Inhibition of hyperpolarization-activated cyclic nucleotide-gated channels with natural flavonoid quercetin

Liang, Yemei; Xu, Zhiwu; Wu, Xiaoyan; Pang, Jianxin; Zhou, Pingzheng; Cao, Ying

doi:10.1016/j.bbrc.2020.09.102

Cited by 3 publications

(2 citation statements)

References 28 publications

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“…Additionally, it is well-established that hyperpolarization-activated cyclic-nucleotide-gated (HCN) channels play a critical role in chronic pain [ 73 , 74 ]. Interestingly, Liang et al demonstrated that quercetin remarkably left-shifted the voltage-dependent activation curves of HCN channels and decelerated the deactivation process [ 75 ]. These results indicate that quercetin might be a potent HCN channels blocker, which sheds light on the mechanism of the analgesic effects of quercetin.…”

Section: Conclusion and Future Perspectivementioning

confidence: 99%

The Emerging Role of Quercetin in the Treatment of Chronic Pain

Liu

Tian

et al. 2022

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Despite much research efforts being devoted to design alternative pharmacological interventions, chronic pain remains to be an unresolved clinical problem. Quercetin, a compound that belongs to the flavonoids family, is abundantly found in fruits and vegetables. Emerging evidence indicates that quercetin possesses anti-nociceptive effects in different rodent models of chronic pain including inflammatory pain, neuropathic pain, and cancer pain. In this review, we summarize the mechanisms underlying the analgesic effect of quercetin in preclinical studies. These studies showed that quercetin exerts potent analgesic effects against chronic pain via suppressing neuroinflammation and oxidative stress as well as modulation of synaptic plasticity, GABAergic system, and opioidergic system. Considering that the safety of quercetin is well established, it has great potential for clinical use in pain treatment.

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Section: Conclusion and Future Perspectivementioning

confidence: 99%

The Emerging Role of Quercetin in the Treatment of Chronic Pain

Liu

Tian

et al. 2022

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“…Histopathological examinations revealed the protection of cardiomyocytes’ membrane integrity and global enhancement in myocardial function after exposure with quercetin. These beneficial effects were associated with decreased infiltration of leukocytes to the site of infarction, maintained overall tissue architecture as well as reduced oedema [ 268 , 269 ]. The reduction in Src kinase activity, caspase 9, signal transducer and activator of transcription 3 (STAT3), intracellular ROS production as well as inducible MnSOD expression are other mechanisms related to cardioprotective effects of quercetin [ 270 ].…”

Section: Impact Of Natural Compounds On Cvd Riskmentioning

confidence: 99%

Ageing, Age-Related Cardiovascular Risk and the Beneficial Role of Natural Components Intake

Rysz

Franczyk

Rysz-Górzyńska

et al. 2021

IJMS

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Ageing, in a natural way, leads to the gradual worsening of the functional capacity of all systems and, eventually, to death. This process is strongly associated with higher metabolic and oxidative stress, low-grade inflammation, accumulation of DNA mutations and increased levels of related damage. Detrimental changes that accumulate in body cells and tissues with time raise the vulnerability to environmental challenges and enhance the risk of major chronic diseases and mortality. There are several theses concerning the mechanisms of ageing: genetic, free radical telomerase, mitochondrial decline, metabolic damage, cellular senescence, neuroendocrine theory, Hay-flick limit and membrane theories, cellular death as well as the accumulation of toxic and non-toxic garbage. Moreover, ageing is associated with structural changes within the myocardium, cardiac conduction system, the endocardium as well as the vasculature. With time, the cardiac structures lose elasticity, and fibrotic changes occur in the heart valves. Ageing is also associated with a higher risk of atherosclerosis. The results of studies suggest that some natural compounds may slow down this process and protect against age-related diseases. Animal studies imply that some of them may prolong the lifespan; however, this trend is not so obvious in humans.

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Non-canonical Molecular Targets for Novel Analgesics: Intracellular Calcium and HCN Channels

Cook

Goldstein

2021

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Pain is a prevalent biopsychosocial condition that poses a significant challenge to healthcare providers, contributes substantially to disability, and is a major economic burden worldwide. An overreliance on opioid analgesics, which primarily target the μ-opioid receptor, has caused devastating morbidity and mortality in the form of misuse and overdose-related death. Thus, novel analgesic medications are needed that can effectively treat pain and provide an alternative to opioids. A variety of cellular ion channels contribute to nociception, the response of the sensory nervous system to a noxious stimulus that commonly leads to pain. Ion channels involved in nociception may provide a suitable target for pharmacologic modulation to achieve pain relief. This narrative review summarizes the evidence for two ion channels that merit consideration as targets for non-opioid pain medications: ryanodine receptors (RyRs), which are intracellular calcium channels, and hyperpolarization-activated cyclic nucleotide-gated (HCN) channels, which belong the superfamily of voltage-gated K+ channels. The role of these channels in nociception and neuropathic pain is discussed and suitability as targets for novel analgesics and antihyperalgesics is considered.

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Inhibition of hyperpolarization-activated cyclic nucleotide-gated channels with natural flavonoid quercetin

Cited by 3 publications

References 28 publications

The Emerging Role of Quercetin in the Treatment of Chronic Pain

The Emerging Role of Quercetin in the Treatment of Chronic Pain

Ageing, Age-Related Cardiovascular Risk and the Beneficial Role of Natural Components Intake

Non-canonical Molecular Targets for Novel Analgesics: Intracellular Calcium and HCN Channels

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