Remedial plants have been utilized for their therapeutic potential since time immemorial. Synthetic drugs has a lot of side effects and are cost-effective; therefore traditional medication has stayed the most approachable and affordable source of treatment. Among medicinal plants, Tinospora cordifolia, regularly called as Guduchi, a member of Menispermeaceae family, is one of the most multifaceted reviving shrubs. Its therapeutic applications are because of the presence of several bioactive constituents, like alkaloids, terpenoids, lactones, steroids, glycosides, polysaccharides and aliphatic compounds, present in all division of the plant especially in the roots, barks, and leaves. Tinospora has been widely utilized in Unani Homeopathic and Ayurveda medicines overall particularly in Indian subcontinent in the treatment and avoidance of different infections such as gastrointestinal, hepatoprotection, cardioprotective, antimicrobial, antioxidative, anti-diarrheal, anticancer, antiallergic, anti-inflammatory, antimalarial, antituberculosis, antipyretic, immunomodulatory, antiulcer, antihyperglycemic, antihyperlipidemic, antidiabetic, anti-HIV potential, mental disorder, antiviral, and anti-osteoporotic. Due to these pharmacological properties, it has shown incredible capacity for the betterment of commercial utilization of biopharmaceuticals to cure various diseases and industrial products. In this review we summarized the information on bioactive constituents, their chemical structures, and possible mechanisms followed for therapeutic aspects of Tinospora cordifolia.