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Antinociception produced by Thalassia testudinum extract BM-21 is mediated by the inhibition of acid sensing ionic channels by the phenolic compound thalassiolin B.
- Source :
-
Molecular pain [Mol Pain] 2011 Jan 24; Vol. 7, pp. 10. Date of Electronic Publication: 2011 Jan 24. - Publication Year :
- 2011
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Abstract
- Background: Acid-sensing ion channels (ASICs) have a significant role in the sensation of pain and constitute an important target for the search of new antinociceptive drugs. In this work we studied the antinociceptive properties of the BM-21 extract, obtained from the sea grass Thalassia testudinum, in chemical and thermal models of nociception in mice. The action of the BM-21 extract and the major phenolic component isolated from this extract, a sulphated flavone glycoside named thalassiolin B, was studied in the chemical nociception test and in the ASIC currents of the dorsal root ganglion (DRG) neurons obtained from Wistar rats.<br />Results: Behavioral antinociceptive experiments were made on male OF-1 mice. Single oral administration of BM-21 produced a significant inhibition of chemical nociception caused by acetic acid and formalin (specifically during its second phase), and increased the reaction time in the hot plate test. Thalassiolin B reduced the licking behavior during both the phasic and tonic phases in the formalin test. It was also found that BM-21 and thalassiolin B selectively inhibited the fast desensitizing (τ < 400 ms) ASIC currents in DRG neurons obtained from Wistar rats, with a nonsignificant action on ASIC currents with a slow desensitizing time-course. The action of thalassiolin B shows no pH or voltage dependence nor is it modified by steady-state ASIC desensitization or voltage. The high concentration of thalassiolin B in the extract may account for the antinociceptive action of BM-21.<br />Conclusions: To our knowledge, this is the first report of an ASIC-current inhibitor derived of a marine-plant extract, and in a phenolic compound. The antinociceptive effects of BM-21 and thalassiolin B may be partially because of this action on the ASICs. That the active components of the extract are able to cross the blood-brain barrier gives them an additional advantage for future uses as tools to study pain mechanisms with a potential therapeutic application.
- Subjects :
- Acid Sensing Ion Channels
Amiloride pharmacology
Animals
Complex Mixtures
Ganglia, Spinal drug effects
Ganglia, Spinal metabolism
Hydrogen-Ion Concentration drug effects
Ion Channel Gating drug effects
Male
Mice
Motor Activity drug effects
Nerve Tissue Proteins metabolism
Pain Measurement
Plant Extracts chemistry
Protons
Rats
Rotarod Performance Test
Sodium Channels metabolism
Temperature
Flavonoids pharmacology
Hydrocharitaceae chemistry
Nerve Tissue Proteins antagonists & inhibitors
Nociceptors metabolism
Phenols pharmacology
Plant Extracts pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1744-8069
- Volume :
- 7
- Database :
- MEDLINE
- Journal :
- Molecular pain
- Publication Type :
- Academic Journal
- Accession number :
- 21261973
- Full Text :
- https://doi.org/10.1186/1744-8069-7-10