Prodifferentiation Activity of Novel Vitamin D₂ Analogs PRI-1916 and PRI-1917 and Their Combinations with a Plant Polyphenol in Acute Myeloid Leukemia Cells.

1α,25-dihydroxyvitamin D₃ (1,25D3) is a powerful differentiation inducer for acute myeloid leukemia (AML) cells. However, 1,25D3 doses required for differentiation of AML cells may cause lethal hypercalcemia in vivo. There is evidence that vitamin D₂ is less toxic than vitamin D₃ in animals.

Novel analogs of 1,25-dihydroxyvitamin D combined with a plant polyphenol as highly efficient inducers of differentiation in human acute myeloid leukemia cells.

1α,25-Dihydroxyvitamin D [1,25(OH)D] is known to act as a powerful differentiation inducer in various types of cancer cells, including acute myeloid leukemia (AML) cells. However, supraphysiological concentrations of 1,25(OH)D required to induce terminal maturation of AML cells can cause lethal hypercalcemia in vivo. Here we characterized the differentiation-inducing effects of novel double-point modified analogs of 1,25-dihydroxyvitamin D [1,25(OH)D], PRI-5201 and PRI-5202 [Pietraszek et al.