Drug Discov Ther. 2013;7(6):248-253. (DOI: 10.5582/ddt.2013.v7.6.248)

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

Hu CL, Peng XZ, Tang YP, Liu YW


SUMMARY

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.


KEYWORDS: Synthesis of peptides of Carapax Trionycis, hepatic stellate cells, extracellular matrix (ECM), TGF-β/Smad

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