ArticleBiochimica et biophysica acta2011
Synergistic inhibition of butyrylcholinesterase by galantamine and citalopram.
Article in Biochimica et biophysica acta, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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12 citing papers in PubMed, 35 citations in OpenAlex.
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- Phytochemical profiling and in vitro screening for anticholinesterase, antioxidant, antiglucosidase and neuroprotective effect of three traditional medicinal plants for Alzheimer's Disease and Diabetes Mellitus dual therapy.BMC complementary and alternative medicine · 2018Article
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- Synthesis and biological evaluation of lycorine derivatives as dual inhibitors of human acetylcholinesterase and butyrylcholinesterase.Chemistry Central journal · 2012Article
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
backgroundMany persons with Alzheimer's disease (AD) treated with galantamine appear to receive additional cognitive benefit from citalopram. Both drugs inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). These enzymes co-regulate acetylcholine catabolism. In AD brain, AChE is diminished while BuChE is not, suggesting BuChE inhibition may be important in raising acetylcholine levels. BuChE is subject to activation at high acetylcholine levels reached at the synaptic cleft. The present study explores one way combining galantamine and citalopram could be beneficial in AD.
methodsSpectrophotometric studies of BuChE catalysis in the absence or presence of galantamine or citalopram or both, were performed using the Ellman method. Data analysis involved expansion of our previous equation describing BuChE catalysis.
resultsGalantamine almost completely inhibited BuChE at low substrate concentrations (V(S)=43.6 μM/min; V(S(gal))=0.34 μM/min) without influencing the substrate-activated form of the enzyme (V(SS)=64.0 μM/min;V(SS(gal))=62.3 μM/min). Conversely, citalopram inhibited both un-activated (V(S)=43.6 μM/min; V(S(cit))=10.2 μM/min) and substrate-activated (V(SS)=64.0 μM/min; V(SS(cit))=47.3 μM/min) forms of BuChE. Combined galantamine and citalopram increased inhibition of un-activated BuChE (V(S)=43.6 μM/min; V(S(gal)(cit))=2.73 μM/min) and substrate-activated form (V(SS)=64.0 μM/min; V(SS(gal)(cit))=42.2 μM/min).
conclusionCitalopram and galantamine produce a combined inhibition of BuChE that is considered to be synergistic. GENERAL SIGNIFICANCE: Clinical benefit from combined galantamine and citalopram may be related to a synergistic inhibition of BuChE, facilitating cholinergic neurotransmission. This emphasizes the importance of further study into use of drug combinations in AD treatment.
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