In Vitro Ability of Currently Available Oximes to Reactivate Organophosphate Pesticide-Inhibited Human Acetylcholinesterase and Butyrylcholinesterase
Abstract
:1. Introduction
2. Results and Discussion
3. Experimental Section
4. Conclusions
Acknowledgments
References
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AChE | Paraoxon [17] | Dichlorvos | DFP [18] | Leptophos-oxon [19] | Methamidophos | |||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
100 μM | 10 μM | 100 μM | 10 μM | 100 μM | 10 μM | 100 μM | 10 μM | 100 μM | 10 μM | |||||||||||
Mean | SD | Mean | SD | Mean | SD | Mean | SD | Mean | SD | Mean | SD | Mean | SD | Mean | SD | Mean | SD | Mean | SD | |
Methoxime | 23.4 | 4.5 | 4.3 | 1.5 | 0 | 0 | 0.2 | 0.6 | 6.4 | 0.5 | 1.5 | 0.5 | 52.6 | 0.5 | 11.9 | 0.9 | 61.7 | 2.4 | 68.1 | 11.4 |
Pralidoxime | 18.1 | 0.9 | 1.3 | 0.9 | 2.6 | 0.6 | 0.2 | 0.6 | 2.3 | 0.2 | 0 | 0 | 13.2 | 0.9 | 4.1 | 1.3 | 53.4 | 3.1 | 53.8 | 22.6 |
Obidoxime | 96.8 | 0.9 | 59.4 | 0.9 | 0 | 0 | 0.6 | 0.1 | 17.1 | 0.1 | 7.4 | 0.5 | 50.3 | 0.9 | 31.4 | 0.2 | 5.8 | 4.8 | 57.0 | 18.7 |
Trimedoxime | 86.0 | 1.6 | 45.3 | 0.8 | 0 | 0 | 0 | 0 | 23.8 | 0.2 | 6.4 | 0.2 | 51.3 | 0.5 | 26.4 | 2.7 | 9.4 | 7.5 | 53.1 | 10.9 |
HI-6 | 16.1 | 0.2 | 3.9 | 0.9 | 0 | 0 | 0.6 | 1.1 | 0 | 0 | 0 | 0 | 32.8 | 8.0 | 11.6 | 0.4 | 37.4 | 12.3 | 75.2 | 14.6 |
BChE | Paraoxon [17] | Dichlorvos | DFP [18] | Leptophos-oxon [19] | Methamidophos | |||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
100 μM | 10 μM | 100 μM | 10 μM | 100 μM | 10 μM | 100 μM | 10 μM | 100 μM | 10 μM | |||||||||||
Mean | SD | Mean | SD | Mean | SD | Mean | SD | Mean | SD | Mean | SD | Mean | SD | Mean | SD | Mean | SD | Mean | SD | |
Methoxime | 6.1 | 0.6 | 0.9 | 0.8 | 0.2 | 0.1 | 0.2 | 0.1 | 8.2 | 1.3 | 0.8 | 0.5 | 6.4 | 0.4 | 1.9 | 1.8 | 4.8 | 0.2 | 1.0 | 0.2 |
Pralidoxime | 5.5 | 0.1 | 1.0 | 0.3 | 1.0 | 0.1 | 0.4 | 0.2 | 6.4 | 0.8 | 0.7 | 0.1 | 2.3 | 1.8 | 0 | 0 | 3.5 | 0.3 | 0 | 0 |
Obidoxime | 9.9 | 0.4 | 2.2 | 0.4 | 3.1 | 0.2 | 1.6 | 0.4 | 9.5 | 1.0 | 1.5 | 0.6 | 14.3 | 0.6 | 6.5 | 4.2 | 4.2 | 0.3 | 1.0 | 0.2 |
Trimedoxime | 12.1 | 1.7 | 1.3 | 0.3 | 1.2 | 0.1 | 0.4 | 0.2 | 7.3 | 0.5 | 0.8 | 0.5 | 8.5 | 2.4 | 2.1 | 0.4 | 5.2 | 0.7 | 0.6 | 0.8 |
HI-6 | 2.3 | 0.3 | 0.8 | 0.5 | 0.6 | 0.1 | 0.4 | 0.1 | 3.8 | 0.1 | 0.7 | 0.2 | 5.6 | 4.9 | 0 | 0 | 4.8 | 0.2 | 0.1 | 0.2 |
Inhibitor | AChE | BChE | ||
---|---|---|---|---|
IC95 (M) | 7 × T1/2 (min) | IC95 (M) | 7 × T1/2 (min) | |
Paraoxon | 3.38 × 10−6 | 2.17 | 1.41 × 10−7 | 1.82 |
Dichlorvos | 3.30 × 10−4 | 0.32 | 2.08 × 10−6 | 2.20 |
DFP | 5.00 × 10−6 | 0.93 | 8.30 × 10−8 | 1.75 |
Leptophos−oxon | 4.16 × 10−7 | 2.45 | 7.06 × 10−6 | 0.75 |
Methamidophos | 4.26 × 10−5 | 2.22 | 2.08 × 10−4 | 2.83 |
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Jun, D.; Musilova, L.; Musilek, K.; Kuca, K. In Vitro Ability of Currently Available Oximes to Reactivate Organophosphate Pesticide-Inhibited Human Acetylcholinesterase and Butyrylcholinesterase. Int. J. Mol. Sci. 2011, 12, 2077-2087. https://doi.org/10.3390/ijms12032077
Jun D, Musilova L, Musilek K, Kuca K. In Vitro Ability of Currently Available Oximes to Reactivate Organophosphate Pesticide-Inhibited Human Acetylcholinesterase and Butyrylcholinesterase. International Journal of Molecular Sciences. 2011; 12(3):2077-2087. https://doi.org/10.3390/ijms12032077
Chicago/Turabian StyleJun, Daniel, Lucie Musilova, Kamil Musilek, and Kamil Kuca. 2011. "In Vitro Ability of Currently Available Oximes to Reactivate Organophosphate Pesticide-Inhibited Human Acetylcholinesterase and Butyrylcholinesterase" International Journal of Molecular Sciences 12, no. 3: 2077-2087. https://doi.org/10.3390/ijms12032077