Synthesis and biological evaluation of novel analogues of Gly-l-Pro-l-Glu (GPE) as neuroprotective agents

Add time:09/09/2019    Source:sciencedirect.com

This study investigated the anti-inflammatory effects of novel pseudotripeptides (GPE 1–3) as potential candidates to counteract neuroinflammation processes in Alzheimer’s disease.GPE 1–3 pseudotripeptides are synthetic derivatives of Gly-l-Pro-l-Glu (GPE), the N-terminal tripeptide of IGF-1, obtained through the introduction of isosteres of the amidic bond (aminomethylene unit) to increase the metabolic stability of the native tripeptide. The results showed that all synthetic derivatives possessed higher half-lives (t1/2 > 4 h) than GPE (t1/2 = 30 min) in human plasma and had good water solubility. The biological results demonstrated that GPE 1–3 had protective properties in several experimental models of treated THP-1 cells. Notably, the novel pseudotripeptides influenced inflammatory cytokine expression (IL-1β, IL-18, and TNF-α) in Aβ25–35-, PMA-, and LPS-treated THP-1 cells. In PMA-differentiated THP-1 macrophages, both GPE 1 and GPE 3 reduced the expression levels of all selected cyto-chemokines, even though GPE 3 showed the best neuroprotective properties.

We also recommend Trading Suppliers and Manufacturers of GLY-PRO-GLY-GLY (cas 13054-03-0). Pls Click Website Link as below: cas 13054-03-0 suppliers

Prev:Increased central adiposity is associated with pro-inflammatory immunoglobulin G N-glycans
Next:Effects of rambutan (Nephelium lappaceum) peel phenolics and Leu-Ser-Gly-Tyr-Gly-Pro on hairless mice skin photoaging induced by ultraviolet irradiation)