Twenty-eight coumarins, including 7 furocoumarins, were examined for their
activity of induction of terminal differentiation of human promyelocytic le
ukemia cells (HL-60) by nitro blue tetrazolium (NBT) reducing, nonspecific
esterase, specific esterase and phagocytic activities. Esculetin, nordalber
gin, 6,7-dihydroxy-4- methylcoumarin and imperatorin had strong activity am
ong the coumarins examined. HL-60 cells treated with these coumarins differ
entiated into mature monocyte/macrophage. The structure-activity relationsh
ip established from the results revealed that 6,7-dihydroxy moiety had an i
mportant role in the induction of differentiation of HL-60.