石胆酸是一种有毒的次级胆汁酸，引起肝内胆汁淤积，具有促肿瘤活性 | MedChemExpress (MCE)

Lithocholic acid

中文名：石胆酸

CAS：434-13-9

品牌：MedChemExpress (MCE)

存储条件：Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.

生物活性：石胆酸是一种有毒的次级胆汁酸，引起肝内胆汁淤积，具有促肿瘤活性。目标：其他 石胆酸已用于一项研究，以评估胆汁淤积及其对大鼠多种器官和组织的作用。它也被用于一项研究，以研究通过 TGFβ 激活 SMAD3 来调节肝磷脂和胆汁酸稳态。它与人类和实验动物的致癌作用有关。初步体外研究表明，LCA 选择性地杀死神经母细胞瘤细胞，同时保留正常神经元细胞，并且在生理学相关浓度下对许多其他恶性细胞类型具有细胞毒性。

体外：Lithocholic Acid 可抑制 CDCA 和 GW4064 诱导的 FXR 激活，IC50分别为 0.7 和 1.4 μM[5]。Lithocholic Acid (10-30 μM，24 小时) 抑制 HepG2 细胞中 100 nM GW4064 诱导的 BSEP 表达[5]。Lithocholic Acid (0-500 μM) 剂量依赖性地抑制神经母细胞瘤细胞 (BE(2)-m17、SK-n-SH、SK-n-MCIXC 和 Lan-1) 的增殖[3] . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内：Lithocholic acid (补充在饮食中 0.6%，7 天) 会增加雄性小鼠 (C57BL/6) 肝脏中 TGFB1、TGFBR1 和 TGFBR2 mRNA 水平，并激活 SMAD3，并诱导胆道损伤[4].Lithocholic acid (125 mg/kg，腹膜内注射，每天两次，持续四天) 会引起雄性 C57BL/6 小鼠的肝损伤，并增加 AST、ALT 和 ALP 水平[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male mice (C57BL/6)[4]. Dosage: 0.6% LCA-supplement diet, with the AIN93G diet as a control Administration: in diet, for 6 days Result: Induced liver injury. Activated TGFβ-SMAD3 signaling. Increased serum ALP activities. Animal Model: Male mice (C57BL/6)[2]. Dosage: 125 mg/kg, dissolved in corn oil Administration: i.p., twice a day for four days Result: Induced liver injury, generated necrosis and neutrophilic-granulocytic infiltrate (H&E staining). Increased AST, ALT and ALP level.

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参考文献：

[1]. Jenkins, D.J., et al., Effect on blood lipids of very high intakes of fiber in diets low in saturated fat and cholesterol. N Engl J Med, 1993. 329(1): p. 21-6.
[2]. Goldberg, A.A., et al., Lithocholic bile acid selectively kills neuroblastoma cells, while sparing normal neuronal cells. Oncotarget, 2011. 2(10): p. 761-82.
[3]. Matsubara, T., et al., TGF-beta-SMAD3 signaling mediates hepatic bile acid and phospholipid metabolism following lithocholic acid-induced liver injury. J Lipid Res, 2012. 53(12): p. 2698-707.
[4]. Yang R, et al. Metabolomic analysis of cholestatic liver damage in mice. Food Chem Toxicol. 2018 Jul 14;120:253-260.
[5]. Yu J, et al. Lithocholic acid decreases expression of bile salt export pump through farnesoid X receptor antagonist activity. J Biol Chem. 2002 Aug 30;277(35):31441-7.