Table 1
Open in new tab

Impact of gliptin treatment on endothelial function

CategoryActive substanceResults
In vitro (aortic segments of C57Bl/6 mice)15AlogliptinAlogliptin incubation-mediated dose-dependent relaxation of the aortic segments, whereas GLP1 pre-incubation had no effect. Endothelial denudation and addition of LNMMA reduced the effect of Alogliptin incubation
In vitro (aortic segments of ApoE-ko mice)9Des-Fluoro-Sitagliptin (DFS, 200 mg/kg/day)Aortic segments of DFS-treated mice on high-fat diet showed an improved vascular function and significant higher eNOs phosphorylation after stimulation with acetylcholine
In vitro (Wistar rats)48Linagliptin (83 mg/kg)The LPS-induced vascular dysfunction of rat aortic segments was significantly improved by Linagliptin treatment (e.g. reduced oxidative burst and suppressed attachment of human neutrophils on activated endothelial cells)
Clinical trial (10 volunteers; 10 days)28Alogliptin (25 mg/day)Alogliptin significantly improved post-prandial endothelial function (increased FMD) and post-prandial lipaemia in healthy volunteers
Clinical trial (31 D.m.2 patients with insufficient blood glucose control, EDGE study; 12 weeks)49Sitagliptin (50 mg/day)Sitagliptin treatment improved FMD, several blood parameters (e.g. cholesterol, HDL, lipids, GLP1, GIP, HbA1, and inflammatory markers), and the number of circulating CD34+ cells
CategoryActive substanceResults
In vitro (aortic segments of C57Bl/6 mice)15AlogliptinAlogliptin incubation-mediated dose-dependent relaxation of the aortic segments, whereas GLP1 pre-incubation had no effect. Endothelial denudation and addition of LNMMA reduced the effect of Alogliptin incubation
In vitro (aortic segments of ApoE-ko mice)9Des-Fluoro-Sitagliptin (DFS, 200 mg/kg/day)Aortic segments of DFS-treated mice on high-fat diet showed an improved vascular function and significant higher eNOs phosphorylation after stimulation with acetylcholine
In vitro (Wistar rats)48Linagliptin (83 mg/kg)The LPS-induced vascular dysfunction of rat aortic segments was significantly improved by Linagliptin treatment (e.g. reduced oxidative burst and suppressed attachment of human neutrophils on activated endothelial cells)
Clinical trial (10 volunteers; 10 days)28Alogliptin (25 mg/day)Alogliptin significantly improved post-prandial endothelial function (increased FMD) and post-prandial lipaemia in healthy volunteers
Clinical trial (31 D.m.2 patients with insufficient blood glucose control, EDGE study; 12 weeks)49Sitagliptin (50 mg/day)Sitagliptin treatment improved FMD, several blood parameters (e.g. cholesterol, HDL, lipids, GLP1, GIP, HbA1, and inflammatory markers), and the number of circulating CD34+ cells

LNMMA, N-Monomethyl-L-arginine.

Table 1
Open in new tab

Impact of gliptin treatment on endothelial function

CategoryActive substanceResults
In vitro (aortic segments of C57Bl/6 mice)15AlogliptinAlogliptin incubation-mediated dose-dependent relaxation of the aortic segments, whereas GLP1 pre-incubation had no effect. Endothelial denudation and addition of LNMMA reduced the effect of Alogliptin incubation
In vitro (aortic segments of ApoE-ko mice)9Des-Fluoro-Sitagliptin (DFS, 200 mg/kg/day)Aortic segments of DFS-treated mice on high-fat diet showed an improved vascular function and significant higher eNOs phosphorylation after stimulation with acetylcholine
In vitro (Wistar rats)48Linagliptin (83 mg/kg)The LPS-induced vascular dysfunction of rat aortic segments was significantly improved by Linagliptin treatment (e.g. reduced oxidative burst and suppressed attachment of human neutrophils on activated endothelial cells)
Clinical trial (10 volunteers; 10 days)28Alogliptin (25 mg/day)Alogliptin significantly improved post-prandial endothelial function (increased FMD) and post-prandial lipaemia in healthy volunteers
Clinical trial (31 D.m.2 patients with insufficient blood glucose control, EDGE study; 12 weeks)49Sitagliptin (50 mg/day)Sitagliptin treatment improved FMD, several blood parameters (e.g. cholesterol, HDL, lipids, GLP1, GIP, HbA1, and inflammatory markers), and the number of circulating CD34+ cells
CategoryActive substanceResults
In vitro (aortic segments of C57Bl/6 mice)15AlogliptinAlogliptin incubation-mediated dose-dependent relaxation of the aortic segments, whereas GLP1 pre-incubation had no effect. Endothelial denudation and addition of LNMMA reduced the effect of Alogliptin incubation
In vitro (aortic segments of ApoE-ko mice)9Des-Fluoro-Sitagliptin (DFS, 200 mg/kg/day)Aortic segments of DFS-treated mice on high-fat diet showed an improved vascular function and significant higher eNOs phosphorylation after stimulation with acetylcholine
In vitro (Wistar rats)48Linagliptin (83 mg/kg)The LPS-induced vascular dysfunction of rat aortic segments was significantly improved by Linagliptin treatment (e.g. reduced oxidative burst and suppressed attachment of human neutrophils on activated endothelial cells)
Clinical trial (10 volunteers; 10 days)28Alogliptin (25 mg/day)Alogliptin significantly improved post-prandial endothelial function (increased FMD) and post-prandial lipaemia in healthy volunteers
Clinical trial (31 D.m.2 patients with insufficient blood glucose control, EDGE study; 12 weeks)49Sitagliptin (50 mg/day)Sitagliptin treatment improved FMD, several blood parameters (e.g. cholesterol, HDL, lipids, GLP1, GIP, HbA1, and inflammatory markers), and the number of circulating CD34+ cells

LNMMA, N-Monomethyl-L-arginine.

Close
This Feature Is Available To Subscribers Only

Sign In or Create an Account

Close

This PDF is available to Subscribers Only

View Article Abstract & Purchase Options

For full access to this pdf, sign in to an existing account, or purchase an annual subscription.

Close