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

Autor:	S. S. Shishkin, K. V. Lisitskaya, Alexander V. Ivanov, Yu. G. Malysheva, S. P. Syatkin, N. A. Sokueva
Rok vydání:	2013
Předmět:	chemistry.chemical_compound Biochemistry Molecular mass chemistry LNCaP Cytotoxic T cell Functional activity Human cell Biology Polyamine Applied Microbiology and Biotechnology
Zdroj:	Applied Biochemistry and Microbiology. 49:100-105
ISSN:	1608-3024 0003-6838
DOI:	10.1134/s0003683813020075
Popis:	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.
Databáze:	OpenAIRE
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