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5-羟色胺1A受体参与槲皮苷的抗焦虑样作用及单胺能系统参与的证据

Involvement of 5-HT1A Receptors in the Anxiolytic-Like Effects of Quercitrin and Evidence of the Involvement of the Monoaminergic System.

作者信息

Li Jian, Liu Qian-Tong, Chen Yi, Liu Jie, Shi Jin-Li, Liu Yong, Guo Jian-You

机构信息

School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.

Key Laboratory of Mental Health, Institute of Psychology, Chinese Academy of Sciences, Beijing 100101, China.

出版信息

Evid Based Complement Alternat Med. 2016;2016:6530364. doi: 10.1155/2016/6530364. Epub 2016 May 19.

DOI:10.1155/2016/6530364
PMID:27298626
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4889836/
Abstract

Quercitrin is a well-known flavonoid that is contained in Flos Albiziae, which has been used for the treatment of anxiety. The present study investigated the anxiolytic-like effects of quercitrin in experimental models of anxiety. Compared with the control group, repeated treatment with quercitrin (5.0 and 10.0 mg/kg/day, p.o.) for seven days significantly increased the percentage of entries into and time spent on the open arms of the elevated plus maze. In the light/dark box test, quercitrin exerted an anxiolytic-like effect at 5 and 10 mg/kg. In the marble-burying test, quercitrin (5.0 and 10.0 mg/kg) also exerted an anxiolytic-like effect. Furthermore, quercitrin did not affect spontaneous locomotor activity. The anxiolytic-like effects of quercitrin in the elevated plus maze and light/dark box test were blocked by the serotonin-1A (5-hydroxytryptamine-1A (5-HT1A)) receptor antagonist WAY-100635 (3.0 mg/kg, i.p.) but not by the γ-aminobutyric acid-A (GABAA) receptor antagonist flumazenil (0.5 mg/kg, i.p.). The levels of brain monoamines (5-HT and dopamine) and their metabolites (5-hydroxy-3-indoleacetic acid, 3,4-dihydroxyphenylacetic acid, and homovanillic acid) were decreased after quercitrin treatment. These data suggest that the anxiolytic-like effects of quercitrin might be mediated by 5-HT1A receptors but not by benzodiazepine site of GABAA receptors. The results of the neurochemical studies suggest that these effects are mediated by modulation of the levels of monoamine neurotransmitters.

摘要

槲皮苷是一种著名的黄酮类化合物,存在于合欢花中,合欢花已被用于治疗焦虑症。本研究在焦虑症实验模型中研究了槲皮苷的抗焦虑样作用。与对照组相比,连续7天用槲皮苷(5.0和10.0毫克/千克/天,口服)重复治疗显著增加了高架十字迷宫开放臂的进入次数百分比和停留时间。在明暗箱试验中,槲皮苷在5和10毫克/千克时发挥抗焦虑样作用。在埋大理石试验中,槲皮苷(5.0和10.0毫克/千克)也发挥了抗焦虑样作用。此外,槲皮苷不影响自发运动活动。槲皮苷在高架十字迷宫和明暗箱试验中的抗焦虑样作用被5-羟色胺-1A(5-HT1A)受体拮抗剂WAY-100635(3.0毫克/千克,腹腔注射)阻断,但未被γ-氨基丁酸-A(GABAA)受体拮抗剂氟马西尼(0.5毫克/千克,腹腔注射)阻断。槲皮苷治疗后,脑单胺(5-HT和多巴胺)及其代谢产物(5-羟基-3-吲哚乙酸、3,4-二羟基苯乙酸和高香草酸)水平降低。这些数据表明,槲皮苷的抗焦虑样作用可能由5-HT1A受体介导,而非由GABAA受体的苯二氮䓬位点介导。神经化学研究结果表明,这些作用是通过调节单胺神经递质水平介导的。

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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/68e6/4889836/1ce10a4cc1a2/ECAM2016-6530364.007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/68e6/4889836/2970a72b0d97/ECAM2016-6530364.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/68e6/4889836/0751a60e0eb9/ECAM2016-6530364.002.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/68e6/4889836/1ce10a4cc1a2/ECAM2016-6530364.007.jpg

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