AbstractAndrographis paniculata is an annual medicinal herb from the family Acanthaceae. Andrographolide is generally considered an essential bioactive component of plant A. paniculata. Since ancient times, it has been widely recognized for its therapeutic qualities and has attracted the scientific and medical communities' attention. This review summarizes the molecular, clinical, and in vitro research of compound andrographolide and its mechanism of action. Andrographolide, when combined with other enhancing agents, offers a wide variety of health benefits. The therapeutic potential of andrographolide has been exemplified and exhibited by directly regulating genes and indirectly interacting with small molecules and different enzymes. This review compiles and consolidates the pharmacological action of andrographolide and its analogs and deciphers the gaps that have hindered its use in medicinal research.