Substance MCS-18 isolated from helleborus purpurascens is a potent antagonist of the capsaicin receptor, TRPV1, in rat cultured sensory neurons

Title:

Substance MCS-18 isolated from helleborus purpurascens is a potent antagonist of the capsaicin receptor, TRPV1, in rat cultured sensory neurons

Creator:

Neacsu, C., Ciobanu, C., Barbu, I., Toader, O., Szegli, G., Kerek, F., and Babes, A.

Identifier:

https://cdk.lib.cas.cz/client/handle/uuid:5ea5109c-1ec5-48b7-8f44-d077fd93a5e4
uuid:5ea5109c-1ec5-48b7-8f44-d077fd93a5e4

Subject:

Fyziologie člověka a srovnávací fyziologie, bolest, rostlinné extrakty, pain, plant extracts, TRP channels, DRG, capsaicin, 14, and 612

Type:

article, články, model:article, and TEXT

Format:

print

Description:

Extracts of Helleborus roots were traditionally used in the Balkan area for their analgesic action. We report that the pure natural product MCS-18 isolated from this source is a potent, specific and reversible antagonist of the capsaicin receptor, TRPV1, expressed in rat dorsal root ganglion (DRG) neurons. TRPV1 is a nonselective cation channel expressed in a subset of cutaneous and visceral sensory nerve endings and activated by noxious heat, acidity and fatty acid metabolites of arachidonic acid, with a decisive role in inflammatory heat hyperalgesia. MCS-18 inhibited the increase in intracellular calcium concentration evoked in DRG neurons by capsaicin (300 nM) and low pH (5.5) but not by heat (43 ºC). The substance had no effect on the responses mediated by acid-sensing ion channels (ASICs) or the irritant receptor TRPA1. Whole-cell patch-clamp was used to confirm the inhibition of capsaicin-induced currents by MCS-18 which was dose-dependent. The mechanism of inhibition does not require an intact cell, as capsaicin-induced currents were also inhibited in the excised outside-out configuration. The antagonism of the capsaicin and proton action on native TRPV1 by MCS-18 may be of interest for pain therapy., C. Neacsu ... [et al.]., and Obsahuje bibliografii a bibliografické odkazy

Language:

English

Rights:

http://creativecommons.org/licenses/by-nc-sa/4.0/
policy:public

Source:

Physiological research | 2010 Volume:59 | Number:2

Harvested from:

CDK

Metadata only:

false