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狭叶旋覆花提取物作为三重单胺摄取抑制剂。

Extracts of Sideritis scardica as triple monoamine reuptake inhibitors.

机构信息

IBAM GbR, Ferdinand-Porsche-Strasse 5, 79211, Denzlingen, Germany.

出版信息

J Neural Transm (Vienna). 2012 Dec;119(12):1477-82. doi: 10.1007/s00702-012-0824-9. Epub 2012 May 24.

DOI:10.1007/s00702-012-0824-9
PMID:22622367
Abstract

Sideritis species are traditionally used within the Mediterranean area as teas, flavouring agents or for therapeutical purposes. The aim of this study was to investigate the effects of Sideritis scardica extracts on the monoamine transporters and to derive and explain possible medicinal applications from the pharmacological profile of the extracts. We have studied the effect of various S. scardica extracts on serotonin, noradrenaline and dopamine uptake in rat brain synaptosomes and serotonin uptake in human JAR cells. All extracts inhibited the uptake of all three monoamines into rat brain synaptosomes by their respective transporters, the alcoholic extracts being more effective than the water extract. EC(50) values were in the range of 30-40 μg/ml. Inhibition of the human serotonin transporter by the methanol extract was even more effective (EC(50) 1.4 μg/ml). Combining Sideritis ethanol extract and fluvoxamine resulted in a leftward shift of the fluvoxamine concentration-response curve. The pharmacological profile of S. scardica extracts as triple monoamine reuptake inhibitors suggests their use in the phytochemical therapy of mental disorders associated with a malfunctioning monoaminergic neurotransmission, such as anxiety disorders, major depression, attention-deficit hyperactivity disorder, mental impairment or neurodegenerative diseases.

摘要

传统上,地中海地区的人们将羊奶菜属植物用作茶、调味剂或用于治疗目的。本研究旨在研究羊奶菜提取物对单胺转运体的影响,并从提取物的药理学特征中得出并解释可能的药用应用。我们研究了各种羊奶菜提取物对大鼠脑突触体中 5-羟色胺、去甲肾上腺素和多巴胺摄取以及人 JAR 细胞中 5-羟色胺摄取的影响。所有提取物均通过各自的转运体抑制三种单胺进入大鼠脑突触体的摄取,其中醇提取物比水提取物更有效。EC(50)值在 30-40μg/ml 范围内。甲醇提取物对人 5-羟色胺转运体的抑制作用甚至更有效(EC(50)为 1.4μg/ml)。羊奶菜乙醇提取物和氟伏沙明联合使用导致氟伏沙明浓度反应曲线向左移位。羊奶菜提取物作为三单胺再摄取抑制剂的药理学特征表明,它们可用于治疗与单胺能神经传递功能障碍相关的精神障碍的植物化学疗法,例如焦虑障碍、重度抑郁症、注意缺陷多动障碍、智力障碍或神经退行性疾病。

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