Synthesis and Biological Studies on (KLAKLAK)2-NH2 Analog Containing Unnatural Amino Acid β-Ala and Conjugates with Second Pharmacophore

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dc.contributor.authorSirine Jaber
dc.contributor.authorVeronica Nemska
dc.contributor.authorIvan Iliev
dc.contributor.authorElena Ivanova
dc.contributor.authorTsvetelina Foteva
dc.contributor.authorNelly Georgieva
dc.contributor.authorIvan Givechev
dc.contributor.authorEmilia Naydenova
dc.contributor.authorVeronika Karadjova
dc.contributor.authorDancho Danalev
dc.date.accessioned2024-05-10T06:59:44Z
dc.date.available2024-05-10T06:59:44Z
dc.date.issued2021-12-02
dc.description.abstract<jats:p>(1) Background: Peptides are good candidates for anticancer drugs due to their natural existence in the body and lack of secondary effects. (KLAKLAK)2 is an antimicrobial peptide that also shows good anticancer properties. (2) Methods: The Solid Phase Peptide Synthesis (Fmoc-strategy) was used for the synthesis of target molecules, analogs of (KLAKLAK)2-NH2. The purity of all compounds was monitored by HPLC, and their structures were proven using mass spectrometry. Cytotoxicity and antiproliferative effects were studied using 3T3 NRU and MTT tests, respectively. For determination of antimicrobial activity, the disc-diffusion method was used. Hydrolytic stability at three pH values, which mimic the physiological pH in the body, was investigated by means of the HPLC technique. (3) Results: A good selective index against MCF-7 tumor cell lines, combined with good cytotoxicity and antiproliferative properties, was revealed for conjugates NphtG-(KLAKLAK)2-NH2 and Caf-(KLAKLAK)2-NH2. The same compounds showed very good antifungal properties and complete hydrolytic stability for 72 h. The compound Caf-(KLβ-AKLβ-AK)2-NH2 containing β-Ala in its structures exhibited good antimicrobial activity against Escherichia coli K12 407 and Bacillus subtilis 3562, in combination with very good antiproliferative and cytotoxic properties, as well as hydrolytic stability. (4) Conclusions: The obtained results reveal that all synthesized conjugates could be useful for medical practice as anticancer or antimicrobial agents.</jats:p>
dc.identifier.doi10.3390/molecules26237321
dc.identifier.issn1420-3049
dc.identifier.urihttps://rlib.uctm.edu/handle/123456789/22
dc.publisherMDPI AG
dc.relation.ispartofMolecules
dc.titleSynthesis and Biological Studies on (KLAKLAK)2-NH2 Analog Containing Unnatural Amino Acid β-Ala and Conjugates with Second Pharmacophore
dc.typejournal-article
oaire.citation.issue23
oaire.citation.volume26
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