Table 3.
Inhibitory Effects of Circumdatins toward NF-κB Activation and AChE Activity.
| Compounds | NF-κB Activation | AChE Activity | AChE Affinity |
|---|---|---|---|
| IC50 (μM)a | IC50 (μM)b | Kd(M)c | |
| circumdatin C | 15.6 ± 2.3 | 13.9 ± 0. 7 | 8.5 × 10−5 |
| circumdatin D | 8.7 ± 1.3 | 2.4 ± 0.5 | 1.9 × 10−6 |
| circumdatin F | 11.8 ± 0.9 | 10.0 ± 1.9 | 2.4 × 10−4 |
| circumdatin G | 18.9 ± 2.1 | 15.8 ± 2.0 | 1.2 × 10−4 |
| circumdatin H | 33.3 ± 1.4 | 98.0 ± 5.7 | 9.5 × 10−5 |
| circumdatin I | 18.6 ± 1.9 | 11.6 ± 2.6 | 6.5 × 10−5 |
| 2-hydroxycircumdatin C | 16.5 ± 1.9 | 5.6 ± 0.9 | 3.6 × 10−6 |
| galanthamine | 0.1 ± 0.2 | 4.9 × 10−7 |
a
SW480 cells are stably transfected with NF-κB luciferase reporter gene. IC50 values of circumdatins against NF-κB activation in SW480 cells induced by LPS. Values were expressed as mean ± SD (n = 3). The reported values are the mean of at least three independent measurements.
b
IC50 values of circumdatins against AChE enzyme activity tested using modified Ellman's colorimetric method. Values were expressed as mean ± SD (n = 3). The reported values are the mean of at least three independent measurements.
c
Equilibrium dissociation constants (Kd) values were determined by SPR analysis on AChE-circumdatins complexes.