A new anti-fibrinolytic hemostatic compound 8-O-acetyl shanzhiside methylester extracted from Lamiophlomis rotata
A new anti-fibrinolytic hemostatic compound 8-O-acetyl shanzhiside methylester extracted from Lamiophlomis rotata
复制标题
从轮叶草中提取的新型抗纤溶止血化合物8-O-乙酰山栀苷甲酯。
DOI：
10.1016/j.jep.2016.04.016
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发表时间：
2016-07-01
影响因子：
5.4
通讯作者：
Jia, Zheng-Ping
中科院分区：
文献类型：
--
作者：
Fan, Peng-Cheng;Ma, Hui-Ping;Jia, Zheng-Ping
背景：纤溶作用可防止血栓的生长和形成问题。抗纤溶药物被用作纤溶的抑制剂。在确定了主要副作用，特别是对肾脏的副作用后，抑肽酶被怀疑。赖氨酸类似物有其自身的缺陷，它们是否是抑肽酶的适当替代品仍存在疑问。轮纹毒蛾Lamiophlomis roata(Bth.)工藤。先前发现有止血活性。目的：寻找罗汉果中的主要止血成分，确定其止血机制。方法：采用小鼠创伤出血模型，观察药物治疗组和对照组小鼠及血小板的凝血活性。采用小鼠静脉注射尿激酶法建立纤溶亢进模型。测定毛细血管凝血时间、活化部分凝血活酶时间、凝血酶原时间、凝血酶原时间、纤维蛋白原和优球蛋白溶解时间。结果：L提取物中环烯醚苷含量最高的环烯醚苷类化合物8-O-乙酰山枝苷甲酯具有抗纤溶活性。ASM能显著缩短CBCT(P<；0.05)，减少体内失血量，但对小鼠APTT、PT或TT无明显影响。特别是，它显著延长了纤溶亢进小鼠的ECLT。提示ASM具有抑制纤溶作用。对纤溶亢进小鼠的CBCT、创伤性出血量及ECLT也有一定的抑制作用。结论：丹参是L的主要止血成分。其止血机制是通过抗纤溶作用实现的。ASM是一种新型的纤溶抑制剂，是一种环烯醚苷类化合物。(C)2016爱思唯尔爱尔兰有限公司。保留所有权利。
Background: Fibrinolysis prevents blood clots from growing and becoming problematic. Antifibrinolytics are used as inhibitors of fibrinolysis. Aprotinin was doubted after identification of major side effects, especially on kidney. Lysine analogues has their own defects and whether they are adequate substitutes for aprotinin is still under doubt. Lamiophlomis rotata (Benth.) Kudo. was previous found to have hemostatic activity. But the active compound in L. rotata and its hemostatic mechanism were unknown.Objectives: To find the major hemostatic compound in L. rotata and identify its haemostasis mechanism.Methods: Traumatic hemorrhage model and coagulant activity assays were monitored in mice and platelets in drug treatment group and control group. Hyperfibrinolysis model was established by intravenous administration of urokinase in mice. Capillary blood clotting time (CBCT), activated partial thromboplastin time (APTT), prothrombin time (PT), thrombin time (TT), fibrinogen and euglobulin clot lysis time (ECLT) were measured.Results: The anti-fibrinolytic activity come from 8-O-Acetyl shanzhiside methylester (ASM) one of the highest iridoid glycosides contents in TIG extracted from L rotata. ASM significantly (P < 0.05) shorten CBCT and reduced blood loss volume in vivo, but did not influence mice APTT, PT or TT. In particular, it significantly prolonged ECLT in hyperfibrinolysis mice. It indicated that ASM could inhibit fibrinolysis. ASM was also effective in CBCT, traumatic bleeding volume and ECLT in hyperfibrinolysis mice model.Conclusions: ASM was the major hemostatic compound in L rotata. The haemostasis mechanism of ASM was achieved by anti-fibrinolytic activity. ASM was a new fibrinolysis inhibitor as iridoid glycoside compound. (C) 2016 Elsevier Ireland Ltd. All rights reserved.