Kimmich G A, Randles J
Membr Biochem. 1978;1(3-4):221-37. doi: 10.3109/09687687809063849.
Flavanones and flavones are structural analogues of phloretin. Like phloretin they inhibit the non-Na+-dependent, facilitated diffusion transport system for sugars associated with the lateral serosal boundary of intestinal epithelial cells. The degree of inhibition varies with the extent and position of hydroxylation of the flavonoid nucleus. Flavones are more potent than corresponding flavanones. Tri- and tetrahydroxylated forms are more inhibitory than similar penta- and hexahydroxylated molecules. With one exception, none of the 18 flavonoids tested has secondary effects as metabolic inhibitors, as does phloretin. Inhibition of the passive sugar transport system with flavonoids allows the concentrative Na+-dependent sugar transport system to establish a better concentration gradient than is observed in untreated cells. The degree of gradient enhancement is proportional to the degree of inhibition of the sugar "leak." The flavonoid glycosides, which can be considered as phlorizin analogues, also inhibit the non-Na+-dependent sugar carrier, but less well than corresponding nonglycosylated agents. Only one of the glycosides inhibits the Na+-dependent transport system, and much less potently than phlorizin.
黄烷酮和黄酮是根皮素的结构类似物。与根皮素一样，它们抑制与肠上皮细胞侧浆膜边界相关的非钠离子依赖性、易化扩散糖类转运系统。抑制程度随黄酮核羟基化的程度和位置而变化。黄酮比相应的黄烷酮更有效。三羟基和四羟基化形式比类似的五羟基和六羟基化分子更具抑制性。除了一个例外，所测试的18种黄酮类化合物中没有一种像根皮素那样具有作为代谢抑制剂的次要作用。用黄酮类化合物抑制被动糖类转运系统可使钠离子依赖性浓缩糖类转运系统建立比未处理细胞中观察到的更好的浓度梯度。梯度增强程度与糖类“渗漏”的抑制程度成正比。可被视为根皮苷类似物的黄酮糖苷也抑制非钠离子依赖性糖类载体，但效果不如相应的非糖基化试剂。只有一种糖苷抑制钠离子依赖性转运系统，且效力远低于根皮苷。
