Chromatographic purification of the DCM sub-extract of Uvaria grandiflora led to the isolation and characterization of a new polyoxygenated cyclohexane derivative, grandifloranol (1), together with five known compounds. Among the compounds isolated, zeylenone (3) showed moderate antitubercular activity against Mycobacterium tuberculosis H37Rv with MIC90 value of 51.2 μM and antiproliferative or cytotoxic activity against human myeloid leukaemia (K-562) and HeLa cells with IC50 values of 2.3 and 18.3 μM, respectively.