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Your search keyword '"(±)-Taxifolin (PubChem CID: 439533)"' showing total 2 results
Start Over Descriptor "(±)-Taxifolin (PubChem CID: 439533)" Topic long qt syndrome
2 results on '"(±)-Taxifolin (PubChem CID: 439533)"'

1. Flavonoids and hERG channels: Friends or foes?

Author

Saponara S, Fusi F, Iovinelli D, Ahmed A, Trezza A, Spiga O, Sgaragli G, and Valoti M

Subjects
Action Potentials, Animals, ERG1 Potassium Channel chemistry, ERG1 Potassium Channel metabolism, Humans, Long QT Syndrome metabolism, Long QT Syndrome physiopathology, Myocytes, Cardiac metabolism, Protein Conformation, Risk Assessment, Risk Factors, Structure-Activity Relationship, Torsades de Pointes metabolism, Torsades de Pointes physiopathology, ERG1 Potassium Channel antagonists & inhibitors, Flavonoids toxicity, Heart Rate drug effects, Long QT Syndrome chemically induced, Myocytes, Cardiac drug effects, Potassium Channel Blockers toxicity, Torsades de Pointes chemically induced
Abstract

The cardiac action potential is regulated by several ion channels. Drugs capable to block these channels, in particular the human ether-à-go-go-related gene (hERG) channel, also known as K V 11.1 channel, may lead to a potentially lethal ventricular tachyarrhythmia called "Torsades de Pointes". Thus, evaluation of the hERG channel off-target activity of novel chemical entities is nowadays required to safeguard patients as well as to avoid attrition in drug development. Flavonoids, a large class of natural compounds abundantly present in food, beverages, herbal medicines, and dietary food supplements, generally escape this assessment, though consumed in consistent amounts. Continuously growing evidence indicates that these compounds may interact with the hERG channel and block it. The present review, by examining numerous studies, summarizes the state-of-the-art in this field, describing the most significant examples of direct and indirect inhibition of the hERG channel current operated by flavonoids. A description of the molecular interactions between a few of these natural molecules and the Rattus norvegicus channel protein, achieved by an in silico approach, is also presented., (Copyright © 2021 Elsevier B.V. All rights reserved.)

Published
2021
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2. Flavonoids and hERG channels: Friends or foes?

Author

Massimo Valoti, Fabio Fusi, Simona Saponara, Daniele Iovinelli, Alfonso Trezza, Giampietro Sgaragli, Ottavia Spiga, and Amer Ahmed

Subjects
0301 basic medicine, ERG1 Potassium Channel, Protein Conformation, Ventricular Tachyarrhythmias, Silybinin (PubChem CID: 31553), Action Potentials, Genistein (PubChem CID: 5280961), Hesperetin (PubChem CID: 72281), (±)-Taxifolin (PubChem CID: 439533), Long QT syndrome Chemical compounds studied in this article: Torsades de pointes(±)-Naringenin (PubChem CID: 932), 0302 clinical medicine, Heart Rate, Risk Factors, Myocytes, Cardiac, Docking simulation Flavonoid, Liquiritigenin (PubChem CID: 114829), biology, Chemistry, Docking simulation Flavonoid, Patch-clamp, hERG channel, Long QT syndrome Chemical compounds studied in this article: Torsades de pointes(±)-Naringenin (PubChem CID: 932), 7,8-Dimethoxyflavone (PubChem CID:689014), Acacetin (PubChem CID: 5280442), Apigenin (PubChem CID: 5280443), Apigenin trimethyl-ether (PubChem CID: 79730), Baicalein (PubChem CID: 5281605), Daidzein (PubChem CID: 5281708), Docking simulation, Epigallocatechin gallate (PubChem CID: 65064), Fisetin (PubChem CID: 5281614), Flavonoid, Galangin (PubChem CID: 5281616), hERG channel, Isorhamnetin (PubChem CID: 5281654), Kaempferol (PubChem CID: 5280863), Long QT syndrome, Luteolin (PubChem CID: 5280445), Morin (PubChem CID 5281670), Myricetin (PubChem CID: 5281672), Naringin (PubChem CID: 442428), Patch-clamp, Quercetin (PubChem CID: 5280343), Rutin (PubChem CID: 5280805), Torsades de pointes, Cardiac action potential, Drug development, Communication channel, In silico, hERG, Computational biology, Risk Assessment, 8-Dimethoxyflavone (PubChem CID:689014), Structure-Activity Relationship, 03 medical and health sciences, Potassium Channel Blockers, medicine, Animals, Humans, Ion channel, Flavonoids, Pharmacology, medicine.disease, 030104 developmental biology, biology.protein, 030217 neurology & neurosurgery
Abstract

The cardiac action potential is regulated by several ion channels. Drugs capable to block these channels, in particular the human ether-a-go-go-related gene (hERG) channel, also known as KV11.1 channel, may lead to a potentially lethal ventricular tachyarrhythmia called "Torsades de Pointes". Thus, evaluation of the hERG channel off-target activity of novel chemical entities is nowadays required to safeguard patients as well as to avoid attrition in drug development. Flavonoids, a large class of natural compounds abundantly present in food, beverages, herbal medicines, and dietary food supplements, generally escape this assessment, though consumed in consistent amounts. Continuously growing evidence indicates that these compounds may interact with the hERG channel and block it. The present review, by examining numerous studies, summarizes the state-of-the-art in this field, describing the most significant examples of direct and indirect inhibition of the hERG channel current operated by flavonoids. A description of the molecular interactions between a few of these natural molecules and the Rattus norvegicus channel protein, achieved by an in silico approach, is also presented.

Published
2021

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