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Article

Is the Membrane Lipid Matrix a Key Target for Action of Pharmacologically Active Plant Saponins?

Institute of Cytology of Russian Academy of Sciences, 199034 Saint Petersburg, Russia
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Author to whom correspondence should be addressed.
Academic Editors: Marie-Laure Fauconnier and William N. Setzer
Int. J. Mol. Sci. 2021, 22(6), 3167; https://doi.org/10.3390/ijms22063167
Received: 5 February 2021 / Revised: 28 February 2021 / Accepted: 18 March 2021 / Published: 20 March 2021
This study was focused on the molecular mechanisms of action of saponins and related compounds (sapogenins and alkaloids) on model lipid membranes. Steroids and triterpenes were tested. A systematic analysis of the effects of these chemicals on the physicochemical properties of the lipid bilayers and on the formation and functionality of the reconstituted ion channels induced by antimicrobial agents was performed. It was found that digitonin, tribulosin, and dioscin substantially reduced the boundary potential of the phosphatidylcholine membranes. We concluded that saponins might affect the membrane boundary potential by restructuring the membrane hydration layer. Moreover, an increase in the conductance and lifetime of gramicidin A channels in the presence of tribulosin was due to an alteration in the membrane dipole potential. Differential scanning microcalorimetry data indicated the key role of the sapogenin core structure (steroid or triterpenic) in affecting lipid melting and disordering. We showed that an alteration in pore forming activity of syringomycin E by dioscin might be due to amendments in the lipid packing. We also found that the ability of saponins to disengage the fluorescent marker calcein from lipid vesicles might be also determined by their ability to induce a positive curvature stress. View Full-Text
Keywords: saponins; terpenes; lipid bilayers; liposomes; membrane boundary potential; lipid melting; calcein release; ion channel; gramicidin A; syringomycin E; nystatin saponins; terpenes; lipid bilayers; liposomes; membrane boundary potential; lipid melting; calcein release; ion channel; gramicidin A; syringomycin E; nystatin
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MDPI and ACS Style

Efimova, S.S.; Ostroumova, O.S. Is the Membrane Lipid Matrix a Key Target for Action of Pharmacologically Active Plant Saponins? Int. J. Mol. Sci. 2021, 22, 3167. https://doi.org/10.3390/ijms22063167

AMA Style

Efimova SS, Ostroumova OS. Is the Membrane Lipid Matrix a Key Target for Action of Pharmacologically Active Plant Saponins? International Journal of Molecular Sciences. 2021; 22(6):3167. https://doi.org/10.3390/ijms22063167

Chicago/Turabian Style

Efimova, Svetlana S., and Olga S. Ostroumova 2021. "Is the Membrane Lipid Matrix a Key Target for Action of Pharmacologically Active Plant Saponins?" International Journal of Molecular Sciences 22, no. 6: 3167. https://doi.org/10.3390/ijms22063167

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