Department of Pharmaceutical Sciences, University of Piemonte Orientale, Novara, Italy.
Department of Health Sciences, University of Piemonte Orientale, Novara, Italy.
Fitoterapia. 2018 Jun;127:252-256. doi: 10.1016/j.fitote.2018.02.030. Epub 2018 Feb 27.
The discovery of taste receptors hTAS2Rs expression in extra oral tissue, especially in the gastrointestinal tract and in the respiratory system, has endowed bitter receptors of functionalities that exceed the simple perception of taste and flavour. In particular, stimulation of hTAS2Rs by bitter agents in the airway smooth muscle triggers bronchodilation of possible pharmacological relevance. To study the receptor localization in pulmonary smooth muscle cells and to investigate their biological response to hTAS2R38 activation, we have developed a fluorescent probe for hTAS2R38 starting from the sesquiterpene lactone costunolide, available in multigram amounts from Artemisia umbelliformis Lam. The N-methylanthranilate-containing probe demonstrated a very low cytotoxicity compared to the natural product toward human airway smooth muscle cells and epithelial bronchial cells, but fully retained its binding to hTAS2R38, making it possible the fluorescent detection of cells expressing this bitter receptor.
味觉受体 hTAS2Rs 在口腔外组织（特别是胃肠道和呼吸系统）中的表达的发现，使苦味受体具有了超越单纯味觉感知的功能。特别是，气道平滑肌中苦味剂对 hTAS2Rs 的刺激引发了可能具有药理学相关性的支气管扩张。为了研究肺平滑肌细胞中的受体定位，并研究它们对 hTAS2R38 激活的生物学反应，我们从 Artemisia umbelliformis Lam. 中大量获得的倍半萜内酯科伦诺内酯出发，开发了一种用于 hTAS2R38 的荧光探针。与天然产物相比，含有 N-甲基邻氨基苯甲酸酯的探针对人气道平滑肌细胞和上皮支气管细胞的细胞毒性非常低，但完全保留了与 hTAS2R38 的结合，从而可以通过荧光检测表达这种苦味受体的细胞。
