Abstract: Inflammation and oxidative stress are two major causes of various life-threatening diseases. Hesperidin (Hsd) and its aglycone， hesperetin (Hst)， are two flavonoids from citrus species that have numerous biological properties， particularly antioxidant and anti-inflammatory. New findings showed that the antioxidant activity of Hsd/Hst was not only limited to its radical scavenging activity， but it augmented the antioxidant cellular defenses via the ERK/Nrf2 signaling pathway as well. Various in vitro and in vivo studies have been conducted to evaluate Hsd， its metabolites， or its synthetic derivatives which could play an anti-inflammatory role by inhibiting the activation of relevant inflammatory signaling pathways， reducing inflammatory targets including NF-κB， iNOS， and COX-2， and the markers of chronic inflammation. In this review， new findings regarding the antioxidant and anti-inflammatory effects of Hsd and Hst and the related molecular mechanisms are discussed.