Table 3.
Effect of coumarins on GTPase and polymerization activity of MtbFtsZ.
Compound | polymerization activity* IC50 ± SD (μM) | GTPaseactivity** IC50 ± SD (μM) | ||||
---|---|---|---|---|---|---|
Wild type | G103S | G103A | Wild type | G103S | G103A | |
Esculetin | 84.6 ± 4.7 | 48.5 ± 2.5 | 74 ± 5.3 | 65 ± 4.6 | 55.5 ± 2.4 | 69.8 ± 1.7 |
Umbelliferone | 124.2 ± 7.5 | 52.8 ± 3.8 | 85 ± 4.72.7 | 135.2 ± 5.9 | 52.8 ± 3.5 | 85 ± 2.3 |
4-Methylumbelliferone | 99.2 ± 3.2 | 102.4 ± 2.7 | 112.6 ± 3.4 | 125.1 ± 4.9 | 102.4 ± 6.7 | 112.6 ± 3.9 |
4-Hydroxycoumarin | >200 | >200 | 150 ± 6.4 | 198 ± 3.5 | >200 | 178.7 |
Coumarin | >200 | 73 ± 6.6 | 89 ± 5.4 | >200 | 69.5 ± 5.7 | 88.3 ± 2.9 |
7-Diethylamino-4-methyl coumarin | 81.54 ± 6.4 | 65.2 ± 1.8 | 72.5 ± 3.9 | 110.3 ± 0.3 | 78.47 ± 1.8 | 57.97 ± 3.5 |
6-Methylcoumarin | >200 | 124.7 ± 6.7 | 148.4 ± 3.6 | >200 | 136.1 ± 2.9 | 178.4 ± 2.1 |
Daphnetin | 89.5 ± 6.3 | 55.2 ± 5.4 | 78.7 ± 6.1 | 62.5 ± 5.8 | 89.5 ± 5.2 | 94.7 ± 2.9 |
7-Dimethyl-4-methyl coumarin | 74.1 ± 2.8 | 64.1 ± 2.9 | 60.9 ± 4.8 | 64.47 ± 6.7 | 45.7 ± 1.8 | 44.2 ± 5.4 |
The IC50 values were calculated for the polymerization activity and GTPase activity by light scattering assay* and Malachite green assay** respectively as indicated in experimental section. Data here is represented as mean ± SD of three independent experiments.