KPV - 5MG

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KPV - 5MG
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Product Overview

KPV Peptide

KPV (Lys–Pro–Val) is a tripeptide derived from the C-terminus of α-MSH with potent anti-inflammatory and mucosal-healing actions. KPV primarily inhibits NF-κB and MAPK signaling, lowering pro-inflammatory cytokine secretion in epithelial and immune cells. It is actively transported via PepT1, which is upregulated in the inflamed colon—focusing activity to diseased tissue.[1]

Mechanism & Cellular Uptake

  • Suppresses NF-κB/MAPK pathways → ↓ TNF-α, IL-1β, other cytokines in gut epithelium and immune cells.[1,2,4,5]
  • PepT1-mediated entry enhances epithelial uptake during IBD flares (PepT1 upregulated).[1]
  • Anti-inflammatory activity partly melanocortin-receptor independent → minimal pigmentary effects versus α-MSH.[2,4,5]

Efficacy in Colitis & Mucosal Healing

  • DSS/TNBS colitis (mice): oral/rectal KPV ↓ histologic inflammation, cytokines, and MPO; improves weight recovery and mucosal repair.[1–3]
  • Oral mucositis: mucoadhesive KPV hydrogels reduce inflammation/bacterial burden and promote epithelial repair.[6]

Broader Anti-Inflammatory Applications

  • Peritonitis and other sterile inflammation models: ↓ neutrophil infiltration and pro-inflammatory mediators.[4]
  • Vascular disease: carrier-free KPV nanodrugs show anti-inflammation and anti-calcification effects in preclinical models.[8]

Formulation & Delivery

  • Hydrogel encapsulation improves peptide stability, mucosal retention, and in vivo efficacy in colitis.[3,6]
  • Transdermal strategies (iontophoresis/microneedles, microporated skin) enable enhanced delivery across human skin.[7]

Safety

  • KPV and derivatives (e.g., (CKPV)2) show a favorable preclinical safety profile with no significant cytotoxicity or pigmentary effects reported.[2,4,5,9]

Key Takeaways

  • Targeted gut delivery: PepT1-guided epithelial uptake concentrates action in inflamed colon.
  • Multi-pathway anti-inflammation: NF-κB/MAPK inhibition plus cytokine reduction and epithelial repair.
  • Translational flexibility: oral/rectal hydrogels and transdermal systems broaden therapeutic options.

References

  1. Dalmasso G, Charrier-Hisamuddin L, Nguyen HT, et al. Gastroenterology. 2008;134(1):166-178. doi:10.1053/j.gastro.2007.10.026.[1]
  2. Kannengiesser K, Maaser C, Heidemann J, et al. Inflamm Bowel Dis. 2008;14(3):324-331. doi:10.1002/ibd.20334.[2]
  3. Sun J, Xue P, Liu J, et al. ACS Biomater Sci Eng. 2021;7(10):4859-4869. doi:10.1021/acsbiomaterials.1c00792.[3]
  4. Getting SJ, Schiöth HB, Perretti M. J Pharmacol Exp Ther. 2003;306(2):631-637. doi:10.1124/jpet.103.051623.[4]
  5. Brzoska T, Böhm M, Lügering A, et al. Adv Exp Med Biol. 2010;681:107-116. doi:10.1007/978-1-4419-6354-3_8.[5]
  6. Shao W, Chen R, Lin G, et al. Biomater Sci. 2021;10(1):227-242. doi:10.1039/d1bm01466h.[6]
  7. Pawar K, Kolli CS, Rangari VK, Babu RJ. J Pharm Sci. 2017;106(7):1814-1820. doi:10.1016/j.xphs.2017.03.017.[7]
  8. Zhang L, Li D, Aierken Y, et al. Adv Healthc Mater. 2024;13(32):e2402320. doi:10.1002/adhm.202402320.[8]
  9. Gatti S, Carlin A, Sordi A, et al. J Surg Res. 2006;131(2):209-214. doi:10.1016/j.jss.2005.08.009.[9]

All information provided is for research purposes only.

ALL ARTICLES AND PRODUCT INFORMATION PROVIDED ON THIS WEBSITE ARE FOR INFORMATIONAL AND EDUCATIONAL PURPOSES ONLY. The products offered on this website are furnished for in-vitro studies only. In-vitro studies (Latin: in glass) are performed outside of the body. These products are not medicines or drugs and have not been approved by the FDA to prevent, treat or cure any medical condition, ailment or disease. Bodily introduction of any kind into humans or animals is strictly forbidden by law.