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The Human Bitter Taste Receptor hTAS2R50 Is Activated by the Two Natural Bitter Terpenoids Andrographolide and Amarogentin

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Maik Behrens†, Anne Brockhoff†, Claudia Batram†, Christina Kuhn†, Giovanni Appendino§ and Wolfgang Meyerhof*†

^† Department of Molecular Genetics, German Institute of Human Nutrition Potsdam-Rehbruecke, Arthur-Scheunert-Allee 114−116, 14558 Nuthetal, Germany

^§ Dipartimento di Scienze Chimiche, Università del Piemonte, Orientale, Alimentari, Farmaceutiche e Farmacologiche, Via Bovio 6, 28100 Novara, Italy

J. Agric. Food Chem., 2009, 57 (21), pp 9860–9866

DOI: 10.1021/jf9014334

Publication Date (Web): October 9, 2009

*Author to whom correspondence should be addressed (telephone +49 33200 88282; fax +49 33200 88384; e-mail meyerhof@dife.de).

This article is part of the

12th Weurman Symposium

special issue.

Abstract

Bitterness perception in mammals is mediated through activation of dedicated bitter taste receptors located in the oral cavity. Genomic analyses revealed the existence of orthologous mammalian bitter taste receptor genes, which presumably recognize the same compounds in different species, as well as species-specific receptor gene expansions believed to fulfill a critical role during evolution. In man, 8 of the 25 bitter taste receptors (hTAS2Rs) are closely related members of such an expanded subfamily of receptor genes. This study identified two natural bitter terpenoids, andrographolide and amarogentin, that are agonists for the orphan receptor hTAS2R50, the most distant member of the subfamily. This paper presents the pharmacological characterization of this receptor and analyzes its functional relationship with the previously deorphaned hTAS2R43, hTAS2R44, hTAS2R46, and hTAS2R47. Insights into the general breadth of tuning, functional redundancies, and relationships between pharmacological activation patterns and amino acid homologies for this receptor subfamily are presented.

Keywords (keywords):

Bitter taste; TAS2Rs; heterologous expression; andrographolide; amarogentin

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This article has been cited by 1 ACS Journal articles (1 most recent appear below).

Five Bitter Compounds Display Different Anti-inflammatory Effects through Modulating Cytokine Secretion Using Mouse Primary Splenocytes in Vitro
Wei-Chi Lin and Jin-Yuarn Lin
Journal of Agricultural and Food Chemistry2011 59 (1), 184-192
- Five Bitter Compounds Display Different Anti-inflammatory Effects through Modulating Cytokine Secretion Using Mouse Primary Splenocytes in Vitro
  Wei-Chi Lin and Jin-Yuarn Lin
  Journal of Agricultural and Food Chemistry2011 59 (1), 184-192
  Bitter foods are generally recognized as anti-inflammatory agents in traditional Chinese medicine. To verify the anti-inflammatory effects of some bitter compounds in foods or plants, five bitter compounds, aloperine, amygdalin, berberine, crotaline, and ...
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