School of Pharmaceutical Sciences, Jilin University, Changchun 130021, China.
Department of Chinese Medicine, Changchun University of Chinese Medicine, Changchun 130021, China.
Biomed Pharmacother. 2024 Nov;180:117534. doi: 10.1016/j.biopha.2024.117534. Epub 2024 Oct 13.
Ulcerative colitis (UC), an incurable and recurrent inflammatory bowel disease, presents a significant threat to health and highlights the need for novel therapeutic strategies. Oleanolic acid 28-O-β-D-glucopyranoside (OAG) is a naturally occurring pentacyclic triterpenoid found in ginseng. In this study, we demonstrated that OAG exhibited remarkable anti-UC activity in LPS-induced Caco-2 cells and DSS-induced model mice. First, OAG alleviated the symptoms of UC by mitigating weight loss, reducing the DAI score, and increasing colon length. Second, the inflammatory response was inhibited after OAG intervention, evidenced decreases in the spleen coefficient, cytokine levels, and inflammatory cell infiltration in colon tissue. Thirdly, OAG also enhanced intestinal epithelial barrier function, as evidenced by elevated TEER values, increased expression of tight junction proteins, diminished bacterial translocation, and maintained intact ultrastructure of colonic mucosal cells. Notably, compared with 5-aminosalicylic acid, OAG demonstrated superior efficacy in enhancing mucosal barrier function. Fourth, OAG increased microbial diversity, promoted the abundance of beneficial bacteria, reduced the abundance of harmful bacteria, and rebalanced the gut microbiome. Finally, the PI3K-AKT and MAPK signaling pathways were identified as crucial mechanisms underlying the therapeutic effects of OAG against UC through multi-omics. In summary, we identified OAG as a novel therapeutic agent against UC, demonstrating anti-inflammatory, barrier-preserving, and gut microbiota-modulating effects, highlighting its promising potential as a candidate UC drug.
溃疡性结肠炎(UC)是一种不可治愈且反复发作的炎症性肠病,对健康构成重大威胁,突显了新型治疗策略的必要性。齐墩果酸 28-O-β-D-吡喃葡萄糖苷(OAG)是一种天然存在的五环三萜,存在于人参中。在这项研究中,我们证明了 OAG 在 LPS 诱导的 Caco-2 细胞和 DSS 诱导的模型小鼠中表现出显著的抗 UC 活性。首先,OAG 通过减轻体重减轻、降低 DAI 评分和增加结肠长度来缓解 UC 症状。其次,OAG 干预后抑制了炎症反应,脾系数、细胞因子水平和结肠组织中炎症细胞浸润减少。第三,OAG 还增强了肠道上皮屏障功能,表现为 TEER 值升高、紧密连接蛋白表达增加、细菌易位减少以及结肠黏膜细胞超微结构完整。值得注意的是,与 5-氨基水杨酸相比,OAG 在增强黏膜屏障功能方面表现出更好的疗效。第四,OAG 增加了微生物多样性,促进了有益细菌的丰度,减少了有害细菌的丰度,并使肠道微生物组重新平衡。最后,通过多组学研究确定了 OAG 治疗 UC 的关键机制是 PI3K-AKT 和 MAPK 信号通路。总之,我们确定 OAG 是一种治疗 UC 的新型治疗剂,具有抗炎、保护屏障和调节肠道微生物群的作用,突显了其作为候选 UC 药物的潜在应用价值。