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Planta Med 2013; 79(05): 322-326
DOI: 10.1055/s-0032-1328262
Biological and Pharmacological Activity
Original Papers
Georg Thieme Verlag KG Stuttgart · New York

[6]-Gingerol: A Novel AT1 Antagonist for the Treatment of Cardiovascular Disease

Qing Liu
1   School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, China
,
Jinjin Liu
2   Beijing Institute of Genomics, Chinese Academy of Sciences, Beijing, China
,
Haili Guo
2   Beijing Institute of Genomics, Chinese Academy of Sciences, Beijing, China
,
Shengnan Sun
2   Beijing Institute of Genomics, Chinese Academy of Sciences, Beijing, China
,
Shifeng Wang
1   School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, China
,
Yanling Zhang
1   School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, China
,
Shiyou Li
2   Beijing Institute of Genomics, Chinese Academy of Sciences, Beijing, China
,
Yanjiang Qiao
1   School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, China
› Author Affiliations
Further Information

Publication History

received 27 November 2012
revised 21 January 2013

accepted 22 January 2013

Publication Date:
11 March 2013 (online)

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Abstract

Considering the prevalence of cardiovascular disease in public health and the limited validated therapeutic options, this study aimed to find novel compounds targeting the angiotensin II type 1 receptor, accepted as a therapeutic target in cardiovascular disease. A small library consisting of 89 compounds from 39 Chinese herbs was profiled using a cell-based calcium mobilization assay which was developed and characterized for high-throughput screening. [6]-Gingerol derived from Zingiber officinale Roscoe (ginger) was identified as a novel angiotensin II type 1 receptor antagonist, with an IC50 value of 8.173 µM. The hit was further tested by a specificity assay indicating that it had no antagonistic effects on other evaluated GPCRs, such as endothelin receptors. The major ingredient of ginger, [6]-gingerol, could inhibit angiotensin II type 1 receptor activation, which partially clarified the mechanism of ginger regulating blood pressure and strengthening heart in the cardiovascular system.

Key words

[6]-gingerol - AT1 antagonist - calcium assay - high-throughput screening - cardiovascular disease - Chinese herb

Supporting Information

 

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