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In vitro effects of acetylcholinesterase inhibitors and reactivators on Complex I of electron transport chain
J. Hroudová, Z. Fisar, J. Korábečný, K. Kuča,
Jazyk angličtina Země Švédsko
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
21712782
Knihovny.cz E-zdroje
- MeSH
- cholinesterasové inhibitory farmakologie MeSH
- elektronový transportní řetězec antagonisté a inhibitory účinky léků MeSH
- energetický metabolismus účinky léků MeSH
- mitochondrie účinky léků metabolismus MeSH
- mozek - chemie účinky léků MeSH
- oximy farmakologie MeSH
- prasata MeSH
- reaktivátory cholinesterasy farmakologie MeSH
- respirační komplex I metabolismus MeSH
- takrin analogy a deriváty farmakologie MeSH
- techniky in vitro MeSH
- transport elektronů účinky léků MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
OBJECTIVES: Inhibition of the enzyme acetylcholinesterase (AChE) is the main mechanism both of therapeutic action of drugs for the treatment of Alzheimer's disease and toxic action of organophosphorus compounds. Various types of oximes reactivate AChE and are commonly used as antidotes against organophosphates (pesticides, nerve agents). METHODS: Effects both of AChE inhibitors (tacrine, 7-methoxytacrine) and oximes (pralidoxime, trimedoxime, obidoxime, methoxime, HI-6) on Complex I of electron transport chain (ETC) were examined. The enzyme activity was measured spectrophotometrically in crude mitochondrial fraction isolated from pig brain. RESULTS: Our results showed statistically significant Complex I inhibition by tacrine, other drugs did not affect the enzyme activity significantly. CONCLUSIONS: These observations suggest the possibility of tacrine-induced side effects related to disturbance in ETC. On the contrary, it seems that oximes do not affect cellular energetic metabolism.
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- $a Hroudová, Jana $u Department of Psychiatry, 1st Faculty of Medicine, Charles University in Prague and General University Hospital in Prague, Prague, Czech Republic.
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- $a OBJECTIVES: Inhibition of the enzyme acetylcholinesterase (AChE) is the main mechanism both of therapeutic action of drugs for the treatment of Alzheimer's disease and toxic action of organophosphorus compounds. Various types of oximes reactivate AChE and are commonly used as antidotes against organophosphates (pesticides, nerve agents). METHODS: Effects both of AChE inhibitors (tacrine, 7-methoxytacrine) and oximes (pralidoxime, trimedoxime, obidoxime, methoxime, HI-6) on Complex I of electron transport chain (ETC) were examined. The enzyme activity was measured spectrophotometrically in crude mitochondrial fraction isolated from pig brain. RESULTS: Our results showed statistically significant Complex I inhibition by tacrine, other drugs did not affect the enzyme activity significantly. CONCLUSIONS: These observations suggest the possibility of tacrine-induced side effects related to disturbance in ETC. On the contrary, it seems that oximes do not affect cellular energetic metabolism.
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