Departamento de Análises Clínicas, Toxicológicas e Bromatológicas, Faculdade de Ciências Farmacêuticas de Ribeirão Preto-USP, 14040-903 Ribeirão Preto, São Paulo, Brasil.
Toxicon. 2012 Jul;60(1):70-82. doi: 10.1016/j.toxicon.2012.03.018. Epub 2012 Mar 30.
The structures and functional activities of metalloproteinases from snake venoms have been widely studied because of the importance of these molecules in envenomation. Batroxase, which is a metalloproteinase isolated from Bothrops atrox (Pará) snake venom, was obtained by gel filtration and anion exchange chromatography. The enzyme is a single protein chain composed of 202 amino acid residues with a molecular mass of 22.9 kDa, as determined by mass spectrometry analysis, showing an isoelectric point of 7.5. The primary sequence analysis indicates that the proteinase contains a zinc ligand motif (HELGHNLGISH) and a sequence C₁₆₄ I₁₆₅M₁₆₆ motif that is associated with a "Met-turn" structure. The protein lacks N-glycosylation sites and contains seven half cystine residues, six of which are conserved as pairs to form disulfide bridges. The three-dimensional structure of Batroxase was modeled based on the crystal structure of BmooMPα-I from Bothrops moojeni. The model revealed that the zinc binding site has a high structural similarity to the binding site of other metalloproteinases. Batroxase presented weak hemorrhagic activity, with a MHD of 10 μg, and was able to hydrolyze extracellular matrix components, such as type IV collagen and fibronectin. The toxin cleaves both α and β-chains of the fibrinogen molecule, and it can be inhibited by EDTA, EGTA and β-mercaptoethanol. Batroxase was able to dissolve fibrin clots independently of plasminogen activation. These results demonstrate that Batroxase is a zinc-dependent hemorrhagic metalloproteinase with fibrin(ogen)olytic and thrombolytic activity.
蛇毒中的金属蛋白酶的结构和功能活性已得到广泛研究,因为这些分子在蛇毒中毒中非常重要。从巴西矛头蝮蛇(帕拉州)蛇毒中分离得到的巴曲酶是一种金属蛋白酶,通过凝胶过滤和阴离子交换层析获得。该酶是由 202 个氨基酸残基组成的单链蛋白质,分子量为 22.9 kDa,质谱分析表明等电点为 7.5。序列分析表明,蛋白酶含有锌配体基序(HELGHNLGISH)和 C₁₆₄ I₁₆₅M₁₆₆序列基序,与“Met-turn”结构有关。该蛋白不含 N-糖基化位点,含有七个半胱氨酸残基,其中六个残基保守形成二硫键。巴曲酶的三维结构基于 Bothrops moojeni 的 BmooMPα-I 的晶体结构进行建模。该模型表明,锌结合位点与其他金属蛋白酶的结合位点具有高度的结构相似性。巴曲酶表现出较弱的出血活性,MHD 为 10 μg,能够水解细胞外基质成分,如 IV 型胶原和纤维连接蛋白。该毒素切割纤维蛋白原分子的α和β链,可被 EDTA、EGTA 和 β-巯基乙醇抑制。巴曲酶能够独立于纤溶酶原激活溶解纤维蛋白凝块。这些结果表明,巴曲酶是一种锌依赖性出血性金属蛋白酶,具有纤维蛋白(原)溶解和溶栓活性。