Expression and functional activity of bitter taste receptors in primary renal tubular epithelial cells and M-1 cells

Mol Cell Biochem. 2017 Apr;428(1-2):193-202. doi: 10.1007/s11010-016-2929-1. Epub 2017 Feb 24.


The kidney is essential in the maintenance of in vivo homeostasis by body fluid and electrolyte conservation and metabolic waste removal. Previously, we reported the expression of a novel G protein family (Tas2rs), which includes bitter taste receptors, in the kidney tubule system, including the nephrons and the collecting duct system. Bitter taste receptors could affect kidney function via Ca2+ intake. Alkaloids such as phenylthiocarbamide stimulate these receptors and cause an increase in Ca2+ intake. In this study, we determined the expression of bitter taste receptors in the immature kidney and small intestine and in primary renal epithelial cells and M-1 (collecting tubule cell line) cells, by using QPCR and immunostaining. We found no expression of bitter taste receptors in the immature kidney and small intestine several days after birth; the relative abundance of Tas2rs transcripts varied depending on the developmental stage. Tas2rs were expressed in primary renal epithelial cells and M-1 cells. The traditional Chinese medicinal plant extracts phellodendrine and coptisine caused a rapid rise in intracellular Ca2+ concentration, which was inhibited by the phospholipase C (PLC) inhibitor U-73122. Thus, phellodendrine and coptisine could change the physiological status of renal cells in vitro by mediation of bitter taste receptors in a PLC-dependent manner. Our results provide new insights on the expression and role of bitter taste receptors in renal development and function.

Keywords: Alkaloid; Bitter taste receptors; Kidney; M-1 cells; Primary renal tubular epithelial cells.

MeSH terms

  • Animals
  • Berberine / analogs & derivatives
  • Berberine / pharmacology
  • Calcium / metabolism
  • Cell Line
  • Cells, Cultured
  • Epithelial Cells / drug effects
  • Epithelial Cells / metabolism*
  • Gene Expression Regulation / drug effects
  • Intestine, Small / metabolism*
  • Kidney Tubules / cytology*
  • Kidney Tubules / drug effects
  • Kidney Tubules / metabolism
  • Mice
  • Quinolizines / pharmacology
  • Receptors, G-Protein-Coupled / genetics*
  • Receptors, G-Protein-Coupled / metabolism*
  • Taste


  • Quinolizines
  • Receptors, G-Protein-Coupled
  • coptisine
  • Berberine
  • phellodendrine
  • Calcium