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Recent Progress in Health Benefits from Capsaicin and Its Analogues

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: closed (31 August 2022) | Viewed by 9551

Special Issue Editor


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Guest Editor
Department of Neural and Pain Sciences, School of Dentistry, Program in Neuroscience, Center to Advance Chronic Pain Research, University of Maryland, Baltimore, MD, USA
Interests: ion channels; pain; electrophysiology; nociceptors; transient receptor potential ion channels, trigeminal ganglia
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Special Issue Information

Dear Colleagues,

Capsaicin is an active ingredient in chili peppers that produces intense burning pain in humans. Capsaicin has been widely used as a food additive and as an invaluable tool in pain research. Despite its strong algogenic effect, capsaicin also has long been used as an analgesic agent. Recent development of a topical capsaicin formulation has greatly increased its clinical application for treating chronic pain from peripheral neuropathy. Therefore, capsaicin is a valuable non-opioidergic drug for alleviating pain with few side effects. Capsaicin has also been considered to treat wide variety of pathological conditions, such as psoriasis, obesity, urological, airway, cardiovascular and gastrointestinal disorders, and cancer. Not only capsaicin, but also its analogues, such as resiniferatoxin, are under active developments for treating intractable cancer pain in patients or domesticated animals.

This Special Issue is devoted to highlight recent developments of capsaicin or its analgoues for health benefits. The scope includes, but not limited to therapeutic effects of capsaicin or its analogues on various pathological conditions in humans or experimental animals, effects of capsaicin on cellular and neural responses under pathophysiological conditions, molecular mechanisms of capsaicin leading to therapeutic effects, novel delivery methods of capsaicin or its analogues in vivo or in humans, and novel development of capsaicin analogues to improve therapeutic efficacy and tolerance.

Prof. Dr. Man-Kyo Chung
Guest Editor

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Keywords

  • Capsaicin
  • Resiniferatoxin
  • TRPV1
  • Peripheral neuropathy
  • Pain
  • Itch
  • Clinical trials
  • Preclinical studies
  • Veterinary applications
  • Drug delivery

Published Papers (2 papers)

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Review

12 pages, 670 KiB  
Review
Capsaicin-Sensitive Vagal Afferent Nerve-Mediated Interoceptive Signals in the Esophagus
by Mingwei Yu, Crystal Chang, Bradley J. Undem and Shaoyong Yu
Molecules 2021, 26(13), 3929; https://doi.org/10.3390/molecules26133929 - 28 Jun 2021
Cited by 8 | Viewed by 4538
Abstract
Heartburn and non-cardiac chest pain are the predominant symptoms in many esophageal disorders, such as gastroesophageal reflux disease (GERD), non-erosive reflux disease (NERD), functional heartburn and chest pain, and eosinophilic esophagitis (EoE). At present, neuronal mechanisms underlying the process of interoceptive signals in [...] Read more.
Heartburn and non-cardiac chest pain are the predominant symptoms in many esophageal disorders, such as gastroesophageal reflux disease (GERD), non-erosive reflux disease (NERD), functional heartburn and chest pain, and eosinophilic esophagitis (EoE). At present, neuronal mechanisms underlying the process of interoceptive signals in the esophagus are still less clear. Noxious stimuli can activate a subpopulation of primary afferent neurons at their nerve terminals in the esophagus. The evoked action potentials are transmitted through both the spinal and vagal pathways to their central terminals, which synapse with the neurons in the central nervous system to induce esophageal nociception. Over the last few decades, progress has been made in our understanding on the peripheral and central neuronal mechanisms of esophageal nociception. In this review, we focus on the roles of capsaicin-sensitive vagal primary afferent nodose and jugular C-fiber neurons in processing nociceptive signals in the esophagus. We briefly compare their distinctive phenotypic features and functional responses to mechanical and chemical stimulations in the esophagus. Then, we summarize activation and/or sensitization effects of acid, inflammatory cells (eosinophils and mast cells), and mediators (ATP, 5-HT, bradykinin, adenosine, S1P) on these two nociceptive C-fiber subtypes. Lastly, we discuss the potential roles of capsaicin-sensitive esophageal afferent nerves in processing esophageal sensation and nociception. A better knowledge of the mechanism of nociceptive signal processes in primary afferent nerves in the esophagus will help to develop novel treatment approaches to relieve esophageal nociceptive symptoms, especially those that are refractory to proton pump inhibitors. Full article
(This article belongs to the Special Issue Recent Progress in Health Benefits from Capsaicin and Its Analogues)
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11 pages, 9436 KiB  
Review
Injectable Capsaicin for the Management of Pain Due to Osteoarthritis
by James N. Campbell, Randall Stevens, Peter Hanson, James Connolly, Diana S. Meske, Man-Kyo Chung and Benedict Duncan X. Lascelles
Molecules 2021, 26(4), 778; https://doi.org/10.3390/molecules26040778 - 3 Feb 2021
Cited by 20 | Viewed by 4132
Abstract
Capsaicin is a potent agonist of the TRPV1 channel, a transduction channel that is highly expressed in nociceptive fibers (pain fibers) throughout the peripheral nervous system. Given the importance of TRPV1 as one of several transduction channels in nociceptive fibers, much research has [...] Read more.
Capsaicin is a potent agonist of the TRPV1 channel, a transduction channel that is highly expressed in nociceptive fibers (pain fibers) throughout the peripheral nervous system. Given the importance of TRPV1 as one of several transduction channels in nociceptive fibers, much research has been focused on the potential therapeutic benefits of using TRPV1 antagonists for the management of pain. However, an antagonist has two limitations. First, an antagonist in principle generally only affects one receptor. Secondly, most antagonists must have an ongoing presence on the receptor to have an effect. Capsaicin overcomes both liabilities by disrupting peripheral terminals of nociceptive fibers that express TRPV1, and thereby affects all of the potential means of activating that pain fiber (not just TRPV1 function). This disruptive effect is dependent on the dose and can occur within minutes. Thus, unlike a typical receptor antagonist, continued bioavailability at the level of the receptor is not necessary. By disrupting the entire terminal of the TRPV1-expressing nociceptive fiber, capsaicin blocks all the activation mechanisms within that fiber, and not just TRPV1 function. Topical capsaicin, an FDA approved treatment for neuropathic pain, addresses pain from abnormal nociceptor activity in the superficial layers of the skin. Effects after a single administration are evident over a period of weeks to months, but in time are fully reversible. This review focuses on the rationale for using capsaicin by injection for painful conditions such as osteoarthritis (OA) and provides an update on studies completed to date. Full article
(This article belongs to the Special Issue Recent Progress in Health Benefits from Capsaicin and Its Analogues)
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