Table 1.
Inhibition of insect trehalases from silkworm (B. mori) and tobacco cutworm (S. litura), fungi trehalase from R. solani, porcine kidney and porcine intestine trehalases by compounds 2, 3, 4, 5 and 8.
| Compound | Silkworm (B. mori), IC50 (Ki) | Tobacco Cutworm (S. litura), IC50 (Ki) | R. solani, IC50 (Ki) | Porcine Kidney, IC50 (Ki) | Porcine Intestine, IC50 (Ki) |
|---|---|---|---|---|---|
| 2 | n.d. | 370 nM [19] | 72 µM [18] | 250 µM [21] | 420 nM [19] |
| 3 a | n.d. | 48 nM [19] (43 nM) [20] |
140 nM (1.9 nM) [18] |
2.4 nM [21] | 14 nM [19] |
| 4 | 8.3 µM [31] | n.d. | n.d. | (0.18 µM) [30] | n.d. |
| 5 b,c | 49 nM [36] 52 nM [35] (10 nM) [35] |
n.d. | 66 nM [42] | 15.5 nM [39] d (2.1 nM) [39] |
n.d. |
| 8 a | n.d. | n.d. | n.d. | 83.0 nM [39] (30.4 nM) [39] |
n.d. |
a Compounds 3 and 8 are potent inhibitors of Tre37A enzyme from E. coli with Ki values of 10 nM and 9 nM, respectively [40]; b IC50 values of 5.5 nM and 3.7 nM were also reported towards silkworm and porcine trehalase, respectively [32]; c 5 also inhibits locust flight muscle trehalase with Ki = 10 nM (in extracts) and Ki = 8 nM (on purified enzyme) [13]; d IC50 = 16 nM [35] and IC50 = 19 nM [21] were also reported for natural 5; n.d.: not determined.