Glycocholic acid is a crystalline bile acid involved in fat emulsification. It is a combination of bile acid and glycine and exists in mammalian bile in the form of sodium salt[1]. Glycocholic acid has anti-tumor activity and can target resistance pumps and non-resistance pump pathways[2]. Glycocholic acid can be used as a phenotypic biomarker for cholangiocarcinoma[3]. Glycocholic acid can treat bile acid amidation defects[4].
In vitro, treatment of Caco-2 cells with Glycocholic acid (10, 100μM) for 48h significantly increased the expression of Hsp90β protein, and exerted a synergistic effect when used in combination with butyrate[5].
In vivo, Glycocholic acid (10μg/mL) was used to treat lipopolysaccharide (LPS)-induced zebrafish inflammation model by microinjection, which significantly reduced the accumulation of macrophages in zebrafish and inhibited the upregulation of interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α), and cc motif chemokine ligand-2 (CCL-2)[6].
References:
[1] Holm R, Müllertz A, Mu H. Bile salts and their importance for drug absorption[J]. International Journal of Pharmaceutics, 2013, 453(1): 44-55.
[2] Lo Y L, Ho C T, Tsai F L. Inhibit multidrug resistance and induce apoptosis by using glycocholic acid and epirubicin[J]. European journal of pharmaceutical sciences, 2008, 35(1-2): 52-67.
[3] Song W S, Park H M, Ha J M, et al. Discovery of glycocholic acid and taurochenodeoxycholic acid as phenotypic biomarkers in cholangiocarcinoma[J]. Scientific Reports, 2018, 8(1): 11088.
[4] Heubi J E, Setchell K D R, Jha P, et al. Treatment of bile acid amidation defects with glycocholic acid[J]. Hepatology, 2015, 61(1): 268-274.
[5] Casselbrant A, Fändriks L, Wallenius V. Glycocholic acid and butyrate synergistically increase vitamin D-induced calcium uptake in Caco-2 intestinal epithelial cell monolayers[J]. Bone reports, 2020, 13: 100294.
[6] Ge X, Huang S, Ren C, et al. Taurocholic acid and glycocholic acid inhibit inflammation and activate farnesoid X receptor expression in LPS-stimulated zebrafish and macrophages[J]. Molecules, 2023, 28(5): 2005.
Glycocholic acid是一种参与脂肪乳化的结晶胆汁酸，是胆酸与甘氨酸的结合物，它以钠盐的形式存在于哺乳动物的胆汁中[1]。Glycocholic acid 具有抗肿瘤活性，可靶向作用于耐药泵和非耐药泵通路[2]。Glycocholic acid能够作为胆管癌的表型生物标志物[3]。Glycocholic acid 能够治疗胆汁酸酰胺化缺陷[4]。
在体外，Glycocholic acid（10, 100μM）处理Caco-2细胞48h，显著增加了Hsp90β蛋白的表达，与丁酸盐联合使用发挥了协同效应[5]。
在体内，Glycocholic acid（10µg/mL）通过显微注射治疗脂多糖（LPS）诱导的斑马鱼炎症模型，显著减少了斑马鱼体内巨噬细胞蓄积，抑制了白细胞介素-6（IL-6）、肿瘤坏死因子-α（TNF-α）和cc基序趋化因子配体-2（CCL-2）的上调[6]。