Laboratorio de Inmunoquímica y Ultraestructura, Instituto Anatómico de la Universidad Central de Venezuela, Caracas, Venezuela.
Arch Toxicol. 2013 Jan;87(1):197-208. doi: 10.1007/s00204-012-0914-3. Epub 2012 Aug 25.
Colombienases are acidic, low molecular weight metalloproteinases (Mr of 23,074.31 Da colombienase-1 and 23,078.80 Da colombienase-2; pI of 6.0 and 6.2, respectively) isolated from Bothrops colombiensis snake venom. The chromatographic profile in RP-HPLC and its partial sequence confirmed its high homogeneity. Both colombienases present fibrino(geno)lytic activity, but did not show any hemorrhagic, amidolytic, plasminogen activator or coagulant activities, and no effect on platelet aggregation induced by collagen or ADP. Both enzymes were strongly active on fibrinogen Aα chains followed by the Bβ chains, and colombienases-2, at high doses, also degraded the γ chains. This activity was stable at temperatures ranging between 4 and 37 °C, with a maximum activity at 25 °C, and at pHs between 7 and 9. The homology demonstrated by the comparison of sequences, with zinc-dependent metalloproteinases, as well as the metal chelant effects on, confirmed that the colombienases were metalloproteinases, particularly to α-fibrinogenases belonging to the P-I class of SVPMs (20-30 kDa), which contain only the single-domain proteins. The biological characteristics of the colombienases confer a therapeutic potential, since they contain a high fibrino(geno)lytic activity, devoid of hemorrhagic activity. These metalloproteinases might be explored as thrombolytic agents given that they dissolve fibrin clots or prevent their formation.
哥伦比亚酶是从矛头蝮蛇(Bothrops colombiensis)蛇毒中分离得到的酸性、低分子量金属蛋白酶(Mr 分别为 23074.31 Da 的哥伦比亚酶-1 和 23078.80 Da 的哥伦比亚酶-2;pI 分别为 6.0 和 6.2)。RP-HPLC 的色谱图谱及其部分序列证实了其高度均一性。两种哥伦比亚酶均具有纤维蛋白(原)溶解活性,但不具有任何出血、氨肽酶、纤溶酶原激活剂或凝血活性,也不影响胶原或 ADP 诱导的血小板聚集。两种酶对纤维蛋白原 Aα链具有强烈的活性,其次是 Bβ链,并且在高剂量下,哥伦比亚酶-2 也降解 γ链。该活性在 4 至 37°C 的温度范围内稳定,在 25°C 时具有最大活性,在 pH 值为 7 至 9 之间稳定。序列比较显示的同源性、锌依赖性金属蛋白酶以及金属螯合剂对其的影响证实,哥伦比亚酶是金属蛋白酶,特别是属于 SVPMs(20-30 kDa)的 P-I 类 α-纤维蛋白溶酶,它们只含有单一结构域的蛋白质。哥伦比亚酶的生物学特性赋予了其治疗潜力,因为它们具有高纤维蛋白(原)溶解活性而没有出血活性。这些金属蛋白酶可以作为溶栓剂进行探索,因为它们可以溶解纤维蛋白凝块或阻止其形成。