Kufotokozera

Obeticholic acid (INT-747) ndi FXR agonist yamphamvu, yosankha komanso yogwira pakamwa yokhala ndi EC50 ya 99 nM.Obeticholic acid imakhala ndi anticholeretic ndi anti-inflammatory effect.Obeticholic acid imapangitsanso autophagy [1] [2] [3].

Mbiri

Obeticholic Acid (6alpha-ethyl-chenodeoxycholic acid, 6-ECDCA, INT-747) ndi agonist wamphamvu komanso wosankha wa FXR wokhala ndi EC50 mtengo wa 99 nM [1].

Farnesoid X receptor (FXR) ndi nyukiliya ya bile acid receptor yomwe imakhudzidwa ndi bile acid homeostasis, chiwindi fibrosis, kutupa kwa chiwindi ndi matumbo ndi matenda amtima [2].

Obeticholic Acid ndi FXR agonist wamphamvu komanso wosankha wokhala ndi anticholeretic [1].Obeticholic Acid ndi semisynthetic bile acid yochokera ku FXR ligand yamphamvu.Mu makoswe opangidwa ndi estrogen-induced cholestasis, 6-ECDCA yotetezedwa ku cholestasis yopangidwa ndi 17α-ethynylestradiol (E217α) [2].Mumitundu ya makoswe a cirrhotic portal hypertension (PHT), INT-747 (30 mg/kg) idayambitsanso njira yolozera ya FXR ndikuchepetsa kuthamanga kwa portal pochepetsa kutsika kwa intrahepatic vascular resistance (IHVR) popanda kuwononga systemic hypotension.Izi zidalumikizidwa ndi kuchuluka kwa eNOS [3].Mu chitsanzo cha Dahl rat cha hypertension ya mchere ndi insulin-resistance (IR), zakudya zamchere (HS) zimachulukitsa kwambiri kuthamanga kwa magazi komanso kutsika kwa minofu ya DDAH.INT-747 idakulitsa chidwi cha insulin ndikuletsa kuchepa kwa mawu a DDAH [4].

Zolozera:
[1].Pellicciari R, Fiorucci S, Camaioni E, et al.6alpha-ethyl-chenodeoxycholic acid (6-ECCDA), FXR agonist yamphamvu komanso yosankha yopatsidwa ntchito ya anticholestatic.J Med Chem, 2002, 45(17): 3569-3572.
[2].Fiorucci S, Clerici C, Antonelli E, et al.Chitetezo cha 6-ethyl chenodeoxycholic acid, farnesoid X receptor ligand, mu estrogen-induced cholestasis.J Pharmacol Exp Ther, 2005, 313(2): 604-612.
[3].Verbeke L, Farre R, Trebicka J, et al.Obeticholic acid, farnesoid X receptor agonist, amathandizira kuthamanga kwa magazi kwa portal ndi njira ziwiri zosiyana za makoswe ozungulira.Hepatology, 2014, 59 (6): 2286-2298.
[4].Ghebremariam YT, Yamada K, Lee JC, et al.FXR agonist INT-747 imayang'anira mawu a DDAH ndikuwonjezera chidwi cha insulin mu makoswe a Dahl omwe amadyetsedwa mchere wambiri.PLoS One, 2013, 8(4): e60653.

Product Citation

• 1. Selina Costa."Kuwonetsa Ligand Novel ya Farnesoid X Receptor pogwiritsa ntchito Transgenic Zebrafish."Yunivesite ya Toronto.Jun-2018.
• 2. Kent, Rebeka."Zotsatira za Fenofibrate pa CYP2D6 ndi Kuwongolera kwa ANG1 ndi RNOSE4 ndi FXR Agonist Obeticholic Acid."indigo.uic.edu.2017.

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