期刊
BIOMEDICINE & PHARMACOTHERAPY
卷 88, 期 -, 页码 109-113出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.biopha.2017.01.043
关键词
Dimeric napthoquione; Sedative-hypnotic effect; Molecular docking
资金
- institute of Scientific Research and Revival of Islamic Heritage at Umm Al-Qura University [43410009]
- Fundacio'n Se'neca-Agencia de Ciencia y Tecnologi'a de la Regio'n de Murcia [18946/JLI/13, 19419/PI/14-1]
- Centro de Alto Rendimiento de la Region de Murcia [CFE-CAR-23/15]
- European Regional Development Fund (ERDF)
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 GABAA. 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 GABAA. Conclusions: Results from this investigation reveal that compound 1 possesses sedative-hypnotic-like properties which can be of interest in therapeutic research. (C) 2017 Elsevier Masson SAS. All rights reserved.
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