Synthesis and Biological Studies of New Temporin A Analogs Containing Unnatural Amino Acids in Position 7

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creativework.keywordsantibacterial activity, antimicrobial peptides, antimicrobial resistance, antiproliferative activity, cytotoxicity, phototoxicity, solid-phase peptide synthesis, Temporin A
creativework.publisherMultidisciplinary Digital Publishing Institute (MDPI)en
dc.contributor.authorDimitrova D.
dc.contributor.authorNemska V.
dc.contributor.authorFoteva T.
dc.contributor.authorIliev I.
dc.contributor.authorGeorgieva N.
dc.contributor.authorDanalev D.
dc.date.accessioned2024-07-10T14:27:06Z
dc.date.accessioned2024-07-10T14:51:33Z
dc.date.available2024-07-10T14:27:06Z
dc.date.available2024-07-10T14:51:33Z
dc.date.issued2024-06-01
dc.description.abstract(1) Background: Antimicrobial resistance is growing at an extreme pace and has proven to be an urgent topic, for research into alternative treatments. Such a prospective possibility is hidden in antimicrobial peptides because of their low to no toxicity, effectiveness at low concentrations, and most importantly their ability to be used for multiple treatments. This work was focused on the study of the effect of the modification in position 7 of Temporin A on its biological activity; (2) Methods: The targeted peptides were synthesized using Fmoc/Ot-Bu SPPS. The antibacterial activity of the analogs was determined using the broth microdilution method and disk-diffusion method. In vitro tests were performed to determine the cytotoxicity, phototoxicity, and antiproliferative activity of the peptide analogs on a panel of tumor and normal cell lines; (3) Results: All analogs except DTCit showed good antibacterial activity, with DTDab having the best activity according to the disk-diffusion method. However, DTCit had an acceptable cytotoxicity, combined with good selectivity against the test MCF-7 cell line; (4) Conclusions: The obtained results revealed the importance of the basicity and length of the side chain at position 7 in the Temporin A sequence for both tested activities.
dc.identifier.doi10.3390/pharmaceutics16060716
dc.identifier.issn1999-4923
dc.identifier.scopusSCOPUS_ID:85197116601en
dc.identifier.urihttps://rlib.uctm.edu/handle/123456789/965
dc.language.isoen
dc.source.urihttps://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85197116601&origin=inward
dc.titleSynthesis and Biological Studies of New Temporin A Analogs Containing Unnatural Amino Acids in Position 7
dc.typeArticle
oaire.citation.issue6
oaire.citation.volume16
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