TABLE 1.
Antimicrosporidial activity of drugs in vitro
| Test compound | Mol wt | Highest nontoxic dosea (μM) | % Inhibition (mean ± SD)b
|
Approximate IC50c (μM)
|
||
|---|---|---|---|---|---|---|
| E. intestinalis | V. corneae | E. intestinalis | V. corneae | |||
| Fumagillin | 458.60 | 4 | 72.1 ± 2.8 | 72.8 ± 3.1 | 0.0025 | 0.002 |
| TNP-470 | 401.88 | 50 | 92.1 ± 1.6 | 90.4 ± 4.3 | 0.0035 | 0.002 |
| Ovalicin | 296.36 | 10 | 73.0 ± 14.9 | 78.9 ± 8.5 | 0.004 | 0.002 |
| 9168d | 458.54 | >100e | 71.7 ± 13.0 | 78.2 ± 19.1 | 0.02 | 0.42 |
| 9665d | 282.38 | >100e | 74.3 ± 30.1 | 93.4 ± 28.6 | 0.001 | 0.066 |
| 56407d | 192.17 | >100e | 70.6 ± 12.3 | 54.9 ± 5.0 | 8.90 | 57.00 |
| 58368d | 639.86 | 10 | 58.7 ± 10.5 | 75.5 ± 10.7 | 6.25 | 0.20 |
| 141538d | 296.36 | 10 | 58.0 ± 9.9 | 54.1 ± 8.9 | 0.75 | 8.20 |
| 141539d | 298.38 | 10 | 83.3 ± 8.9 | 66.8 ± 17.7 | 0.07 | 0.08 |
| 676019d | 431.00 | 10 | 29.5 ± 6.1 | 28.0 ± 14.0 | 50.4 | 97.0 |
| 174554d | 241.28 | >100e | 80.8 ± 11.6 | 91.2 ± 3.3 | 47.1 | 52.9 |
a
Concentrations of compounds that caused the viability of host cells (RK-13 cells) to fall below 85% of medium-treated host cells were considered to be toxic.
b
Inhibition values were presented for the highest nontoxic dose of compound.
c
IC50 values were estimated by interpolation using Graphpad Prism software.
d
The numbers for these compounds refer to National Cancer Institute database NSC entry numbers, and additional information can be accessed at the website http://dtp.nci.nih.gov/dtpstandard/ChemData/index.jsp.
e
The highest concentration tested for each compound was 100 μM, and these compounds were not toxic at this dose.