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反枝苋提取物及其各部位通过抗凝血、抗血小板活化和抗纤溶作用对血瘀大鼠发挥预防作用,并采用 UHPLC-qTOF-MS/MS 进行化学表征。

Lagopsis supina extract and its fractions exert prophylactic effects against blood stasis in rats via anti-coagulation, anti-platelet activation and anti-fibrinolysis and chemical characterization by UHPLC-qTOF-MS/MS.

机构信息

Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China.

Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China.

出版信息

Biomed Pharmacother. 2020 Dec;132:110899. doi: 10.1016/j.biopha.2020.110899. Epub 2020 Oct 20.

DOI:10.1016/j.biopha.2020.110899
PMID:33096352
Abstract

Lagopsis supina (Steph.) IK. -Gal. ex Knorr. has been used for centuries as an empiric treatment for blood stasis syndrome in China without scientific validation. The aim of this study was to evaluate for the first time the chemical profiling, efficacy and mechanism of L. supina ethanol extract (LS) and its four fractions (LSA∼D) in Dextran 500-induced acute blood stasis model rats. Oral administration of LS (229.0∼916.0 mg/kg) and LSC (17.6∼70.4 mg/kg) once daily for seven consecutive days significantly improved microcirculation hemodynamics function (blood flow, blood concentration and blood flow velocity), hemorheological parameters (whole blood viscosity, whole blood reduced viscosity, plasma viscosity, platelet aggregation rate, hematokrit, erythrocyte assembling index and erythrocyte deformation index), and coagulation parameters (thrombin time, prothrombin time, activated partial thromboplastin time, fibrinogen and antithrombin III). Furthermore, their markedly down-regulated thromboxane B2 and 6-keto-prostaglandin F1α levels. In addition, it significantly decreased tissue-type plasminogen activator (t-PA), urokinasetype plasminogen activator (u-PA) and plasminogen activator inhibitor-1 (PAI-1) levels, as well as PAI-1/t-PA and PAI-1/u-PA rations. In parallel, 51 chemical constituents were identified from LS based on ultra-high-performance liquid chromatography-quadrupole time-of-flight tandem mass spectrometry (UHPLC-qTOF-MS/MS), and quantitative analysis showed that the two major constituents of stachysoside A and acteoside were present in 0.90 ± 0.01 and 1.36 ± 0.01 mg/g of the L. supina whole plant, respectively. These findings suggest that LS and LSC possess prominent anti-blood stasis effect on rats by modulating the anti-coagulation, anti-platelet activation and anti-fibrinolysis, and supports the traditional folk use of this plant.

摘要

翻白草(Steph.)IK. -Gal. ex Knorr. 在中国被用作血瘀证的经验性治疗已有数百年历史,但没有科学验证。本研究旨在首次评估翻白草乙醇提取物(LS)及其四个馏分(LSA∼D)在葡聚糖 500 诱导的急性血瘀模型大鼠中的化学成分分析、功效和作用机制。LS(229.0∼916.0 mg/kg)和 LSC(17.6∼70.4 mg/kg)每天口服一次,连续 7 天,可显著改善微循环血液动力学功能(血流、血液浓度和血流速度)、血液流变学参数(全血黏度、全血低切黏度、血浆黏度、血小板聚集率、血细胞比容、红细胞聚集指数和红细胞变形指数)和凝血参数(凝血酶时间、凝血酶原时间、活化部分凝血活酶时间、纤维蛋白原和抗凝血酶 III)。此外,它们还显著下调血栓素 B2 和 6-酮-前列腺素 F1α 水平。此外,它还显著降低组织型纤溶酶原激活物(t-PA)、尿激酶型纤溶酶原激活物(u-PA)和纤溶酶原激活物抑制剂-1(PAI-1)水平,以及 PAI-1/t-PA 和 PAI-1/u-PA 比率。同时,基于超高效液相色谱-四极杆飞行时间串联质谱(UHPLC-qTOF-MS/MS)从 LS 中鉴定出 51 种化学成分,定量分析表明,獐牙菜苦苷 A 和獐牙菜苷的两种主要成分分别存在于翻白草全草的 0.90±0.01 和 1.36±0.01 mg/g 中。这些发现表明 LS 和 LSC 通过调节抗凝、抗血小板激活和抗纤溶作用对大鼠具有显著的抗血瘀作用,支持该植物的传统民间用途。

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