Nature derived product drew a lot of interest because of their potential nutritional and therapeutics value. Most natural compounds are now processed and developed as possible antioxidative, antimitotic, antimicrobial, anti-inflammatory, antiangiogenic, and anti-carcinogenic pharmaceutical agents. Indeed, several natural products have been used as lead compounds in the development of most potent physiologically relevant chemicals for therapeutic application. In the current study antioxidant and anticancer potential of tuber extract of Dioscorea bulbifera have been determined as well as its antimicrobial potential against pathogenic bacteria. The IC50 value for the extract was found to be 55µg/ml for MCF-7 and 75µg/ml for MD-AMB-231 human breast cancer adenocarcinoma whereas minimum inhibitory concentration (MIC) value of the methanolic extract against S. aureus was 0.19 mg/ml and minimum bactericidal concentration (MBC) was 1.56 mg/ml. Further to identify compounds responsible for antioxidant, anticancer and antimicrobial activity GCMS analysis of the extract was conducted. Histopathological and haematological assay were carried out on animal model to identify any toxic effect of extract on vital organ system. This study may be used to provide the groundwork for the creation of novel nature-derived drugs whose biological activity can be determined by further purification, characterization, and validation of the active phytochemicals and their mechanism of action.