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GABA-苯二氮䓬受体拮抗剂氟马西尼消除了西红花酸活性成分在大鼠中的抗焦虑作用。

The GABA-Benzodiazepine Receptor Antagonist Flumazenil Abolishes the Anxiolytic Effects of the Active Constituents of L. Crocins in Rats.

机构信息

Department of Pharmacology, Faculty of Medicine, School of Health Sciences, University of Thessaly, Biopolis, Panepistimiou 3, 415-00 Larissa, Greece.

Laboratory of Chemistry, Department of Food Science and Human Nutrition, School of Food and Nutritional Sciences, Agricultural University of Athens, 118-55 Athens, Greece.

出版信息

Molecules. 2020 Nov 30;25(23):5647. doi: 10.3390/molecules25235647.

Abstract

Anxiety is a chronic severe psychiatric disorder. Crocins are among the various bioactive components of the plant L. (Iridaceae) and their implication in anxiety is well-documented. However, which is the mechanism of action underlying the anti-anxiety effects of crocins remains unknown. In this context, it has been suggested that these beneficial effects might be ascribed to the agonistic properties of these bioactive ingredients of saffron on the GABA type A receptor. The current experimentation was undertaken to clarify this issue in the rat. For this research project, the light/dark and the open field tests were used. A single injection of crocins (50 mg/kg, i.p., 60 min before testing) induces an anti-anxiety-like effect revealed either in the light-dark or open field tests. Acute administration of the GABA-benzodiazepine receptor antagonist flumazenil (10 mg/kg, i.p., 30 min before testing) abolished the above mentioned anxiolytic effects of crocins. The current findings suggest a functional interaction between crocins and the GABA receptor allosteric modulator flumazenil on anxiety.

摘要

焦虑症是一种慢性严重的精神障碍。西红花中的藏红花酸是各种生物活性成分之一,其在焦虑症中的作用已得到充分证明。然而,藏红花酸发挥抗焦虑作用的机制尚不清楚。在这种情况下,有人认为这些有益的作用可能归因于藏红花这些生物活性成分对 GABA 型 A 受体的激动特性。目前的实验旨在澄清这一问题在大鼠中。为此研究项目,采用了明暗和旷场测试。单次注射西红花酸(50mg/kg,ip,测试前 60 分钟)可在明暗或旷场测试中诱导出类似焦虑的效果。GABA-苯二氮䓬受体拮抗剂氟马西尼(10mg/kg,ip,测试前 30 分钟)可消除西红花酸的上述抗焦虑作用。目前的研究结果表明,西红花酸和 GABA 受体变构调节剂氟马西尼之间存在功能性相互作用,可用于治疗焦虑症。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d755/7730330/8ee47acbe77c/molecules-25-05647-g001.jpg

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