Sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors are the current focus on the indication for the management of hyperglycemia in diabetes. Here, a novel series of C-linked indolylxyloside-based inhibitors of SGLT2 has been discovered. Structure-activity relationship studies revealed that substituents at the 7-position of the indole moiety and a p-cyclopropylphenyl group in the distal position were necessary for optimum inhibitory activity. The pharmacokinetic study demonstrates that the most potent compound 1i is metabolically stable with a low clearance in rats. In further efficacy study, 1i is found to significantly lower blood glucose levels of streptozotocin (STZ)-induced diabetic rats.
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Aims: To compare the effects of ipragliflozin, a sodium-dependent glucose transporter-2 inhibitor, and those of metformin on the visceral fat area (VFA), a prospective, multi-centre, open-label, blinded-endpoint, randomized, controlled study was undertaken. The generated data were used to examine the effects of ipragliflozin and metformin on indices of hepatic steatosis and liver fibrosis.
Materials And Methods: In total, 103 Japanese patients with type-2 diabetes (T2D), body mass index (BMI) of ≥22 kg/m and glycated haemoglobin level of 7%-10% were randomly administered ipragliflozin 50 mg or metformin 1000 mg for 24 weeks.
Immunolocalization of sodium-dependent glucose co-transporter 1 and sodium-dependent glucose co-transporter 2 in chicken's (Gallus gallus domesticus) kidneys.
Pol J Vet Sci
September 2024
Chair of Veterinary Biomedicine and Food Hygiene, Institute of Veterinary Medicine and Animal Sciences, Estonian University of Life Sciences, Kreutzwaldi Str.62, Tartu 51006, Estonia.
In homeostasis, which plays an important role in the proper functioning and maintenance of the internal functioning of the body, kidneys play a key role in being responsible for the proper homeostasis of glucose. Among glucose transporters, sodium-dependent glucose co-transporters (SGLTs) have a major role in the kidney's ability to reabsorb glucose. Although the localization of these transporters has been extensively studied in mammals, there are still gaps in knowledge of the localization of SGLTs in birds of different age groups.
View Article and Find Full Text PDFSodium-dependent glucose transporter 2 inhibitors: Transforming diabetic cardiomyopathy management.
World J Cardiol
December 2024
Department of Biochemistry, School of Medicine, College of Medicine, China Medical University, Taichung 404328, Taiwan.
This article addresses the substantial findings of a study on sodium-dependent glucose transporter 2 inhibitors (SGLT2is) and their effects on myocardial function in patients with type 2 diabetes and asymptomatic heart failure. The editorial explores the broader implications of the study findings for clinical practice, thus highlighting the pivotal role of SGLT2is in improving cardiac function, reducing oxidative stress, and attenuating inflammation. It emphasizes the importance of early intervention with SGLT2is in preventing the progression of diabetic cardiomyopathy; hence, these inhibitors have the potential to transform the management of asymptomatic heart failure in patients with diabetes.
View Article and Find Full Text PDFImmunolocalization of Na(+)-Dependent Glucose Co-Transporters in Chicken Kidneys in Norm and During T-2 Mycotoxicosis (Primary Study).
Curr Issues Mol Biol
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Faculty of Veterinary Medicine, Ss. Cyril & Methodius University in Skopje, 1000 Skopje, North Macedonia.
The kidney plays an essential role in the proper homeostasis of glucose. In the kidney, glucose transport is carried out across cell membranes by two families of glucose transporters-facilitated diffusion glucose transporters (GLUTs) and Na(+)-dependent glucose co-transporters (SGLT family). Among the transporters, sodium-dependent glucose co-transporters play a major role in the kidney's ability to reabsorb glucose.
View Article and Find Full Text PDFEffect of the SGLT2 inhibitor ipragliflozin on the expression of genes that regulate skin function.
Diabet Med
December 2024
Department of Biomolecular Pharmacology, Hoshi University, Tokyo, Japan.
Aims: Skin disorders occur more frequently with sodium-dependent glucose cotransporter type 2 (SGLT2) inhibitors than with other antidiabetic drugs. We conducted basic research using ipragliflozin, with the aim of identifying new measures to prevent skin disorders caused by SGLT2 inhibitors.
Methods: db/db type 2 diabetes model mice were orally administered ipragliflozin (10 mg/kg or 30 mg/kg) once a day for 28 days and skin function genes were analysed by real-time RT-PCR or Western blotting.
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