Mode of action of the plant-derived silphinenes on insect and mammalian GABA(A) receptor/chloride channel complex

Mode of action of the plant-derived silphinenes on insect and mammalian GABA(A) receptor/chloride channel complex

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7 pages, 6 figures, 1 table.-- Available online Dec 23, 2007.

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Main Authors: Bloomquist, Jeffrey R., Boina, Dhana Raj, Chow, Ella, Carlier, Paul R., Reina, Matías, González-Coloma, Azucena
Other Authors: Virginia Polytechnic Institute and State University
Format: artículo biblioteca
Language:English
Published: Elsevier 2008-05
Subjects:GABA antagonist, Senecio palmensis, Insecticide, Antifeedants, rdl,
Online Access:http://hdl.handle.net/10261/12619
http://dx.doi.org/10.13039/100007263
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spelling dig-ica-es-10261-126192009-04-27T22:00:00Z Mode of action of the plant-derived silphinenes on insect and mammalian GABA(A) receptor/chloride channel complex Bloomquist, Jeffrey R. Boina, Dhana Raj Chow, Ella Carlier, Paul R. Reina, Matías González-Coloma, Azucena Virginia Polytechnic Institute and State University Ministerio de Educación y Ciencia (España) GABA antagonist Senecio palmensis Insecticide Antifeedants rdl 7 pages, 6 figures, 1 table.-- Available online Dec 23, 2007. The silphinenes are tricyclic sesquiterpenes that have antifeedant and toxic effects in insects and structural similarity to the known GABA antagonist, picrotoxinin. In murine synaptoneurosomes, silphinenes block GABA-stimulated influx of Cl-36(−) with EC-50s in the range of 10–30 μM. In insects, silphinenes were tested in neurophysiological recordings of central neurons from third instar Drosophila melanogaster larvae. Silphinenes reversed the blockage of neuronal firing induced by GABA, but had little effect below 100 μM. The structure–activity profile observed in the murine chloride flux assay was also observed in the larval neurophysiological assay, indicating little selectivity for the silphinenes. A reference silphinene was equally active on nerve preparations from the rdl strain of D. melanogaster, which is resistant to channel-blocking antagonists via an altered GABA receptor. This latter finding suggests that silphinenes interact with the insect GABA receptor in a manner somewhat different from PTX, and that rdl resistance in the field may have little effect on silphinene efficacy. We thank the Virginia Tech Biological Sciences Initiative for funding this research, as well as Grant CTQ2006-15597-C02-01/PPQ from the government of Spain. 2009-04-28T07:18:12Z 2009-04-28T07:18:12Z 2008-05 artículo http://purl.org/coar/resource_type/c_6501 Pesticide Biochemistry and Physiology 91(1): 17-23 (2008) 0048-3575 http://hdl.handle.net/10261/12619 10.1016/j.pestbp.2007.12.002 http://dx.doi.org/10.13039/100007263 en http://dx.doi.org/10.1016/j.pestbp.2007.12.002 none 2373 bytes 358247 bytes text/plain application/pdf Elsevier
institution ICA ES
collection DSpace
country España
countrycode ES
component Bibliográfico
access En linea
databasecode dig-ica-es
tag biblioteca
region Europa del Sur
libraryname Biblioteca del ICA España
language English
topic GABA antagonist
Senecio palmensis
Insecticide
Antifeedants
rdl
GABA antagonist
Senecio palmensis
Insecticide
Antifeedants
rdl
spellingShingle GABA antagonist
Senecio palmensis
Insecticide
Antifeedants
rdl
GABA antagonist
Senecio palmensis
Insecticide
Antifeedants
rdl
Bloomquist, Jeffrey R.
Boina, Dhana Raj
Chow, Ella
Carlier, Paul R.
Reina, Matías
González-Coloma, Azucena
Mode of action of the plant-derived silphinenes on insect and mammalian GABA(A) receptor/chloride channel complex
description 7 pages, 6 figures, 1 table.-- Available online Dec 23, 2007.
author2 Virginia Polytechnic Institute and State University
author_facet Virginia Polytechnic Institute and State University
Bloomquist, Jeffrey R.
Boina, Dhana Raj
Chow, Ella
Carlier, Paul R.
Reina, Matías
González-Coloma, Azucena
format artículo
topic_facet GABA antagonist
Senecio palmensis
Insecticide
Antifeedants
rdl
author Bloomquist, Jeffrey R.
Boina, Dhana Raj
Chow, Ella
Carlier, Paul R.
Reina, Matías
González-Coloma, Azucena
author_sort Bloomquist, Jeffrey R.
title Mode of action of the plant-derived silphinenes on insect and mammalian GABA(A) receptor/chloride channel complex
title_short Mode of action of the plant-derived silphinenes on insect and mammalian GABA(A) receptor/chloride channel complex
title_full Mode of action of the plant-derived silphinenes on insect and mammalian GABA(A) receptor/chloride channel complex
title_fullStr Mode of action of the plant-derived silphinenes on insect and mammalian GABA(A) receptor/chloride channel complex
title_full_unstemmed Mode of action of the plant-derived silphinenes on insect and mammalian GABA(A) receptor/chloride channel complex
title_sort mode of action of the plant-derived silphinenes on insect and mammalian gaba(a) receptor/chloride channel complex
publisher Elsevier
publishDate 2008-05
url http://hdl.handle.net/10261/12619
http://dx.doi.org/10.13039/100007263
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