Abstract
The effects of 1'S-1'-acetoxychavicol acetate and related phenylpropanoids isolated from the rhizomes of Alpinia galanga on ethanol-induced gastric lesions in rats were examined. Among them, 1'S-1'-acetoxychavicol acetate and 1'S-1'-acetoxyeugenol acetate markedly inhibited the ethanol-induced gastric mucosal lesions (ED(50)=0.61 and ca. 0.90 mg/kg). In addition, 1'S-1'-acetoxychavicol acetate inhibited the lesions induced by 0.6 M HCl (ED(50)=0.73 mg/kg) and aspirin (ED(50)=0.69 mg/kg) but it did not show a significant effect on indomethacin-induced gastric lesions and acid output in pylorus-ligated rats at doses of 0.5-5.0 mg/kg. From the gastroprotective effects of various related compounds, the 1'-acetoxyl group of 1'S-1'-acetoxychavicol acetate and 1'S-1'-acetoxyeugenol acetate was found to be essential for their strong activity. With regard to the mode of action, the gastroprotective effects of 1'S-1'-acetoxychavicol acetate were attenuated by pretreatment with indomethacin and N-ethylmaleimide, and 1'S-1'-acetoxychavicol acetate significantly increased the glutathione levels of gastric mucosa in rats. These findings suggest that endogenous prostaglandins and sulfhydryl compounds are involved in the protective effect of 1'S-1'-acetoxychavicol acetate.
MeSH terms
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Administration, Oral
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Alpinia* / chemistry
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Animals
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Aspirin / administration & dosage
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Aspirin / adverse effects
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Benzyl Alcohols
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Drugs, Chinese Herbal / pharmacology
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Ethanol / administration & dosage
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Ethanol / adverse effects
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Ethylmaleimide / administration & dosage
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Ethylmaleimide / pharmacokinetics
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Gastric Mucosa / drug effects
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Gastric Mucosa / metabolism
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Gastric Mucosa / pathology
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Gastrointestinal Agents / pharmacology
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Gastrointestinal Agents / therapeutic use*
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Indomethacin / administration & dosage
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Indomethacin / adverse effects
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Injections, Intraperitoneal
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Injections, Subcutaneous*
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Male
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Molecular Structure
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NG-Nitroarginine Methyl Ester / administration & dosage
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NG-Nitroarginine Methyl Ester / pharmacokinetics
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NG-Nitroarginine Methyl Ester / therapeutic use
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Peptic Ulcer / chemically induced
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Peptic Ulcer / drug therapy
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Phenylpropionates / chemistry
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Phenylpropionates / pharmacology
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Phenylpropionates / therapeutic use*
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Phytotherapy*
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Plant Extracts / pharmacology*
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Rats
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Rats, Sprague-Dawley
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Rhizome / chemistry*
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Structure-Activity Relationship
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Terpenes / administration & dosage
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Terpenes / pharmacokinetics
Substances
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Benzyl Alcohols
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Drugs, Chinese Herbal
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Gastrointestinal Agents
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Phenylpropionates
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Plant Extracts
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Terpenes
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Ethanol
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Ethylmaleimide
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Aspirin
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1'-acetoxychavicol acetate
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NG-Nitroarginine Methyl Ester
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Indomethacin