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Pharmacological profile of an essential oil derived from Melissa officinalis with anti-agitation properties: focus on ligand-gated channels

Pharmacological profile of an essential oil derived from Melissa officinalis with anti-agitation properties: focus on ligand-gated channels
Pharmacological profile of an essential oil derived from Melissa officinalis with anti-agitation properties: focus on ligand-gated channels
A dual radioligand binding and electrophysiological study, focusing on a range of ligand-gated ion channels, was performed with a chemically-validated essential oil derived from Melissa officinalis (MO), which has shown clinical benefit in treating agitation. MO inhibited binding of [S-35] t-butylbicyclophosphorothionate (TBPS) to the rat forebrain gamma-aminobutyric acid (GABA)A receptor channel (apparent IC50 0.040 +/- 0.001 mg mL(-1)), but had no effect on N-methyl-D-aspartate (NMDA), alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropianate (AMPA) or nicotinic acetylcholine receptors. Electrophysiological analyses with primary cultures of rat cortical neurons demonstrated that MO reversibly inhibited GABA-induced currents in a concentration-dependent manner (0.01-1 mg mL(-1)), whereas no inhibition of NMDA- or AMPA-induced currents was noted. Interestingly, MO elicited a significant dose-dependent reduction in both inhibitory and excitatory transmission, with a net depressant effect on neurotransmission (in contrast to the classical GABA(A) antagonist picrotoxinin which evoked profound epileptiform burst firing in these cells). The anti-agitation effects in patients and the depressant effects of MO in in-vitro we report in neural membranes are unlikely to reflect a sedative interaction with any of the ionotropic receptors examined here
receptor-binding, dementia, placebo-controlled trial, neurons, rat cortex, alzheimers-disease, behavioral symptoms, double-blind, rat, aromatherapy, laboratory-induced stress, lemon balm
0022-3573
377-384
Abuhamdah, Sawsan
33c655b6-f428-4ade-a742-109b9303ed47
Huang, Liping
bc24ed9b-1290-4073-8306-c9aa1626b8fc
Elliott, Mark S.J
5f8ce019-2a57-420a-bb78-d3adcc136cd4
Howes, Melanie-Jayne R
d76394b1-6172-4d68-8bd9-fff9c4da844b
Ballard, Clive
e244c4e5-5dd4-4c66-9efb-6bf2006bdb7e
Holmes, Clive
ada5abf3-8459-4cf7-be40-3f4e9391cc96
Burns, Alistair
3b42ceb2-cc8b-4159-807b-fe1bc095f723
Perry, Elaine K
72c7693b-d9c5-42a1-8346-eca3e5806921
Francis, Paul T
3c1916c5-598f-4540-8058-986e016b5adf
Lees, George
e3466d33-d282-4d5b-b942-5d5061687c48
Chazot, Paul L
ed3519ac-82a1-4aa1-88a7-7bbc8a6405fc
Abuhamdah, Sawsan
33c655b6-f428-4ade-a742-109b9303ed47
Huang, Liping
bc24ed9b-1290-4073-8306-c9aa1626b8fc
Elliott, Mark S.J
5f8ce019-2a57-420a-bb78-d3adcc136cd4
Howes, Melanie-Jayne R
d76394b1-6172-4d68-8bd9-fff9c4da844b
Ballard, Clive
e244c4e5-5dd4-4c66-9efb-6bf2006bdb7e
Holmes, Clive
ada5abf3-8459-4cf7-be40-3f4e9391cc96
Burns, Alistair
3b42ceb2-cc8b-4159-807b-fe1bc095f723
Perry, Elaine K
72c7693b-d9c5-42a1-8346-eca3e5806921
Francis, Paul T
3c1916c5-598f-4540-8058-986e016b5adf
Lees, George
e3466d33-d282-4d5b-b942-5d5061687c48
Chazot, Paul L
ed3519ac-82a1-4aa1-88a7-7bbc8a6405fc

Abuhamdah, Sawsan, Huang, Liping, Elliott, Mark S.J, Howes, Melanie-Jayne R, Ballard, Clive, Holmes, Clive, Burns, Alistair, Perry, Elaine K, Francis, Paul T, Lees, George and Chazot, Paul L (2008) Pharmacological profile of an essential oil derived from Melissa officinalis with anti-agitation properties: focus on ligand-gated channels. Journal of Pharmacy and Pharmacology, 60 (3), 377-384. (doi:10.1211/jpp.60.3.0014).

Record type: Article

Abstract

A dual radioligand binding and electrophysiological study, focusing on a range of ligand-gated ion channels, was performed with a chemically-validated essential oil derived from Melissa officinalis (MO), which has shown clinical benefit in treating agitation. MO inhibited binding of [S-35] t-butylbicyclophosphorothionate (TBPS) to the rat forebrain gamma-aminobutyric acid (GABA)A receptor channel (apparent IC50 0.040 +/- 0.001 mg mL(-1)), but had no effect on N-methyl-D-aspartate (NMDA), alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropianate (AMPA) or nicotinic acetylcholine receptors. Electrophysiological analyses with primary cultures of rat cortical neurons demonstrated that MO reversibly inhibited GABA-induced currents in a concentration-dependent manner (0.01-1 mg mL(-1)), whereas no inhibition of NMDA- or AMPA-induced currents was noted. Interestingly, MO elicited a significant dose-dependent reduction in both inhibitory and excitatory transmission, with a net depressant effect on neurotransmission (in contrast to the classical GABA(A) antagonist picrotoxinin which evoked profound epileptiform burst firing in these cells). The anti-agitation effects in patients and the depressant effects of MO in in-vitro we report in neural membranes are unlikely to reflect a sedative interaction with any of the ionotropic receptors examined here

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Published date: March 2008
Keywords: receptor-binding, dementia, placebo-controlled trial, neurons, rat cortex, alzheimers-disease, behavioral symptoms, double-blind, rat, aromatherapy, laboratory-induced stress, lemon balm

Identifiers

Local EPrints ID: 62226
URI: https://eprints.soton.ac.uk/id/eprint/62226
ISSN: 0022-3573
PURE UUID: 659fe773-5257-4b94-a9ab-740232aee7cb
ORCID for Clive Holmes: ORCID iD orcid.org/0000-0003-1999-6912

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Date deposited: 17 Sep 2008
Last modified: 05 Nov 2019 01:56

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Contributors

Author: Sawsan Abuhamdah
Author: Liping Huang
Author: Mark S.J Elliott
Author: Melanie-Jayne R Howes
Author: Clive Ballard
Author: Clive Holmes ORCID iD
Author: Alistair Burns
Author: Elaine K Perry
Author: Paul T Francis
Author: George Lees
Author: Paul L Chazot

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