I-Melanotan-I (MT-I), okanye ngokuchanekileyo [Nle4,D-Phe7]-α-MSH, yianalog ye α-MSH (ihomoni evuselela i-melanocyte). I-linear tridecapeptide, iyakhuthaza imelanin ukwakheka ngokuvula okukhethiweyo kwe I-MC1R (melanocortin-1 receptor).
Ubungqina bovavanyo buxhasa inkangeleko yayo engeyotyhefu kunye nengeyo-carcinogenic, zombini kwi-vivo nakwiimodeli ezahlukeneyo ze-vitro. Xa kuthelekiswa nendalo α-MSH, I-Melanotan-ndinesiqingatha sobomi obude kakhulu; ithengiswe ngempumelelo kwiManyano yaseYurophu.
Ulandelelwano
Ac-Ser-Tyr-Ser-Nle-Glu-His-D-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH₂
Inombolo yeCAS
75921-69-6
Ifomula yeemolekyuli
I-C78H111N21O19
Ubunzima beMolekyuli
1646.85
Uphando lweMelanotan-I
I melanocortin inkqubo iqulunqwe ii-receptors ezintlanu ezahlukeneyo (MC1-R nge I-MC5-R), i-melanocortin peptides ekhankanywe ngasentla (Proopiomelanocortin/POMC iipeptides ezifunyenweyo), kunye nesibini abachasi endogenous.
I-Melanotan-I ngokukhetha ibophelela kwaye isebenze i-receptor yokuqala, I-MC1R. Ulandelelwano olungundoqo (His-Phe-Arg-Trp) unoxanduva lolu nxibelelwano lukhethekileyo.
Ukusebenza kwe-receptor kukhokelela kwi-intracellular cyclic adenosine monophosphate (Inkampu) kwaye konke okulandelayo PKA-iindlela ezixhomekeke; i-melanin-synthesizing enzymes (tyrosinase ngumzekelo obalaseleyo) ekugqibeleni bayanda kumsebenzi.
Yandisiwe eumelanin ukuveliswa kolusu kubangela ukuba kubekho umbala ophucukileyo – isithintelo esiyingxenye kodwa esixabisekileyo ngokuchasene ne-ultraviolet kunye nokungena kokukhanya okubonakalayo. Ukucocwa kweentlobo zeoksijini ezisebenzayo ezibangelwa yi-UV (DNA, iprotheni, kunye nomonakalo we-lipid) Kukholelwa ukuba ilawulwa yi-eumelanin.
I-Melanotan-I yenze impembelelo enkulu yokukhusela ekunyuseni le eumelanin yokukhusela. Ulingo oluyimfama oluphindwe kabini lulinganisa iiparamitha ezahlukeneyo zokhuseleko lwefoto; kufunyenwe izifundo zokutshiswa lilanga okuphantsi 3 imijikelo yeenaliti ezingaphantsi kwesikhumba.
Ukuxinana kwe-melanin yolusu kunyukile njengoko bekutshiwo ngaphambili, and most epidermal sunburn cells were reduced. Photoprotection, at least to a significant degree, is an important end goal of human skin exposure to UVR.
Melanotan-I induces skin pigmentation in EPP(Erythropoietic Protoporphyria) izigulane, reducing photosensitivity and subsequently alleviating the associated skin pain.⁵ EPP itself is a rare genetic disorder; the accumulation of a photosensitizer, protoporphyrin IX, causes this sensitivity to visible light.
An open-label study spanning over 4 months was conducted on five EPP subjects; subcutaneous Melanotan-I implants were administered at Day 7 and Week 8. Compared to baseline, increases in skin melanin density were measured, along with significantly improved tolerance to light stimulation – the specific metric used being the ‘time to reach intolerable pain’ under illumination.
The U.S. Ulawulo lokutya kunye neziyobisi (I-FDA) Imeko evunyiweyo (afamelanotide), uhlobo lwangoku lweMelanotan-I implanti, ngenxa yale njongo kanye.
Uphononongo lwaphambi kweklinikhi lubonakalise ubutyhefu obusezantsi noko (Akukho kujongwa umhlaza njengoko kubonisiwe kwi-vitro kunye nazo zonke ezivavanyiweyo kwiimodeli ze-vivo.
Ukungeniswa okusebenzayo kombala obalulekileyo wolusu yenye yezona ziphumo zibhalwe kakuhle zeMelanotan-I.; iintlobo zolusu ezingathathi ntweni (kufutshane nokusilela okupheleleyo kolusu kuba sisiphelo) zuza lukhulu kuyo.
Ukunciphisa impendulo yetyhefu yolusu kwimitha ye-ultraviolet yinyani, isiphelo esinqwenelekayo sayo yonke le nto – ukutshiswa lilanga kunye nomonakalo onxulumeneyo uyancitshiswa, ubuncinane ngokuyinxenye, nguMelanotan-I.
I-COA
HPLC
NKSK
