Abstract: Disclosed are a Saussurea involucrate extract, pharmaceutical composition and use thereof for anti-fatigue and anti-aging. In the embodiments of the present invention, a low dose of ethyl acetate fraction of Saussurea involucrate (preferably 30 mg/kg) and Rutin (preferably 30 mg/kg) can inhibit MDA expression level and increase GPx activity. Additionally, both decrease the expression of COX-2, PARP and caspase-3, via downregulation of NF-kappaB, resulting in neuroprotection. Further, syringe feeding of Saussurea involucrate extract is also performed in aging mouse model. In the future, Saussurea involucrate extract of the present invention can be used in neuroprotection, particularly in treatment or prevention of cerebral diseases, nerve diseases, neurodegenerative diseases, chronic neurodegenerative diseases, aging, and fatigue, caused by oxidative injury.