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Among the pathologic hypotheses of Alzheimer’s disease (AD), cholinergic deficit and oxidative stress have been implicated as two major hallmarks. Therefore, inhibition of cholinesterase and oxidation are the two promising strategies in the development of a drug for AD. Thunbergia grandiflora leaf extract (TGEx) is used in this research to investigate its anticholinesterase and antioxidant potentials. Anticholinesterase activity was measured by modified Ellman method. Antioxidant potentials were evaluated by the assay of reducing power, radical scavenging and inhibition of lipid peroxidation. The Methanolic extract showed strong anticholinesterase effect. Additionally, the extract exhibited pronounced reducing capacity, radical scavenging ability, and lipid peroxidation inhibitory effect. The IC50 values of the extract for DPPH and hydroxyl free radical scavenging and lipid peroxidation were 10.50 ± 0.68, 24.98 ± 1.39 and 21.84 ± 0.91 μg/ml, respectively. Phytochemical screening of the extract revealed the presence of significant amount of total phenolics and flavonoids. The tested sample reflects potential antioxidative and anticholinesterase inhibitory effect which may warrant its effectiveness in the treatment of AD.