Na Cocer Peptides 
27 lā aku nei
ʻO nā ʻatikala a me nā ʻike huahana i hāʻawi ʻia ma kēia pūnaewele pūnaewele wale nō no ka hoʻolaha ʻana i ka ʻike a me nā kumu hoʻonaʻauao.
ʻO nā huahana i hāʻawi ʻia ma kēia pūnaewele i manaʻo wale ʻia no ka noiʻi in vitro. Hana ʻia ka noiʻi in vitro (Latin: *i ke aniani*, ʻo ia hoʻi i ka ipu aniani) ma waho o ke kino kanaka. ʻAʻole kēia mau huahana he lāʻau lapaʻau, ʻaʻole i ʻae ʻia e ka US Food and Drug Administration (FDA), a ʻaʻole pono e hoʻohana ʻia no ka pale ʻana, mālama, a hoʻōla paha i kekahi maʻi olakino, maʻi, a maʻi paha. Ua pāpā loa ʻia e ke kānāwai ke hoʻokomo i kēia mau huahana i loko o ke kino kanaka a holoholona paha ma kekahi ʻano.
Nānā nui
ʻO Melanotan-1 (MT-1) he ultra-high-efficiency synthetic melanocyte-stimulating peptide, he synthetic formulation o ka hormone melanocortin kūlohelohe, i loaʻa i ka manaʻo nui i ka ʻoihana nani. He kuleana koʻikoʻi nā analogues Melanocortin i nā kaʻina hana physiological o ka ʻili, e launa pū me nā mea hoʻokipa kūikawā e hoʻoponopono i ka hana melanin. ʻO Melanotan - 1 e hoʻohālike i ke ʻano kūlohelohe o ka melanocortin, e hoʻopili ana i ke kaʻina pigmentation o ka ʻili, kahi kumu no kāna noi ʻana i ka ʻoihana nani.
Kiʻi 2 ʻO ka hana kemika o Melanotan - 1.
Ma ka mōʻaukala, ua hoʻomaka ka noiʻi ʻana ma Melanotan-1 me ka ʻimi hohonu ʻana i nā ʻano hoʻoponopono hoʻoponopono pigmentation ʻili. Ke hoʻomau nei ka ʻimi ʻana o ka poʻe i ka nani, ʻoi aku ka nui o ke koi ʻana i nā hopena tanning ʻili, ua hoʻonui nui ka poʻe noiʻi i nā mea hiki ke hoʻoponopono i ka hana melanin.
Mechanism of Action
(1) Hoʻopaʻa iā Melanocortin Receptors
ʻO ke kī i ka pono o Melanotan-1 aia i kona hiki ke hoʻopaʻa i nā melanocortin receptors (MC1R). ʻO MC1R kahi mea hoʻokipa G protein-coupled i hōʻike mua ʻia ma ka ʻili o nā melanocytes. Ke hoʻopaʻa ʻia ʻo Melanotan-1 i ka MC1R, hoʻomaka ia i kahi hanana o nā hanana transduction hōʻailona intracellular. Hoʻopili kēia hoʻopaʻa ʻana i ka protein G i hui pū ʻia me MC1R, ka mea e hoʻāla ai i ka adenylate cyclase, e alakaʻi ana i ka piʻi ʻana o ka intracellular second messenger cyclic adenosine monophosphate (cAMP) pae. ʻO ka piʻi ʻana o ka cAMP e hoʻāla hou i ka protein kinase A (PKA), ka mea e hoʻoponopono ai i ka hōʻike ʻana o ka melanin synthesis-related genes ma o ka phosphorylating i ka downstream transcription factor, ka microphthalmia-associated transcription factor (MITF).
Kiʻi 2 Hui ma waena o ka hoʻololi kiʻekiʻe o ka melanin density a me ka baseline melanin density ma ka lima o loko o ka poʻe ITT.
(2) Hoʻoponopono i ka hōʻike gene pili i ka melanin synthesis
ʻO MITF kahi kumu transcription koʻikoʻi i ke kaʻina hana melanin synthesis, hiki ke hoʻoponopono i ka hōʻike ʻana o nā genes e hoʻopili ana i nā enzyme i komo i ka melanin synthesis, me ka tyrosinase ka mea nui loa. ʻO Tyrosinase ka enzyme e kaupalena ana i ka melanin synthesis, e hoʻopololei ana i ka hoʻololi mālie ʻana o tyrosine i dopaquinone, a laila synthesized i melanin. Hoʻolaha ʻo Melanotan-1 i ka hana MITF, hoʻonui i ka hōʻike ʻana o tyrosinase a me nā enzymes pili i ka melanin synthesis, a laila e hoʻolōʻihi i ka hana melanin synthesis. Hiki i ka Melanotan-1 ke hoʻololi i ka hōʻike o nā genes ʻē aʻe e pili ana i ka melanin synthesis, e like me ka dopa-colorin interconverting enzyme (DCT), a me nā mea ʻē aʻe. Hana pū kēia mau enzymes i ka hoʻoikaika ʻana i ka melanin synthesis a me ka hōʻiliʻili ʻana, e alakaʻi ana i ka ʻili ʻeleʻele.
(3) Nā hopena synergistic o nā ala hōʻailona intracellular
Ma waho aʻe o ke ala hōʻailona cAMP-PKA-MITF maʻamau i ʻōlelo ʻia ma luna, hiki i Melanotan-1 ke hoʻoponopono i ka synthesis melanin ma o nā ala hōʻailona intracellular ʻē aʻe. Hiki ke hoʻololi i ke ala hōʻailona mitogen-activated protein kinase (MAPK). I loko o nā melanocytes, komo ke ala hōʻailona MAPK i ka hoʻoponopono ʻana i nā kaʻina hana ola like ʻole e like me ka hoʻonui ʻana o nā cell, ka ʻokoʻa, a me ke ola. Hiki i ka Melanotan-1 ke ho'āla i ke ala hōʻailona MAPK no ka hoʻonui ʻana i ka melanocyte proliferation a me ka melanin synthesis. Hiki ke hoʻopili ʻia ke ala hōʻailona PI3K-Akt me nā hopena o Melanotan-1. He kuleana koʻikoʻi kēia ala i ka ulu ʻana o ka cell, ola, a me ka hoʻoponopono metabolic, hiki ke hāʻawi i ke kumu metabolic e pono ai no ka melanin synthesis ma o ka hoʻoponopono ʻana i nā kaʻina metabolic intracellular.
Ke kuleana ma ka ʻoihana Nani
(1) Hoʻolaha i ka ʻili ʻili
Hōʻike ʻia o nā hopena ʻili
ʻO ka hopena cosmetic kaulana loa o Melanotan-1 kona hiki ke hoʻoikaika i ka ʻili ʻili. Ua hōʻike ʻia nā haʻawina ma hope o ka lawelawe ʻana iā Melanotan-1 ma o ka hoʻokele subcutaneous a i ʻole nā ala kūpono o ka lawelawe ʻana, hiki ke ʻike ʻia kahi pōʻeleʻele nui o ka ʻili i nā kumuhana. I loko o kahi noiʻi e pili ana i nā kāne olakino olakino, ʻo ka subcutaneous injection o Melanotan-1 ma kahi maʻi o 0.08-0.21 mg / kg i hoʻomau mau ʻia no 5 mau lā ma luna o 2 mau pule (10 doses). Ua hōʻike ʻia nā hopena i ka tanning nui ma nā wahi e like me ka lae, nā lima, a me ka ʻāʻī o nā kumuhana. ʻAʻole i hoʻokumu ʻia kēia hopena tanning ma muli o ka pōʻino i hoʻoiho ʻia e UV akā ma ka hoʻonui ʻia ʻana o ka melanin synthesis endogenous, ka hopena i ka ʻili o ka ʻili maoli.
Ka lōʻihi o ka hopena tanning
ʻO ka hopena tanning ʻili i hoʻokomo ʻia e Melanotan-1 he ʻano hoʻomau. Ua ʻike nā haʻawina ua hiki ka hopena tanning i kona kiʻekiʻe ma kahi o hoʻokahi pule ma hope o ka lawelawe ʻana, a ʻekolu pule ma hope o ka hoʻopau ʻana i ka regimen ʻumi-dose, ʻoi aku ka ʻeleʻele o ka ʻili ma mua o ka mālama ʻana. Hōʻike kēia ʻaʻole ʻo Melanotan-1 wale nō e hoʻoikaika i ka melanin synthesis akā hiki ke mālama ʻia ka melanin i hana ʻia ma o kēia kaʻina hana synthesis i ka ʻili no kekahi manawa, a laila e hoʻomau i ka hopena tanning.
(2) Nā hopena pale o ka ʻili
ʻO ka mīkini pale UV
Hana ʻo Melanin ma ke ʻano he pale kūlohelohe koʻikoʻi no ka ʻili e kūʻē i ka radiation UV. Ma ka hoʻonui ʻana i ka melanin synthesis, hoʻomaikaʻi ʻo Melanotan-1 i ka hiki o ka ʻili ke komo a hoʻopuehu i nā kukuna UV, a laila e hōʻemi ana i ka pōʻino o ka ʻili o ka ʻili. Hoʻopili ʻo Melanin i ka ikehu UV a hoʻololi iā ia i ka ikehu wela no ka hoʻokuʻu ʻana, a laila e hoʻohaʻahaʻa i ka hopena o ka pōʻino o UV i nā macromolecules biological e like me DNA a me nā protein. Eia hou, hiki i ka melanin ke hoʻoponopono i ka ʻōnaehana pale ʻana o ka ʻili e hōʻemi i nā pane inflammatory i hoʻoiho ʻia e UV, e pale hou aku i ka ʻili mai ka pōʻino.
Nā hōʻike noiʻi pili
ʻOiai ua kaupalena ʻia nā haʻawina lāʻau lapaʻau e pili ana i nā hopena pale pale ʻili o Melanotan-1 i kēia manawa, hiki ke noʻonoʻo ʻia kona hiki no ka pale UV ma muli o nā hana physiological o ka melanin a me Melanotan-1 hiki ke hoʻoikaika i ka synthesis melanin. Ua hōʻike ʻia kekahi mau haʻawina in vitro e hōʻike ana nā melanocytes i mālama ʻia me Melanotan-1 i nā pae haʻahaʻa haʻahaʻa o nā ʻano oxygen reactive (ROS) a hoʻemi ʻia nā helu apoptosis ma hope o ka hoʻolaha ʻana o UV, e manaʻo ana e hiki i ka Melanotan-1 ke hoʻomaikaʻi i ka hoʻomanawanui ʻana o ka ʻili i ka radiation UV ma o ka hoʻonui ʻana i ka synthesis melanin.
(3) Nā hopena ʻē aʻe e pili ana i ka ʻili
Hoʻomaikaʻi ʻia ke ʻano ʻili
Manaʻo kekahi e loaʻa i ka Melanotan-1 ka hopena maikaʻi i ke ʻano o ka ʻili. Hiki i ka hoʻonui ʻana i ka melanin synthesis ke hoʻonui i ka metabolism cellular, e hoʻoikaika ana i ka synthesis a me ka hoʻohou ʻana o ka collagen a me nā elastic fibers. Ma kekahi mau haʻawina hoʻonaʻauao liʻiliʻi, ua hōʻike kekahi poʻe i ʻoi aku ka paʻa o ko lākou ʻili, ʻoi aku ka elastic, a hōʻike i ka hoʻomaikaʻi ʻana i nā laina maikaʻi a me nā wrinkles ma hope o ka hoʻohana ʻana iā Melanotan-1. Pili kēia i ka hoʻoponopono ʻana o ka ʻili extracellular matrix metabolism e nā ala hōʻailona intracellular i hoʻāla ʻia i ka wā melanin synthesis.
Hoʻemi i ka pigmentation o ka ʻili
Ua ʻike pū kekahi mau haʻawina e loaʻa paha i ka Melanotan-1 kekahi hopena i ka pigmentation ʻili. ʻO ka hoʻokumu ʻana o ka pigmentation ʻili e pili pinepine me nā pilikia i ka metabolism melanin. Ma ka hoʻoponopono ʻana i ka synthesis a me ka hāʻawi ʻana i ka melanin, hiki i ka Melanotan-1 ke kōkua i ka puʻunaue ʻana i ka melanin i loko o ka ʻili, a laila e hōʻemi i ka ʻike o ka pigmentation.
Nā noi ma ke kahua o ka aesthetics
Ma hope o ka hoʻokele subcutaneous, hoʻopili piha ʻia ʻo Melanotan-1 e ke kino, e hōʻike ana i ka bioavailability like me ka intravenous administration. I loko o kahi noiʻi pharmacokinetic e hoʻohālikelike ana i nā ala like ʻole o ka hoʻokele, subcutaneous injection o Melanotan-1 ma nā doses o 0.08-0.21 mg / kg i hopena i ka ʻike ʻia o ka lāʻau lapaʻau i loko o ka plasma, me ka hapalua-ola o ka plasma o 0.07-0.79 mau hola i ka wā absorption a me 0.8-1.7 mau hola i ka manawa β. ʻO nā mea maikaʻi o ka hoʻokele subcutaneous e pili ana i ka hoʻokele maʻalahi a me ka absorption lāʻau paʻa; akā naʻe, loaʻa iā ia kekahi mau palena, e like me ka ʻeha kūloko, ʻulaʻula, a me nā hopena ʻē aʻe o ka wahi injection.
4. Hoʻohālikelike me nā ʻano hana nani ʻē aʻe
Hoʻohālikelike me nā ʻano kuʻuna Sunbathing
He ala maʻamau ka hoʻomaʻamaʻa ʻana i ka lā maʻamau no ka loaʻa ʻana o nā hopena tanning ʻili, akā he nui nā hemahema o kēia ʻano. ʻO ka lōʻihi o ka hoʻolaha ʻana i ka radiation ultraviolet (UV) e hoʻonui i ka pilikia o ka maʻi maʻi ʻili, ke kiʻi paʻi kiʻi, a me nā kūlana ʻē aʻe, ʻoiai hiki ke hoʻoulu i ka lā, maloʻo, a me nā wrinkles. Loaʻa ka ʻili ʻili i hoʻokomo ʻia e Melanotan-1 ma o ka hoʻonui ʻana i ka melanin synthesis endogenous, me ka pale ʻana i ka pōʻino i hana ʻia e ka ʻike UV pololei. Eia nō naʻe, ʻoiai ʻaʻole i hoʻokumu piha ʻia ka palekana o Melanotan-1, ʻaʻole hiki ke hoʻololi piha i ka sunbathing kuʻuna ma ke ʻano he hana tanning palekana a hilinaʻi.
Hoʻohālikelike ʻia me nā Huahana Hoʻolima Artificial
Loaʻa kekahi mau mea hoʻomaʻemaʻe kino i loaʻa ma ka mākeke, e like me nā lotions hoʻomaʻemaʻe ponoʻī, e hana maʻamau me nā waikawa amino ma ka ʻili o ka ʻili e hana i kahi waihoʻoluʻu e like me ke kala. Ke hoʻohālikelike ʻia me Melanotan-1, hana nā huahana tanning artificial ma ka ʻili o ka ʻili, e hopena i nā hopena pōkole a hiki ke hoʻoulu i nā pilikia e like me ke kala ʻole a i ʻole ke kala kūlohelohe. ʻO Melanotan-1, ma ka ʻaoʻao ʻē aʻe, hoʻololi i ka waihoʻoluʻu o ka ʻili mai loko mai ma o ka hoʻoponopono ʻana i ka melanin synthesis, hiki ke loaʻa i nā hopena mau loa a kūlohelohe.
Ka hopena
Ma keʻano he peptide hormone melanocyte-stimulating synthetic, Melanotan-1 ka hana nui ma ka hoʻopaʻa ʻana i nā mea hoʻopaʻa hormone melanocyte-stimulating, hoʻoulu i nā ala hōʻailona intracellular, a me ka hoʻoponopono ʻana i ka hōʻike ʻana o nā genes e pili ana i ka melanin synthesis, a laila hoʻolaha i ka synthesis melanin. Ma ke ʻano o nā hopena hoʻonaninani, hoʻolaha maikaʻi ia i ka ʻili ʻili me kahi pae o ka hoʻomau ʻana, a loaʻa paha i nā hopena pale-ʻili a me nā hopena maikaʻi ʻē aʻe i ka nānā ʻana i ka ʻili.
Nā kumu
[1] Habbema L, Halk AB, Neumann M, et al. Nā pilikia o ka hoʻohana ʻole ʻia o ka alpha-melanocyte-stimulating hormone analogues: kahi loiloi [J]. International Journal of Dermatology, 2017,56(10):975-980.DOI:10.1111/ijd.13585.
[2] Fitzgerald LM, Fryer JL, Dwyer T, a me al. Ka hopena o MELANOTAN, [Nle(4), D-Phe(7)]-alpha-MSH, ma ka melanin synthesis i loko o ke kanaka me MC1R ano like ole [J]. Peptides, 2006,27(2):388-394.DOI:10.1016/j.peptides.2004.12.038.
[3] Ugwu S, Blanchard J, Dorr R, a me al. ʻO ka pigmentation ʻili a me nā pharmacokinetics o melanotan-I i loko o nā kānaka [J]. Biopharmaceutics & Drug Disposition, 1997,18:259-269.DOI:10.1002/(SICI)1099-081X(199704)18:33.0.CO;2-X.
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