2-环戊烯-1-酮及相关化合物的胃细胞保护活性

Gastric cytoprotective activity of 2-cyclopenten-1-one and related compounds.

作者信息

María A O, Wendel G H, Guardia T, Guzmán J A, Pestchanker M J, Guerreiro E, Giordano O S

机构信息

Departmento de Farmacologia, Universidad Nacional de San Luis, Argentina.

出版信息

Biol Pharm Bull. 1995 Dec;18(12):1784-6. doi: 10.1248/bpb.18.1784.

DOI:10.1248/bpb.18.1784

PMID:8787809

Abstract

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.

摘要

报道了几种倍半萜内酯的分离官能团的细胞保护活性。其中，α-亚甲基-γ-丁内酯和2-环戊烯-1-酮表现出最高的活性。那些β-碳被烷基取代基阻碍的迈克尔受体所表现出的活性总是较低或几乎为零。提出了一种三方面的作用机制：a）还原型谷胱甘肽合成，b）前列腺素合成，c）粘膜糖蛋白合成。