1. Vasorelaxant Activity of (2S)-Sakuranetin and Other Flavonoids Isolated from the Green Propolis of the Caatinga Mimosa tenuiflora.
- Author
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Son, Ninh The, Gianibbi, Beatrice, Panti, Alice, Spiga, Ottavia, Bastos, Jairo Kenupp, and Fusi, Fabio
- Subjects
CARDIOVASCULAR disease prevention ,IN vitro studies ,COMPUTER-assisted molecular modeling ,VASODILATORS ,VASODILATION ,POTASSIUM antagonists ,FLAVONOIDS ,ANIMALS ,FUNCTIONAL foods ,IN vivo studies ,CALCIUM antagonists ,PLANT extracts ,PROPOLIS ,RATS ,EXPERIMENTAL design ,ANIMAL experimentation ,ELECTROPHYSIOLOGY ,MEMBRANE proteins ,PHARMACODYNAMICS - Abstract
Some in vitro and in vivo evidence is consistent with the cardiovascular beneficial activity of propolis. As the single actors responsible for this effect have never been identified, an in-depth investigation of flavonoids isolated from the green propolis of the Caatinga Mimosa tenuiflora was performed and their mechanism of action was described. A comprehensive electrophysiology, functional, and molecular docking approach was applied. Most flavanones and flavones were effective Ca
V 1.2 channel blockers with a potency order of (2S)-sakuranetin > eriodictyol-7,3′-methyl ether > quercetin 3-methyl ether > 5,4′-dihydroxy-6,7-dimethoxyflavanone > santin > axillarin > penduletin > kumatakenin, ermanin and viscosine being weak or modest stimulators. Except for eriodictyol 5-O-methyl ether, all the flavonoids were also effective spasmolytic agents of vascular rings, kumatakenin and viscosine also showing an endothelium-dependent activity. (2S)-Sakuranetin also stimulated KCa 1.1 channels both in single myocytes and vascular rings. In silico analysis provided interesting insights into the mode of action of (2S)-sakuranetin within both CaV 1.2 and KCa 1.1 channels. The green propolis of the Caatinga Mimosa tenuiflora is a valuable source of multi-target vasoactive flavonoids: this evidence reinforces its nutraceutical value in the cardiovascular disease prevention arena. [ABSTRACT FROM AUTHOR]- Published
- 2024
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