Brazilin is a promising natural red dye, extracted from the wood of Caesalpinia sappan L. It exhibits several pharmacological activities including anti-inflammatory, antioxidant, anti-depressant and anxiolytic, anti-diabetic, anticancer, antibacterial, and vasorelaxant. Moreover, bioavailability studies demonstrated that brazilin is quickly absorbed into the bloodstream. The data were collected from several databases as ScienceDirect, Web of Science, Pubmed and Proquest. This review is designed to conduct an in-depth search on its pharmacological activities, as well as the underlying cell signaling pathways and mechanism of actions. In addition, we have addressed the bioavailability and structural analysis of brazilin and its close derivatives, safety and quality profiles, and toxicological status. Brazilin with its safety characteristics and acceptable bioavailability, has the potential to touch numerous natural grids, thus, it is possible that this medicinally effective molecule will assist as a promising principal for the development of drug in management of different disorders.
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