Rauf Abdur, Uysal Sengul, Hadda Taibi Ben, Uddin Ghias, Nawaz Muhammad Asif, Khan Haroon, Siddiqui Bina S, Raza Muslim, Bawazeer Saud, Zengin Gokhan
Department of Chemistry, University of Swabi, Swabi, Anbar, 23561 Khyber Pakhtunkhwa, Pakistan.
Deparment of Biology, University of Selcuk, Konya, Turkey.
Biomed Pharmacother. 2017 Mar;87:678-682. doi: 10.1016/j.biopha.2017.01.021. Epub 2017 Jan 12.
Diospyros lotus L. possesses different therapeutic activities such as antioxidant, anti-proliferative, anti-microbial and sedative. However, no studies on the sedative-hypnotic activity of 7-methyljuglone are reported. In the present study, we have evaluated in vivo the anxiolytic-hypnotic like effects of 7-methyljuglone in mice with open field and phenobarbitone-induced sleeping time tests. We have also assessed in silico the involvement of GABA, GABA and 5HT1 neurotransmission in its mechanism of action. The intraperitoneal administration of 7-methyljuglone (2.5-10mg/kg) reduce significantly the number of crossed lines in mice open field test and concomitantly it shown a significant activity in term of onset of sleeping time and also in its duration. Moreover, 7-methyljuglone demonstrated in silico an interesting interaction with GABA but not GABA and 5HT1binding sites. All of these results, taken together, 7-methyljuglone may be an innovative candidate for designing new pharmaceutical and therapeutic applications.
君迁子具有多种治疗活性,如抗氧化、抗增殖、抗菌和镇静作用。然而,目前尚无关于7-甲基胡桃醌镇静催眠活性的研究报道。在本研究中,我们通过旷场试验和苯巴比妥诱导的睡眠时间试验,在体内评估了7-甲基胡桃醌的抗焦虑样和催眠样作用。我们还通过计算机模拟评估了γ-氨基丁酸(GABA)、GABA和5-羟色胺1(5HT1)神经传递在其作用机制中的参与情况。腹腔注射7-甲基胡桃醌(2.5-10mg/kg)可显著减少小鼠旷场试验中的穿越线次数,同时在睡眠时间的起始和持续时间方面均显示出显著活性。此外,7-甲基胡桃醌在计算机模拟中显示出与GABA有有趣的相互作用,但与GABA和5HT1结合位点无相互作用。综合所有这些结果,7-甲基胡桃醌可能是设计新型药物和治疗应用的创新候选物。