2015/06/02 by Amer H. Taráwneh, Francisco León, Sara Pettaway +5 · 1 citation
Biochemistry, Genetics and Molecular Biology · Chemistry · #Pharmacological Receptor Mechanisms and Effects #Axial and Atropisomeric Chirality Synthesis #Electron Spin Resonance Studies #Radioligand #Cannabinoid #Opioid #Stereochemistry #Opioid receptor #Receptor #Chemistry #Cannabinoid receptor #Pharmacognosy #Flavonoid #In vitro #Pharmacology #Biological activity #Biochemistry #Biology #Antagonist
paper · doi:10.1021/acs.jnatprod.5b00218
openalex publication_date 2015/06/02 · openalex created_date 2016/06/24 · openalex updated_date 2026/08/01
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 δ opioid receptor with Ki values ranging from 3.1 to 26.0 μM. In addition, the binding mode of the compounds in the active site of the δ opioid receptor was investigated through molecular modeling algorithms. This study may have implications in better understanding non-nitrogenous δ opioid receptor ligands.