Diosmetin as a novel transient receptor potential vanilloid 1 antagonist with antinociceptive activity in mice.
Analgesics
/ administration & dosage
Animals
Calcium
/ metabolism
Capsaicin
/ pharmacology
Disease Models, Animal
Diterpenes
/ metabolism
Dose-Response Relationship, Drug
Flavonoids
/ administration & dosage
Inflammation
/ drug therapy
Male
Mice
Neuralgia
/ drug therapy
Pain
/ drug therapy
Pain Measurement
Spinal Cord
/ drug effects
Synaptosomes
/ drug effects
TRPV Cation Channels
/ antagonists & inhibitors
Toxicity Tests
Capsaicin
Diosmin
Inflammation
Neuropathy
Pain
Resiniferatoxin
Journal
Life sciences
ISSN: 1879-0631
Titre abrégé: Life Sci
Pays: Netherlands
ID NLM: 0375521
Informations de publication
Date de publication:
01 Jan 2019
01 Jan 2019
Historique:
received:
03
08
2018
revised:
01
11
2018
accepted:
12
11
2018
pubmed:
18
11
2018
medline:
8
1
2019
entrez:
18
11
2018
Statut:
ppublish
Résumé
Diosmetin is an O‑methylated flavone found naturally in citrus fruit, and it was identified in Amphilophium crucigerum (L.), a plant popularly used as an analgesic. This compound had different pharmacological effects and presented a chemical structure like the flavonoid eriodyctiol that exhibited antinociceptive effects by TRPV1 antagonism. However, the possible antinociceptive effect of this compound was not well documented. Thus, the goal of the present study was to evaluate the antinociceptive effect of diosmetin and its mechanism of action. The diosmetin effect on different pain models and its possible adverse effects were assessed on adult Swiss male mice (25-30 g). Mice spinal cord samples were used on calcium influx and binding assays using TRPV1 agonists. First, it was observed that the diosmetin reduced calcium influx mediated by capsaicin in synaptosomes and displace the specific binding to [
Identifiants
pubmed: 30447303
pii: S0024-3205(18)30734-3
doi: 10.1016/j.lfs.2018.11.029
pii:
doi:
Substances chimiques
Analgesics
0
Diterpenes
0
Flavonoids
0
TRPV Cation Channels
0
TRPV1 protein, mouse
0
resiniferatoxin
A5O6P1UL4I
Capsaicin
S07O44R1ZM
Calcium
SY7Q814VUP
diosmetin
TWZ37241OT
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
215-226Informations de copyright
Copyright © 2018 Elsevier Inc. All rights reserved.