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▎ Gịnị bụ Semaglutid?
Semaglutid bụ onye na-anabata glucagon-dị ka peptide-1 (GLP-1) agonist nke na-agbatị ọkara ndụ nke GLP-1 eke site na mgbanwe nhazi. Ọ na-eṅomi mmetụta physiological nke GLP-1, na-akwalite mmepụta insulin n'ụzọ dabere na glucose, na-egbochi mwepụta glucagon, na-egbu oge ịgbasa afọ, na ime ka satiety dịkwuo elu. Ọ na-achịkwa ọkwa glucose ọbara nke ọma n'ime ndị ọrịa nwere ụdị ọrịa shuga 2, na-ebelata oke ahụ na ndị buru oke ibu ma ọ bụ buru oke ibu, na-ebelata ohere nke ihe omume obi. Ọ bụ peptide nwere uru abụọ nke njikwa glucose ọbara, mbelata ịdị arọ, yana nchebe nke obi.
▎ Semaglutid Structure
Isi mmalite: Pub Chem |
Usoro: 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 Ụdị mkpụrụ ndụ: C 187H 291N 45O59 Ibu molekụla: 4114 g/mol Nọmba CAS 910463-68-2 PubChem CID 56843331 Ụdị okwu: Rybelsus; Ozempic ; Wegovy |
▎ Semaglutid Research
Kedu ihe ndabere nyocha nke Semaglutid?
Mmepe nke Semaglutid sitere na nyocha nke mmetụta physiological GLP-1. Ndị ọkà mmụta sayensị sitere n'ike mmụọ nsọ exendin-4 na mmiri ngwere iji mepụta agonist nke nnabata GLP-1 nke ọgbọ mbụ. Iji na-agbaso nhọrọ ọgwụgwọ na-eme ogologo oge, Semaglutid mepụtara site na mgbanwe kemịkalụ nke GLP-1 peptide chain, yana mgbakwunye nke eriri acid fatty acid iji gbasaa ọkara ndụ ya. Ka nyocha na-aga n'ihu, ikike ọ nwere na mbelata ibu na mgbochi ọrịa obi na ọgwụgwọ pụtakwara ìhè.
Gịnị bụ usoro nke Semaglutid?
Usoro insulin na mmepụta glucagon: +
Dị ka onye na-anabata GLP-1 agonist (GLP-1 RA), Semaglutid na-akpali sel β-pancreatic ka ọ na-ezochi insulin ma na-egbochi α-cell na nzuzo glucagon. Mgbe ị risịrị nri, mgbe ọkwa glucose ọbara na-ebili, semaglutide na-ejikọta ya na ndị na-anabata GLP-1, na-eme ka ụzọ mgbama dị n'okpuru na-akpali sel beta ịhapụ insulin, na-eme ka ahụ na-erite uru na iji glucose, na-ebelata ọkwa glucose ọbara. Site na igbochi secretion glucagon na ibelata mmepụta glucose imeju, ọ na-eme ka ọkwa glucose dị n'ọbara kwụsie ike. N'okpuru ọnọdụ physiological nkịtị, ahụ na-edobe ọkwa glucose ọbara kwụsiri ike site na ịhazi nguzozi n'etiti insulin na glucagon. Semaglutid na-eṅomi mmetụta nke GLP-1, na-ebuli usoro nhazi a [1,2].

Ọgụgụ 1 Mmetụta ọrịa shuga na oke ibu nke GLP-1 [3].
Mgbochi nke gluconeogenesis imeju:
Semaglutid na-egbochi usoro gluconeogenesis imeju. Gluconeogenesis bụ ụzọ imeju na-emepụta glucose n'oge ọnụnụ ọnụ ma ọ bụ ọnọdụ agụụ, na-ejigide nkwụsi ike nke glucose ọbara mgbe ọkwa glucose dị ala. Otú ọ dị, n'ọnọdụ ndị dị ka ọrịa shuga mellitus, gluconeogenesis nwere ike ịmalite ịrụ ọrụ nke ọma, na-eduga n'ọkwa glucose dị elu. Semaglutid na-arụ ọrụ na ụzọ mgbaàmà dị mkpa iji belata okwu ma ọ bụ ọrụ nke enzymes gluconeogenesis bụ isi, si otú a na-ebelata mmepụta glucose imeju na inye aka na njikwa glucose ọbara [1]..
Mmetụta na ike metabolism na agụụ:
Semaglutid nwere mmetụta nchịkwa na metabolism ike na agụụ. Ọ na-ebelata oriri ume, nke nwere ike site n'ime usoro nhụjuanya nke etiti na-emetụta ụlọ ọrụ nchịkwa agụụ, na-ebute mmetụta nke afọ ojuju na ibelata oriri. Na mgbakwunye, Semaglutid nwere mmetụta pere mpe na mmefu ike, na-enweta ụkpụrụ ịdị arọ site na mbelata ume ike, nke na-enyere aka belata ibu maka ndị ọrịa buru ibu. N'ime ule, ndị ọrịa na-eji Semaglutid na-akọkarị mbelata agụụ na mbelata ibu na-esote [1,4].
Usoro nwere ike ime na usoro obi: Semaglutid nwere ike inwe mmetụta bara uru na usoro obi site na ọtụtụ usoro. N'otu aka, ọ nwere ike iwetu glucose ọbara na ịdị arọ nke ahụ, si otú a na-ebelata mmebi nke nsogbu metabolic na-akpata na sistem obi. N'aka nke ọzọ, Semaglutid nwere ike na-arụ ọrụ ozugbo na anụ ahụ obi, dị ka site na imeziwanye ọrụ endothelial vaskụla, ibelata nzaghachi mkpali na nrụgide oxidative, na-eme ka plaques atherosclerotic guzosie ike, na ibelata ihe ize ndụ nke ọrịa obi. Nnyocha Cigrovski na-egosi na Semaglutid nwere ike imeziwanye ọrụ nke mkpụrụ ndụ endothelial vaskụla na-ezobe nitric oxide, kwalite vasodilation, ma chebe usoro obi obi [5]..
Mmetụta ozugbo na ọrụ obi:
Nnyocha e mere n'oge na-adịbeghị anya achọpụtala na nnukwu ikpughe na Semaglutid nwere ike ịkpata mmetụta inotropic siri ike na-adabere na dose na trabeculae nke mmadụ na-enweghị mmụba nke arrhythmias. Mmetụta a nwere ike ịpụta site n'ịbawanye sarcoplasmic reticulum Ca2+ reuptake, na-eme ka ọrụ atrial dịkwuo mma, ma na-enwe mmetụta dị mma maka enyemaka mgbaàmà na ndị ọrịa obi mgbawa. N'ime nnwale ndị metụtara ya, trabeculae atrial ekpughere na Semaglutid gosipụtara ike nkwekọrịta na-abawanye nke ọma na-enweghị mmụba na arrhythmias [6].
Kedu ihe bụ ngwa nke Semaglutid?
Maka ụdị ọrịa shuga 2:
A na-eji Semaglutid agwọ ụdị ọrịa shuga 2. Ma a na-enye ya ọnụ ma ọ bụ site na ntụtụ subcutaneous, ọ na-ebelata ọkwa hemoglobin A1c (HbA1c) nke ọma [1].
Maka ọgwụgwọ oke ibu:
Semaglutid na-egosiputa nrụpụta dị ukwuu na ọgwụgwọ oke ibu. Nnwale ụlọ ọgwụ na-egosi na ndị ọrịa buru ibu na-agwọ semaglutide na-enweta oke ibu, yana mbelata okirikiri úkwù, mmụba ọbara mgbali elu, wedata ọkwa HbA1c, yana profaịlụ lipid dị mma (dịka ọmụmaatụ, mbelata mkpokọta cholesterol, obere njupụta lipoprotein cholesterol, na triglycerides, yana ịba ụba lipoprotein cholesterol dị elu). Mmetụta ọnwụ ya dị elu karịa nke placebos na ọgwụ ndị ọzọ na-efunahụ ibu, na-ezute ụkpụrụ ndị EMA na FDA setịpụrụ maka ọgwụ na-efunahụ ibu, na ịnye nhọrọ ọgwụgwọ ọhụrụ maka ndị ọrịa buru ibu [1,2].
Mbelata ihe ize ndụ nke ọrịa obi:
Maka ndị okenye nwere ụdị ọrịa shuga 2 na ọrịa obi ama ama, Semaglutid nwere ike belata ihe ize ndụ nke ọrịa obi. Nnyocha ndị dị ka SUSTAIN 6 na ule 6 PIONEER gosipụtara adịghị ala na nchekwa nke Semaglutid subcutaneous na oral na ahụike obi, na ikpe SELECT kwadoro uru ọ nwere n'ịkwalite nsonaazụ obi, na-enyere aka belata ihe ize ndụ nke ihe omume obi [1].
Mmetụta nchebe gbasara akụrụ:
Na ụdị òké nke renal ischemia-reperfusion mmerụ, Semaglutid gosipụtara mmetụta nchebe gbasara akụrụ. Ọ na-ebelata ọkwa nke ụmụ irighiri ihe na-egbuke egbuke dị ka tumor necrosis factor-α (TNF-α) na onye na-anabata ya, interleukin-6 (IL-6), na-ebelata mmepụta F8 prostaglandin, na-abawanye ọkwa PI3K na AKT na anụ ahụ, ma na-ebelata mmerụ ahụ, na-atụ aro na Semaglutid nwere ike ịnwe ọgwụgwọ ọgwụgwọ maka nnukwu mmerụ ahụ akụrụ [7].
Mmechi
Dị ka onye na-anabata GLP-1, Semaglutid na-achịkwa ọkwa glucose ọbara nke ọma na ndị ọrịa nwere ụdị ọrịa shuga 2 nke ọma site na ịhazi insulin na secretion glucagon, na-egbochi gluconeogenesis imeju, na-emetụta metabolism ike na agụụ, ebe ọ na-ebelata oke ahụ na ndị buru oke ibu. Ọ nwere mmetụta nchebe nke obi, na-ebelata ihe ize ndụ nke ọrịa obi, ma na-echebe akụrụ. Ọ nwere mmetụta ọgwụgwọ na nnukwu mmerụ ahụ akụrụ, nephropathy na-arịa ọrịa shuga, na ọrịa akụrụ ndị ọzọ.
Banyere Onye dere ya
Ihe niile a kpọtụrụ aha n'elu bụ Cocer Peptides na-enyocha, dezie ma chịkọta ya.
Onye ode akwụkwọ akụkọ sayensị
Hegner, P. dabere na Mahadum Regensburg na Germany ma nwee ọtụtụ mmasị nyocha. Ndị a na-agụnye usoro obi na ọrịa obi, ebe ọ na-enyocha usoro na ọgwụgwọ nke ọrịa obi; biochemistry na molecular bayoloji, na-elekwasị anya na ikpughe usoro mmeghachi omume biochemical na usoro nhazi; nkà mmụta ọgwụ na ụlọ ahịa ọgwụ, na-emesi mmepe ọgwụ ike na nyocha arụmọrụ; na usoro iku ume yana ọgwụ n'ozuzu na nke ime, na-etinye uche na nyocha na ọgwụgwọ nke ọrịa iku ume na ọnọdụ ahụike dị n'ime. Ọ bụ ọkà mmụta nwere ihe ọ rụpụtara n'ọtụtụ ngalaba ọgwụ. Edepụtara Hegner P na ntụnye aka [6].
▎ Okwu ndị dị mkpa
[1] Oleszczuk R, Kozińska I, Gras-Ozimek J, et al. Semaglutid maka ọgwụgwọ oke ibu [J]. Akwụkwọ akụkọ nke Education, Health and Sport, 2022. https://api.semanticscholar.org/CorpusID:245423376.
[2] Christou GA, Katiki N, Blundell J, et al. Semaglutid dị ka ọgwụ mgbochi oke ibu na-ekwe nkwa [J]. Nlebanya oke ibu, 2019,20(6):805-815.DOI:10.1111/obr.12839.
[3] Kurtzhals P, Flindt Kreiner F, Singh Bindra R. Ọrụ njikwa ibu na njikwa ụdị ọrịa shuga mellitus 2: Echiche na semaglutide [J]. Nnyocha ọrịa shuga na omume ụlọ ọgwụ, 2023,203.DOI:10.1016/j.diabres.2023.110881.
[4] Chao AM, Tronieri JS, Amaro A, et al. Semaglutid maka ọgwụgwọ oke ibu [J]. Ụdị na ọgwụgwọ ọrịa obi, 2023,33 (3): 159-166.DOI: 10.1016 / j.tcm.2021.12.008.
[5] Cigrovski BM, Strollo F. Semaglutid-anya na-enweta nsonaazụ[J]. Akwụkwọ akụkọ ụwa nke ọrịa shuga, 2023,14 (4): 424-434.DOI: 10.4239 / wjd.v14.i4.424.
[6] Hegner P, Seitz S, Schopka S, et al. Semaglutid na-akwalite ọrụ nkwekọrịta na atrium mmadụ dịpụrụ adịpụ[J]. Akwụkwọ akụkọ obi European, 2024,45 (Mgbakwunye_1):ehae666-ehae3729.DOI:10.1093/eurheartj/ehae666.3729.
[7] Tiba AT, Qassam H, Hadi N R. Semaglutid na renal ischemia-reperfusion mmerụ na ụmụ oke[J]. J Med Ndụ, 2023,16 (2):317-324.DOI:10.25122/jml-2022-0291.
Edemede na ozi ngwaahịa niile enyere na webụsaịtị a bụ naanị maka mgbasa ozi na ebumnuche mmụta.
Ngwaahịa ndị enyere na webụsaịtị a bụ naanị maka nyocha in vitro. A na-eme nyocha in vitro (Latin: * na iko *, nke pụtara na ihe eji enyo) na mpụga ahụ mmadụ. Ngwaahịa ndị a abụghị ọgwụ, ndị US Food and Drug Administration (FDA) akwadoghị ya, ha agaghịkwa eji ya gbochie, gwọọ, ma ọ bụ gwọọ ọnọdụ ahụike ọ bụla, ọrịa, ma ọ bụ ọrịa. Iwu amachibidoro nke ọma iwebata ngwaahịa ndị a n'ime ahụ mmadụ ma ọ bụ anụmanụ n'ụdị ọ bụla.