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西番莲属对γ-氨基丁酸(GABA)系统的调制作用

Modulation of the γ-aminobutyric acid (GABA) system by Passiflora incarnata L.

机构信息

VivaCell Biotechnology GmbH, Denzlingen, Germany.

出版信息

Phytother Res. 2011 Jun;25(6):838-43. doi: 10.1002/ptr.3352. Epub 2010 Nov 19.

DOI:10.1002/ptr.3352
PMID:21089181
Abstract

Passiflora incarnata L. (Passifloraceae) is important in herbal medicine for treating anxiety or nervousness, Generalized Anxiety Disorder (GAD), symptoms of opiate withdrawal, insomnia, neuralgia, convulsion, spasmodic asthma, ADHD, palpitations, cardiac rhythm abnormalities, hypertension, sexual dysfunction and menopause. However, the mechanism of action is still under discussion. Despite gaps in our understanding of neurophysiological processes, it is increasingly being recognized that dysfunction of the GABA system is implicated in many neuropsychiatric conditions, including anxiety and depressive disorders. Therefore, the in vitro effects of a dry extract of Passiflora incarnata (sole active ingredient in Pascoflair® 425 mg) on the GABA system were investigated. The extract inhibited [(3) H]-GABA uptake into rat cortical synaptosomes but had no effect on GABA release and GABA transaminase activity. Passiflora incarnata inhibited concentration dependently the binding of [(3) H]- SR95531 to GABA(A) -receptors and of [(3) H]-CGP 54626 to GABA(B) -receptors. Using the [(35) S]-GTPγS binding assay Passiflora could be classified as an antagonist of the GABA(B) receptor. In contrast, the ethanol- and the benzodiazepine-site of the GABA(A) -receptor were not affected by this extract. In conclusion, the first evidence was shown that numerous pharmacological effects of Passiflora incarnata are mediated via modulation of the GABA system including affinity to GABA(A) and GABA(B) receptors, and effects on GABA uptake.

摘要

鸡蛋果(西番莲科)在草药学中被广泛应用于治疗焦虑或紧张、广泛性焦虑障碍(GAD)、阿片类药物戒断症状、失眠、神经痛、惊厥、痉挛性哮喘、多动症、心悸、心律失常、高血压、性功能障碍和更年期等症状。然而,其作用机制仍在讨论中。尽管我们对神经生理过程的理解存在差距,但越来越多的人认识到 GABA 系统功能障碍与许多神经精神疾病有关,包括焦虑和抑郁障碍。因此,研究了鸡蛋果干提取物(Pascoflair®425mg 的唯一活性成分)对 GABA 系统的体外作用。该提取物抑制了大鼠皮质突触小体摄取 [(3)H]-GABA,但对 GABA 释放和 GABA 转氨酶活性没有影响。鸡蛋果提取物浓度依赖性地抑制了 [(3)H]-SR95531 与 GABA(A)受体和 [(3)H]-CGP 54626 与 GABA(B)受体的结合。使用 [(35)S]-GTPγS 结合测定法,鸡蛋果可被分类为 GABA(B)受体拮抗剂。相比之下,这种提取物对 GABA(A)受体的乙醇和苯二氮䓬结合位点没有影响。总之,首次证明鸡蛋果的许多药理作用是通过调节 GABA 系统介导的,包括对 GABA(A)和 GABA(B)受体的亲和力以及对 GABA 摄取的影响。

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