Jiang Luxia, Ma Xueni, Yan Qi, Pu Dan, Fu Xu, Zhang Dekui
Department of Cardiac Surgery ICU, Second Hospital & Clinical Medical School, Lanzhou University, Lanzhou, China; Key Laboratory of Digestive Diseases, Second Hospital & Clinical Medical School, Lanzhou University, Lanzhou, China; Cuiying Biomedical Research Center, Second Hospital & Clinical Medical School, Lanzhou University, Lanzhou, China.
Department of Gastroenterology, Second Hospital & Clinical Medical School, Lanzhou University, Lanzhou, China; Key Laboratory of Digestive Diseases, Second Hospital & Clinical Medical School, Lanzhou University, Lanzhou, China.
Int J Pharm. 2025 Feb 10;670:125155. doi: 10.1016/j.ijpharm.2024.125155. Epub 2024 Dec 31.
Dihydromyricetin (DHM), the primary active compound in vine tea possesses various pharmacological effects such as anti-inflammatory and antioxidant properties, along with high biosafety. However, its oral delivery remains a significant challenge. Montmorillonite (MMT), the primary component of bentonite, is a commonly used drug in the clinical treatment of gastrointestinal diseases and serves as an excellent drug carrier due to its intercalation capability. In this study, we intercalated DHM into the interlayer spaces of MMT via solution intercalation method combined with rotary evaporation and used it to treat ulcerative colitis in mice. SEM, XRD, and FTIR analyses confirmed the successful synthesis of the DHM/MMT intercalation compound. In vitro studies shown that DHM/MMT eliminated intracellular ROS and suppressed inflammatory genes IL-1β, IL-6, and TNF-α. Moreover, DHM/MMT demonstrated notable therapeutic effects in ulcerative colitis (UC) mice, significantly restoring the intestinal mucosa. Importantly, the therapeutic mechanism of DHM/MMT is closely linked to the inhibition of the NLRP3 signaling pathway. Additionally, this strategy modulated gut microbiota by increasing probiotics and suppressing harmful bacteria, thereby maintaining intestinal homeostasis. In conclusion, DHM/MMT presents a promising strategy for UC treatment.
二氢杨梅素(DHM)是藤茶中的主要活性成分,具有抗炎、抗氧化等多种药理作用,且生物安全性高。然而,其口服给药仍然是一个重大挑战。蒙脱石(MMT)是膨润土的主要成分,是临床治疗胃肠道疾病常用的药物,因其具有插层能力,可作为优良的药物载体。在本研究中,我们通过溶液插层法结合旋转蒸发将DHM插层到MMT的层间,并用于治疗小鼠溃疡性结肠炎。扫描电子显微镜(SEM)、X射线衍射(XRD)和傅里叶变换红外光谱(FTIR)分析证实了DHM/MMT插层化合物的成功合成。体外研究表明,DHM/MMT可消除细胞内活性氧(ROS),并抑制炎症基因白细胞介素-1β(IL-1β)、白细胞介素-6(IL-6)和肿瘤坏死因子-α(TNF-α)。此外,DHM/MMT在溃疡性结肠炎(UC)小鼠中显示出显著的治疗效果,可显著修复肠黏膜。重要的是,DHM/MMT的治疗机制与抑制NLRP3信号通路密切相关。此外,该策略通过增加益生菌和抑制有害细菌来调节肠道微生物群,从而维持肠道稳态。总之,DHM/MMT为UC治疗提供了一种有前景的策略。