PGPIPN

Key Benefits#

• Anti-inflammatory effects via cytokine suppression
• Gut mucosal protection and intestinal barrier support
• Opioid receptor modulation for gut motility regulation
• Potential analgesic activity via central and peripheral opioid pathways
• Explored for inflammatory bowel conditions and gut dysbiosis
• Natural origin (food-derived) with favorable safety profile

Mechanism of Action#

PGPIPN interacts with mu- and delta-opioid receptors in the gastrointestinal tract and centrally, contributing to gut motility modulation and potential analgesia. It inhibits pro-inflammatory cytokines including TNF-alpha and IL-6, likely via NF-kappaB pathway suppression. Its proline-rich structure confers resistance to digestive proteases, allowing intact peptide to reach the gut and potentially the systemic circulation for bioavailability.

Dosing Protocols#

Side Effects#

• Generally very well-tolerated given food-derived origin
• Theoretical opioid-mediated constipation at high doses
• Rare milk protein allergy in casein-sensitive individuals

Contraindications#

Casein or milk protein allergyCaution with concurrent opioid medications (additive mu-receptor activity)Pregnancy: insufficient data at pharmacological doses

Storage#

Lyophilized: store at -20 degrees C. Oral formulations: room temperature in sealed, moisture-free container. Stable in acidic conditions (gastric environment).

1. 1.
   Bioactive Hexapeptide Reduced the Resistance of Ovarian Cancer Cells to DDP by Affecting HSF1/HSP70 Signaling Pathway

   Guo R, Xu Q, Liu L, Liu H, Liu Y, Wei W et al. · Journal of Cancer · 2021PubMed Verified

2. 2.
   Milk‑derived hexapeptide PGPIPN prevents and attenuates acute alcoholic liver injury in mice by reducing endoplasmic reticulum stress

   Xu Q, Xi H, Chen X, Xu Y, Wang P, Li J et al. · International journal of molecular medicine · 2020PubMed Verified

3. 3.
   Therapeutic hexapeptide (PGPIPN) prevents and cures alcoholic fatty liver disease by affecting the expressions of genes related with lipid metabolism and oxidative stress

   Qi N, Liu C, Yang H, Shi W, Wang S, Zhou Y et al. · Oncotarget · 2017PubMed Verified

4. 4.
   Construction of an Anticancer Fusion Peptide (ACFP) Derived from Milk Proteins and an Assay of Anti-ovarian Cancer Cells in vitro

   Zhou J, Yang X, Zhang W, Wang J, Wei C, Gu F et al. · Anti-cancer agents in medicinal chemistry · 2017PubMed Verified

5. 5.
   The milk-derived hexapeptide PGPIPN inhibits the invasion and migration of human ovarian cancer cells by regulating the expression of MTA1 and NM23H1 genes

   Zhao M, Wei C, Yang X, Zhou J, Wang J, Gu F et al. · International journal of oncology · 2016PubMed Verified

6. 6.
   PGPIPN, a therapeutic hexapeptide, suppressed human ovarian cancer growth by targeting BCL2

   Wang W, Gu F, Wei C, Tang Y, Zheng X, Ren M et al. · PloS one · 2013PubMed Verified