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SemaglutidStructure Imiterere ya
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-Tr-Arp-Leu Inzira ya molekulari: C 187H 291N 45O.59 Uburemere bwa molekuline: 4114 g / mol CAS Numero 910463-68-2 PubChem CID 56843331 Synonyme: Rybelsus; Ozempic; Wegovy |
Research Ubushakashatsi bwa Semaglutid
Ni ubuhe bushakashatsi bwakozwe na Semaglutid?
Iterambere rya Semaglutid 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, Semaglutid yakozwe hifashishijwe uburyo bwo guhindura imiti ya peptide ya GLP-1, 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.
Nubuhe buryo bwo gukora bwa Semaglutid?
Kugena imisemburo ya insuline na glucagon:
Nka GLP-1 reseptor agonist (GLP-1 RA), Semaglutid itera pancreatic β-selile gusohora insuline mugihe ibuza α-selile gusohora glucagon. Nyuma yo kurya, iyo glucose yamaraso yiyongereye, semaglutide 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. Mugihe cyimiterere isanzwe yumubiri, umubiri ugumana glucose yamaraso ihamye muguhuza uburinganire hagati ya insuline na glucagon. Semaglutid yigana ingaruka za GLP-1, igahindura iyi nzira yo kugenzura [1,2].
Igishushanyo 1 Diyabete- n'ingaruka ziterwa n'umubyibuho ukabije wa GLP-1 [3].
Kubuza gluconeogenezi ya hepatike:
Semaglutid 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. Semaglutid ikora ku nzira zerekana ibimenyetso kugira ngo igabanye imvugo cyangwa ibikorwa by'imisemburo ya gluconeogenezi, bityo igabanye umusaruro wa glucose wa hepatike no gufasha mu kugenzura amaraso ya glucose [1].
Ingaruka kuri metabolism yingufu no kurya:
Semaglutid igira ingaruka zingirakamaro kuri metabolism 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, Semaglutid 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 Semaglutid bakunze kuvuga ko igaburo ryagabanutse ndetse no gutakaza ibiro nyuma [1,4].
Uburyo bushoboka bwibikorwa kuri sisitemu yumutima nimiyoboro: Semaglutid 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, Semaglutid irashobora gukora ku buryo butaziguye ku ngingo z'umutima n'imitsi, nko kunoza imikorere ya endoteliyale y'amaraso, kugabanya ibisubizo bitera umuriro hamwe na stress ya okiside, guhagarika plaque ya aterosklerotike, no kugabanya ibyago byo kurwara umutima. Ubushakashatsi bwa Cigrovski bwerekana ko Semaglutid ishobora kunoza imikorere ya selile 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 Semaglutid bishobora gutera ingaruka zikomeye ziterwa na inotropique nziza kuri trabeculae yo mu bwoko bwa muntu itarinze kongera ubushake bwo kurwara. 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 Semaglutid yerekanaga imbaraga ziyongera cyane ku masezerano nta kwiyongera kwa arththmias [6].
Ni ubuhe buryo bukoreshwa na Semaglutid?
Kuri diyabete yo mu bwoko bwa 2:
Semaglutid 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:
Semaglutid yerekana akamaro gakomeye mukuvura umubyibuho ukabije. Igeragezwa rya Clinical ryerekana ko abarwayi bafite umubyibuho ukabije bavuwe na semaglutide bagabanuka cyane, 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 bakuze barwaye diyabete yo mu bwoko bwa 2 n'indwara z'umutima zizwi, Semaglutid irashobora kugabanya ibyago byo kurwara umutima. Ubushakashatsi nka SUSTAIN 6 na PIONEER 6 bwerekanye ko butari munsi y’umutekano n’umutekano wa Semaglutid yo mu nsi 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, Semaglutid 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 ibikomere byimpyiko, byerekana ko Semaglutid ishobora kuba ifite ubushobozi bwo kuvura impyiko zikabije [7].
Umwanzuro
Nka GLP-1 yakira reseptor agonist, Semaglutid igenzura neza urugero glucose yamaraso kubarwayi barwaye diyabete yo mu bwoko bwa 2 igenga imisemburo ya insuline na glucagon, ikabuza gluconeogenezi ya hepatike, kandi ikagira ingaruka ku mikorere ya metabolisme 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].
