The previous study was to investigate the anti-cancer activity of aqueous extracts from Inonotus obliquus (IO), Cordyceps militaris (CM) and Uncaria tomentosa (UT). The antioxidant and immunomodulatory activities of aqueous extracts were measured and compared. The results showed UT exhibited excellent SOD-like activity (113.1 U/mg) and stronger DPPH radical scavenging activity (EC50, 0.442 mg/ml). Moreover, inhibition ratio of U2OS cells was reached to 92.17% at 7mg/ml for 72 h. In addition, BALB/c mice were inoculated with DLD-1 cells and fed with three samples to be determined weight, tumor diameter and tumor necrosis factor (TNF) α. UT also performed marvelous anti-cancer activity on inhibition ratio of weight (44.2%) and tumor diameter(48.12%) and TNF-α concentration (69.23%). All these results indicated that aqueous extract from UT exhibited potent anti-cancer activity and also could provide a theoretical basis for utilization as a nutritious function material.