Melanotan-I (MT-I), ko fiye daidai [Nle4,D-Phe7]-α-MSH, analog na α-MSH (melanocyte-stimulating hormone). Tridecapeptide madaidaiciya, yana inganta melanin samuwar ta hanyar zaɓin kunnawa Saukewa: MC1R (melanocortin-1 mai karɓa).
Shaidar gwaji tana goyan bayan bayananta marasa guba da marasa cutar kansa, duka a cikin vivo kuma a cikin nau'ikan in vitro daban-daban. Idan aka kwatanta da α-MSH na halitta, Melanotan-I yana da tsawon rabin rayuwa; an yi nasarar sayar da shi a cikin Tarayyar Turai.
Jeri
Ac-Ser-Tyr-Ser-Nle-Glu-His-D-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH₂
Lambar CAS
75921-69-6
Tsarin kwayoyin halitta
Saukewa: C78H111N21O19
Nauyin Kwayoyin Halitta
1646.85
Binciken Melanotan-I
The melanocortin tsarin ya ƙunshi masu karɓa daban-daban guda biyar (Saukewa: MC1-R Saukewa: MC5-R), peptides na melanocortin da aka ambata a baya (Proopiomelanocortin/POMC peptides da aka samu), kuma biyu endogenous antagonists.
Melanotan-I yana zaɓin ɗaure zuwa kuma yana kunna mai karɓa na farko, Saukewa: MC1R. Ainihin jerin (His-Phe-Arg-Trp) ke da alhakin wannan takamaiman hulɗar.
Kunna mai karɓa yana kaiwa zuwa cikin salula adenosine monophosphate cyclic (cAMP) da duk mai biyo baya PKA-hanyoyin dogaro; melanin-synthesizing enzymes (tyrosinase shine babban misali) a ƙarshe suna ƙaruwa cikin aiki.
Ƙara eumelanin samarwa a cikin fata yana haifar da ingantaccen pigmentation – shinge mai ban sha'awa amma mai kima da kariya daga ultraviolet da shigar hasken da ake iya gani. Haɓaka nau'ikan iskar oxygen da ke haifar da UV (DNA, furotin, da lalacewar lipid) An kuma yi imanin cewa eumelanin ne ya shiga tsakani.
Melanotan-I ya yi mafi girman tasirin kariya akan haɓaka wannan takamaiman eumelanin na kariya. Gwajin makafi biyu ya auna sigogi daban-daban na kariya ta hoto; ƙananan abubuwan da ke da wuyar kunar rana a jiki sun karɓa 3 hawan keke na subcutaneous injections.
Yawan melanin fata ya ƙaru kamar yadda aka ambata a baya, kuma an rage yawancin kwayoyin cutar kumburin rana. Kariyar kariya, aƙalla zuwa matsayi mai mahimmanci, muhimmiyar maƙasudin ƙarshen bayyanar fatar ɗan adam zuwa UVR.
Melanotan-I yana haifar da pigmentation na fata EPP(Erythropoietic Protoporphyria) marasa lafiya, yana rage jin daɗin gani kuma daga baya yana rage ciwon fata da ke hade da shi.; tarin na'urar daukar hoto, Protoporphyrin IX, yana haifar da wannan ji na gani ga haske.
Binciken buɗaɗɗen lakabin da ke tafe 4 an gudanar da watanni a kan batutuwa biyar na EPP; Melanotan-I na subcutaneous an gudanar da shi a Rana 7 da Mako 8. Idan aka kwatanta da asali, an auna yawan melanin na fata, tare da ingantaccen haɓakar haƙuri ga haɓakar haske – ƙayyadaddun ma'aunin da aka yi amfani da shi shine 'lokacin da za a kai ga zafin da ba za a iya jurewa ba’ karkashin haske.
U.S. Gudanar da Abinci da Magunguna (FDA) tabbatattun Scenesse (afamelanotide), nau'in halittar Melanotan-I na yanzu, saboda wannan manufa.
Nazarin preclinical sun nuna ƙarancin guba (ba a lura da cutar sankara ba kamar yadda aka nuna a cikin in vitro da duk waɗanda aka gwada a cikin vivo samfuran.
Ingantacciyar shigar da gagarumin pigmentation na fata yana ɗaya daga cikin ingantaccen ingantaccen tasirin Melanotan-I; nau'in fata mara kyau na hoto (kusa da cikakken tanning gazawar kasancewa ƙarshen batu) amfana sosai da shi.
Rage martanin mai guba na fata ga radiation ultraviolet shine gaskiya, sakamakon da ake so na duk wannan – kunar rana da kuma lahani masu alaƙa sun ragu, a kalla partially, by Melanotan-I.
COA
HPLC
MS
