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1kits （10Ibikoresho）
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▎ ya GHRP-2 Imiterere
Inkomoko: PubChem |
Urukurikirane: AXAWFK Inzira ya molekulari: C 45H 55N 9O.6 Uburemere bwa molekuline: 817.98 g / mol Numero ya CAS: 158861-67-7 PubChem CID ： 6918245 Synonyme: Pralmorelin ； pralmorelina ； KP-102 ； pralmoreline |
▎ GHRP-2 Ubushakashatsi
Ni ubuhe bushakashatsi bwakozwe na GHRP-2?
Imisemburo ikura igira uruhare runini mu mikurire yumuntu, iterambere, no kuringaniza metabolike. Abahanga mu bya siyansi bamaze igihe kinini bashaka ibintu bishobora kugenzura neza ururenda rwarwo. Gukura imisemburo irekura peptide (GHRPs), icyiciro cya oligopeptide ya sintetike itera imisemburo ikura, byagaragaye nkubushakashatsi bwibanze.
GHRP-2 yigana ibikorwa bya ghrelin ihuza reseptor ya ghrelin, igakora inzira yerekana ibimenyetso kugirango irekure neza GH. Irerekana ubushobozi mugupima no kuvura kubura imisemburo ikura, kwivanga muri anorexia, no kurinda kwangirika kwingingo, gutwara ubushakashatsi bwimbitse muburyo bukoreshwa.
Ni ubuhe buryo bwo gukora kuri GHRP-2?
Amabwiriza yo gukura kwa Hormone
Gukina kuri Hypothalamic-Pitoito Axis:
GHRP-2 itera imisemburo ikura (GH) kurekura binyuze mubikorwa bidasanzwe byombi byuzuzanya byibasira hypothalamus na glande ya pitoito (Bowers CY). Ku rwego rwa pitoito, GHRP-2 ihuza imisemburo ikura ya hormone irekura imisemburo (GHS-R). Iyo uhujwe na GHS-R, GHRP-2 itangiza caskade yibimenyetso byerekana ibimenyetso. Kurugero, ikora fosifolipase C (PLC), itera hydrolysis ya phosphatidylinositol-4,5-bisphosifate (PIP2) kuri membrane selile muri inositol trisphosphate (IP3) na diacylglycerol (DAG). IP3 iteza imbere calcium ion isohoka muri endoplasmic reticulum, mugihe DAG ikora protein kinase C (PKC), amaherezo iganisha kuri GH irekurwa (Roh SG,). Mu bushakashatsi bwakoresheje ingirabuzimafatizo ya bovine, GHRP-2 yibitekerezo bitandukanye (10⁻⊃1; ⊃3; kugeza 10⁻⁷ M) byongereye cyane ururenda rwa GH (P <0.05), byerekana ingaruka zitaziguye za GHRP-2 ku gusohora kwa GH na selile pitoito [1].
Igikorwa cyo guhuza hamwe no gukura kwa Hormone-Kurekura Hormone (GHRH):
GHRP-2 yerekana ingaruka zifatika hamwe na GHRH mukubyutsa irekurwa rya GH. Iyo bafatanije na selile pitoito, bakora binyuze munzira zitandukanye zerekana ibimenyetso amaherezo bihurira hamwe kugirango biteze imbere GH. Ubushakashatsi bwerekana ko GHRH ikora cyane cyane adenylate cyclase (AC), ikazamura urwego rwimitsi ya cAMP kugirango ikore poroteyine kinase A (PKA), bityo iteze imbere kwanduza gene ya GH hamwe na synthesis ya GH. Ibinyuranye, GHRP-2 ikora ingaruka zayo ikoresheje inzira ya PLC-IP3 / DAG-PKC yasobanuwe haruguru. Imikoranire yabo yongerera cyane GH kurekura. Mu bushakashatsi bwakorewe intama za pitoito, GHRH (10 nM) na GHRP-2 (100 nM) kugiti cyabo byongereye urwego rwa GH mRNA no kurekura GH muburyo bushingiye kumasaha 0.5-2; iyi ngaruka yazamutse cyane iyo ihujwe [2].
Amabwiriza yo gukura kwa hormone Gukura:
GHRP-2 itera imisemburo ikura (GH) kurekura binyuze mubikorwa bidasanzwe byuzuzanya, icyarimwe byibasira hypothalamus na glande ya pitoito (Bowers CY). Ku rwego rwa pitoito, GHRP-2 ihuza imisemburo ikura ya hormone irekura imisemburo (GHS-R). Iyo uhujwe na GHS-R, GHRP-2 itangiza caskade yibimenyetso byerekana ibimenyetso. Kurugero, ikora fosifolipase C (PLC), itera hydrolysis ya phosphatidylinositol 4,5-bisphosifate (PIP2) kuri membrane selile muri inositol trisphosphate (IP3) na diacylglycerol (DAG). IP3 iteza imbere calcium ion irekurwa muri endoplasmic reticulum, mugihe DAG ikora protein kinase C (PKC), amaherezo bigatuma GH irekurwa (Roh SG,). Mu bushakashatsi bwifashishije ingirabuzimafatizo za bovine, GHRP-2 yibitekerezo bitandukanye (10⁻⊃1; ⊃3; kugeza 10⁻⁷ M) byongereye cyane ururenda rwa GH (P <0.05), byerekana ingaruka zitaziguye za GHRP-2 ku gusohora kwa GH na selile pitoito [1].
Ingaruka zo kuvura kuri Anorexia:
Ku barwayi bafite anorexia, imiyoborere ya GHRP-2 yongera inzara no gufata ibiryo, igabanya guhaga hakiri kare, kandi ikanagaragaza ibimenyetso bya hypoglycemia. Nyuma y'amezi 14 y'ubuyobozi bwa GHRP-2, abarwayi biyongereyeho ibiro 6.7 muburemere bw'umubiri. Ubu buryo bushobora kuba bukubiyemo GHRP-2 ikora nka ghrelin reseptor agonist yigana ingaruka za ghrelin, bityo igahindura ikigo cyinshyi kandi ikanoza imyitwarire yabarwayi ndetse nimirire yabo [3].
Igishushanyo 1 (A) Impinduka muburemere bwumubiri, ubwinshi bwimitsi, hamwe namavuta nyuma yo kuvurwa hamwe na hormone yo gukura irekura peptide-2 (GHRP-2). Ibinure n'imitsi byasuzumwe hakoreshejwe uburyo bwa bio-impedance. Ibipimo byose byiyongereye buhoro buhoro, hamwe nuburemere bwumubiri hamwe ningufu za buri munsi byazamutseho −1.5 kugeza kuri 2,4 kg na 12% kugeza kuri 36%, nyuma ya ghrelin. . GH yagabanutse mugihe IGF-1 yiyongereye nyuma y'amezi 12. (C) Impinduka mumirire. Retinol ihuza poroteyine (RBP) hamwe na poroteyine zose (TP) byazamutse vuba, albumin (Alb) yiyongera nyuma y'amezi 4. Ibipimo byiyongereye nyuma y'amezi 12. (D) Impinduka murwego rwa acyl ghrelin (AG) na des-acyl ghrelin (DAG) nyuma yubuyobozi bwa GHRP-2. Kwiyiriza ubusa DAG na AG byariyongereye, kandi igipimo cya DAG / AG cyaragabanutse nyuma y'amezi 10. BW; uburemere bw'umubiri.
Inkomoko: Byatangajwe [3]
Ni ubuhe buryo bwo kuvura GHRP-2?
Gupima imisemburo ikura ya hormone ikura: GHRP-2 ikoreshwa mubuvuzi nkigikoresho cyo gusuzuma kubura imisemburo ikura. Kubura imisemburo ikuze yabantu bakuru, ikizamini mpuzamahanga cyo kwisuzumisha kumurongo wambere ni ikizamini cyo kwihanganira insuline (ITT). Ariko, kubera ubushobozi bwayo bwo guteza ibintu bikomeye, birabujijwe kubarwayi bamwe. Ubushakashatsi bwasabye gukoresha GHRP-2 kugirango hamenyekane kubura imisemburo ikura (GHD). Ubushakashatsi bwanditse ku ngingo 77 zifite ubuzima bwiza n’abarwayi 58 bafite impanuka ya GH <3 μg / L nkuko byagenwe na ITT. Amasomo yose yahawe inshinge 100 μg GHRP-2, hanyuma hakurikiraho guterwa amaraso mumasaha 2 yakurikiye. Urwego rwa GH rwapimwe hifashishijwe ubudahangarwa bw'umubiri. Ibisubizo byerekanye ko amasomo yose yerekanaga serumu ya GH muminota 60 nyuma yubuyobozi bwa GHRP-2. GH yitabira GHRP-2 ntabwo byatewe nuburinganire. Nubwo ibisubizo byari bike mubibazo byabasaza nabantu bafite umubyibuho ukabije, ibi ntibyabangamiye isuzuma rya GHD. Gusubiramo ibizamini byerekanaga kubyara ubu buryo. Iyo ukoresheje GHRP-2 kugirango usuzume GHD, igabanywa rya 15 μg / L rihuye nagaciro ko gupima 3 μg / L muri ITT, byerekana ko gushyiraho serumu ikwiye ya GH igabanya ubukana bwerekana neza ko imisemburo ikura ikabije [4].
Umuti wa Anorexia: Ku barwayi bafite amateka maremare ya anorexia, GHRP-2 irashobora guhagararira imiti ivura ibyiringiro. Ubushakashatsi bumwe bwatanze GHRP-2 imbere mbere ya buri funguro kumwaka umwe kumurwayi ufite amateka yimyaka 20 ya anorexia. Mbere yo kuvurwa, nubwo umurwayi afite ubwoba bwo kurya no kwifuza kunanuka yari yagabanutse binyuze mu buvuzi bwabanje, imikorere mibi ya gastrointestinal yabujije gufata ibiryo no kwiyongera ibiro. Mu bimenyetso harimo kuruka nyuma yo kubyara, kuribwa mu nda, kubuza amara, na hypoglycemia. Nyuma y’ubuyobozi bwa GHRP-2, umurwayi yagize inzara n’ibiribwa, agabanuka guhaga hakiri kare, ibimenyetso bya hypoglycemia byateye imbere, kandi ibiro by’umubiri byiyongereye buhoro buhoro ibiro 6.7 (kuva kuri 21.1 kg kugeza 27.8 kg) mu mezi 14 atangiye kwivuza. Umunaniro n'imbaraga z'imitsi byateye imbere, ibikorwa byumubiri nibitekerezo byiyongera, kandi nta ngaruka zikomeye zagaragaye hamwe nubuyobozi bwigihe kirekire. Ibi byerekana ko GHRP-2 ishobora kuba uburyo bwiza bwo kuvura abarwayi bafite anorexia idakira [3].
Kugabanya Imikorere Yatewe no Gutwika: Nyuma yo gutwikwa gukabije, kongera umusaruro wa hormone catabolike na cytokine ikongora hamwe no kugabanya imisemburo ya anabolike itera hyperactivite ya metabolike, kugabanuka kwinshi kwumubiri, no guta imitsi. Nubwo hashyizweho uburyo butandukanye bwo kuvura nko gukora siporo no gukoresha imisemburo ya anabolike (insuline, imisemburo ikura, IGF-I, cyangwa steroid), ingaruka zayo ntizihagije. Ibisubizo byubushakashatsi byerekana ko anti-cachexia peptide ghrelin nshya yitaruye imbeba nyuma yo gutwikwa. Exhène ghrelin irashobora kugarura ibiro mukongera ibiryo no kongera imitsi yimbeba. Iragabanya kandi cyane kwangirika kwimitsi ya proteine ya skeletale mu mbeba zaka muguhindura imitsi mRNA imvugo ya E3 ubiquitin ligase, MuRF1, na MAFbx. Ubuzima bucye bwa ghrelin bugabanya imikoreshereze yubuvuzi. Ibinyuranye na byo, imisemburo ya hexapeptide ikura ya hormone irekura peptide 2 (GHRP-2) ni reseptor ya GHRP reseptor agonist yongera uburemere bwumubiri mu nzoka, ikagaragaza ingaruka zo kurwanya indwara y’imbeba ya rubagimpande, kandi igahindura metabolisme ya catabolike ku barwayi barembye cyane. GHRP-2 igira ingaruka nziza ku buremere bw'umubiri, gufata ibiryo, no kugabanuka kwa poroteyine yo mu mitsi ya skeletale mu mbeba zahiye, bikagabanya imikorere mibi iterwa no gutwikwa [5].
Umwanzuro
GHRP-2 ituma imisemburo ikura ikura itera inzira yerekana ibimenyetso binyuze mubikorwa byayo kuri GHS-R muri hypothalamic-pituito axis. Mubuvuzi, irashobora gusuzuma kubura imisemburo ikura no kuvura indwara nka anorexia, septique acute impyiko, hamwe no kudakora nyuma yo gutwikwa, mugihe ikanagaragaza ingaruka zidasanzwe na antioxydeant.
Ibyerekeye Umwanditsi
Ibikoresho byavuzwe haruguru byose byakorewe ubushakashatsi, byahinduwe kandi byakozwe na Cocer Peptides.
Umwanditsi w'ikinyamakuru
Haruta I ni umuganga-siyanse wifatanije n’ishami ry’ubuvuzi bw’imbere mu mutwe mu Ishuri Rikuru ry’Ubuvuzi n’Ubuvuzi bw’amenyo muri kaminuza ya Kagoshima. Ubushakashatsi bwe bwasobanuye bwibanze kuri endocrine na metabolic intervention muri anorexia nervosa ikabije. Haruta I yanditse kurutonde rwa citation [3].
