9‐Hydroxybenfluron induced inhibition of proliferation and metabolism in hela cells

Abstract

The highest concentration of 9-hydroxybenfluron (HBF) tested, namely 4.05 mumol l-1, induced immediate cytotoxic effects which were manifested by total inhibition of cell proliferation after only 24 h of culture. In a certain proportion of the cells cytolytic effects were observed at longer times of culture. Lower concentrations of HBF induced toxicity that was concentration- and time-dependent. The toxic effect appeared to occur in two phases. Cells, which had lost their ability to divide, did not stop their metabolism in which glutamine was the main source of energy. The results suggest that HBF primarily interferes with one of the phases of the cell cycle and only secondarily influences energy processes. Because benfluron (BF) and HBF have similar effects, it is suggested that the cytotoxicity of BF can be ascribed to the influence of its metabolite, HBF.

The Influence of Dimethoxybenfluron on Biochemical and Haematological Parameters in Rabbits

“…An interesting, marked increase in the values of glucose, especially following the lower dose of dimethoxybenfluron, was found at the end of experiment. It is not possible to exclude that this increase may be related to the previously described influence of NO-1-B on the energy processes of HeL cells (7). Furthermore, the values of the other biochemical parameters mostly did not change and were not significantly different in comparison with the values in the control group (except a decrease in the values of bilirubin and ALP).…”

Use of chiral liquid chromatography for the evaluation of stereospecificity in the carbonyl reduction of potential benzo[c]fluorene antineoplastics benfluron and dimefluron in various species

“…Higher antineoplastic efficiency of D (in comparison with B) could be expected in vivo [25][26][27] and the respective studies have been done or are currently in progress.…”

Disposition study of a new potential antineoplastic agent dimefluron in rats using high-performance liquid chromatography with ultraviolet and mass spectrometric detection

“…The starting structure from the group of basic benzo[c]fluorene derivatives, benfluron (5-(2-dimethylaminoethoxy)-7H-benzo[c]fluoren-7-one hydrochloride [2][3][4]), exhibited an interesting spectrum of pharmacodynamic properties in experiments carried out in vitro and in vivo [5][6][7][8]. The disposition of benfluron in experimental animals was studied by TLC [9][10][11][12], HPLC [13][14][15], MS [16] and NMR [17] methods using a comparison of the metabolites with their synthesized standards [18,19].…”