Archer, Jennifer J.

Grant, Kathryn B.

Joung, Sunhwa

Nguyen, Khoa T.

Phanstiel, Otto, IV

English

ScholarWorks @ Georgia State University

  Evaluation of Polyamine-Anthracene Conjugates as DNA Ligands: a Potential Anti-Cancer Agent By: Nguyen, Khoa The; Joung, Sunhwa; Archer, Jennifer J.; Phanstiel, Otto, IV; Grant, Kathryn B.  The uptake of polyamine-anthracene conjugates into cells is facilitated by the polyamine transport system (PTS). As a result, polyamine-anthracene conjugates have been utilized to selectively target cancer cells that display high PTS activity. While cellular uptake is an essential first step, the cytotoxic effects of the polyamine-anthracenes are likely to involve interactions with macromolecules inside of the cell. The planar aromatic ring system of anthracene coupled with the high positive charge of the polyamine component makes the conjugates potentially excellent DNA ligands. To test this hypothesis, we have examined the DNA interactions of five polyamine conjugates that share a common anthracene core. Data from UV-visible absorption experiments, thermal melting analyses, and gel shift assays suggest that charged polyamine amino groups contribute to binding. The anthracenes with two polyamine chains were accordingly found to display the highest DNA affinity. Possible correlations to PTS activity and cytotoxicity will be discussed.    

Evaluation of Polyamine-Anthracene Conjugates as DNA Ligands: a Potential Anti-Cancer Agent

Georgia State University

  
Evaluation of Polyamine-Anthracene Conjugates as DNA Ligands: a 
Potential Anti-Cancer Agent 
By: Nguyen, Khoa The; Joung, Sunhwa; Archer, Jennifer J.; Phanstiel, Otto, 
IV; Grant, Kathryn B.  
The uptake of polyamine-anthracene conjugates into cells is facilitated by the polyamine 
transport system (PTS). As a result, polyamine-anthracene conjugates have been 
utilized to selectively target cancer cells that display high PTS activity. While cellular 
uptake is an essential first step, the cytotoxic effects of the polyamine-anthracenes are 
likely to involve interactions with macromolecules inside of the cell. The planar aromatic 
ring system of anthracene coupled with the high positive charge of the polyamine 
component makes the conjugates potentially excellent DNA ligands. To test this 
hypothesis, we have examined the DNA interactions of five polyamine conjugates that 
share a common anthracene core. Data from UV-visible absorption experiments, thermal 
melting analyses, and gel shift assays suggest that charged polyamine amino groups 
contribute to binding. The anthracenes with two polyamine chains were accordingly 
found to display the highest DNA affinity. Possible correlations to PTS activity and 
cytotoxicity will be discussed. 
 
 
 


https://scholarworks.gsu.edu/cgi/viewcontent.cgi?article=1331&amp;context=gsurc

Evaluation of Polyamine-Anthracene Conjugates as DNA Ligands: a Potential Anti-Cancer Agent

Abstract

Similar works

Full text

Available Versions

ScholarWorks @ Georgia State University

Georgia State University