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▎ Melanotan-1 Ọdịdị
Isi mmalite: PubChem |
Usoro: Ser-Tyr-Ser-Nle-Glu-His-D-Phe-Arg-Trp-Gly-Lys-Pro-Val Ụdị mkpụrụ ndụ: C 78H 111N 21O19 Arọ molekụla: 1646.8g/mol Nọmba CAS: 75921-69-6 PubChem CID: 16154396 Ụdị okwu: Afamelanotida; NDP-MSH |
▎ Melanotan-1 Nnyocha
Kedu ihe ndabere nyocha nke Melanotan-1?
Melanotan-1 bụ analog sịntetik nke α-melanocyte-stimulating hormone (α-MSH). A na-emepụta α-MSH site na mkpụrụ ndụ ụfọdụ n'ime ahụ mmadụ ma na-arụ ọrụ dị mkpa na usoro physiological dị ka pigmenti. Iji nyochaa ngwa ya na mpaghara dị iche iche, ndị nchọpụta mepụtara Melanotan-1. Nnyocha miri emi na α-MSH mere ka ọmụmụ Melanotan-1 pụta. A maara α-MSH ka ọ na-ekere òkè dị mkpa n'ịkwalite mmepụta nke melanin, yana Melanotan-1 e mere ka ọ nwee ike ịrụ ọrụ siri ike na ọrụ ndị a kapịrị ọnụ, dị ka ịcha akpụkpọ anụ na mmetụta photoprotective pụrụ iche [1] .
Gịnị bụ Melanotan-1?
Melanotan-1 bụ analọg sịntetik nke α-melanocyte na-akpali akpali. Site na ijikọ na MC1R na melanocytes, ọ na-akpali melanocytes imepụta melanin. O gosiputara nrụpụta dị ukwuu na ọgwụgwọ erythropoietic protoporphyria ma nweekwa atụmanya ngwa n'ịgwọ ọrịa anụ ahụ ndị ọzọ.
Melanotan-1 nwere njirimara nke mmetụta na-adịte aka. Ọ nwere ike na-akpali melanocytes n'ime ahụ ka ọ mepụta melanin, si otú a na-enye mmetụta ọgwụgwọ ogologo oge. E jiri ya tụnyere usoro ọgwụgwọ ndị ọzọ, Melanotan-1 anaghị achọ nchịkwa ugboro ugboro, na-ebelata ibu ọgwụgwọ na ndị ọrịa. Na nyocha ụlọ ọgwụ, Melanotan-1 egosila ezigbo nchekwa. Mmeghachi omume ọjọọ ndị a na-ahụkarị gụnyere isi ọwụwa, ọgbụgbọ, ọgbụgbọ, wdg, mana ha na-adịkarị nwayọọ ma nwee ike nweta ahụ efe site na ọgwụgwọ kwesịrị ekwesị. Na mgbakwunye, Melanotan-1 nwere obere nsị na akụkụ ahụ dị mkpa dị ka imeju na akụrụ, na-enye ụfọdụ nkwa nchekwa maka ngwa ụlọ ọgwụ ya.
Kedu usoro a kapịrị ọnụ nke Melanotan-1 na-egbochi mmebi anyanwụ?
Melanin na akpụkpọ ahụ na-ekere òkè n'inweta ụzarị ultraviolet na radicals efu, si otú a na-echebe akpụkpọ ahụ pụọ na mmebi ultraviolet. Ụzarị ultraviolet nwere ike ime ka mmụgharị dị na mkpụrụ ndụ ihe nketa nke mkpụrụ ndụ akpụkpọ ahụ ma bụrụ isi ihe na-akpata ọrịa cancer akpụkpọ anụ dị iche iche. Ọnụnọ nke melanin nwere ike ibelata mkpughe nke ụzarị ultraviolet na mkpụrụ ndụ akpụkpọ ahụ ma belata ohere nke mmụgharị mkpụrụ ndụ ihe nketa. Mgbe akpụkpọ ahụ gbasasịrị na ụzarị ultraviolet, ọ ga-eme ka ọrụ nke melanocyte na-eme ka ndị na-anabata hormone na-akpali akpali, na-eme ka eumelanin na-abawanye na melanocytes epidermal. Dị ka ihe analog nke α-melanocyte-stimulating hormone, Melanotan-1 nwere ike iṅomi usoro a ma kwalite mmepụta nke melanin [2] . Site n'ịba ụba ọdịnaya melanin na akpụkpọ ahụ, Melanotan-1 nwere ike belata mmebi nke ụzarị ultraviolet na sel akpụkpọ ahụ. Nnyocha e mere egosiwo na mgbe ejiri Melanotan-1 mee ihe, a na-eme ka ntachi obi anụ ahụ na ụzarị ultraviolet dịkwuo elu, na njedebe nke ntachu na-ebelata. E jiri ya tụnyere usoro tanning ọdịnala dị ka ntanye anwụ na iji ngwaahịa tanning, Melanotan-1 nwere ụfọdụ uru pụrụ iche. Nchacha anwụ na-achọ ikpughe ogologo oge na anyanwụ, nke nwere ike ịkpata ntachu anụ ahụ, ịka nká, yana ohere dị ukwuu nke ọrịa kansa anụ ahụ. Ojiji nke tanning ngwaahịa nwere ike inwe nsogbu dị ka mgbakasị ahụ akpụkpọ na allergies nke ihe kemịkal kpatara. Melanotan-1, site na ntụtụ subcutaneous, nwere ike ịchịkwa mmepụta nke melanin nke ọma ma belata mmetụta ọjọọ na akpụkpọ ahụ.
Kedu usoro a kapịrị ọnụ nke Melanotan-1 na ọgwụgwọ vitiligo?
Mmepụta melanin na-akpali akpali: Melanotan-1 nwere ike ime ka melanocytes mepụta melanin. Melanin bụ ihe dị mkpa na-ekpebi agba akpụkpọ. N'ime ndị ọrịa nwere vitiligo, n'ihi melanocytes mebiri emebi ma ọ bụ nke na-adịghị mma, akwa ọcha na-apụta na akpụkpọ ahụ. Melanotan-1 na-akwalite mmụba na ọdịiche nke melanocytes ma na-abawanye njikọ nke melanin site n'ịgbalite ụzọ mgbaàmà kpọmkwem [3]..
Ịchịkwa usoro ahụ ji alụso ọrịa ọgụ: A na-ewere Vitiligo dị ka ọrịa autoimmune, nke usoro ahụ ji alụso ọrịa ọgụ na-awakpo melanocytes n'ụzọ na-adịghị mma. Melanotan-1 nwere ike ịrụ ọrụ n'ịhazi usoro ahụ ji alụso ọrịa ọgụ na ibelata ọgụ na melanocytes. Ọ nwere ike ịhazi nzaghachi mgbochi ahụ site n'ịmetụta ọrụ na ọrụ nke mkpụrụ ndụ na-alụso ọrịa ọgụ, si otú a na-ewepụ ihe mgbaàmà nke vitiligo.
Mmetụta Antioxidant: Nchegbu oxidative na-arụkwa ọrụ dị mkpa na pathogenesis nke vitiligo. Melanotan-1 nwere ike ịnwe ụfọdụ ikike antioxidant ma belata mmebi nke nrụgide oxidative na melanocytes. Ọ nwere ike wepụ radicals free, chebe melanocytes site na mmebi oxidative, ma nyere aka ịnọgide na-arụ ọrụ nkịtị nke melanocytes.
Kedu data nyocha na-akwado mmetụta kpọmkwem nke Melanotan-1 na ọgwụgwọ erythropoietic protoporphyria?
Erythropoietic protoporphyria (EPP) bụ ọrịa metabolic porphyrin eketa nke ndị ọrịa na-enweta nnukwu mmeghachi omume phototoxic nke na-emetụta ụdị ndụ ha nke ukwuu. Dị ka ihe analog sịntetik nke hormone na-akpali akpali nke α-melanocyte, Melanotan-1 nwere data nyocha ndị a iji kwado mmetụta ya kpọmkwem na ọgwụgwọ EPP:
Ịkwalite nnabata ọkụ: N'ọtụtụ ọmụmụ ụlọ ọgwụ, Melanotan-1 egosila na ọ ga-eme ka ndị ọrịa EPP dịkwuo mma. Dịka ọmụmaatụ, na nnwale nke Phase III CUV039, ọgwụgwọ na Melanotan-1 mere ka ndị ọrịa EPP dịkwuo mfe. E jiri ya tụnyere placebo, ọgwụgwọ na Melanotan-1 nyere ndị ọrịa aka itinyekwu oge na ìhè anyanwụ na-enweghị mgbu ma mụbaa oge ruo mgbe mgbaàmà mbụ nke phototoxicity kpatara site na isi iyi ọkụ pụtara [4]. .
Imeziwanye ndụ ndụ: Ọtụtụ nchọpụta egosila na ọgwụgwọ Melanotan-1 nwere ike imeziwanye ndụ ndụ nke ndị ọrịa EPP. N'ime ule ụlọ ọgwụ dị iche iche, mgbe ị nwetasịrị ọgwụgwọ Melanotan-1, a na-enyocha ụdị ndụ ndị ọrịa site na iji akwụkwọ ajụjụ ndị a kwadoro, na nsonaazụ gosipụtara ọganihu na ndụ ndụ [4]..
Mmetụta nchebe na ọrụ imeju: Nnyocha achọpụtala na Melanotan-1 nwere ike inwe mmetụta nchebe na ọrụ imeju nke ndị ọrịa EPP. N'ime nyocha nlegharị anya n'azụ, 2933 nyocha ọrụ imeju, 1186 protoporphyrin ule nyocha, na 1659 Melanotan-1 ngwa ntinye nke ndị ọrịa 70 EPP gụnyere. Nsonaazụ gosiri na dị ka ọnụ ọgụgụ nke ụbọchị ebe ọ bụ na ikpeazụ Melanotan-1 implant mụbara, protoporphyrin (PPIX) ịta ụbara nke ukwuu (p <0.0001); ebe n'ime ụbọchị 365 gara aga, ka Melanotan-1 dose na-abawanye, alanine aminotransferase (ALAT) na bilirubin belatara nke ukwuu (p = 0.012, p = 0.0299). Nke a na-egosi na Melanotan-1 nwere mmetụta nchebe na-adabere na dose na ọrụ imeju nke ndị ọrịa EPP [5] .
Mmekọrịta nke PPIX na parampat imeju. Eserese (A): Histogram (green) na-egosi nkesa data ụlọ nyocha. Egosipụtara ntụnyere otu ụzọ maka data ụlọ nyocha niile. Eserese (B): A na-egosipụta data ndekọ ọnụ ọgụgụ maka ule ọ bụla, gụnyere pụtara, SD, etiti, kacha nta na kacha.
Isi mmalite: PubMed [5]
Ụlọ ọrụ Australian EpiTan emela nyocha banyere usoro ọhụrụ nke Melanotan (Ⅰ):
Melanotan (Ⅰ) bụ ihe analọg nke α-melanocyte na-akpali akpali, eji egbochi mmebi anyanwụ. Ọ na-akpali mmepụta nke melanin, na-eme ka akpụkpọ ahụ gbaa ọchịchịrị, ma si otú a na-echebe akpụkpọ ahụ pụọ na radieshon ultraviolet.
Enwere ọmụmụ ụlọ ọgwụ atọ gosipụtara nchekwa nke Melanotan-1. N'ime ọmụmụ ihe mbụ, a na-ekenye isiokwu 4 ka ha nweta Melanotan-1 (0.08mg / kg injection subcutaneous kwa ụbọchị), na ihe ọzọ 4 natara isotonic sodium chloride (9%) ngwọta ngwọta maka ụbọchị 10, na-esote UV-B ìhè irradiation na 3 ugboro kacha nta erythema dose (MED) n'olu.
Nsonaazụ gosiri na 3 n'ime isiokwu 4 ndị natara Melanotan-1 nwetara tanning, na ọnụ ọgụgụ nke mkpụrụ ndụ anwụ na-acha ọkụ na mpaghara olu nke ihe ndị a na-ebelata site na 47% (Dorr RT).
Na ọmụmụ nke abụọ, a na-abawanye dose nke MT-1 na 0.16mg / kg kwa ụbọchị maka ụbọchị 10.
N'oge (n = 7) ma ọ bụ mgbe (n = 5) oge nchịkwa MT-1, a na-ekpughe mpaghara buttock na radieshon UV-B (0.25 - 0.75 MED). Nsonaazụ gosiri na ọnụ ọgụgụ dị elu nke MT-1 gbara ọchịchịrị karịa ebe akpụkpọ anụ (Dorr RT) .N'ọmụmụ ihe nke atọ, a na-ekenye isiokwu 8 ka ha nweta ọkara azụ ìhè anyanwụ maka 3 - 5 ụbọchị ma ọ bụ ìhè anyanwụ gbakwunyere 0.16mg / kg nke MT-1, 5 ụbọchị n'izu maka izu 4. Nsonaazụ gosiri na azụ tanning na otu MT-1 ka emelitere nke ukwuu, na mmetụta tanning a dịruo ma ọ dịkarịa ala izu 3 karịa nke otu njikwa na-enweta naanị ìhè anyanwụ, ebe otu njikwa chọrọ 50% karịa oge ikpughe ìhè anyanwụ iji nweta otu ogo nke tanning [6]..
Ngwa nke Melanotan-1 na nyocha melanoma:
Melanoma bụ etuto akpụkpọ anụ nke na-adịghị njọ nke ukwuu, ụzọ ọgwụgwọ ugbu a gụnyere ịwa ahụ, ọgwụgwọ redio, chemotherapy, na immunotherapy. Dịka agonist MCR, Melanotan-1 nwere ike ịrụ ọrụ ọgwụgwọ nwere ike site n'ịhazi uto, ọdịiche, na apoptosis nke mkpụrụ ndụ melanoma. Ụfọdụ nnyocha egosila na Melanotan-1 nwere ike igbochi mmụba na mbuso agha nke mkpụrụ ndụ melanoma ma mee ka apoptosis nke mkpụrụ ndụ melanoma [7] pụta..
Kedu ọrịa Melanotan-1 nwere ike iji gwọọ?
erythropoietic protoporphyria (EPP):
Erythropoietic protoporphyria bụ ihe nketa nketa site na obere ọrụ ferrochelatase, na-eduga na mkpokọta protoporphyrin na sel ọbara uhie, plasma, imeju na akpụkpọ ahụ. Ndị ọrịa na-enwekarị mmetụta maka ìhè anyanwụ, ma mgbe anwụ na-ekpuchi ha, ha ga-enweta mgbaàmà dịka mgbu akpụkpọ ahụ, itching, erythema, na blisters. Melanotan-1 na-ebelata mgbaàmà nke ndị ọrịa EPP site n'ịkwalite mmepụta nke melanin na akpụkpọ ahụ yana ịbawanye nchebe akpụkpọ ahụ megide ụzarị ultraviolet. Nnyocha egosiwo na Melanotan-1 nwere ike belata ugboro ugboro na ịdị njọ nke mmeghachi omume phototoxic na ndị ọrịa EPP ma melite ogo ndụ ha [8]..
Ọrịa erythropoietic porphyria (CIPA):
Congenital erythropoietic porphyria bụ ọrịa mkpụrụ ndụ ihe nketa na-adịghị ahụkebe nke autosomal, nke sitere na mmụgharị na mkpụrụ ndụ hydroxymethylbilane synthase (HMBS), na-eduga na metabolism porphyrin na-adịghị mma. Ndị ọrịa na-enwe mmetụta nke ukwuu maka ìhè, na akpụkpọ ahụ na anya ha na-emebi ngwa ngwa. Melanotan-1 nwekwara ike inye ụfọdụ nchebe megide ụzarị ultraviolet maka ndị ọrịa CIPA site n'ịbawanye mmepụta nke melanin akpụkpọ na ibelata mgbaàmà ha [9]. .
Urticaria anyanwụ:
Maka ndị ọrịa nwere urticaria anyanwụ, Melanotan-1 nwekwara ike ịkwalite nchebe akpụkpọ ahụ megide ụzarị ultraviolet ma belata ugboro na ogo mgbaàmà urticaria [10]..
Mgbawa ọkụ polymorphous (PMLE):
Nnyocha egosiwo na Melanotan-1 nwekwara mmetụta ọgwụgwọ ụfọdụ na ndị ọrịa PMLE, nke nwere ike ibelata ihe omume nke rashes ma melite ogo ndụ nke ndị ọrịa [10]..
Vitiligo:
Melanotan-1 nwere ike ịrụ ọrụ ụfọdụ n'ịkwalite mmechi nke ndị ọrịa vitiligo site n'ịkwalite mmụba na ọdịiche nke melanocytes. Ọ bụ ezie na enwere ọmụmụ ole na ole na ntinye ya na ọgwụgwọ vitiligo ugbu a, nsonaazụ mbụ na-egosi ụfọdụ ikike [10]..
Ihe otutu:
Mmetụta ọgwụgwọ Melanotan-1 na ihe otutu nwere ike jikọta ya na nhazi ya nke usoro ahụ ji alụso ọrịa ọgụ na mbelata nzaghachi mkpali. Ụfọdụ nnyocha achọpụtala na Melanotan-1 nwere ike ịkwụsị mgbaàmà mkpali nke ihe otutu ma kwalite ọgwụgwọ ọnya anụ ahụ [10]..
Ọrịa Hailey-Hailey:
Melanotan-1 egosikwala ụfọdụ mmetụta ọgwụgwọ na ọgwụgwọ nke ọrịa Hailey-Hailey. Ihe e ji mara ọrịa akpụkpọ ahụ a na-adịghị ahụkebe site na ọnya na ọzịza ugboro ugboro na akpụkpọ ahụ. Melanotan-1 nwere ike imeziwanye mgbaàmà nke ndị ọrịa site n'ịhazi ọrụ nke mkpụrụ ndụ akpụkpọ ahụ [10].
N'ikpeazụ, dị ka analog synthetic nke α-melanocyte-stimulating hormone (α-MSH), Melanotan-1 (melanotan I) dị oke mkpa na ngalaba ahụike anụ ahụ. Ọ nwere ike ịbawanye ọdịnaya melanin na akpụkpọ ahụ, na-enyere akpụkpọ ahụ aka iguzogide mmebi nke ụzarị ultraviolet, si otú a na-egbochi ntachu anwụ, ibelata ịka nká akpụkpọ, na ibelata ohere nke ọrịa cancer akpụkpọ ahụ. Site n'ịgbalite melanocortin receptor, Melanotan-1 na-akwalite mmepụta na nkesa nke melanin, na-emepụta ihe okike 'sunscreen' iji chebe mkpụrụ ndụ akpụkpọ ahụ site na mmebi DNA nke ụzarị ultraviolet kpatara na mmebi nke free radicals.
Na ọgwụgwọ ọrịa anụ ahụ, Melanotan-1 na-egosikwa uru ngwa nwere ike. Maka nsogbu nke pigmenti dị ka vitiligo, ọ nwere ike kpalie ọrụ nke melanocytes ma kwalite njikọ nke melanin, na-enyere aka weghachite pigmenti nkịtị nke akpụkpọ ahụ. Na mgbakwunye, ọ nwekwara ike ụfọdụ n'ịgwọ ọrịa na-enweghị isi pigmenti dị ka melasma. Site n'ịhazi nkesa na metabolism nke melanin, ọ nwere ike melite agba akpụkpọ ahụ na ịdị n'otu.
Dị ka ihe polypeptide, Melanotan-1 na-eji nwayọọ nwayọọ na-enweta nlebara anya na nyocha na ngalaba nke dermatology na cosmetology, na-enye ndị mmadụ nhọrọ ọhụrụ iji nagide nsogbu ndị metụtara pigmenti akpụkpọ anụ. Ekwesiri iburu n'uche na ngwa ahụike nke Melanotan-1 ka na-achọ nyocha siri ike. Ugbu a, ọtụtụ ọmụmụ ihe nwere obere ihe nlele na oke data nchekwa ogologo oge. Agbanyeghị, site na mmepe nke usoro mwepụta ọhụrụ na usoro nnyefe ọgwụ mpaghara, atụmanya ya maka ntụgharị ụlọ ọgwụ na-ekwe nkwa.
Banyere Onye dere ya
Ihe niile a kpọtụrụ aha n'elu bụ Cocer Peptides na-enyocha, dezie ma chịkọta ya.
Onye ode akwụkwọ akụkọ sayensị
Elizabeth A. Langan bụ onye ama ama UK ọkachamara gbasara akpụkpọ ahụ na onye nyocha ahụike. Ọ na-ejide ọkwa agụmakwụkwọ n'ọtụtụ ụlọ ọrụ, gụnyere Prọfesọ na Mahadum Lubeck na Mahadum Manchester, yana ọrụ na Mahadum Heidelberg na Mahadum Queen Mary nke London. Langan na-arụ ọrụ na ụlọ ọrụ ahụike ama ama dịka ụlọ ọgwụ Mahadum Schleswig-Holstein na Salford Royal NHS Foundation Trust. O bipụtala ọtụtụ akwụkwọ na akwụkwọ akụkọ ọkachamara dị ka Sayensị Dermatological. Mpaghara nyocha ya na-ekpuchi dermatology, ọgwụ izugbe na nke ime, ịwa ahụ, oncology, na nyocha & ọgwụ nnwale. A maara ọrụ ya n'ọtụtụ ebe ma nyekwa aka nke ukwuu na ngalaba ahụike ndị a. Edepụtara Elizabeth A. Langan na ntụaka ntụaka [1].
