Wikstroemia indica (L.) C. A. Mey. is a member of family Thymelaeaceae and mainly distributes in middle and southeast part of China. As a traditional Chinese herb, this plant has long been employed as antipyretics, detoxicants, expectorants, vermifuges as well as aborticides in clinic practice. However, its use has mainly been based on empirical findings during hundreds and thousands of years. Recent studies indicated that W. indica contains abundant bioactive components including flavonoids, biflavonoids, coumarins, lignans, volatile oils, polysaccharides etc. This paper provides a comprehensive review of pharmacological relevant compounds of W. indica that have been characterized to date, and introduces the research progresses supporting its pharmacological action and clinical application. Particular attention has been given to antibacterial, antiviral, anti-inflammatory, anti-tumor and antifertility effects. Some examples of clinical applications of prepared W. indica in treatment of various diseases are outlined. Finally, the trend and necessity of future research, such as quantification of individual constituents extracted from W. indica and the assessment of their pharmacological activities in human body are proposed.