Euphorbia helioscopia L. (Euphorbiaceae), also known as “Sun spurge” is one of used herbs in most parts of the world since thousands of years. This work aims to provide updated comprehensive and categorized information on chemical composition, pharmacological and toxical properties of this plant. To achieve this purpose, several scientific databases were used, including Wiley, PubMed, Web of Science, Springer, Science Direct, Elsevier, and Google Scholar and related books published up to December 2019 were also used as references. After description of its history, botanical characteristics and distribution, this review highlights the different types of secondary metabolites, such as diterpenoids, tannins, glucosides and steroids, which have been isolated from E. helioscopia L. in several researches over the last four decades. Related Twenty five pharmacological activities (among them: antibacterial, antiviral, antioxidant, antifungal, phytotoxic, anthelmintic, antitumor, anti-allergic, anti-asthmatic, cytotoxic, anticancer, allelopathic, anti-nociceptive, anti-inflammatory, anti-pyretic, vasodepressor, antileishmanial, lipid-lowering activity, and triglyceride-lowering activity) are presented and discussed. E. helioscopia L. toxicity related studies against Humans, snails and some herbs are summarised and presented with correspondent references. This study can be used by researches interested by this plant since it resumes all relevant published papers in link with E. helioscopia L.
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