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黄蝉中绿原酸的结构解析及其对人血小板聚集的抑制作用

Structure elucidation and inhibitory effects on human platelet aggregation of chlorogenic acid from Wrightia tinctoria.

作者信息

Amin Ripal P, Kunaparaju Naveen, Kumar Sunil, Taldone Tony, Barletta Michael A, Zito S William

机构信息

Department of Pharmaceutical Sciences, College of Pharmacy and Health Professions, St. John’s University, Jamaica, NY 11439, USA.

出版信息

J Complement Integr Med. 2013 May 24;10:/j/jcim.2013.10.issue-1/jcim-2012-0048/jcim-2012-0048.xml. doi: 10.1515/jcim-2012-0048.

Abstract

BACKGROUND

Interest in natural compounds as sources of potentially new treatment options is growing rapidly. Preliminary screening of many different plant extracts showed that Wrightia tinctoria acts as a potent human platelet aggregation inhibitor. The aim of the present study was to isolate and characterize the active compound responsible for potent inhibition of human platelet aggregation in vitro.

METHODS

A 70% ethanolic extract derived from W. tinctoria seeds was fractionated with chloroform followed by ethyl acetate. The ethyl acetate fraction was further fractionated and purified through a series of three successive column chromatographic separations using silica gel, Sephadex LH-20, and C-18 columns. Liquid chromatography coupled to negative electrospray ionization tandem mass spectrometry (LC-MS/MS) and nuclear magnetic resonance (NMR) studies were performed in the structure determination of the active phenolic compound present in the ethyl acetate fraction of W. tinctoria seeds.

RESULTS

A phenolic compound has been isolated and identified as chlorogenic acid by LC-MS/MS and NMR studies. Chlorogenic acid showed concentration-dependent inhibitory effect on collagen-induced platelet aggregation in vitro with an IC50 of 0.2363 μg/μl.

CONCLUSION

The present data suggest that chlorogenic acid can be developed as potential antiplatelet agent in the treatment of cardiovascular diseases in diabetes mellitus.

摘要

背景

对天然化合物作为潜在新治疗选择来源的兴趣正在迅速增长。对许多不同植物提取物的初步筛选表明,鸡骨常山可作为一种有效的人类血小板聚集抑制剂。本研究的目的是分离并鉴定在体外对人类血小板聚集有强效抑制作用的活性化合物。

方法

用氯仿接着用乙酸乙酯对从鸡骨常山种子中提取的70%乙醇提取物进行分级分离。乙酸乙酯级分通过使用硅胶、葡聚糖凝胶LH - 20和C - 18柱的一系列三次连续柱色谱分离进一步分级分离和纯化。在对鸡骨常山种子乙酸乙酯级分中存在的活性酚类化合物进行结构测定时,进行了液相色谱与负电喷雾电离串联质谱(LC - MS/MS)和核磁共振(NMR)研究。

结果

通过LC - MS/MS和NMR研究分离并鉴定出一种酚类化合物为绿原酸。绿原酸在体外对胶原诱导的血小板聚集显示出浓度依赖性抑制作用,IC50为0.2363μg/μl。

结论

目前的数据表明,绿原酸可被开发为治疗糖尿病心血管疾病的潜在抗血小板药物。

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