Biological aggregates play a crucial role in the pathogenesis of thrombotic diseases, especially thrombin-induced biological aggregates. Therefore, the efficient discovery of thrombin inhibitors is of great significance for the prevention and treatment of thrombotic diseases. In this study, the aggregation precursor protein fluorescent probe was successfully prepared for monitoring the production of biological aggregates induced by thrombin. In this program, the aggregation degree of biomolecules can be quickly monitored through a fluorescence sensing technology. To facilitate the modulation of the biological aggregation process, the application of this advanced fluorescence sensing technology was utilized for the screening of thrombin inhibitors, which are pivotal regulatory molecules in biological aggregation. In addition, by combining the target fishing technique, an integrated model for rapid screening of potential inhibitors in complex extracts was further established. This model not only swiftly detects the presence of inhibitory components within complex systems but also precisely captures and identifies active monomers. After positive drug validation of the screening model, three active monomers, namely, ginkgetin, isoginkgetin, and bilobetin, were accurately screened from 30 natural products. These results highlighted the immense potential of the proposed approach for screening active ingredients from a wide range of natural products.
Junxia Yu,Huantong Su,Shuda Wei,Fangping Chen,Changsheng Liu
Blood coagulates are closely related to calcium ions (coagulation factor IV), and calcium-doped biomaterials have been reported to be effective in hemostasis. However, the effects exerted by calcium on hemostatic agents have not been previously investigated. The aims of this work were to develop calcium-modified oxidized microporous starch (CaOMS) with controllable calcium contents and to explore the relationship between calcium content and hemostatic effects. The results showed that low calcium content promoted coagulation, while high calcium content inhibited coagulation. CaOMS3 with 2.2 mg/g calcium content was optimal because of its excellent water absorption performance that enhanced physical coagulation, the rapid initiation of coagulation cascade reactions, and the enhanced chemical coagulation by RBC aggregation and platelet activation. The synergistic effects of chemical activation and physical absorption endowed CaOMS with the potential to control internal organ bleeding. These results suggested that CaOMS may be a promising hemostatic agent with wide spread applications.
危险品化学品经营许可证（带存储）