Systemic Anti-inflammatory Effects of Linagliptin in Type 2 Diabetes

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Linagliptin 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].” 

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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.