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The Cytotoxicity of Benzaldehyde Nitrogen Mustard-2-Pyridine Carboxylic Acid Hydrazone Being Involved in Topoisomerase IIα Inhibition
المؤلفون المشاركون
Liu, Youxun
Fu, Yun
Li, Changzheng
Yang, Yingli
Sun, Xingzhi
Zhou, Sufeng
المصدر
العدد
المجلد 2014، العدد 2014 (31 ديسمبر/كانون الأول 2014)، ص ص. 1-11، 11ص.
الناشر
Hindawi Publishing Corporation
تاريخ النشر
2014-06-05
دولة النشر
مصر
عدد الصفحات
11
التخصصات الرئيسية
الملخص 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.
نمط استشهاد جمعية علماء النفس الأمريكية (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
نمط استشهاد الجمعية الأمريكية للغات الحديثة (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
نمط استشهاد الجمعية الطبية الأمريكية (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
نوع البيانات
مقالات
لغة النص
الإنجليزية
الملاحظات
Includes bibliographical references
رقم السجل
BIM-478750
قاعدة معامل التأثير والاستشهادات المرجعية العربي "ارسيف Arcif"
أضخم قاعدة بيانات عربية للاستشهادات المرجعية للمجلات العلمية المحكمة الصادرة في العالم العربي
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