SNAP — 8 (Acetil Octapéptido — 1 yá Acetil Octapéptido — 3) ge 'nar péptido sintético da contiene 'nar secuencia 8 — aminoácidos da imita ar proteína SNAP — 25.
ge 'nar nt'ot'e extendida ar Acetil Hexapéptido — 8 (Argirelina®)ho̲ntho alargado ko yoho aminoácidos Nthuts'i – alanina ne ácido aspártico pa mejorar nzäm'bu ne antiarrugas efecto1.
ár diseño ar modelado ir nge ar estructura N — terminal ar Synaptosome asociado proteína — 25 (SNAP — 25), funcionando imitando nuna ar estructura ne compitiendo ir nge ár nt'o̲t'e mbo jar complejo SNARE.
Komongu ar toxina botulínica klase A (Botox), SNAP — 8 reduce contracciones musculares involuntarias 'nar bí atenuada, ne ar gi japu̲'be̲fi pa da mä 'met'o nte líneas finas ne arrugas.
Secuencia
Ac-Glu-Glu-Met-Gln-Arg-Arg-Ala-Asp — NH2
'bede ya CAS
868844-74-0
Fórmula molecular
C₄₁H₇₀N₁₆O₁₆S
Be̲xu molecular
1075.16
SNAP — 8 relacionados ár nthoni
1.Ts'o̲e fisiológico: Molecular Basis of Neuromuscular Contraction
Under normal physiological conditions, the neurotransmisor responsible for contraction of facial expression muscles is acetilcolina(ACh).
This is dependent on a protein complex called SNARE (Soluble N-ethylmaleimide-sensitive factor Attachment protein REceptor).
The complex is composed of a triad of proteins including SNAP-25 and Syntaxin at the presynaptic membrane, and VAMP on the vesicle membrane.
When these three forms assemble properly, they create a stable “molecular zippper” that pulls the vesicles containing acetylcholine towards the presynaptic membrane, where they fuse and release neurotransmitter into synapse’s cleft to cause muscle contraction.
2.Anti-wrinkle Mechanism of SNAP-8
Anti-wrinkle Mechanism of SNAP-8 The anti-wrinkle activity of SNAP-8 is also based on its competition with the SNARE complex2.
More specifically, the process is as follows:
(1).Competitive Inhibition
The amino acid sequence of SNAP-8 is patterned after the N — terminal region of the SNAP-25 protein.
So when SNAP-8 enters the skin and comes into contact with terminal nerve endings it can “mimic” itself as a section of the SNAP-25 protein, and in competition take up the space that would usually be claimed by SNAP-25 in the SNARE complex.
This prevents the complete assembly of the SNARE complex with its partner proteins such as Syntaxin and VAMP3.
(2).Blockade of Neurotransmitter Release
The conformational instability of the SNARE complex triggered by SNAP-8 binding results in a poor efficiency of vesicle fusion with the presynaptic membrane, so that acetylcholine is released at radically reduced levels.
Nerve transmissions are weakened, which means less contraction signals are sent to facial muscles and thus muscle relaxation occurs.
This relaxing of the muscle leads toward a depth and length in expression lines (crow’s feet, forehead, glabellar), which can be avoided to prevent new-wrinkles.
In vitro studies have demonstrated that 1.5 mM SNAP-8 can inhibit 43% of glutamate release, and it can decrease the depth of wrinkles caused by wrinkle-inducing agents by an estimated 30–62% in clinical trials4.
(3).Synergy Amplification
In vitro evaluations reveal that SNAP-8 and Leuphasyl work independently but collaboratively on synergism.
They shared inhibitory activities of 38% ne 7%, respectively, in relevant inhibition assays.
When tested simultaneously at equimolar doses (0.75 mM), the maximal inhibition was 47%2.
3.Experimental and Clinical Research Evidence
Research Lipotec S.A.U. Ar fabricante SNAP — 8, xi publicado nsadi pa proporcionar evidencia ár rendimiento.
ya experimentos in vitro demuestran SNAP — 8 ndi inhibir parcialmente ar formación complejo SNARE ne estabilizar liberación ar acetilcolina.
ja ya nsadi clínicos in vivo, ar evaluación ya técnicas komongu ar análisis réplica silicona 'mefa xta nt'ot'e ya formulaciones ko SNAP — 8 Nxoge 'nar período pa resultó ja 'nar reducción significativa jar profundidad arrugas ('nar máximo 63.13% bí registrado ja 'nar estudio).
Nuya resultados o̲t'e ar ndui evidencia comercial directa ar nt'ot'e antiarrugas ar SNAP — 8.
4.Comparación mecanicista ko ar toxina botulínica klase A
Ar nt'ot'e mbo ya nt'ot'e SNAP — 8 ar na similar jar ar ar toxina botulínica klase A (BoNT yá A).
Ambos pe̲ts'i jar común da actúan dige ar complejo SNARE.
Pe ar diferencia básica te̲ni komongu ar nt'ot'e ne Ntsuni.
BoNT/A is a protease that causes irreversible cleavage of SNAP-25 protein and thus totally eliminates the activity of the SNARE complex.
Whereas SNAP-8 does its work by competing, results in the inhibition of exocytosis which is both reversible and less severe.
BoNT/A is an injectable drug which carries risks such as nerve paralysis and stiffness of the face, for which proper doctor should be responsible.
SNAP — 8, wat'i, is used topically and affects only the epidermis and dermis rather than being administered through an injection,and therefore involve no associated risks, furthermore more convenient.
This makes it a highly convenient and safer alternative.
5.Conclusion and Outlook
In conclusion, as an emerging active ingredient in cosmetic industry, SNAP-8 shows good anti-wrinkle activity by acting on release (chemo/exocytosis) of neurotransmitter acetylcholine, wherein it has been verified to reduce the formation of SNARE complex competitively with SNAP-25 thereby blocking glutamate release and reducing muscle contraction.
This concept is similar to Botulinum Toxin but provides a non-invasive approach.
The skin permeation and efficacy of such peptides is thought to be further enhanced by technologies such as nanoencapsulation6.
COA
HPLC
MS
