The anti-wrinkle hexapeptide ARGIRELINE@ represents the discovery of a positive hit based on a scientific pathway from rational design to GMP production.
The study of the basic biochemical mechanisms of anti-wrinkle activity has led to this revolutionary hexapeptide which has taken the cosmetic world by storm.
Finally, an anti-wrinkle treatment which can compete with the efficacy of Botulinum Toxin but leaves aside the risks, the injections and the high cost: ARGIRELINE®.
One of the most striking signs of skin aging is increased wrinkling of the face. This can occur naturally over time and is identified by certain biochemical, histological and physiological changes that are enhanced by environmental exposure. There are other secondary factors that can cause characteristic folds, furrows and creases of the face. These include the constant pull of gravity, frequent and constant positional pressure of the skin of the face (e.g. during sleep) or repeated facial movements caused by the contraction of the muscles of facial expression. In any case and independently of the ultimate physiological pathway, the molecular mechanism involved in face aging is directly related to changes in the conformation of the collagen triple helix, degradation of the elastin polypeptides and certain disorder in the packing of the lipidic matrix of the skin. It has been clearly established that these conformational changes and the disturbance of the perfect packing of the lipid matrix can be significantly avoided by modulating muscle contraction.
Muscles are contracted when they receive neurotransmitter released from inside a vesicle. The SNARE (SNAp REceptor) complex is essential for this neurotransmitter release at the synapsis (A. Ferrer Montiel et al, The Journal of Biological Chemistry, 1997, 272, 2634-2638). It is a ternary complex formed by the proteins VAMP, Syntaxin and SNAP25 (SyNaptosomal Associated Protein). This complex is like a cellular hook which captures vesicles and fuses them with the membrane for the release of neurotransmitter.
ARGIRELINE® is a mimic of the N-terminal end of SNAP-25 which competes with SNAP-25 for a position in the SNARE complex, thereby modulating its formation. If the SNARE complex is slightly destabilized, the vesicle can not release neurotransmitters efficiently and therefore muscle contraction is attenuated, preventing the formation of lines and wrinkles (see Fig.1 below).