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从海洋褐藻角叉菜中分离得到的一种杜拉烷二萜的抗凝和抗血小板作用。

Anticoagulation and antiplatelet effects of a dolastane diterpene isolated from the marine brown alga Canistrocarpus cervicornis.

机构信息

Departamento de Biologia Molecular e Celular, Instituto de Biologia, Universidade Federal Fluminense, Niterói 24001970, Brazil.

出版信息

J Thromb Thrombolysis. 2011 Feb;31(2):235-40. doi: 10.1007/s11239-010-0545-6.

Abstract

Marine brown algae of the family Dictyotaceae are rich sources of monocyclic, bicyclic, and tricyclic diterpenes. These molecules are responsible for a wide range of pharmacological and ecological functions, as antitumor and antiviral. Here, we analyzed the effect of the dolastane diterpene (4R, 9S, 14S)-4α-Acetoxy-9β,14α-dihydroxydolast-1(15),7-diene, isolated from the marine brown alga, Canistrocarpus cervicornis on blood clotting and platelet aggregation. The dolastane diterpene was able to inhibit either plasma or fibrinogen coagulation induced by thrombin as well as delayed coagulation in the recalcification test. The dolastane diterpene impaired, in a concentration-dependent manner platelet aggregation induced by collagen or adenosine diphosphate with no lysis on such cells. Thus, the dolastane diterpene maybe a promising source of natural inhibitors for hemostatic disturbs (clotting and platelet aggregation) leading to the discovery of drugs of potential use as antithrombotic and antiplatelet. In addition, the dolastane diterpene may be used as a molecular model for development of new antithrombotic agents giving new approaches to the management to the treatment of thrombotic disturbs.

摘要

红藻门褐藻富含单环、双环和三环二萜类化合物。这些分子具有广泛的药理和生态功能,如抗肿瘤和抗病毒。在这里,我们分析了从海洋褐藻 Canistrocarpus cervicornis 中分离得到的达玛烷二萜(4R,9S,14S)-4α-乙酰氧基-9β,14α-二羟基达玛-1(15),7-二烯对血液凝固和血小板聚集的影响。该达玛烷二萜可抑制凝血酶诱导的血浆或纤维蛋白原凝固以及再钙化试验中的凝血延迟。该达玛烷二萜可浓度依赖性地抑制胶原或二磷酸腺苷诱导的血小板聚集,而对这些细胞没有裂解作用。因此,达玛烷二萜类化合物可能是一种有前途的天然止血(凝血和血小板聚集)抑制剂来源,可发现具有抗血栓和抗血小板作用的潜在药物。此外,该达玛烷二萜类化合物可用作新型抗血栓药物的分子模型,为治疗血栓紊乱提供新的方法。

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