Ka morao

Ezetimibe ke inhibitor e matla le e ncha ea ho monya k'holeseterole [1].

Cholesterol ke molek'hule ea lipid 'me e hlokahala ho haha ​​​​le ho boloka lera le ts'epahalo ea sebopeho le mokelikeli.Hape, e sebetsa e le selelekela sa vithamine D, bile acid le lihomone tsa steroid.

Liseleng tse fapaneng tsa Caco-2 tse kenngoeng ka carotenoid (1 μM), ezetimibe (10 mg / L) e thibela lipalangoang tsa carotenoid ka 50% thibela bakeng sa ɑ-carotene le β-carotene.Hape, e ne e thibela ho tsamaisoa ha β-cryptoxanthin, lycopene le lutein:zeaxanthin(1:1).Ka nako e ts'oanang, ezetimibe e ile ea thibela lipalangoang tsa k'holeseterole ka 31%.Ezetimibe e fokolitse polelo ea li-receptor tse holimo tsa SR-BI, sepalangoang sa lik'hasete se tlamang ATP, lelapa le ka tlase la A (ABCA1), mofuta oa Niemann-Pick C1 Joalo ka protheine e 1 (NPC1L1) le retinoid acid receptor (RAR) γ, sterol-regulatory element e tlamang liprotheine SREBP -1 le SREBP-2, le sebete sa X receptor (LXR)β [3].

Ho apolipoprotein E knockout (apoE-/-) litoeba, ezetimibe (3 mg/kg) e thibela ho monya k'holeseterole ka 90%.Ezetimibe e fokotsa k'holeseterole ea plasma, ea eketsa maemo a HDL, 'me e thibela tsoelo-pele ea atherosclerosis [1].Mokhahlelong oa III oa liteko tsa batho, Ezetimibe (10 mg) e fokolitse haholo maemo a LDL cholesterol, cholesterol eohle le triglycerides mme ea eketsa boemo ba HDL cholesterol [2].

Litšupiso:
[1].Davis HR Jr, Compton DS, Hoos L, et al.Ezetimibe, e leng "cholesterol absorption inhibitor" e matla, e thibela nts'etsopele ea atherosclerosis ho litoeba tsa ApoE knockout.Arterioscler Thromb Vasc Biol, 2001, 21 (12): 2032-2038.
[2].Clader JW.Ho sibolloa ha ezetimibe: pono e tsoang kantle ho moamoheli.J Med Chem, 2004, 47(1): 1-9.
[3].Nakong ea A, Dawson HD, Harrison EH.Lipalangoang tsa carotenoid li fokotsehile mme polelo ea li-lipid transporters SR-BI, NPC1L1, le ABCA1 e fokotsehile ka liseleng tsa Caco-2 tse tšoaroang ka ezetimibe.J Nutr, 2005, 135 (10): 2305-2312.

Tlhaloso

Ezetimibe (SCH 58235) ke inhibitor e matla ea ho monya cholesterol.Ezetimibe ke inhibitor ea Niemann-Pick C1-like1 (NPC1L1), 'me ke activator e matla ea Nrf2.

Ka Vitro

Ezetimibe (Eze) e sebetsa joalo ka activator e matla ea Nrf2 ntle le ho baka cytotoxicity.Ezetimibe e ntlafatsa phetisetso ea Nrf2, joalo ka ha e senotsoe ke tlhahlobo ea moqolotsi oa litaba oa luciferase.Ezetimibe e boetse e laola liphatsa tsa lefutso tsa Nrf2, ho akarelletsa le GSTA1, heme oxygenase-1 (HO-1) le Nqo-1 ho Hepa1c1c7 le lisele tsa MEF.Ezetimibe e laola liphatsa tsa lefutso tsa Nrf2 ho lisele tsa Nrf2 +/+ MEF, athe tlhahiso ena e koetsoe ka ho feletseng liseleng tsa Nrf2-/- MEF.Ha e kopantsoe hammoho, Ezetimibe e sebetsa joalo ka moqapi oa Nrf2 ka mokhoa o ikemetseng oa ROS[1].Li-hepatocyte tsa huh7 tsa motho li entsoe pele ka Ezetimibe (10μM, 1 h) le ho kenngoa ka palmitic acid (PA, 0.5 mM, 24 h) ho susumetsa sebete sa steatosis.Kalafo ea Ezetimibe e nyenyefatsa haholo maemo a PA-keketseho ea triglycerides (TG), e lumellanang le thuto ea rona ea liphoofolo.Kalafo ea PA e hlahisitse phokotseho e ka bang 20% ​​ho polelo ea mRNA ea ATG5, ATG6, le ATG7, e neng e ekelitsoe ke kalafo ea Ezetimibe.Ntle le moo, kalafo ea Ezetimibe e ile ea eketsa haholo phokotso e bakoang ke PA ho bongata ba liprotheine tsa LC3[2].

MCE ha e e-so tiise ka boikemelo ho nepahala ha mekhoa ena.Ke tsa litšupiso feela.

Tsamaiso ea Ezetimibe (Eze) e fokotsa boima ba sebete ba litoeba tse fepang lijo tsa methionine- le choline-deficient (MCD).Sena se lumellana le litlamorao tse ntle tsa Ezetimibe ho hepatic steatosis.Histology ea sebete e bonts'a marotholi a mangata a mafura a macrovesicular ho litoeba lijong tsa MCD, empa kalafo ea Ezetimibe e fokotsa palo le boholo ba marotholi ao haholo.Ho feta moo, hepatic fibrosis ho litoeba tse fepang lijo tsa MCD e fokotsoa haholo ke Ezetimibe[1].Maemo a mali le sebete a lipid ho kenyelletsa TG, mafura a mahala a acid (FFA), le k'holeseterole kaofela (TC) a fokotsehile haholo ho likhoto tsa OLETF tse tšoaroang ke Ezetimibe.Ho feta moo, likhoto tsa OLETF li bonts'a maemo a phahameng a serum a tsoekere, insulin, HOMA-IR, TG, FFA, le TC ho feta liphoofolo tsa LETF, tse fokolitsoeng haholo ke Ezetimibe.Ntle le moo, tlhahlobo ea nalane ea nalane e bonts'itse hore likhoto tsa taolo ea OLETF li bonts'itse marotholi a maholo a lipid ho hepatocyte ho feta taolo ea LETO e lekanang le lilemo, e fokotsoang ke tsamaiso ea Ezetimibe[2].

Polokelo

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