The use of indigenous drug industry in India has been widely expanded in recent years. Tinospora cordifolia (Guduchi) belonging to family Menispermaceae has a wide array of bioactive principles in exploring nutraceuticals from plant materials. It is a versatile resource for all forms of life and can be an alternative for synthetic drugs considering their adverse effects and also for economic purposes. T. cordifolia is considered as an important herbal drug of Indian System of Medicines (ISM). The herb is known for its therapeutic efficacy and used in treatment of dyspepsia, diabetes, fever, urinary problems, jaundice, chronic diarrhoea, cardiac disease, dysentry, helmenthiasis, skin diseases, leprosy and many more diseases. Present review highlights the classical anti-toxin, anti diabetic, anticancer, immunomodulatory, antioxidant, antimicrobial, hepato-protective activity of Guduchi and their validation through existing literature. The plant is reported to contain alkaloids, glycosides, steroids and terpenoids. The current study is undertaken to explore and establish the phytochemistry and pharmacological activity of T. cordifolia.