Bioactive natural products continue to play an important role in the discovery of lead compounds for new-drug developments. Although for more than a century, extensive studies have been made on isolation and identification of bioactive substances from marine and terrestrial microorganisms, medicinal plants and animals, Chemistry of natural product is still of great importance as a basic science since natural products have made significant contributions to development of new drugs as well as to progress of basic studies of life sciences. The Combretaceae are a family of flowering plants in the order Myrtales and widespread in the subtropics and tropics. Combretaceae is a large family, which is distributed in approximately 20 genera with 600 species. Among them Combretum and Terminalia are the largest two with about 370 and 200 species respectively. Both species possess significant biological activities and also used in traditional medicine. This review mainly discussed about the importance of Combretum and Terminalia species against the different types of diseases.