Sedative-hypnotic-like effect and molecular docking of di-naphthodiospyrol from Diospyros lotus in an animal model - 13/03/17
, Taibi Ben Hadda b, Ghias Uddin c, José P. Cerón-Carrasco d, Jorge Peña-García d, Horacio Pérez-Sánchez d, Haroon Khan e, Saud Bawazeer f, Seema Patel g, Mohammad S. Mubarak h, ⁎ , Tareq Abu-Izneid f, Yahia Nasser Mabkhot iBienvenue sur EM-consulte, la référence des professionnels de santé.
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Graphical abstract |
Graphical abstract showing the sedative-hypnotic like effect and molecular docking of Di-naphthodiospyrol from Diospyros lotus root extract in animal model.
Abstract |
Background |
Diospyros lotus Linn commonly known as date-plum, or Caucasian persimmon has multiple uses in folk medicine. Various parts of this plant is used for alleviating lumbago, dysponea, hemorrhage, insomnia, and hiccup. The plant extracts possess a variety of biological activities, such as anti-inflammatory, sedative, febrifuge, anti-microbial, vermifuge, and anti-hypertensive.
Aim/hypothesis |
The aim of the present work is to investigate the sedative-hypnotic effect of a rare dimeric napthoquione 1 obtained from the chloroform soluble fraction of D. lotus extracts.
Methods |
Compound 1 , di-naphthodiospyrol at 5, 10, and 15 mg/kg intraperitoneal doses was assessed for its in vivo sedative effect in an open-field using a phenobarbitone-induced sleeping time model. The geometry of di-naphthodiospyrol was also optimized with the aid of density functional theory. In addition, molecular docking of compound 1 was performed with the receptor GABA A .
Results |
The animal protocol-based assay showed significant sedative-hypnotic-like effects of compound 1 at various test doses (5, 10, and 15 mg/kg i.p.). Docking studies indicated that this compound interacts strongly with important residues in receptor GABA A .
Conclusions |
Results from this investigation reveal that compound 1 possesses sedative-hypnotic- like properties which can be of interest in therapeutic research.
Le texte complet de cet article est disponible en PDF.Abbreviations : TLC, S.E.M., DFT, PDB, GABA A
Keywords : Dimeric napthoquione, Sedative-hypnotic effect, Molecular docking
Plan
Vol 88
P. 109-113 - avril 2017 Retour au numéro
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