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Selectively Halogenated Flavonolignans—Preparation and Antibacterial Activity
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SYSNO ASEP 0566377 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Selectively Halogenated Flavonolignans—Preparation and Antibacterial Activity Author(s) Hurtová, Martina (MBU-M) ORCID
Káňová, Kristýna (MBU-M) ORCID
Dobiasová, S. (CZ)
Holasová, K. (CZ)
Čáková, D. (CZ)
Hoang, L. (CZ)
Biedermann, David (MBU-M) RID, ORCID
Kuzma, Marek (MBU-M) ORCID, RID
Cvačka, Josef (UOCHB-X) RID, ORCID
Křen, Vladimír (MBU-M) RID, ORCID
Viktorová, J. (CZ)
Valentová, Kateřina (MBU-M) RID, ORCIDArticle number 15121 Source Title International Journal of Molecular Sciences. - : MDPI
Roč. 23, č. 23 (2022)Number of pages 18 s. Language eng - English Country CH - Switzerland Keywords bacteria ; biological activity ; flavonoids ; flavonolignans ; halogenation ; multidrug resistance Subject RIV CE - Biochemistry OECD category Medicinal chemistry Subject RIV - cooperation Institute of Organic Chemistry and Biochemistry - Analytical Chemistry, Separation R&D Projects LTC20070 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) GA21-00551S GA ČR - Czech Science Foundation (CSF) Method of publishing Open access Institutional support MBU-M - RVO:61388971 ; UOCHB-X - RVO:61388963 UT WOS 000897443500001 EID SCOPUS 85143809536 DOI 10.3390/ijms232315121 Annotation A library of previously unknown halogenated derivatives of flavonolignans (silybins A and B, 2,3-dehydrosilybin, silychristin A, and 2,3-dehydrosilychristin A) was prepared. The effect of halogenation on the biological activity of flavonolignans was investigated. Halogenated derivatives had a significant effect on bacteria. All prepared derivatives inhibited the AI-2 type of bacterial communication (quorum sensing) at concentrations below 10 µM. All prepared compounds also inhibited the adhesion of bacteria (Staphyloccocus aureus and Pseudomonas aeruginosa) to the surface, preventing biofilm formation. These two effects indicate that the halogenated derivatives are promising antibacterial agents. Moreover, these derivatives acted synergistically with antibiotics and reduced the viability of antibiotic-resistant S. aureus. Some flavonolignans were able to reverse the resistant phenotype to a sensitive one, implying that they modulate antibiotic resistance. Workplace Institute of Microbiology Contact Eliška Spurná, eliska.spurna@biomed.cas.cz, Tel.: 241 062 231 Year of Publishing 2023 Electronic address https://www.mdpi.com/1422-0067/23/23/15121
Number of the records: 1