Keshavarz Maryam, Ruppert Anna-Lena, Meiners Mirjam, Poharkar Krupali, Liu Shuya, Mahmoud Wafaa, Winterberg Sarah, Hartmann Petra, Mermer Petra, Perniss Alexander, Offermanns Stefan, Kummer Wolfgang, Schütz Burkhard
Institute for Anatomy and Cell Biology, German Center for Lung Research, Justus Liebig University, Giessen, Germany.
Excellence Cluster Cardio-Pulmonary Institute, Justus Liebig University, Giessen, Germany.
Sci Rep. 2024 Aug 8;14(1):18447. doi: 10.1038/s41598-024-69287-6.
Disorders of gallbladder motility can lead to serious pathology. Bitter tastants acting upon bitter taste receptors (TAS2R family) have been proposed as a novel class of smooth muscle relaxants to combat excessive contraction in the airways and other organs. To explore whether this might also emerge as an option for gallbladder diseases, we here tested bitter tastants for relaxant properties and profiled Tas2r expression in the mouse gallbladder. In organ bath experiments, the bitter tastants denatonium, quinine, dextromethorphan, and noscapine, dose-dependently relaxed the pre-contracted gallbladder. Utilizing gene-deficient mouse strains, neither transient receptor potential family member 5 (TRPM5), nor the Tas2r143/Tas2r135/Tas2r126 gene cluster, nor tuft cells proved to be required for this relaxation, indicating direct action upon smooth muscle cells (SMC). Accordingly, denatonium, quinine and dextromethorphan increased intracellular calcium concentration preferentially in isolated gallbladder SMC and, again, this effect was independent of TRPM5. RT-PCR revealed transcripts of Tas2r108, Tas2r126, Tas2r135, Tas2r137, and Tas2r143, and analysis of gallbladders from mice lacking tuft cells revealed preferential expression of Tas2r108 and Tas2r137 in tuft cells. A TAS2R143-mCherry reporter mouse labeled tuft cells in the gallbladder epithelium. An in silico analysis of a scRNA sequencing data set revealed Tas2r expression in only few cells of different identity, and from in situ hybridization histochemistry, which did not label distinct cells. Our findings demonstrate profound tuft cell- and TRPM5-independent relaxing effects of bitter tastants on gallbladder smooth muscle, but do not support the concept that these effects are mediated by bitter receptors.
胆囊运动障碍可导致严重病变。作用于苦味受体(TAS2R家族)的苦味剂已被提议作为一类新型的平滑肌松弛剂,用于对抗气道和其他器官的过度收缩。为了探究这是否也可能成为治疗胆囊疾病的一种选择,我们在此测试了苦味剂的松弛特性,并分析了小鼠胆囊中Tas2r的表达情况。在器官浴实验中,苦味剂地那铵、奎宁、右美沙芬和那可丁能剂量依赖性地松弛预先收缩的胆囊。利用基因缺陷小鼠品系,发现瞬时受体电位家族成员5(TRPM5)、Tas2r143/Tas2r135/Tas2r126基因簇以及簇状细胞都不是这种松弛作用所必需的,这表明苦味剂是直接作用于平滑肌细胞(SMC)。相应地,地那铵、奎宁和右美沙芬优先增加分离的胆囊SMC中的细胞内钙浓度,而且这种作用同样不依赖于TRPM5。RT-PCR显示了Tas2r108、Tas2r126、Tas2r135、Tas2r137和Tas2r143的转录本,对缺乏簇状细胞的小鼠胆囊进行分析发现,Tas2r108和Tas2r137在簇状细胞中优先表达。一只TAS2R143-mCherry报告基因小鼠标记了胆囊上皮中的簇状细胞。对一个单细胞RNA测序数据集的计算机分析显示,Tas2r仅在少数不同类型的细胞中表达,原位杂交组织化学也未标记出特定的细胞。我们的研究结果表明,苦味剂对胆囊平滑肌具有显著的、不依赖于簇状细胞和TRPM5的松弛作用,但不支持这些作用是由苦味受体介导的这一概念。