Glycodeoxycholic Acid is a glycine-conjugated form of the secondary bile acid deoxycholic acid[1]. Glycodeoxycholic Acid participates in bile formation and fat digestion and absorption, and also plays an important role in regulating cholesterol metabolism and maintaining gut microbiota balance[2]. Glycodeoxycholic Acid is mainly used in the research of bile acid metabolism and related diseases[3].
In vitro, treatment of primary hepatocytes isolated from rats with Glycodeoxycholic Acid (250μM; 4h) significantly increased hepatocyte MDA levels, decreased membrane fluidity, elevated ALT levels, and induced hepatocyte injury[4]. Glycodeoxycholic Acid (0.5mM; 24h) significantly inhibited the proliferation and migration, and increased cells apoptosis in human hepatocellular carcinoma (HCC) SUN-449 and HepG2 cells[5].
In vivo, Glycodeoxycholic Acid (100mg/kg/day; oral gavage from postnatal day 11 to 34) delayed the onset of puberty, increased hypothalamic Sirt1 expression, and decreased serum LH levels, Kiss1 and GnRH expression in high-fat diet-induced central precocious puberty (CPP) female rats[6]. Intraduodenal infusion of Glycodeoxycholic Acid at a rate equivalent to the hepatic bile acid flux (32.90±9.04mg/h) for 24 hours reduced cholesterol 7α-hydroxylase activity and inhibited endogenous bile acid synthesis in the rabbit model with bile fistula[7].
References:
[1] Lefebvre P, Cariou B, Lien F, Kuipers F, Staels B. Role of bile acids and bile acid receptors in metabolic regulation. Physiol Rev. 2009;89(1):147-191.
[2] Jia Y, Yang X, Wilson LM, et al. Diet-Related and Gut-Derived Metabolites and Health Outcomes: A Scoping Review. Metabolites. 2022;12(12):1261.
[3] Farooqui N, Elhence A, Shalimar. A Current Understanding of Bile Acids in Chronic Liver Disease. J Clin Exp Hepatol. 2022;12(1):155-173.
[4] Huang W, Kang G, Tu Z. Zhonghua Gan Zang Bing Za Zhi. 1999;7(1):46-47.
[5] Shen R, Ke L, Li Q, et al. Abnormal bile acid-microbiota crosstalk promotes the development of hepatocellular carcinoma. Hepatol Int. 2022;16(2):396-411.
[6] Wu N, Jiang X, Liu Y, et al. Glycodeoxycholic acid alleviates central precocious puberty by modulating gut microbiota and metabolites in high-fat diet-fed female rats. Cell Mol Life Sci. 2025;82(1):163.
[7] Xu G, Salen G, Batta AK, et al. Glycocholic acid and glycodeoxycholic acid but not glycoursocholic acid inhibit bile acid synthesis in the rabbit. Gastroenterology. 1992;102(5):1717-1723.
Glycodeoxycholic Acid是脱氧胆酸的甘氨酸结合形式[1]。Glycodeoxycholic Acid参与胆汁的形成以及脂肪的消化吸收，并在调节胆固醇代谢和维持肠道微生物群平衡方面发挥重要作用[2]。Glycodeoxycholic Acid主要用于胆汁酸代谢及相关疾病的研究[3]。
在体外，用Glycodeoxycholic Acid（250μM；4小时）处理从大鼠分离的原代肝细胞，显著增加了肝细胞丙二醛（MDA）水平，降低了细胞膜流动性，提高了丙氨酸转氨酶（ALT）水平，并诱导肝细胞损伤[4]。Glycodeoxycholic Acid（0.5mM；24小时）显著抑制了人肝细胞癌（HCC）SUN-449和HepG2细胞的增殖和迁移，并增加了细胞凋亡[5]。
在体内，Glycodeoxycholic Acid（100mg/kg/天；从出生后第11天至第34天口服灌胃）延迟了高脂饮食诱导的中枢性性早熟（CPP）雌性大鼠的青春期发育，增加了下丘脑Sirt1表达，并降低了血清黄体生成素（LH）水平、Kiss1和GnRH表达[6]。在带有胆汁瘘的兔子模型中，以相当于肝脏胆汁酸通量（32.90±9.04mg/h）的速率进行24小时的Glycodeoxycholic Acid十二指肠内灌注降低了胆固醇7α-羟化酶活性，抑制了内源性胆汁酸合成[7]。