Prenylated flavonoids combating mycobacteria

ŠKOVRANOVÁ, Gabriela, Marie ČULENOVÁ, Lenka MOLČANOVÁ, Jakub TREML, Fabian ALPERTH, Franz BUCAR and Alice SYCHROVÁ. Prenylated flavonoids combating mycobacteria. In Natural Products in Drug Discovery and Development – Advances and Perspectives: PSE Meeting September 19–22, 2022, Iasi, Romania. 2022.

Basic information

• Original name: Prenylated flavonoids combating mycobacteria
• Authors: ŠKOVRANOVÁ, Gabriela (703 Slovakia, belonging to the institution), Marie ČULENOVÁ (203 Czech Republic, belonging to the institution), Lenka MOLČANOVÁ (703 Slovakia, belonging to the institution), Jakub TREML (203 Czech Republic, belonging to the institution), Fabian ALPERTH (40 Austria), Franz BUCAR (40 Austria) and Alice SYCHROVÁ (203 Czech Republic, belonging to the institution).
• Edition: Natural Products in Drug Discovery and Development – Advances and Perspectives: PSE Meeting September 19–22, 2022, Iasi, Romania, 2022.

Other information

• Original language: English
• Type of outcome: Presentations at conferences
• Field of Study: 30104 Pharmacology and pharmacy
• Confidentiality degree: is not subject to a state or trade secret
• WWW: Abstracts Book
• RIV identification code: RIV/00216224:14160/22:00134039
• Organization unit: Faculty of Pharmacy
• Keywords in English: antimicrobial activity; membrane disruption; mycobacterium; prenylated flavonoids
• Tags: rivok, ÚMF, ÚPL

Abstract

Globally, tuberculosis is one of the primary causes of death. Resistant strains of Mycobacterium tuberculosis as well as other strains of mycobacteria are prompting the search for new drugs and solutions. Twelve prenylated compounds were tested against mycobacterial strains, and the microdilution method revealed a significant antibacterial effect with minimal inhibitory concentrations ranging from 2-16 µg/mL. Membrane damage and permeability disruption is one of the mechanisms of action by which prenylated flavonoids exerted ≤40% effect. The effect of the compounds on the viability of THP-1 cells differentiated into macrophages demonstrated their toxicity with respect to the concentrations used. However, prenylated phenolics represent potential model structures for the development of new antituberculosis drugs.

Abstract (in Czech)

Tuberkulóza celosvetovo patrí medzi primárne príčiny smrti. Rezistentné kmene Mycobacterium tuberculosis ako aj iné kmene mykobaktérií nabádajú k hľadaniu nových liečiv a riešení. Dvanásť prenylovaných zlúčenín bolo testovaných voči mykobakteriálnym kmeňom, pričom mikrodilučná metóda odhalila významný antibakteriálny efekt s minimálnou inhibičnou koncentráciou v rozmedzí 2–16 µg/mL. Poškodenie membrány a narušenie permeability je jedným z mechanizmov účinku, ktorými prenylované flavonoidy účinkovali na ≤40%. Vplyv látok na viabilitu THP-1 buniek diferencovaných v makrofágy preukázal ich toxicitu vzhľadom k použitým koncentráciám. Prenylované fenoly však predstavujú potenciálne modelové štruktúry pre vývoj nových antituberkulotík.

Links

• GF21-38204L, research and development project: Name: Komplexy vybraných přechodných kovů s rostlinnými látkami s anti-NF-kappa B a pro-PPAR duální aktivitou

Investor: Czech Science Foundation, Partner Agency

• MUNI/A/1279/2021, interní kód MU: Name: Mechanizmus antimikrobiálneho účinku fenolických látok voči Gram-pozitívnym baktériám.

Investor: Masaryk University