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Ezetimibe

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Magaca API	Tilmaam	Tilmaamid	US DMF	Midowga Yurub DMF	CEP
Ezetimibe	Hyperlipidemia	Guriga dhexdiisa/USP	24511	√

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Asalkii hore

Ezetimibe waa horjooge awood leh oo hor leh oo ka hortagaya nuugista kolestaroolka [1].

Kolestaroolku waa unugyadu dufan waxaana looga baahan yahay inay dhisto oo ilaaliso hufnaanta qaabdhismeedka xuubka iyo dareeraha.Sidoo kale, waxay u adeegtaa sidii horudhac u ah fitamiin D, bile acids iyo hormoonnada steroids.

Unugyada Caco-2 ee kala duwan oo lagu daray carotenoid (1 μM), ezetimibe (10 mg / L) waxay joojiyeen gaadiidka carotenoid oo leh 50% xannibaad ɑ-carotene iyo β-carotene.Sidoo kale, waxay hakisay gaadiidka β-cryptoxanthin, lycopene iyo lutein: zeaxanthin (1: 1).Isla mar ahaantaana, ezetimibe waxay joojisay gaadiidka kolestaroolka 31%.Ezetimibe waxay hoos u dhigtay muujinta soo-dhoweynta dusha sare ee SR-BI, ATP-ga-qaadista cajaladaha, ATP-dabiiciga ah, qoyska A (ABCA1), Niemann-Pick nooca C1 Like 1 protein (NPC1L1) iyo retinoid acid reseptor (RAR) -1 iyo SREBP-2, iyo beerka X reseptor (LXR) β [3].

Marka lagu jiro apolipoprotein E knockout (apoE-/-) jiirarka, ezetimibe (3 mg/kg) waxay joojisay nuugista kolestaroolka 90%.Ezetimibe waxay hoos u dhigtay kolestaroolka balaasmaha, waxay kordhisay heerarka HDL, waxayna joojisaa horumarka atherosclerosis [1].Marxaladda III ee tijaabooyinka aadanaha, Ezetimibe (10 mg) ayaa si weyn hoos ugu dhigay heerarka LDL kolestaroolka, wadarta kolestaroolka iyo triglycerides waxayna kordhisay heerka kolestaroolka HDL [2].

Tixraacyo:
[1]Davis HR Jr, Compton DS, Hoos L, iyo al.Ezetimibe, oo ah horjoogaha nuugista kolestaroolka ee xoogga leh, wuxuu horjoogsadaa horumarinta atherosclerosis ee jiirarka garaaca ApoE.Arterioscler Thromb Vasc Biol, 2001, 21 (12): 2032-2038.
[2].Clader JW.Helitaanka ezetimibe: aragti ka baxsan receptor.J Med Chem, 2004, 47 (1): 1-9.
[3]Inta lagu jiro A, Dawson HD, Harrison EH.Gaadiidka Carotenoid waa la dhimay iyo muujinta gaadiidleyda dufanka leh ee SR-BI, NPC1L1, iyo ABCA1 ayaa hoos loo dhigay unugyada Caco-2 ee lagu daweeyay ezetimibe.J Nutr, 2005, 135 (10): 2305-2312.

Sharaxaada

Ezetimibe (SCH 58235) waa ka hortag awood badan oo nuugista kolestaroolka.Ezetimibe waa Niemann-Pick C1-like1 (NPC1L1) horjooge, waana firfircoone Nrf2 awood leh.

In Vitro

Ezetimibe (Eze) wuxuu u shaqeeyaa sidii firfircooni Nrf2 awood leh isagoon keenin cytotoxicity.Ezetimibe waxay wanaajisaa wax ka beddelka Nrf2, sida uu shaaca ka qaaday qiimaynta wariye luciferase.Ezetimibe waxay sidoo kale kor u qaaddaa hiddo-wadaha Nrf2, oo ay ku jiraan GSTA1, heme oxygenase-1 (HO-1) iyo Nqo-1 ee Hepa1c1c7 iyo unugyada MEF.Ezetimibe waxay hagaajisaa hiddo-wadaha bartilmaameedka Nrf2 ee unugyada Nrf2 +/+ MEF, halka soo-gelintani ay gebi ahaanba xannibtay unugyada Nrf2-/- MEF.Isku soo wada duuboo, Ezetimibe wuxuu u dhaqmaa sidii sheeko Nrf2 inducer si madax-banaan ROS[1].Human huh7 hepatocytes waxaa lagu sii daaweeyay Ezetimibe (10μM.Daaweynta Ezetimibe waxay si weyn u yaraynaysaa heerarka PA-kordhinta triglycerides (TG), taas oo la socota daraasaddeena xayawaanka.Daaweynta PA waxay keentay in ku dhawaad 20% hoos u dhac ku yimaado muujinta mRNA ee ATG5, ATG6, iyo ATG7, oo ay kordhisay daawaynta Ezetimibe.Intaa waxaa dheer, daaweynta Ezetimibe waxay si weyn u kordhisay hoos u dhigista PA-ku-dhimista ee borotiinka LC3.

MCE si madaxbanaan uma xaqiijin saxnaanta hababkan.Waxay yihiin tixraac kaliya.

Maamulka Ezetimibe (Eze) wuxuu yareeyaa miisaanka beerka ee jiirarka la quudiyo methionine- iyo choline-deficient (MCD).Tani waxay la socotaa saamaynta faa'iidada leh ee Ezetimibe ee steatosis cagaarshow.Histology-ga beerka ayaa muujinaya dhibco dufan badan oo makrovesicular ah oo ku jira jiirarka cuntada MCD, laakiin daaweynta Ezetimibe waxay si muuqata u yaraynaysaa tirada iyo xajmiga dhibcahaas.Intaa waxaa dheer, fibrosis cagaarshow ee jiirarka la quudiyo cuntada MCD waxaa si weyn u yareeyey Ezetimibe[1].Heerarka dufanka beerka iyo dhiigga oo ay ku jiraan TG, acids dufanka bilaashka ah (FFA), iyo wadarta kolestaroolka (TC) ayaa si weyn hoos ugu dhacay jiirka OLETF ee Ezetimibe-daaweeyay.Waxaa intaa dheer, jiirarka OLETF waxay muujinayaan heerarka serum ee gulukooska, insulin, HOMA-IR, TG, FFA, iyo TC marka loo eego xayawaanka LETF, kuwaas oo ay si weyn hoos ugu dhigtay Ezetimibe.Intaa waxaa dheer, falanqaynta taariikhiga ah waxay muujisay in kontoroolka OLETF uu muujiyay dhibcaha dufanka weyn ee hepatocytes marka loo eego kontaroolada LETO ee da'da ah, kuwaas oo ay hoos u dhigeen maamulka Ezetimibe[2].

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