| Summary: | 碩士 === 高雄醫學大學 === 醫學系藥理學科碩士班 === 104 === Chalcone is a class of plant flavonoids with multiple pharmacological activities, including anti-inflammatory and anti-oxidative effects. The peroxisome proliferator-activated receptor (PPAR) regulatory pathway plays a critical role in the regulation of inflammation. A chalcone derivative AN07 was reported its novel therapeutic potential against atherosclerosis through PPAR- γ activation. In this study, we investigated the effects of AN07 on lipopolysaccharide (LPS)-induced inflammation and oxidative stress, and the role of PPAR- γ in AN07 protection in macrophage RAW264.7. Results indicated that AN07 inhibited LPS-induced expressions of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) and phosphor - nuclear factor of kappa light polypeptide gene enhancer in B-cells inhibitor alpha (p-IκBα) in RAW264.7. LPS-induced nitric oxide (NO) production was also attenuated by AN07. Moreover, AN07 not only attenuated gp91phox expression and ROS production, but it also enhanced expression of Nrf2, HO-1 activation and production of glutathione (GSH) in LPS-stimulated RAW264.7 cells. Furthermore, PPAR-γ antagonist GW9662 significantly attenuated AN07-induced COX-2 inhibition and Nrf2 activation in LPS-stimulated RAW264.7 cells. Taken together, the present results demonstrate that AN07 exerts anti-inflammatory and anti-oxidant effects in macrophages, at least in part, through partial PPAR- γ activation, suggesting AN07 possesses a potential to be an anti-inflammatory and anti-oxidant agent.
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