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6-甲基芹菜素和橙皮苷:对中枢神经系统有活性的新缬草类黄酮。

6-methylapigenin and hesperidin: new valeriana flavonoids with activity on the CNS.

作者信息

Marder Mariel, Viola Haydeé, Wasowski Cristina, Fernández Sebastián, Medina Jorge H, Paladini Alejandro C

机构信息

Facultad de Farmacia y Bioquímica, Instituto de Química y Fisicoquímica Biológicas, Junín 956 (1113), Buenos Aires, Argentina.

出版信息

Pharmacol Biochem Behav. 2003 Jun;75(3):537-45. doi: 10.1016/s0091-3057(03)00121-7.

DOI:10.1016/s0091-3057(03)00121-7
PMID:12895671
Abstract

Valerian is an ancient tranquillizing drug obtained from the underground organs of several Valeriana species. Its active principles were assumed to be terpenoids in the form of valepotriates and/or as components of the essential oil. However, unknown active compounds were not discarded and synergic effects were suspected. We have recently isolated 6-methylapigenin (MA) from Valeriana wallichii and proved that it is a benzodiazepine binding site (BDZ-bs) ligand [Planta Med. 68 (2002) 934]. The present paper is the first report of the presence of 2S(-)-hesperidin in valeriana and describes that it has sedative and sleep-enhancing properties. MA, in turn, was found to have anxiolytic properties and was able to potentiate the sleep-enhancing properties of hesperidin (HN).MA and HN are new members of the growing family of natural flavonoids with activity on the CNS, and their properties suggest that they are promising drug leads in the field.

摘要

缬草是一种从多种缬草属植物的地下器官中获取的古老镇静药物。其活性成分被认为是缬草三酯形式的萜类化合物和/或作为精油的成分。然而,未知的活性化合物并未被排除,并且怀疑存在协同作用。我们最近从尼泊尔缬草中分离出6-甲基芹菜素(MA),并证明它是一种苯二氮䓬结合位点(BDZ-bs)配体[《植物医学》68(2002)934]。本文是关于缬草中存在2S(-)-橙皮苷的首次报道,并描述了它具有镇静和增强睡眠的特性。反过来,发现MA具有抗焦虑特性,并且能够增强橙皮苷(HN)的助眠特性。MA和HN是越来越多对中枢神经系统有活性的天然黄酮类家族的新成员,它们的特性表明它们是该领域有前景的药物先导物。

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