The HL-60 differentiation-inducing compounds in bergamot fruits were isolat
ed with column chromatography and identified as bergamottin, bergapten, and
citropten by H-1 and C-13 NMR. Their HL-60 differentiation-inducing activi
ty was measured by examining nitro blue tetrazolium (NBT) reducing, nonspec
ific acid esterase (NSE), specific esterase (SE), and phagocytic activities
, and bergamottin showed the strongest activity among the coumarins isolate
d from bergamot fruits. The structure-activity relationship obtained from H
L-60 differentiation assay suggests that hydrophobicity of furocoumarins is
correlated with their activity.