- Title
-
Aaptamine - a dual acetyl - and butyrylcholinesterase inhibitor as potential anti-Alzheimer's disease agent
- Authors
- Miao, S., He, Q., Li, C., Wu, Y., Liu, M., Chen, Y., Qi, S., Gong, K.
- Source
- Full text @ Pharm Biol
Figure 2. Dose-response and IC50 values of aaptamine and donepezil against AChE and BuChE. |
Figure 3. (A) The binding model between aaptamine and AChE. (B) Binding model between aaptamine and BuChE. Orange dashed line: π–π conjugate effect; Yellow dashed line: hydrogen bond. Yellow sticks structure: compound aaptamine; Green sticks structure: protein AChE; Magenta sticks structure: protein BuChE. |
Figure 4. (A) Lineweaver–Burk plot for the inhibition of AChE by aaptamine at different concentrations for substrate ATChI. (B) Secondary plot for calculation of the steady-state inhibition constant (Ki = 1.74 ± 0.04 μM against AChE) of aaptamine. (C) Lineweaver–Burk plot for the inhibition of BuChE by aaptamine at different concentrations for substrate BTChI. (D) Secondary plot for calculation of the steady-state inhibition constant (Ki = 1.59 ± 0.02 μM against BuChE) of aaptamine. |
Figure 5. (A) Biacore analysis of aaptamine binding to AChE. (B) Steady state of affinity fitting of aaptamine – AChE interaction. (C) Biacore analysis of aaptamine binding to BuChE. (D) Steady state of affinity fitting of aaptamine – BuChE interaction. |
Figure 6. (A,B) The effect of aaptamine on motility distance of AD zebrafish ###p < 0.001 vs. Control group, **p < 0.01 vs. AlCl3 group. (C,D) Effect of aaptamine on speed change in AD zebrafish. ###p < 0.001 vs. Control group, **p < 0.01 vs. AlCl3 group. PHENOTYPE:
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