Traditional herbs have always been pioneers in the development of new therapeutics. According to Ayurveda, India has always been a hub of many herbs and shrubs that possess numerous polyphenols and flavonoids with promising anticancer, antioxidant, and antibacterial properties. The present study aimed to elucidate the anticancer activity of various methanol, ethanol and petroleum ether extracts of Bergera koenigii seeds against THP-1 cells. In addition to phytochemical analysis, total phenol and flavonoid content (TPC, TFC) and antioxidant assays were also performed to estimate the potential of the Bergera koenigii seeds. Among these, the methanolic extract of Bergera koenigii seeds inhibited leukemic THP-1 cells due to the presence of bioactive compounds such as hexadecanoic acid, octadecadienoic acid, octadecatrienoic acid, tricosanoic acid and γ-sitosterol, as revealed by GC‒MS analysis. According to the radical scavenging capacity, both hexadecanoic acid and octadecadienoic acid exhibited the highest anticancer activity, with IC50 values of 15±8.37 and 15±0.23 µg/ml, respectively. Additionally, the methanolic extract had a TPC of 959.97 mg/GAE and a TFC of 1443.20 mg/QE, and the antioxidant activity had an IC50 value of 369.09, Antibacterial activity with 10 ± 0.5 mmEscherichia coli, 8 ± 0.82 mm for Pseudomonas aeruginosa and15 ± 1.7 mm for Staphylococcus aureus. Thus, the above results indicate that the methanolic extracts of Bergera koenigii seeds are more promising drugs against leukemic THP-1 cell lines than are the chloroform and pet ether extracts.