Antiproliferative, Antimicrobial and Antiviral Activity of β-Aryl-δ-iodo-γ-lactones, Their Effect on Cellular Oxidative Stress Markers and Biological Membranes

Biomolecules

Piotr Kuropka¹  Witold Gładkowski²  Aleksandra Włoch³  Hanna Pruchnik³  Dominika Stygar⁴  Elżbieta Chełmecka⁵  Barbara Bażanów⁶  Fouad Bahri⁷ 

[1] Department of Biostructure and Animal Physiology, Wrocław University of Environmental and Life Sciences, C.K. Norwida 31, 50-375 Wrocław, Poland;Department of Chemistry, Wrocław University of Environmental and Life Sciences, Norwida 25, 50-375 Wrocław, Poland;Department of Physics and Biophysics, Wrocław University of Environmental and Life Sciences, C.K. Norwida 25, 50-375 Wrocław, Poland;Department of Physiology in Zabrze, Medical University of Silesia, Poniatowskiego 15, 40-751 Katowice, Poland;Department of Statistics, Department of Instrumental Analysis, Medical University of Silesia, Ostrogórska 30, 41-200 Sosnowiec, Poland;Department of Veterinary Microbiology, Wroclaw University of Environmental and Life Sciences, Norwida 31, 50-375 Wrocław, Poland;Laboratory of Microbiology and Plant Biology, University of Mostaganem, Mostaganem 27000, Algeria;

关键词: iodolactones;    antimicrobial activity;    antitumor activity;    cytotoxic activity;    antiviral activity;    oxidative stress markers;   

DOI  :  10.3390/biom10121594

来源: DOAJ

【 摘 要 】

The aim of this work was the examination of biological activity of three selected racemic cis-β-aryl-δ-iodo-γ-lactones. Tested iodolactones differed in the structure of the aromatic fragment of molecule, bearing isopropyl (1), methyl (2), or no substituent (3) on the para position of the benzene ring. A broad spectrum of biological activity as antimicrobial, antiviral, antitumor, cytotoxic, antioxidant, and hemolytic activity was examined. All iodolactones showed bactericidal activity against Proteus mirabilis, and lactones 1,2 were active against Bacillus cereus. The highest cytotoxic activity towards HeLa and MCF7 cancer cell lines and NHDF normal cell line was found for lactone 1. All assessed lactones significantly disrupted antioxidative/oxidative balance of the NHDF, and the most harmful effect was determined by lactone 1. Contrary to lactone 1, lactones 2 and 3 did not induce the hemolysis of erythrocytes after 48 h of incubation. The differences in activity of iodolactones 1–3 in biological tests may be explained by their different impact on physicochemical properties of membrane as the packing order in the hydrophilic area and fluidity of hydrocarbon chains. This was dependent on the presence and type of alkyl substituent. The highest effect on the membrane organization was observed for lactone 1 due to the presence of bulky isopropyl group on the benzene ring.

【 授权许可】

Unknown