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黄酮苷元系列化合物抗聚集活性评价。

Evaluation of antiaggregatory activity of flavonoid aglycone series.

机构信息

University of Zagreb, Faculty of Pharmacy and Biochemistry, Department of Medicinal Chemistry, A, Kovačića 1, 10000 Zagreb, Croatia.

出版信息

Nutr J. 2011 Jul 11;10:73. doi: 10.1186/1475-2891-10-73.

DOI:10.1186/1475-2891-10-73
PMID:21745360
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3166895/
Abstract

BACKGROUND

Among natural compounds, present in every day diet, flavonoids have shown beneficial effect in prevention of cardiovascular diseases that can be attributed, at least partially to the described antiaggregatory activity i.e. antiplatelet effects of flavonoids. Due to the ever increasing pharmacological interest in antiplatelet agents a systematic experimental evaluation of large flavonoid series is needed.

METHODS

A set of thirty flavonoid aglycones has been selected for the evaluation. All measurements of aggregation were done under standardized and firmly controlled in vitro conditions. The whole blood samples, multiple platelet functional analyzer and adenosine diphosphate (ADP) as a weak agonist of aggregation were selected for this purpose.

RESULTS

The results were expressed as minimal concentration of flavonoid that can significantly lower the platelet aggregation compared to the corresponding untreated sample (minimal antiaggregatory concentration--MINaAC). All analyzed flavonoids exhibited antiaggregatory activity MINaAC ranging from 0.119 μM to 122 μM, while the most potent representatives were 3,6-dihydroxyflavone (0.119 μM) and syringetin (0.119 μM).

CONCLUSIONS

Measurable antiplatelet activity established at submicromolar flavonoid concentrations suggests that even a dietary consumption of some flavonoids can make an impact on in vivo aggregation of platelets. These findings also point out a therapeutical potential of some flavonoids.

摘要

背景

在天然化合物中,类黄酮存在于日常饮食中,已显示出对心血管疾病的有益作用,这至少部分归因于其描述的抗聚集活性,即类黄酮的抗血小板作用。由于对抗血小板药物的药理兴趣不断增加,需要对大量类黄酮系列进行系统的实验评估。

方法

选择了一组 30 种黄酮苷元进行评估。所有聚合测量均在标准化和严格控制的体外条件下进行。为此目的,选择全血样本、多血小板功能分析仪和二磷酸腺苷(ADP)作为聚合的弱激动剂。

结果

结果表示为可以显著降低与相应未处理样品相比的血小板聚集的最小黄酮浓度(最小抗聚集浓度-MINAAC)。所有分析的类黄酮均表现出 MINAAC 的抗聚集活性,范围从 0.119 μM 到 122 μM,而最有效的代表是 3,6-二羟基黄酮(0.119 μM)和丁香脂素(0.119 μM)。

结论

在亚微摩尔类黄酮浓度下建立的可测量的抗血小板活性表明,即使饮食中摄入一些类黄酮也会对体内血小板聚集产生影响。这些发现还指出了一些类黄酮的治疗潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1e46/3166895/ce5855c0ab88/1475-2891-10-73-2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1e46/3166895/1e9c523ed7f0/1475-2891-10-73-1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1e46/3166895/ce5855c0ab88/1475-2891-10-73-2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1e46/3166895/1e9c523ed7f0/1475-2891-10-73-1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1e46/3166895/ce5855c0ab88/1475-2891-10-73-2.jpg

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