[6]-Gingerol: A Novel AT1 Antagonist for the Treatment of
Cardiovascular Disease ([original](https://doi.org/10.1055/s-0032-1328262)) ([raw](?raw))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
Qing Liu
1School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, China
Jinjin Liu
2Beijing Institute of Genomics, Chinese Academy of Sciences, Beijing, China
,
Haili Guo
2Beijing Institute of Genomics, Chinese Academy of Sciences, Beijing, China
,
Shengnan Sun
2Beijing Institute of Genomics, Chinese Academy of Sciences, Beijing, China
,
Shifeng Wang
1School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, China
,
Yanling Zhang
1School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, China
,
Shiyou Li
2Beijing Institute of Genomics, Chinese Academy of Sciences, Beijing, China
,
Yanjiang Qiao
1School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, China
Further Information
Publication History
received 27 November 2012
revised 21 January 2013
accepted 22 January 2013
Publication Date:
11 March 2013 (online)
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
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