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© 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.

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.

Details

Title
Antioxidative and Analgesic Effects of Naringin through Selective Inhibition of Transient Receptor Potential Vanilloid Member 1
Author
Eom, Sanung 1 ; Bo-Bae, Lee 2 ; Lee, Shinhui 1   VIAFID ORCID Logo  ; Park, Youngseo 1 ; Hye Duck Yeom 1 ; Kim, Tae-Hwan 3   VIAFID ORCID Logo  ; Seung-Hee Nam 4 ; Lee, Junho H 1   VIAFID ORCID Logo 

 Department of Biotechnology, Chonnam National University, Gwangju 61186, Korea; [email protected] (S.E.); [email protected] (S.L.); [email protected] (Y.P.); [email protected] (H.D.Y.) 
 Fruit Research Institute of Jeollanamdo Agricultural Research and Extension Services, Haenam, Naju 59021, Korea; [email protected] 
 Department of Animal Science, Chonnam National University, Gwangju 61186, Korea; [email protected] 
 Institute of Agricultural Science and Technology, Chonnam National University, Gwangju 61186, Korea 
First page
64
Publication year
2022
Publication date
2022
Publisher
MDPI AG
e-ISSN
20763921
Source type
Scholarly Journal
Language of publication
English
ProQuest document ID
2621248424
Copyright
© 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.