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Triterpenoid–peg ribbons targeting selectivity in pharmacological effects
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SYSNO ASEP 0549087 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Triterpenoid–peg ribbons targeting selectivity in pharmacological effects Tvůrce(i) Özdemir, Zülal (UEB-Q) ORCID
Bildziukevich, Uladzimir (UEB-Q) RID, ORCID
Čapková, M. (CZ)
Lovecká, P. (CZ)
Rárová, L. (CZ)
Šaman, David (UOCHB-X) RID, ORCID
Zgarbová, Michala (UOCHB-X)
Lapuníková, Barbora (UOCHB-X)
Weber, Jan (UOCHB-X) RID, ORCID
Kazakova, O. (GB)
Wimmer, Zdeněk (UEB-Q) RID, ORCIDCelkový počet autorů 11 Číslo článku 951 Zdroj.dok. Biomedicines. - : MDPI
Roč. 9, č. 8 (2021)Poč.str. 14 s. Jazyk dok. eng - angličtina Země vyd. CH - Švýcarsko Klíč. slova Amide bond ; Antimicrobial activity ; Anti‐HIV activity ; Cytotoxicity ; Huisgen 1,3‐dipolar cycloaddition ; Molecular ribbon ; Multifunctional PEG3 derivative ; Supramolecular self‐assembly ; Triterpenoid Obor OECD Biochemical research methods CEP FV30300 GA MPO - Ministerstvo průmyslu a obchodu EF16_019/0000738 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy Způsob publikování Open access Institucionální podpora UEB-Q - RVO:61389030 ; UOCHB-X - RVO:61388963 UT WOS 000688878800001 EID SCOPUS 85112313481 DOI 10.3390/biomedicines9080951 Anotace (1) Background: To compare the effect of selected triterpenoids with their structurally resembling derivatives, designing of the molecular ribbons was targeted to develop compounds with selectivity in their pharmacological effects. (2) Methods: In the synthetic procedures, Huisgen 1,3‐ dipolar cycloaddition was applied as a key synthetic step for introducing a 1,2,3‐triazole ring as a part of a junction unit in the molecular ribbons. (3) Results: The antimicrobial activity, antiviral activity, and cytotoxicity of the prepared compounds were studied. Most of the molecular ribbons showed antimicrobial activity, especially on Staphylococcus aureus, Pseudomonas aeruginosa, and Enterococcus faecalis, with a 50–90% inhibition effect (c = 25 μg∙mL−1). No target compound was effective against HSV‐1, but 8a displayed activity against HIV‐1 (EC50 = 50.6 ± 7.8 μM). Cytotoxicity was tested on several cancer cell lines, and 6d showed cytotoxicity in the malignant melanoma cancer cell line (G‐361, IC50 = 20.0 ± 0.6 μM). Physicochemical characteristics of the prepared compounds were investigated, namely a formation of supramolecular gels and a self‐assembly potential in general, with positive results achieved with several target compounds. (4) Conclusions: Several compounds of a series of triterpenoid molecular ribbons showed better pharmacological profiles than the parent compounds and displayed certain selectivity in their effects. Pracoviště Ústav experimentální botaniky Kontakt David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469 Rok sběru 2022 Elektronická adresa http://doi.org/10.3390/biomedicines9080951
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