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dc.contributor.authorEngelbrecht, Idalet
dc.contributor.authorPetzer, Jacobus P.
dc.contributor.authorPetzer, Anél
dc.date.accessioned2019-09-02T07:52:27Z
dc.date.available2019-09-02T07:52:27Z
dc.date.issued2019
dc.identifier.citationEngelbrecht, I. et al. 2019. Evaluation of selected natural compounds as dual inhibitors of catechol-o-methyltransferase and monoamine oxidase. Central nervous system agents in medicinal chemistry, 19(2):133-145. [https://doi.org/10.2174/1871524919666190619090852]en_US
dc.identifier.issn1871-5249
dc.identifier.issn1875-6166 (Online)
dc.identifier.urihttp://hdl.handle.net/10394/33266
dc.identifier.urihttp://www.eurekaselect.com/172772/article
dc.identifier.urihttps://doi.org/10.2174/1871524919666190619090852
dc.description.abstractBackground: The most effective symptomatic treatment of Parkinson’s disease remains the metabolic precursor of dopamine, L-dopa. To enhance the efficacy of L-dopa, it is often combined with inhibitors of the enzymes, catechol-O-methyltransferase (COMT) and monoamine oxidase (MAO) B, key metabolic enzymes of L-dopa and dopamine. Objective: This study attempted to discover compounds that exhibit dual inhibition of COMT and MAO-B among a library of 40 structurally diverse natural compounds. Such dual acting inhibitors may be effective as adjuncts to L-dopa and offer enhanced value in the management of Parkinson’s disease. Methods: Selected natural compounds were evaluated as in vitro inhibitors of rat liver COMT and recombinant human MAO. Reversibility of MAO inhibition was investigated by dialysis. Results: Among the natural compounds morin (IC50 = 1.32 µM), chlorogenic acid (IC50 = 6.17 µM), (+)-catechin (IC50 = 0.86 µM), alizarin (IC50 = 0.88 µM), fisetin (IC50 = 5.78 µM) and rutin (IC50 = 25.3 µM) exhibited COMT inhibition. Among these active COMT inhibitors only morin (IC50 = 16.2 µM), alizarin (IC50 = 8.16 µM) and fisetin (IC50 = 7.33 µM) were noteworthy MAO inhibitors, with specificity for MAO-A. Conclusion: None of the natural products investigated here are dual COMT/MAO-B inhibitors. However, good potency COMT inhibitors have been identified, which may serve as leads for future development of COMT inhibitorsen_US
dc.language.isoenen_US
dc.publisherBentham Scienceen_US
dc.subjectCatechol-O-methyltransferaseen_US
dc.subjectInhibitionen_US
dc.subjectMonoamine oxidaseen_US
dc.subjectMulti-target-directeden_US
dc.subjectNatural compoundsen_US
dc.subjectParkinson's diseaseen_US
dc.titleEvaluation of selected natural compounds as dual inhibitors of catechol-o-methyltransferase and monoamine oxidaseen_US
dc.typeArticleen_US
dc.contributor.researchID12264954 - Petzer, Anél
dc.contributor.researchID10727388 - Petzer, Jacobus Petrus
dc.contributor.researchID21639159 - Engelbrecht, Idalet


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