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  3. Sedative-hypnotic like effect of 5-methoxyflavone in mice and investigation on possible mechanisms by in vivo and in silico methods

Sedative-hypnotic like effect of 5-methoxyflavone in mice and investigation on possible mechanisms by in vivo and in silico methods

  • Biomed Pharmacother. 2018 Dec;108:85-94. doi: 10.1016/j.biopha.2018.08.117.
Jaikumar Shanmugasundaram 1,  Viswanathan Subramanian 2,  Jagan S Nadipelly 3,  Parimala Kathirvelu 4,  Vijaykumar Sayeli 5,  Binoy Varghese Cheriyan 6
Affiliations

Affiliations

  • 1 Department of Pharmacology, Meenakshi Medical College & Research Institute, Meenakshi Academy of Higher Education and Research, Kanchipuram, 631552, India. Electronic address: jaiku23@rediffmail.com.
  • 2 Department of Pharmacology, Meenakshi Medical College & Research Institute, Meenakshi Academy of Higher Education and Research, Kanchipuram, 631552, India. Electronic address: visu53@hotmail.com.
  • 3 Faculty of Medicine, Department of Pharmacology, Texila American University, Georgetown, Guyana. Electronic address: jaganalwaysright@gmail.com.
  • 4 Department of Pharmacology, Meenakshi Medical College & Research Institute, Meenakshi Academy of Higher Education and Research, Kanchipuram, 631552, India. Electronic address: drparimala2004@gmail.com.
  • 5 Department of Pharmacology, Mamata Medical College, Khammam, 507002, Telangana, India. Electronic address: vijaykumarsayeli@gmail.com.
  • 6 Department of Pharmaceutical Chemistry, VISTAS, VELS school of Pharmaceutical Sciences, Chennai, 600117, Tamilnadu, India. Electronic address: lallybinoy@gmail.com.
PMID: 30218862 DOI: 10.1016/j.biopha.2018.08.117
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.

Keywords

5-methoxyflavone; Adenosine; Central nervous system; Docking; Gamma-amino butyric acid A; Sedative-hypnotic.

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