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(-)-Adaline from the Adalia Genus of Ladybirds Is a Potent Antagonist of Insect and Specific Mammalian Nicotinic Acetylcholine Receptors.
Richards, David P; Patel, Rohit N; Duce, Ian R; Khambay, Bhupinder P S; Birkett, Michael A; Pickett, John A; Mellor, Ian R.
Afiliação
  • Richards DP; School of Life Sciences, University of Nottingham, University Park, Nottingham NG7 2RD, UK.
  • Patel RN; School of Life Sciences, University of Nottingham, University Park, Nottingham NG7 2RD, UK.
  • Duce IR; School of Life Sciences, University of Nottingham, University Park, Nottingham NG7 2RD, UK.
  • Khambay BPS; Protecting Crops and the Environment, Rothamsted Research, West Common, Harpenden AL5 2JQ, UK.
  • Birkett MA; Protecting Crops and the Environment, Rothamsted Research, West Common, Harpenden AL5 2JQ, UK.
  • Pickett JA; Protecting Crops and the Environment, Rothamsted Research, West Common, Harpenden AL5 2JQ, UK.
  • Mellor IR; School of Chemistry, Cardiff University, Cardiff CF10 3AT, UK.
Molecules ; 27(20)2022 Oct 20.
Article em En | MEDLINE | ID: mdl-36296666
Ladybird beetles (Coleoptera: Coccinellidae) possess strong chemical defences that are secreted in response to stress and are also found on the coating of eggs, which are rich in alkaloids that are responsible for their toxicity to other species. Recent studies have shown that alkaloids from several species of ladybird beetle can target nicotinic acetylcholine receptors (nAChRs) acting as receptor antagonists. Here, we have explored the actions of (-)-adaline, found in the 2-spot (Adalia bipunctata) and 10-spot (Adalia decempunctata) ladybirds, on both mammalian (α1ß1γδ, α7, α4ß2, α3ß4) and insect nAChRs using patch-clamp of TE671 cells and locust brain neurons natively expressing nAChRs, as well as two-electrode voltage clamp of Xenopus laevis oocytes recombinantly expressing nAChRs. All nAChR subtypes were antagonised by (-)-adaline in a time-dependent, voltage-dependent and non-competitive manner with the lowest IC50s at rat α3ß4 (0.10 µM) and locust neuron (1.28 µM) nAChRs, at a holding potential of -75 mV. The data imply that (-)-adaline acts as an open channel blocker of nAChRs.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Besouros / Receptores Nicotínicos / Alcaloides Limite: Animals Idioma: En Revista: Molecules Assunto da revista: BIOLOGIA Ano de publicação: 2022 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Besouros / Receptores Nicotínicos / Alcaloides Limite: Animals Idioma: En Revista: Molecules Assunto da revista: BIOLOGIA Ano de publicação: 2022 Tipo de documento: Article