Departamento de Análises Clínicas, Toxicológicas e Bromatológicas, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, FCFRP-USP, Av. do Café, s/n°, CEP 14040-903, Ribeirão Preto, SP, Brazil.
Biochimie. 2012 Dec;94(12):2545-58. doi: 10.1016/j.biochi.2012.07.007. Epub 2012 Jul 17.
This study reports the isolation and biochemical characterization of two different serine proteases from Bothrops pirajai snake venom, thus providing a comparative analysis of the enzymes. The isolation process consisted of three consecutive chromatographic steps (Sephacryl S-200, Benzamidine Sepharose and C2/C18), resulting in two serine proteases, named BpirSP27 and BpirSP41 after their molecular masses by mass spectrometry (27,121 and 40,639 Da, respectively). Estimation by SDS-PAGE under denaturing conditions showed that, when deglycosylated with PNGase F, BpirSP27 and BpirSP41 had their molecular masses reduced by approximately 15 and 42%, respectively. Both are acidic enzymes, with pI of approximately 4.7 for BpirSP27 and 3.7 for BpirSP41, and their N-terminal amino acid sequences showed 57% identity to each other, with high similarity to the sequences of other snake venom serine proteases (SVSPs). The enzymes showed different actions on bovine fibrinogen, with BpirSP27 acting preferentially on the Bβ chain and BpirSP41 on both Aα and Bβ chains. The two serine proteases were also able to degrade fibrin and blood clots in vitro depending on the doses and incubation periods, with higher results for BpirSP41. Both enzymes coagulated the human plasma in a dose-dependent manner, and BpirSP41 showed a higher coagulant potential, with minimum coagulant dose (MCD) of ∼3.5 μg versus 20 μg for BpirSP27. The enzymes were capable of hydrolyzing different chromogenic substrates, including S-2238 for thrombin-like enzymes, but only BpirSP27 acted on the substrate S-2251 for plasmin. They also showed high stability against variations of temperature and pH, but their activities were significantly reduced after preincubation with Cu(2+) ion and specific serine protease inhibitors. In addition, BpirSP27 induced aggregation of washed platelets to a greater extent than BpirSP41. The results showed significant structural and functional differences between B. pirajai serine proteases, providing interesting insights into the structure-function relationship of SVSPs.
本研究报告了从矛头蝮蛇毒液中分离和生化表征两种不同的丝氨酸蛋白酶,从而对这些酶进行了比较分析。分离过程包括三个连续的色谱步骤(Sephacryl S-200、苯甲脒琼脂糖和 C2/C18),得到两种丝氨酸蛋白酶,分别命名为 BpirSP27 和 BpirSP41,根据质谱法(分别为 27,121 和 40,639 Da)确定其分子量。SDS-PAGE 估计结果表明,经 PNGase F 去糖基化后,BpirSP27 和 BpirSP41 的分子量分别减少了约 15%和 42%。两种酶均为酸性酶,BpirSP27 的等电点约为 4.7,BpirSP41 的等电点约为 3.7,其 N 端氨基酸序列彼此间有 57%的同源性,与其他蛇毒丝氨酸蛋白酶(SVSPs)的序列高度相似。两种酶对牛纤维蛋白原的作用不同,BpirSP27 优先作用于 Bβ 链,BpirSP41 则同时作用于 Aα 和 Bβ 链。两种丝氨酸蛋白酶还能在体外降解纤维蛋白和血凝块,取决于剂量和孵育时间,BpirSP41 的效果更高。两种酶均能以剂量依赖的方式凝固人血浆,BpirSP41 表现出更高的凝固潜能,最低凝固剂量(MCD)约为 3.5μg,而 BpirSP27 则为 20μg。两种酶均能水解不同的显色底物,包括类似凝血酶的 S-2238,但只有 BpirSP27 作用于 S-2251 作为纤溶酶的底物。它们对温度和 pH 的变化也具有较高的稳定性,但在与 Cu(2+)离子和特定的丝氨酸蛋白酶抑制剂预孵育后,其活性显著降低。此外,BpirSP27 诱导洗涤血小板聚集的程度大于 BpirSP41。研究结果表明,B. 矛头蝮蛇丝氨酸蛋白酶在结构和功能上存在显著差异,为 SVSP 的结构-功能关系提供了有趣的见解。