Sesquiterpene lactones are potent and irreversible inhibitors of the antibacterial target enzyme MurA

Sesquiterpenoids in subtribe Centaureinae (Cass.) Dumort (tribe Cardueae, Asteraceae): Distribution, 13C NMR spectral data and biological properties

“…They covalently bind the thiol group of Cys115 and their unsaturated ester side chain has pivotal importance for the inhibition of MurA. These results provided evidence that MurA is a target protein of sesquiterpene lactones (SLs), which is probably highly relevant for their known antibacterial effect (Bachelier et al, 2006).…”

Phytotoxicity and cytotoxicity of Lepidaploa rufogrisea (Asteraceae) extracts in the plant model Lactuca sativa (Asteraceae)

“…In addition, phenolic allelochemicals have the capacity of altering the integrity of the DNA and RNA (Zeng, Luo, & Shi, 2001). Among the mechanisms proposed to sesquiterpene lactones action, for example, is the ability of the lactone molecule to react with nucleophiles present in the DNA molecules or sulfur atoms from amino acids of proteins/enzymes, unleashing an oxidative process (Bachelier et al, 2006). Oxidative stress is a process closely related to cell death, which is evidenced, cytologically, as a condensed nucleus (Vermes, Haanem, & Reutelingsperger, 2000), that was observed in treated cells of this work.…”

Design, synthesis and biological evaluation of novel sesquiterpene mustards as potential anticancer agents

“…In addition, natural products a and b (Fig. 1) with a-methylene-b-lactone group have been proved to efficiently deplete GSH [34,35] and show a diverse range of biological activities, including anticancer [36,37], anti-inflammatory [38], antibacterial [39] and fungicidal properties [40]. Also, they can easily penetrate the cell membrane into the cell.…”