Preparation of Terpenoid-Invasomes with Selective Activity against <i>S. aureus</i> and Characterization by Cryo Transmission Electron Microscopy
Terpenoids are natural plant-derived products that are applied to treat a broad range of human diseases, such as airway infections and inflammation. However, pharmaceutical applications of terpenoids against bacterial infection remain challenging due to their poor water solubility. Here, we produce...
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| Format: | Article |
| Language: | English |
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MDPI AG
2020-05-01
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| Series: | Biomedicines |
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| Online Access: | https://www.mdpi.com/2227-9059/8/5/105 |
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| author | Bernhard P. Kaltschmidt Inga Ennen Johannes F. W. Greiner Robin Dietsch Anant Patel Barbara Kaltschmidt Christian Kaltschmidt Andreas Hütten |
| author_facet | Bernhard P. Kaltschmidt Inga Ennen Johannes F. W. Greiner Robin Dietsch Anant Patel Barbara Kaltschmidt Christian Kaltschmidt Andreas Hütten |
| author_sort | Bernhard P. Kaltschmidt |
| collection | DOAJ |
| description | Terpenoids are natural plant-derived products that are applied to treat a broad range of human diseases, such as airway infections and inflammation. However, pharmaceutical applications of terpenoids against bacterial infection remain challenging due to their poor water solubility. Here, we produce invasomes encapsulating thymol, menthol, camphor and 1,8-cineol, characterize them via cryo transmission electron microscopy and assess their bactericidal properties. While control- and cineol-invasomes are similarly distributed between unilamellar and bilamellar vesicles, a shift towards unilamellar invasomes is observable after encapsulation of thymol, menthol or camphor. Thymol- and camphor-invasomes show a size reduction, whereas menthol-invasomes are enlarged and cineol-invasomes remain unchanged compared to control. While thymol-invasomes lead to the strongest growth inhibition of <i>S. aureus</i>, camphor- or cineol-invasomes mediate cell death and <i>S. aureus</i> growth is not affected by menthol-invasomes. Flow cytometric analysis validate that invasomes comprising thymol are highly bactericidal to <i>S. aureus</i>. Notably, treatment with thymol-invasomes does not affect survival of Gram-negative <i>E. coli.</i> In summary, we successfully produce terpenoid-invasomes and demonstrate that particularly thymol-invasomes show a strong selective activity against Gram-positive bacteria. Our findings provide a promising approach to increase the bioavailability of terpenoid-based drugs and may be directly applicable for treating severe bacterial infections such as methicillin-resistant <i>S. aureus</i>. |
| first_indexed | 2024-03-10T20:06:08Z |
| format | Article |
| id | doaj.art-0930de264efe4e0b91da0d910988be58 |
| institution | Directory Open Access Journal |
| issn | 2227-9059 |
| language | English |
| last_indexed | 2024-03-10T20:06:08Z |
| publishDate | 2020-05-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Biomedicines |
| spelling | doaj.art-0930de264efe4e0b91da0d910988be582023-11-19T23:12:49ZengMDPI AGBiomedicines2227-90592020-05-018510510.3390/biomedicines8050105Preparation of Terpenoid-Invasomes with Selective Activity against <i>S. aureus</i> and Characterization by Cryo Transmission Electron MicroscopyBernhard P. Kaltschmidt0Inga Ennen1Johannes F. W. Greiner2Robin Dietsch3Anant Patel4Barbara Kaltschmidt5Christian Kaltschmidt6Andreas Hütten7Thin Films & Physics of Nanostructures, Bielefeld University, Universitätsstrasse 25, 33615 Bielefeld, GermanyThin Films & Physics of Nanostructures, Bielefeld University, Universitätsstrasse 25, 33615 Bielefeld, GermanyDepartment of Cell Biology, Bielefeld University, Universitätsstrasse 25, 33615 Bielefeld, GermanyFermentation and Formulation of Biologicals and Chemicals, Bielefeld University of Applied Sciences, Interaktion 1, 33619 Bielefeld, GermanyFermentation and Formulation of Biologicals and Chemicals, Bielefeld University of Applied Sciences, Interaktion 1, 33619 Bielefeld, GermanyDepartment of Cell Biology, Bielefeld University, Universitätsstrasse 25, 33615 Bielefeld, GermanyDepartment of Cell Biology, Bielefeld University, Universitätsstrasse 25, 33615 Bielefeld, GermanyThin Films & Physics of Nanostructures, Bielefeld University, Universitätsstrasse 25, 33615 Bielefeld, GermanyTerpenoids are natural plant-derived products that are applied to treat a broad range of human diseases, such as airway infections and inflammation. However, pharmaceutical applications of terpenoids against bacterial infection remain challenging due to their poor water solubility. Here, we produce invasomes encapsulating thymol, menthol, camphor and 1,8-cineol, characterize them via cryo transmission electron microscopy and assess their bactericidal properties. While control- and cineol-invasomes are similarly distributed between unilamellar and bilamellar vesicles, a shift towards unilamellar invasomes is observable after encapsulation of thymol, menthol or camphor. Thymol- and camphor-invasomes show a size reduction, whereas menthol-invasomes are enlarged and cineol-invasomes remain unchanged compared to control. While thymol-invasomes lead to the strongest growth inhibition of <i>S. aureus</i>, camphor- or cineol-invasomes mediate cell death and <i>S. aureus</i> growth is not affected by menthol-invasomes. Flow cytometric analysis validate that invasomes comprising thymol are highly bactericidal to <i>S. aureus</i>. Notably, treatment with thymol-invasomes does not affect survival of Gram-negative <i>E. coli.</i> In summary, we successfully produce terpenoid-invasomes and demonstrate that particularly thymol-invasomes show a strong selective activity against Gram-positive bacteria. Our findings provide a promising approach to increase the bioavailability of terpenoid-based drugs and may be directly applicable for treating severe bacterial infections such as methicillin-resistant <i>S. aureus</i>.https://www.mdpi.com/2227-9059/8/5/105terpenoidsinvasomesthymolmentholcamphorcineol |
| spellingShingle | Bernhard P. Kaltschmidt Inga Ennen Johannes F. W. Greiner Robin Dietsch Anant Patel Barbara Kaltschmidt Christian Kaltschmidt Andreas Hütten Preparation of Terpenoid-Invasomes with Selective Activity against <i>S. aureus</i> and Characterization by Cryo Transmission Electron Microscopy Biomedicines terpenoids invasomes thymol menthol camphor cineol |
| title | Preparation of Terpenoid-Invasomes with Selective Activity against <i>S. aureus</i> and Characterization by Cryo Transmission Electron Microscopy |
| title_full | Preparation of Terpenoid-Invasomes with Selective Activity against <i>S. aureus</i> and Characterization by Cryo Transmission Electron Microscopy |
| title_fullStr | Preparation of Terpenoid-Invasomes with Selective Activity against <i>S. aureus</i> and Characterization by Cryo Transmission Electron Microscopy |
| title_full_unstemmed | Preparation of Terpenoid-Invasomes with Selective Activity against <i>S. aureus</i> and Characterization by Cryo Transmission Electron Microscopy |
| title_short | Preparation of Terpenoid-Invasomes with Selective Activity against <i>S. aureus</i> and Characterization by Cryo Transmission Electron Microscopy |
| title_sort | preparation of terpenoid invasomes with selective activity against i s aureus i and characterization by cryo transmission electron microscopy |
| topic | terpenoids invasomes thymol menthol camphor cineol |
| url | https://www.mdpi.com/2227-9059/8/5/105 |
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