Lindahl U, Kolset S O, Bøgwald J, Osterud B, Seljelid R
Biochem J. 1982 Aug 15;206(2):231-7. doi: 10.1042/bj2060231.
The formation and secretion of coagulation Factor X/Xa by mouse peritoneal macrophages was studied with a luminogenic peptide substrate (S-2613; t-butyloxycarbonylisoleucylglutamyl-gamma-piperidylglycylarginylisoluminol). Amidolysis was quantified by measuring the light emitted during oxidation of isoluminol, released by Factor Xa. A lower detection limit of about 0.5ng of Factor Xa was established; the assay was linear with enzyme concentration up to at least 100ng/ml. Factor X was determined after treatment with the Factor X-activating component of Russell's-viper (Vipera russelli) venom. Macrophages, cultured in the absence of serum, released Factor X/Xa into the culture medium. The concentration of coagulation enzyme in the medium increased in an essentially linear fashion over a period of at least 3 days, at a rate corresponding to 6-8ng produced/24h per 10(6) cells. The ratio of Factor Xa/X+Xa varied from about 60 to 100%, showing that activation of Factor X to Xa is not prerequisite to release of the enzyme from the cells. Factor Xa activity was suppressed in the presence of warfarin [3-(alpha-acetonylbenzyl)-4-hydroxycoumarin; 12.5mug/ml of medium], but could be restored by adding vitamin K (0.1mug/ml) along with the warfarin. Cultures to which Sepharose beads containing covalently bound anti-(Factor X) antibodies had been added showed decreased amounts of free Factor X/Xa in the culture medium. The missing activity could be demonstrated by incubating the recovered conjugate with the substrate peptide S-2613. Factor Xa produced by the macrophages was efficiently inactivated by heparin in the presence of antithrombin, heparin with high affinity for antithrombin being more effective than the corresponding low-affinity species.
利用一种发光肽底物(S-2613;叔丁氧羰基异亮氨酰谷氨酰-γ-哌啶基甘氨酰精氨酰异鲁米诺)研究了小鼠腹腔巨噬细胞凝血因子X/Xa的形成与分泌。通过测量Xa因子释放的异鲁米诺氧化过程中发出的光来定量酰胺水解。确定了约0.5ng Xa因子的较低检测限;该测定法与酶浓度呈线性关系,直至至少100ng/ml。用罗素蝰蛇(蝰蛇属)毒液的X因子激活成分处理后测定X因子。在无血清条件下培养的巨噬细胞将因子X/Xa释放到培养基中。培养基中凝血酶的浓度在至少3天的时间内基本呈线性增加,速率相当于每10⁶个细胞每24小时产生6 - 8ng。Xa因子/X + Xa因子的比例在约60%至100%之间变化,表明X因子激活为Xa因子并非该酶从细胞中释放的先决条件。在华法林[3-(α-丙酮基苄基)-4-羟基香豆素;培养基中12.5μg/ml]存在的情况下,Xa因子活性受到抑制,但通过与华法林一起添加维生素K(0.1μg/ml)可恢复。添加了共价结合抗(因子X)抗体的琼脂糖珠的培养物显示培养基中游离因子X/Xa的量减少。通过将回收的缀合物与底物肽S-2613孵育可证明缺失的活性。在抗凝血酶存在的情况下,巨噬细胞产生的Xa因子被肝素有效灭活,与抗凝血酶具有高亲和力的肝素比相应的低亲和力种类更有效。