Selective inhibition of platelet lipoxygenase by baicalein

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Abstract

The effects of various flavonoids on platelet lipoxygenase and cyclooxygenase activities were studied. Baicalein selectively inhibited platelet lipoxygenase. The concentration for 50% inhibition (ID50) was 0.12 μM for platelet lipoxygenase and 0.83 mM for platelet cyclooxygenase. Therefore, the ID50 value for the cyclooxygenase was 6917 times that for the lipoxygenase. Baicalin also selectively inhibited the lipoxygenase, but it was less potent (ID50=100 μM). Other flavonoids tested had no inhibitory effect on either enzyme.

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    Similarly, oroxylin A has been shown to inhibit COX-2 expression and reduce the synthesis of PGE2 in LPS-induced macrophages [78,79]. Furthermore, baicalin can selectively inhibit the activity of platelet LOX [184] and 5-LOX and reduce production of the 5-LOX metabolite LT [185,186]. Baicalin has also been shown to inhibit the expression of COX-2 in rats with brain injury [187,188], and found to have significant anti-depressant activity in mice with mild chronic stress by inhibiting COX-2 expression and activity and reducing PGE2 levels in the frontal cortex and hippocampus [189].

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