Nowadays, phytotherapy is considered by many scientists as the ancestor and the basis of the actual medicine. This old discipline rely in the pharmacological properties of plants to treat various diseases and conditions and supported human beings in all aspect throughout their evolution which allowed several civilizations to develop several remedies, for example to treat wounds, problems related to gastrointestinal transit and even poison. The different plant species that compose Asteraceae family contribute in several sectors, especially in gastronomy, cosmetics and medicine. Indeed, Centaurea is considered an important genus in this family and several phytocompounds contained in Centaurea species are considered nowadays a reference for pharmaceutical industries to develop new drugs with fewer side effects. However, several mechanisms remain ambiguous for scientific community to clearly explain the pharmacological properties of secondary metabolites of plants in order to fully exploit this natural resource. The objective of this book is to summarize and valorize the phytochemical and pharmacological properties of some Centaurea species previously studied.