Melanotan II

Kodi Melanotan II ndi chiyani?

Melanotan II (yomwe imatchedwanso Melanotan 2, MT2, MT-2, MT-II) ndi mtundu wopangidwa mwaluso wa timadzi ta peptide timene timapangidwa mwachilengedwe m'thupi lomwe limayambitsa melanogenesis, njira yomwe imayambitsa khungu. Alpha-Melanocyte Stimulating Hormone, yomwe nthawi zambiri imadziwika kuti MSH, imagwira ntchito poyambitsa ma melanocortin receptors kuti apange zotsatira zake. Zowonadi, kudzera mu zolandilira za melanocortin izi, MSH imakhudzanso kwambiri kagayidwe ka lipid, njala, ndi chilakolako chogonana. Zotsatira zake, kafukufuku wawonetsa kuti Melanotan 2 ili ndi zotsatira zomwe zimapitilira kuwonjezera kutenthetsa khungu, monga kupondereza njala, kulimbikitsa lipolysis, ndi kulimbikitsa libido. Chifukwa cha kuthekera kwake koyambitsa matenda a melanogenesis, Melanotan 2 yaphunziridwa bwino kuti igwiritsidwe ntchito popewa kuwonongeka kwa ma radiation a UV kuchokera ku dzuwa.

Kukula kwa Melanotan 2

Kupanga koyambirira kwa peptide ya Melanotan 2 kutha kuperekedwa ku University of Arizona. Panthawi yofufuza yomwe cholinga chake chinali kupanga chitetezo ku khansa yapakhungu, cholinga chake chinali kupanga njira yolimbikitsira melanogenesis yachilengedwe, kapena chilengedwe. Kupanga a melanin pakhungu, osakhudzidwa mwachindunji ndi cheza cha ultraviolet chomwe chingakhale chovulaza padzuwa. Poyambirira, ofufuza aku University of Arizona anayesa kupereka mwachindunji zomwe zimachitika mwachilengedwe timadzi alpha-MSH kuti mupeze zotsatira zomwe mukufuna. Ngakhale njira iyi idawonetsa zotsatira zabwino, zidatsimikiziridwa kuti MSH yochitika mwachilengedwe inali ndi theka la moyo wautali kuti ikhale yogwiritsidwa ntchito ngati njira yochizira. Komabe, zotsatira zabwino zomwe zapezedwa kuchokera ku oyang'anira a MSH zidalimbikitsa kufufuza kwina pakukula kwa Melanotan 1 ndi Melanotan 2, yomwe ikuwonetsa zofanana. zotsatira pokhala ndi theka la moyo wautali kuti agwiritsidwe ntchito pochiza.

Melanin ndi chiyani?

Melanin ndi mtundu wa pigment womwe umapangidwa kuti uteteze khungu lathu ku kuwala kwa dzuwa ndi kuwonongeka. Zitha kuonedwa ngati zoteteza thupi lathu ku dzuwa. Kuchepa kwa melanin kumatanthauza kuti khungu limatha kuwonongeka kwambiri ndi DNA chifukwa chokhala ndi dzuwa. Kusowa kwa melanin komanso kutetezedwa kwake ku radiation ya UV kumatanthauza kuti anthu omwe ali ndi khungu loyera amakhala ndi chizolowezi choyaka komanso kuwononga ma DNA ambiri. Zikutanthauzanso kuti nthawi yochuluka imayikidwa kuti athe kupanga tani mosatekeseka popanda kuwotcha.

Kulandira vitamini D wokwanira kuchokera kudzuwa popanda kukhala pachiwopsezo chotenga khansa ya melanoma ndi njira yokhazikika. Kafukufuku wapeza kale kuti kusakhala padzuwa kuti mupewe khansa ya melanoma kungayambitse kuchepa kwa vitamini D. Melanotan II imachulukitsa kupanga melanin kudzera pakukondoweza kwa maselo a pigment a khungu otchedwa melanocytes.

Kodi Melanotan II amagwira ntchito bwanji?

Melanotan II (MT2) imagwira ntchito polumikizana ndi zolandilira zina m'thupi lotchedwa melanocortin receptors. Nayi kulongosola momwe Melanotan II imagwirira ntchito:

Kumanga kwa melanocortin receptors

Melanotan II imamangiriza ndi kuyambitsa ma receptor a melanocortin, makamaka ma MC1R ndi MC4R receptors. Ma receptor awa amapezeka makamaka pa melanocyte, maselo apadera apakhungu omwe amapanga melanin.

Kulimbikitsa kupanga melanin

Pamene Melanotan II imamangiriza ku melanocortin receptors, imayambitsa zochitika zingapo za biochemical mkati mwa melanocytes. Kukondoweza kumeneku kumapangitsa kupanga melanin, pigment yomwe imayang'anira khungu, tsitsi, ndi maso.

Kuyambitsa njira za melanin

Melanotan II imayendetsa njira zowonetsera zomwe zimakhudzidwa ndi melanogenesis, njira ya melanin synthesis. Izi zikuphatikiza njira ya cyclic adenosine monophosphate (cAMP), yomwe imagwira ntchito yofunika kwambiri pakuwongolera kupanga ndi kugawa kwa melanin.

Kuwonjezeka kwa ntchito ya melanocyte

Melanotan II imalimbikitsa kuchulukana ndi ntchito za melanocyte, zomwe zimapangitsa kuti pakhale kuchuluka kwa melanin. Izi zimabweretsa mdima wa khungu ndipo zimatha kutengera zotsatira za kufufuta kwachilengedwe.

Zotsatira zachitetezo cha dzuwa

Powonjezera kupanga melanin, Melanotan II ikhoza kupereka chitetezo china ku radiation ya UV. Melanin imayamwa kuwala kwa UV, kuwalepheretsa kulowa mkati mwa khungu ndikupangitsa kuwonongeka kwa DNA, kupsa ndi dzuwa, ndi zina zoyipa zomwe zimadza chifukwa chokhala ndi dzuwa kwambiri.

Ndikofunika kuzindikira kuti mphamvu ndi nthawi ya zotsatira zowotcha za Melanotan II zimatha kusiyana pakati pa anthu chifukwa cha zinthu monga majini, mlingo, ndi kuchuluka kwa ntchito. Kuonjezera apo, pamene Melanotan II ikhoza kupereka chitetezo cha dzuwa, sichidzalowa m'malo mwa njira zotetezera dzuwa, monga kuvala zoteteza ku dzuwa ndi kuchepetsa kuwala kwa UV.

Melanotan II (MT2) yowotcha peptide imapindula

Melanotan II (MT2) ili ndi zinthu zingapo zapadera zomwe zimasiyanitsa ndi njira zina zowotcha komanso zopaka utoto wa khungu. Nazi zina zodziwika bwino:

Kuchulukitsa kupanga melanin

Melanotan II idapangidwa kuti ilimbikitse kupanga melanin, pigment yomwe imapangitsa khungu, tsitsi, ndi maso. Izi Peptide Amamangirira ku melanocortin receptors, zomwe zimayambitsa kutulutsidwa kwa melanin, zomwe zimapangitsa khungu kukhala mdima.

Kutha kuchepetsedwa kukhala padzuwa (Melanotan II pakuwotcha)

Chimodzi mwazofunikira ubwino wa Melanotan II ndi kuthekera kwake kuchepetsa kuchuluka kwa dzuwa lomwe limafunikira kuti lifike tani. Polimbikitsa kupanga melanin, imatha kupangitsa kuti khungu liwoneke ngati silikhala ndi nthawi yochepa padzuwa, kuchepetsa chiopsezo cha kupsa ndi dzuwa komanso kuwonongeka kwa khungu.

Melanotan II amalola iwo omwe samatenthedwa ndi kutentha nthawi zonse padzuwa kuti akhale ndi tani lachilengedwe. Synthetic melanotropin peptide supplements imapereka mwayi wosintha moyo kwa odwala omwe ali ndi ziwengo zadzuwa / zolandilira zosinthika. Kutentha kwachilengedwe komwe kumayamba pakapita nthawi ndiye chitetezo champhamvu kwambiri cha khansa chomwe khungu loyera lingathe kukwaniritsa masiku ano. Melanotan idapangidwa ndi cholinga chochepetsa chiwopsezo cha khansa ndipo mwina kukhala wothandizira wowotcha popanda dzuwa.

Othamanga ndi okonda masewera olimbitsa thupi amagwiritsa ntchito Melanotan 2 kuti azitha kufufuta mwachangu, kuwonjezeka kwa libido, komanso kuchepetsa chilakolako. Melanotan 2 adatchedwa mankhwala a Barbie ndipo adawonetsedwa m'magazini ya Wired. Synthetic melanocortin therapy imathandizira kuti pakhale tani lopanda kukhudzidwa pang'ono ndi cheza chowopsa cha ultraviolet. Melanotan II ikupitilizabe kukhala peptide yotentha kwambiri yogulitsidwa pa intaneti. Chonde onetsetsani gulani MT2 kuchokera kwa Wopanga peptide wodalirika chifukwa zinthu zopangidwa bwino zimatha kukhala ndi zoopsa zina.

Mapulogalamu azachipatala omwe angathe

Kupitilira kupukuta khungu, Melanotan II amawonetsa lonjezano pazachipatala. Mwachitsanzo, angagwiritsidwe ntchito ngati njira yochizira anthu omwe ali ndi vitiligo, matenda apakhungu omwe amadziwika ndi zotupa zapakhungu. Kuphatikiza apo, idaphunziridwa chifukwa chake zotheka pakuwongolera erythropoietic protoporphyria (EPP), matenda osowa cholowa omwe amachititsa chidwi kwambiri ndi kuwala kwa dzuwa.

Adanenedwa kukulitsa libido

Chochititsa chidwi chokhudzana ndi Melanotan 2 ndi zotsatira zake pa libido ndi ntchito yogonana. Ogwiritsa ntchito ena anena za kuchuluka kwa chilakolako chogonana ndi chilakolako monga a zotheka mbali zotsatira kugwiritsa ntchito peptide iyi. Komabe, ndi ndikofunikira kuzindikira kuti zotsatira izi ndi zongopeka ndipo sizingachitike ndi ogwiritsa ntchito onse.

Melanotan II kuchepetsa thupi

Ngakhale kuti sichinali cholinga chake chachikulu, kafukufuku wina wasonyeza kuti Melanotan II ikhoza kuthandizira kuchepetsa chilakolako komanso kuwonda. Komabe, kufufuza kwina kumafunika kuti mumvetse bwino zotsatira zake pa metabolism ndi kulemera kwa thupi.

Mtundu womwe ulipo wa Melanotan II (MT2) pamsika

Pali zambiri za Melanotan II za kugulitsa pa intaneti, ndipo kupezeka kwa MT2 ndi kwakukulu.MT2 ili ndi mawonekedwe opopera a M'mphuno, jakisoni wa Melanotan 2 wosakanizidwa kale, mapiritsi, oral melanotan2, ndi jakisoni wa Melanotan II. Komabe, peptide Melanotan II (MT2) makamaka likupezeka pamsika mu mawonekedwe a lyophilized ufa kwa reconstitution ndi wotsatira makonzedwe. Nawa mitundu yodziwika bwino ya Melanotan II yomwe ilipo:

Fomu la Powor

Melanotan II amagulitsidwa ngati lyophilized ufa, womwe ndi mawonekedwe owuma a peptide. Nthawi zambiri amabwera mu mbale kapena zotengera zazing'ono. Melanoan 2 wogulitsa AASRAW sikuti amapereka ufa waiwisi kuchokera ku peptides komanso lyophilized ufa mu Mbale.

Kukonzanso

Musanagwiritse ntchito, ufa uyenera kukonzedwanso ndi chosungunulira choyenera, madzi osabala kapena madzi a bacteriostatic. Malangizo obwezeretsa akhoza kusiyana malingana ndi mankhwala enieni ndi MT2 wopanga, choncho ndikofunika kutsatira mosamala malangizo omwe aperekedwa.

Kupweteka

Pamene ufawo umakonzedwanso, Melanotan II nthawi zambiri imayendetsedwa kudzera mu jekeseni wa subcutaneous. Singano yaying'ono imagwiritsidwa ntchito kubaya jekeseni pansi pa khungu, makamaka pamimba kapena ntchafu. M'malo mwa kugula jekeseni m'dziko lakwawo, zimamupulumutsa ndalama kuti agule ufa wa lyophilized wa Melanotan 2 kuti apange jakisoni wawo wa MT2. Gulani Melanotan 2 yogulitsa mupeza mtengo wabwino.

Ndikofunikira kuwonetsetsa kuti mankhwalawa ndi ovomerezeka pogula Melanotan II, chifukwa mitundu yabodza kapena yopangidwa molakwika imatha kubweretsa zoopsa zina.

Zotsatira za Melanotan II

Melanotan II peptide yoperekedwa pang'onopang'ono imanenedwa kuti ndi yotetezeka komanso yothandiza pamiyeso yovomerezeka. Mbali zotsatira Zomwe zidanenedwa ndi Melanotan II zikuphatikizapo:

nseru

Kupweteka m'mimba

utachepa chilakolako

Kukudula

Khungu lakuda

Kukoka kwa mbolo modzidzimutsa

Kusintha mu mawonekedwe a mole

Pazifukwa zowopsa kwambiri, pali zoopsa zomwe zitha kukhala zazikulu kwambiri zotsatira zoyipazi, Kuphatikizapo:

Mtundu waukulu wa khansa yapakhungu (melanoma)

Kupanga ma moles atsopano ndi atypical melanocytic naevi

Rhabdomyolysis (kuwonongeka kwa maselo a minofu komwe kungathe kupha)

Encephalopathy syndrome

Kulephera kugonana

Ndikofunikiranso kumvetsetsa kuti ngati singano zigawidwa kapena osayeretsedwa bwino musanagwiritse ntchito, pali chiopsezo chotenga kachilomboka. Monga jekeseni iliyonse, kufiira, ndi kuwawa pamalo opangira jakisoni ndizotheka. Kokha kugula peptide Melanotan II yokhala ndi chiyero cha 98% kapena kupitilira apo.

Sikoyenera kugwiritsa ntchito Chithunzi cha PT-141 jekeseni nthawi imodzi ndi PDE5 inhibitor mwa amuna chifukwa cha chiopsezo cha priapism.

Izi siziyenera kugwiritsidwa ntchito ngati muli ndi pakati kapena mukuyamwitsa. Palibe umboni wokwanira wosonyeza momwe zilili zotetezeka kwa anthu omwe ali mgululi. Mofanana ndi mankhwala ena aliwonse, nthawi zonse muyenera kukaonana ndi dokotala musanayambe mankhwala aliwonse. Izi ndizofunikira makamaka ngati mukugwiritsa ntchito mankhwala ena aliwonse. Pakadali pano, palibe kuyanjana kwamankhwala komwe kumadziwika, koma ndikwabwino kusamala kuposa kupepesa.

Ofufuza omwe ali ndi chidwi chofufuza mbali ya Melanotan 2 zotsatira zitha kukhala chidwi kudziwa kumene kugula mankhwala ofufuza awa pa intaneti. Tsoka ilo, kupeza chovomerezeka Wopereka ma peptides amtundu wa kafukufuku zingakhale zovuta.AASRAW ndi wopanga ma peptide odalirika kukhulupirira.

Lipoti Loyesa la Melanotan II-HNMR

Kodi HNMR ndi chiyani ndipo mawonekedwe a HNMR amakuuzani chiyani? H Nuclear Magnetic Resonance (INMR) spectroscopy ndi njira yowunikira yomwe imagwiritsidwa ntchito poyang'anira khalidwe ndi kufufuza kuti mudziwe zomwe zili ndi kuyera kwa chitsanzo komanso momwe maselo ake amapangidwira. Mwachitsanzo, NMR imatha kusanthula mochulukira zosakaniza zomwe zili ndi mankhwala odziwika. Pazinthu zosadziwika, NMR ingathe (mwina kugwiritsidwa ntchito kufananiza ndi malaibulale owoneka bwino kapena kutengera kapangidwe kake mwachindunji. Kapangidwe koyambira kadziwika, NMR itha kugwiritsidwa ntchito kudziwa momwe ma molekyulu amathandizira komanso kuphunzira zakuthupi pamlingo wa mamolekyulu. monga kusinthana kwa conformational, kusintha kwa gawo, kusungunuka, ndi kufalikira.

Kodi mungagule bwanji Melanotan II kuchokera ku AASraw?

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Wolemba nkhaniyi:
Dr. Monique Hong adamaliza maphunziro awo ku UK Imperial College London Faculty of Medicine

Scientific Journal paper Wolemba:
1. Mariël P Ter Laak
Dipatimenti ya Medical Pharmacology, Rudolf Magnus Institute of Neuroscience, University Medical Center Utrecht
2. Chase W. Mallory BHS
Herbert Wertheim College of Medicine, Florida International University, Miami, FL, USA
3. Miia Kilpeläinen
School of Pharmacy, Pharmaceutical Technology, University of Eastern Finland, Kuopio, Finland
4. Ryouichi Banno
Dipatimenti ya Matenda a Metabolic, Field of Internal Medicine, Nagoya University Graduate School of Medicine, Japan
Dokotala/wasayansiyu savomereza kapena kulimbikitsa kugula, kugulitsa, kapena kugwiritsa ntchito mankhwalawa pazifukwa zilizonse. Aasraw alibe chiyanjano kapena ubale, wonenedwa kapena ayi, ndi dokotala uyu. Cholinga chotchula dokotalayu ndikuvomereza ndikuyamikira ntchito yofufuza ndi chitukuko yomwe asayansi akugwira ntchitoyi.

Zothandizira

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[2] Peters B, Hadimeri H, Wahlberg R, Afghahi H.”Melanotan II: chomwe chingakhale chifukwa cha infarction yaimpso: kuwunikanso zolemba ndi lipoti lamilandu. "CEN Case Rep. 2020 May; 9(2): 159-161. doi: 10.1007/s13730-020-00447-z. Epub 2020 Jan 18.PMID: 31953620

[3] Tomassi S, Dimmito MP, Cai M, D'Aniello A, Del Bene A, Messere A, Liu Z, Zhu T, Hruby VJ, Stefanucci A, Cosconati S, Mollica A, Di Maro S."CLIPSing Melanotan-II to Discover Ma hMCR Agonists Ogwira Ntchito Angapo." J Med Chem. 2022 Marichi 10; 65 (5): 4007-4017. doi: 10.1021/acs.jmedchem.1c01848. Epub 2022 Feb 21.PMID: 35188390

[4] Giuliano F, Clément P, Droupy S, Alexandre L, Bernabé J. ”Melanotan-II: Kufufuza zotsatira za inducer ndi otsogolera pakupanga mbolo mu makoswe opangidwa ndi anesthetized.” Neuroscience. 2006;138(1):293-301. doi: 10.1016/j.neuroscience.2005.11.008. Epub 2005 Dec 19.PMID: 16360286

[5] Hjuler KF, Lorentzen HF." Melanoma yokhudzana ndi kugwiritsa ntchito melanotan-II." Dermatology. 2014;228(1):34-6. doi: 10.1159/000356389. Epub 2013 Dec 18.PMID: 24355990

[6] Jain S, Panyutin A, Liu N, Xiao C, Piñol RA, Pundir P, Girardet C, Butler AA, Dong X, Gavrilova O, Reitman ML.” Melanotan II imayambitsa hypothermia mu mbewa poyambitsa ma cell mast za histamine 1 zolandilira." Am J Physiol Endocrinol Metab. 2018 Sep 1; 315(3):E357-E366. doi: 10.1152/ajpendo.00024.2018. Epub 2018 May 29.PMID: 29812984

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