Study summary · research use only
A synthetic hexapeptide (Argireline) with antiwrinkle activity
Plain-language summary
Paraphrased from the published abstract below — not a verdict on whether anything works.
In this study, the authors examined a synthetic hexapeptide, Ac-EEMQRR-NH2 (Argireline), with reported antiwrinkle activity, using human volunteers and in vitro mechanistic assays. They describe designing a non-toxic molecule to mimic botulinum neurotoxins. Skin topography analysis of an oil/water emulsion containing 10% of the hexapeptide on healthy women reduced wrinkle depth up to 30% after 30 days. Mechanistic analysis showed Argireline inhibited neurotransmitter release with a potency the authors describe as similar to botulinum neurotoxin A, though with much lower efficacy than the neurotoxin; the abstract attributes this to interference with the SNARE vesicular fusion complex required for Ca2+-dependent exocytosis. The authors state the peptide did not exhibit oral toxicity or primary irritation at high doses, and describe it as a biosafe alternative to botulinum neurotoxins in cosmetics.
Abstract
Botulinum neurotoxins (BoNTs) represent a revolution in cosmetic science because of their remarkable and long-lasting antiwrinkle activity. However, their high neurotoxicity seriously limits their use. Thus, there is a need to design and validate non-toxic molecules that mimic the action of BoNTs. The hexapeptide Ac-EEMQRR-NH(2) (coined Argireline) was identified as a result of a rational design programme. Noteworthy, skin topography analysis of an oil/water (O/W) emulsion containing 10% of the hexapeptide on healthy women volunteers reduced wrinkle depth up to 30% upon 30 days treatment. Analysis of the mechanism of action showed that Argireline significantly inhibited neurotransmitter release with a potency similar to that of BoNT A, although as expected, it displayed much lower efficacy than the neurotoxin. Inhibition of neurotransmitter release was due to the interference of the hexapeptide with the formation and/or stability of the protein complex that is required to drive Ca(2+)-dependent exocytosis, namely the vesicular fusion (known as SNARE) complex. Notably, this peptide did not exhibit in vivo oral toxicity nor primary irritation at high doses. Taken together, these findings demonstrate that Argireline is a non-toxic, antiwrinkle peptide that emulates the action of currently used BoNTs. Therefore, this hexapetide represents a biosafe alternative to BoNTs in cosmetics.
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