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Lignan from thyme possesses inhibitory effect on ASIC3 channel current.
Dubinnyi MA
,
Osmakov DI
,
Koshelev SG
,
Kozlov SA
,
Andreev YA
,
Zakaryan NA
,
Dyachenko IA
,
Bondarenko DA
,
Arseniev AS
,
Grishin EV
.
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A novel compound was identified in the acidic extract of Thymus armeniacus collected in the Lake Sevan region of Armenia. This compound, named "sevanol," to our knowledge is the first low molecular weight natural molecule that has a reversible inhibition effect on both the transient and the sustained current of human ASIC3 channels expressed in Xenopus laevis oocytes. Sevanol completely blocked the transient component (IC(50) 353 ± 23 μM) and partially (∼45%) inhibited the amplitude of the sustained component (IC(50) of 234 ± 53 μM). Other types of acid-sensing ion channel (ASIC) channels were intact to sevanol application, except ASIC1a, which showed more than six times less affinity to it as compared with the inhibitory action on the ASIC3 channel. To elucidate the structure of sevanol, the set of NMR spectra in two solvents (d(6)-DMSO and D(2)O) was collected, and the complete chemical structure was confirmed by liquid chromatography-mass spectrometry with electrospray ionization (LC-ESI(+)-MS) fragmentation. This compound is a new lignan built up of epiphyllic acid and two isocitryl esters in positions 9 and 10. In vivo administration of sevanol (1-10 mg/kg) significantly reversed thermal hyperalgesia induced by complete Freund's adjuvant injection and reduced response to acid in a writhing test. Thus, we assume the probable considerable role of sevanol in known analgesic and anti-inflammatory properties of thyme.
Andreev,
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Andreev,
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,
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Andreev,
Molecules to selectively target receptors for treatment of pain and neurogenic inflammation.
2012,
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Baser,
Biological and pharmacological activities of carvacrol and carvacrol bearing essential oils.
2008,
Pubmed
Bässler,
Molecular and functional characterization of acid-sensing ion channel (ASIC) 1b.
2001,
Pubmed
,
Xenbase
Chen,
A role for ASIC3 in the modulation of high-intensity pain stimuli.
2002,
Pubmed
Das,
Anti-inflammatory responses of resveratrol.
2007,
Pubmed
Deval,
ASIC3, a sensor of acidic and primary inflammatory pain.
2008,
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Deval,
Acid-sensing ion channels (ASICs): pharmacology and implication in pain.
2010,
Pubmed
Diochot,
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2004,
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,
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Elhabazi,
Study on the antinociceptive effects of Thymus broussonetii Boiss extracts in mice and rats.
2006,
Pubmed
Escoubas,
Isolation of a tarantula toxin specific for a class of proton-gated Na+ channels.
2000,
Pubmed
,
Xenbase
Figueiredo,
Portuguese Thymbra and Thymus species volatiles: chemical composition and biological activities.
2008,
Pubmed
Garateix,
Antinociception produced by Thalassia testudinum extract BM-21 is mediated by the inhibition of acid sensing ionic channels by the phenolic compound thalassiolin B.
2011,
Pubmed
Grishin,
Novel peptide from spider venom inhibits P2X3 receptors and inflammatory pain.
2010,
Pubmed
Hazzit,
Composition of the essential oils of Thymus and Origanum species from Algeria and their antioxidant and antimicrobial activities.
2006,
Pubmed
Hesselager,
pH Dependency and desensitization kinetics of heterologously expressed combinations of acid-sensing ion channel subunits.
2004,
Pubmed
Hotta,
Carvacrol, a component of thyme oil, activates PPARalpha and gamma and suppresses COX-2 expression.
2010,
Pubmed
Jasti,
Structure of acid-sensing ion channel 1 at 1.9 A resolution and low pH.
2007,
Pubmed
Karczewski,
Reversal of acid-induced and inflammatory pain by the selective ASIC3 inhibitor, APETx2.
2010,
Pubmed
Kuduk,
Identification of non-amidine inhibitors of acid-sensing ion channel-3 (ASIC3).
2011,
Pubmed
Mahmoudi,
Anti-inflammatory and antinociceptive activity of Thymus pubescens extract.
2008,
Pubmed
Marino,
Antimicrobial activity of the essential oils of Thymus vulgaris L. measured using a bioimpedometric method.
1999,
Pubmed
Miura,
Antioxidant activity of chemical components from sage (Salvia officinalis L.) and thyme (Thymus vulgaris L.) measured by the oil stability index method.
2002,
Pubmed
NULL,
Removal of blood from laboratory mammals and birds. First report of the BVA/FRAME/RSPCA/UFAW Joint Working Group on Refinement.
1993,
Pubmed
Newcomb,
Selective peptide antagonist of the class E calcium channel from the venom of the tarantula Hysterocrates gigas.
1998,
Pubmed
,
Xenbase
Ramezani,
Antinociceptive effect of Elaeagnus angustifolia fruit seeds in mice.
2001,
Pubmed
Salinas,
Structural elements for the generation of sustained currents by the acid pain sensor ASIC3.
2009,
Pubmed
,
Xenbase
Voilley,
Nonsteroid anti-inflammatory drugs inhibit both the activity and the inflammation-induced expression of acid-sensing ion channels in nociceptors.
2001,
Pubmed