Abstract: This study focuses on the anti-inflammatory activity of andrographolide, a diterpenoid compound from Andrographis paniculata, that have been observed in animals and in vitro in different cells of human and animals. Studies included activities of andrographolide and the features of the target, especially limited to transcription factors NF-kappaB. The active site of NF-kappaB, called DNA binding region is found to have mainly positive potential. In order to have an electrostatic complementarity specific inhibitor should have negative potential. Andrographolide has three hydrogen bond donors (H atoms in hydroxyl groups attached to C-3, C-19 and C-14), five hydrogen bond acceptors (O atoms in hydroxyl groups attached to C-3, C-19 and C-14, carbonyl and lactone) and log P-value 2.9. It fulfills Lipinski’s rules of five criteria of drug properties. This compound has different mechanisms of anti-inflammatory activity. It can inhibit the activation of NF-kappaB, suppresses inducible nitric oxide synthase (iNOS) expression. It also prevents oxygen radical production by human neutrophils and inhibits COX-2 expression in human fibroblast cells. This compound also exerts anticancer and antitumour activities, hepatoprotective against various inducers, immunomodulator, antioxidant, antidiabetic, antimicrobe and antivirus activities. Synthetic analogues of the compound which have been created and analyzed also showed similar activities.