Abstract
Eighty percent (80%) aqueous acetone extract from fruit of Piper chaba (Piperaceae) was found to have a hepatoprotective effect on D-galactosamine (D-GalN)/lipopolysaccharide (LPS)-induced liver injury in mice. Among the isolates, several amide constituents inhibited D-GalN/tumor necrosis factor-alpha (TNF-alpha)-induced death of hepatocytes, and the following structural requirements were suggested: i) the amide moiety was essential for strong activity; ii) the 1,9-decadiene structure between the benzene ring and the amide moiety tended to enhance the activity. Moreover, a principal constituent, piperine, exhibited strong in vivo hepatoprotective effect at a dose of 5 mg/kg, p.o. and its mode of action was suggested to depend on the reduced sensitivity of hepatocytes to TNF-alpha.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Alkaloids / isolation & purification
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Alkaloids / pharmacology
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Alkaloids / therapeutic use
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Amides / chemistry
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Amides / isolation & purification*
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Amides / pharmacology*
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Amides / therapeutic use
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Animals
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Benzodioxoles / isolation & purification
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Benzodioxoles / pharmacology
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Benzodioxoles / therapeutic use
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Cells, Cultured
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Chemical and Drug Induced Liver Injury / drug therapy*
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Disease Models, Animal
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Dose-Response Relationship, Drug
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Galactosamine
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Hepatocytes / metabolism*
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Lipopolysaccharides
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Mice
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Piper / chemistry*
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Piperidines / isolation & purification
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Piperidines / pharmacology
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Piperidines / therapeutic use
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Polyunsaturated Alkamides / isolation & purification
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Polyunsaturated Alkamides / pharmacology
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Polyunsaturated Alkamides / therapeutic use
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Structure-Activity Relationship
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Tumor Necrosis Factor-alpha / metabolism*
Substances
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Alkaloids
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Amides
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Benzodioxoles
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Lipopolysaccharides
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Piperidines
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Polyunsaturated Alkamides
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Tumor Necrosis Factor-alpha
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Galactosamine
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piperine