Table 3.
Minimal inhibitory concentration (MIC) values, and inhibition obtained at the maximal solubility in 3.5% DMSO of the compounds tested in this study, against H. pylori 26695 strain cell cultures.
Inhibitor | MW | MICa |
Maximal solubility |
% of H. pylori cell culture inhibition at inhibitor maximal solubility | ||
---|---|---|---|---|---|---|
[µg mL−1] | [µM] | [µg mL−1] | [µM] | |||
DMSO | 78.13 | – | – | 55.0b | – | 60e |
38.5b | – | 26e | ||||
27.5b | – | 0e | ||||
2,6-diCl-Pu | 189.00 | 473 | 2500 | 236 | 1250 | 93 |
6BnO-2Cl-Pu | 260.68 | – | – | 25c | 95c | 35 |
91d | 350d | 75 | ||||
6BnS-2Cl-Pu | 276.74 | 69d | 250d | 11.1 | 40 | 92 |
6BnS-Pu | 242.3 | 48d | 200d | 21 | 85 | 83 |
6BnS-2Cl-Pu-9dr | 393.87 | 79d | 200d | 4.3c | 10.8c | 5 |
metronidazole | 171.15 | 8f | 47 | 2g | 12g | 89–92 |
kanamycin | 484.5 | 0.5–64f | 1.1–132 | 25g | 52g | 92–96 |
BHI medium untreated with H. pylori | – | – | – | – | – | 95h |
The results are presented as the mean of three repetitions (see Materials and methods).
aMIC is the minimal concentration used in the series of 2-fold dilutions that gave full inhibition of H. pylori cell culture growth, i.e. comparable to that observed for the positive control with 25 µg/mL kanamycin, i.e. by 92–96%.
bThese correspond to 5%, 3.5%, and 2.5% (v/v), respectively, and in this case, this is not the maximal solubility; DMSO density 1.1 g/cm³.
cIt was a maximal concentration possible to obtain in given conditions (at this concentration saturation was observed, see Table S1).
dInhibitor partially precipitated, so actual concentration of dissolved compound is lower.
eIn each experiment, the inhibition by DMSO was always checked to see its effect in this particular case, and compared with the effect of the HpPNP inhibitor tested. It was necessary as inhibition observed for the particular % of DMSO differs slightly among the experiments.
gIn this case this concentration is not the maximal solubility.
hIn this case there is no H. pylori, so the value shown is treated as a negative control.