Eity Tanzila Akter, Bhuia Md Shimul, Chowdhury Raihan, Sheikh Salehin, Ansari Siddique Akber, Ahammed Nowreen Tabassum, Kamli Hossam, Islam Muhammad Torequl
Department of Biotechnology and Genetic Engineering, Gopalganj Science and Technology University, Gopalganj, Bangladesh.
Bioinformatics and Drug Innovation Laboratory, BioLuster Research Center Ltd., Gopalganj, Bangladesh.
Brain Behav. 2025 May;15(5):e70524. doi: 10.1002/brb3.70524.
Lonicerin (LON) has been identified to have different biological properties, such as anticancer, anti-inflammatory, immunomodulatory, antibacterial, antimicrobial, and neuroprotective. This study aims to assess the sedative effect of LON in Swiss albino mice, which is yet to be discovered.
Mice were treated with two different doses of LON (5 and 10 mg/kg) and 2 mg/kg of diazepam (DZP), which is the referral GABAergic medication, and the latency time and sleeping duration of animals were observed. A computational study was also conducted to evaluate the docking scores and display the binding sites of LON and receptor (GABA α1 and β2 subunits). The study also investigated the pharmacokinetics and drug-likeness properties of LON along with toxicological analysis by using SwissADME and Protox-3 software, respectively.
Findings revealed that the higher concentration of LON reduced the latency (9.86 ± 1.44 min) and increased the sleep duration (191.29 ± 7.43 min) compared to the lower concentration. Besides, the combination group of LON and DZP showed the lowest latency (6.17 ± 0.82 min) and highest sleeping time (219.00 ± 6.39 min). In the in silico study, LON exhibited a strong docking score (-8.1 kcal/mol) with the macromolecules, which is closer to the binding affinity of DZP (-8.3 kcal/mol), indicating that LON could show strong sedative activity by binding with the GABA receptor. Computational toxicity analysis revealed that LON is non-hepatotoxic, non-neurotoxic, noncarcinogenic, noncytotoxic, non-ecotoxic, and non-mutagenic.
Therefore, LON may be effective for the treatment of insomnia in the near future.
已证实忍冬苷（LON）具有多种生物学特性，如抗癌、抗炎、免疫调节、抗菌、抗微生物和神经保护作用。本研究旨在评估LON对瑞士白化小鼠的镇静作用，该作用尚未被发现。
用两种不同剂量的LON（5和10毫克/千克）以及2毫克/千克的地西泮（DZP，一种参考性GABA能药物）对小鼠进行处理，并观察动物的潜伏期和睡眠时间。还进行了一项计算研究，以评估对接分数并展示LON与受体（GABAα1和β2亚基）的结合位点。该研究还分别使用SwissADME和Protox - 3软件研究了LON的药代动力学和类药性质以及毒理学分析。
研究结果显示，与低浓度相比，高浓度的LON缩短了潜伏期（9.86±1.44分钟）并延长了睡眠时间（191.29±7.43分钟）。此外，LON与DZP的联合组显示出最短的潜伏期（6.17±0.82分钟）和最长的睡眠时间（219.00±6.39分钟）。在计算机模拟研究中，LON与大分子显示出较强的对接分数（-8.1千卡/摩尔），这与DZP的结合亲和力（-8.3千卡/摩尔）相近，表明LON可能通过与GABA受体结合而表现出较强的镇静活性。计算毒性分析表明LON无肝毒性、无神经毒性、无致癌性、无细胞毒性、无生态毒性且无致突变性。
因此，LON在不久的将来可能对失眠治疗有效。
