We studied the cognitive improving and cerebral protective constituents in the roots of Polygala tenuifolia Willdenow, a well-known Chinese traditional medicine prescribed for amnesia, neurasthenia, palpitation, noctural emission and insomnia. Tenuifoliside B (1), which is one of the acylated oligosaccharides in the roots of P. tenuifolia, showed the cerebral protective effect on potassium cyanide (KCN)-induced anoxia in mice, widely used as an animal model for cerebrovascular disease, and also had an ameliorative effect on the scopolamine-induced impairment of performance in passive avoidance task in rats. Compound 1 significantly enhanced oxotremorine-induced tremors in mice, suggesting that it ameliorated the scopolamine-induced impairment of passive avoidance response by enhancing the cholinergic system. These findings show that compound 1 has cognitive improving and cerebral protective effects.