Skip to main content

Research Repository

Advanced Search

(−)-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.

(−)-Adaline from the Adalia Genus of Ladybirds Is a Potent Antagonist of Insect and Specific Mammalian Nicotinic Acetylcholine Receptors Thumbnail


Authors

David P. Richards

Rohit N. Patel

Ian R. Duce

Bhupinder P. S. Khambay

Michael A. Birkett

John A. Pickett

Profile Image

IAN MELLOR IAN.MELLOR@NOTTINGHAM.AC.UK
Assistant Professor



Abstract

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 (α1β1γδ, α7, α4β2, α3β4) 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 α3β4 (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.

Citation

Richards, D. P., Patel, R. N., Duce, I. R., Khambay, B. P. S., Birkett, M. A., Pickett, J. A., & Mellor, I. R. (2022). (−)-Adaline from the Adalia Genus of Ladybirds Is a Potent Antagonist of Insect and Specific Mammalian Nicotinic Acetylcholine Receptors. Molecules, 27(20), Article 7074. https://doi.org/10.3390/molecules27207074

Journal Article Type Article
Acceptance Date Oct 17, 2022
Online Publication Date Oct 20, 2022
Publication Date Oct 2, 2022
Deposit Date Jan 11, 2023
Publicly Available Date Mar 28, 2024
Journal Molecules
Electronic ISSN 1420-3049
Publisher MDPI AG
Peer Reviewed Peer Reviewed
Volume 27
Issue 20
Article Number 7074
DOI https://doi.org/10.3390/molecules27207074
Keywords Chemistry (miscellaneous); Analytical Chemistry; Organic Chemistry; Physical and Theoretical Chemistry; Molecular Medicine; Drug Discovery; Pharmaceutical Science
Public URL https://nottingham-repository.worktribe.com/output/12624562
Publisher URL https://www.mdpi.com/1420-3049/27/20/7074

Files




You might also like



Downloadable Citations