Fa'amatalaga

Obeticholic acid (INT-747) o se agonist FXR malosi, filifilia ma tautala fa'atasi ma le EC50 o le 99 nM. Obeticholic acid ei ai le anticholeretic ma le anti-inflammation aafiaga. Obeticholic acid e fa'aosoina ai fo'i le autophagy[1][2][3].

Talaaga

Obeticholic Acid (6alpha-ethyl-chenodeoxycholic acid, 6-ECDCA, INT-747) o se agonist malosi ma filifilia o le FXR ma le EC50 tau o le 99 nM [1].

O le farnesoid X receptor (FXR) o le faʻamaʻi faʻamaʻi faaniukilia o loʻo aʻafia i le homeostasis acid, fibrosis ate, faʻamaʻi o le ate ma le intestinal ma maʻi cardiovascular [2].

Obeticholic Acid o se agonist FXR malosi ma filifilia ma le anticholeretic gaioiga [1]. Obeticholic Acid o se semisynthetic bile acid e maua mai ma malosi FXR ligand. I le estrogen-induced cholestasis rats, 6-ECDCA puipuia mai cholestasis induced e 17α-ethynylestradiol (E217α) [2]. I fa'ata'ita'iga o isumu o le toto toto maualuga (PHT), INT-747 (30 mg/kg) toe fa'agaoioia le ala fa'ailoga o le FXR i lalo ma fa'aitiitia le mamafa o le faitoto'a e ala i le fa'aitiitia o le fa'ato'aga toto toto (IHVR) e aunoa ma le fa'aleagaina o le toto. O lenei aafiaga na fesoʻotaʻi ma le faʻateleina o le eNOS [3]. I le faʻataʻitaʻiga a le Dahl rat o le maualuga o le masima maʻaleʻale ma le inisalini-resistance (IR), taumafa masima maualuga (HS) faʻateleina le maualuga o le toto toto ma faʻaititia le faʻaaliga DDAH. INT-747 faʻaleleia le faʻaogaina o le inisalini ma faʻalavelaveina le faʻaitiitia o le faʻamatalaga DDAH [4].

Fa'asinomaga:
[1]. Pellicciari R, Fiorucci S, Camaioni E, et al. 6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), o se agonist FXR malosi ma filifilia ua faʻamanuiaina i le gaioiga anticholestatic. J Med Chem, 2002, 45(17): 3569-3572.
[2]. Fiorucci S, Clerici C, Antonelli E, et al. O a'afiaga puipuia o le 6-ethyl chenodeoxycholic acid, o le farnesoid X receptor ligand, i le estrogen-induced cholestasis. J Pharmacol Exp Ther, 2005, 313(2): 604-612.
[3]. Verbeke L, Farre R, Trebicka J, et al. Obeticholic acid, ose fanesoid X receptor agonist, fa'aleleia le toto toto maualuga e ala i auala ma'oti se lua i isumu cirrhotic. Hepatology, 2014, 59 (6): 2286-2298.
[4]. Ghebremariam YT, Yamada K, Lee JC, et al. FXR agonist INT-747 faʻaleleia le faʻamatalaga DDAH ma faʻaleleia le faʻaogaina o le inisalini i luga o le masima fafaga Dahl rats. PLoS Tasi, 2013, 8(4): e60653.

Fa'amatalaga o oloa

• 1. Selina Costa. "Faʻailogaina o se Ligand Novel mo le Farnesoid X Receptor faʻaaogaina Transgenic Zebrafish." Iunivesite o Toronto. Iuni-2018.
• 2. Keni, Repeka. "Aafiaga o Fenofibrate i luga ole CYP2D6 ma Tulafono Faʻatonutonu o ANG1 ma RNASE4 e le FXR Agonist Obeticholic Acid." indigo.uic.edu.2017.

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