Division of Diabetes and Nutrition, RARiS, Tohoku University, 6-6-11 Aramakiaza-Aoba, Aoba-ku, Sendai 980-8579, Miyagi, Japan.
Int J Mol Sci. 2024 Jul 16;25(14):7784. doi: 10.3390/ijms25147784.
Liraglutide, a glucagon-like peptide 1 analog used to treat type 2 diabetes and obesity, is a potential new treatment modality for bile acid (BA) diarrhea. Here, we show that administration of liraglutide significantly decreased total BAs, especially the primary BAs, including cholic acid, chenodeoxycholic acid, taurocholic acid, taurochenodeoxycholic acid, glycocholic acid, and β-muricholic acid, in the liver and feces. In addition, liraglutide significantly decreased tryptophan metabolites, including L-tryptophan, serotonin, 5-hydroxy indole-3-acetic acid, L-kynurenine, and xanthurenic acid, in the colon, whereas it significantly increased indole-3-propionic acid. Moreover, the administration of liraglutide remarkably decreased the expression of apical sodium-dependent bile acid transporter, which mediates BA uptake across the apical brush border member in the ileum, ileal BA binding protein, and fibroblast growth factor 15 in association with decreased expression of the BA-activated nuclear receptor farnesoid X receptor and the heteromeric organic solute transporter Ostα/β, which induces BA excretion, in the ileum. Liraglutide acutely decreased body weight and blood glucose levels in association with decreases in plasma insulin and serotonin levels in food-deprived mice. These findings suggest the potential of liraglutide as a novel inhibitor of primary BAs and serotonin in the colon.
利拉鲁肽是一种胰高血糖素样肽 1 类似物,用于治疗 2 型糖尿病和肥胖症,它是一种治疗胆酸(BA)腹泻的潜在新方法。在这里,我们表明,利拉鲁肽的给药显著降低了总 BAs,特别是初级 BAs,包括胆酸、鹅脱氧胆酸、牛磺胆酸、牛磺鹅脱氧胆酸、甘氨胆酸和β-鼠胆酸,在肝脏和粪便中。此外,利拉鲁肽显著降低了色氨酸代谢物,包括 L-色氨酸、血清素、5-羟色胺-3-乙酸、L-犬尿氨酸和黄尿酸,在结肠中,而它显著增加了吲哚-3-丙酸。此外,利拉鲁肽的给药显著降低了顶端钠依赖性胆酸转运体的表达,该转运体介导 BA 在回肠中的顶端刷状边界成员中的摄取,回肠 BA 结合蛋白和成纤维细胞生长因子 15,同时降低了 BA 激活核受体法尼醇 X 受体和异质有机溶质转运蛋白 Ostα/β的表达,从而诱导 BA 排泄,在回肠中。利拉鲁肽在禁食小鼠中急性降低体重和血糖水平,同时降低血浆胰岛素和血清素水平。这些发现表明利拉鲁肽作为结肠中初级 BAs 和血清素的新型抑制剂的潜力。