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 alpha-methylen-gamma-butyrolactone and 2-cyclopenten-1-one. The activity shown by those Michael acceptors with a beta 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.
María
A O
AO
Departmento de Farmacologia, Universidad Nacional de San Luis, Argentina.
Wendel
G H
GH
Guardia
T
T
Guzmán
J A
JA
Pestchanker
M J
MJ
Guerreiro
E
E
Giordano
O S
OS
D000818:Animals; D003517:Cyclopentanes / Q000494:pharmacology*; D005753:Gastric Mucosa / Q000187:drug effects* / Q000473:pathology; D005765:Gastrointestinal Agents / Q000494:pharmacology*; D051381:Rats; D013276:Stomach Ulcer / Q000517:prevention & control; D013329:Structure-Activity Relationship
D003517:Cyclopentanes; D005765:Gastrointestinal Agents; C013905:cyclopentenone