Khan Faisal, Saify Zafar Saeed, Jamali Khawar Saeed, Naz Saima, Hassan Sohail, Siddiqui Sonia
Department of Neuroscience, Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan.
HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi.
Pak J Pharm Sci. 2018 Jan;31(1(Suppl.)):297-303.
Vitex negundo (Vn) extract is famous for the treatment of neurological diseases such as migraine and epilepsy. These neurological diseases have been associated with abnormally increased influx of sodium ions into the neurons. Drugs that inhibit voltage gated sodium channels can be used as potent anti-epileptics. Till now, the effects of Vn on sodium channels have not been investigated. Therefore, we have investigated the effects of methalonic fraction of Vn extract in Murine Neuro 2A cell line. Cells were cultured in a defined medium with or without the Vn extract (100 μg/ml). Sodium currents were recorded using whole-cell patch clamp method. The data show that methanolic extract of Vn inhibited sodium currents in a dose dependent manner (IC50 =161μg/ml). Vn (100 μg/ml) shifted the steady-state inactivation curve to the left or towards the hyper polarization state. However, Vn did not show any effects on outward rectifying potassium currents. Moreover, Vn (100 μg/ml) significantly reduced the sustained repetitive (48±4.8%, P<0.01) firing from neonatal hippocampal neurons at 12 DIV. Hence, our data suggested that inhibition of sodium channels by Vn may exert pharmacological effects in reducing pain and convulsions.
黄荆提取物因可治疗偏头痛和癫痫等神经疾病而闻名。这些神经疾病与钠离子异常大量流入神经元有关。抑制电压门控钠通道的药物可作为有效的抗癫痫药物。到目前为止，尚未研究黄荆对钠通道的影响。因此，我们研究了黄荆提取物的甲醇组分对小鼠Neuro 2A细胞系的影响。细胞在添加或不添加黄荆提取物（100μg/ml）的特定培养基中培养。使用全细胞膜片钳方法记录钠电流。数据表明，黄荆的甲醇提取物以剂量依赖性方式抑制钠电流（IC50 = 161μg/ml）。黄荆（100μg/ml）使稳态失活曲线向左或向超极化状态移动。然而，黄荆对外向整流钾电流没有任何影响。此外，黄荆（100μg/ml）显著降低了12日龄新生海马神经元的持续重复放电（48±4.8%，P<0.01）。因此，我们的数据表明，黄荆对钠通道的抑制作用可能在减轻疼痛和惊厥方面发挥药理作用。
