Since ancient, Chelidonium majus is well organized for its therapeutic values. Only recently, scientists have been aware of its new medicinal aspects. Regarding ongoing reports and new medicinal properties of this plant we were prompted to update Phytochemistry and pharmacology of C. majus. Data were gathered using of scientific books, journals, articles and websites including Pubmed, Scopus and Google Scholar up to 10th June 2012. C. majus extracts are important in drug development with numerous pharmacological functions in the western phytotherapy and in traditional medicines especially in China. C. majus is famous in traditional medicines for the treatment of gallstones and dyspepsia and various inflammatory diseases including atopic dermatitis and extensively used against various liver ailments. In addition, C. majus has recently been shown to have antiinflammatory, antimicrobial, antitumoral, anti-osteoporotic , antitussive, antiviral, antifungal, oncostatic, hepatoprotective, diuretic, and eye-regenerative, radioprotection, antioxidant ,cytotoxic effects, as well as anthelmintic ,phototoxic, algicide, cyanocide and cytostatic activities. The valuable therapeutic aspects of this plant are mostly correlated to the existence of isoquinoline alkaloids, flavonoids, phenolic acids and proteins. Due to the easy collection of the plant and remarkable biological activities, this plant has become a potent medicine in many parts of the world. This overview presents comprehensive analyzed information on the chemical and clinical aspects of C. majus.