Novel piperazine core compound induces death in human liver cancer cells: possible pharmacological properties

Abstract

The current study evaluates the cytotoxic mechanism of a novel piperazine derivate designated as PCC against human liver cancer cells. In this context, human liver cancer cell lines, SNU-475 and 243, human monocyte/macrophage cell line, CRL-9855, and human B lymphocyte cell line, CCL-156, were used to determine the IC50 of PCC using the standard MTT assay. PCC displayed a strong suppressive effect on SNU-475 and SNU-423 cells with an IC50 value of 6.98 ± 0.11 μg/ml and 7.76 ± 0.45 μg/ml respectively, after 24 h of treatment. Significant dipping in the mitochondrial membrane potential and elevation in the released of cytochrome c from the mitochondria indicated the induction of the intrinsic apoptosis pathway by PCC. Activation of this pathway was further evidenced by significant activation of caspase 3/7 and 9. PCC was also shown to activate the extrinsic pathways of apoptosis via activation of caspase-8 which is linked to the suppression of NF-ƙB translocation to the nucleus. Cell cycle arrest in the G1 phase was confirmed by flow cytometry and up-regulation of glutathione reductase expression was quantified by qPCR. This study suggests that PCC is a simultaneous inducer of intrinsic and extrinsic pathways of apoptosis in liver cancer cell lines.

The molecular mechanism of the anticancer effect of Artonin E in MDA-MB 231 triple negative breast cancer cells

“…Aliquots of 20 μL of the cell suspension were examined under Carl Zeiss Axioskop plus-2 fluorescence microscope. At least 200 cells in each of three fields were immediately assessed for viability, early, late apoptosis and necrosis [ 12 ]. The experiment was carried out in triplicate.…”

“…There are two major pathways of apoptosis viz: the extrinsic and mitochondrial (intrinsic) pathways [ 11 ]. Both pathways are controlled by a number of gene families which finally lead to the phagocytosis of cells by adjacent cells [ 12 ], [ 13 ]. In spite of the unique attribute of conventional chemotherapies in inducing apoptosis, many of them are constantly facing resistance coupled with their alarming side effects.…”

Apoptosis-Inducing Effect of Artonin E in Breast Cancer

“…A compromise in the phospholipid membrane asymmetry of a cell, results in the externalization of phosphatidylserine. To further strengthen the assessment of the apoptotic mode of cell death, annexin V FITC in combination with a DNA binding fluorochrome, PI were utilized [9,19,20]. In this study, Artonin E has been seen to significantly reduce the population of viable breast cancer cells in a concentration and time dependent manner while increasing the population undergoing apoptosis.…”

“…Acridine Orange (AO) and propidium iodide (PI) double staining assay was employed to determine the effect of Artonin E in the induction of breast cancer cell death. A total of 3 × 10 5 MCF-7 breast cancer cells were seeded in a six-well plate and exposed to various treatment as well as necrosis [9]. The experiment was performed in triplicate.…”

Retraction: Mechanism of action of novel piperazine containing a toxicant against human liver cancer cells

“…An investigation by PeerJ has determined that several of the images in the publication cited above have been inappropriately manipulated (for example Figure 7, Figure 12, Figure 13); that some of the images have been inappropriately re-used either in, or from, other publications (for example, versions of Figures 2 through 8 have all appeared in different publications suggesting to represent different cells, cell lines, or conditions (Samie et al, 2016a; Samie et al, 2016b)); and that large sections of the text have appeared in other publications (Samie et al, 2016a; Samie et al, 2016b; Muszalska et al, 2005). …”