Synthesis of peptides of Carapax Trionycis and their inhibitory effects on TGF-β1–induced hepatic stellate cells

Abstract

We previous identified the antifibrotic active ingredients from Carapax Trionycis as two peptides. Here, we synthesized these two peptides (peptide 1 and peptide 2) by a solid phase method and examined their effects on proliferation and activation of cultured hepatic stellate cells (HSC) which are the main ECM (extracellular matrix)-producing cells in fibrosis progression. We demonstrated that peptide 1 and peptide 2 significantly reduced HSC proliferation and activation in a dose dependent manner. Further, peptide 1 and peptide 2 could interfere with TGF-signaling by down-regulating Smad 3 phosphorylation. Thus, these synthetic peptides of Carapax Trionycis could inhibit proliferation and activation of HSC and might be used as a candidate for treatment of liver fibrosis.

A Novel Matrine Derivative WM130 Inhibits Activation of Hepatic Stellate Cells and Attenuates Dimethylnitrosamine-Induced Liver Fibrosis in Rats

“…Activation of hepatic stellate cells (HSCs) is acknowledged as a critical event in process of hepatic fibrosis [ 2 ]. Hepatocyte damage caused by a variety of pathogenic factors can lead to the high expression of growth-stimulating factors, such as transforming growth factor- β (TGF- β ), platelet-derived growth factor (PDGF), endothelin (ET), fibroblast growth factor (FGF), connective tissue growth factor (CTGF), and leptin [ 3 ].…”