1. Antiinflammatory and neurological activity of pyrithione and related sulfur-containing pyridine N-oxides from Persian shallot (Allium stipitatum)
- Author
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Petra Kučerová, Gary I. Stafford, Roman Kubec, Petra Krejčová, and Anna K. Jäger
- Subjects
Monoamine Oxidase Inhibitors ,Pyridines ,Aché ,Serotonin transport ,Pharmacology ,Shallots ,chemistry.chemical_compound ,Drug Discovery ,Animals ,Cyclooxygenase Inhibitors ,Receptor ,Monoamine Oxidase ,IC50 ,Horseradish Peroxidase ,biology ,Allium stipitatum ,Brain ,RNA-Binding Proteins ,Thiones ,Receptors, GABA-A ,biology.organism_classification ,Acetylcholinesterase ,language.human_language ,Rats ,Monoamine neurotransmitter ,chemistry ,Cyclooxygenase 2 ,Cyclooxygenase 1 ,language ,biology.protein ,Cholinesterase Inhibitors ,Cyclooxygenase - Abstract
Ethnopharmacological relevance Persian shallot (Allium stipitatum) is a bulbous plant native to Turkey, Iran and Central Asia. It is frequently used in folk medicine for the treatment of a variety of disorders, including inflammation and stress. Antiinflammatory and neurological activities of pyrithione and four related sulfur-containing pyridine N-oxides which are prominent constituents of Allium stipitatum were tested. Methods The antiinflammatory activity was tested by the ability of the compounds to inhibit cyclooxygenase (COX-1 and COX-2), whereas the neurological activities were evaluated by assessing the compounds ability to inhibit monoamine oxidase-A (MAO-A) and acetylcholinesterase (AChE). The compounds׳ affinity for the serotonin transport protein (SERT) and the GABAA–benzodiazepine receptor were also investigated. Results 2-[(Methylthio)methyldithio]pyridine N-oxide showed very high antiinflammatory effects which are comparable with those of common pharmaceuticals (IC50 of 7.8 and 15.4 µM for COX-1 and COX-2, respectively). On the other hand, neurological activities of the compounds were rather modest. Some compounds moderately inhibited AChE (IC50 of 104–1041 µM) and MAO-A (IC50 of 98–241 µM) and exhibited an affinity for the SERT and GABAA–benzodiazepine receptor. Conclusions Our findings may help to rationalize the wide use of Persian shallot for the treatment of inflammatory disorders.
- Published
- 2014
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