Cytotoxic effect of TDZ on human cervical cancer cells

被引:20
作者
Enkhtaivan, Gansukh [1 ]
Kim, Doo Hwan [1 ]
Pandurangan, Muthuraman [1 ]
机构
[1] Konkuk Univ, Dept Bioresources & Food Sci, Seoul 143701, South Korea
关键词
Thiadiazol; Mitochondrial membrane potential; HeLa cells; Anticancer; DEATH IN-SITU; AUTODOCK VINA; THIDIAZURON; DOCKING; IDENTIFICATION; REGENERATION; MITOCHONDRIA; CASPASE-3; ACCURACY;
D O I
10.1016/j.jphotobiol.2017.06.032
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The present study investigates the anticancer activity of Thidiazuron (TDZ). Anticancer activity of TDZ was evaluated in cervical carcinoma cells (HeLa cells). Sulforhodamine-B (SRB) assay indicates that TDZ was about 100 times more toxic to the cancer cell than normal cells. TUNEL assay showed TDZ induced DNA damage in tumor cells. The loss of mitochondrial membrane potential (MMP) in cancer cells was observed following TDZ treatment. The Bax and bc1-2 gene expression ratio are highly responsible for the regulation of MMP balance, and these ratio was significantly altered following TDZ treatment. The p53 and caspase-3 expressions were increased in cancer cells following treatment. Caspase-3 activation is the key factor for apoptosis. Cytotoxicity of TDZ on HeLa cells was 100 times higher than normal kidney cell (MDCK cells). Moreover, the anticancer activity of TDZ was tested by DNA damage, mitochondrial dysfunction, some gene expression and caspase-3 inhibition in silica. TDZ detected has higher ability on early apoptosis of cancer cell through DNA damage. Additionally, cancer cellular MMP was significantly reduced under inoculation of TDZ. In silica assay confirmed that TDZ was able to bind with the active site of the capase-3 protein. Therefore, taking all these data together it is suggested that the TDZ may be a potential agent to act against cervical cancer cells.
引用
收藏
页码:493 / 498
页数:6
相关论文
共 31 条
[1]   Comparing the Suitability of Autodock, Gold and Glide for the Docking and Predicting the Possible Targets of Ru(II)-Based Complexes as Anticancer Agents [J].
Adeniyi, Adebayo A. ;
Ajibade, Peter A. .
MOLECULES, 2013, 18 (04) :3760-3778
[2]   Pharmacophore Modeling, Docking and Molecular Dynamics Studies on Caspase-3 Activators Binding at β-Tubulin Site [J].
Bhunia, Shome S. ;
Singh, Supriya ;
Saxena, Shruti ;
Saxena, Anil K. .
CURRENT COMPUTER-AIDED DRUG DESIGN, 2015, 11 (01) :72-83
[3]   Stress, inflammation and cardiovascular disease [J].
Black, PH ;
Garbutt, LD .
JOURNAL OF PSYCHOSOMATIC RESEARCH, 2002, 52 (01) :1-23
[4]   There is no evidence that mitochondria are the main source of reactive oxygen species in mammalian cells [J].
Brown, Guy C. ;
Borutaite, Vilmante .
MITOCHONDRION, 2012, 12 (01) :1-4
[5]  
Cagmat E, 2012, J NEUROTRAUM, V29, pA147
[6]   An In Silico Appraisal of Azoic and Disulphide Derivatives for Anticancer Activity Against HPV E6 Oncoprotein to Medicate Cervical Cancer [J].
Choudhury, Arpita Das ;
Choudhury, Manabendra Dutta ;
Chetia, Pankaj ;
Chowdhury, Abhishek ;
Talukdar, Anupam Das .
COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING, 2014, 17 (01) :38-46
[7]   ANTICANCER DRUGS Advancing precision medicine in silico [J].
Cully, Megan .
NATURE REVIEWS DRUG DISCOVERY, 2015, 14 (05) :311-311
[8]  
Enkhtaivan G, 2016, SAUDI J BIOL SCI
[9]  
Esch T, 2002, MED SCI MONITOR, V8, pRA93
[10]   Probing the impact of quercetin-7-O-glucoside on influenza virus replication influence [J].
Gansukh, Enkhtaivan ;
Kazibwe, Zakayo ;
Pandurangan, Muthuraman ;
Judy, Gopal ;
Kim, Doo Hwan .
PHYTOMEDICINE, 2016, 23 (09) :958-967