大鼠外翻肠囊对N4-D-吡喃葡萄糖基磺胺二甲嘧啶的吸收

Absorption of N4-D-glucopyranosylsulphamethazine by rat everted intestinal sacs.

作者信息

Wang Y, Grigg R, McCormack A, Symonds H, Bowmer C

机构信息

Department of Pharmacology, University of Leeds, U.K.

出版信息

Biochem Pharmacol. 1993 Nov 17;46(10):1864-6. doi: 10.1016/0006-2952(93)90595-n.

DOI:10.1016/0006-2952(93)90595-n

PMID:8250974

Abstract

Absorption of the N4-D-glucose conjugate of sulphamethazine (glucose-SMZ, 0.5 mM) by isolated everted sacs of the rat small intestine was studied at 37 degrees and pH 6.6. Phlorizin (0.5-2.0 mM) significantly reduced (P < 0.05) both mucosal and serosal transfer of glucose-SMZ and inhibition of mucosal transfer appeared to be concentration-dependent. Phloretin (0.5 mM) and removal of Na+ from the incubation medium also diminished absorption of glucose-SMZ. Furthermore, D-glucose (0.5 and 5.0 mM) inhibited mucosal and serosal transfer of the glycoside. The results suggest the D-glucose/Na+ cotransporter mediates absorption of glucose-SMZ from the small intestine of the rat. Thus, glucose-SMZ might be bioavailable from ingested tissues in which it is present.

摘要

在37摄氏度和pH值为6.6的条件下，研究了磺胺二甲嘧啶的N4-D-葡萄糖共轭物（葡萄糖-磺胺二甲嘧啶，0.5 mM）被大鼠小肠分离外翻肠囊的吸收情况。根皮苷（0.5 - 2.0 mM）显著降低（P < 0.05）葡萄糖-磺胺二甲嘧啶的黏膜和浆膜转运，且对黏膜转运的抑制似乎呈浓度依赖性。根皮素（0.5 mM）以及从孵育培养基中去除Na+也减少了葡萄糖-磺胺二甲嘧啶的吸收。此外，D-葡萄糖（0.5和5.0 mM）抑制了糖苷的黏膜和浆膜转运。结果表明，D-葡萄糖/Na+共转运体介导了葡萄糖-磺胺二甲嘧啶从大鼠小肠的吸收。因此，葡萄糖-磺胺二甲嘧啶可能从其存在的摄入组织中被生物利用。