1株诱变的枯草杆菌溶栓酶体内外溶栓性质初探

目的从一株诱变的枯草杆菌的发酵液中分离纯化得到新型溶栓酶FSC2-13，并对它的体内外溶栓性质进行初步研究。方法采用纤维蛋白平板法、加热纤维蛋白平板法和聚丙稀酰胺凝胶电泳SDS—PAGE法分别对FSC2—13体外水解纤维蛋白和纤维蛋白原进行研究，并且采用大鼠血栓形成抑制模型对其经肠道给药后的体内药效学进行初步研究。结果FSC2—13在体外能够水解纤维蛋白和纤维蛋白原，并且在纤维蛋白原三条肽链上均有水解位点。FSC2—13在经肠道给药后能够明显的抑制大鼠静脉血栓的形成，血栓形成抑制率为68％，活化的部分凝血活酶时间(APTT)延长51％，纤维蛋白原含量下降49％，纤维蛋白降解产物(FDP)含量也有明显的提高，但纤维蛋白溶酶原的含量并未有明显变化。结论FSC2—13具有体内外溶纤活性，而且方式特殊，有望开发成新一代的口服溶栓药物。

Preliminary Studies on in vitro and in vivo Thrombolytic Activities of Thrombolytic Enzyme from an Induced Bacillus subtilis Strain

Objective To separate and purify a novel thrombolytic enzyme (FSC2-13) from culture media of an induced Bacillus subtilis strain and to study its in vitro and in vivo thrombolytic activities. Methods Employed fibrin plate method, pyrogenation (heating up) fibrin plate method and SDS-PAGE were used respectively to study FSC2-13 hydrolyzing fibrin and fibrinogen in vitro. Investigations were made on its in vivo pharmacodynamics using rat thrombogenesis inhibition model after it was administrated by intestinal route. Results FSC2-13 could hydrolyze fibrin and fibrinogen in vitro and had hydrolysis sites on three peptide chains of fibrinogen. FSC2-13 could significantly inhibit the formation of rat venous thrombus after being administrated by intestinal route. Thrombogenesis inhibition rate was 68%. Activated partial thromboplastin time increased by 51%, fibrinogen content decreased by 49%, fibrin degradation product (FDP) content also increased obviously, but the plasminogen content did not change obviously. Conclusion FSC2-13 possessed in vitro and in vivo thrombolytic activities in a special way. There seem to be prospects for researches to develope it into a new generation of oral thrombolytic drug.