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沙棘浆果中异鼠李素及其衍生物的抗血小板和抗凝活性的全血测定。

Antiplatelet and Anticoagulant Activity of Isorhamnetin and Its Derivatives Isolated from Sea Buckthorn Berries, Measured in Whole Blood.

机构信息

Department of Biochemistry, Institute of Soil Science and Plant Cultivation, State Research Institute, 24-100 Puławy, Poland.

Department of General Biochemistry, Faculty of Biology and Environmental Protection, University of Lodz, 90-236 Lodz, Poland.

出版信息

Molecules. 2022 Jul 11;27(14):4429. doi: 10.3390/molecules27144429.

DOI:10.3390/molecules27144429
PMID:35889302
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9319006/
Abstract

Blood platelets play a crucial role in hemostasis, the process responsible for keeping blood flowing in the circulatory system. However, unnecessary platelet activation can lead to aggregation at the site of atherosclerotic plaque rapture and the formation of a thrombus, which promotes atherothrombotic diseases. Various dietary components, such as phenolic compounds, are known to demonstrate antiplatelet and anticoagulant properties, and it is possible that these could form an important element in the prophylaxis and therapy of cardiovascular diseases. Our present study examined the biological activity of isorhamnetin () and two isorhamnetin derivatives, (): 3--beta-glucoside-7--alpha-rhamnoside and (): 3--beta-glucoside-7--alpha-(3″'-isovaleryl)-rhamnoside, isolated from the phenolic fraction of sea buckthorn fruit, against human washed blood platelets and human whole blood in vitro. The anti-platelet and anticoagulant potential was determined using (A) flow cytometry, (B) the thrombus-formation analysis system (T-TAS) and (C) colorimetry. The results of the T-TAS test indicate that the AUC (Area Under the Curve) of the tested phenolic compounds (compounds , and ; 50 µg/mL) was markedly reduced compared to the control values. Moreover, flavonol demonstrated anti-platelet potential, including anti-adhesive activity, with these effects being more intense in compound than isorhamnetin. Different actions of flavonol on platelet activation may depend on their binding ability to various receptors on blood platelets. However, the mechanism of their anti-platelet potential requires further additional studies, including in vitro and in vivo experiments.

摘要

血小板在止血过程中起着至关重要的作用,止血过程负责保持循环系统中的血液流动。然而,血小板的不必要激活会导致动脉粥样硬化斑块破裂部位的聚集和血栓的形成,从而促进动脉粥样硬化性疾病的发生。已知各种膳食成分,如酚类化合物,具有抗血小板和抗凝作用,这些成分可能成为心血管疾病预防和治疗的重要因素。本研究检测了从沙棘果酚类部分分离得到的异鼠李素()和两种异鼠李素衍生物():3--β-葡萄糖苷-7--α-鼠李糖苷和():3--β-葡萄糖苷-7--α-(3″′-异戊酰基)-鼠李糖苷对人洗涤血小板和人全血的体外生物活性。使用(A)流式细胞术、(B)血栓形成分析系统(T-TAS)和(C)比色法测定抗血小板和抗凝潜能。T-TAS 试验的结果表明,与对照值相比,测试的酚类化合物(化合物、和;50 µg/mL)的 AUC(曲线下面积)明显降低。此外,类黄酮表现出抗血小板作用,包括抗黏附活性,其中化合物的作用比异鼠李素更强。类黄酮对血小板激活的不同作用可能取决于它们与血小板上各种受体的结合能力。然而,其抗血小板作用的机制需要进一步的额外研究,包括体外和体内实验。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10ef/9319006/f1ee49e435e1/molecules-27-04429-g007.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10ef/9319006/0819e326dde6/molecules-27-04429-g002.jpg
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