Int J Biochem Mol Biol 2011;2(1):78-88
Original Article
Novel piperazine induces apoptosis in U937 cells
Josiah J. Sampson, III, Isaac O. Donkor, Tien L. Huang, Samuel E. Adunyah
Department of Biochemistry and Cancer Biology, Meharry Medical College, Nashville, TN, 37208, USA; Department of Pharmaceutical
Sciences, University of Tennessee at Memphis, Memphis, Tennessee, 38163, USA; College of Pharmacy, Xavier University, New Orleans, LA,
70125, USA.
Received January 12, 2011; accepted January 26, 2011; Epub January 30, 2011; published February 15, 2011
Abstract: The effect of 1,4-bis-(4-(1H-benzo[d]imidazol-2-yl-phenyl)) piperazine (BIPP), a newly synthesized piperazine derivative, on U937
leukemia cell viability was investigated. We show that BIPP induces dose-responsive apoptotic cell death in U937 cells by intrinsic
mechanisms of apoptosis. Maximum apoptotic effect of BIPP on U937 cells was observed at 12.8μM. BIPP-induced apoptosis was evident by
characteristics such as altered annexin-V binding, caspase activation, loss of mitochondrial membrane potential (MMP) and cytochrome c
release. BIPP also differentially activates initiator and effector caspases combined with the loss of MMP strongly suggesting that BIPP causes
an intrinsic apoptosis in U937 leukemia cells. Due to our observations that BIPP induces leukemia cell death without significantly affecting
normal cells, our data suggests that it may be a potential therapeutic agent for human myeloid leukemia. (IJBMB1101003).
Keywords: Piperazine, apoptosis, cancer, caspase, mitochondria, membrane potential
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Address all correspondence to:
Dr. Samuel E. Adunyah
Department of Biochemistry and Cancer Biology
Meharry Medical College, 1005 Dr. D.B. Todd Blvd.
Nashville, TN, 37208, USA.
Tel: 615-327-6345
E-mail: sadunyah@mmc.edu

