Abstract
Transient receptor potential vanilloid member 1 (TRPV1) is activated in response to capsaicin, protons, temperature, and free reactive oxygen species (ROS) released from inflammatory molecules after exposure to harmful stimuli. The expression level of TRPV1 is elevated in the dorsal root ganglion, and its activation through capsaicin and ROS mediates neuropathic pain in mice. Its expression is high in peripheral and central nervous systems. Although pain is a response evolved for survival, many studies have been conducted to develop analgesics, but no clear results have been reported. Here, we found that naringin selectively inhibited capsaicin-stimulated inward currents in Xenopus oocytes using a two-electrode voltage clamp. The results of this study showed that naringin has an IC50 value of 33.3 μM on TRPV1. The amino acid residues D471 and N628 of TRPV1 were involved in its binding to naringin. Our study bridged the gap between the pain suppression effect of TRPV1 and the preventive effect of naringin on neuropathic pain and oxidation. Naringin had the same characteristics as a model selective antagonist, which is claimed to be ideal for the development of analgesics targeting TRPV1. Thus, this study suggests the applicability of naringin as a novel analgesic candidate through antioxidative and analgesic effects of naringin.
Highlights
IntroductionMany neurodegenerative dysfunctions are associated with excessive production of free reactive oxygen species (ROS), which may be eliminated or inhibited by antioxidants [1]
Introduction published maps and institutional affilMany neurodegenerative dysfunctions are associated with excessive production of free reactive oxygen species (ROS), which may be eliminated or inhibited by antioxidants [1].Herbal plants, including several fruits and vegetables, are compounds of natural antioxidants such as phenolic compounds and flavonoids, which exert antioxidant properties [2].Pain is a complex phenomenon attributed to the transmission of electrical signals through neurons to the brain [3,4]
Naringin was dissolved in dimethyl sulfoxide (DMSO) and further diluted in a bath solution to be used as a stock
Summary
Many neurodegenerative dysfunctions are associated with excessive production of free reactive oxygen species (ROS), which may be eliminated or inhibited by antioxidants [1]. Pain is a complex phenomenon attributed to the transmission of electrical signals through neurons to the brain [3,4]. It is a response evolved to protect our body from external and internal dangers and reduces our quality of life. Pain can be classified in various types but typically is categorized as neuropathic or nociceptive type [5]. Neuropathic pain is associated with the malfunction of the neuronal system in response to injury, disease, or inflammation and serves as a message to the brain [6,7]. Neuropathic pain is chronic when nociceptors interact with internal and external harmful stimuli, resulting in the generation iations
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