Gastric Cytoprotective Activity of 2-Cyclopenten-1-one and Related Compounds

The cytoprotective activity of the isolated functional groups of several sesquiterpene lactones is reported. Among them the highest activity is shown by α-methylen-γ-butyrolactone and 2-cyclopenten-1-one. The activity shown by those Michael acceptors with a β carbon hindered by an alkyl substituent...

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Veröffentlicht in:	Biological & pharmaceutical bulletin 1995/12/15, Vol.18(12), pp.1784-1786
Hauptverfasser:	MARIA, Alejandra O., WENDEL, Graciela H., GUARDIA, Teresita, GUZMAN, Jorge A., PESTCHANKER, Mauricio J., GUERREIRO, Eduardo, GIORDANO, Oscar S.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Cyclopentanes - pharmacology cytoprotection Digestive system Gastric Mucosa - drug effects Gastric Mucosa - pathology Gastrointestinal Agents - pharmacology Medical sciences Michael acceptor Pharmacology. Drug treatments Rats reduced glutathione Stomach Ulcer - prevention & control Structure-Activity Relationship
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Zusammenfassung:	The cytoprotective activity of the isolated functional groups of several sesquiterpene lactones is reported. Among them the highest activity is shown by α-methylen-γ-butyrolactone and 2-cyclopenten-1-one. The activity shown by those Michael acceptors with a β carbon hindered by an alkyl substituent was always lower or almost null. A three-way mechanism of action is proposed : a) reduced glutathione synthesis, b) prostaglandin synthesis and c) mucosal glycoprotein synthesis.
ISSN:	0918-6158 1347-5215
DOI:	10.1248/bpb.18.1784