肠道钠/葡萄糖共转运体（SGLT1）对氨肽酶抗性纤维二糖偶联酪氨酰甘氨酰甘氨酸的转运与识别：SGLT1对糖结合物的识别比对其转运的限制要少得多。

Transport and recognition of aminopeptidase-resistant cellobiose-coupled tyrosylglycylglycine by intestinal Na+/glucose cotransporter (SGLT1): recognition of sugar conjugates by SGLT1 is much less restricted than transport.

作者信息

Mizuma T, Sakai N, Hagi K, Awazu S

机构信息

Department of Biopharmaceutics and Drug Rational Research Center, School of Pharmacy, Tokyo University of Pharmacy and Life Science, Hachioji, Japan.

出版信息

Biol Pharm Bull. 1999 Aug;22(8):876-9. doi: 10.1248/bpb.22.876.

DOI:10.1248/bpb.22.876

PMID:10480331

Abstract

Transport and recognition of aminopeptidase-resistant cellobiose-coupled tyrosylglycylglycine (CcpTGG) by intestinal Na+/glucose cotransporter (SGLT1) was examined in rat small intestine. Inhibitory effect of phloridzin (SGLT1 inhibitor) on the CcpTGG transport was extremely low. Concentration dependence of the CcpTGG transport was observed, but the primary component of transport was passive diffusion. However, CcpTGG significantly inhibited SGLT1-mediated transport, indicating its recognition by SGLT1. Other glucose-conjugates also inhibited SGLT1-mediated transport. These results indicate that recognition of sugar conjugates by SGLT1 is much less restricted than transport, and that it should be relatively easier to design SGLT1 inhibitors than SGLT1-transportable sugar conjugates.

摘要

在大鼠小肠中检测了氨基肽酶抗性纤维二糖偶联酪氨酰甘氨酰甘氨酸（CcpTGG）被肠道钠/葡萄糖共转运体（SGLT1）转运和识别的情况。根皮苷（SGLT1抑制剂）对CcpTGG转运的抑制作用极低。观察到CcpTGG转运的浓度依赖性，但转运的主要成分是被动扩散。然而，CcpTGG显著抑制SGLT1介导的转运，表明它被SGLT1识别。其他葡萄糖结合物也抑制SGLT1介导的转运。这些结果表明，SGLT1对糖结合物的识别比转运受到的限制要少得多，并且设计SGLT1抑制剂应该比设计可被SGLT1转运的糖结合物相对更容易。