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Eur J Med Chem. 2017 May 5;131:68-80. doi: 10.1016/j.ejmech.2017.03.004. Epub 2017 Mar 6.

Therapeutic potentials of baicalin and its aglycone, baicalein against inflammatory disorders.

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Department of Chemistry, Tripura University, Suryamaninagar 799022, Tripura, India. Electronic address:
Department of Chemistry, Dasaratha Deb Memorial College, Khowai 799201, Tripura, India.
Department of Chemistry, National Institute of Technology, Agartala 799055, Tripura, India.
Department of Chemistry, Tripura University, Suryamaninagar 799022, Tripura, India.
Department of Biochemistry and Molecular Genetics, University of Virginia, School of Medicine, Charlottesville, 1300 Jefferson Park Ave, VA22908, USA.


The flavonoids, baicalin (5,6-dihydroxy-2-phenyl-4H-1-benzopyran-4-one-7-O-d-β-glucuronic acid) 1 and its aglycone, baicalein 2 are found in edible medicinal plants, Scutellaria baicalensis Georgi and Oroxylum indicum (L.) Kurz in abundant quantities. The antioxidant and anti-inflammatory effects of these flavonoids have been demonstrated in various disease models, including diabetes, cardiovascular diseases, inflammatory bowel diseases, gout and rheumatoid arthritis, asthma, neurodegenerative-, liver- and kidney diseases, encephalomyelitis, and carcinogenesis. These flavonoids have almost no toxicity to human normal epithelial, peripheral and myeloid cells. Their antioxidant and anti-inflammatory activities are largely due to their abilities to scavenge the reactive oxygen species (ROS) and improvement of antioxidant status by attenuating the activity of NF-κB and suppressing the expression of several inflammatory cytokines and chemokines including monocyte chemotactic protein-1 (MCP-1), nitric oxide synthase, cyclooxygenases, lipoxygenases, cellular adhesion molecules, tumor necrosis factor and interleukins. In this review, we summarize the antioxidant and anti-inflammatory effects of baicalin and baicalein with molecular mechanisms for their chemopreventive and chemotherapeutic applications in the treatment of inflammatory-related diseases.


Baicalein; Baicalin; Chemoprevention; Flavonoids; Inflammatory diseases

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