Bioactive Cytotoxic Agents and Chemokine Production Inhibitors in LPS-Induced Raw264.7 Macrophage Cell Line from Flowers of Crepis Senecioides

Abstract

Crepis senecioides is one of the endemic plant species found in Libya. The ethanol extract (E) of the flowers was partitioned on silica gel column with dichloromethane affording four compounds. Their structures were elucidated by the physicochemical and spectral data as germanicol acetate (1), 3`,3``butyl, 8`,8``carboxy) di-octyl phethalate (2), taraxasterol (3) and β-sitosterol (4). effect of the tested samples 1 and 2 on the viability of RAW macrophage 264.7 were studied. anti-cancer activity was tested on several human cell lines. Anti-inflammatory effect was also screened. Compound 1 had promising cellular cytotoxicity with IC₅₀ 60.26µg/mL on HepG2. Compound 2 had a talented cellular cytotoxicity with IC₅₀ 50.18 µg/mL on PC3. Both 1 and 2 exerted alike cytotoxicity with IC₅₀ µg/mL 78.53, 78.14 on PC3 and MCF-7 carcinoma cell lines respectively. The treatment of LPS-stimulated macrophage with 2 led to a highly significant inhibition 45.05% in the nitrite concentration in LPS-stimulated macrophage. Compound 1 had a promising cellular cytotoxicity on HepG2, while 2 exhibited an inhibition on chemokine expression in LPS-induced RAW 264.7 macrophages and had talented cellular cytotoxicity on PC3.

Keywords: Crepis senecioide;, Asteraceae; Anti-inflammatory; cytotoxic effect; terpenoids; phethalate derivative.