Andrographolide is a main chemical constituent of Andrographis paniculata that having medicinal and pharmacological properties for various diseases. In this present work, we study their multiple pharmacological properties - antimicrobial, anticancer, antifertility, anti-inflammatory and antidiabetic activities. Andrographolide is an intriguing pharmacophore that has potential to be developed as a chemotherapeutic drug for the treatment of cancer. This suggests, it has anticancer and immunomodulatory properties. In order to understand the Andrographis paniculata plant as a multifunctional medicinal agent, we have investigated the several aspects of the plant and collated its extensive pharmacological properties with their applications in this review. The plant is widely cultivated in many parts of the world, and as more and more evidence of its numerous therapeutic applications suggesting the plant has dominant significance as a medicinal plant. Further, Andrographolide is an extremely bitter substance, so this is referred the “King of Bitters”. Moreover, leaves and roots of Andrographis paniculata contain a labdane diterpenoid called andrographolide, which has anti-HIV, anti-inflammatory, and anti-cancer activities. It performs functions as a metabolite, analgesic, anti-HIV, and antineoplastic medication. It is a labdane diterpenoid, a labdane alcohol, a primary alcohol, a secondary alcohol, a carbocyclic molecule, and a gamma-lactone.