ANTIFLAMMIN-2 (HDMNKVLDL) DOES NOT INHIBIT PHOSPHOLIPASE-A2 ACTIVITIES

被引：23

作者：

HOPE, WC ^{[1
]}

PATEL, BJ ^{[1
]}

BOLIN, DR ^{[1
]}

机构：

[1] HOFFMANN LA ROCHE INC,DEPT PEPTIDE RES,NUTLEY,NJ 07110

来源：

AGENTS AND ACTIONS | 1991年 / 34卷 / 1-2期

关键词：

D O I：

10.1007/BF01993243

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A basic nonapeptide P2 (antiflammin-2, HDMNKVLDL) which is identical to a portion of the amino acid sequence (residues 246-254) of lipocortin I, has been described to have antiinflammatory activity in a rat paw edema model (Nature 335: 726-730 [1988]). P2 (0.05-mu-M) was also reported to inhibit porcine pancreatic phospholipase A2 (PLA2). The effect of synthetic P2 (98% pure) on PLA2 was evaluated in two assay systems. Using porcine pancreatic PLA2 and phosphatidylcholine/deoxycholate mixed micellar substrate, P2 (0.005-50-mu-M) had no effect on PLA2 activity, even in the presence of 2-mercaptoethanol to prevent peptide oxidation. In another assay, using human synovial fluid PLA2 as the enzyme and [14-C]-oleate-labelled E. coli substrate, P2 (0.005-50-mu-M) had no significant effect on PLA2 activity. A reported PLA2 inhibitor, manoalide, was a potent inhibitor of PLA2 in both assay systems. On the basis of these results, we conclude that P2 is devoid of PLA2 inhibitory activity.

引用

页码：77 / 80

页数：4

共 9 条

[1] ANTIINFLAMMATORY PEPTIDES (ANTIFLAMMINS) INHIBIT SYNTHESIS OF PLATELET-ACTIVATING FACTOR, NEUTROPHIL AGGREGATION AND CHEMOTAXIS, AND INTRADERMAL INFLAMMATORY REACTIONS [J].