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盾叶薯蓣中甾体皂苷的抗血栓活性及化学成分研究

Anti-thrombotic activity and chemical characterization of steroidal saponins from Dioscorea zingiberensis C.H. Wright.

机构信息

Institute for Nanobiomedical Technology and Membrane Biology, Laboratory of Ethnopharmacology, West China Hospital, West China Medical School, Sichuan University, No 1, Keyuan 4lu, Gaopeng Avenue, Gaoxinqu, Chengdu 610041, China.

出版信息

Fitoterapia. 2010 Dec;81(8):1147-56. doi: 10.1016/j.fitote.2010.07.016. Epub 2010 Jul 23.

DOI:10.1016/j.fitote.2010.07.016
PMID:20659537
Abstract

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 2weeks. 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.

摘要

甾体皂苷因其结构多样性和显著的生物活性而长期受到科学界的关注。从盾叶薯蓣根茎中提取的总甾体皂苷(TSS)是治疗心血管疾病的有效药物。然而,盾叶薯蓣根茎中含有的有效成分及其药理学特性尚未完全阐明。本研究旨在采用指纹图谱技术测定和定量分析盾叶薯蓣根茎中的活性成分,并通过灌胃 TSS 1 或 2 周后,采用下腔静脉结扎血栓形成大鼠模型和肺血栓形成小鼠模型来评价其抗血栓活性。在该研究中,首次建立并验证了一种化学指纹图谱方法,以定量和标准化包括偏诺皂苷、原薯蓣皂苷、原薯蓣皂苷元、原纤细薯蓣皂苷、盾叶薯蓣皂苷、deltonin、薯蓣皂苷和川陈皮素在内的盾叶薯蓣根茎中的 TSS。从盾叶薯蓣根茎中提取的 TSS 显示出对血小板聚集(PAG)和血栓形成的抑制作用,并在大鼠中呈剂量依赖性延长活化部分凝血活酶时间(APTT)、凝血酶时间(TT)和凝血酶原时间(PT)。TSS 还在小鼠中呈剂量依赖性地延长出血时间和凝血时间。结果表明,TSS 可通过改善抗凝活性和抑制 PAG 作用来抑制血栓形成,提示盾叶薯蓣根茎中的 TSS 具有通过抗血栓作用降低心血管疾病风险的潜力。

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