Ethnopharmacological relevance: The use of Lawsonia inermis L. (henna) for medicinal and cosmetic purposes is inextricably linked to ancient and modern cultures of North Africa and Asia. Literature and artwork indicates that Lawsonia inermis played an important holistic role in the daily lives of some ancient cultures, providing psychological and medicinal benefits, as well as being used for personal adornment. Although henna was historically applied to the hands and feet to protect against fungal pathogens and to hair to combat lice and dandruff, other traditional uses include the treatment of liver and digestive disorders, reduction of tissue loss in leprosy, diabetic foot disorders and ulcers.Phytochemistry: Almost 70 phenolic compounds have been isolated from various parts of the plant. Naphthaquinones, which include the dyeing principle lawsone, have been linked to many of the pharmacological activities. The terpene, beta-ionone is largely responsible for the pungent odour of the essential oil isolated from the flowers. In addition to other volatile terpenes, some non-volatile terpenoids, a single sterol, two alkaloids and two dioxin derivatives have also been isolated from the plant.Bioactivity: Henna is a pharmacologically important plant with significant in vitro and in vivo biological activities. Although a myriad of pharmacological activities have been documented, the antioxidant and antimicrobial activities are the most thoroughly investigated. Some incidents of adverse reactions following application to the skin have been reported, but these are mainly confined to cases involving individuals with glucose-6-phosphate dehydrogenase deficiency and reactions to adulterants added to henna products.Conclusions: Adulteration of henna is very common and may have resulted in unwarranted scientific findings. Phytochemical profiling studies of the plant, which are crucial for the establishment of proper quality control protocols, are lacking and hamper the development of medicinal products. Although many in vitro studies have been conducted to evaluate the pharmacological activities and many in vivo studies have focussed on the toxicity of extracts, more in vivo studies to validate pharmacological activities are needed. The roles of specific compounds and their synergies have not been comprehensively investigated. (C) 2014 Elsevier Ireland Ltd. All rights reserved.