Phytoecdysteroids from aerial parts of Silene guntensis B. Fedtsch were investigated and three phytoecdysteroids were isolated: 2,3-diacetate-22-benzoate-20-hydroxyecdysone (1), 2-deoxy-20-hydroxyecdysone (2), and 20-hydroxyecdysone (3). Their chemical structures were elucidated by DEPT, COSY, 1H and 13C NMR spectroscopy. The isolated compounds 1-3 and crude extracts were evaluated for their antiproliferative and antioxidant activities. They exhibited substantial inhibition of cell growth against human cervix adenocarcinoma (HeLa), hepatocellular carcinoma (HepG-2), and breast adenocarcinoma (MCF-7) cells. The chloroform extract showed potent cytotoxic effects [IC50 values (26.58 +/- 1.88) microg/mL, (20.99 +/- 1.64) microg/mL, and (18.89 +/- 2.36) microg/mL, respectively]. The new compound 1 was mildly cytotoxic compared to extracts [(127.97 +/- 11.34), (106.76 +/- 7.81), and (203.10 +/- 19.56) microg/mL, respectively]. Water and n-butanol extracts exhibited good antioxidant activities [IC50 values of (68.90 +/- 6.45) microg/mL and (69.12 +/- 5.85) microg/mL, respectively].