Diprotin A is an inhibitor of DPP-IV. Diprotin A induces phosphorylation of Src[Tyr 416] and VE-cadherin[Tyr731] and disrupts endothelial cell-cell junctions in human endothelial cells under normoxic and H/R conditions after treatment with a CXCR4 receptor blocker or Src inhibitor at a concentration of 100 μM for 30 min, whereas CXCR4 (SDF-1α receptor) blockers or Src inhibitors attenuate this effect[1].
Diprotin A 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Canine skeletal muscle-derived cells
5 mM
2 hours
To evaluate the inhibitory effect of Diprotin A on CD26/DPP-IV activity, results showed that Diprotin A significantly inhibited the production of p-nitroaniline.
Skelet Muscle. 2012 Feb 16;2(1):4
Canine bone marrow cells
5 mM
2 hours
To evaluate the inhibitory effect of Diprotin A on CD26/DPP-IV activity, results showed that Diprotin A significantly inhibited the production of p-nitroaniline.
Skelet Muscle. 2012 Feb 16;2(1):4
Flk22CD341 ST-HSCs
20 μM
15 minutes
Inhibition of CD26/DPPIV activity enhanced the migration of Flk22CD341 ST-HSCs
Blood Adv. 2022 Aug 9;6(15):4373-4391
Flk22CD342 LT-HSCs
20 μM
15 minutes
Inhibition of CD26/DPPIV activity enhanced the migration of Flk22CD342 LT-HSCs
Blood Adv. 2022 Aug 9;6(15):4373-4391
mouse dorsal root ganglia (DRG) neurons
10 µM
24 to 48 hours
To evaluate the impact of Diprotin A on neurite outgrowth of DRG neurons, results showed Diprotin A significantly increased neurite length
Int J Mol Sci. 2024 Aug 15;25(16):8881
human umbilical vein endothelial cells (HUVECs)
10 mM
6 hours
To investigate the effect of DPP4 activity inhibition on endothelial Tissue Factor expression and platelet adhesion. Results showed that diprotin A significantly increased Tissue Factor expression and induced platelet adhesion under flow conditions.
Basic Res Cardiol. 2012 Jan;107(1):233
human plasma
1 mM
60 minutes
To evaluate the effect of Diprotin A on the degradation of GRH(1-44)-NH2. Results showed that Diprotin A significantly reduced the conversion of GRH(1-44)-NH2 to GRH(3-44)-NH2.
J Clin Invest. 1989 May;83(5):1533-40
Diprotin A 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Irradiated bone marrow transplantation model
Tail vein injection
20 μM
Single dose, analyzed at 10, 18, and 30 days post-transplantation
Pretreatment with Dip A significantly enhanced the engraftment of Flk22CD342 LT-HSCs in recipient mice
Blood Adv. 2022 Aug 9;6(15):4373-4391
NOD/SCID mice
Muscle regeneration model
Intramuscular injection
5 mM
Single injection, observed for 4 weeks
To evaluate the effect of Diprotin A on donor cell engraftment and proliferation, results showed that Diprotin A significantly increased the number of fibers expressing canine dystrophin, the number of nuclei expressing canine lamin A/C, and the number of Pax7/canine lamin A/C double-positive nuclei.
Skelet Muscle. 2012 Feb 16;2(1):4
Rat
Isolated perfused rat heart
Perfusion
100 μM
Single application
Inhibition of dipeptidylaminopeptidase IV (DPAP) activity, reducing [4-9]-BK generation and causing accumulation of the intermediate product [2-9]-BK
Br J Pharmacol. 1997 Nov;122(6):1179-87
Diprotin A 动物研究
Animal study
Administered intraperitoneally twice daily for 7 days at a dose of 70 μg/kg, Diprotin A increases phosphorylation of Src and VE-cadherin and exacerbates vascular leakage in the retina by potentiating the SDF-1α/CXCR4/Src/VE-cadherin signalling pathway[1].
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