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Identification of the functional activity of synthetic polyamine analogues using a biotest system based on highly proliferating cultured human cells

Identification of the functional activity of synthetic polyamine analogues using a biotest system... A new biotest system was developed based on highly proliferating human cell cultures (lines LNCaP and PC-3). With the help of this system, two known synthetic polyamines—α-difluoromethylornithine (DFMO) and methylglioxalbis(guanylhydrason) (MGBG)—as well as four new synthetic analogues difenylcontaining amines (DFCA-1-DFCA-4) with molecular weights of 725.5 (DFCA-1), 755.5 (DFCA-2), 655.5 (DFCA-3), and 681.5 Da (DFCA-4) were tested. In this biotest system, DFMO (0.1–400 μM) did not reveal functional activity, whereas for MGBG a cytotoxic effect was registered (100–200 μM). DFCA-1, DFCA-2, and DFCA-4 had a similar effect at concentrations of 10 μM and higher; DFCA-3, at a concentration of 50 μM and higher. Thus, DFCA-1 has a higher level of antiproliferating activity and may be considered as the most potent cytostatic agent. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Applied Biochemistry and Microbiology Springer Journals

Identification of the functional activity of synthetic polyamine analogues using a biotest system based on highly proliferating cultured human cells

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Publisher
Springer Journals
Copyright
Copyright © 2013 by Pleiades Publishing, Ltd.
Subject
Life Sciences; Biochemistry, general; Microbiology; Medical Microbiology
ISSN
0003-6838
eISSN
1608-3024
DOI
10.1134/S0003683813020075
Publisher site
See Article on Publisher Site

Abstract

A new biotest system was developed based on highly proliferating human cell cultures (lines LNCaP and PC-3). With the help of this system, two known synthetic polyamines—α-difluoromethylornithine (DFMO) and methylglioxalbis(guanylhydrason) (MGBG)—as well as four new synthetic analogues difenylcontaining amines (DFCA-1-DFCA-4) with molecular weights of 725.5 (DFCA-1), 755.5 (DFCA-2), 655.5 (DFCA-3), and 681.5 Da (DFCA-4) were tested. In this biotest system, DFMO (0.1–400 μM) did not reveal functional activity, whereas for MGBG a cytotoxic effect was registered (100–200 μM). DFCA-1, DFCA-2, and DFCA-4 had a similar effect at concentrations of 10 μM and higher; DFCA-3, at a concentration of 50 μM and higher. Thus, DFCA-1 has a higher level of antiproliferating activity and may be considered as the most potent cytostatic agent.

Journal

Applied Biochemistry and Microbiology – Springer Journals

Published: Feb 26, 2013

References