Mizuma T, Awazu S
Department of Biopharmaceutics, School of Pharmacy, Tokyo University of Pharmacy and Life Science, Hachioji, Japan.
Biochim Biophys Acta. 1998 Jan 8;1379(1):1-6. doi: 10.1016/s0304-4165(97)00074-3.
Intestinal absorption of beta-disaccharide (cellobiose, maltose and lactose) conjugates of p-nitrophenol (p-nitrophenyl beta-disaccharide) were examined in terms of the hydrolysis of disaccharide conjugate to monosaccharide conjugate and the transport of monosaccharide conjugate by Na+/glucose transport carrier (SGLT1). beta-Cellobioside, beta-maltoside and beta-lactoside of p-nitrophenol (p-NP) were hydrolyzed to p-nitrophenyl beta-glucoside (p-NPbeta glc) on the mucosal side, and p-NPbeta glc appeared on the serosal side. Although p-NP beta-disaccharide, p-NP and p-NP glucuronide also appeared on the serosal side, their amounts were much lower than that of p-NPbeta glc. The amount of p-NPbeta glc transported to the serosal side was decreased in the presence of phloridzin (transport inhibitor of SGLT1) and in the absence of Na+ (a cosubstrate of SGLT1), indicating that p-NPbeta glc was formed from p-NP beta-disaccharide on the mucosal side and transported to the serosal side by SGLT1. Furthermore, the absorption clearance of p-NPbeta glc, which was formed from p-NP beta-cellobioside and p-NP beta-lactoside by lactase-phloridzin hydrolase (LPH), was much higher than that of p-NPbeta glc itself, although the absorption clearance of p-NPbeta glc, which was formed from p-NP beta-maltoside by maltase was similar to that of p-NPbeta glc itself. These results indicated that p-NPbeta glc was transported by the vectorial cooperation of SGLT1 with LPH from mucosal p-NP beta-cellobioside or p-NP beta-lactoside.
对硝基苯酚(对硝基苯基β-二糖)的β-二糖(纤维二糖、麦芽糖和乳糖)共轭物的肠道吸收,根据二糖共轭物水解为单糖共轭物以及单糖共轭物通过Na⁺/葡萄糖转运载体(SGLT1)的转运情况进行了研究。对硝基苯酚的β-纤维二糖苷、β-麦芽糖苷和β-乳糖苷在黏膜侧水解为对硝基苯基β-葡萄糖苷(p-NPβglc),且p-NPβglc出现在浆膜侧。虽然对硝基苯酚β-二糖、对硝基苯酚和对硝基苯酚葡糖醛酸也出现在浆膜侧,但其量远低于p-NPβglc。在根皮苷(SGLT1的转运抑制剂)存在以及无Na⁺(SGLT1的共底物)的情况下,转运至浆膜侧的p-NPβglc量减少,这表明p-NPβglc是在黏膜侧由对硝基苯酚β-二糖形成,并通过SGLT1转运至浆膜侧。此外,由乳糖酶-根皮苷水解酶(LPH)作用于对硝基苯酚β-纤维二糖苷和对硝基苯酚β-乳糖苷形成的p-NPβglc的吸收清除率,远高于p-NPβglc本身的吸收清除率,尽管由麦芽糖酶作用于对硝基苯酚β-麦芽糖苷形成的p-NPβglc的吸收清除率与p-NPβglc本身的相似。这些结果表明,p-NPβglc是通过SGLT1与LPH从黏膜侧的对硝基苯酚β-纤维二糖苷或对硝基苯酚β-乳糖苷的向量协同作用进行转运的。