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Medicinal plants are a valuable source of supplementary remedies for the treatment of various ailments. Lawsonia inermis (belongs to family Lythraceae) or commonly known as Henna is a glabrous and branching small tree that is indigenous to the subtropical regions of Asia and North Africa. It has traditionally been used as a dandruff-fighting and antifungal agent when applied to the hair, hands, and feet. The staining properties of Henna are derived from the lawsone content, which is found primarily in the leaves. The purpose of this review is to conduct a literature search and critically review the relevant published articles on the phytochemical and pharmacological activities of L. inermis. The phytochemical screening reported that naphthoquinone derivatives, Henna essential oil, flavonoids, tannins, phenols, quinones, alkaloids, glycosides and saponins can be isolated from various parts of the Henna tree. The selection of appropriate solvents is critical in phytochemical screening, as different solvents resulted in different extraction yields. The pharmacological activities found in Henna are ameliorative activity, alleviating wound healing process, antifungal, antioxidant, antibacterial, hepatoprotective, nootropic, anti-ulcer, anti-inflammatory and anti-cancer activity. In conclusion, phytochemical screening is critical for identification of plants constituents, and Henna possesses wide range of pharmacological properties. As a result, further studies on Henna's phytochemical and pharmacological qualities should be done to fully exploit its benefits. [ABSTRACT FROM AUTHOR]