Vasorelaxant Activity of (2S)-Sakuranetin and Other Flavonoids Isolated from the Green Propolis of the Caatinga Mimosa tenuiflora

Ninh The Son; Beatrice Gianibbi; Alice Panti; Ottavia Spiga; Jairo Kenupp Bastos; Fabio Fusi

doi:10.1055/a-2294-7042

Planta Medica, Table of Contents

Planta Med 2024; 90(06): 454-468
DOI: 10.1055/a-2294-7042

Biological and Pharmacological Activity

Original Papers

Vasorelaxant Activity of (2S)-Sakuranetin and Other Flavonoids Isolated from the Green Propolis of the Caatinga Mimosa tenuiflora

Ninh The Son‡

²Institute of Chemistry, Vietnam Academy of Science and Technology (VAST), Hanoi, Vietnam

³Department of Chemistry, Graduate University of Science and Technology, Vietnam Academy of Science and Technology, Caugiay, Hanoi, Vietnam

,

Beatrice Gianibbi‡

⁴Dipartimento di Biotecnologie, Chimica e Farmacia, Università di Siena, Siena, Italy

,

Alice Panti‡

⁵Dipartimento di Scienze della Vita, Università di Siena, Siena, Italy

,

Ottavia Spiga

⁴Dipartimento di Biotecnologie, Chimica e Farmacia, Università di Siena, Siena, Italy

,

Jairo Kenupp Bastos

¹School of Pharmaceutical Sciences of Ribeirão Preto, Ribeirão Preto, University of São Paulo, Ribeirão Preto-SP, Brazil

,

Fabio Fusi

⁴Dipartimento di Biotecnologie, Chimica e Farmacia, Università di Siena, Siena, Italy

› Author Affiliations

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_V1.2 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 K_Ca1.1 channels both in single myocytes and vascular rings. In silico analysis provided interesting insights into the mode of action of (2S)-sakuranetin within both Ca_V1.2 and K_Ca1.1 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.

Keywords

Green propolis - (2S)-sakuranetin - Mimosa tenuiflora - Ca_V1.2 channels - K_Ca1.1 channels - Fabaceae

Full Text

References

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