Caesalpinia sappan L. (CS) is a plant of Leguminosae family, commonly known as Brazil or Sappan wood. CS is distributed in Southeast Asia and its dried heartwood has been used as traditional ingredient of food or beverages and has a wide variety of medicinal properties. Higher extraction yield of CS wood was achieved with 95% ethanol for 2 h. Chemical constituent's investigation of sappan wood resulted in the isolation of various structural types of phenolic components including one xanthone, one coumarin, three chalcones, two flavones three homoisoflavonoids and brazilin. Brazilin [(6a S-cis)-7, 11b-dihydrobenz[b]indeno[1,2-d]pyran-3,6a,9,10(6H)- tetrol], a major and active compound found in CS heartwood. Most of the folkloric uses of brazilin were validated by the scientific studies such as antioxidant, antibacterial, anti-inflammatory, anti-photoaging, hypoglycemic, vasorelaxant, hepatoprotective and anti-acne activity. CS heartwood extract is safe and did not produce any acute or subacute toxicity in both male and female rats. Brazilin is the safe natural compound having potential to develop as a medicinal compound with application in food, beverage, cosmetics and pharmaceutical industries to screen its clinical use in modern medicine. The information gained could provide the important and potential approach for pharmaceutical researcher to implicate the knowledge of brazilin in the formulation of new drug and to reveal therapeutic and gaps requiring future research opportunities. More studies are needed to evaluate the potential application of brazilin as preservative and coloring agent in food processing industries.