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藻类类肝素及其抗凝、出血活性和血小板聚集。

Heparinoids algal and their anticoagulant, hemorrhagic activities and platelet aggregation.

作者信息

de Azevedo Tarciana Carvalho G, Bezerra Maria Emília B, Santos Maria da Glória de L, Souza Leonardo Augusto, Marques Cybelle T, Benevides Norma Maria B, Leite Edda Lisboa

机构信息

Departamento de Bioquímica, Centro de Biociências, Universidade Federal do Rio Grande do Norte, 3000 Campus Universitário, Bairro Lagoa Nova, CEP 59072-970 Natal, Rio Grande do Norte, Brazil.

出版信息

Biomed Pharmacother. 2009 Aug;63(7):477-83. doi: 10.1016/j.biopha.2008.09.012. Epub 2008 Oct 26.

Abstract

Polysaccharides extracted from brown marine algae represent a source of marine compounds with potential applications in medicine. Heparin-like compounds, fucoidans, have been proposed as alternatives to the anticoagulant heparin, which is prepared from mucous membrane of mammals. In this study, the activity of anticoagulant in activated partial thromboplastin time (APTT) and prothrombin time (PT) tests was assessed in the fucoidan (TF), from seaweed Fucus vesiculosus, partially desulfated fucoidans (PDF), desulfated fucoidans (DF) and purified fractions F1, F2 and F3 in acetone. Studies were also conducted to assess these polysaccharides for platelet aggregation and hemorrhagic activity. The APTT test showed high activity at 5 microg (> or = 240s) for TF, F1 and F2 (P<0.001). PT test showed high anticoagulant activity at 50 microg (> or = 120s) for F1 (P<0.001). Fraction F3, with low MW (15.2 kDa) and sulfate content (26.1%), had little effect in these two in vitro tests (P<0.001). These compounds demonstrated a two-phase response to platelet aggregation at 50 microg/mL. However, at a concentration of 0.1 mg/mL, a hypoaggregate profile was observed for all fractions tested (P<0.001). The analysis showed that fucoidans irreversibly induced platelet aggregation in high concentration. These polymers have low hemorrhagic effect when compared to heparin.

摘要

从褐藻中提取的多糖是一类具有潜在医学应用价值的海洋化合物来源。类肝素化合物岩藻聚糖,已被提议作为从哺乳动物粘膜制备的抗凝血剂肝素的替代品。在本研究中,对来自墨角藻的岩藻聚糖(TF)、部分脱硫酸岩藻聚糖(PDF)、脱硫酸岩藻聚糖(DF)以及丙酮中的纯化级分F1、F2和F3,在活化部分凝血活酶时间(APTT)和凝血酶原时间(PT)试验中的抗凝血活性进行了评估。还开展了研究以评估这些多糖的血小板聚集和出血活性。APTT试验显示,TF、F1和F2在5微克时具有高活性(>或=240秒)(P<0.001)。PT试验显示,F1在50微克时具有高抗凝血活性(>或=120秒)(P<0.001)。分子量低(15.2 kDa)且硫酸盐含量低(26.1%)的级分F3,在这两项体外试验中作用很小(P<0.001)。这些化合物在50微克/毫升时对血小板聚集表现出双相反应。然而,在0.1毫克/毫升的浓度下,所有测试级分均观察到低聚集特征(P<0.001)。分析表明,岩藻聚糖在高浓度下不可逆地诱导血小板聚集。与肝素相比,这些聚合物的出血作用较低。

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