Saussurea lappa is a traditionally well-known plant for its medicinal uses in different indigenous systems of medicine. It is widely used in the treatment of asthma, ulcer, stomach problems and inflammatory diseases. In current study the phytochemical screening of S. lappa showed the presence of sesquiterpenes, anthraquinones, lignans, alkaloids, flavonoids, glycosides and steroids. Antimicrobial potential of subject plant was also investigated against three bacterial strains and maximum antibacterial activity was observed by CEE against S. aureus, CAE against P. aeruginosa, while CME, CEE, EAE and PEE showed almost same significant activity against E. coli. The CME (1000 ppm) was found to have maximum anti-tumor activity with 75% tumor inhibition potential. Significant DNA protection (of plasmid pBR322) activity was observed in 100 ppm CME and EAE. Therefore, S. lappa can be considered as promising candidate for isolation of bioactive compounds having antibacterial, antitumor and DNA protective potential.