Dracaena cinnabari (D. cinnabari) is an endemic plant located in Socotra Island, Yemen. Deep red resin attained from different plant species including D. cinnabari is commonly known as dragon’s blood. In folk medicine, it is prescribed for the treatment of traumatic dermal, dental, and eye injuries as well as blood stasis, pain, and gastrointestinal diseases in humans. Numerous studies have investigated that this resinous medicine has antidiarrheal, antiulcer, antimicrobial, antiviral, antitumor, anti-inflammatory, analgesic, wound healing, and antioxidant activity. Several phytochemicals have been isolated from D. cinnabari, including the biflavonoid cinnabarone, triflavonoids, metacyclophanes, chalcones, chalcanes, dihydrochalcones, sterols, and terpenoids. The present review highlights the structures and bioactivities of main phytochemicals isolated from D. cinnabari regarding the botany and pharmacological effects of the resin derived from this plant.