Abstract
The antiproliferative and antimicrobial effects of thirteen compounds isolated from Inula viscosa (L.) were tested in this study. The antiproliferative activity was tested against three cell lines using the MTT assay. The microdilution method was used to study the antimicrobial activity against two Gram positive bacteria, two Gram negative bacteria and one fungus. The apoptotic activity was determined using a TUNEL colorimetric assay. Scanning electron microscopy was used to study the morphological changes in treated cancer cells and bacteria. Antiproliferative activity was observed in four flavonoids (nepetin, 3,3′-di-O-methylquercetin, hispidulin, and 3-O-methylquercetin). 3,3′-di-O-Methylquercetin and 3-O-methylquercetin showed selective antiproliferative activity against MCF-7 cells, with IC50 values of 10.11 and 11.23 µg/mL, respectively. Both compounds exert their antiproliferative effect by inducing apoptosis as indicted by the presence of DNA fragmentation, nuclear condensation, and formation of apoptotic bodies in treated cancer cells. The antimicrobial effect of Inula viscosa were also noticed in 3,3′-di-O-methylquercetin and 3-O-methyquercetin that inhibited Bacillus cereus at MIC of 62.5 and 125 µg/mL, respectively. Salmonella typhimurium was inhibited by both compounds at MIC of 125 µg/mL. 3,3′-di-O-Methylquercetin induced damage in bacterial cell walls and cytoplasmic membranes. Methylated quercetins isolated from Inula viscosa have improved anticancer and antimicrobial properties compared with other flavonoids and are promising as potential anticancer and antimicrobial agents.
Highlights
Treatment of cancer and microbial infections have drawn the attention and interest of researchers due to their great impact on the population’s health
Methylated quercetins isolated from Inula viscosa have improved anticancer and antimicrobial properties compared with other flavonoids and are promising as potential anticancer and antimicrobial agents
Our results agree with previous studies that reported high antiproliferative activity of nepetin isolated from Eupatorium ballotaefolium HBK. (Asteraceae) [20]
Summary
Treatment of cancer and microbial infections have drawn the attention and interest of researchers due to their great impact on the population’s health. Inula viscosa has many uses, including anti-inflammatory [7], anthelmintic, lung disorders [8], antipyretic, antiseptic, and antiphlogistic activities [9,10] in addition to treating gastroduodenal disorders [11]. In previous studies we reported the potent antiproliferative [17] and antimicrobial [18] activities of an Inula viscosa methanol extract. In vitro antiproliferative and antimicrobial screening of plant products can provide valuable preliminary data for the potential use of these products to treat cancer and/or microbial infections. Taking into account the use of Inula viscosa in traditional medicine, its wide distribution, and the lack of studies that evaluate the biological activity of its pure compounds, the present study was undertaken to evaluate the antiproliferative, antimicrobial and apoptosis induction effects of thirteen compounds isolated from
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