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  Thioglycosides as inhibitors of hSGLT1 and hSGLT2: Potential therapeutic agents for the control of hyperglycemia in diabetes

Castaneda, F., Burse, A., Boland, W., & Kinne, R.-K.-H. (2007). Thioglycosides as inhibitors of hSGLT1 and hSGLT2: Potential therapeutic agents for the control of hyperglycemia in diabetes. International Journal of Medical Sciences, 4(3), 131-139.

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Castaneda, Francisco, Author
Burse, Antje1, 2, Author              
Boland, Wilhelm2, Author              
Kinne, Rolf K-H., Author
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1Research Group Dr. A. Burse, Chemical Defense of Leaf Beetles, Department of Bioorganic Chemistry, Prof. Dr. W. Boland, MPI for Chemical Ecology, Max Planck Society, ou_543545              
2Department of Bioorganic Chemistry, Prof. Dr. W. Boland, MPI for Chemical Ecology, Max Planck Society, ou_24028              

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 Abstract: 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 alpha-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-beta-D-glucopyranoside) inhibited hSGLT2 stronger than hSGLT1 and to a larger extent than phlorizin. Thioglycoside VII (2-hydroxymethyl-phenyl-1'-thio-beta-D-galacto-pyranoside) had a pronounced inhibitory effect on hSGLT1 but not on hSGLT2. Kinetic studies confirmed the inhibitory effect of these thioglycosides on hSGLT1 or hSGLT2, demonstrating competitive inhibition as the mechanism of action. Therefore, these thioglycosides represent promising therapeutic agents for the control of hyperglycemia in patients with diabetes.

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 Dates: 2007-04-302007-05-052007
 Publication Status: Published in print
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 Identifiers: Other: BOL412
ISSN: 1449-1907
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Title: International Journal of Medical Sciences
Source Genre: Journal
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Publ. Info: Ivyspring International Publisher
Pages: - Volume / Issue: 4 (3) Sequence Number: - Start / End Page: 131 - 139 Identifier: ISSN: 1449-1907
CoNE: https://pure.mpg.de/cone/journals/resource/111088195230532