Anti-inflammatory effects of linagliptin in diabetes patients

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Patients taking linagliptin had decreased HbA1c as well as reactive oxygen species generation and plasma lipid peroxide levels.
Patients taking linagliptin had decreased HbA1c as well as reactive oxygen species generation and plasma lipid peroxide levels.

Linagliptin has anti-inflammatory effects and suppresses CD26 expression in patients with well-controlled type 2 diabetes, according to a study presented at ENDO 2017: the 99th Annual Meeting & Expo, April 1-4, in Orlando, Florida.

Researchers from the State University of New York at Buffalo evenly divided 34 patients with type 2 diabetes into 2 groups to test the potential anti-inflammatory effects of linagliptin.

The first group was treated with linagliptin 5 mg daily, and the other was treated with placebo. Blood samples were collected before up to 6 hours after the first dose of linagliptin, and thereafter at 2, 6, and 12 weeks.

After a single dose of linagliptin, a suppression of reactive oxygen species generation by mononuclear (MNC) and polymorphonuclear (PMN) cells, and the expression of c-Jun N-terminal kinase 1 (JNK1) and CD26 in MNC, by 16%±6% and 15%±5%, respectively, was observed.

At 12 weeks, HbA1c in patients with type 2 diabetes decreased from 6.9%±0.2% to 6.5%±0.2%. Reactive oxygen species generation by PMN was reduced by 19%±6%, plasma lipid peroxide levels measured as thiobarbituric acid reactive substances (TBARS) decreased by 21%±8%, and nuclear factor kappa-light-chain-enhancer of activated B cells (NFκB binding in MNCs decreased by 14%±5% in fasting blood samples.

The expression of interleukin 1β and JNK1 had also significantly diminished by 32%±8% and 21%±9%, respectively, at 12 weeks.

After consuming a high-fat, high-calorie meal, patients treated with linagliptin had diminished reactive oxygen species generation by PMN and MNC, as well as JNK1 expression. Glucose excursion also decreased, and patients experienced a trend toward increased glucagon-like peptide-1 and insulin secretion.

"We conclude that linagliptin exerts an anti-inflammatory effect even in well controlled patients with type 2 diabetes," the researchers wrote. "In addition, it suppresses CD26 expression, the cellular equivalent of [dipeptidyl peptidase IV]." 

Reference

  1. Ghanim H, Batra M, Hejna J, et al. Linagliptin exerts an anti-inflammatory effect in well controlled patients with type 2 diabetes. Presented at: ENDO 2017: the 99th Annual Meeting & Expo; April 1-4, 2017; Orlando, FL. Abstract 80. 
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