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dc.contributor.authorBloomquist, Jeffrey R.en_US
dc.contributor.authorBoina, Dhana Rajen_US
dc.contributor.authorChow, Ellaen_US
dc.contributor.authorCarlier, Paul R.en_US
dc.contributor.authorReina, Matíasen_US
dc.contributor.authorGonzález-Coloma, Azucenaen_US
dc.date.accessioned2009-04-28T07:18:12Z-
dc.date.available2009-04-28T07:18:12Z-
dc.date.issued2008-05en_US
dc.identifier.citationPesticide Biochemistry and Physiology 91(1): 17-23 (2008)en_US
dc.identifier.issn0048-3575-
dc.identifier.urihttp://hdl.handle.net/10261/12619-
dc.description7 pages, 6 figures, 1 table.-- Available online Dec 23, 2007.-
dc.description.abstractThe 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.-
dc.description.sponsorshipWe 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.-
dc.format.extent2373 bytes-
dc.format.extent358247 bytes-
dc.format.mimetypetext/plain-
dc.format.mimetypeapplication/pdf-
dc.language.isoengen_US
dc.publisherElsevier-
dc.rightsclosedAccessen_US
dc.subjectGABA antagonist-
dc.subjectSenecio palmensis-
dc.subjectInsecticide-
dc.subjectAntifeedant-
dc.subjectrdl-
dc.titleMode of action of the plant-derived silphinenes on insect and mammalian GABA(A) receptor/chloride channel complexen_US
dc.typeArtículoen_US
dc.identifier.doi10.1016/j.pestbp.2007.12.002-
dc.relation.publisherversionhttp://dx.doi.org/10.1016/j.pestbp.2007.12.002-
dc.contributor.funderVirginia Polytechnic Institute and State University-
dc.contributor.funderMinisterio de Educación y Ciencia (España)-
dc.identifier.funderhttp://dx.doi.org/10.13039/100007263es_ES
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