Investigation of Antimicrobial, Anti‐Quorum Sensing, and Cytotoxic Activities of Flavonoids Isolated from Pulicaria armena Boiss. & Kotschy ex Boiss. (Asteraceae)

Abstract

This is the first report on the separation and biological assessment of all metabolites derived from Pulicaria armena (Asteraceae) which is an endemic species narrowly distributed in the eastern part of Turkey. The phytochemical analysis of P. armena resulted in the identification of one simple phenolic glucoside together with eight flavon and flavonol derivatives whose chemical structures were elucidated by NMR experiments and by the comparison of the spectral data with the relevant literature. The screening of all molecules for their antimicrobial, anti-quorum sensing, and cytotoxic activities revealed the biological potential of some of the isolated compounds. Additionally, quorum sensing inhibitory activity of quercetagetin 5,7,3' trimethyl ether was supported by molecular docking studies in the active site of LasR which is the primary regulator of this cell-tocell communication system in bacteria. Lastly, the critical molecular properties indicating drug-likeness of the compounds isolated from P. armena were predicted. As microbial infections can be a serious problem for cancer patients with compromised immune systems, this comprehensive phytochemical research on P. armena with its anti-quorum sensing and cytotoxic compounds can provide a new approach to the treatment.

Polyphenols of the Inuleae-Inulinae and Their Biological Activities: A Review

“…Spinacetin and 3,5,4'-trihydroxy-6,7,3'trimethoxyflavone demonstrated sEH inhibitory activity in vitro (IC50: 16.58 μM and 14.13 μM, respectively) that supported their role as anti-inflammatory agents [103]. Quercetagetin 3,7,3'trimethyl ether (chrysosplenol C) from P. armena and P. inuloides demonstrated moderate cytotoxicity towards A549, HCT116, and PC3 human cancer cell lines in vitro (IC50: 16.8-20.0 μg/mL) [83,184]. According to Ayaz et al [248], chrysosplenol C extracted from C. montanum, was cytotoxic against the human breast (MCF-7), cervical (HeLa), and lung (A549) cancer cell lines (conc.…”