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▎ Imiterere ya GLP-1
Inkomoko: Pub Chem |
Urukurikirane: His-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys (Aeea-Aeea-γ-glu-octadecanedioic) -Glu-Phe-Ile-Ala-Trp-Aru Inzira ya molekulari: C 187H 291N 45O.59 Uburemere bwa molekuline: 4114 g / mol CAS Umubare 910463-68-2 PubChem CID 56843331 Synonyme: Rybelsus; Ozempic; Wegovy |
G GLP-1 Ubushakashatsi
Ni ubuhe bushakashatsi bwakozwe na GLP-1?
Iterambere rya GLP-1 ryaturutse ku bushakashatsi ku ngaruka za physiologiya ya GLP-1. Abahanga bahumekewe na exendin-4 mumacandwe ya lizard kugirango batezimbere igisekuru cya mbere GLP-1 reseptor agonist. Kugirango ukurikirane uburyo bwo kuvura igihe kirekire, GLP-1 yakozwe hifashishijwe uburyo bwo guhindura imiti ya GLP-1 peptide, hiyongeraho iminyururu ya aside irike kugirango yongere ubuzima bwayo. Ubushakashatsi bugenda butera imbere, ubushobozi bwayo mu kugabanya ibiro no kwirinda indwara z'umutima n'imitsi nabyo byagaragaye.
Ni ubuhe buryo bwo gukora bwa GLP-1?
Kugena insuline na glucagon:
Nka GLP-1 reseptor agonist (GLP-1 RA), GLP-1 itera pancreatic β-selile gusohora insuline mugihe ibuza α-selile gusohora glucagon. Nyuma yo kurya, mugihe amaraso ya glucose yiyongereye, GLP-1 ihuza reseptor ya GLP-1, igakora inzira yerekana ibimenyetso byerekana inzira β selile kurekura insuline, kongera umubiri no gukoresha glucose, no kugabanya glucose yamaraso. Muguhagarika imisemburo ya glucagon no kugabanya umusaruro wa glucose ya hepatike, irusheho gutuma urugero rwa glucose rwamaraso. Mubihe bisanzwe byimiterere yumubiri, umubiri ugumana glucose yamaraso ihamye muguhuza uburinganire hagati ya insuline na glucagon. GLP-1 yigana ingaruka za GLP-1, itezimbere ubu buryo bwo kugenzura [1,2].
Igishushanyo 1 Diyabete- n'ingaruka ziterwa n'umubyibuho ukabije wa GLP-1 [3].
Kubuza gluconeogenezi ya hepatike:
GLP-1 ibuza inzira ya gluconeogenezi ya hepatike. Gluconeogenezi ninzira umwijima utanga glucose mugihe cyo kwiyiriza ubusa cyangwa inzara ivuga, bikomeza glucose mumaraso mugihe glucose yamaraso iba mike. Nyamara, mubihe byindwara nka diyabete, gluconeogenezi irashobora gukora cyane, bigatuma glucose yiyongera. GLP-1 ikora inzira zerekana ibimenyetso kugirango igabanye imvugo cyangwa ibikorwa byimisemburo ya gluconeogenezi, bityo igabanye umusaruro wa glucose hepatike no gufasha mu kugenzura glucose yamaraso [1].
Ingaruka kuri diyabete yingufu no kurya:
GLP-1 igira ingaruka zingirakamaro kuri diyabete yingufu no kurya. Igabanya gufata ingufu, birashoboka mugukora kuri sisitemu yo hagati yo hagati kugirango ihindure ibigo bigenzura ibyifuzo, bitera kumva byuzuye no kugabanya ibiryo. Byongeye kandi, GLP-1 igira ingaruka nkeya ku gukoresha ingufu, cyane cyane kugera ku kugabanya ibiro binyuze mu kugabanya ingufu, bifasha mu kugabanya ibiro ku barwayi bafite umubyibuho ukabije. Mu bigeragezo, abarwayi bakoresha GLP-1 bakunze kuvuga ko igaburo ryagabanutse ndetse no gutakaza ibiro nyuma [1,4].
Uburyo bushoboka bwibikorwa kuri sisitemu yumutima nimiyoboro: GLP-1 irashobora kugira ingaruka nziza mumikorere yumutima nimiyoboro y'amaraso binyuze muburyo bwinshi. Ku ruhande rumwe, irashobora kugabanya glucose yamaraso nuburemere bwumubiri, bityo bikagabanya ibyangijwe nindwara ziterwa na metabolike sisitemu yumutima. Ku rundi ruhande, GLP-1 irashobora gukora ku buryo butaziguye ku ngingo zifata umutima, nko kunoza imikorere ya endoteliyale y'amaraso, kugabanya ibisubizo bitera umuriro hamwe na stress ya okiside, guhagarika icyapa cya aterosklerotike, no kugabanya ibyago byo kwandura indwara z'umutima. Ubushakashatsi bwa Cigrovski bwerekana ko GLP-1 ishobora kunoza imikorere y'uturemangingo twa endoteliyale y'amaraso mu gusohora aside nitide, kongera vasodilasiya, no kurinda sisitemu y'umutima n'imitsi [5].
Ingaruka zitaziguye kumikorere yumutima:
Ubushakashatsi buherutse gukorwa bwerekanye ko guhura cyane na GLP-1 bishobora gutera ingaruka zikomeye ziterwa na inotropic ingaruka nziza kuri trabeculae yo mu bwoko bwa muntu itiriwe yongera ubukana bwa rubagimpande. Izi ngaruka zishobora guturuka ku kwiyongera kwa sarcoplasmic reticulum Ca2 + reuptake, kunoza imikorere yimbere, kandi bigira ingaruka nziza kuburwayi bwibimenyetso kubarwayi bananirwa kumutima. Mu bushakashatsi bujyanye na bwo, trabeculae yo mu bwoko bwa GLP-1 yerekanye imbaraga ziyongera cyane mu masezerano nta kwiyongera kwa arththmias [6].
Ni ubuhe buryo bukoreshwa muri GLP-1?
Kuri diyabete yo mu bwoko bwa 2:
GLP-1 ikoreshwa mu kuvura diyabete yo mu bwoko bwa 2. Byaba byatanzwe mu kanwa cyangwa binyuze mu gutera inshinge, bigabanya neza urwego rwa hemoglobine A1c (HbA1c) [1].
Kuvura umubyibuho ukabije:
GLP-1 yerekana akamaro gakomeye mukuvura umubyibuho ukabije. Igeragezwa ry’amavuriro ryerekana ko abarwayi bafite umubyibuho ukabije bavuwe na GLP-1 bahura n’ibiro byinshi, biherekejwe no kugabanya umuzenguruko w’ikibuno, kunoza ibipimo by’umuvuduko wamaraso, kugabanya urugero rwa HbA1c, no kunoza imyirondoro ya lipide (urugero, kugabanya cholesterol yuzuye, cholesterol ya lipoprotein nkeya, na triglyceride, hamwe na cholesterol ya lipoproteine). Ingaruka zayo zo kugabanya ibiro ziruta iz'imiti ya mitiweli hamwe n’indi miti igabanya ibiro, yujuje ibipimo byashyizweho na EMA na FDA ku miti igabanya ibiro, kandi itanga uburyo bushya bwo kuvura abarwayi bafite umubyibuho ukabije [1,2].
Kugabanya ibyago byindwara zifata umutima:
Ku bantu bakuru barwaye diyabete yo mu bwoko bwa 2 n'indwara z'umutima zizwi, GLP-1 irashobora kugabanya ibyago byo kurwara umutima. Ubushakashatsi nka SUSTAIN 6 na PIONEER 6 bwerekanye ko butari munsi y’umutekano n’umutekano wa GLP-1 yo mu kanwa no mu kanwa mu buzima bw’umutima n’imitsi, kandi ikizamini cya SELECT cyashimangiye ibyiza byacyo mu kuzamura ingaruka z’umutima n’imitsi, bifasha kugabanya ibyago by’indwara zifata umutima [1].
Ingaruka zo gukingira impyiko:
Muburyo bwimbeba yimpyiko ischemia-reperfusion igikomere, GLP-1 yerekanye ingaruka zo gukingira impyiko. Igabanya urugero rwa molekile yaka umuriro nkibibyimba bya nekrosis-α (TNF-α) hamwe na reseptor yayo, interleukin-6 (IL-6), igabanya umusaruro wa prostaglandine F8, ikongera urugero rwa PI3K na AKT mubice byimpyiko, ikanagabanya imvune zimpyiko, byerekana ko GLP-1 ishobora kuba ifite ubushobozi bwo kuvura impyiko zikabije [7].
Umwanzuro
Nka GLP-1 yakira reseptor agonist, GLP-1 igenzura neza urugero rwa glucose yamaraso kubarwayi barwaye diyabete yo mu bwoko bwa 2 igenga imisemburo ya insuline na glucagon, ikabuza gluconeogenezi ya hepatike, kandi ikagira ingaruka kuri diyabete y’ingufu no kurya, mu gihe igabanya cyane ibiro by’umubiri ku bantu bafite umubyibuho ukabije. Ifite ingaruka zo gukingira umutima nimiyoboro, kugabanya ibyago byindwara zifata umutima, kandi ikingira impyiko. Ifite ingaruka zo kuvura ibikomere bikabije byimpyiko, nepropatique diabete, nizindi ndwara zimpyiko.
Ibyerekeye Umwanditsi
Ibikoresho byavuzwe haruguru byose byakorewe ubushakashatsi, byahinduwe kandi byakozwe na Cocer Peptides.
Umwanditsi w'ikinyamakuru
Hegner, P. afite icyicaro muri kaminuza ya Regensburg mu Budage kandi afite inyungu nyinshi z’ubushakashatsi. Muri byo harimo sisitemu y'umutima n'imitsi, aho akora ubushakashatsi ku buryo bwo kuvura indwara z'umutima; ibinyabuzima na biyolojiya y’ibinyabuzima, byibanda ku kuvumbura uburyo bwa molekuline y’ibinyabuzima na biohimiki byerekana uburyo bwo kugenzura; farumasi na farumasi, byibanda ku iterambere ry’ibiyobyabwenge no gusuzuma neza; na sisitemu y'ubuhumekero kimwe n'ubuvuzi rusange ndetse n'imbere, byibanda ku gusuzuma no kuvura indwara z'ubuhumekero hamwe n'ubuvuzi rusange bw'imbere. Numuhanga ufite ibyagezweho mubice byinshi byubuvuzi. Hegner P yashyizwe ku rutonde rw'ibisobanuro byatanzwe [6].
