Gentiana, a cosmopolitan and important genus of the Gentianaceae family, comprises over 300 species distributed among the world. Phytochemical investigations on the title genus have led to characterization of almost two hundred secondary metabolites. Some of them have shown promising bioactivities. Herein, we have summarized the phytochemical and pharmacological progress of this genus. This review covers the period 1960-June, 2009.