The present work aims to investigate the acetylcholinesterase (AChE) inhibition and antioxidant activity of red yeast rice (RYR) extract in hypercholesterolemic rats. In this study, rats were assessed for AChE activity in brain and serum by the colorimetric method. In vitro antioxidant activity was determined by measuring their capability to scavenge 2, 2´-azinobis [3-ethylbenzthiazoline]-6-sulfonic acid (ABTS) radical. Our results showed that the AChE activity significantly increased in the brain and serum of hypercholesterolemic rats. Treatment of hypercholesterolemic rats with RYR extract at 1g/kg and 2 g/kg showed a significant decrease in this parameter. Furthermore, the RYR extract showed a high ABTS radical inhibition of 70.64 + 1.31 % at a concentration of 100 mg/ml. These findings suggested that RYR extract have a strong antiacetylcholinesterase and antioxidant properties. Thus, these extracts may have a therapeutic application in the treatment of hypercholesterolemia-induced Alzheimer's disease.