Boldine is an aporphine (isoquinoline) alkaloid found in many angiosperms, particularly the more “primitive” families. Despite its wide distribution, it is seldom abundant and the only commercial source is the bark of the Chilean boldo tree (Peumus boldus Mol.). Due to the medicinal use of boldo leaf infusions in Chile and later in numerous other countries, an early chemical study led to the discovery of boldine followed by the study of its pharmacological properties. In line with its traditional use as an aid to digestion, it was first shown to increase bile flow, and later on to have strong antioxidant and antiinflammatory properties and to antagonize adrenergic and dopaminergic neurotransmission. More recently a plethora of novel pharmacological actions has been revealed, initiating several highly promising research avenues with high potential for clinical development.