A phytochemical investigation into the stem bark of Bauhinia Rufescens (Fabaceae) has resulted in the isolation of α-amyrin acetate, sitosterol 3-O-β-D-xylopyranoside, menisdaurin, sequoyitol and linoleic acid. Their structures were determined using spectroscopic data as well as comparison with literature data. The antimicrobial assay has been tested against Gram positive, Gram negative bacteria and fungal strains, while the tyrosinase inhibition assay was examined using L-Dopa as a substrate of tyrosinase enzyme. α-amyrin acetate, sitosterol 3-O-β-D-xylopyranoside, menisdaurin and sequoyitol showed minimum inhibition concentration (MIC) values in the range of 900-450 µg/mL against all bacterial strains, while the MIC values for the fungal strains were recorded in the range of 450-112 µg/mL. In the tyrosinase inhibition assay, α-amyrin acetate was found to be moderately active against tyrosinase enzyme with an inhibition of 62.0% lower than the positive control, kojic acid (85.0%).