Natural products with medicinal value are gradually gaining importance in clinical research due to their well-known property of no side effects as compared to drugs. Plants have been one of the important sources of medicines since the beginning of human civilization. There is a growing demand for plant based medicines, health products, pharmaceuticals, food supplements, cosmetics etc. A review of chemical constituents present in various parts of Tinospora cordifolia and their pharmacological actions is given in the present article. Tinospora cordifolia commonly named as “Guduchi” is known for its immense application in the treatment of various diseases in the traditional ayurvedic literature. Guduchi (Tinospora cordifolia) is a popular medicinal plant spread across the tropics. Its effectiveness in therapy is well known globally. Lesser known are its dietary benefits. Guduchi [Tinospora cordifolia (Willd.) Hook. F. Thoms] is being used in Diet by various tribal people of India and it also forms a part of traditional Indian cuisine. Ayurveda also states its dietary utility. Recently the discovery of active components from the plant and their biological function in disease control has led to active interest in the plant across the globe. The future scope of the review remains in exploiting the biochemical and signaling pathways affected by the compounds isolated from Tinospora so as to enable new and effective formulation in disease eradication. This review can be used for further research as well as clinical purpose.