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Soy isoflavones are suggested to produce several biological effects related to health benefits, such as anti-inflamatory and antioxidant activities. However, to be efficiently absorbed and to provide these benefits, the isoflavones must be transformed from glycosylated to aglycone form. For this purpose, the enzymatic biotransformation has shown great potential. This study aimed to evaluate, in in vitro assays, the effects of the enzymatically biotransformed soymilk on anti-inflamatory and antioxidant activities. The soymilk was biotransformed with tannase and β-glycosidase enzymes and the antioxidant capacity was measured by ORAC and FRAP assays. The anti-inflammatory test was performed using RAW 264.7 murine macrophages. Cells were stimulated with lipopolysaccharides from E. coli and treated with samples for 24 hours. Cytokines concentration (TNF-α and IL-6) was measured using BD OptEIATM ELISA kit assay and nitric oxide levels were also quantified. According to ORAC assay, the results demonstrated that the sample of “soymilk + free tannase” presented the higher antioxidant capacity corresponding to an increase of 2.3 times compared to untreated soymilk. The antioxidant capacity by FRAP assay increased in 24.9% to “soymilk + free tannase” and decreased in 3.5% to “soymilk + immobilized β-glycosidase”. Concerning the anti-inflammatory test, the treatment with 10 µl/ml of “soymilk + free tannase” was able to reduce the secretion of TNF-α in 44.6% compared to control and IL-6 was not detected in this condition. The oxid nitric was not detected when the treatment with 5 µl/ml of “soymilk + tannase” and “soymilk + β-glycosidase” were tested in immobilized forms. In conclusion it can be said that the biotransformed soymilk by tannase was responsible for increasing the antioxidant potential and reducing significantly the secretion of pro-inflammatory cytokines, being a product or an ingredient with high antioxidant power and with promising results to combat inflammation.