The flavonoids, baicalin, and its aglycone baicalein possess multi-fold therapeutic properties and are mainly found in the roots of Oroxylum indicum (L.) Kurz and Scutellaria baicalensis Georgi. These flavonoids have been reported to possess various pharmacological properties, including antibacterial, antiviral, anticancer, anticonvulsant, anti-oxidant, hepatoprotective, and neuroprotective effects. The pharmacological properties of baicalin and baicalein are due to their abilities to scavenge reactive oxygen species (ROS) and interaction with various signaling molecules associated with apoptosis, inflammation, autophagy, cell cycle, mitochondrial dynamics, and cytoprotection. In this review, we summarized the molecular mechanisms underlying the chemopreventive and chemotherapeutic applications of baicalin and baicalein in the treatment of cancer and inflammatory diseases. In addition, the preventive effects of baicalin and baicalein on mitochondrial dynamics and functions were highlighted with a particular emphasis on their anti-oxidative and cytoprotective properties. The current review highlights could be useful for future prospective studies to further improve the pharmacological applications of baicalein and baicalin. These studies should define the threshold for optimal drug exposure, dose optimization and focus on therapeutic drug monitoring, objective disease markers, and baicalin/baicalein drug levels.
Keywords: Baicalein; Baicalin; Cancer; Inflammatory diseases; Mitochondrial functions.