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Tarawneh A , Leon F , Pettaway S , Elokely KM , Klein ML , Lambert J , Mansoor A , Cutler SJ
Flavonoids from Perovskia atriplicifolia and Their in Vitro Displacement of the Respective Radioligands for Human Opioid and Cannabinoid Receptors
J Nat Prod. 2015 Jun 26;78(6) :1461-5
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Abstract
Bioassay-guided fractionation of the leaves of Perovskia atriplicifolia (Russian sage) resulted in the isolation of four previously known flavonoid derivatives, 5-hydroxy-6,7,3',4'-tetramethoxyflavone (1), 5,7-dihydroxy-6,3',4'-trimethoxyflavone (2), 5-hydroxy-6,7,4'-trimethoxyflavone (3), and 5,7-dihydroxy-6,4'-dimethoxyflavone (4). Compounds 1, 3, and 4 showed displacement of the radioligand for the cloned human delta opioid receptor with Ki values ranging from 3.1 to 26.0 muM. In addition, the binding mode of the compounds in the active site of the delta opioid receptor was investigated through molecular modeling algorithms. This study may have implications in better understanding non-nitrogenous delta opioid receptor ligands.
Notes
Tarawneh, Amer Leon, Francisco Pettaway, Sara Elokely, Khaled M Klein, Michael L Lambert, Janet Mansoor, Arsala Cutler, Stephen J P20 GM104932/GM/NIGMS NIH HHS/United States United States J Nat Prod. 2015 Jun 26;78(6):1461-5. doi: 10.1021/acs.jnatprod.5b00218. Epub 2015 Jun 2.