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

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. © 2013 Pleiades Publishing, Ltd.