Inhibition of hyperpolarization-activated cyclic nucleotide-gated channels with natural flavonoid quercetin.
Biochem Biophys Res Commun
; 533(4): 952-957, 2020 12 17.
Article
em En
| MEDLINE
| ID: mdl-33008592
ABSTRACT
Quercetin is a natural flavonoid which has been reported to be analgesic in different animal models of pain. However, the mechanism underlying the pain-relieving effects is still unclear. Hyperpolarization-activated cyclic nucleotide-gated (HCN) channels play critical roles in controlling pacemaker activity in cardiac and nervous systems, making the channel a new target for therapeutic exploration. In this study, we explored a series of flavonoids for their modulation on HCN channels. Among all tested flavonoids, quercetin was the most potent inhibitor for HCN channels with an IC50 value of 27.32 ± 1.19 µM for HCN2. Furthermore, quercetin prominently left shifted the voltage-dependent activation curves of HCN channels and decelerated deactivation process. The results presented herein firstly characterize quercetin as a novel and potent inhibitor for HCN channels, which represents a novel structure for future drug design of HCN channel inhibitors.
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Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Quercetina
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Canais Disparados por Nucleotídeos Cíclicos Ativados por Hiperpolarização
Idioma:
En
Revista:
Biochem Biophys Res Commun
Ano de publicação:
2020
Tipo de documento:
Article
País de afiliação:
China