Antiproliferative, Antimicrobial and Antiviral Activity of β-Aryl-δ-iodo-γ-lactones, Their Effect on Cellular Oxidative Stress Markers and Biological Membranes
Aleksandra Włoch , Dominika Stygar , Fouad Bahri , Barbara Bażanów , Piotr Kuropka , Elżbieta Chełmecka , Hanna Pruchnik , Witold Gładkowski
AbstractThe 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.
|Journal series||Biomolecules, ISSN 2218-273X, e-ISSN 2218-273X, (N/A 100 pkt)|
|Publication size in sheets||1|
|Keywords in English||iodolactones; antimicrobial activity; antitumor activity; cytotoxic activity; antiviral activity; oxidative stress markers; hemolytic activity; biophysics research|
|License||Journal (articles only); published final; ; with publication|
|Score||= 100.0, 28-04-2021, ArticleFromJournal|
|Publication indicators||= 1; = 3; : 2018 = 1.641; : 2018 = 4.694 (2)|
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