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Pharmacological profile of essential oils derived from Lavandula angustifolia and Melissa officinalis with anti-agitation properties: focus on ligand-gated channels

Pharmacological profile of essential oils derived from Lavandula angustifolia and Melissa officinalis with anti-agitation properties: focus on ligand-gated channels
Pharmacological profile of essential oils derived from Lavandula angustifolia and Melissa officinalis with anti-agitation properties: focus on ligand-gated channels
Both Melissa officinalis (Mo) and Lavandula angustifolia (La) essential oils have putative anti-agitation properties in humans, indicating common components with a depressant action in the central nervous system. 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 La, which has shown clinical benefit in treating agitation. La inhibited [35S] TBPS binding 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-isoxazolepropionic acid (AMPA) or nicotinic acetylcholine receptors. A 50:50 mixture of Mo and La essential oils inhibited [3H] flunitrazepam binding, whereas the individual oils had no significant effect. Electrophysiological analyses with rat cortical primary cultures demonstrated that La 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. La elicited a significant dose-dependent reduction in both inhibitory and excitatory transmission, with a net depressant effect on neurotransmission (in contrast to the classic GABA(A) antagonist picrotoxin which evoked profound epileptiform burst firing in these cells). These properties are similar to those recently reported for Mo. The anti-agitation effects in patients and the depressant effects of La we report in neural membranes in-vitro are unlikely to reflect a sedative interaction with any of the ionotropic receptors examined here. These data suggest that components common to the two oils are worthy of focus to identify the actives underlying the neuronal depressant and anti-agitation activities reported.
0022-3573
267
Huang, Liping
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Abuhamdah, Sawsan
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Howes, Melanie-Jayne R.
ef66d5ae-cde1-4f81-a23d-3581516ab3cd
Dixon, Christine L.
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Elliot, Mark S.J.
a8dda288-4f0b-482d-924a-52b4e15de749
Ballard, Clive
e244c4e5-5dd4-4c66-9efb-6bf2006bdb7e
Holmes, Clive
ada5abf3-8459-4cf7-be40-3f4e9391cc96
Burns, Alistair
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Perry, Elaine K.
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Francis, Paul T.
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Lees, George
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Chazot, Paul L.
7210d43e-7a5a-4b90-a5ef-68e32e5698e7
Huang, Liping
bc24ed9b-1290-4073-8306-c9aa1626b8fc
Abuhamdah, Sawsan
33c655b6-f428-4ade-a742-109b9303ed47
Howes, Melanie-Jayne R.
ef66d5ae-cde1-4f81-a23d-3581516ab3cd
Dixon, Christine L.
77760dc6-648e-4ef6-8f49-8390db8449c8
Elliot, Mark S.J.
a8dda288-4f0b-482d-924a-52b4e15de749
Ballard, Clive
e244c4e5-5dd4-4c66-9efb-6bf2006bdb7e
Holmes, Clive
ada5abf3-8459-4cf7-be40-3f4e9391cc96
Burns, Alistair
3b42ceb2-cc8b-4159-807b-fe1bc095f723
Perry, Elaine K.
6ac4d5db-e9ed-4e4c-b7bf-29929cc42825
Francis, Paul T.
dd258c08-f8e0-4ec7-899d-8ccea3673801
Lees, George
e3466d33-d282-4d5b-b942-5d5061687c48
Chazot, Paul L.
7210d43e-7a5a-4b90-a5ef-68e32e5698e7

Huang, Liping, Abuhamdah, Sawsan, Howes, Melanie-Jayne R., Dixon, Christine L., Elliot, Mark S.J., Ballard, Clive, Holmes, Clive, Burns, Alistair, Perry, Elaine K., Francis, Paul T., Lees, George and Chazot, Paul L. (2009) Pharmacological profile of essential oils derived from Lavandula angustifolia and Melissa officinalis with anti-agitation properties: focus on ligand-gated channels. Journal of Pharmacy and Pharmacology, 61 (2), 267.

Record type: Article

Abstract

Both Melissa officinalis (Mo) and Lavandula angustifolia (La) essential oils have putative anti-agitation properties in humans, indicating common components with a depressant action in the central nervous system. 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 La, which has shown clinical benefit in treating agitation. La inhibited [35S] TBPS binding 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-isoxazolepropionic acid (AMPA) or nicotinic acetylcholine receptors. A 50:50 mixture of Mo and La essential oils inhibited [3H] flunitrazepam binding, whereas the individual oils had no significant effect. Electrophysiological analyses with rat cortical primary cultures demonstrated that La 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. La elicited a significant dose-dependent reduction in both inhibitory and excitatory transmission, with a net depressant effect on neurotransmission (in contrast to the classic GABA(A) antagonist picrotoxin which evoked profound epileptiform burst firing in these cells). These properties are similar to those recently reported for Mo. The anti-agitation effects in patients and the depressant effects of La we report in neural membranes in-vitro are unlikely to reflect a sedative interaction with any of the ionotropic receptors examined here. These data suggest that components common to the two oils are worthy of focus to identify the actives underlying the neuronal depressant and anti-agitation activities reported.

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Published date: February 2009

Identifiers

Local EPrints ID: 152275
URI: http://eprints.soton.ac.uk/id/eprint/152275
ISSN: 0022-3573
PURE UUID: 79c9716a-5259-4f63-a276-125fe82fa32e
ORCID for Clive Holmes: ORCID iD orcid.org/0000-0003-1999-6912

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Date deposited: 14 May 2010 08:19
Last modified: 08 Jan 2022 02:50

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Contributors

Author: Liping Huang
Author: Sawsan Abuhamdah
Author: Melanie-Jayne R. Howes
Author: Christine L. Dixon
Author: Mark S.J. Elliot
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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