van Binsbergen J, Slotboom A J, Aarsman A J, de Haas G H
Centre for Biomembranes and Lipid Enzymology, Utrecht, The Netherlands.
FEBS Lett. 1989 Apr 24;247(2):293-7. doi: 10.1016/0014-5793(89)81355-9.
Two anti-inflammatory peptides corresponding to a high amino acid similarity region between lipocortins were synthesized and tested on their ability to inhibit porcine pancreatic phospholipase A2. Kinetic assays using monomeric and aggregated phospholipids did not reveal any phospholipase A2 inhibitory activity. The peptides did not inhibit phospholipase A2 activity on monolayers of negatively charged substrate and did not prevent phospholipase A2 action on mixed micelles of 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine and sodiumdeoxycholate. Ultraviolet difference spectroscopy did not show binding of the peptides to phospholipase A2. Therefore we conclude that these anti-inflammatory peptides do not inhibit pancreatic phospholipase A2 in vitro, in contrast to the results recently published [(1988) Nature 335, 726-730].
合成了两种与脂皮质素之间高氨基酸相似性区域相对应的抗炎肽,并测试了它们抑制猪胰磷脂酶A2的能力。使用单体和聚集磷脂的动力学分析未显示出任何磷脂酶A2抑制活性。这些肽在带负电荷底物的单层上不抑制磷脂酶A2活性,也不能阻止磷脂酶A2对1-硬脂酰-2-花生四烯酰-sn-甘油-3-磷酸胆碱和脱氧胆酸钠混合胶束的作用。紫外差示光谱未显示肽与磷脂酶A2的结合。因此,我们得出结论,与最近发表的结果[(1988) Nature 335, 726 - 730]相反,这些抗炎肽在体外不抑制胰磷脂酶A2。