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机构地区:[1]贵州大学药学院,贵州贵阳 [2]贵州习酒集团有限公司,贵州习水
出 处:《药物化学》2017年第2期24-29,共6页Hans Journal of Medicinal Chemistry
基 金:贵州省社会发展科技攻关项目(SY字[2013]3058号);贵大(国)创字20(022);国家自然科学基金(81460531)。
摘 要:血栓性疾病已成为人类疾病死亡的主要原因,微生物是抗血栓药物的主要来源之一,从微生物发酵产物中发现安全有效的新型溶血栓药物具有重要价值。本试验分别采用化学方法和小鼠模型,研究了类短短芽孢杆菌YZC01株发酵产物的溶血栓组分和体内溶血栓活性。结果表明YZC01株发酵产物溶血栓活性组分含糖基环肽类化合物,当剂量为10 mg/kg时,溶血栓活性组分具有延长小鼠断尾出血时间和溶血栓作用,但是体外抗血小板凝集的活性并不明显,推测其作用机制与阻断凝血因子受体有关。Thrombotic disorders have been emerged to be the main causes of human mortality. Now microbes are one of the main sources of antithrombotic drugs. Therefore, it is of great value to find safe and effective new type of thrombolytic drugs from microbial fermentation products. In this study, the thrombolytic components and in vivo thrombolytic activity of the fermentation products of Breviba-cillus parabrevis YZC01 were performed by us based on chemical methods and mice models respec-tively. The results showed that the crude extract of the fermentation products of YZC01 contained cyclic peptide with glycosylation structure. In mice tail bleeding time test, the extract has prolonged bleeding time in mice at dosage of 10 mg/ml. However, in in vitro assay, the activity of antiplatelet agglutination of the extract was not significant. It is indicated that the thrombolytic activity of the GYZC01 extract can be linked to blocking the coagulation factor receptor.
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