A synthetic hexapeptide (Argireline) with antiwrinkle activity
Open accessAbstract
Synopsis: 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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In a split-face controlled study of ten healthy subjects with little photodamaged skin, 10% Argireline significantly reduced rhytide depth after 30 days compared with vehicle lotion.
“The authors found that compared to the control, 10% Argireline can significantly reduce rhytide depth after 30 days of treatment (Level IIb Evidence).”
From Cosmeceuticals in photoaging: A review. (2024) · cites this paper as [45]
The ‘Antiwrinkle test on healthy humans’ section describes ten healthy women applying 10% Argireline to one side of the face and the base emulsion to the other for 30 days. ‘Argireline attenuates wrinkle depth in vivo in healthy volunteers’ reports significantly reduced wrinkle depth with Argireline and no significant topographic change with the base emulsion. Our copy does not describe the volunteers as having little photodamaged skin. (LLM, conf=0.85)
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Flagged first, then by citations
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- Authors
- Blanes‐Mira, C., Clemente, J., Jodas, G., Gil, A., Fernández‐Ballester, G., Ponsati, B., Gutierrez, L., Pérez‐Payá, E., & Ferrer‐Montiel, A.
- Affiliations
- Universitat de Miguel Hernández d'Elx (ES)
- Lipotec (Spain) (ES)
- Universitat de València (ES)
- Venue
- International Journal of Cosmetic Science
- Publisher
- Wiley
- Published
- 2002-10
- Volume
- 24
- Issue
- 5
- Pages
- 303-310
- ISSN
- 0142-5463 (ISSN-L)
- 1468-2494
- OpenAlex
- W2144640136
- Cited by
- 187
- References
- 13
- Citations by year
- 2026: 16 · 2025: 12 · 2024: 11 · 2023: 14 · 2022: 11 · 2021: 13 · 2020: 12 · 2019: 8 · 2018: 7 · 2017: 7 · 2016: 7 · 2015: 10 · 2014: 4 · 2013: 11 · 2012: 7
- FWCI
- 1.11
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- International Journal of Cosmetic Science (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Neurology › Botulinum Toxin and Related Neurological Disorders
- Health Sciences › Medicine › Dermatology › Facial Rejuvenation and Surgery Techniques
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Venomous Animal Envenomation and Studies
- Keywords
- hexapeptide, botulinum toxin, neurotransmitter release inhibition, SNARE complex, wrinkle depth, skin topography, cosmetic safety, rational peptide design
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