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Phytother Res. 2016 Jan;30(1):144-51. doi: 10.1002/ptr.5515. Epub 2015 Nov 9.

Identification and Characterization of Baicalin as a Phosphodiesterase 4 Inhibitor.

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Bio-Center, Gyeonggi Institute of Science and Technology Promotion, Suwon, Gyeonggi-do, 443-270, Korea.
Bio Convergence Center, Jeju Technopark, Jeju city, Jeju-do, 699-121, Korea.


Asthma is a chronic inflammatory disease of lung airways, and pharmacological inhibitors of cyclic adenosine monophosphate-specific phosphodiesterase 4 (PDE4) have been considered as therapeutics for the treatment of asthma. However, development of PDE4 inhibitors in clinical trials has been hampered because of the severe side effects of non-selective PDE4 inhibitors. Here, screening of a plant extract library in conjunction with dereplication technology led to identification of baicalin as a new type of PDE4-selective inhibitor. We demonstrated that while rolipram inhibited the enzyme activity of a range of PDE4 subtypes in in vitro enzyme assays, baicalin selectively inhibited the enzyme activity of PDE4A and 4B. In addition, baicalin suppressed lipopolysaccharide-induced TNF-α expression in macrophage where PDE4B plays a key role in lipopolysaccharide-induced signaling. Furthermore, baicalin treatment in an animal model of allergic asthma reduced inflammatory cell infiltration and TNF-α levels in bronchoalveolar lavage fluids, indicating that the antiinflammatory effects of baicalin in vivo are attributable, in part, to its ability to inhibit PDE4.


TNF-α; asthma; baicalin; phosphodiesterase

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