The effects of linagliptin on fat content in diet-induced obese rats were compared with those of the appetite suppressant sibutramine. Female Wistar rats fed a high-fat diet (HFD) for 3 months received vehicle, linagliptin (10 mg/kg) or sibutramine (5 mg/kg) treatment orally, once daily for 6 additional weeks, while continuing the HFD. Magnetic resonance spectroscopy analysis of fat content was performed at baseline and at the end of the 6-week treatment period. Linagliptin treatment profoundly reduced hepatic fat compared with vehicle, with an effect comparable to that of sibutramine. The vehicle-corrected mean change (95% CI) from baseline in hepatic fat and intramyocellular lipid was -59.0% (-104.3%, -13.6%; p = 0.015) and -62.1% (-131.6%, 7.4%; p = 0.073), respectively, for linagliptin compared with -54.3% (-101.5%, -7.1%; p = 0.027) and -72.4% (-142.4%, -2.4%; p = 0.044), respectively, for sibutramine.
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http://dx.doi.org/10.1111/j.1463-1326.2012.01629.x | DOI Listing |
Diabetol Metab Syndr
January 2025
Bahrain Defence Force Royal Medical Services, Riffa, Kingdom of Bahrain.
Background: Dipeptidyl peptidase-4 inhibitors (DPP-4is) and drugs interfering with the renin-angiotensin-aldosterone system (RAAS) are frequently co-prescribed in type 2 diabetes management. Both drug classes have been independently associated with angioedema, raising concerns about potential interaction risks. This study aimed to evaluate the safety signals and interaction patterns for angioedema associated with DPP-4is alone and in combination with RAAS-interfering drugs.
View Article and Find Full Text PDFBiomed Pharmacother
January 2025
Department of Research, Mount Sinai Medical Center, Miami Beach, FL, USA. Electronic address:
Background: Excessive inflammation in sepsis causes microvascular dysfunction associated with organ dysfunction and high mortality. The present studies aimed to examine the therapeutic potential of linagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor in a clinically relevant polymicrobial sepsis model in mice.
Methods: Sepsis was induced by cecal ligation and puncture (CLP).
Eur J Med Chem
February 2025
Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Moga-142 001 (Punjab), India. Electronic address:
The inhibition of enzyme DPP-4 is pivotal for targeting type 2 diabetes mellitus (DM). The study introduces two series of novel 1,3-dimethyl-3,7-dihydro-1H-purine-2,6-diones derivatives (PB01-PB10) and 3,7-dihydro-1H-purine-2,6-diones compounds (PB11-PB16) were developed using linagliptin scaffold. Sixteen derivatives were synthesized and screened in vitro against DPP-4, revealing IC ranging from 15.
View Article and Find Full Text PDFFood Chem
March 2025
Division of Nutritional Sciences, University of Illinois at Urbana-Champaign, Champaign, IL 61801, USA; Department of Food Science and Human Nutrition, University of Illinois at Urbana-Champaign, Champaign, IL 61801, USA. Electronic address:
Adzuki bean (AB) is a legume with a low glycemic index and is traditionally used in Asian cultures to modulate type 2 diabetes (T2D). Our objectives were to characterize the functional peptides from purified AB β-vignin after simulated gastrointestinal digestion in comparison to soybean β-conglycinin, to evaluate their DPP IV inhibitory capacity, and to determine in vitro the effect of digested AB β-vignin on diabetic-related outcomes using HepG2 cells in healthy and insulin-resistant states. Five peptides (215-742 Da) from AB β-vignin and five peptides (215-447 Da) from β-conglycinin were identified to exhibit bioactivity as DPP IV inhibitors.
View Article and Find Full Text PDFInt Immunopharmacol
January 2025
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Cairo University, 11562, Egypt. Electronic address:
In recent years, special attention has been paid to highlighting the antiparkinsonian effect of linagliptin. However, the mechanism of its action has not yet been well investigated. The present study aimed to verify the neuroprotective effect of linagliptin in the rotenone model of Parkinson's disease (PD) and further explore its potential molecular mechanisms.
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