Anti-nociceptive,anti-inflammatory and sedative activities of the extracts and chemical constituents of Diospyros lotus L. |
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| Affiliation: | 1. Institute of Chemical Sciences, University of Peshawar, Peshawar 25120, KPK, Pakistan;2. Department of Pharmacy, Abdul Wali Khan University, Mardan, Pakistan;3. H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan;1. University Teaching Department, Sarguja University, Amibakpur, Chhattisgarh, India;2. Columbia Institute of Pharmacy, Village Tekari, Raipur, Chhattisgarh, India;3. Indian Institute of Integrative Medicine, Jammu, Jammu and Kashmir, India;4. University Institute of Pharmacy, Pt. Ravishankar Shukla University, Raipur, Chhattisgarh, India;1. Pharmacognosy Department, National Research Centre, Dokki, Giza, Egypt;2. Institute for Biological Research “Siniša Stanković”, University of Belgrade, Blvd. Despota Stefana 142, 11000 Belgrade, Serbia;1. Institute of Chemical Sciences, University of Peshawar, Peshawar 25120, KPK, Pakistan;2. H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan;3. Department of Pharmacy, Abdul Wali Khan University, Mardan 23200, Pakistan;4. Computational Medicinal Chemistry Laboratory, Department of Biochemistry, Abdul Wali Khan University Mardan, Mardan 23200, Pakistan;1. Department of Organic Chemistry, Faculty of Sciences, P.O. Box 187, University of Toliara, 601 Toliara, Madagascar;2. Malagasy Institute of Applied Research, Avarabohitra Itaosy lot AVB 77, P. O. BOX 3833, 102 Antananarivo, Madagascar;3. Antananarivo Poly-technique High School, University of Antananarivo, 101 Antananarivo, Madagascar;4. Department of Organic Chemistry, Faculty of Sciences, P.O. Box 906 University of Antananarivo, 101 Antananarivo, Madagascar;5. Institute of Natural Products Chemistry, National Centre for Scientific Research CNRS 91198, Gif Sur Yvette-Paris, France;6. Department of Biology, Faculty of Science, University of Kinshasa, P.O. BOX 190 Kinshasa XI, Democratic Republic of the Congo;1. Department of Geology, University of Swabi, Anbar, K.P.K 23561, Pakistan;2. Institute of Chemical Sciences, University of Peshawar, Peshawar, KP 25120, Pakistan;3. H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan;4. Department of Pharmacy, Abdul Wali Khan University, Mardan 23200, Pakistan;5. Department of Pharmacy, Sarhad University of Science & Information Technology (SUIT), Peshawar, Pakistan;6. LCM Laboratory, University of Mohamed 1st, Faculty of Sciences, Oujda 60000, Morocco;7. Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia;8. Department of Chemistry, COMSATS Institute of Information Technology, Abbottabad 22060, Pakistan |
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| Abstract: | Diospyros lotus L. is traditionally used in various diseases including pain and sleep disorders. The pain and inflammation are the common problems, which are treated with various synthetic analgesic drugs, and associated the side effects. The natural products have gained significant importance over synthetic drugs. The importance of phyto-medicine the current study has been designed with the aim to investigate the analgesic and anti-inflammatory effects of Diospyros lotus and bioassay guided isolation from its crude fractions. Seven known compounds; lupeol (1), 7-methyljuglone (2), β-Sitosterol (3), stigmasterol (4) betulinic acid (5), diospyrin (6; DS) and 8-hydroxyisodiospyrin (7; HDS) which were hitherto unreported from D. lotus. The chloroform fraction (CFDL) and isolated compounds DS and HDS were evaluated for anti-nociceptive, sedative and anti-inflammatory effects. The acetic acid induced writing was significantly (p < 0.001) protected by CFDL (72.43%), DS (40.87%) and HDS (65.76%) at higher doses which exhibited peripheral and central analgesic effects in acetic acid and hot-plat pain paradigms. Regarding the anti-inflammatory effect the CFDL (77.43%), DS (80.54%) and HDS (75.87%) protected the carrageenan paw edema after 3rd h. The central analgesic effect was significantly antagonized with naloxone (0.5 mg/kg), showing opiodergic mechanism of action. The CFDL, DS and HDS were also proved sedative in open field animal models. In acute toxicity study the chloroform fraction [CFDL (50, 100 and 150 mg/kg)], DS (5 and 10 mg/kg) and HDS (5 and 10 mg/kg) were found safe.Our study concluded that CFDL, DS and HDS have marked anti-nociceptive, anti-inflammatory and sedative effect. The anti-nociceptive and anti-inflammatory effects of the roots of D. lotus are partially attributed due to the presence of analgesic constituents like diospyrin (DS), 8-hydroxyisodiospyrin (HDS) and strongly supports the ethno-pharmacological uses of D. lotus as anti-nociceptive, anti-inflammatory and sedative. |
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| Keywords: | Anti-nociceptive Anti-inflammatory Sedative activity |
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