Alkaloids Modulate the Functioning of Ion Channels Produced by Antimicrobial Agents via an Influence on the Lipid Host

Frontiers in Cell and Developmental Biology
Svetlana S EfimovaOlga S Ostroumova

Abstract

It is widely recognized that an alteration in membrane physical properties induced by the adsorption of various drugs and biologically active compounds might greatly affect the functioning of peptides and proteins embedded in the membrane, in particular various ion channels. This study aimed to obtain deep insight into the diversity of the molecular mechanisms of membrane action of one of the most numerous and extremely important class of phytochemicals, the alkaloids. Protoalkaloids (derivatives of β-phenylethylamine, benzylamines, and colchicines), heterocyclic alkaloids (derivatives of purine, quinolysidine, piperidine, pyridine, quinoline, and isoquinoline), and steroid alkaloids were tested. We evaluated the effects of 22 compounds on lipid packing by investigating the thermotropic behavior of membrane lipids and the leakage of a fluorescent marker from unilamellar lipid vesicles. The alteration in the transmembrane distribution of the electrical potential was estimated by measuring the alkaloid induced changes in the boundary potential of planar lipid bilayers. We found that benzylamines, the chili pepper active components, capsaicin and dihydrocapsaicin, strongly affect not only the elastic properties of the lipid host, ...Continue Reading

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Citations

Apr 4, 2021·International Journal of Molecular Sciences·Svetlana S Efimova, Olga S Ostroumova

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Methods Mentioned

BETA
NMR
X-ray
gel filtration

Software Mentioned

pClamp
HyperChem
Calisto Processing
ChemAxon
Nys
Origin

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