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On the basis of our previous finding that humulone, a bitter acid from beer hop extract, was a potent inhibitor of bone resorption and inhibited the catalytic activity of cyclooxygenase-2 (COX-2) and more potently the transcription of the COX-2 gene, we examined the effect of humulone on
Humulone, a bone resorption inhibitor isolated from hop extract, induced apoptosis in the premyocytic leukemia cell line HL-60 between 1 and 100 micrograms/ml. Our data suggested that there was a correlation between the apoptosis-inducing activity of humulone and its antioxidative activity.
The active form of vitamin D, 1alpha,25-dihydroxyvitamin D3 (VD3), inhibits proliferation and induces differentiation of myelomonocytic leukemia cells, but its clinical use is limited by the adverse effect of hypercalcemia. VD3 mobilizes calcium stores from bone by inducing the dissolution of bone
We searched hop extract for active component(s) that inhibited bone resorption in the pit formation assay, and isolated xanthohumol and humulone as active ingredients. Especially humulone had extraordinarily strong inhibitory activity and the IC50 (concentration of 50% inhibition) value was 5.9 x