Kumazawa T, Nomura T, Kurihara K
Faculty of Pharmaceutical Sciences, Hokkaido University, Sapporo, Japan.
Biochemistry. 1988 Feb 23;27(4):1239-44. doi: 10.1021/bi00404a025.
Various bitter substances were found to depolarize liposomes. The results obtained are as follows: (1) Changes in the membrane potential of azolectin liposomes in response to various bitter substances were monitored by measuring changes in the fluorescence intensity of 3,3'-dipropylthiocarbocyanine iodide [diS-C3(5)]. All the bitter substances examined increased the fluorescence intensity of the liposome-dye suspension, which indicates that the substances depolarize the liposomes. There existed a good correlation between the minimum concentrations of the bitter substances to depolarize the liposomes and the taste thresholds in humans. (2) The effects of changed lipid composition of liposomes on the responses to various bitter substances vary greatly among bitter substances, suggesting that the receptor sites for bitter substances are multiple. The responses to N-C=S substances and sucrose octaacetate especially greatly depended on the lipid composition; these compounds depolarized only liposomes having certain lipid composition, while no or hyperpolarizing responses to these compounds were observed in other liposomes examined. This suggested that the difference in "taster" and "nontaster" for these substances can be explained in terms of difference in the lipid composition of taste receptor membranes. (3) It was confirmed that the membrane potential of the planar lipid bilayer is changed in response to bitter substances. The membrane potential changes in the planar lipid bilayer as well as in liposomes in response to the bitter substances occurred under the condition that there is no ion gradient across the membranes. These results suggested that the membrane potential changes in response to bitter substances stem from the phase boundary potential changes induced by adsorption of the substances on the hydrophobic region of the membranes.
研究发现多种苦味物质可使脂质体去极化。得到的结果如下:(1) 通过测量3,3'-二丙基硫代羰花青碘化物[diS-C3(5)]的荧光强度变化,监测偶氮卵磷脂脂质体膜电位对各种苦味物质的响应。所有检测的苦味物质均增加了脂质体-染料悬浮液的荧光强度,这表明这些物质使脂质体去极化。使脂质体去极化的苦味物质的最低浓度与人类味觉阈值之间存在良好的相关性。(2) 脂质体脂质组成的变化对各种苦味物质响应的影响在不同苦味物质之间差异很大,这表明苦味物质的受体位点是多样的。对N-C=S物质和蔗糖八乙酸酯的响应尤其极大地依赖于脂质组成;这些化合物仅使具有特定脂质组成的脂质体去极化,而在其他检测的脂质体中未观察到对这些化合物的响应或超极化响应。这表明这些物质的“味觉者”和“非味觉者”差异可以用味觉受体膜脂质组成的差异来解释。(3) 已证实平面脂质双层的膜电位会因苦味物质而改变。在膜两侧不存在离子梯度的条件下,平面脂质双层以及脂质体的膜电位会因苦味物质而发生变化。这些结果表明,对苦味物质的膜电位变化源于物质吸附在膜疏水区域所诱导的相界电位变化。