Plant sources, chemical properties, bioactivities, as well as the synthesis of indigo dye and its derivatives, are reviewed in this paper. These compounds were chosen because of their significant benefits and scope of application as both coloring agents in the textile industry and as pharmacologically active natural products. Their use in traditional chinese medicine (TCM) has directed the attention of European researchers and medical doctors alike. The preparation of indigoferous plants--Indigo naturalis is currently about to be introduced into the European Pharmacopoeia.