scholarly journals Mechanism of action of novel piperazine containing compound toxicant against human liver cancer cells

PeerJ ◽  
2016 ◽  
Vol 4 ◽  
pp. e1588 ◽  
Author(s):  
Nima Samie ◽  
Sekaran Muniandy ◽  
MS Kanthimathi ◽  
Batoul Sadat Haerian

The purpose of this study was to assess the cytotoxic potential of a novel piperazine derivative (PCC) against human liver cancer cells. SNU-475 and 423 human liver cancer cell lines were used to determine the IC50 of PCC using the standard MTT assay. PCC displayed a strong suppressive effect on liver cancer cells with an IC50 value of 6.98 ± 0.11 µM and 7.76 ± 0.45 µM against SNU-475 and SNU-423 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-κB 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. Results of this study suggest that PCC is a potent anti-cancer agent inducing both intrinsic and extrinsic pathways of apoptosis in liver cancer cell lines.

2016 ◽  
Vol 6 (1) ◽  
Author(s):  
Nima Samie ◽  
Sekaran Muniandy ◽  
M. S. Kanthimathi ◽  
Batoul Sadat Haerian ◽  
Raja Elina Raja Azudin

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.


BMC Cancer ◽  
2011 ◽  
Vol 11 (1) ◽  
Author(s):  
Laura Pelletier ◽  
Sandra Rebouissou ◽  
Danijela Vignjevic ◽  
Paulette Bioulac-Sage ◽  
Jessica Zucman-Rossi

2018 ◽  
Vol 47 (43) ◽  
pp. 15338-15343
Author(s):  
Fatai Afolabi ◽  
Wided Souissi ◽  
Guillaume Rivière ◽  
Clément Lemaitre ◽  
S. Mark Roe ◽  
...  

A series of cationic gold(i) pyrazole complexes were synthesised regioselectively and in excellent yields and tested against human liver cancer cell lines HepG2.


Kanzo ◽  
1989 ◽  
Vol 30 (3) ◽  
pp. 338-344 ◽  
Author(s):  
Yuuji SAKAI ◽  
Yoshihiro FUKUDA ◽  
Kanji HASE ◽  
Itsuo YAMAMOTO ◽  
Shigeharu DOKOH ◽  
...  

Sign in / Sign up

Export Citation Format

Share Document