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Animal study · 2008 · cited for KPV, GHK-Cu + BPC-157 + TB-500 + KPV

PepT1-mediated tripeptide KPV uptake reduces intestinal inflammation

Dalmasso G, Charrier-Hisamuddin L, Nguyen HT, Yan Y, Sitaraman S, Merlin D. Gastroenterology 2008;134(1):166-78. doi:10.1053/j.gastro.2007.10.026 · PubMed 18061177

In brief

KPV is the three-residue C-terminal fragment of alpha-MSH (Lys-Pro-Val) and is anti-inflammatory, but how it enters cells was unknown. This paper shows that it uses PepT1, a transporter of small peptides that is normally confined to the small intestine and is switched on in the colon during inflammatory bowel disease. In intestinal epithelial cells and Jurkat T cells stimulated with pro-inflammatory cytokines, nanomolar KPV blocked activation of NF-κB and MAP-kinase signalling and reduced cytokine secretion, and competition experiments showed uptake through PepT1. In mice with colitis induced by DSS or TNBS, KPV given orally in drinking water reduced inflammation on histology and lowered inflammatory cytokine messenger RNA.

Study design

Human intestinal epithelial and T-cell lines exposed to inflammatory cytokines with or without KPV, plus two chemically induced colitis models in mice with KPV in drinking water.

What it does not show

Cell lines and chemically induced colitis in mice, with KPV taken by mouth. The oral route and the induced-colitis models are specific to this experiment and do not describe any other route or condition.

Results in rodents or other animals often do not reproduce in people. Species, route, dose and the injury or disease model all shape the outcome, and an effect in a rat is a reason for further study, not a conclusion.

Where this paper is cited

  • KPV — KPV is taken up by the PepT1 transporter in intestinal epithelial cells and reduced inflammation in two mouse colitis models.
  • GHK-Cu + BPC-157 + TB-500 + KPV — KPV is taken up by the PepT1 transporter in intestinal epithelial cells and reduced inflammation in two mouse colitis models.

Other papers cited for KPV and GHK-Cu + BPC-157 + TB-500 + KPV

Further reading

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