1 khoom (10Vials)
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▎ GLP-1 yog dab tsi?
GLP-1 yog qhov ua haujlwm ntev glucagon-zoo li peptide-1 (GLP-1) receptor agonist uas txuas ntxiv ib nrab-lub neej ntawm ntuj GLP-1 los ntawm kev hloov kho cov qauv. Nws ua raws li cov txiaj ntsig ntawm lub cev ntawm GLP-1, txhawb kev tsim cov tshuaj insulin hauv cov piam thaj hauv cov ntshav, inhibiting glucagon tso tawm, ncua kev ua pa ntawm plab, thiab txhawb kev satiety. Nws tswj tau cov ntshav qabzib hauv cov neeg mob uas muaj ntshav qab zib hom 2, txo lub cev hnyav hauv cov neeg rog lossis rog, thiab txo cov kev pheej hmoo ntawm cov hlab plawv. Nws yog peptide nrog ob qhov txiaj ntsig ntawm kev tswj ntshav qabzib, poob phaus, thiab muaj peev xwm tiv thaiv kab mob plawv.
▎ GLP-1 Structure
Source: Pub Chem |
Sequence: 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 Molecular Formula: C 187H 291N 45O59 Molecular Luj: 4114 g / mol CAS Nr .: 910463-68-2 PubChem CID 56843331 Synonyms: Rybelsus; Ozempic; Wegovy |
▎ GLP-1 Kev Tshawb Fawb
Kev tshawb fawb keeb kwm ntawm GLP-1 yog dab tsi?
Txoj kev loj hlob ntawm GLP-1 pib los ntawm kev tshawb fawb ntawm GLP-1's physiological teebmeem. Cov kws tshawb fawb tau tshwm sim los ntawm exendin-4 hauv lizard qaub ncaug los tsim thawj tiam GLP-1 receptor agonist. Txhawm rau nrhiav txoj kev kho mob ntev dua, GLP-1 tau tsim los ntawm kev hloov tshuaj lom neeg ntawm GLP-1 peptide saw, nrog rau kev ntxiv cov roj fatty acid chains kom ntev nws ib nrab-lub neej. Raws li kev tshawb fawb tau ua tiav, nws lub peev xwm hauv kev poob phaus thiab kev tiv thaiv kab mob plawv thiab kev kho mob kuj tau tshwm sim.
GLP-1 mechanism ntawm kev txiav txim yog dab tsi?
Kev tswj hwm ntawm insulin thiab glucagon secretion:
Raws li GLP-1 receptor agonist (GLP-1 RA), GLP-1 txhawb nqa pancreatic β-hlwb kom tso cov tshuaj insulin thaum inhibiting α-hlwb los ntawm secreting glucagon. Tom qab noj mov, thaum cov ntshav qabzib nce siab, GLP-1 khi rau GLP-1 receptors, ua kom cov kab mob qis qis kom ua rau β hlwb tso tawm insulin, txhim kho lub cev kev noj qab haus huv thiab kev siv cov piam thaj, thiab txo cov ntshav qabzib. Los ntawm inhibiting glucagon secretion thiab txo cov piam thaj hauv siab, nws ntxiv stabilizes cov ntshav qabzib. Nyob rau hauv cov xwm txheej zoo li qub, lub cev tswj hwm cov ntshav qabzib hauv cov ntshav los ntawm kev tswj hwm qhov sib npaug ntawm insulin thiab glucagon. GLP-1 mimics cov teebmeem ntawm GLP-1, optimizing cov txheej txheem tswj hwm no [1,2].

Daim duab 1 Ntshav Qab Zib- thiab kev rog muaj feem cuam tshuam ntawm GLP-1 [3].
Inhibition ntawm hepatic gluconeogenesis:
GLP-1 inhibits cov txheej txheem hepatic gluconeogenesis. Gluconeogenesis yog txoj hauv kev uas lub siab tsim cov piam thaj thaum lub sijhawm yoo mov lossis tshaib plab, tswj cov ntshav qabzib kom ruaj khov thaum cov ntshav qabzib qis. Txawm li cas los xij, hauv cov kab mob pathological xws li ntshav qab zib mellitus, gluconeogenesis tuaj yeem ua haujlwm dhau, ua rau cov ntshav qabzib nce siab. GLP-1 ua raws li cov kev taw qhia tseem ceeb los txo cov kev qhia lossis kev ua haujlwm ntawm cov enzymes tseem ceeb gluconeogenesis, yog li txo qis cov piam thaj hauv siab thiab pab tswj cov ntshav qabzib [1].
Cov teebmeem ntawm lub zog ntshav qab zib thiab qab los noj mov:
GLP-1 muaj kev tswj xyuas cov teebmeem ntawm lub zog ntshav qab zib thiab qab los noj mov. Nws txo qis kev noj qab haus huv, muaj peev xwm los ntawm kev ua haujlwm ntawm lub paj hlwb hauv nruab nrab los cuam tshuam cov chaw tswj kev noj qab haus huv, ua rau muaj kev nkag siab ntawm kev puv thiab txo cov khoom noj. Tsis tas li ntawd, GLP-1 muaj qhov cuam tshuam me me ntawm kev siv hluav taws xob, feem ntau ua tiav kev tswj hwm qhov hnyav los ntawm kev txo qis zog, uas pab txo qhov hnyav rau cov neeg mob rog. Hauv kev sim, cov neeg mob uas siv GLP-1 feem ntau qhia txo qis qab los noj mov thiab poob phaus tom qab [1,4].
Cov txheej txheem muaj peev xwm ntawm kev ua haujlwm ntawm cov hlab plawv: GLP-1 tuaj yeem ua rau muaj txiaj ntsig zoo ntawm cov hlab plawv los ntawm ntau lub tshuab. Ntawm ib sab tes, nws tuaj yeem txo cov ntshav qabzib thiab lub cev hnyav, yog li txo qhov kev puas tsuaj los ntawm cov kab mob metabolic rau cov hlab plawv. Ntawm qhov tod tes, GLP-1 tuaj yeem ua ncaj qha rau ntawm cov hlab plawv, xws li los ntawm kev txhim kho vascular endothelial muaj nuj nqi, txo cov lus teb inflammatory thiab oxidative kev nyuaj siab, stabilizing atherosclerotic plaques, thiab txo cov kev pheej hmoo ntawm cov kab mob plawv. Cigrovski txoj kev tshawb fawb qhia tau hais tias GLP-1 tuaj yeem txhim kho txoj haujlwm ntawm vascular endothelial hlwb hauv secreting nitric oxide, txhim kho vasodilation, thiab tiv thaiv cov hlab plawv [5].
Qhov cuam tshuam ncaj qha rau kev ua haujlwm ntawm lub plawv:
Cov kev tshawb fawb tsis ntev los no tau pom tias qhov raug mob hnyav rau GLP-1 tuaj yeem ua rau muaj qhov ua tau zoo ntawm cov tshuaj inotropic zoo rau tib neeg atrial trabeculae yam tsis tau ua rau muaj kev cuam tshuam rau arrhythmias. Cov nyhuv no tuaj yeem tshwm sim los ntawm kev nce sarcoplasmic reticulum Ca2+ reuptake, txhim kho atrial function, thiab tuav cov txiaj ntsig zoo rau cov tsos mob nyem rau cov neeg mob plawv. Hauv cov kev sim cuam tshuam, atrial trabeculae raug rau GLP-1 tau nthuav tawm qhov ua kom muaj zog contractile tsis muaj qhov nce hauv arrhythmias [6].
Dab tsi yog cov ntawv thov ntawm GLP-1?
Rau ntshav qab zib hom 2:
GLP-1 yog siv los kho mob ntshav qab zib hom 2. Txawm hais tias siv qhov ncauj lossis los ntawm kev txhaj tshuaj subcutaneous, nws txo qis hemoglobin A1c (HbA1c) qib [1].
Rau kev kho mob rog:
GLP-1 qhia tau hais tias muaj txiaj ntsig zoo hauv kev kho mob rog. Cov kev sim tshuaj ntsuam xyuas qhia tias cov neeg mob rog tau kho nrog GLP-1 muaj kev poob ceeb thawj, nrog rau kev txo lub duav ncig, txhim kho cov ntshav siab, txo qis HbA1c, thiab txhim kho lipid profile (piv txwv li, txo tag nrho cov roj cholesterol, qis lipoprotein cholesterol, thiab triglycerides, thiab nce siab lipoproteinity). Nws cov txiaj ntsig poob phaus yog qhov zoo tshaj rau cov placebos thiab lwm yam tshuaj poob phaus, ua tau raws li cov qauv tsim los ntawm EMA thiab FDA rau cov tshuaj poob phaus, thiab muab cov kev xaiv kho tshiab rau cov neeg mob rog [1,2].
Txo kev pheej hmoo ntawm kab mob plawv:
Rau cov neeg laus uas muaj ntshav qab zib hom 2 thiab paub kab mob plawv, GLP-1 tuaj yeem txo qhov kev pheej hmoo ntawm cov kab mob plawv. Cov kev tshawb fawb xws li SUSTAIN 6 thiab PIONEER 6 kev sim ua tau pom qhov tsis muaj qhov tsis zoo thiab kev nyab xeeb ntawm subcutaneous thiab qhov ncauj GLP-1 hauv plawv plawv, thiab SELECT sim ntxiv tau lees paub nws cov txiaj ntsig zoo hauv kev txhim kho cov txiaj ntsig ntawm cov hlab plawv, pab txo qis kev pheej hmoo ntawm cov kab mob plawv [1].
Kev tiv thaiv rau lub raum:
Hauv tus qauv nas ntawm lub raum ischemia-reperfusion raug mob, GLP-1 tau qhia txog kev tiv thaiv lub raum. Nws txo cov qib ntawm cov kab mob inflammatory xws li qog necrosis factor-α (TNF-α) thiab nws cov receptor, interleukin-6 (IL-6), txo F8 prostaglandin ntau lawm, nce PI3K thiab AKT qib hauv lub raum cov ntaub so ntswg, thiab alleviates lub raum raug mob, qhia tias GLP-1 yuav muaj peev xwm kho mob rau mob [7] mob..
Xaus
Raws li GLP-1 receptor agonist, GLP-1 zoo tswj cov ntshav qabzib hauv cov neeg mob ntshav qab zib hom 2 los ntawm kev tswj cov tshuaj insulin thiab glucagon secretion, inhibiting hepatic gluconeogenesis, thiab cuam tshuam rau cov ntshav qab zib thiab qab los noj mov, thaum txo lub cev hnyav hauv cov neeg rog. Nws muaj kev tiv thaiv kab mob plawv, txo qis kev pheej hmoo ntawm kab mob plawv, thiab tiv thaiv lub raum. Nws muaj kev kho mob rau mob raum raug mob, mob ntshav qab zib nephropathy, thiab lwm yam kab mob raum.
Hais Txog Tus Sau
Cov ntaub ntawv hais saum toj no yog txhua yam tshawb fawb, kho thiab sau los ntawm Cocer Peptides.
Scientific Journal Author
Hegner, P. yog nyob ntawm University of Regensburg hauv lub teb chaws Yelemees thiab muaj ntau yam kev tshawb fawb txaus siab. Cov no suav nrog cov kab mob plawv thiab cov hlab plawv, uas nws tshawb txog cov txheej txheem thiab kev kho mob ntawm cov kab mob plawv; biochemistry thiab molecular biology, tsom mus rau uncovering molecular biological thiab biochemical tshuaj tiv thaiv mechanisms thiab cov txheej txheem tswj; pharmacology thiab chaw muag tshuaj, hais txog kev txhim kho tshuaj thiab kev ntsuas kev ua tau zoo; thiab cov kab mob ua pa nrog rau cov tshuaj dav dav thiab sab hauv, tsom mus rau kev kuaj mob thiab kev kho mob ntawm cov kab mob ua pa thiab cov kab mob sab hauv. Nws yog ib tug kws tshawb fawb nrog kev ua tiav hauv ntau yam tshuaj. Hegner P tau teev nyob rau hauv kev siv ntawm cov ntaub ntawv pov thawj [6].
▎ Cov Lus Qhia Tseem Ceeb
[1] Oleszczuk R, Kozińska I, Gras-Ozimek J, et al. GLP-1 rau kev kho mob rog rog [J]. Phau ntawv Journal of Education, Health thiab Sport, 2022. https://api.semanticscholar.org/CorpusID:245423376.
[2] Christou GA, Katsiki N, Blundell J, et al. GLP-1 raws li kev cog lus tshuaj tiv thaiv kev rog [J]. Obesity Reviews, 2019,20(6):805-815.DOI:10.1111/obr.12839.
[3] Kurtzhals P, Flindt Kreiner F, Singh Bindra R. Lub luag haujlwm ntawm kev tswj qhov hnyav hauv kev tswj hwm hom 2 mob ntshav qab zib mellitus: Kev Pom Zoo ntawm GLP-1[J]. Diabetes Research and Clinical Practice, 2023,203.DOI:10.1016/j.diabres.2023.110881.
[4] Chao AM, Tronieri JS, Amaro A, et al. GLP-1 rau kev kho mob rog rog [J]. Trends in Cardiovascular Medicine, 2023,33(3):159-166.DOI:10.1016/j.tcm.2021.12.008.
[5] Cigrovski BM, Strollo F. GLP-1-qhov muag-catching results[J]. World Journal of diabetes, 2023,14(4):424-434.DOI:10.4239/wjd.v14.i4.424.
[6] Hegner P, Seitz S, Schopka S, et al. GLP-1 txhim kho kev ua haujlwm contractile hauv tib neeg atrium [J]. European Heart Journal, 2024,45(Supplement_1):ehae666-ehae3729.DOI:10.1093/eurheartj/ehae666.3729.
[7] Tiba AT, Qassam H, Hadi N R. GLP-1 nyob rau hauv lub raum ischemia-reperfusion raug mob hauv nas[J]. J Med Lub Neej, 2023,16(2):317-324.DOI:10.25122/jml-2022-0291.
Tag nrho cov kab lus thiab cov ntaub ntawv ntawm cov khoom lag luam muab rau ntawm lub vev xaib no tsuas yog rau cov ntaub ntawv tshaj tawm kev tshaj tawm thiab cov hom phiaj kev kawm.
Cov khoom muab rau hauv lub vev xaib no yog npaj tshwj xeeb rau kev tshawb fawb hauv vitro. Kev tshawb fawb hauv vitro (Latin: * hauv iav *, lub ntsiab lus hauv iav) yog ua los ntawm tib neeg lub cev. Cov khoom no tsis yog tshuaj, tsis tau txais kev pom zoo los ntawm US Food and Drug Administration (FDA), thiab yuav tsum tsis txhob siv los tiv thaiv, kho, lossis kho txhua yam mob, kab mob, lossis mob. Nws raug txwv nruj raws li txoj cai los qhia cov khoom no rau hauv tib neeg lossis tsiaj lub cev hauv txhua daim ntawv.