Lawsonia inermis is a single-species genus of the Lythraceae family, its leaves, stem bark, roots, flowers and seeds have been used in traditional medicine. It has been paid more attention by scholars from many countries because of their various types of compounds and significant physiological activities. The plant is reported to contain quinones, phenylpropanoids, flavonoids, terpenoids, phenolic compounds and fatty acids. Modern pharmacological studies have demonstrated that the plant performs antimicrobial, antioxidant, anticancer and antiparasitic activity. This article mainly summarizes the research advances of chemical constituents and biological activities of Lawsonia inermis, for its further development and utilization.