Keeb kwm

Ezetimibe yog lub zog thiab tshiab inhibitor ntawm kev nqus cov cholesterol [1].

Cov roj (cholesterol) yog ib qho lipid molecule thiab yuav tsum tau tsim thiab tswj cov ntaub so ntswg kev ncaj ncees thiab fluidity.Tsis tas li, nws ua haujlwm ua ntej ntawm vitamin D, kua tsib acids thiab steroid hormones.

Nyob rau hauv sib txawv Caco-2 hlwb incubated nrog ib tug carotenoid (1 μM), ezetimibe (10 mg / L) inhibited carotenoid thauj nrog 50% inhibition rau ɑ-carotene thiab β-carotene.Tsis tas li ntawd, nws inhibited kev thauj mus los ntawm β-cryptoxanthin, lycopene thiab lutein: zeaxanthin (1: 1).Nyob rau tib lub sijhawm, ezetimibe inhibited cholesterol thauj los ntawm 31%.Ezetimibe txo qhov kev qhia ntawm qhov chaw receptors SR-BI, ATP binding cassette transporter, subfamily A (ABCA1), Niemann-Pick hom C1 Zoo li 1 protein (NPC1L1) thiab retinoid acid receptor (RAR)γ, sterol-regulatory element binding proteins SREBP -1 thiab SREBP-2, thiab daim siab X receptor (LXR)β [3].

Hauv apolipoprotein E knockout (apoE-/-) nas, ezetimibe (3 mg / kg) inhibited cholesterol absorption los ntawm 90%.Ezetimibe txo cov roj cholesterol hauv plasma, nce qib HDL, thiab inhibits kev loj hlob ntawm atherosclerosis [1].Hauv theem III tib neeg kev sim, Ezetimibe (10 mg) txo qis cov roj cholesterol LDL, tag nrho cov roj cholesterol thiab triglycerides thiab nce qib HDL cholesterol [2].

Cov ntaub ntawv:
[1].Davis HR Jr, Compton DS, Hoos L, et al.Ezetimibe, uas muaj peev xwm nqus tau cov roj cholesterol inhibitor, inhibits kev loj hlob ntawm atherosclerosis hauv ApoE knockout nas.Arterioscler Thromb Vasc Biol, 2001, 21(12): 2032-2038.
[2].Clader JW.Kev tshawb pom ntawm ezetimibe: kev pom los ntawm sab nraum lub receptor.J Med Chem, 2004, 47(1): 1-9.
[3].Thaum A, Dawson HD, Harrison EH.Carotenoid thauj yog txo qis thiab qhia txog cov lipid transporters SR-BI, NPC1L1, thiab ABCA1 yog downregulated nyob rau hauv Caco-2 hlwb kho nrog ezetimibe.J Nutr, 2005, 135(10): 2305-2312.

Kev piav qhia

Ezetimibe (SCH 58235) yog ib qho muaj zog cholesterol absorption inhibitor.Ezetimibe yog Niemann-Pick C1-like1 (NPC1L1) inhibitor, thiab yog Nrf2 activator muaj zog.

Hauv Vitro

Ezetimibe (Eze) ua raws li lub zog Nrf2 activator tsis ua rau cytotoxicity.Ezetimibe txhim kho kev hloov pauv ntawm Nrf2, raws li qhia los ntawm tus kws tshuaj xyuas luciferase.Ezetimibe kuj upregulates Nrf2 hom noob, suav nrog GSTA1, heme oxygenase-1 (HO-1) thiab Nqo-1 hauv Hepa1c1c7 thiab MEF hlwb.Ezetimibe upregulates Nrf2 lub hom phiaj noob hauv Nrf2 +/+ MEF hlwb, qhov no induction tag nrho thaiv hauv Nrf2-/- MEF hlwb.Noj ua ke, Ezetimibe ua raws li tus tshiab Nrf2 inducer nyob rau hauv ib tug ROS-ywj siab yam [1].Tib neeg huh7 hepatocytes yog pretreated nrog Ezetimibe (10μM, 1 h) thiab incubated nrog palmitic acid (PA, 0.5 mM, 24 h) induce hepatic steatosis.Kev kho Ezetimibe ua rau txo qis PA-nce triglycerides (TG) qib, uas zoo ib yam nrog peb txoj kev tshawb fawb tsiaj.Kev kho PA ua rau muaj kwv yees li 20% txo qis hauv mRNA qhia ntawm ATG5, ATG6, thiab ATG7, uas tau nce los ntawm kev kho Ezetimibe.Tsis tas li ntawd, Ezetimibe kev kho mob tau nce qhov PA-vim txo qis hauv LC3 protein ntau [2].

MCE tsis tau lees paub qhov tseeb ntawm cov txheej txheem no.Lawv yog rau siv xwb.

Kev tswj hwm ntawm Ezetimibe (Eze) txo lub siab hnyav ntawm cov nas noj methionine- thiab choline-deficient (MCD) noj.Qhov no zoo ib yam nrog cov txiaj ntsig zoo ntawm Ezetimibe ntawm hepatic steatosis.Lub siab histology qhia tau hais tias muaj ntau yam macrovesicular cov roj hauv cov nas ntawm MCD noj, tab sis kev kho Ezetimibe ua rau txo qis thiab qhov loj ntawm cov tee dej no.Tsis tas li ntawd, cov kab mob siab fibrosis hauv cov nas noj MCD noj zaub mov yog qhov txo qis los ntawm Ezetimibe[1].Cov ntshav thiab siab lipid qib suav nrog TG, cov rog dawb (FFA), thiab tag nrho cov roj (TC) tau txo qis hauv Ezetimibe-kho OLETF nas.Ntxiv mus, OLETF nas qhia cov ntshav qabzib ntau dua ntawm cov piam thaj, insulin, HOMA-IR, TG, FFA, thiab TC dua li LETF tsiaj, uas txo qis los ntawm Ezetimibe.Tsis tas li ntawd, kev soj ntsuam histological tau qhia tias OLETF tswj nas pom cov lipid loj dua hauv hepatocytes dua li cov hnub nyoog sib tw LETO tswj, uas tau txo qis los ntawm kev tswj hwm ntawm Ezetimibe[2].

Cia

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