Glycine-β-muricholic Acid is an effective, stable, and arginine-selective oral bioactive FXR inhibitor. It is the glycine-bound form of the murine primary bile acid β-muricholic acid. FXR is an important sensor and regulator of bile acid, lipid, and glucose metabolism [1]. Glycine-β-muricholic Acid can be used in studies of metabolic disorders [2].
In vivo, Glycine-β-muricholic Acid (10 and 50mg/kg; 5 weeks; oral) significantly reduced the absolute fat mass and fat-to-weight ratio of obese and insulin-resistant mice induced by HFD, as well as insulin resistance and hepatic steatosis, with a significant decrease in liver lipid droplets [1]. Glycine-β-muricholic Acid (10mg/kg/day; 23d once every 2 days; Gavage) treatment significantly reduced the protective effect of Lactobacillus reuteri on alcohol-induced lipid accumulation in the liver of mice. Lactobacillus reuteri and its metabolites may regulate liver inflammation through the FXR signaling regulatory axis [3].
References:
[1] Jiang, C., Xie, C., Lv, Y., et al. Intestine-selective farnesoid X receptor inhibition improves obesity-related metabolic dysfunction. Nat. Commun. 6, 10166 (2015).
[2] Hasan M N, Wang H, Luo W, et al. Gly-β-MCA is a potent anti-cholestasis agent against “human-like” hydrophobic bile acid-induced biliary injury in mice[J]. Journal of Lipid Research, 2024, 65(10).
[3] Cheng Y, Xiang X, Liu C, et al. Transcriptomic analysis reveals Lactobacillus reuteri alleviating alcohol-induced liver injury in mice by enhancing the farnesoid X receptor signaling pathway[J]. Journal of agricultural and food chemistry, 2022, 70(39): 12550-12564.
Glycine-β-muricholic Acid是一种有效的、稳定的、对精氨酸有选择性的口服生物活性FXR抑制剂，是鼠特异性初级胆汁酸β-鼠胆酸的甘氨酸结合形式。FXR是胆汁酸、脂质和葡萄糖代谢的重要传感器和调节因子 [1]。Glycine-β-muricholic Acid可用于代谢障碍的研究 [2]。
在体内，Glycine-β-muricholic Acid（10和50mg/kg; 5 weeks; oral）显著降低了HFD诱导的肥胖和胰岛素抵抗小鼠的绝对脂肪质量和脂肪/瘦体重比，以及胰岛素抵抗和肝脂肪变性，肝脏脂滴显著减少 [1]。Glycine-β-muricholic Acid（10mg/kg/day; 23d once every 2 days; gavage）显著降低了Lactobacillus reuteri对酒精诱导的小鼠肝脏脂质蓄积的保护作用，Lactobacillus reuteri及其代谢产物可能通过FXR信号调节轴调节肝脏炎症 [3]。