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Báo cáo y học: "Thioglycosides as inhibitors of hSGLT1 and hSGLT2: Potential therapeutic agents for the control of hyperglycemia in diabetes"

Tuyển tập các báo cáo nghiên cứu khoa học ngành y học tạp chí Medical Sciences dành cho các bạn sinh viên ngành y tham khảo đề tài: Thioglycosides as inhibitors of hSGLT1 and hSGLT2: Potential therapeutic agents for the control of hyperglycemia in diabetes. | Int. J. Med. Sci. 2007 4 131 Research Paper International Journal of Medical Sciences ISSN 1449-1907 www.medsci.org 2007 4 3 131-139 Ivyspring International Publisher. All rights reserved Thioglycosides as inhibitors of hSGLTl and hSGLT2 Potential therapeutic agents for the control of hyperglycemia in diabetes Francisco Castaneda1 Antje Burse2 Wilhelm Boland2 Rolf K-H. Kinne1 1. Laboratory for Molecular Pathobiochemistry and Clinical Research Max Planck Institute of Molecular Physiology Dortmund Germany 2. Max Planck Institute for Chemical Ecology Dortmund Germany Correspondence to Francisco Castaneda MD Laboratory for Molecular Pathobiochemistry and Clinical Research Max Planck Institute for MolecUlar Physiology Otto-Hahn-Str. 11 44227 Dortmund Germany Tel. 49-231-9742-6490 Fax. 49-231-133-2699 E-mail francisco.castaneda@mpi-dortmund.mpg.de Received 2007.04.14 Accepted 2007.04.30 Published 2007.05.05 The treatment of diabetes has been mainly focused on maintaining normal blood glucose concentrations. Insulin and hypoglycemic agents have been used as standard therapeutic strategies. HoWever these are characterized by limited efficacy and adverse side effects making the development of new therapeutic alternatives mandatory. Inhibition of glucose reabsorption in the kidney mediated by SGLT1 or SGLT2 represents a promising therapeutic approach. Therefore the aim of the present study was to evaluate the effect of thioglycosides on human SGLT1 and SGLT2. For this purpose stably transfected Chinese hamster ovary CHO cells expressing human SGLT1 and SGLT2 were used. The inhibitory effect of thioglycosides was assessed in transport studies and membrane potential measurements using a-methyl-glucoside uptake and fluorescence resonance energy transfer respectively. We found that some thioglycosides inhibited hSGLT more strongly than phlorizin. Specifically thioglycoside I phenyl-1 -thio-P-D-glucopyranoside inhibited hSGLT2 stronger than hSGLT1 and to a larger extent than .