C.quadrangularis L. belongs to the family Vitaceae, an edible plant found in India. It is commonly known as “bone setter. The stems of C.quadrangularis are reported to have great medicinal value. Considering above, in the present work antioxidant, anticancer and toxicity study was evaluated. In in vitro antioxidant studies, the antioxidant activity of FS-II was better than that of ME and FS-I. FS-II showed best ABTS radical scavenging activity followed by hydroxyl radical scavenging activity, DPPH free radical scavenging activity. In anticancer studies, ME showed potent proliferation inhibitory activity against A549 and HeLa cell lines. This is the first report on the anticancer properties of C.quadrangularis. In vivo antioxidant activity revealed that FS-II of C.quadrangularis protects oxidative injury induced by CCl4 and water immersion stress. In acute toxicity study, the FS-II had no mortality andobservable acute toxic effect during the entire period in male and female rats dosed up to 800mg/kg b.w. orally.These studies have shown that the ME of C.quadrangularis and its fractions contain some active ingredients with the potential of being good antioxidant and anticancer agents.