Acridones as inducers of HL-60 cell differentiation

Fifteen acridone alkaloids were examined for their activity of induction of human promyelocytic leukemia cell (HL-60) differentiation. HL-60 cells wer e differentiated into mature monocyte/macrophage by atalaphyllidine (9), at alaphyllinine (12), and des-N-methylnoracronycine (13). The activities of N ET reduction, nonspecific esterase, and phagocytosis, were induced by 2.5 m u M of 9, 12, and 13. After a 4-day treatment, 9, 12, and 13 at 10 mu M inh ibited clonal proliferation of HL-60 cells by 28, 96, and 63%, respectively . The structure-activity relationship established from the results revealed that hydroxyl group at C-1 and prenyl group at C-2 had an important role. (C) 1999 Elsevier Science Ltd. All rights reserved.