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1kits （10Ibikoresho）
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▎ ya Melanotan-1 Imiterere
Inkomoko: PubChem |
Urukurikirane: Ser-Tyr-Ser-Nle-Glu-We-D-Phe-Arg-Trp-Gly-Lys-Pro-Val Inzira ya molekulari: C 78H 111N 21O.19 Uburemere bwa molekuline: 1646.8g / mol Numero ya CAS: 75921-69-6 PubChem CID: 16154396 Synonyme: Afamelanotida; NDP-MSH |
▎ Melanotan-1 Ubushakashatsi
Ni ubuhe bushakashatsi bwakozwe na Melanotan-1?
Melanotan-1 ni ikigereranyo cyogukora imisemburo ya α-melanocyte (α-MSH). α-MSH ikorwa ningirabuzimafatizo zihariye mumubiri wumuntu kandi igira uruhare runini mubikorwa bya physiologique nka pigmentation. Mu rwego rwo gucukumbura ibyakoreshejwe mubice bitandukanye, abashakashatsi bakoze Melanotan-1. Ubushakashatsi bwimbitse kuri α-MSH bwatumye havuka Melanotan-1. α-MSH izwiho kugira uruhare runini mu kuzamura umusaruro wa melanin, kandi Melanotan-1 yari igamije kugira ibikorwa bikomeye n'imirimo yihariye, nko mu gutwika uruhu n'ingaruka zishobora gufotora [1] .
Melanotan-1 ni iki?
Melanotan-1 ni ikigereranyo cyogukora imisemburo ya α-melanocyte. Muguhuza MC1R kuri melanocytes, itera melanocytes kubyara melanin. Yagaragaje akamaro gakomeye mu kuvura erythropoietic protoporphyria kandi ifite amahirwe yo gukoreshwa mu kuvura izindi ndwara z’uruhu.
Melanotan-1 ifite ibiranga ingaruka zirambye. Irashobora gukomeza gukangura melanocytes mu mubiri kugirango itange melanine, bityo itange ingaruka zo kuvura igihe kirekire. Ugereranije nubundi buryo bwo kuvura, Melanotan-1 ntabwo isaba ubuyobozi kenshi, kugabanya umutwaro wo kuvura abarwayi. Mu bushakashatsi bw’ubuvuzi, Melanotan-1 yerekanye umutekano mwiza. Ingaruka mbi zisanzwe zirimo kubabara umutwe, isesemi, kuruka, nibindi, ariko mubisanzwe biroroshye kandi birashobora koroherwa hakoreshejwe uburyo bukwiye. Byongeye kandi, Melanotan-1 ifite uburozi buke ku ngingo zingenzi nkumwijima nimpyiko, bitanga ingwate yumutekano kugirango ikoreshwe kwa muganga.
Nubuhe buryo bwihariye Melanotan-1 ikumira izuba?
Melanin mu ruhu igira uruhare mu kwinjiza imirasire ya ultraviolet na radicals yubusa, bityo ikarinda uruhu kwangirika kwa ultraviolet. Imirasire ya Ultraviolet irashobora gutera ihinduka ryimiterere ya selile yuruhu kandi niyo ntandaro ya kanseri zitandukanye zuruhu. Kubaho kwa melanine birashobora kugabanya imishwarara ya ultraviolet igaragara mu ngirabuzimafatizo z'uruhu kandi bikagabanya ibyago byo guhinduka kwa gene. Uruhu rumaze guhura nimirasire ya ultraviolet, bizatera kwiyongera mubikorwa bya reseptor ya melanocyte itera imisemburo ya melanocyte, bigatuma eumelanine yiyongera muri melanocytes epidermal. Nkikigereranyo cya hormone itera α-melanocyte, Melanotan-1 irashobora kwigana iyi nzira no guteza imbere umusaruro wa melanine [2] . Mu kongera ibinure bya melanin mu ruhu, Melanotan-1 irashobora kugabanya kwangirika kwimirasire ya ultraviolet kumasoko yuruhu. Ubushakashatsi bwerekanye ko nyuma yo gukoresha Melanotan-1, uruhu rwihanganira imirasire ya ultraviolet rwiyongera, kandi izuba rikagabanuka. Ugereranije nuburyo gakondo bwo gutwika nko gukanura izuba no gukoresha ibicuruzwa byogosha, Melanotan-1 ifite ibyiza byihariye. Izuba ryinshi risaba izuba igihe kirekire, rishobora gutera izuba ryinshi, gusaza, ndetse na kanseri y'uruhu ikiyongera. Gukoresha ibicuruzwa byogosha bishobora kugira ibibazo nko kurakara kuruhu na allergie biterwa nibigize imiti. Melanotan-1, binyuze mu gutera inshinge, irashobora kugenzura neza umusaruro wa melanin no kugabanya ingaruka mbi ku ruhu.
Nubuhe buryo bwihariye bwibikorwa bya Melanotan-1 mukuvura vitiligo?
Gukangura umusaruro wa melanin: Melanotan-1 irashobora gutera melanocytes kubyara melanine. Melanin ni ikintu cyingenzi kigena ibara ryuruhu. Ku barwayi barwaye vitiligo, kubera melanocytes yangiritse cyangwa idasanzwe, ibara ryera rigaragara ku ruhu. Melanotan-1 iteza imbere gukwirakwiza no gutandukanya melanocytes kandi ikongerera synthesis ya melanin ukoresheje inzira zerekana ibimenyetso [3].
Kugenga sisitemu yumubiri: Vitiligo ifatwa nkindwara ya autoimmune, aho sisitemu yumubiri yibasira melanocytes idasanzwe. Melanotan-1 irashobora kugira uruhare mukugenzura ubudahangarwa bw'umubiri no kugabanya igitero kuri melanocytes. Irashobora kugenga ubudahangarwa bw'umubiri muguhindura ibikorwa n'imikorere ya selile immunite, bityo bikagabanya ibimenyetso bya vitiligo.
Ingaruka ya Antioxydeant: Guhangayikishwa na Oxidative nabyo bigira uruhare runini mu gutera vitiligo. Melanotan-1 irashobora kugira ubushobozi bwa antioxydeant kandi ikagabanya kwangirika kwa okiside kuri melanocytes. Irashobora gutesha agaciro radicals yubuntu, kurinda melanocytes kwangirika kwa okiside, no gufasha gukomeza imikorere isanzwe ya melanocytes.
Ni ubuhe bushakashatsi bwakozwe bushyigikira ingaruka zihariye za Melanotan-1 mu kuvura protoporphyria ya erythropoietic?
Erythropoietic protoporphyria (EPP) ni indwara yo mu bwoko bwa porphyrin metabolic disorder aho abarwayi bahura n’amafoto akomeye, bigira ingaruka zikomeye ku mibereho yabo. Nkikigereranyo cyogukora imisemburo itera α-melanocyte, Melanotan-1 ifite imibare yubushakashatsi ikurikira kugirango ishyigikire ingaruka zayo mukuvura EPP:
Kunoza kwihanganira urumuri: Mu bushakashatsi bwinshi bw’ubuvuzi, Melanotan-1 byagaragaye ko bizamura urumuri rw’abarwayi ba EPP. Kurugero, mugupima icyiciro cya III CUV039, kuvura hamwe na Melanotan-1 byongereye kwihanganira urumuri abarwayi ba EPP. Ugereranije na platbo, kuvura hamwe na Melanotan-1 byafashaga abarwayi kumara igihe kinini ku zuba ryinshi nta bubabare kandi byongereye igihe kugeza igihe ibimenyetso bya mbere byerekana amafoto yatewe n’isoko risanzwe ryagaragaye [4] .
Kuzamura imibereho: Ubushakashatsi bwinshi bwerekanye ko kuvura hamwe na Melanotan-1 bishobora kuzamura imibereho y’abarwayi ba EPP. Mu bigeragezo bitandukanye by’amavuriro, nyuma yo kuvurwa kwa Melanotan-1, ubuzima bw’abarwayi bwasuzumwe hifashishijwe ibibazo byemewe, kandi ibisubizo byagaragaje ko ubuzima bwazamutse [4].
Ingaruka zo gukingira imikorere yumwijima: Ubushakashatsi bwerekanye ko Melanotan-1 ishobora kugira ingaruka zo kurinda imikorere yumwijima y’abarwayi ba EPP. Mu bushakashatsi bwihuse bwo kureba, 2933 bipimishije imikorere yumwijima, 1186 protoporphyrine yibizamini, hamwe na 1659 Melanotan-1 yatewe abarwayi 70 ba EPP. Ibisubizo byerekanaga ko uko iminsi imaze kuva Melanotan-1 iheruka gushyirwaho, kwiyongera kwa protoporphyrine (PPIX) byiyongereye cyane (p <0.0001); mugihe muminsi 365 ishize, uko igipimo cya Melanotan-1 cyiyongereye, alanine aminotransferase (ALAT) na bilirubin byagabanutse cyane (p = 0.012, p = 0.0299). Ibi byerekana ko Melanotan-1 igira ingaruka ziterwa no gukingira imikorere yumwijima y’abarwayi ba EPP [5] .
Isano rya PPIX nibipimo byumwijima. Igishushanyo (A): Histogrammes (icyatsi) yerekana ikwirakwizwa rya data ya laboratoire. Kugereranya byombi kubintu byose bya laboratoire birerekanwa. Igishushanyo (B): Amakuru y'ibarurishamibare kuri buri kizamini, harimo ibisobanuro, SD, hagati, ntarengwa, na byinshi, birerekanwa.
Inkomoko: PubMed [5]
Isosiyete yo muri Ositaraliya EpiTan yakoze ubushakashatsi ku mikorere mishya ya Melanotan (Ⅰ):
Melanotan (Ⅰ) ni ikigereranyo cya hormone itera α-melanocyte, ikoreshwa mu gukumira izuba. Itera umusaruro wa melanin, yijimye uruhu, bityo ikarinda uruhu imirasire ya ultraviolet.
Hariho ubushakashatsi butatu bwamavuriro bwagenzuye umutekano wa Melanotan-1. Mu bushakashatsi bwa mbere, amasomo 4 yashizweho ku bushake bwo kwakira Melanotan-1 (0.08mg / kg inshinge zo munsi y’ubutaka ku munsi), naho andi masomo 4 yakiriye inshinge ya isotonic sodium chloride (9%) yumuti wiminsi 10, hanyuma hakurikiraho imirasire yumucyo UV-B inshuro 3 byibuze urugero rwa erythma (MED) ku ijosi.
Ibisubizo byerekanye ko amasomo 3 kuri 4 yakiriye Melanotan-1 yageze ku gukonjesha, kandi umubare w’utugingo ngengabuzima twaka izuba mu gice cy’ijosi ryaka ry’amasomo wagabanutseho 47% (Dorr RT).
Mu bushakashatsi bwa kabiri, igipimo cya MT-1 cyongerewe kugera kuri 0.16mg / kg kumunsi iminsi 10.
Mugihe (n = 7) cyangwa nyuma ya (n = 5) mugihe cyubutegetsi bwa MT-1, agace ka buttock kagaragayemo imirasire ya UV-B (0,25 - 0,75 MED). Ibisubizo byerekanye ko igipimo kinini cya MT-1 cyijimye cyane ahantu h'uruhu (Dorr RT) .Mu bushakashatsi bwa gatatu, amasomo 8 yashizweho ku bushake bwo kwakira igice cy’inyuma y’izuba mu minsi 3 - 5 cyangwa izuba ryinshi hiyongereyeho 0.16mg / kg ya MT-1, iminsi 5 mu cyumweru mu byumweru 4. Ibisubizo byerekanye ko gutwika inyuma mu itsinda rya MT-1 byongerewe imbaraga ku buryo bugaragara, kandi iyi ngaruka yo kumanika yamaze byibura ibyumweru 3 kurenza iy'itsinda rishinzwe kugenzura imirasire y'izuba gusa, mu gihe itsinda rishinzwe kugenzura ryari rikeneye igihe cyo kumurika izuba 50% kugira ngo rigere ku ntera imwe yo gukanika [6].
Ikoreshwa rya Melanotan-1 mubushakashatsi bwa melanoma:
Melanoma ni ikibyimba cy'uruhu kibi cyane, kandi uburyo bwo kuvura burimo kubaga, radiotherapi, chimiotherapie, hamwe na immunotherapie. Nka MCR agonist, Melanotan-1 irashobora kugira uruhare runini rwo kuvura muguhindura imikurire, itandukaniro, na apoptose ya selile ya melanoma. Ubushakashatsi bumwe bwerekanye ko Melanotan-1 ishobora kubuza ikwirakwizwa rya selile na melanoma no gutera apoptose ya selile melanoma [7].
Ni izihe ndwara Melanotan-1 yakoreshwa mu kuvura?
Erythropoietic protoporphyria (EPP):
Erythropoietic protoporphyria ni porphiria yumurage iterwa nigikorwa cya ferrochelatase nkeya, bigatuma habaho kwirundanya kwa protoporphyrine mu maraso atukura, plasma, umwijima, nuruhu. Ubusanzwe abarwayi bumva urumuri rw'izuba, kandi iyo bahuye n'izuba, bazagaragaza ibimenyetso nko kubabara uruhu, kuribwa, erythma, na bliste. Melanotan-1 igabanya ibimenyetso by’abarwayi ba EPP mu kongera umusaruro wa melanine mu ruhu no kongera uruhu kurinda imirasire ya ultraviolet. Ubushakashatsi bwerekanye ko Melanotan-1 ishobora kugabanya cyane ubukana n’uburemere bw’ifoto ifata abarwayi ba EPP no kuzamura imibereho yabo [8].
Indwara ya erythropoietic porphyria (CIPA):
Indwara ya erythropoietic porphyria ni indwara idasanzwe ya autosomal recessive genetique, iterwa ahanini no guhinduka kwa gene hydroxymethylbilane synthase (HMBS), biganisha kuri metabolisme idasanzwe ya porphirine. Abarwayi bumva cyane urumuri, kandi uruhu n'amaso byangiritse byoroshye. Melanotan-1 irashobora kandi gukingira imishwarara ya ultraviolet ku barwayi ba CIPA mu kongera umusaruro wa melanin y'uruhu no kugabanya ibimenyetso byayo [9] .
Imirasire y'izuba:
Ku barwayi bafite urticaria izuba, Melanotan-1 irashobora kandi kongera uburinzi bwuruhu kurinda imirasire ya ultraviolet no kugabanya inshuro nuburemere bwibimenyetso bya urticaria [10].
Urumuri rwa polimorphous (PMLE):
Ubushakashatsi bwerekanye ko Melanotan-1 nayo igira ingaruka zimwe na zimwe zo kuvura abarwayi ba PMLE, zishobora kugabanya ibibyimba ndetse no kuzamura imibereho y’abarwayi [10].
Vitiligo:
Melanotan-1 irashobora kugira uruhare runini mugutezimbere kwimurwa ry abarwayi ba vitiligo mugutezimbere no gutandukanya melanocytes. Nubwo muri iki gihe hari ubushakashatsi buke ku ikoreshwa ryabwo mu kuvura vitiligo muri iki gihe, ibisubizo bibanza byerekana ubushobozi bumwe [10].
Acne:
Ingaruka zo kuvura Melanotan-1 kuri acne zirashobora kuba zifitanye isano no kugenzura imikorere yumubiri no kugabanya ibisubizo byumuriro. Ubushakashatsi bumwe bwerekanye ko Melanotan-1 ishobora kugabanya ibimenyetso bya acne kandi bigatera gukira ibikomere byuruhu [10].
Indwara ya Hailey-Hailey:
Melanotan-1 yerekanye kandi ingaruka zimwe na zimwe zo kuvura mu kuvura indwara ya Hailey-Hailey. Iyi ndwara idasanzwe y'uruhu irangwa no guhinda inshuro nyinshi no gutwarwa nuruhu. Melanotan-1 irashobora kunoza ibimenyetso by'abarwayi igenga imikorere y'uturemangingo tw'uruhu [10].
Mu gusoza, nkikigereranyo cyogukora imisemburo ya α-melanocyte itera imbaraga (α-MSH), Melanotan-1 (melanotan I) ifite akamaro kanini mubuzima bwuruhu. Irashobora kongera melanin iri mu ruhu, ifasha uruhu kurwanya neza kwangirika kwimirasire ya ultraviolet, bityo bikarinda izuba, kugabanya gusaza kwuruhu, no kugabanya ibyago byo kurwara kanseri yuruhu. Mugukoresha reseptor ya melanocortin, Melanotan-1 iteza imbere umusaruro nogukwirakwiza melanin, ikora 'izuba ryizuba ' kugirango irinde ingirabuzimafatizo zuruhu kwangirika kwa ADN iterwa nimirasire ya ultraviolet no kwangirika kwa radicals yubuntu.
Mu kuvura indwara zuruhu, Melanotan-1 irerekana kandi agaciro gashoboka. Kurwara pigmentation nka vitiligo, irashobora gukangura ibikorwa bya melanocytes no guteza imbere synthesis ya melanin, ifasha kugarura pigmentation isanzwe yuruhu. Byongeye kandi, ifite kandi ubushobozi runaka mukuvura indwara zifite pigmentation itaringaniye nka melasma. Muguteganya ikwirakwizwa na metabolism ya melanin, irashobora kunoza ibara ryuruhu hamwe nuburinganire.
Nkibintu bya polypeptide, Melanotan-1 iragenda yitabwaho nubushakashatsi mubijyanye na dermatology na cosmetology, biha abantu uburyo bushya bwo gukemura ibibazo bijyanye nuruhu. Twabibutsa ko ubuvuzi bwa Melanotan-1 bugikeneye isuzumwa rikomeye. Kugeza ubu, ubushakashatsi bwinshi bufite ingano ntoya hamwe namakuru yigihe kirekire yumutekano. Ariko, hamwe nogutezimbere uburyo bushya burambye-burekura hamwe na sisitemu yo gutanga ibiyobyabwenge byaho, ibyifuzo byayo byo guhindura ivuriro biratanga ikizere.
Ibyerekeye Umwanditsi
Ibikoresho byavuzwe haruguru byose byakorewe ubushakashatsi, byahinduwe kandi byakozwe na Cocer Peptides.
Umwanditsi w'ikinyamakuru
Elizabeth A. Langan ni umuhanga mu kuvura indwara z’indwara z’Ubwongereza akaba n'umushakashatsi mu by'ubuvuzi. Afite imyanya y'amasomo mu bigo byinshi, birimo Porofeseri muri kaminuza ya Lubeck na kaminuza ya Manchester, ndetse n'inshingano muri kaminuza ya Heidelberg na kaminuza ya Mwamikazi Mary y'i Londere. Langan akora mu bigo by'ubuvuzi bizwi nk'ibitaro bya kaminuza bya Schleswig-Holstein ndetse na Salford Royal NHS Foundation Trust. Yasohoye impapuro nyinshi mubinyamakuru byumwuga nka Dermatology Science. Ibice bye byubushakashatsi bikubiyemo dermatologiya, ubuvuzi rusange n’imbere, kubaga, oncologiya, nubushakashatsi & ubuvuzi bwikigereranyo. Ibikorwa bye birazwi cyane kandi byagize uruhare runini muriyi nzego z'ubuvuzi. Elizabeth A. Langan yanditse ku rutonde rw'ibitekerezo [1].
