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Article ; Online: Sedative-hypnotic effect and in silico study of dinaphthodiospyrols isolated from Diospyros lotus Linn.

Al-Awthan, Yahya S / Rauf, Abdur / Rashid, Umer / Bawazeer, Sami / Naz, Saima / Bahattab, Omar / Bawazeer, Saud / Muhammad, Naveed / Waggas, Dania Saad / Batiha, Gaber El-Saber / Shariati, Mohammad Ali / Derkho, Marina / Suleria, Hafiz Ansar Rasul

Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie

2021  Volume 140, Page(s) 111745

Abstract: Traditionally, Diospyros lotus Linn is used for insomnia and other associated disorders. Insomnia is a worldwide disorder with different etiology which is treated with different synthetic medicine associated with addiction. Natural products are generally ...

Abstract Traditionally, Diospyros lotus Linn is used for insomnia and other associated disorders. Insomnia is a worldwide disorder with different etiology which is treated with different synthetic medicine associated with addiction. Natural products are generally devoid of such addition with good efficacy. Current research was conducted to evaluate the sedative and hypnotic effects of dimeric naphthoquinones such as dinaphthodiospyrol A (1), dinaphthodiospyrol B (2), dinaphthodiospyrol C (3), dinaphthodiospyrol D (4), dinaphthodiospyrol E (5) and dinaphthodiospyrol F (6) isolated from the chloroform fractions of D. lotus. The sedative and hypnotic effects at the dose of 5 and 10 mg/kg (each compound) were assessed through open field and phenobarbital induced sleep test, respectively. In the case of open field test the administration of tested compounds significantly hindered the movement of animals, while in case of hypnotic effect the tested samples significantly improved the onset and duration of sleep as compared to control. The overall effects were in a dose dependent manner. The compounds were also assessed for acute toxicity, but no toxicity was observed. In this regard, our research triumphantly announced the strong chemical base for the folkloric values of the plant with their fringe benefits and implemented a platform for further aspects of mechanistic and clinical studies. A possible mechanism of in vivo inhibition was studied by using docking simulations on GABA receptors. Binding orientations and types of interactions revealed that a possible mechanism behind these pharmacological actions might be interaction with GABA receptors.
MeSH term(s) Animals ; Diospyros ; Female ; Hypnotics and Sedatives/pharmacology ; Hypnotics and Sedatives/toxicity ; Male ; Mice ; Molecular Docking Simulation ; Naphthoquinones/pharmacology ; Naphthoquinones/toxicity ; Plant Roots ; Receptors, GABA/metabolism ; Sleep/drug effects
Chemical Substances Hypnotics and Sedatives ; Naphthoquinones ; Receptors, GABA
Language English
Publishing date 2021-05-19
Publishing country France
Document type Journal Article
ZDB-ID 392415-4
ISSN 1950-6007 ; 0753-3322 ; 0300-0893
ISSN (online) 1950-6007
ISSN 0753-3322 ; 0300-0893
DOI 10.1016/j.biopha.2021.111745
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