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Gastroprotective Efficacy and Safety Evaluation of Scoparone Derivatives on Experimentally Induced Gastric Lesions in Rodents

by Dong Ju Son 1, Gyung Rak Lee 2, Sungil Oh 2, Sung Eun Lee 1,*,† and Won Sik Choi 2,*,†
1
School of Applied Bioscience, Kyungpook National University, Daegu 702-701, Korea
2
Department of Biotechnology, College of Natural Sciences, Soonchunhyang University, Asan, Chungnam 336-745, Korea
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Nutrients 2015, 7(3), 1945-1964; https://doi.org/10.3390/nu7031945
Received: 29 January 2015 / Revised: 28 February 2015 / Accepted: 3 March 2015 / Published: 13 March 2015
This study investigated the gastroprotective efficacy of synthesized scoparone derivatives on experimentally induced gastritis and their toxicological safety. Six scoparone derivatives were synthesized and screened for gastroprotective activities against HCl/ethanol- and indomethacin-induced gastric ulcers in rats. Among these compounds, 5,6,7-trimethoxycoumarin and 6,7,8-trimethoxycoumarin were found to have gastroprotective activity greater than the standard drug rebamipide; 6-methoxy-7,8-methylenedioxycoumarin, 6-methoxy-7,8-(1-methoxy)-methylenedioxycoumarin, 6,7-methylenedioxycoumarin, and 6,7-(1-methoxy)-methylenedioxycoumarin were found to be equipotent or less potent that of rebamipide. Pharmacological studies suggest that the presence of a methoxy group at position C-5 or C-8 of the scoparone’s phenyl ring significantly improves gastroprotective activity, whereas the presence of a dioxolane ring at C-6, C-7, or C-8 was found to have decreased activity. In order to assess toxicological safety, two of the potent gastroprotective scoparone derivatives—5,6,7-trimethoxycoumarin and 6,7,8-trimethoxycoumarin—were examined for their acute toxicity in mice as well as their effect on cytochrome P450 (CYP) enzyme activity. These two compounds showed low acute oral toxicity in adult male and female mice, and caused minimal changes to CYP3A4 and CYP2C9 enzyme activity. These results indicate that compared to other scoparone derivatives, 5,6,7-trimethoxycoumarin and 6,7,8-trimethoxycoumarin can improve gastroprotective effects, and they have low toxicity and minimal effects on drug-metabolizing enzymes. View Full-Text
Keywords: scoparone; 5,6,7-trimethoxycoumarin; 6,7,8-trimethoxycoumarin; gastric ulcer; peptic ulcer; gastric mucus scoparone; 5,6,7-trimethoxycoumarin; 6,7,8-trimethoxycoumarin; gastric ulcer; peptic ulcer; gastric mucus
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Son, D.J.; Lee, G.R.; Oh, S.; Lee, S.E.; Choi, W.S. Gastroprotective Efficacy and Safety Evaluation of Scoparone Derivatives on Experimentally Induced Gastric Lesions in Rodents. Nutrients 2015, 7, 1945-1964.

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