Yoon Byung Hoon, Jung Ji Wook, Lee Jong-Ju, Cho Young-Wuk, Jang Choon-Gon, Jin Changbae, Oh Tae Hwan, Ryu Jong Hoon
Department of Oriental Pharmaceutical Science and Kyung Hee East-West Pharmaceutical Research Institute, College of Pharmacy, Kyung Hee University, Hoeki-dong, Dongdaemoon-ku, Seoul 130-701, Republic of Korea.
Life Sci. 2007 Jun 27;81(3):234-40. doi: 10.1016/j.lfs.2007.05.007. Epub 2007 May 21.
Sinapic acid is a phenylpropanoid compound and is found in various herbal materials and high-bran cereals. With the exception of its antioxidant activities, the pharmacological properties of sinapic acid have been rarely reported. The purpose of this study was to characterize the putative anxiolytic-like properties of sinapic acid using an elevated plus-maze (EPM) and hole-board test. Control mice were orally treated with an equal volume of vehicle (10% Tween 80 solution), and positive control mice were treated with diazepam (1 mg/kg, i.p.). Sinapic acid (4 mg/kg, p.o.) significantly increased the percentages of time spent in the open arms of the EPM test (P<0.05). In the hole-board test, sinapic acid also significantly increased the number of head-dips at 4 mg/kg (P<0.05). In addition, the anxiolytic-like properties of sinapic acid examined in the EPM test were blocked by flumazenil or bicuculline, which are GABA(A) antagonists. Moreover, sinapic acid markedly potentiated GABA current in single cortical neurons in a dose-dependant manner, and reactive I(GABA) increased to 1.8 times at 1 muM of sinapic acid. These results suggested that sinapic acid is a prominent anxiolytic agent, and that its anxiolytic-like effects are mediated via GABA(A) receptors and potentiating Cl(-) currents.
芥子酸是一种苯丙烷类化合物,存在于多种草药材料和高麸谷物中。除了其抗氧化活性外,芥子酸的药理特性鲜有报道。本研究的目的是使用高架十字迷宫(EPM)和洞板试验来表征芥子酸假定的抗焦虑样特性。对照组小鼠口服等体积的赋形剂(10%吐温80溶液),阳性对照组小鼠腹腔注射地西泮(1 mg/kg)。芥子酸(4 mg/kg,口服)显著增加了EPM试验中在开放臂停留时间的百分比(P<0.05)。在洞板试验中,芥子酸在4 mg/kg时也显著增加了探头次数(P<0.05)。此外,在EPM试验中检测到的芥子酸的抗焦虑样特性被氟马西尼或荷包牡丹碱阻断,这两种都是GABA(A)拮抗剂。此外,芥子酸以剂量依赖的方式显著增强单个皮质神经元中的GABA电流,在1 μM芥子酸时,反应性I(GABA)增加到1.8倍。这些结果表明,芥子酸是一种显著的抗焦虑剂,其抗焦虑样作用是通过GABA(A)受体介导并增强Cl(-)电流实现的。