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Anti-thrombotic activity and chemical characterization of steroidal saponins from Dioscorea zingiberensis CH Wright

机译:盾叶薯os甾体皂苷的抗血栓形成活性和化学表征

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Steroidal saponins have long attracted scientific attention, due to their structural diversity and significant biological activities. Total steroidal saponins (TSS) extracted from the rhizomes of Dioscorea zingiberensis C.H. Wright (DZW) constitute an effective treatment for cardiovascular disease. However, the active constituents contained in DZW rhizomes and their pharmacological properties are not fully understood. The aim of this work is to determine and quantify the active constituents in DZW rhizomes using fingerprint technique, and evaluate its anti-thrombotic activity using inferior vena cava ligation thrombosis rat model and pulmonary thrombosis mice model after being gavaged with TSS for 1 or 2 weeks. In the study, a chemical fingerprint method was firstly established and validated to quantify and standardize TSS from DZW rhizomes including parvifloside, protodeltonin, protodioscin, protogracillin, zingiberensis saponin, deltonin, dioscin and trillin. TSS extracted from DZW rhizomes were showed to have the inhibitions on platelet aggregation (PAG) and thrombosis, and prolong activated partial thromboplastin time (APTT), thrombin time (TT), and prothrombin time (PT) in a dose-dependent manner in rats. TSS also prolonged the bleeding time and clotting time in a dose-dependent manner in mice. The results indicate that TSS could inhibit thrombosis by both improving the anticoagulation activity and inhibiting PAG action, suggesting that TSS from DZW rhizomes have the potential to reduce the risk of cardiovascular diseases by anti-thrombotic action
机译:甾体皂苷由于其结构多样性和重要的生物活性而长期以来一直引起科学关注。从盾叶薯os的根茎中提取的总甾体皂苷(TSS)。赖特(DZW)构成了治疗心血管疾病的有效方法。但是,DZW根茎中所含的活性成分及其药理特性尚未得到充分了解。这项工作的目的是使用指纹技术确定和定量DZW根茎中的活性成分,并在下颌静脉结扎血栓形成大鼠模型和肺血栓形成小鼠模型对TSS灌胃1或2周后评估其抗血栓形成活性。在这项研究中,首先建立并验证了一种化学指纹方法,用于量化和标准化DZW根茎中TSS的含量,其中包括小白菊甙,原降钙素,原二薯cin素,原草素,姜黄皂苷,降钙素,薯os皂甙和三氢紫苏苷。从DZW根茎提取的TSS对大鼠的血小板聚集(PAG)和血栓形成具有抑制作用,并且以剂量依赖的方式延长大鼠部分凝血活酶时间(APTT),凝血酶时间(TT)和凝血酶原时间(PT)的活化。 TSS还以剂量依赖性方式延长了小鼠的出血时间和凝血时间。结果表明,TSS可以通过提高抗凝活性和抑制PAG活性来抑制血栓形成,表明DZW根茎中的TSS可以通过抗血栓作用降低心血管疾病的风险

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