Anticancer and Targeting Activity of Phytopharmaceutical Structural Analogs of a Natural Peptide from <i>Trichoderma longibrachiatum</i> and Related Peptide-Decorated Gold Nanoparticles
In the large field of bioactive peptides, peptaibols represent a unique class of compounds. They are membrane-active peptides, produced by fungi of the genus <i>Trichoderma</i> and known to elicit plant defenses. Among the short-length peptaibols, trichogin GA IV is nonhemolytic, proteol...
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| Format: | Article |
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MDPI AG
2023-03-01
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| Series: | International Journal of Molecular Sciences |
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| Online Access: | https://www.mdpi.com/1422-0067/24/6/5537 |
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| author | Francesca Moret Luca Menilli Celeste Milani Giorgia Di Cintio Chiara Dalla Torre Vincenzo Amendola Marta De Zotti |
| author_facet | Francesca Moret Luca Menilli Celeste Milani Giorgia Di Cintio Chiara Dalla Torre Vincenzo Amendola Marta De Zotti |
| author_sort | Francesca Moret |
| collection | DOAJ |
| description | In the large field of bioactive peptides, peptaibols represent a unique class of compounds. They are membrane-active peptides, produced by fungi of the genus <i>Trichoderma</i> and known to elicit plant defenses. Among the short-length peptaibols, trichogin GA IV is nonhemolytic, proteolysis-resistant, antibacterial, and cytotoxic. Several trichogin analogs are endowed with potent activity against phytopathogens, thus representing a sustainable alternative to copper for plant protection. In this work, we tested the activity of trichogin analogs against a breast cancer cell line and a normal cell line of the same derivation. Lys-containing trichogins showed an IC<sub>50</sub> below 12 µM, a peptide concentration not significantly affecting the viability of normal cells. Two analogs were found to be membrane-active but noncytotoxic. They were anchored to gold nanoparticles (GNPs) and further investigated for their ability to act as targeting agents. GNP uptake by cancer cells increased with peptide decoration, while it decreased in the corresponding normal epithelial cells. This work highlights the promising biological properties of peptaibol analogs in the field of cancer therapy either as cytotoxic molecules or as active targeting agents in drug delivery. |
| first_indexed | 2024-03-11T06:25:43Z |
| format | Article |
| id | doaj.art-088a7a0bd2b442e7b5139a012a4ea1c5 |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-11T06:25:43Z |
| publishDate | 2023-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | International Journal of Molecular Sciences |
| spelling | doaj.art-088a7a0bd2b442e7b5139a012a4ea1c52023-11-17T11:35:19ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672023-03-01246553710.3390/ijms24065537Anticancer and Targeting Activity of Phytopharmaceutical Structural Analogs of a Natural Peptide from <i>Trichoderma longibrachiatum</i> and Related Peptide-Decorated Gold NanoparticlesFrancesca Moret0Luca Menilli1Celeste Milani2Giorgia Di Cintio3Chiara Dalla Torre4Vincenzo Amendola5Marta De Zotti6Department of Biology, University of Padova, 35131 Padova, ItalyDepartment of Biology, University of Padova, 35131 Padova, ItalyDepartment of Biology, University of Padova, 35131 Padova, ItalyDepartment of Chemical Sciences, University of Padova, 35131 Padova, ItalyDepartment of Chemical Sciences, University of Padova, 35131 Padova, ItalyDepartment of Chemical Sciences, University of Padova, 35131 Padova, ItalyDepartment of Chemical Sciences, University of Padova, 35131 Padova, ItalyIn the large field of bioactive peptides, peptaibols represent a unique class of compounds. They are membrane-active peptides, produced by fungi of the genus <i>Trichoderma</i> and known to elicit plant defenses. Among the short-length peptaibols, trichogin GA IV is nonhemolytic, proteolysis-resistant, antibacterial, and cytotoxic. Several trichogin analogs are endowed with potent activity against phytopathogens, thus representing a sustainable alternative to copper for plant protection. In this work, we tested the activity of trichogin analogs against a breast cancer cell line and a normal cell line of the same derivation. Lys-containing trichogins showed an IC<sub>50</sub> below 12 µM, a peptide concentration not significantly affecting the viability of normal cells. Two analogs were found to be membrane-active but noncytotoxic. They were anchored to gold nanoparticles (GNPs) and further investigated for their ability to act as targeting agents. GNP uptake by cancer cells increased with peptide decoration, while it decreased in the corresponding normal epithelial cells. This work highlights the promising biological properties of peptaibol analogs in the field of cancer therapy either as cytotoxic molecules or as active targeting agents in drug delivery.https://www.mdpi.com/1422-0067/24/6/5537phytochemicalpeptaibolantitumor peptidebreast cancerpeptide-decorated gold nanoparticles |
| spellingShingle | Francesca Moret Luca Menilli Celeste Milani Giorgia Di Cintio Chiara Dalla Torre Vincenzo Amendola Marta De Zotti Anticancer and Targeting Activity of Phytopharmaceutical Structural Analogs of a Natural Peptide from <i>Trichoderma longibrachiatum</i> and Related Peptide-Decorated Gold Nanoparticles International Journal of Molecular Sciences phytochemical peptaibol antitumor peptide breast cancer peptide-decorated gold nanoparticles |
| title | Anticancer and Targeting Activity of Phytopharmaceutical Structural Analogs of a Natural Peptide from <i>Trichoderma longibrachiatum</i> and Related Peptide-Decorated Gold Nanoparticles |
| title_full | Anticancer and Targeting Activity of Phytopharmaceutical Structural Analogs of a Natural Peptide from <i>Trichoderma longibrachiatum</i> and Related Peptide-Decorated Gold Nanoparticles |
| title_fullStr | Anticancer and Targeting Activity of Phytopharmaceutical Structural Analogs of a Natural Peptide from <i>Trichoderma longibrachiatum</i> and Related Peptide-Decorated Gold Nanoparticles |
| title_full_unstemmed | Anticancer and Targeting Activity of Phytopharmaceutical Structural Analogs of a Natural Peptide from <i>Trichoderma longibrachiatum</i> and Related Peptide-Decorated Gold Nanoparticles |
| title_short | Anticancer and Targeting Activity of Phytopharmaceutical Structural Analogs of a Natural Peptide from <i>Trichoderma longibrachiatum</i> and Related Peptide-Decorated Gold Nanoparticles |
| title_sort | anticancer and targeting activity of phytopharmaceutical structural analogs of a natural peptide from i trichoderma longibrachiatum i and related peptide decorated gold nanoparticles |
| topic | phytochemical peptaibol antitumor peptide breast cancer peptide-decorated gold nanoparticles |
| url | https://www.mdpi.com/1422-0067/24/6/5537 |
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