Abstract

Department of Pharmacy, Hanyang University, Ansan 426-791, KoreaReceived May 15, 2014, Accepted May 29, 2014Twelve thienyl/furanyl-hydroxyphenylpropenones were systematically designed and synthesized, andevaluated for their inhibitory effect on LPS-induced ROS and NO production in RAW 264.7 macrophages.Compound 11 displayed the most significant inhibitory activity of LPS-induced ROS and NO production inRAW 264.7 macrophages. Structure-activity relationship study indicated that para-hydroxyphenyl moietyplays an important role for inhibitory activities on both LPS-induced ROS and NO production as well as 3-thienyl moiety on molecule.Key Words : Thieny/Furanyl-hydroxyphenylpropenones, LPS-induced ROS and NO, Inhibition, Structure-activity relationship studyIntroductionReactive oxygen species (ROS), the molecules containinghighly reactive oxygen, actively interact with variousintracellular molecules. Excessive ROS production results inalterations of diverse intracellular signaling pathways andcauses significant damages to the target cells, collectivelyknown as oxidative stress. Abnormally high production ofROS contributes to the development of diverse pathologicalevents, such as DNA mutation, carcinogenesis, aging, celldeath and inflammation,

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