KCNQ5 Potassium Channel Activation Underlies Vasodilation by Tea
| Autor: | Thomas A. Jepps, Kaitlyn E Redford, Geoffrey W. Abbott, Salomé Rognant |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
0301 basic medicine
Male Protein Conformation alpha-Helical Vascular smooth muscle Patch-Clamp Techniques Physiology Protein Conformation Wistar Kv7 Vasodilation Green tea extract Pharmacology lcsh:Physiology Catechin Membrane Potentials Tissue Culture Techniques chemistry.chemical_compound KCNQ Xenopus laevis 0302 clinical medicine Protein Isoforms lcsh:QD415-436 Mesenteric arteries Electrical impedance myography lcsh:QP1-981 KCNQ Potassium Channels Chemistry food and beverages Resting potential Potassium channel Mesenteric Arteries Molecular Docking Simulation medicine.anatomical_structure Milk 030220 oncology & carcinogenesis KCNQ1 Potassium Channel Protein Binding Polyphenol Hypotensive complex mixtures Article lcsh:Biochemistry 03 medical and health sciences medicine Animals Rats Wistar Binding Sites Tea Plant Extracts alpha-Helical Myography Green tea IKS Rats 030104 developmental biology Epicatechin gallate Oocytes beta-Strand Protein Conformation beta-Strand |
| Zdroj: | Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology Cellular Physiology and Biochemistry, vol 55, iss S3 Cellular Physiology and Biochemistry, Vol 55, Iss S3, Pp 46-64 (2021) Redford, K E, Rognant, S, Jepps, T A & Abbott, G W 2021, ' KCNQ5 Potassium Channel Activation Underlies Vasodilation by Tea ', Cellular Physiology and Biochemistry, vol. 55, no. S3, pp. 46-64 . https://doi.org/10.33594/000000337 |
| ISSN: | 1421-9778 1015-8987 |
| Popis: | BACKGROUND/AIMS: Tea, produced from the evergreen Camellia sinensis, has reported therapeutic properties against multiple pathologies, including hypertension. Although some studies validate the health benefits of tea, few have investigated the molecular mechanisms of action. The KCNQ5 voltage-gated potassium channel contributes to vascular smooth muscle tone and neuronal M-current regulation.METHODS: We applied electrophysiology, myography, mass spectrometry and in silico docking to determine effects and their underlying molecular mechanisms of tea and its components on KCNQ channels and arterial tone.RESULTS: A 1% green tea extract (GTE) hyperpolarized cells by augmenting KCNQ5 activity >20-fold at resting potential; similar effects of black tea were inhibited by milk. In contrast, GTE had lesser effects on KCNQ2/Q3 and inhibited KCNQ1/E1. Tea polyphenols epicatechin gallate (ECG) and epigallocatechin-3-gallate (EGCG), but not epicatechin or epigallocatechin, isoform-selectively hyperpolarized KCNQ5 activation voltage dependence. In silico docking and mutagenesis revealed that activation by ECG requires KCNQ5-R212, at the voltage sensor foot. Strikingly, ECG and EGCG but not epicatechin KCNQ-dependently relaxed rat mesenteric arteries.CONCLUSION: KCNQ5 activation contributes to vasodilation by tea; ECG and EGCG are candidates for future anti-hypertensive drug development. |
| Databáze: | OpenAIRE |
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