A synthetic hexapeptide (Argireline) with antiwrinkle activity

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.

Acetyl hexapeptide-3 in a cosmetic formulation acts on skin mechanical properties - clinical study

“…It is concluded that acetyl hexapeptide-3 is an effective anti-aging compound as already mentioned by Blanes-Mira et al (2002). The author, using silicone replicas, observed that topical application of an emulsion containing the peptide attenuated the depth of wrinkles in the periocular region after 30 days of treatment, when compared with the vehicle.…”

“…An in vitro study demonstrated that acetyl hexapeptide-3 inhibits neurotransmitter release with a potency similar to that of botulinum neurotoxin, although as expected, it displayed much lower efficacy than the neurotoxin (Sivilia et al, 2008;Blanes-Mira et al, 2002).…”

“…Acetyl hexapeptide-3 has been used in anti-aging topical formulations due to its effects in improving the skin appearance (Blanes-Mira et al, 2002;Zhang, Falla, 2009). However there are few basic studies about its effects on skin, as well as, about its mechanism of action.…”

Anti-Aging Cosmetics Approaches and Components in Products

“…Etki mekanizması üzerinde yapılan çalışmalar heksapeptitlerinBotulinum nörotoksinlerine (BoNT) benzer şekilde nörotransmitter salımını inhibe ettiklerini ancak etkisinin çok daha düşük olduğunu göstermiştir. Sonuç olarak, elde edilen bulgular hekzapeptitlerin toksik olmadığı ve kırışıklık önleyici moleküller olduğunu kanıtlamıştır 57 . Matrikin kompleksi (Matrixyl ™ 3000); palmitoil oligopeptit ve palmitoiltetrapeptit-7 adlı iki matrikinin bileşiminden oluşmaktadır.…”

A botulinum neurotoxin-like function ofPotentilla chinensisextract that inhibits neuronal SNARE complex formation, membrane fusion, neuroexocytosis, and muscle contraction

“…Several peptide inhibitors have been developed for this purpose (Gutierrez et al, 1995(Gutierrez et al, , 1997Ferrer-Montiel et al, 1998;Cornille et al, 1995;Blanes-Mira et al, 2003Apland et al, 2003;Blanes-Mira et al, 2002;Jung et al, 2008). Most peptide inhibitors were screened from SNARE-patterned sequences.…”