Baicalein

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Baicalein (5,6,7-trihydroxyflavone) is a flavone, a type of flavonoid,[1] originally isolated from the roots of Scutellaria baicalensis and Scutellaria lateriflora. It is also a constituent of Oroxylum indicum (Indian trumpetflower) and thyme.[2] It is the aglycone of baicalin.

Pharmacology

Baicalein, along with its glucuronide baicalin, is a positive allosteric modulator of the benzodiazepine site and a non-benzodiazepine site of the GABAA receptor, but with an affinity over 250× lower than diazepam.[3][4][5] It displays subtype selectivity for α2 and α3 subunit-containing GABAA receptors.[6]

The flavonoid has been shown to inhibit certain types of lipoxygenases.[7]

Baicalein is an inhibitor of CYP2C9,[8] an enzyme of the cytochrome P450 system that metabolizes drugs in the body.

A derivative of baicalin is a known prolyl endopeptidase inhibitor.[9]

See also

References

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