Ognibene Elisa, Bovicelli Paolo, Adriani Walter, Saso Luciano, Laviola Giovanni
Behavioural Neuroscience Section, Department of Cell Biology & Neuroscience, Istituto Superiore di Sanità, Viale Regina Elena 299, 00161, Rome, Italy.
Prog Neuropsychopharmacol Biol Psychiatry. 2008 Jan 1;32(1):128-34. doi: 10.1016/j.pnpbp.2007.07.023. Epub 2007 Aug 6.
Benzodiazepines (BDZs) are the most used psychoactive drugs in the pharmacotherapy of anxiety. A large number of structurally different classes of ligands are also active in the modulation of anxiety, showing high affinity for the benzodiazepine binding site (BDZ-bs) of the GABA (A) receptor complex. Various synthetic derivatives of natural flavonoids have been found to have very potent anxiolytic properties. This study was undertaken to provide a behavioral characterization of two novels halogenated flavonoids, 5-methoxy-6, 8-dibromoflavanone (FV1), and 6-bromoflavanone (FV2). These compounds were tested and compared to diazepam (0.5 mg/kg) and to the natural flavonoid chrysin (1 mg/kg) as a standard of activity. When injected in mice (0.5, 1 mg/kg i.p) both synthetic flavonoids increased the locomotor activity and the exploratory skills of the animals, as measured in the open-field and in the hole-board tests. Both compounds, indeed, had a clear anxiolytic activity in the elevated plus-maze, as measured by an increased number of entries and the percentage of time spent in the open arms. At the tested doses, both compounds did not induce sedative action or compulsive behaviour. These results encourage making deeper investigations on this field.
苯二氮䓬类药物（BDZs）是焦虑症药物治疗中使用最广泛的精神活性药物。大量结构不同的配体类别在焦虑调节方面也具有活性，对GABA（A）受体复合物的苯二氮䓬结合位点（BDZ-bs）表现出高亲和力。已发现天然黄酮类化合物的各种合成衍生物具有非常有效的抗焦虑特性。本研究旨在对两种新型卤代黄酮类化合物5-甲氧基-6,8-二溴黄酮（FV1）和6-溴黄酮（FV2）进行行为特征描述。将这些化合物进行测试，并与地西泮（0.5mg/kg）和天然黄酮类化合物白杨素（1mg/kg）作为活性标准进行比较。当以0.5、1mg/kg腹腔注射给小鼠时，两种合成黄酮类化合物均增加了动物的运动活性和探索技能，这在旷场试验和洞板试验中得以测量。实际上，通过增加进入次数和在开放臂中花费的时间百分比来衡量，两种化合物在高架十字迷宫中均具有明显的抗焦虑活性。在测试剂量下，两种化合物均未诱导镇静作用或强迫行为。这些结果鼓励在该领域进行更深入的研究。
