Graduate School of Information Science and Electrical Engineering, Kyushu University, 744 Motooka, Nishi-ku, Fukuoka 819-0395, Japan.
Research and Development Center for Five-Sense Devices, Kyushu University, 744 Motooka, Nishi-ku, Fukuoka 819-0395, Japan.
Molecules. 2024 May 23;29(11):2452. doi: 10.3390/molecules29112452.
Taste sensors with an allostery approach have been studied to detect non-charged bitter substances, such as xanthine derivatives, used in foods (e.g., caffeine) or pharmaceuticals (e.g., etofylline). In this study, the authors modified a taste sensor with 3-bromo-2,6-dihydroxybenzoic acid and used it in conjunction with sensory tests to assess the bitterness of non-charged pharmaceuticals with xanthine scaffolds (i.e., acefylline and doxofylline), as well as allopurinol, an analogue of hypoxanthine. The results show that the sensor was able to differentiate between different levels of sample bitterness. For instance, when assessing a 30 mM sample solution, the sensor response to acefylline was 34.24 mV, which corresponded to the highest level of bitterness (τ = 3.50), while the response to allopurinol was lowest at 2.72 mV, corresponding to relatively weaker bitterness (τ = 0.50). Additionally, this study extended the application of the sensor to detect pentoxifylline, an active pharmaceutical ingredient in pediatric medicines. These results underscore the taste sensor's value as an additional tool for early-stage assessment and prediction of bitterness in non-charged pharmaceuticals.
作者用 3-溴-2,6-二羟基苯甲酸对味觉传感器进行修饰，并结合感官测试，评估含黄嘌呤骨架的非离子型药物（即醋氨己酸和 doxofylline）以及黄嘌呤类似物别嘌呤醇的苦味。结果表明，该传感器能够区分不同水平的样本苦味。例如，在评估 30mM 样品溶液时，传感器对醋氨己酸的响应为 34.24mV，对应于最高水平的苦味（τ=3.50），而对别嘌呤醇的响应最低，为 2.72mV，对应于相对较弱的苦味（τ=0.50）。此外，这项研究将传感器的应用扩展到了儿科药物中一种活性药物成分——己酮可可碱的检测。这些结果强调了味觉传感器作为一种非离子型药物早期苦味评估和预测的附加工具的价值。
