黄酮类化合物作为阿片受体配体：鉴定及初步构效关系
Flavonoids as opioid receptor ligands: identification and preliminary structure-activity relationships.
作者信息
Katavic Peter L, Lamb Kenneth, Navarro Hernan, Prisinzano Thomas E
机构信息
Division of Medicinal & Natural Products Chemistry, College of Pharmacy, The University of Iowa, Iowa City, Iowa 52242, USA.
出版信息
J Nat Prod. 2007 Aug;70(8):1278-82. doi: 10.1021/np070194x. Epub 2007 Aug 9.
Abstract
Flavonoids have been recognized as the active ingredients of many medicinal plant extracts due to interactions with proteins via phenolic groups and low toxicity. Here, we report the investigation of the flavonoid core as a potential new scaffold for the development of opioid receptor ligands. Biological results suggest that stereochemistry of the C2 and C3 positions is important for antagonist activity and selectivity. Our results also suggest that the actions of Hypericum perforatum may be mediated in part by opioid receptors.
摘要
由于黄酮类化合物通过酚羟基与蛋白质相互作用且毒性较低，它们已被公认为许多药用植物提取物的活性成分。在此，我们报告了对黄酮类核心结构作为开发阿片受体配体潜在新支架的研究。生物学结果表明，C2和C3位的立体化学对拮抗剂活性和选择性很重要。我们的结果还表明，贯叶连翘的作用可能部分由阿片受体介导。
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