Fage

Ezetimibe mai ƙarfi ne kuma sabon abu mai hana sha cholesterol [1].

Cholesterol kwayar halitta ce ta lipid kuma ana buƙatar ginawa da kiyaye amincin tsarin membranes da ruwa.Hakanan, yana aiki azaman mafarin bitamin D, bile acid da hormones na steroid.

A cikin sel Caco-2 daban-daban waɗanda aka haɗa tare da carotenoid (1 μM), ezetimibe (10 mg / L) ya hana jigilar carotenoid tare da hana 50% don ɑ-carotene da β-carotene.Hakanan, ya hana jigilar β-cryptoxanthin, lycopene da lutein: zeaxanthin (1: 1).A lokaci guda, ezetimibe ya hana jigilar cholesterol da kashi 31%.Ezetimibe ya rage bayyanar da masu karɓa na saman SR-BI, mai ɗaukar kaset na ATP, rukunin gida A (ABCA1), nau'in Niemann-Pick C1 Kamar furotin 1 (NPC1L1) da mai karɓar mai karɓar acid na retinoid (RAR) γ, sterol-regulatory element mai ɗaure sunadarai -1 da SREBP-2, da kuma hanta X mai karɓa (LXR) β [3].

A cikin apolipoprotein E knockout (apoE-/-) mice, ezetimibe (3 mg / kg) ya hana ƙwayar cholesterol ta 90%.Ezetimibe ya rage ƙwayar cholesterol na plasma, ƙara yawan matakan HDL, kuma yana hana ci gaban atherosclerosis [1].A cikin gwaji na mutum na III, Ezetimibe (10 MG) ya rage mahimmancin matakan LDL cholesterol, jimlar cholesterol da triglycerides kuma ya haɓaka matakin HDL cholesterol [2].

Magana:
[1].Davis HR Jr, Compton DS, Hoos L, et al.Ezetimibe, mai hana ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar cuta ta ApoE.Arterioscler Thromb Vasc Biol, 2001, 21 (12): 2032-2038.
[2].Clader JW.Gano ezetimibe: ra'ayi daga wajen mai karɓa.J Med Chem, 2004, 47 (1): 1-9.
[3].Lokacin A, Dawson HD, Harrison EH.An rage jigilar Carotenoid kuma an rage bayanin masu jigilar lipid SR-BI, NPC1L1, da ABCA1 a cikin ƙwayoyin Caco-2 da aka bi da su tare da ezetimibe.J Nutr, 2005, 135 (10): 2305-2312.

Bayani

Ezetimibe (SCH 58235) shine mai hana ƙwayar cholesterol mai ƙarfi.Ezetimibe mai hana Niemann-Pick C1-like1 (NPC1L1), kuma mai kunnawa Nrf2 ne mai ƙarfi.

A cikin Vitro

Ezetimibe (Eze) yana aiki azaman mai kunnawa Nrf2 mai ƙarfi ba tare da haifar da cytotoxicity ba.Ezetimibe yana haɓaka ma'amala na Nrf2, kamar yadda wani bincike na luciferase ya bayyana.Ezetimibe kuma yana haɓaka kwayoyin Nrf2 manufa, ciki har da GSTA1, heme oxygenase-1 (HO-1) da Nqo-1 a cikin kwayoyin Hepa1c1c7 da MEF.Ezetimibe yana haɓaka ƙwayoyin Nrf2 manufa a cikin ƙwayoyin Nrf2 +/+ MEF, yayin da wannan ƙaddamarwar an katange gaba ɗaya a cikin ƙwayoyin Nrf2-/- MEF.A hade tare, Ezetimibe yana aiki a matsayin sabon labari Nrf2 inducer a cikin tsarin ROS mai zaman kansa[1].Human huh7 hepatocytes an riga an gyara su tare da Ezetimibe (10μM, 1 h) kuma an haɗa shi da palmitic acid (PA, 0.5 mM, 24 h) don haifar da steatosis na hanta.Maganin Ezetimibe yana haɓaka matakan haɓakar triglycerides (TG) na PA, wanda ya yi daidai da binciken dabbarmu.Maganin PA ya haifar da raguwar kusan 20% a cikin maganganun mRNA na ATG5, ATG6, da ATG7, wanda jiyya na Ezetimibe ya karu.Bugu da ƙari, jiyya na Ezetimibe ya ƙaru da raguwar da aka haifar da PA a cikin yawan furotin LC3 [2].

MCE ba ta tabbatar da daidaiton waɗannan hanyoyin da kanta ba.Suna don tunani kawai.

Gudanar da Ezetimibe (Eze) yana rage nauyin hanta na berayen da ake ciyar da abincin methionine- da choline-ranci (MCD).Wannan ya yi daidai da amfanin amfanin Ezetimibe akan steatosis na hanta.Ilimin tarihin hanta yana nuna ɗigon kitse masu yawa a cikin beraye akan abincin MCD, amma magani na Ezetimibe yana rage adadin da girman waɗancan ɗigon.Bugu da ƙari, fibrosis na hanta a cikin berayen da ke ciyar da abinci na MCD yana da mahimmanci ta hanyar Ezetimibe[1].Matakan lipid na jini da hanta ciki har da TG, free fatty acids (FFA), da jimillar cholesterol (TC) sun ragu sosai a cikin berayen OLETF da Ezetimibe ke yi wa magani.Bugu da ƙari, berayen OLETF suna nuna matakan jini mafi girma na glucose, insulin, HOMA-IR, TG, FFA, da TC fiye da dabbobin LETF, waɗanda Ezetimibe ya ragu sosai.Bugu da ƙari, nazarin tarihi ya nuna cewa berayen masu kula da OLETF sun nuna ɗigon lipid mafi girma a cikin hepatocytes fiye da shekarun da suka dace da LETO controls, waɗanda ke ragewa ta hanyar gudanarwa na Ezetimibe[2].

Ajiya

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