Apejuwe

Obeticholic acid (INT-747) jẹ alagbara, yiyan ati agonist FXR ti n ṣiṣẹ ni ẹnu pẹlu EC50 ti 99 nM. Obeticholic acid ni ipa anticholeretic ati egboogi-iredodo. Obeticholic acid tun fa autophagy [1][2][3].

abẹlẹ

Obeticholic Acid (6alpha-ethyl-chenodeoxycholic acid, 6-ECDCA, INT-747) jẹ agonist ti o lagbara ati yiyan ti FXR pẹlu iye EC50 ti 99 nM [1].

Olugba farnesoid X (FXR) jẹ olugba bile acid iparun kan ti o ni ipa ninu homeostasis bile acid, ẹdọ fibrosis, ẹdọ ẹdọ ati iredodo ifun ati arun inu ọkan ati ẹjẹ [2].

Obeticholic Acid jẹ agonist FXR ti o lagbara ati yiyan pẹlu iṣẹ anticholeretic [1]. Obeticholic Acid jẹ itọsẹ bile acid semisynthetic ati ligand FXR ti o lagbara. Ninu awọn eku cholestasis ti estrogen ti o fa, 6-ECDCA ni aabo lodi si cholestasis ti o fa nipasẹ 17a-ethynylestradiol (E217α) [2]. Ni cirrhotic portal haipatensonu (PHT) awọn awoṣe eku, INT-747 (30 miligiramu/kg) tun mu FXR ti ọna ifihan agbara isale ati dinku titẹ ẹnu-ọna nipasẹ gbigbe silẹ lapapọ intrahepatic resistance resistance (IHVR) laisi haipatensonu eto eto. Ipa yii ni nkan ṣe pẹlu iṣẹ eNOS ti o pọ si [3]. Ninu awoṣe eku Dahl ti haipatensonu ifamọ iyọ ati insulin-resistance (IR), iyọ ti o ga (HS) ounjẹ ti o pọ si ni titẹ ẹjẹ eto eto ati ikosile DDAH tissu isalẹ. INT-747 ṣe imudara ifamọ hisulini ati ṣe idiwọ idinku ti ikosile DDAH [4].

Awọn itọkasi:
[1]. Pellicciari R, Fiorucci S, Camaioni E, ati al. 6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), agonist FXR ti o lagbara ati yiyan ti a fun ni iṣẹ ṣiṣe anticholestatic. J Med Chem, 2002, 45 (17): 3569-3572.
[2]. Fiorucci S, Clerici C, Antonelli E, et al. Awọn ipa aabo ti 6-ethyl chenodeoxycholic acid, ligand olugba ti farnesoid X, ni estrogen-induced cholestasis. J Pharmacol Exp Ther, 2005, 313 (2): 604-612.
[3]. Verbeke L, Farre R, Trebicka J, ati al. Obeticholic acid, agonist olugba olugba farnesoid X, ṣe ilọsiwaju haipatensonu ẹnu-ọna nipasẹ awọn ipa ọna ọtọtọ meji ni awọn eku cirrhotic. Hepatology, 2014, 59 (6): 2286-2298.
[4]. Ghebremariam YT, Yamada K, Lee JC, ati al. FXR agonist INT-747 ṣe atunṣe ikosile DDAH ati mu ifamọ hisulini pọ si ni awọn eku Dahl ti o jẹ iyọ-giga. PLoS Ọkan, 2013, 8 (4): e60653.

Itọkasi ọja

• 1. Selina Costa. "Ṣiṣe apejuwe Ligand aramada kan fun Olugba Farnesoid X nipa lilo Zebrafish Transgenic." Yunifasiti ti Toronto. Oṣu Kẹjọ-2018.
• 2. Kent, Rebeka. "Awọn ipa ti Fenofibrate lori CYP2D6 ati Ilana ti ANG1 ati RNASE4 nipasẹ FXR Agonist Obeticholic Acid." indigo.uic.edu.2017.

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Jẹmọ Biological Data

Jẹmọ Biological Data