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- Title
Linagliptin Has Wide-Ranging Anti-Inflammatory Points of Action in Human Umbilical Vein Endothelial Cells.
- Authors
Yuya Nakamura; Masahiro Inagaki; Mayumi Tsuji; Toshihiko Gocho; Kazuaki Handa; Hitomi Hasegawa; Akihiko Yura; Tomoko Kawakami; Isao Ohsawa; Yoshikazu Goto; Hiromichi Gotoh; Yuji Kiuchi
- Abstract
BACKGROUND: Because of the potential anti-inflammatory effects, linagliptin, a therapeutic dipeptidyl peptidase-4 inhibitor, is used as an effective drug for diabetic patients for whom inflammation is a prognosis-related factor. We investigated the anti-inflammatory mechanism of linagliptin using seven markers. METHODS: We pretreated human umbilical vein endothelial cells (HUVECs), with linagliptin and lipopolysaccharide (LPS). The cytosolic fractions were evaluated for protein kinase A (PKA), protein kinase B (PKB), protein kinase C (PKC), ratio of reactive oxygen species (ROS) and Cu/Zn superoxide dismutase (SOD), activator protein 1 (AP-1), and adenosine 3',5'-cyclic monophosphate (cAMP). RESULTS: Linagliptin increased the PKA and PKC activities and the cAMP levels in LPS-treated cells. However, it inhibited LPS-induced PKB phosphorylation, ratio of ROS and Cu/Zn SOD, and LPS-stimulated AP-1 nuclear translocation. CONCLUSION: We reaffirmed the anti-inflammatory and antioxidant effects of linagliptin. These effects might be related to the three protein kinases. Our findings suggest that linagliptin has a wide range of anti-inflammatory effects.
- Subjects
ANTI-inflammatory agents; INFLAMMATION; ENDOTHELIAL cells; UMBILICAL veins; OXIDATIVE stress
- Publication
Japanese Clinical Medicine, 2016, Issue 7, p27
- ISSN
1179-6707
- Publication type
Article
- DOI
10.4137/JCM.S39317