NDLI: Novel naphthalimide polyamine derivatives as potential antitumor agents

Content Provider	Springer Nature Link
Author	Seliga, Robert Pilatova, Martina Sarissky, Marek Viglasky, Viktor Walko, Martin Mojzis, Jan
Copyright Year	2013
Abstract	A novel series of naphthalimide polyamine conjugates were designed, synthesized and evaluated for in vitro antiproliferative activity against human leukemia (Jurkat), human cervical adenocarcinoma (HeLa), human breast adenocarcinoma (MCF-7) and human lung adenocarcinoma (A549) cell lines. From the six derivatives, the new I1 and A3 exhibited highest antiproliferative activity with the IC$_{50}$ values of 5.67–11.02 μmol·L$^{−1}$. Cell cycle analysis of Jurkat cells exposed to I1 at a concentration of 30 μmol × L$^{−1}$ for 24 h exhibited a mild increase in S and G$_{2}$/M fraction caused by accumulation of cells. This arrest was followed by an increase in sub-G$_{0}$/G$_{1}$ after 48 h of incubation. Jurkat cells exposed to A3 at a concentration of 30 μmol × L$^{−1}$ for 24 h showed an increase in G$_{0}$/G$_{1}$ fraction and after 48 h an increase in G$_{2}$/M fraction followed by an increase in sub-G$_{0}$/G$_{1}$ after 72 h of incubation. Moreover, the A3 compound was observed to displace the intercalating agent ethidium bromide from calf thymus DNA using fluorescence spectroscopy. The apparent binding constant was estimated to be 3.1 × 10$^{6}$ M$^{−1}$ what indicates non-intercalating mode of DNA binding. On the other hand, we found no inhibitory effect of studied compounds on topoisomerase I and topoisomerase II activity. Finally, the localization of these compounds in the cells due to their inherent fluorescence was investigated with the fluorescence microscopy. Our results suggest that the naphthalimide polyamine conjugates rapidly penetrate to the cancer cells. Further studies are necessary to investigate the precise mechanism of action and to find out the relationship between the structure, character and position of substituents of naphthalimide polyamine conjugates and their biological activities.
Starting Page	4129
Ending Page	4137
Page Count	9
File Format	PDF
ISSN	03014851
Journal	Molecular Biology Reports
Volume Number	40
Issue Number	6
e-ISSN	15734978
Language	English
Publisher	Springer Netherlands
Publisher Date	2013-05-03
Publisher Place	Dordrecht
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Naphthalimides Polyamine derivatives Antiproliferative activity DNA-binding Synthesis Animal Anatomy / Morphology / Histology Animal Biochemistry
Content Type	Text
Resource Type	Article
Subject	Genetics Medicine Molecular Biology

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1	Ministry of Education (GoI), Department of Higher Education	Sanctioning Authority	https://www.education.gov.in/ict-initiatives
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3	National Digital Library of India Office, Indian Institute of Technology Kharagpur	The administrative and infrastructural headquarters of the project	Dr. B. Sutradhar bsutra@ndl.gov.in
4	Project PI / Joint PI	Principal Investigator and Joint Principal Investigators of the project	Dr. B. Sutradhar bsutra@ndl.gov.in Prof. Saswat Chakrabarti will be added soon
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