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天然非营养性甜味剂甜菊糖苷和莱鲍迪苷A抗惊厥作用的计算机辅助鉴定

Computer-Aided Identification of Anticonvulsant Effect of Natural Nonnutritive Sweeteners Stevioside and Rebaudioside A.

作者信息

Di Ianni Mauricio E, Del Valle María E, Enrique Andrea V, Rosella María A, Bruno Fiorella, Bruno-Blanch Luis E, Talevi Alan

机构信息

1 Medicinal Chemistry, Department of Biological Sciences, Faculty of Exact Sciences, National University of La Plata , Buenos Aires, Argentina .

2 Natural Products, Department of Biological Sciences, Faculty of Exact Sciences, National University of La Plata , Buenos Aires, Argentina .

出版信息

Assay Drug Dev Technol. 2015 Jul-Aug;13(6):313-8. doi: 10.1089/adt.2015.29010.meddrrr.

Abstract

Steviol glycosides are natural constituents of Stevia rebaudiana (Bert.) Bert. (Asteraceae) that have recently gained worldwide approval as nonnutritive sweeteners by the Joint Food and Agriculture Organization/World Organization Expert Committee on Food Additives. Cheminformatic tools suggested that the aglycone steviol and several of its phase I metabolites were predicted as potential anticonvulsant agents effective in the seizure animal model maximal electroshock seizure (MES) test. Thus, aqueous infusion from S. rebaudiana was tested in the MES test (mice, intraperitoneal administration), confirming dose-dependent anticonvulsant effect. Afterward, isolated stevioside and rebaudioside A were tested in the MES test, with positive results. Though drug repositioning most often focuses on known therapeutics, this article illustrates the possibilities of this strategy to find new functionalities and therapeutic indications for food constituents and natural products.

摘要

甜菊糖苷是甜叶菊(菊科)的天然成分,最近已获得联合国粮食及农业组织/世界卫生组织食品添加剂联合专家委员会的全球批准,作为非营养性甜味剂使用。化学信息学工具表明,苷元甜菊醇及其几种I相代谢物被预测为在癫痫动物模型最大电休克发作(MES)试验中有效的潜在抗惊厥剂。因此,在MES试验(小鼠,腹腔注射)中对甜叶菊水浸液进行了测试,证实了其剂量依赖性抗惊厥作用。随后,对分离出的甜菊糖苷和莱鲍迪苷A进行了MES试验,结果呈阳性。尽管药物重新定位通常侧重于已知的治疗方法,但本文阐述了该策略为食品成分和天然产物寻找新功能和治疗适应症的可能性。

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本文引用的文献

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Non-nutritive sweeteners: review and update.非营养性甜味剂:综述与更新。
Nutrition. 2013 Nov-Dec;29(11-12):1293-9. doi: 10.1016/j.nut.2013.03.024. Epub 2013 Jul 8.
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Stress and GABA receptors.应激与 GABA 受体。
J Neurochem. 2010 Mar;112(5):1115-30. doi: 10.1111/j.1471-4159.2009.06539.x. Epub 2009 Dec 10.
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Characterization of the anticonvulsant profile of valpromide derivatives.
Bioorg Med Chem. 2004 Jul 15;12(14):3857-69. doi: 10.1016/j.bmc.2004.05.003.

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