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1 kits (10 Vials)
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▎ Tsarin GLP-1
Source: Pub Chem |
Jerin: 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-Leu-Val-Arg-Gly-Arg-Gly-OH Tsarin kwayoyin halitta: C 187H 291N 45O59 Nauyin Kwayoyin: 4114 g/mol Lambar CAS 910463-68-2 Farashin 56843331 Ma'ana: Rybelsus; Ozempic ; Wegovy |
▎ GLP-1 Bincike
Menene asalin bincike na GLP-1?
Haɓaka GLP-1 ya samo asali ne daga binciken abubuwan GLP-1 na ilimin lissafi. Masana kimiyya sun yi wahayi zuwa ga exendin-4 a cikin lizard salva don haɓaka agonist mai karɓa na farko na GLP-1. Don bin zaɓin magani mai tsayi, GLP-1 an haɓaka ta hanyar gyaran sinadarai na sarkar peptide GLP-1, tare da ƙari na sarƙoƙi na fatty acid don tsawaita rabin rayuwarsa. Yayin da bincike ya ci gaba, yuwuwar sa a cikin asarar nauyi da rigakafin cututtukan zuciya da jiyya shima ya bayyana.
Menene tsarin aikin GLP-1?
Dokokin insulin da kuma fitar da glucagon:
A matsayin GLP-1 agonist mai karɓa (GLP-1 RA), GLP-1 yana motsa ƙwayoyin β-pancreatic don ɓoye insulin yayin da yake hana α-cell daga ɓoye glucagon. Bayan cin abinci, lokacin da matakan glucose na jini ya tashi, GLP-1 yana ɗaure ga masu karɓar GLP-1, yana kunna hanyoyin siginar ƙasa don sa ƙwayoyin β su saki insulin, haɓaka haɓakar jiki da amfani da glucose, da rage matakan glucose na jini. Ta hanyar hana fitowar glucagon da rage yawan fitowar glucose na hanta, yana ƙara daidaita matakan glucose na jini. A ƙarƙashin yanayin ilimin lissafi na al'ada, jiki yana kiyaye matakan glucose na jini ta hanyar daidaita ma'auni tsakanin insulin da glucagon. GLP-1 yana kwaikwayon tasirin GLP-1, yana inganta wannan tsarin tsari [1,2].
Hoto 1 Abubuwan da ke da alaƙa da ciwon sukari da kiba na GLP-1 [3].
Hanta na hanta gluconeogenesis:
GLP-1 yana hana tsarin gluconeogenesis na hanta. Gluconeogenesis ita ce hanyar da hanta ke samar da glucose a lokacin azumi ko jihohin yunwa, kiyaye kwanciyar hankali na glucose na jini lokacin da matakan glucose na jini ya yi ƙasa. Koyaya, a cikin yanayin cututtukan cututtuka irin su ciwon sukari, gluconeogenesis na iya zama mai aiki da yawa, yana haifar da haɓakar matakan glucose na jini. GLP-1 yana aiki akan hanyoyin siginar da suka dace don rage magana ko ayyukan enzymes na gluconeogenesis, don haka rage haɓakar glucose na hanta da kuma taimakawa cikin sarrafa glucose na jini [1]..
Tasiri kan makamashin ciwon sukari da ci:
GLP-1 yana da tasiri mai tasiri akan makamashin ciwon sukari da ci. Yana rage yawan kuzari, mai yuwuwa ta hanyar yin aiki akan tsarin juyayi na tsakiya don yin tasiri ga cibiyoyin sarrafa abinci, haifar da jin daɗin cikawa da rage cin abinci. Bugu da ƙari, GLP-1 yana da ƙarancin tasiri akan kashe kuzarin kuzari, da farko yana samun ka'idojin nauyi ta hanyar rage yawan kuzari, wanda ke taimakawa rage nauyi ga marasa lafiya masu kiba. A cikin gwaji, marasa lafiya da ke amfani da GLP-1 sukan ba da rahoton rage yawan ci da asarar nauyi mai zuwa [1,4].
Hanyoyi masu yuwuwar aiki akan tsarin cututtukan zuciya: GLP-1 na iya yin tasiri mai amfani akan tsarin zuciya da jijiyoyin jini ta hanyoyi da yawa. A gefe guda, yana iya rage yawan glucose na jini da nauyin jiki, ta haka yana rage lalacewar da ke haifar da cututtuka na rayuwa zuwa tsarin zuciya. A gefe guda, GLP-1 na iya yin aiki kai tsaye akan kyallen jini na zuciya, kamar ta hanyar inganta aikin endothelial na jijiyoyin jini, rage martanin kumburi da damuwa na oxidative, daidaita plaques atherosclerotic, da rage haɗarin cututtukan zuciya. Binciken Cigrovski ya nuna cewa GLP-1 na iya inganta aikin ƙwayoyin endothelial na jijiyoyin jini a cikin ɓoye nitric oxide, haɓaka vasodilation, da kare tsarin zuciya [5]..
Tasirin kai tsaye akan aikin zuciya:
Nazarin kwanan nan sun gano cewa m bayyanar da GLP-1 zai iya haifar da kashi-dogara mai karfi inotropic sakamako mai kyau a kan ɗan adam atrial trabeculae ba tare da kara hali na arrhythmias. Wannan sakamako na iya fitowa daga ƙarar sarcoplasmic reticulum Ca2+ reuptake, inganta aikin atrial, kuma yana riƙe da tasiri mai kyau ga alamar cututtuka a cikin marasa lafiya na zuciya. A cikin gwaje-gwaje masu alaƙa, trabeculae na atrial da aka fallasa ga GLP-1 ya nuna ingantaccen ƙarfin kwangila ba tare da haɓaka arrhythmias ba [6].
Menene aikace-aikacen GLP-1?
Don nau'in ciwon sukari na 2:
Ana amfani da GLP-1 don kula da nau'in ciwon sukari na 2. Ko ana gudanar da shi ta baki ko ta hanyar allurar subcutaneous, yana rage yawan haemoglobin A1c (HbA1c) yadda ya kamata [1].
Don maganin kiba:
GLP-1 yana nuna tasiri mai mahimmanci a cikin maganin kiba. Gwaje-gwaje na asibiti sun nuna cewa marasa lafiya masu kiba da aka yi musu magani tare da GLP-1 sun sami babban asarar nauyi, tare da rage girman kugu, ingantattun sigogin hawan jini, saukar da matakan HbA1c, da ingantaccen bayanan lipid (misali, rage jimlar cholesterol, ƙarancin ƙarancin lipoprotein cholesterol, da triglycerides, da ƙara yawan lipoprotein cholesterol mai yawa). Sakamakon asarar nauyi ya fi na placebos da sauran magungunan asarar nauyi, biyan ka'idodin da EMA da FDA suka tsara don magungunan asarar nauyi, da kuma samar da sabon zaɓi na magani ga marasa lafiya masu kiba [1,2].
Rage haɗarin cututtukan zuciya:
Ga manya masu nau'in ciwon sukari na 2 da sanannun cututtukan zuciya, GLP-1 na iya rage haɗarin cututtukan zuciya. Nazarin irin su SUSTAIN 6 da gwaje-gwajen PIONEER 6 sun nuna rashin rashin ƙarfi da amincin GLP-1 na subcutaneous da na baka a cikin lafiyar zuciya, kuma gwajin SELECT ya kara tabbatar da fa'idodin da yake da shi wajen inganta sakamakon cututtukan zuciya, yana taimakawa wajen rage haɗarin cututtukan zuciya [1].
Tasirin kariya na koda:
A cikin samfurin linzamin kwamfuta na renal ischemia-reperfusion rauni, GLP-1 ya nuna tasirin kariya na koda. Yana rage matakan ƙwayoyin ƙwayoyin kumburi irin su ƙwayar cuta necrosis factor-α (TNF-α) da mai karɓar sa, interleukin-6 (IL-6), yana rage samar da prostaglandin F8, yana ƙaruwa matakan PI3K da AKT a cikin nama na koda, kuma yana rage raunin koda, yana nuna cewa GLP-1 na iya samun damar warkewa don raunin koda [7].
Kammalawa
A matsayin GLP-1 agonist mai karɓa, GLP-1 yadda ya kamata yana sarrafa matakan glucose na jini a cikin marasa lafiya da ke da nau'in ciwon sukari na 2 ta hanyar sarrafa insulin da glucagon secretion, hana hanta gluconeogenesis, da tasirin ciwon sukari da ci abinci mai ƙarfi, yayin da yake rage nauyin jiki a cikin mutane masu kiba. Yana da tasirin kariya na zuciya, yana rage haɗarin cututtukan zuciya, kuma yana kare kodan. Yana da tasirin warkewa akan mummunan rauni na koda, nephropathy na ciwon sukari, da sauran cututtukan koda.
Game da Marubuci
Abubuwan da aka ambata a sama duk bincike ne, gyara su kuma Cocer Peptides ne suka haɗa su.
Mawallafin Jaridar Kimiyya
Hegner, P. yana dogara ne a Jami'ar Regensburg a Jamus kuma yana da fa'idodin bincike da yawa. Waɗannan sun haɗa da tsarin zuciya da jijiyoyin jini da ilimin zuciya, inda ya bincika hanyoyin da maganin cututtukan zuciya; Biochemistry da ilmin kwayoyin halitta, mai da hankali kan gano abubuwan da ke tattare da kwayoyin halitta da hanyoyin amsawar kwayoyin halitta da tsarin tsari; ilimin harhada magunguna da kantin magani, yana mai da hankali kan haɓakar magunguna da kimanta ingancin inganci; da tsarin numfashi da kuma magungunan gabaɗaya da na ciki, suna mai da hankali kan ganowa da kuma kula da cututtukan numfashi da yanayin kiwon lafiya na cikin gida na yau da kullun. Malami ne wanda ya samu nasarori a fannonin likitanci da yawa. An jera Hegner P a cikin ambaton ambaton [6].
