The genus Pinellia(Araceae), consisting of nine species, is mainly distributed in Eastern Asia. In traditional medicine, some Pinellia species have long been used for the treatment of various ailments, such as cough, vomiting, inflammation, epilepsy, cervical cancer and traumatic injury. Pharmacological studies revealed that Pinellia species possess a wide range of biological activities including cytotoxic, anti-tumor, antiemetic, insecticidal, antitussive, antimicrobial and anticonvulsant activities. However, some species also showed significant toxicity such as reproductive toxicity, mucosal irritation and hepatotoxicity. Most of these bioactivities and toxicity can be explained by the presence of various alkaloids and lectins. This review summarizes the ethnopharmacological uses, phytochemical constituents, pharmacological activities and toxicity of Pinellia species. (C) 2013 Elsevier B.V. All rights reserved.