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The Cytotoxicity of Benzaldehyde Nitrogen Mustard-2-Pyridine Carboxylic Acid Hydrazone Being Involved in Topoisomerase IIα Inhibition
Joint Authors
Liu, Youxun
Fu, Yun
Li, Changzheng
Yang, Yingli
Sun, Xingzhi
Zhou, Sufeng
Source
Issue
Vol. 2014, Issue 2014 (31 Dec. 2014), pp.1-11, 11 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2014-06-05
Country of Publication
Egypt
No. of Pages
11
Main Subjects
Abstract EN
The antitumor property of iron chelators and aromatic nitrogen mustard derivatives has been well documented.
Combination of the two pharmacophores in one molecule in drug designation is worth to be explored.
We reported previously the syntheses and preliminary cytotoxicity evaluation of benzaldehyde nitrogen mustard pyridine carboxyl acid hydrazones (BNMPH) as extended study, more tumor cell lines (IC50 for HepG2: 26.1 ± 3.5 μM , HCT-116: 57.5 ± 5.3 μM, K562: 48.2 ± 4.0 μM, and PC-12: 19.4 ± 2.2 μM) were used to investigate its cytotoxicity and potential mechanism.
In vitro experimental data showed that the BNMPH chelating Fe2+ caused a large number of ROS formations which led to DNA cleavage, and this was further supported by comet assay, implying that ROS might be involved in the cytotoxicity of BNMPH.
The ROS induced changes of apoptosis related genes, but the TFR1 and NDRG1 metastatic genes were not obviously regulated, prompting that BNMPH might not be able to deprive Fe2+ of ribonucleotide reductase.
The BNMPH induced S phase arrest was different from that of iron chelators (G1) and alkylating agents (G2).
BNMPH also exhibited its inhibition of human topoisomerase IIα.
Those revealed that the cytotoxic mechanism of the BNMPH could stem from both the topoisomerase II inhibition, ROS generation and DNA alkylation.
American Psychological Association (APA)
Fu, Yun& Zhou, Sufeng& Liu, Youxun& Yang, Yingli& Sun, Xingzhi& Li, Changzheng. 2014. The Cytotoxicity of Benzaldehyde Nitrogen Mustard-2-Pyridine Carboxylic Acid Hydrazone Being Involved in Topoisomerase IIα Inhibition. BioMed Research International،Vol. 2014, no. 2014, pp.1-11.
https://search.emarefa.net/detail/BIM-478750
Modern Language Association (MLA)
Fu, Yun…[et al.]. The Cytotoxicity of Benzaldehyde Nitrogen Mustard-2-Pyridine Carboxylic Acid Hydrazone Being Involved in Topoisomerase IIα Inhibition. BioMed Research International No. 2014 (2014), pp.1-11.
https://search.emarefa.net/detail/BIM-478750
American Medical Association (AMA)
Fu, Yun& Zhou, Sufeng& Liu, Youxun& Yang, Yingli& Sun, Xingzhi& Li, Changzheng. The Cytotoxicity of Benzaldehyde Nitrogen Mustard-2-Pyridine Carboxylic Acid Hydrazone Being Involved in Topoisomerase IIα Inhibition. BioMed Research International. 2014. Vol. 2014, no. 2014, pp.1-11.
https://search.emarefa.net/detail/BIM-478750
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-478750