An overview of pharmacological activities of baicalin and its aglycone baicalein: New insights into molecular mechanisms and signaling pathways

• Published in: Iranian journal of basic medical sciences Vol. 25; no. 1; pp. 14 - 26
• Main Authors: Hu, Zhihua, Guan, Yurong, Hu, Wanying, Xu, Zhiyong, Ishfaq, Muhammad
• Format: Journal Article
• Language: English
• Published: Iran Mashhad University of Medical Sciences 01.01.2022
• Subjects: Antiviral drugs; Asthma; Atherosclerosis; baicalein; baicalin; Cancer; Cell cycle; Chemotherapy; Computer science; Cytokines; Drug dosages; Flavonoids; Hypertension; Inflammation; Inflammatory diseases; Medical imaging; Medical research; mitochondrial functions; Optimization; Proteins; Pulmonary arteries; Reactive oxygen species; Review; Rheumatoid arthritis; Smooth muscle; Therapeutic drug monitoring; Traditional Chinese medicine; Baicalein; Mitochondrial functions; Baicalin; Inflammatory diseases; Cancer
• ISSN: 2008-3866; 2008-3874
• DOI: 10.22038/IJBMS.2022.60380.13381

The flavonoids, baicalin, and its aglycone baicalein possess multi-fold therapeutic properties and are mainly found in the roots of (L.) Kurz and 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.