Krejčová Petra, Kučerová Petra, Stafford Gary I, Jäger Anna K, Kubec Roman
Department of Applied Chemistry, University of South Bohemia, Branišovská 31, 370 05 České Budějovice, Czech Republic.
Natural History Museum of Denmark, University of Copenhagen, Sølvgade 83, Opg. S., DK-1307 Copenhagen K, Denmark; Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, 2 Universitetsparken, DK-2100 Copenhagen Ø, Denmark.
J Ethnopharmacol. 2014 May 28;154(1):176-82. doi: 10.1016/j.jep.2014.03.066. Epub 2014 Apr 8.
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.
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.
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.
Our findings may help to rationalize the wide use of Persian shallot for the treatment of inflammatory disorders.
波斯葱（Allium stipitatum）是一种原产于土耳其、伊朗和中亚的球根植物。它在民间医学中常用于治疗多种疾病，包括炎症和压力。对吡啶硫酮及四种相关的含硫吡啶N-氧化物（它们是波斯葱的主要成分）的抗炎和神经学活性进行了测试。
通过化合物抑制环氧化酶（COX-1和COX-2）的能力来测试其抗炎活性，而通过评估化合物抑制单胺氧化酶-A（MAO-A）和乙酰胆碱酯酶（AChE）的能力来评估其神经学活性。还研究了这些化合物对5-羟色胺转运蛋白（SERT）和GABAA-苯二氮䓬受体的亲和力。
2-[(甲硫基)甲基二硫代]吡啶N-氧化物显示出非常高的抗炎效果，可与常见药物相媲美（对COX-1和COX-2的IC₅₀分别为7.8和15.4 μM）。另一方面，这些化合物的神经学活性相当一般。一些化合物适度抑制AChE（IC₅₀为104 - 1041 μM）和MAO-A（IC₅₀为98 - 241 μM），并对SERT和GABAA-苯二氮䓬受体表现出亲和力。
我们的研究结果可能有助于解释波斯葱在治疗炎症性疾病方面广泛应用的合理性。
