Sánchez-Borzone Mariela Eugenia, Marin Leticia Delgado, García Daniel Asmed
Instituto de Investigaciones Biológicas y Tecnológicas (IIBYT), CONICET-Universidad Nacional de Córdoba, Av. Vélez Sarsfield 1611, Córdoba 5016, Argentina.
Pharmacogn Mag. 2017 Jan-Mar;13(49):114-117. doi: 10.4103/0973-1296.197638.
The genus , an important member of the family, is represented by many species commonly known as mint. The insecticidal activity of oil and its main components has been tested and established against various insects/pests. Among these, the ketone monoterpenes that are most common in different species demonstrated insect toxicity, with pulegone being the most active, followed by carvone and menthone. Considering that the GABA receptor (GABA-R) is one of the main insecticide targets on neurons, and that pulegone would modulate the insect GABA system, it may be expected that the insecticidal properties of ketones are mediated by their interaction with this receptor.
In order to discern the pharmacological actions of these products when used as insecticides on mammalian organisms, we evaluated the pharmacologic activity of ketones, commonly present in plants, on native GABA-R from rats.
Determination of ketones effects on allosterically enhanced benzodiazepine binding, using primary cultures of cortical neurons, which express functional receptors and MTT assay to evaluate their cell toxicity.
Our results seem to indicate that ketone components of , with proven repellent or insecticide activity, were able to behave as GABA-R negative allosteric modulators in murine cells and consequently could exhibit convulsant activity in mammalians. Only pulegone at the highest assayed concentration (2 mM) showed a significant reduction in cell viability after exposure for 24 hr.
The present results strongly suggest that the ketone components of are able to exhibit convulsant activity in mammalian organisms, but functional assays and experiments would be necessary to corroborate this proposed action.
The pharmacological activity of insecticide ketones, commonly present in plants, was evaluated on native GABA receptor from mammalian neurons.All studied compounds: pulegone, menthone and dihydrocarvone, were able to behave as negative allosteric modulators and could exhibit convulsant activity in mammalian organisms.Citotoxicity assays demonstrated that only pulegone affected the cell viability. GABA: gamma aminobutyric acid, GABAA-R: GABAA receptor, MTT: 1-(4,5-dimethylthiazol-2-yl)-3,5-diphenylformazam, DMEM: Dulbecco's modified minimum essential mèdium, [3H]TBOB: [3H] t-Butylbicycloorthobenzoate.
薄荷属是唇形科的重要成员，有许多常见的薄荷品种。薄荷油及其主要成分对多种昆虫/害虫的杀虫活性已得到测试和确认。其中，不同薄荷品种中最常见的酮类单萜表现出昆虫毒性，胡薄荷酮活性最强，其次是香芹酮和薄荷酮。鉴于γ-氨基丁酸受体（GABA-R）是神经元上主要的杀虫剂作用靶点之一，且胡薄荷酮会调节昆虫的GABA系统，因此可以预期薄荷酮类的杀虫特性是通过它们与该受体的相互作用介导的。
为了识别这些产品作为杀虫剂作用于哺乳动物机体时的药理作用，我们评估了薄荷植物中常见的酮类对大鼠天然GABA-R的药理活性。
使用表达功能性受体的皮质神经元原代培养物，测定酮类对变构增强的苯二氮䓬结合的影响，并采用MTT法评估其细胞毒性。
我们的结果似乎表明，具有已证实的驱避或杀虫活性的薄荷酮类成分，在鼠细胞中能够作为GABA-R负变构调节剂，因此在哺乳动物中可能表现出惊厥活性。仅最高检测浓度（2 mM）的胡薄荷酮在暴露24小时后显示细胞活力显著降低。
目前的结果强烈表明，薄荷酮类成分在哺乳动物机体中能够表现出惊厥活性，但需要功能试验和体内实验来证实这一推测的作用。
评估了薄荷植物中常见的杀虫剂酮类对哺乳动物神经元天然GABA受体的药理活性。所有研究的化合物：胡薄荷酮、薄荷酮和二氢香芹酮，都能够作为负变构调节剂，并在哺乳动物机体中表现出惊厥活性。细胞毒性试验表明，只有胡薄荷酮影响细胞活力。 GABA：γ-氨基丁酸，GABAA-R：GABAA受体，MTT：噻唑蓝，DMEM：杜氏改良Eagle培养基，[3H]TBOB：[3H]叔丁基双环邻苯二甲酸酯
