Inkcazo

I-Obeticholic acid (INT-747) yi-agonist enamandla, ekhethiweyo kwaye esebenzayo ngomlomo kunye ne-EC50 ye-99 nM.I-Obeticholic acid ine-anticholeretic kunye ne-anti-inflammation effect.I-Obeticholic acid ikwabangela ukuguga kwemizimba[1][2][3].

Imvelaphi

I-Obeticholic Acid (i-6alpha-ethyl-chenodeoxycholic acid, i-6-ECDCA, i-INT-747) i-agonist enamandla kwaye ekhethiweyo ye-FXR enexabiso le-EC50 le-99 nM [1].

I-farnesoid X receptor (FXR) yi-nuclear bile acid receptor ebandakanyeka kwi-bile acid homeostasis, i-fibrosis yesibindi, ukuvutha kwesibindi kunye namathumbu kunye nesifo senhliziyo [2].

I-Obeticholic Acid inamandla kwaye ikhetha i-agonist yeFXR kunye nomsebenzi we-anticholeretic [1].I-Obeticholic Acid yi-semisynthetic bile acid derivative kunye ne-FXR ligand enamandla.Kwiigundane ze-cholestasis ezenziwe nge-estrogen, i-6-ECDCA ikhuselwe kwi-cholestasis eyenziwa yi-17α-ethynylestradiol (E217α) [2].Kwiimodeli zegundane ze-cirrhotic portal hypertension (PHT), i-INT-747 (30 mg / kg) iphinde yavuselela i-FXR ezantsi kwendlela yomqondiso kunye nokunciphisa uxinzelelo lwe-portal ngokunciphisa i-intrahepatic vascular resistance (IHVR) ngaphandle kokucima i-systemic hypotension.Esi siphumo sasinxulumene nomsebenzi owandisiweyo we-eNOS [3].Kwimodeli ye-Dahl ye-rat ye-salt-sensitive hypertension kunye ne-insulin-resistance (IR), ityuwa ephezulu (HS) yokutya yandisa kakhulu uxinzelelo lwegazi lwenkqubo kunye nokunciphisa ukubonakaliswa kwe-DDAH kwezicubu.I-INT-747 iphucule ubuntununtunu be-insulin kwaye yanqanda ukuhla kwentetho ye-DDAH [4].

IiReferensi:
[1].Pellicciari R, Fiorucci S, Camaioni E, et al.I-6alpha-ethyl-chenodeoxycholic acid (i-6-ECCDA), i-agonist enamandla kwaye ekhethiweyo ye-FXR enikwe umsebenzi we-anticholestatic.J Med Chem, 2002, 45(17): 3569-3572.
[2].Fiorucci S, Clerici C, Antonelli E, et al.Iziphumo ezikhuselayo ze-6-ethyl chenodeoxycholic acid, i-farnesoid X receptor ligand, kwi-cholestasis eyenziwe nge-estrogen.J Pharmacol Exp Ther, 2005, 313 (2): 604-612.
[3].Verbeke L, Farre R, Trebicka J, et al.I-Obeticholic acid, i-farnesoid X receptor agonist, iphucula i-portal hypertension ngeendlela ezimbini ezihlukeneyo kwiigundane ze-cirrhotic.I-Hepatology, i-2014, i-59 (6): 2286-2298.
[4].Ghebremariam YT, Yamada K, Lee JC, et al.I-FXR agonist INT-747 ilawula ukubonakaliswa kwe-DDAH kwaye iphakamisa ukuvakalelwa kwe-insulin kwiigundane ze-Dahl ezinetyuwa eninzi.PLoS One, 2013, 8(4): e60653.

Imveliso Citation

• 1. Selina Costa."Ukulinganisa i-Novel Ligand yeFarnesoid X Receptor usebenzisa iTransgenic Zebrafish."IYunivesithi yaseToronto.Jun-2018.
• 2. UKent, uRebecca."Iimpembelelo zeFenofibrate kwi-CYP2D6 kunye noLawulo lwe-ANG1 kunye ne-RNASE4 yi-FXR Agonist Obeticholic Acid."indigo.uic.edu.2017.

Ugcino

Ubume beMichiza

Idatha yeBiological eNxulumeneyo

Idatha yeBiological eNxulumeneyo