力。

An examination of anthocyanins' and anthocyanidins' affinity for cannabinoid receptors.

机构信息

Department of Psychiatry, University of Regensburg, Regensburg, Germany.

出版信息

J Med Food. 2009 Dec;12(6):1407-10. doi: 10.1089/jmf.2008.0243.

DOI:10.1089/jmf.2008.0243

PMID:20041802

Abstract

A growing body of evidence suggests that anthocyanins and anthocyanidins may possess analgesic properties in addition to neuroprotective and anti-inflammatory activities. These functionalities suggest a role for the cannabinoid receptor (CB) in mediating biological effects. Competitive radioligand binding assays identified cyanidin (K(i) = 16.2 microM) and delphinidin (K(i) = 21.3 microM) as ligands with moderate affinity to human CB1. For CB2, similar affinities were achieved by cyanidin (K(i) = 33.5 microM), delphinidin (K(i) = 34.3 microM), and peonidin (K(i) = 46.4 microM). Inhibition constants >50 microM were obtained for pelargonidin, malvidin, cyanidin-3,5-di-O-glucoside, cyanidin-3-O-glucoside, cyanidin-3-O-galactoside, and cyanidin-3-O-rutinoside for both CB subtypes.

摘要

越来越多的证据表明，花色苷和花色苷元除了具有神经保护和抗炎活性外，还可能具有镇痛作用。这些功能表明大麻素受体（CB）在介导生物学效应中起作用。竞争性放射配体结合分析鉴定出矢车菊素（Ki = 16.2 microM）和飞燕草素（Ki = 21.3 microM）为对人 CB1 具有中等亲和力的配体。对于 CB2，同样的亲和力也可由矢车菊素（Ki = 33.5 microM）、飞燕草素（Ki = 34.3 microM）和芍药素（Ki = 46.4 microM）实现。对于 CB 两种亚型，Pelargonidin、Malvidin、矢车菊素-3,5-二-O-葡萄糖苷、矢车菊素-3-O-葡萄糖苷、矢车菊素-3-O-半乳糖苷和矢车菊素-3-O-芦丁糖苷的抑制常数均大于 50 microM。