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香芹酚乙酸酯(香芹酚的衍生物)在小鼠体内产生的类似抗焦虑的效果。

Anxiolytic-like effects of carvacryl acetate, a derivative of carvacrol, in mice.

机构信息

Postgraduate Program of Pharmacology, Federal University of Piauí, Teresina, Piauí, Brazil.

出版信息

Pharmacol Biochem Behav. 2013 Nov;112:42-8. doi: 10.1016/j.pbb.2013.09.001. Epub 2013 Sep 12.

Abstract

Studies showing anxiolytic-like properties of natural products have grown. This paper evaluated if carvacryl acetate (CA) could be studied as an alternative drug to treat anxiety disorders. Elevated plus maze (EPM) tests , light-dark box (LDB) tests, and marble-burying tests (MBTs) were performed on mice. In the first protocol, the anxiolytic-like activities of CA 25, 50, 75 and 100mg/kg at single doses were compared to those of the vehicle, buspirone 5mg/kg (BUSP) and diazepam 1mg/kg (DZP). In the second protocol, the anxiolytic-like actions of CA were tested for GABAergic and serotonergic systems. The time spent in the open arms (TSOA) and the number of open arms entries (NOAE) were measured in EPM; the time spent in the light box (TSLB) and the number of entries to light box (NELB) were measured in LDB; and the number of marbles buried (NMB) were measured in MBT. CA increased TSOA and NOAE in the EPM, as well as TSLB and NELB in the LDB and the NMB in the MBT. The anxiolytic-like activity of CA 25; 50; 75 and 100mg/kg was not associated with psychomotor retardation in the open field test and in the Rota rod test, contrarily with what happened with DZP. In the second protocol, to suggest the mechanism of action of CA, flumazenil 25mg/kg ip (FLU) and WAY 100,635 10mg/kg ip (WAY-5-HT1A antagonist) were also used. FLU+CA100 reduced TSOA in the EPM when compared to CA100 but WAY+CA100 did not. In LDB, FLU+CA100 reduced the TSLB when compared to CA100 but WAY+CA100 did not. In the MBT, FLU+CA100 inhibited the effect of CA100 on the NMB but WAY+CA100 did not. In conclusion, CA seems to have an anxiolytic-like effect, probably due to GABAergic agonist action, without psychomotor side effects.

摘要

越来越多的研究表明天然产物具有抗焦虑特性。本文旨在评估乙酸香芹酯(CA)是否可作为治疗焦虑症的替代药物。通过高架十字迷宫(EPM)测试、明暗箱(LDB)测试和埋藏大理石测试(MBT)对小鼠进行了研究。在第一个方案中,比较了 CA 25、50、75 和 100mg/kg 单剂量的抗焦虑样活性与载体、丁螺环酮 5mg/kg(BUSP)和地西泮 1mg/kg(DZP)的活性。在第二个方案中,测试了 CA 对 GABA 能和 5-羟色胺能系统的抗焦虑样作用。EPM 中测量了在开放臂中花费的时间(TSOA)和进入开放臂的次数(NOAE);LDB 中测量了在亮箱中花费的时间(TSLB)和进入亮箱的次数(NELB);MBT 中测量了埋藏的大理石数量(NMB)。CA 增加了 EPM 中的 TSOA 和 NOAE,以及 LDB 中的 TSLB 和 NELB 和 MBT 中的 NMB。CA 25、50、75 和 100mg/kg 的抗焦虑样活性与旷场试验和旋转棒试验中的精神运动阻滞无关,而地西泮则相反。在第二个方案中,为了推测 CA 的作用机制,还使用了氟马西尼 25mg/kg ip(FLU)和 WAY 100,635 10mg/kg ip(WAY-5-HT1A 拮抗剂)。与 CA100 相比,FLU+CA100 降低了 EPM 中的 TSOA,但 WAY+CA100 没有。在 LDB 中,与 CA100 相比,FLU+CA100 降低了 TSLB,但 WAY+CA100 没有。在 MBT 中,FLU+CA100 抑制了 CA100 对 NMB 的作用,但 WAY+CA100 没有。总之,CA 似乎具有抗焦虑样作用,可能是由于 GABA 能激动剂作用,而没有运动副作用。

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