Table 1.
a Minimum inhibitory concentrations (MICs) of 2 - 6 in M. tuberculosis H37Rv and cytotoxicity evaluation in HepG2 cells in presence of glucose (Glu) and galactose (Gal). Activity of compounds 2 - 6 against intracellular M. tuberculosis H37Rv.
| Minimum inhibitory concentrations (μM) | Intracellular assay (μM) | |||||
|---|---|---|---|---|---|---|
| Compound | H37Rv MIC90[b] | HepG2 (Glu) IC50[c] | HepG2 (Gal) IC50[c] | Ratio (Glu/Gal) | RAW 264.7 IC50[d] | Intracellular Mtb IC90[e] |
| 2 | >20 (0) | 79 (0.6) | 34 (1.1) | 2.3 | 39 (4.6) | >33 (4.8) |
| 3 | >20 (0) | >100 (0) | >100 (0) | N/A | >100 (0) | >100 (0) |
| 4 | >20 (0) | 69 (1.2) | 41 (0.7) | 1.7 | 8 (1.1) | >3.7 (0) |
| 5 | 13 (2.5) | 36 (0) | 29 (0.5) | 1.2 | 29 (0.5) | 9.3 (0.8) |
| 6 | >20 (0) | >100 (0) | 22 (1.9) | >4.5 | 2.6 (0.6) | >3.7 (1.1) |
| Rifampicin | 0.1 (0.6) | >100 (0) | NA | NA | NA | NA |
The experiments were conducted in triplicate and error values are reported in brackets as Standard Deviation (STDEV) values.
MIC90 was defined as the concentration required to inhibit growth of M. tuberculosis in liquid medium by 90% after 5 days.
IC50 is the concentration required to reduce viability of HepG2 cells (cultured with either glucose or galactose) by 50% after 2 days.
IC50 is the concentration required to reduce viability of RAW 264.7 cells by 50% after 3 days.
IC90 is the concentration required to inhibit the growth of M. tuberculosis in liquid medium by 90% after 3 days. NA = not available.