Opertech Bio, Inc., Philadelphia, Pennsylvania, United States of America.
Department of Pharmaceutical Sciences and Moulder Center for Drug Discovery Research, School of Pharmacy, Temple University, Philadelphia, Pennsylvania, United States of America.
PLoS One. 2024 Nov 18;19(11):e0313128. doi: 10.1371/journal.pone.0313128. eCollection 2024.
The sweet taste of saccharides, such as sucrose and glucose, and other sweeteners is known to result from activation of the TAS1R2/R3 receptor expressed in taste receptor cells (TRCs) of the taste bud. Recent reports have suggested the existence of an additional sweet taste signaling pathway for metabolizable saccharides that is dependent on the activity of glucose transporters, especially SGLT1, also expressed in TRCs. We have investigated the potential contribution of SGLT1 to glucose taste signaling in humans. Concentration-response analysis of glucose mediated changes in membrane potential measured in Chinese hamster ovary (CHO) cells transiently expressing the human SGLT1 (hSGLT1) yielded an EC50 value of 452 μM. The SGLT inhibitor phlorizin inhibited the membrane potential response to 10 mM glucose with an IC50 of 3.5 μM. In contrast, EC50 values of 127 and 132 mM were obtained from concentration-response analysis of glucose taste in vehicles of water or 20 mM NaCl, respectively, by rapid throughput taste discrimination with human subjects. Lactisole, an antagonist of TAS1R2/R3, at a concentration of 1 mM completely inhibited taste responses to glucose concentrations of 250 mM and below. Phlorizin (0.2 mM) and the high potency SGLT1-selective inhibitor mizagliflozin (10 μM) failed to inhibit glucose taste detection measured at peri-threshold concentrations in the rapid throughput taste discrimination assay. A Yes/No experiment using the taste discrimination assay revealed that 0.2 mM phlorizin was discriminable from water for some subjects. Taken together the results indicate that agonist activation of TAS1R2/R3 is sufficient to account for all glucose taste without contribution by an alternative SGLT-mediated signaling pathway. Furthermore, the taste of phlorizin could be a confounding variable for studies evaluating a role for SGLTs in taste.
糖类(如蔗糖和葡萄糖)和其他甜味剂的甜味是已知的,其源于在味觉感受器细胞(TRC)中表达的 TAS1R2/R3 受体的激活。最近的报告表明,对于可代谢的糖类,存在另一种依赖于葡萄糖转运体(尤其是也在 TRC 中表达的 SGLT1)活性的甜味信号通路。我们研究了 SGLT1 对人类葡萄糖味觉信号传递的潜在贡献。在瞬时表达人 SGLT1(hSGLT1)的中国仓鼠卵巢(CHO)细胞中,对葡萄糖介导的膜电位变化的浓度-反应分析得出 EC50 值为 452 μM。SGLT 抑制剂根皮苷对 10 mM 葡萄糖的膜电位反应的 IC50 为 3.5 μM。相比之下,通过人类受试者的快速吞吐量味觉辨别,从水或 20 mM NaCl 载体中葡萄糖味觉的浓度-反应分析中获得 EC50 值分别为 127 和 132 mM。在浓度为 1 mM 时,TAS1R2/R3 的拮抗剂乳酰噻唑完全抑制了葡萄糖浓度为 250 mM 及以下的味觉反应。根皮苷(0.2 mM)和高选择性 SGLT1 抑制剂米格列净(10 μM)未能抑制快速吞吐量味觉辨别测定中阈下浓度的葡萄糖味觉检测。使用味觉辨别试验的是/否实验表明,对于一些受试者,0.2 mM 根皮苷与水可辨别。总之,结果表明,TAS1R2/R3 的激动剂激活足以解释所有葡萄糖味觉,而无需替代的 SGLT 介导的信号通路的贡献。此外,根皮苷的味道可能是评估 SGLTs 在味觉中作用的研究中的混杂变量。