Depressant effects of Agastache mexicana methanol extract and one of major metabolites tilianin
| dc.contributor.affiliation | Laboratorio de Neurofarmacología de Productos Naturales de la Dirección de Investigaciones en Neurociencias. Instituto Nacional de Psiquiatría "Ramón de la Fuente Muñiz", México, D.F.14370, México | |
| dc.contributor.email | enoch@uaem.mx (Samuel Estrada-Soto) | |
| dc.creator | González-Trujano, María Eva | es_ES |
| dc.creator | Ponce-Muñoz, Hilda | es_ES |
| dc.creator | Hidalgo-Figueroa, Sergio | es_ES |
| dc.creator | Navarrete-Vázquez, Gabriel | es_ES |
| dc.creator | Estrada-Soto, Samuel | es_ES |
| dc.date | 2015 | |
| dc.date.accessioned | 2025-09-10T18:31:53Z | |
| dc.date.accessioned | 2026-03-27T15:32:35Z | |
| dc.date.available | 2025-09-10T18:31:53Z | |
| dc.date.issued | 2015 | |
| dc.date.published | 2015 | |
| dc.description | Objective: To determine the depressant-like effects and the possible mechanism of action of tilianin isolated from active methanol extract of Agastache mexicana (A. mexicana). Also, to establish the pharmacophoric requirements of tilianin, as a possible ligand of GABAA/BZD receptor, by the alignment of diazepam, CGS-9896 and diindole, using a previously described pharmacophoric model. Methods: Tilianin (30 to 300 mg/kg, ip. and 300 mg/kg, po.) and methanol crude extract (10 to 300 mg/kg, ip. and 300 mg/kg po.) from A. mexicana were evaluated for potential sedative and anxiolytic-like response drugs by using open-field, hole-board, cylinder of exploration, plus-maze and sodium pentobarbital-induced hypnosis mice methods. Results: Methanol extract and tilianin showed anxiolytic-like activity from a dosage of 30 mg/kg, ip. or 300 mg/kg, po. and were less potent than diazepam 0.1 mg/kg, a reference anxiolytic drug used. Moreover, depressant activity of both potentiates sodium pentobarbital (SP)-induced sleeping time. The anxiolytic-like effect of 30 mg/kg ip. observed for the extract and tilianin, by using the plus-maze model, was partially prevented in the presence of flumazenil (a GABAA/BZD antagonist, 5 mg/kg ip.) but not in the presence of WAY 100635 (a selective 5-HT1A receptor antagonist, 0.32 mg/kg, ip.). Pharmacophoric modeling alignments of three agonist of GABAA/BZD allow identify seven chemical features. Tilianin contains six of the seven features previously determined. Conclusions: Results indicate that tilianin is one of the bioactive metabolites in the anxiolytic-like activity of A. mexicana, reinforcing its central nervous system uses, where GABAA/BZD, but not 5-HT1A, receptors are partially involved. | es_ES |
| dc.format | es_ES | |
| dc.identifier.doi | 10.1016/S1995-7645(14)60312-6 | |
| dc.identifier.eissn | 2352-4146 | |
| dc.identifier.issn | 1995-7645 | |
| dc.identifier.organizacion | Instituto Nacional de Psiquiatría Ramón de la Fuente Muñiz | |
| dc.identifier.place | India | |
| dc.identifier.uri | https://doi.org/10.1016/S1995-7645(14)60312-6 | |
| dc.identifier.uri | https://repositorio.inprf.gob.mx/handle/123456789/8408 | |
| dc.language.iso | eng | es_ES |
| dc.publisher | Wolters Kluwer | es_ES |
| dc.relation | 8(3):185-190 | |
| dc.relation.jnabreviado | ASIAN PAC J TROP MED | |
| dc.relation.journal | Asian Pacific Journal of Tropical Medicine | |
| dc.rights | Acceso Cerrado | es_ES |
| dc.subject.kw | Agastache mexicana | |
| dc.subject.kw | Anxiety | |
| dc.subject.kw | Benzodiazepine | |
| dc.subject.kw | Central nervous system | |
| dc.subject.kw | Sedative | |
| dc.subject.kw | Tilianin | |
| dc.title | Depressant effects of Agastache mexicana methanol extract and one of major metabolites tilianin | es_ES |
| dc.type | Artículo | es_ES |
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