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Anticonvulsant activity of Tetrahydrolinalool: behavioral, electrophysiological, and molecular docking approaches.

Authors :
Fonsêca DV
da Silva PR
Pires HFO
Rocha JS
de Oliveira LEG
Reis FMS
Cavalho EBM
Pazos NDN
de Sousa NF
Guedes EC
Ribeiro LR
de Cassia S Sá R
Salvadori MGSS
Sousa DP
Scotti MT
Felipe CFB
de Almeida RN
Scotti L
Source :
ChemMedChem [ChemMedChem] 2024 Aug 01; Vol. 19 (15), pp. e202400135. Date of Electronic Publication: 2024 Jul 04.
Publication Year :
2024

Abstract

Tetrahydrolinalool (THL) is an acyclic monoterpene alcohol, produced during linalol metabolism and also a constituent of essential oils. As described in the literature, many monoterpenes present anticonvulsant properties, and thus we became interested in evaluating the anticonvulsant activity of Tetrahydrolinalool using in mice model as well as in silico approaches. Our results demonstrated that THL increased latency to seizure onset and also reduced the mortality, in picrotoxin induced seizure tests. The results may be related to GABAergic regulation, which was also suggested in seizure testing induced by 3-mercapto-propionic acid. In the strychnine-induced seizure testing, none of the groups pretreated with THL modulated the parameters indicative of anticonvulsant effect. The electrophysiological results revealed that THL treatment reduces seizures induced by pentylenetetrazole. The in silico molecular docking studies showed that the interaction between THL and a GABAA receptor model formed a stable complex, in comparison to the crystaligraphic structure of diazepam, a structurally related ligand. In conclusion, all the evidences showed that THL presents effective anticonvulsant activity related to the GABAergic pathway, being a candidate for treatment of epileptic syndromes.<br /> (© 2024 Wiley-VCH GmbH.)

Details

Language :
English
ISSN :
1860-7187
Volume :
19
Issue :
15
Database :
MEDLINE
Journal :
ChemMedChem
Publication Type :
Academic Journal
Accession number :
38687623
Full Text :
https://doi.org/10.1002/cmdc.202400135