Douard Véronique, Choi Hye-In, Elshenawy Summer, Lagunoff David, Ferraris Ronaldo P
Department of Pharmacology and Physiology, NJ Medical School, 185 S. Orange Avenue, Newark, NJ 07101, USA.
J Physiol. 2008 Aug 1;586(15):3657-73. doi: 10.1113/jphysiol.2008.155226. Epub 2008 Jun 12.
Fructose consumption has increased dramatically but little is known about mechanisms regulating the intestinal fructose transporter GLUT5 in vivo. In neonatal rats, GLUT5 can be induced only by luminal fructose and only after 14 days of age, unless the gut is primed with dexamethasone prior to fructose perfusion. To elucidate the mechanisms underlying dexamethasone modulation of GLUT5 development, we first identified the receptor mediating its effects then determined whether those effects were genomic. The glucocorticoid receptor (GR) antagonist RU486 dose-dependently prevented the dexamethasone-mediated effects on body weight, intestinal arginase2 (a known GR-regulated gene) and GLUT5. In contrast, an antagonist of the mineralocorticoid receptor as well as agonists of progesterone (PR) and pregnane-X (PXR) receptors did not block the effects of dexamethasone. These receptor antagonists and agonists had no effect on the intestinal glucose transporter SGLT1. Translocation of the GR into the enterocyte nucleus occurred only in dexamethasone-injected pups perfused with fructose, was accompanied by marked increases in brush border GLUT5 abundance, and was blocked by RU486. A priming duration of approximately 24 h is optimal for induction but actinomycin D injection before dexamethasone priming prevented dexamethasone from allowing luminal fructose to induce GLUT5. Actinomycin D had no effect on dexamethasone-independent fructose-induced increases in glucose-6-phosphatase mRNA abundance, suggesting that it did not prevent fructose-induction of GLUT5, but instead prevented dexamethasone-induced synthesis of an intermediate required by fructose for GLUT5 regulation. In suckling rats < 14 days old, developmental regulation of transporters may involve cross-talk between hormonal signals modulating intestinal maturation and nutrient signals regulating specific transporters.
果糖的摄入量已急剧增加,但对于体内调节肠道果糖转运蛋白GLUT5的机制却知之甚少。在新生大鼠中,GLUT5仅在出生14天后才能由肠腔中的果糖诱导产生,除非在果糖灌注前用 dexamethasone 对肠道进行预处理。为了阐明 dexamethasone 调节GLUT5发育的潜在机制,我们首先确定了介导其作用的受体,然后确定这些作用是否是基因组水平的。糖皮质激素受体(GR)拮抗剂RU486能剂量依赖性地阻止dexamethasone对体重、肠道精氨酸酶2(一种已知的受GR调节的基因)和GLUT5的作用。相比之下,盐皮质激素受体拮抗剂以及孕酮(PR)和孕烷-X(PXR)受体激动剂均不能阻断dexamethasone的作用。这些受体拮抗剂和激动剂对肠道葡萄糖转运蛋白SGLT1没有影响。GR易位进入肠上皮细胞核仅发生在注射了dexamethasone并灌注了果糖的幼崽中,同时伴随着刷状缘GLUT5丰度的显著增加,并且被RU486阻断。大约24小时的预处理时间最适合诱导,但在dexamethasone预处理前注射放线菌素D可阻止dexamethasone使肠腔果糖诱导GLUT5。放线菌素D对不依赖dexamethasone的果糖诱导的葡萄糖-6-磷酸酶mRNA丰度增加没有影响,这表明它不是阻止果糖诱导GLUT5,而是阻止dexamethasone诱导果糖调节GLUT5所需的一种中间体的合成。在小于14日龄的乳鼠中,转运蛋白的发育调节可能涉及调节肠道成熟的激素信号与调节特定转运蛋白的营养信号之间的相互作用。