Prolyl endopeptidase inhibitors from caryophylli flos

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Three prolyl endopeptidase inhibitors were isolated and identified as luteolin, quercetin and β-sitosterol-3-O-β-D-glucopyranoside with IC50 of 0.17, 0.19 and 27.5 ppm, respectively. The inhibition of two flavonoids were non-competitive with substrate. Twenty authentic flavonoids were tested in order to investigate structure-activity relationship. No significant relationship was found in them, however, catechol moiety of B-ring and 7-OH group in flavonoid skeleton were seemed to be responsible for the stronger activity.

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