Is the Membrane Lipid Matrix a Key Target for Action of Pharmacologically Active Plant Saponins?
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 an...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-03-01
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| Series: | International Journal of Molecular Sciences |
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| Online Access: | https://www.mdpi.com/1422-0067/22/6/3167 |
| _version_ | 1797540645493014528 |
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| author | Svetlana S. Efimova Olga S. Ostroumova |
| author_facet | Svetlana S. Efimova Olga S. Ostroumova |
| author_sort | Svetlana S. Efimova |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-03-10T13:04:07Z |
| format | Article |
| id | doaj.art-b194215e65c641b3bd695d7437876e52 |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-10T13:04:07Z |
| publishDate | 2021-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | International Journal of Molecular Sciences |
| spelling | doaj.art-b194215e65c641b3bd695d7437876e522023-11-21T11:17:51ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672021-03-01226316710.3390/ijms22063167Is the Membrane Lipid Matrix a Key Target for Action of Pharmacologically Active Plant Saponins?Svetlana S. Efimova0Olga S. Ostroumova1Institute of Cytology of Russian Academy of Sciences, 199034 Saint Petersburg, RussiaInstitute of Cytology of Russian Academy of Sciences, 199034 Saint Petersburg, RussiaThis 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.https://www.mdpi.com/1422-0067/22/6/3167saponinsterpeneslipid bilayersliposomesmembrane boundary potentiallipid melting |
| spellingShingle | Svetlana S. Efimova Olga S. Ostroumova Is the Membrane Lipid Matrix a Key Target for Action of Pharmacologically Active Plant Saponins? International Journal of Molecular Sciences saponins terpenes lipid bilayers liposomes membrane boundary potential lipid melting |
| title | Is the Membrane Lipid Matrix a Key Target for Action of Pharmacologically Active Plant Saponins? |
| title_full | Is the Membrane Lipid Matrix a Key Target for Action of Pharmacologically Active Plant Saponins? |
| title_fullStr | Is the Membrane Lipid Matrix a Key Target for Action of Pharmacologically Active Plant Saponins? |
| title_full_unstemmed | Is the Membrane Lipid Matrix a Key Target for Action of Pharmacologically Active Plant Saponins? |
| title_short | Is the Membrane Lipid Matrix a Key Target for Action of Pharmacologically Active Plant Saponins? |
| title_sort | is the membrane lipid matrix a key target for action of pharmacologically active plant saponins |
| topic | saponins terpenes lipid bilayers liposomes membrane boundary potential lipid melting |
| url | https://www.mdpi.com/1422-0067/22/6/3167 |
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