ABSTRACT Thunbergia grandiflora, commonly called blue trumpet vine, sky vine or sky flower belongs to Acanthaceae, which is native in Australia, Central America, the West Indies, Africa, and numerous islands in the Pacific including Hawaii, Fiji, French Polynesia, Palau, and Samoa. In the present investigation, Thunbergia Grandiflora extracts were studied for in-vivo acute toxicity, anticancer and antioxidant activity. According to the toxicity study, 200 and 400mg/kg body weight was selected as dose. In the evaluation of anticancer activity the tumour yield and tumour burden were not detected up to 4th weeks; but in 8th week, observed the formation of tumours and it become maximum in 16th week in all treated groups of mice. In carcinogenic control group of mice maximum tumors activity was observed due to carcinogenic nature but it got decreased after the treatment with sample 1,2,3 and isolated compound. Also, carcinogen increased LPO and reduced SOD, GSH, and catalase in lung homogenate. Extracts significantly reversed the effect of carcinogen on LPO level. The isolated compound was found more effective than the extracts (200 mg/kg an 400 mg/kg) on LPO, SOD, GSH and catalase. Moreover the extract of Thunbergia grandiflora showed down regulated effect on the levels of TNF-α and IL-6.