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1kits （10Ibikoresho）
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Z Imiterere ya Maz
Inkomoko: PubChem |
Urukurikirane: AEGTFTSDVSSYLEGQAAKFIAWLVKGRG Inzira ya molekulari: C 207H 317N 45O.65 Uburemere bwa molekuline: 4476g / mol Numero ya CAS: 2259884-03-0 PubChem CID: 167312357 Synonyme: GLXC-26803 |
Research Maz Ubushakashatsi
Ni ubuhe bushakashatsi bwakozwe na Maz?
Ikibazo gikomeye cy’umubyibuho ukabije ku isi n'indwara zijyanye nabyo:
Umubyibuho ukabije n'umubyibuho ukabije byarushijeho kuba imbogamizi ku buzima rusange bw'abaturage. Nk’uko ikinyamakuru World Obesity Atlas kibitangaza ngo mu mwaka wa 2020 umubare w'abantu bafite umubyibuho ukabije wageze kuri miliyoni 764 ku isi kandi biteganijwe ko uzagera kuri miliyari imwe mu 2030. Umubyibuho ukabije urashobora gutera ibibazo byinshi by'ubuzima, nk'indwara z'umutima n'imitsi ndetse na metabolism yo mu bwoko bwa 2, bigira ingaruka zikomeye ku mibereho y'umuntu ndetse no ku mutungo w'ubuvuzi ku isi. Ibi byatumye abashakashatsi bashakisha uburyo bwiza bwo kuvura, cyane cyane imiti mishya.
Urufatiro rwiterambere rwibiyobyabwenge bishingiye kuri incretin:
Kuva igitekerezo cya incretin cyatangizwa mu 1932, ubushakashatsi bujyanye nabwo bwagiye butera imbere. Mu 1987, GLP-1 yagaragaye nk'urwego rukomeye rwo kugenzura imisemburo ya insuline muri pancreas, kandi hashyizweho uburyo bwo kuvura ubwoko bwa 2 metabolism bushingiye kuri incretine. Mu 2005, exenatide, GLP-1 ya mbere ku isi yakira reseptor agonist (GLP-1RA), yemerewe kwamamaza, ishyiraho urufatiro rukomeye kandi rufatika rwo gukora ubushakashatsi no guteza imbere ibiyobyabwenge bishya bishingiye kuri incretine nka Maz. Maz ni ikigereranyo cya oxyntomoduline y’inyamabere (OXM). Nkibisekuru bishya byombi agonist yibasira GLP-1R na GCGR, ifite uburyo bwihariye bwibikorwa bibiri hamwe nicyerekezo kinini mugukiza ibiro hamwe nindwara zifitanye isano.
Ni ubuhe buryo bwo gukora bwa Maz?
Ingaruka ya Agonistic kuri reseptor ya glucagon-peptide-1 (GLP-1):
GLP-1 ni imisemburo yo munda ishobora gutera insuline no guhagarika imisemburo ya glucagon muburyo buterwa na glucose, bityo bikagabanya urugero rwa glucose yamaraso [1] . Nka GLP-1 yakira reseptor agonist, Maz yigana ibikorwa bya GLP-1, kongera imisemburo ya insuline no kugabanya irekurwa rya glucagon, ifasha kugenzura glucose yamaraso. Byongeye kandi, GLP-1 reseptor agonist irashobora gutinza gusiba gastrica, kongera guhaga, no kugabanya ibiryo, bifasha mukugenzura ibiro [1, 2].
Ingaruka ya Agonistic kuri reseptor ya glucagon:
Glucagon irashobora guteza imbere isenyuka ryumwijima glycogene na gluconeogenez, bigatuma glucose yiyongera. Maz, mugukoresha reseptor ya glucagon, irashobora kugenga ibintu byinshi bya glucose metabolisme, bikagerwaho neza na glucose yamaraso. Glucagon kandi iteza lipolysis, ifasha kugabanya ibinure hamwe nuburemere bwumubiri [1, 2].
Ingaruka zigenga umuvuduko wamaraso:
Maz irashobora kugabanya umuvuduko wamaraso wa systolique na diastolique. Ku ruhande rumwe, igabanya umuvuduko wamaraso muguhindura glucose na lipide metabolism no kunoza imikorere ya endoteliyale yimitsi; kurundi ruhande, irashobora kugira ingaruka kuburyo bwo kugenzura umuvuduko wamaraso nka sisitemu ya renin-angiotensin.
Nubuhe buryo bwihariye bwa Maz bwo kugabanya ibiro?
Kugenga glucose yamaraso na metabolism:
Nka agoniste ebyiri ya glucagon isa na peptide-1 (GLP-1) hamwe na reseptor ya glucagon, imwe mungaruka nyinshi zifata umubiri wa GLP-1 ni ukugenzura urugero rwamaraso glucose. Itera gusohora insuline, ikabuza gusohora glucagon, igabanya glucose yamaraso [1] , igatinda gusohora gastrica, ikongera guhaga, kandi igabanya ibiryo. Glucagon we, itera lipolysis no gukoresha ingufu. Kubwibyo, Maz ikora reseptors kandi ikagenga metabolisme yamaraso kugirango igabanye ibiro. Ubushakashatsi bwerekanye ko Maz ishobora kugabanya ibiro byumubiri, umuvuduko wamaraso (systolique na diastolique), cholesterol yuzuye, triglyceride, lipoprotein nkeya, hamwe na lipoprotein yuzuye cyane [3] , byerekana ko bishobora gutera kugabanuka no kunoza indwara ziterwa numubyibuho ukabije.
Ingaruka zo kurya no gufata ingufu:
Maz irashobora kugabanya ibiro mukugira ubushake bwo kurya no gufata ingufu. Mu bigeragezo bimwe na bimwe by’amavuriro, abitabiriye amahugurwa bahuye n’igifu nko kugabanya ubushake bwo kurya nyuma yo gukoresha Maz [3] . Ibi birashobora guterwa nigikorwa kiziguye cya Maz kumuyoboro wigifu cyangwa binyuze mumabwiriza na sisitemu yo hagati. Hatitawe ku buryo bwakoreshwa, kugabanuka kwa appetit na gastrointestinal ingaruka bizagabanya gufata ingufu kandi bigabanye kugabanya ibiro. Byongeye kandi, Maz irashobora kugira ingaruka zo kurya mugutunganya neurotransmitter na hormone mubwonko. Kurugero, GLP-1 irashobora gukora kuri hypothalamus kugirango igabanye ubushake bwo kurya no kuringaniza ingufu [4].
Nubuhe buryo bwihariye bwibikorwa bya Maz mugutunganya glucose yamaraso?
Gukangura insuline:
Glucagon imeze nka peptide-1 (GLP-1) reseptor agonist irashobora gutera insuline. Nka agoniste ebyiri ya GLP-1 na reseptor ya glucagon, Maz irashobora gukora reseptor ya GLP-1 kugirango ihite islet pancreatic islet β selile kugirango isohore insuline. Insuline ni umusemburo w'ingenzi mu kugabanya glucose y'amaraso, ishobora gutera ingirabuzimafatizo gufata glucose no kugabanya urugero rwa glucose mu maraso [1].
Kubuza gusohora glucagon:
Muri icyo gihe, Maz irashobora gukora kuri reseptor ya glucagon kugirango ibuze glucagon. Glucagon na insuline birwanya mugenzi we mu kugenzura glucose yamaraso, kandi kugabanya ururenda rwayo bifasha kugabanya glucose yamaraso [1].
Amabwiriza ya glucose metabolism:
Maz irashobora kugenga metabolisme ya glucose mu nzego nyinshi kugirango ikore ingaruka za hypoglycemic, nko kugira ingaruka kuri glucose metabolism mu mwijima, imitsi, hamwe na tipusi ya adipose. Mu mwijima, bigabanya isenyuka ryumwijima glycogene na gluconeogenez, bigabanya umusaruro wa glucose yamaraso; mumitsi yimitsi, iteza imbere gufata no gukoresha glucose; muri tipusi ya adipose, igenga metabolisme ya lipide, igabanya irekurwa rya aside irike yubusa, kandi igira ingaruka ku buryo butaziguye glucose yamaraso [1, 3].
Ingaruka zo kurya no gufata ingufu:
Ubushakashatsi bwerekanye ko Maz ishobora kugabanya ubushake bwo kurya no gufata ingufu, bishoboka ko ikora kuri reseptors muri sisitemu yo hagati yo hagati no kugenzura inzira yerekana ibimenyetso. Kugabanya gufata ibiryo birashobora kugabanya isoko ya glucose yamaraso kandi bigafasha kugenzura urugero rwa glucose yamaraso [3, 5].
Hindura uhereye kumurongo muburemere bwumubiri no kuzenguruka.
a.Ihinduka ryibanze kuva kumurongo muburemere bwumubiri mugihe. b. Hindura kuva kumurongo muburemere bwumubiri mugihe runaka.
Inkomoko: Byatangajwe [2]
Ni ubuhe buryo bukoreshwa na Maz?
Kuvura ubwoko bwa 2 metabolism:
Ikigeragezo cyateganijwe, gihumye-impumyi, igenzurwa na perezidansi yo mu cyiciro cya 2 cyerekanye ko Maz, buri cyumweru gitangwa na agonist ya buri cyumweru ya glucagon imeze nka peptide 1 (GLP-1) hamwe na reseptor ya glucagon, yerekanye imikorere myiza n'umutekano ku barwayi b'Abashinwa bafite metabolism yo mu bwoko bwa 2 [1].
Gusaba kugabanya ibiro:
Ubushakashatsi ku barwayi bafite metabolisme kandi badafite metabolisme: Isuzuma rifatika hamwe na meta-isesengura ryerekanye ko Maz ishobora kugabanya neza uburemere bwumubiri bwabantu bakuru bafite metabolism cyangwa badafite metabolism [3] . Ubushakashatsi bwarimo ibigeragezo birindwi byateganijwe byitabiriwe nabitabiriye 680. Ibisubizo byerekanye ko ugereranije na placebo, Maz yatumye igabanuka ryinshi ryibiro byumubiri (bivuze itandukaniro [MD] = -6.22%, 95% intera yicyizere [CI]: -8.02% kugeza -4.41%, I⊃2; = 90.0%) (Nalisa DL, 2024). Isesengura ryitsinda hamwe na meta-regression ryerekanye ko abarwayi badafite metabolisme bagabanutse cyane, kandi abarwayi bavuwe ibyumweru 24 bagabanutse cyane ibiro ugereranije n’abavuwe mu byumweru 12 - 20 [3].
Gusaba mubashinwa bakuze bafite umubyibuho ukabije cyangwa umubyibuho ukabije:
Isesengura ryigihe giciriritse ryakozwe ku buryo butemewe, ibice bibiri (ikigereranyo cyo hasi kigera kuri 6mg na dose 9mg), impumyi ebyiri, igenzurwa na perezidansi yo mu cyiciro cya 2 cyakorewe mu Bushinwa bakuze bafite umubyibuho ukabije cyangwa umubyibuho ukabije byagaragaje ko Maz yari afite umutekano kandi ufite akamaro muri aba baturage mu gihe cy’ibyumweru 24 bivura, bikazana ibiro bikomeye kandi bifite akamaro mu mavuriro [2] . Mu bushakashatsi, abantu bakuru bafite ibiro byinshi (BMI ≥ 24 kg / m²) baherekejwe na hyperphagia na / cyangwa byibuze kimwe kijyanye no kubyibuha cyane, cyangwa abantu bakuru bafite umubyibuho ukabije (BMI ≥ 28 kg / m²) bahawe amahirwe yo kwakira Maz buri cyumweru kuri dosiye ya 3mg, 4.5mg, 6mg cyangwa umwanya uhuye. Ibisubizo byagaragaje ko kuva ku murongo fatizo kugeza ku cyumweru cya 24, impuzandengo y’ijanisha ry’uburemere bw’umubiri yari -6.7% (ikosa risanzwe 0.7) mu itsinda rya 3mg Maz, -10.4% (0.7) mu itsinda rya 4.5mg, -11.3% (0.7) mu itsinda rya 6mg, na 1.0% (0.7) mu itsinda rya placebo. Ugereranije na placebo, itandukaniro ryo kuvura ryavuye kuri -7.7% kugeza -12.3% (byose p <0.0001) [2].
Mu gusoza, nk'udushya twibasiwe na agonist, binyuze muburyo butandukanye nko kugenga glucose yamaraso, guteza imbere metabolisme yamavuta, no kwirinda ubushake bwo kurya, Maz irashobora kuzamura neza glucose yamaraso yabarwayi bafite metabolism yo mu bwoko bwa 2 kandi igafasha abantu babyibushye guta ibiro. Itera imbaraga nshya mu kuvura indwara ziterwa na metabolike kandi biteganijwe ko izagabanya umutwaro w’umubyibuho ukabije ku isi.
Ibyerekeye Umwanditsi
Ibikoresho byavuzwe haruguru byose byakorewe ubushakashatsi, byahinduwe kandi byakozwe na Cocer Peptides.
Umwanditsi w'ikinyamakuru
Zhang B nintiti yujuje ibyangombwa ihuza imiryango myinshi izwi. Muri byo harimo Ishuri Rikuru ry’Ubuvuzi rya Peking, Ishuri Rikuru ry’Ubuvuzi ry’Ubushinwa -Ishuri Rikuru ry’Ubuvuzi rya Peking, - Ibitaro by’Ubucuti by’Ubuyapani, ibikoresho bya Guizhou Mfg Polytech, Kaminuza ya Shanghai Jiao Tong, Universiti Utara Maleziya, Ishuri ry’ikoranabuhanga rya Yingkou, kaminuza ya Zhejiang, n’ibitaro by’ubuvuzi bya Peking Union. Ihuriro ritandukanye ryinzego zigaragaza amasomo ye yagutse nubushakashatsi.
Kubijyanye nubushakashatsi, Zhang B afite ibyiciro byinshi byibyiciro. Ubuhanga bwe bukubiyemo Endocrinology & Metabolism, Rusange & Imbere mu Gihugu, Oncology, Cardiovascular System & Cardiology, na Radiology, Medicine Nuclear & Medical Imaging. Ibikorwa bye muri izi nzego byerekana ubumenyi bwe bwimbitse n’umusanzu ukomeye mu guteza imbere siyanse y’ubuvuzi no kunoza imikorere y’ubuzima. Zhang B yanditse kurutonde rwerekana [1].
