Sedative–hypnotic like effect of 5–methoxyflavone in mice and investigation on possible mechanisms by in vivo and in silico methods - 13/11/18
, Viswanathan Subramanian a , Jagan S. Nadipelly b , Parimala Kathirvelu a , Vijaykumar Sayeli c , Binoy Varghese Cheriyan d Bienvenue sur EM-consulte, la référence des professionnels de santé.
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Graphical abstract |
Highlights |
• | A dose-dependent reduction in spontaneous locomotor activity was observed. |
• | Duration of pentobarbitone sleeping time and ether anaesthesia were prolonged. |
• | GABAA, glycine, adenosine and NMDA receptors might play a role in the above action. |
• | In silico studies supplemented the in vivo findings at the above receptor sites. |
Abstract |
Flavonoids have been shown to possess central nervous system (CNS) depressant effect mediated through the ionotropic GABAA receptors. In the present study, 5-methoxyflavone was evaluated for sedative-hypnotic like activity in mice and the mechanisms involved by employing a battery of tests including molecular docking studies. In the open field test, 5–methoxyflavone in various doses (50, 100 and 150 mg/kg, i.p) exhibited a significant and dose–dependent reduction in the spontaneous locomotor activity (F (530) = 87.17 P < 0.001). Pretreatment with 5–methoxyflavone decreased the latency to sleep induction after pentobarbitone or ether administration and also significantly increased the duration of sleep (p < 0.001). A significant and dose-dependent myorelaxant effect was observed with 5–methoxyflavone in the inclined plane, horizontal wire test and rota rod test. Pretreatment with picrotoxin, bicuculline, glycine, caffeine or NMDA either decreased or completely abolished the hypnotic effect of 5-methoxyflavone in mice. The above results revealed the involvement of GABAA, adenosine, glycine and NMDA receptors in the hypnotic effect of 5-methoxyflavone. The results of in silico studies indicated that, 5–methoxyflavone exhibits good binding affinity towards these receptors by H-bond interactions. In conclusion, the present study identified a novel and potential sedative-hypnotic like effect of 5–methoxyflavone involving multiple mechanisms.
Le texte complet de cet article est disponible en PDF.Keywords : Adenosine, Central nervous system, Docking, Gamma-amino butyric acid A, Sedative-hypnotic, 5-methoxyflavone
Plan
Vol 108
P. 85-94 - décembre 2018 Retour au numéro
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