ANTIFLAMMINS - 2 NONAPEPTIDE FRAGMENTS OF UTEROGLOBIN AND LIPOCORTIN-I HAVE NO PHOSPHOLIPASE-A2-INHIBITORY AND ANTIINFLAMMATORY ACTIVITY

被引：37

作者：

MARKI, F

PFEILSCHIFTER, J

RINK, H

WIESENBERG, I

机构：

[1] Research Department, Pharmaceuticals Division, Ciba-Geigy Ltd

来源：

FEBS LETTERS | 1990年 / 264卷 / 02期

关键词：

Eicosanoid; Inflammation; Lipocortin; Nonapeptide; Phospholipase A[!sub]2[!/sub; Uteroglobin;

D O I：

10.1016/0014-5793(90)80241-A

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The 'antiflammin' nonapeptides P1 and P2 [(1988) Nature 335, 726-730] were synthesized and tested for inhibition of phospholipase A2 and release of prostaglandin E2, and leukotriene C4 in stimulated cells in vitro, and in vivo for anti-inflammatory activity in rats with carrageenan-induced paw oedema. Porcine pancreatic phospholipase A2, was not inhibited at concentrations of 0.5-50 μM. Prostaglandin E2, and leukotriene C4 release by mouse macrophages stimulated with zymosan or ATP was not affected up to a concentration of 10 μm, nor was prostaglandin release by interleukin 1β-stimulated mesangial cells and angiotensin II-stimulated smooth muscle cells. Both peptides exhibited no anti-inflammatory activity in carrageenan-induced rat paw oedema after topical (250 μg/paw) or systemic administration (1 or 4 mg kg s.c.). These results do not support the claim of potent phospholipase A2-inhibitory and anti-imflammatory activity of the 'antiflammins' P1 and P2 [1]. © 1990.

引用

页码：171 / 175

页数：5

共 26 条

[1] LIPOCORTIN INHIBITION OF EXTRACELLULAR AND INTRACELLULAR PHOSPHOLIPASES-A2 IS SUBSTRATE CONCENTRATION DEPENDENT [J].