Effect of oligoarginine conjugation on the antiwrinkle activity and transdermal delivery of GHK peptide.
Hur. Ga-Hee GH; Han. Sang-Cheol SC; Ryu. A-Reum AR; Eom. Youngsic Y; Kim. Jhin-Wook JW; Lee. Mi-Young MY
Key Findings
- Conjugating Arg4 to GHK (creating GHK‑R4) dramatically speeds up cellular penetration in lab and animal tests.
- GHK‑R4 shows stronger anti‑wrinkle activity and stimulates more collagen than regular GHK at much lower doses.
- The Arg4 segment itself may help by acting as a cell‑penetrating tag and by inhibiting matrix metalloproteinases (MMPs).
Practical Outcomes
- If you can obtain a GHK‑R4 formulation, you may achieve skin‑repair benefits with a lower dose than standard GHK. Look for products that include cell‑penetrating sequences or consider DIY peptide synthesis with an Arg4 tag for enhanced anti‑aging skin effects.
Summary
Adding a short chain of four arginine residues (Arg4) to the skin‑helpful peptide GHK makes it get into skin cells faster and work better at lower amounts, boosting collagen production and reducing wrinkle‑related enzymes.
Abstract
GHK (Gly-His-Lys), a natural peptide found in human skin and plasma, has been widely used in the cosmeceutical and pharmaceutical fields. The hydrophilic GHK and GHK-Cu are limited in their abilities to penetrate deeply into skin; because of this, various strategies for their skin delivery have been developed. In this investigation, Arg<sub>4</sub> was conjugated with GHK to get heptapeptide, GHK-R4, and then in vitro antiwrinkle activity and transdermal delivery were compared between GHK and GHK-R4. Notably, Arg<sub>4</sub> conjugation accelerated the cellular penetration of GHK both in vitro and in vivo. Furthermore, higher in vitro antiwrinkle activity and collagen biosynthesis was obtained with GHK-R4 at much lower doses than with control R4-free GHK. The enhanced activity and delivery of GHK-R4 might be due to the cell penetrating ability and matrix metalloproteinase (MMP) inhibitory activity of R4 itself.
Study Information
pubmed
2019
2019-12-01T00:00:00.000Z
10.1002/psc.3234
10
22