Inhibition of intestinal and renal Na+-glucose cotransporter by naringenin
Inhibition of intestinal and renal Na+-glucose cotransporter by naringenin
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DOI：
10.1016/j.biocel.2005.10.002
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发表时间：
2006-01-01
影响因子：
4
通讯作者：
Cheng, CHK
中科院分区：
文献类型：
--
作者：
Li, JM;Che, CT;Cheng, CHK
减少葡萄糖摄取是控制糖尿病高血糖的一种可能方法。使用纯化的肠刷状边界膜囊泡和外翻肠袖，我们已经证明柚皮素，一种存在于柑橘类水果和果汁中的类黄酮，可以显著抑制肠道中的葡萄糖摄取。此外，柚皮素对肾刷状缘膜小泡的葡萄糖摄取也有抑制作用。柚皮苷是柚皮素中的一种甙，在这些方面完全没有活性。柚皮素对兔肠刷状缘膜小泡的葡萄糖摄取有中等抑制作用，对大鼠外翻型肠套有较强的抑制作用。IC50值分别为205.9和2.4 mu mol/l。Lineweaver-Burk分析表明，柚皮素以竞争方式抑制大鼠肠套的葡萄糖摄取，其K-i值为1.1 μ mol/l。糖尿病大鼠肠和肾刷状膜小泡的葡萄糖摄取活性均明显高于正常大鼠。柚皮素（500 μ M）使糖尿病大鼠肠道和肾脏刷状膜囊泡的葡萄糖摄取减少60%以上，与正常大鼠相似。正常大鼠和糖尿病大鼠肾刷缘膜小泡中柚皮素的IC50值分别为323.9和166.1 μ mol/l。这些结果表明，抑制肠道葡萄糖摄取和肾脏葡萄糖重吸收，至少在一定程度上解释了柚皮素及其衍生物的体内抗高血糖作用。这些天然化合物在控制高血糖中的可能应用值得进一步研究。(c) 2005 Elsevier Ltd版权所有。
Reduction in glucose uptake constitutes a possible means of controlling diabetic hyperglycemia. Using purified intestinal brush border membrane vesicles and everted intestinal sleeves, we have demonstrated that naringenin, a flavonoid present in citrus fruits and juices, significantly inhibited glucose uptake in the intestine. In addition, naringenin also elicited inhibitory actions towards glucose uptake in renal brush border membrane vesicles. Naringin, a glycoside of naringenin, was totally inactive in these aspects. Naringenin exhibited moderate inhibitory action on glucose uptake in rabbit intestinal brush border membrane vesicles, and showed strong inhibitory action in rat everted intestinal sleeves. The IC50 values were 205.9 and 2.4 mu mol/l, respectively. Lineweaver-Burk analysis demonstrated that naringenin inhibited glucose uptake in rat everted intestinal sleeves in a competitive manner with a K-i value of 1.1 mu mol/l. Glucose uptake activities in both the intestinal and renal brush border membrane vesicles of diabetic rats were significantly higher than in normal rats. Naringenin (500 mu M) reduced glucose uptake by more than 60% in both the intestinal and renal brush border membrane vesicles of diabetic rats to a level similar to that of the normal rats. The IC50 values of naringenin in the renal brush border membrane vesicles of normal and diabetic rats were 323.9 and 166.1 mu mol/l, respectively. These results suggest that inhibition of intestinal glucose uptake and renal glucose reabsorption explains, in part at least, the in vivo anti hyperglycemic action of naringenin and its derivatives. The possible application of these natural compounds in controlling hyperglycemia warrants further investigations. (c) 2005 Elsevier Ltd. All rights reserved.