title: [6]-gingerol: a novel AT₁ antagonist for the treatment of cardiovascular disease.
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.
authors.affiliation: School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, China.
authors.forename: Qing
authors.initials: Q
authors.lastname: Liu
authors.forename: Jinjin
authors.initials: J
authors.lastname: Liu
authors.forename: Haili
authors.initials: H
authors.lastname: Guo
authors.forename: Shengnan
authors.initials: S
authors.lastname: Sun
authors.forename: Shifeng
authors.initials: S
authors.lastname: Wang
authors.forename: Yanling
authors.initials: Y
authors.lastname: Zhang
authors.forename: Shiyou
authors.initials: S
authors.lastname: Li
authors.forename: Yanjiang
authors.initials: Y
authors.lastname: Qiao
mesh_terms: D057912:Angiotensin II Type 2 Receptor Blockers / Q000032:analysis*; D002318:Cardiovascular Diseases / Q000188:drug therapy; D002396:Catechols / Q000494:pharmacology* / Q000627:therapeutic use; D004353:Drug Evaluation, Preclinical; D005233:Fatty Alcohols / Q000494:pharmacology* / Q000627:therapeutic use; D020939:Zingiber officinale / Q000737:chemistry; D057809:HEK293 Cells; D057166:High-Throughput Screening Assays; D006801:Humans; D010946:Plants, Medicinal / Q000737:chemistry*
chemical_list: D057912:Angiotensin II Type 2 Receptor Blockers; D002396:Catechols; D005233:Fatty Alcohols; C007845:gingerol