State-Dependent Blockade of Dorsal Root Ganglion Voltage-Gated Na<sup>+</sup> Channels by Anethole
Anethole is a phenolic compound synthesized by many aromatic plants. Anethole is a substance that humans can safely consume and has been studied for years as a biologically active molecule to treat a variety of conditions, including nerve damage, gastritis, inflammation, and nociception. Anethole is...
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| Format: | Article |
| Language: | English |
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MDPI AG
2024-01-01
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| Series: | International Journal of Molecular Sciences |
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| Online Access: | https://www.mdpi.com/1422-0067/25/2/1034 |
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| author | Luiz Moreira-Junior Jose Henrique Leal-Cardoso Antonio Carlos Cassola Joao Luis Carvalho-de-Souza |
| author_facet | Luiz Moreira-Junior Jose Henrique Leal-Cardoso Antonio Carlos Cassola Joao Luis Carvalho-de-Souza |
| author_sort | Luiz Moreira-Junior |
| collection | DOAJ |
| description | Anethole is a phenolic compound synthesized by many aromatic plants. Anethole is a substance that humans can safely consume and has been studied for years as a biologically active molecule to treat a variety of conditions, including nerve damage, gastritis, inflammation, and nociception. Anethole is thought to carry out its biological activities through direct interaction with ion channels. Anethole is beneficial for neurodegenerative Alzheimer’s and Parkinson’s diseases. Nevertheless, nothing has been investigated regarding the effects of anethole on voltage-gated Na+ channels (VGSCs), which are major players in neuronal function. We used cultured dorsal root ganglion neurons from neonatal rats as a source of natively expressed VGSCs for electrophysiological studies using the whole-cell patch-clamp technique. Our data show that anethole interacts directly with VGSCs. Anethole quickly blocks and unblocks (when removed) voltage-activated Na+ currents in this preparation in a fully reversible manner. Anethole’s binding affinity to these channels increases when the inactive states of these channels are populated, similar to lidocaine’s effect on the same channels. Our data show that anethole inhibits neuronal activity by blocking VGSCs in a state-dependent manner. These findings relate to the putative anesthetic activity attributable to anethole, in addition to its potential benefit in neurodegenerative diseases. |
| first_indexed | 2024-03-08T09:52:40Z |
| format | Article |
| id | doaj.art-37a64fd483e5408faa47a6f9c88e7675 |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-08T09:52:40Z |
| publishDate | 2024-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | International Journal of Molecular Sciences |
| spelling | doaj.art-37a64fd483e5408faa47a6f9c88e76752024-01-29T13:56:28ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672024-01-01252103410.3390/ijms25021034State-Dependent Blockade of Dorsal Root Ganglion Voltage-Gated Na<sup>+</sup> Channels by AnetholeLuiz Moreira-Junior0Jose Henrique Leal-Cardoso1Antonio Carlos Cassola2Joao Luis Carvalho-de-Souza3Department of Anesthesiology, University of Arizona, Tucson, AZ 85724, USASuperior Institute of Biomedical Sciences, State University of Ceará, Campus of Itaperi, Fortaleza 607402, CE, BrazilDepartment of Physiology and Biophysics, Biomedical Sciences Institute, University of Sao Paulo, São Paulo 05508, SP, BrazilDepartment of Anesthesiology, University of Arizona, Tucson, AZ 85724, USAAnethole is a phenolic compound synthesized by many aromatic plants. Anethole is a substance that humans can safely consume and has been studied for years as a biologically active molecule to treat a variety of conditions, including nerve damage, gastritis, inflammation, and nociception. Anethole is thought to carry out its biological activities through direct interaction with ion channels. Anethole is beneficial for neurodegenerative Alzheimer’s and Parkinson’s diseases. Nevertheless, nothing has been investigated regarding the effects of anethole on voltage-gated Na+ channels (VGSCs), which are major players in neuronal function. We used cultured dorsal root ganglion neurons from neonatal rats as a source of natively expressed VGSCs for electrophysiological studies using the whole-cell patch-clamp technique. Our data show that anethole interacts directly with VGSCs. Anethole quickly blocks and unblocks (when removed) voltage-activated Na+ currents in this preparation in a fully reversible manner. Anethole’s binding affinity to these channels increases when the inactive states of these channels are populated, similar to lidocaine’s effect on the same channels. Our data show that anethole inhibits neuronal activity by blocking VGSCs in a state-dependent manner. These findings relate to the putative anesthetic activity attributable to anethole, in addition to its potential benefit in neurodegenerative diseases.https://www.mdpi.com/1422-0067/25/2/1034anetholesodium channelstate-dependent blockadedorsal root ganglionpatch clamp |
| spellingShingle | Luiz Moreira-Junior Jose Henrique Leal-Cardoso Antonio Carlos Cassola Joao Luis Carvalho-de-Souza State-Dependent Blockade of Dorsal Root Ganglion Voltage-Gated Na<sup>+</sup> Channels by Anethole International Journal of Molecular Sciences anethole sodium channel state-dependent blockade dorsal root ganglion patch clamp |
| title | State-Dependent Blockade of Dorsal Root Ganglion Voltage-Gated Na<sup>+</sup> Channels by Anethole |
| title_full | State-Dependent Blockade of Dorsal Root Ganglion Voltage-Gated Na<sup>+</sup> Channels by Anethole |
| title_fullStr | State-Dependent Blockade of Dorsal Root Ganglion Voltage-Gated Na<sup>+</sup> Channels by Anethole |
| title_full_unstemmed | State-Dependent Blockade of Dorsal Root Ganglion Voltage-Gated Na<sup>+</sup> Channels by Anethole |
| title_short | State-Dependent Blockade of Dorsal Root Ganglion Voltage-Gated Na<sup>+</sup> Channels by Anethole |
| title_sort | state dependent blockade of dorsal root ganglion voltage gated na sup sup channels by anethole |
| topic | anethole sodium channel state-dependent blockade dorsal root ganglion patch clamp |
| url | https://www.mdpi.com/1422-0067/25/2/1034 |
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