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Table 2 Cytotoxic and antiproliferative activities of genistein synthetic derivatives and their effects on kinetics of GAG synthesis in fibroblasts

From: Synthetic genistein derivatives as modulators of glycosaminoglycan storage

Compound Cytotoxicity LC50[μM] Proliferation IC50[μM] GAG synthesis [%]
IFG-001 13.9 - 120 ± 56
IFG-018 41.7 - 76 ± 38
IFG-021 11.0 - 75 ± 25
IFG-027 13.1 - 69 ± 46
IFG-032 n/c 17.4 57 ± 24
IFG-034 n/c 22.9 65 ± 19
IFG-035 22.6 - 93 ± 70
IFG-036 n/c 11.2 64 ± 21
IFG-037 23.5 - 88 ± 84
IFG-038 n/c 19.9 55 ± 13
IFG-042 22.0 - 48 ± 29
IFG-043 14.5 - 46 ± 41
IFG-046 20.7 - 118 ± 72
IFG-048 20.3 - 73 ± 5
IFG-050 11.6 - 100 ± 65
IFG-051 14.6 - 127 ± 109
IFG-052 15.8 - 74 ± 19
IFG-053 n/c 53.0 92 ± 52
IFG-054 n/c n/a 119 ± 64
IFG-060 14.9 - 31 ± 8
IFG-061 18.8 - 50 ± 25
IFG-062 12.1 - 403 ± 206
IFG-063 51.5 - 76 ± 6
IFG-064 6.6 - 133 ± 77
IFG-065 22.7 - 96 ± 22
IFG-066 n/c 14.6 34 ± 10
IFG-067 15.1 - 96 ± 38
IFG-070 n/c 48.1 101 ± 30
IFG-071 n/c 17.9 49 ± 20
IFG-072 n/c 14.1 79 ± 42
IFG-073 27.5 - 83 ± 32
IFG-074 44.1 - 88 ± 39
Genistein n/c 16.9 55 ± 31
  1. Cytotoxicity is expressed as LC50 index value, i.e. concentration of the tested drug [μM] that is lethal to 50% of cells in a culture exposed to the tested compound for 24 hours. Antiproliferative activity is expressed as IC50 index value, i.e. concentration of the tested drug [μM] that causes 50% inhibition of cell proliferation in a culture exposed to the tested compound for 7 days. Kinetics of GAG synthesis is expressed as relative 35 S incorporation into GAGs after 3-day exposure to derivatives of genistein at 30 μM concentration. Labeling was conducted for 24 hours with 20 μCi/ml H2[35 S]O4. Radioactivity of incorporated 35 S was measured in a scintillation counter, calculated per DNA amount [dpm/ng DNA] and expressed as the percentage of control, where 100% corresponds to the relative 35 S incorporation into control (cell culture treated with 0.05% dimethylformamide).
  2. n/c denotes experiments in which no cytotoxicity was observed (over 90% of cells survived at concentrations ranging from 1 to 30 μM).
  3. n/a denotes experiments in which no antiproliferative activity was observed (relative proliferation was over 95% at concentrations ranging from 1 to 30 μM).
  4. - denotes experiments in which IC50 for antiproliferative activities could not be determined due to cytotoxic effects of the tested compounds.