SEHLOOHO-8 (Acetyl Octapeptide-1/Acetyl Octapeptide-3) ke peptide ea maiketsetso e nang le tatellano ea 8-amino-acid e etsisang protheine SNAP-25..
Ke mofuta o atolositsoeng oa Acetyl Hexapeptide-8 (Argireline®)e kopantsoe le li-amino acid tse peli feela – alanine le aspartic acid ho ntlafatsa botsitso le phello e khahlanong le wrinkle1.
Moralo oa eona o entsoe ka sebopeho sa N-terminal ea Synaptosome-associated protheine - 25 (SEHLOOHO 25), ho sebetsa ka ho etsisa sebopeho sena le ho qothisana lehlokoa le boemo ba sona ka hare ho SNARE e rarahaneng.
Joalo ka mofuta oa chefo ea botulinum A (Botox), SNAP-8 e fokotsa ho honyela ha mesifa ho sa ikemisetseng ka mokhoa o fokolang, 'me e sebelisetsoa ho thibela nts'etsopele ea mela e metle le wrinkles.
Tatelano
Ac-Glu-Glu-Met-Gln-Arg-Ala-Asp-NH2
Nomoro ea CAS
868844-74-0
Foromo ea limolek'hule
C₄₁H₇₀N₁₆O₁₆S
Boima ba Molek'hule
1075.16
Lipatlisiso tse amanang le SNAP-8
1.Semelo sa Fisioloji: Motheo oa Limolek'hule oa Neuromuscular Contraction
Tlas'a maemo a tloaelehileng a fisioloji, the neurotransmitter e ikarabellang bakeng sa ho honyela ha mesifa ea sefahleho ke acetylcholine(ACh).
Sena se itšetlehile ka protheine complex e bitsoang SNARE (Soluble N-ethylmaleimide-sensitive factor Attachment protein Receptor).
E rarahaneng e entsoe ka liprotheine tse tharo tse kenyelletsang SNAP-25 le Syntaxin ho lera la presynaptic, le VAMP ho vesicle lera.
Ha mefuta ena e meraro e kopana hantle, ba etsa setala “zipper ea molek'hule” e hulang li-vesicle tse nang le acetylcholine ho leba lera la presynaptic, moo ba kopanyang le ho lokolla neurotransmitter ho kena lekhalo la synapse ho baka tsitsipano ya mesifa.
2.Mokhoa o khahlanong le wrinkles oa SNAP-8
Anti-wrinkle Mechanism ea SNAP-8 Ts'ebetso ea anti-wrinkle ea SNAP-8 e boetse e thehiloe tlholisanong ea eona le SNARE complex2..
Ka ho toba, mokhoa ona o tjena:
(1).Thibelo ea Tlholisano
Tatelano ea amino acid ea SNAP-8 e entsoe ka mor'a N-terminal sebaka sa protheine ea SNAP-25.
Kahoo ha SNAP-8 e kena letlalong 'me e kopana le lipheletsong tsa methapo ea kutlo e ka khona “etsisa” ka boeona e le karolo ea protheine ea SNAP-25, 'me tlhōlisanong ba nke sebaka seo hangata se neng se tla tsekoa ke SNAP-25 sebakeng sa SNARE complex.
Sena se thibela kopano e feletseng ea SNARE complex le liprotheine tsa molekane oa eona tse kang Syntaxin le VAMP3.
(2).Thibelo ea Phallo ea Neurotransmitter
Ho se tsitse ha komporo ea SNARE e bakiloeng ke tlamo ea SNAP-8 ho fella ka ts'ebetso e mpe ea fusion ea vesicle le membrane ea presynaptic., e le hore acetylcholine e lokolloe maemong a fokotsehileng haholo.
Phetiso ea methapo ea fokola, e bolelang hore matšoao a fokolang a fokolang a romelloa mesifa ea sefahleho 'me kahoo ho phomola ha mesifa ho etsahala.
Ho phutholoha hona ha mesifa ho lebisa botebong le bolelele meleng ea polelo (maoto a lekhoaba, phatla, glabellar), e ka qojoang ho thibela maqeba a macha.
Lithuto tsa in vitro li bontšitse seo 1.5 mM SNAP-8 e ka thibela 43% ho lokolloa ha glutamate, 'me e ka fokotsa botebo ba mats'ope a bakoang ke li-ajenti tse hlohlelletsang mats'otsu ka 30-62% litekong tsa bongaka..
(3).Synergy Amplification
Litlhahlobo tsa in vitro li senola hore SNAP-8 le Leuphasyl li sebetsa ka boikemelo empa li sebelisana 'moho mabapi le synergism..
Ba ne ba kopanela mesebetsi e thibelang ho 38% le 7%, ka ho latellana, litekong tse amehang tsa thibelo.
Ha e lekoa ka nako e le 'ngoe ka litekanyetso tse lekanang (0.75 mM), thibelo e kholo e ne e 47%2.
3.Bopaki ba Lipatlisiso tsa Boiteko le Bongaka
Lipatlisiso tsa Lipotec S.A.U. moetsi oa SNAP-8, ba hatisitse lithuto ho fana ka bopaki ba ts'ebetso ea eona.
Liteko tsa in vitro li bonts'a SNAP-8 e ka thibela sebopeho se rarahaneng sa SNARE le ho tsitsisa tokollo ea acetylcholine..
Lithutong tsa kliniki tsa in vivo, tlhahlobo ea mekhoa e kang silicone replica analysis ka mor'a ts'ebeliso ea liforomo le SNAP-8 ka nako e ile ea fella ka phokotso e kholo ea botebo ba wrinkles. (boholo 63.13% e tlalehiloe thutong e le 'ngoe).
Liphetho tsena li emela bopaki ba pele bo tobileng ba khoebo ba ts'ebetso ea SNAP-85 e khahlanong le wrinkle.
4.Papiso ea Mechini le Mofuta oa Toxin oa Botulinum A
Mokhoa oa ts'ebetso oa SNAP-8 o ts'oana haholo le oa Mofuta oa A oa Chefo ea Botulinum (BONT/A).
Ka bobeli li tšoana ka hore li sebetsa ho SNARE complex.
Empa phapang ea mantlha e ntse e le ts'ebetsong le ts'ireletso.
BoNT/A ke protease e bakang karohano e ke keng ea fetoloa ea protheine ea SNAP-25 mme ka hona e felisa ts'ebetso ea moetso oa SNARE.
Athe SNAP-8 e etsa mosebetsi oa eona ka tlholisano, ho fella ka thibelo ea exocytosis eo e ka kgutlisetswang morao ebile e fokola haholo.
BoNT/A ke sethethefatsi se entang se nang le likotsi tse kang ho holofala ha methapo le ho satalla sefahleho., eo ngaka e nepahetseng e lokelang ho ikarabella ho eona.
SEHLOOHO-8, leha ho le joalo, e sebelisoa ka lihlooho 'me e ama feela epidermis le dermis ho e-na le ho tsamaisoa ka ente,mme ka hona ha e akarelletse likotsi tse amanang le tsona, ho feta moo ho loketseng haholoanyane.
Sena se etsa hore e be khetho e bonolo le e sireletsehileng haholoanyane.
5.Qetello le Outlook
Ha re phethela, e le karolo e hlahang e sebetsang indastering ea litlolo, SNAP-8 e bonts'a ts'ebetso e ntle ea anti-wrinkle ka ho nka khato ha e lokolloa (chemo/exocytosis) ka neurotransmitter acetylcholine, moo ho netefalitsoeng ho fokotsa sebopeho sa SNARE e rarahaneng ka tlholisano le SNAP-25 ka tsela eo e thibela ho lokolloa ha glutamate le ho fokotsa ho hlaka ha mesifa..
Khopolo ena e tšoana le Botulinum Toxin empa e fana ka mokhoa o sa hlaseleng.
Ho kenella ha letlalo le ho sebetsa ha li-peptide tse joalo ho nahanoa hore li matlafatsoa le ho feta ke mahlale a kang nanoecapsulation6..
COA
HPLC
MOF
