Assessment of Sedative Activity of Lonicerin: In Vivo Approach With Pharmacokinetics and Molecular Docking.

BACKGROUND

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.

MATERIALS AND

METHODS

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 (GABAA 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.

RESULTS

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 GABAA receptor. Computational toxicity analysis revealed that LON is non-hepatotoxic, non-neurotoxic, noncarcinogenic, noncytotoxic, non-ecotoxic, and non-mutagenic.

CONCLUSION

Therefore, LON may be effective for the treatment of insomnia in the near future.