Table 3. Antischistosomal Activity of Gallinamides against Ex VivoS. mansoni Adults.
| severity
scoresa |
||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| time (h) | 2 |
6 |
24 |
48 |
||||||||||||
| compound (μM) | 1 | 2 | 5 | 10 | 1 | 2 | 5 | 10 | 1 | 2 | 5 | 10 | 1 | 2 | 5 | 10 |
| gallinamide A | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 2 | 2 | 3 |
| 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 4 | 0 | 2 | 2 | 4 |
| 6 | 0 | 0 | 1 | 2 | 0 | 0 | 1 | 2 | 0 | 0 | 2 | 4 | 0 | 1 | 4 | 4 |
| 9 | 0 | 0 | 1 | 1 | 0 | 0 | 1 | 2 | 0 | 0 | 2 | 4 | 0 | 2 | 4 | 4 |
Phenotypic changes in adult S. mansoni induced by compounds at given concentrations were observed and converted to severity scores on a scale of 0 (no effect) to 4 (severe effects) as described previously.39,42,43 Data are shown as a heat map. The full phenotypic details are presented in Table S3. Compounds were tested in duplicate in two independent assays, and representative data are shown.