依美格列明可预防肠易激综合征大鼠模型的内脏超敏反应和结肠通透性增加。
Imeglimin prevents visceral hypersensitivity and colonic hyperpermeability in irritable bowel syndrome rat model.
作者信息
Nozu Tsukasa, Miyagishi Saori, Ishioh Masatomo, Takakusaki Kaoru, Okumura Toshikatsu
机构信息
Department of Regional Medicine and Education, Asahikawa Medical University, 2-1-1-1 Midorigaoka-Higashi, Asahikawa, Hokkaido, 078-8510, Japan; Center for Medical Education, Asahikawa Medical University, 2-1-1-1 Midorigaoka-Higashi, Asahikawa, Hokkaido, 078-8510, Japan; Department of General Medicine, Asahikawa Medical University, 2-1-1-1 Midorigaoka-Higashi, Asahikawa, Hokkaido, 078-8510, Japan.
Division of Gastroenterology and Hematology/Oncology, Department of Medicine, Asahikawa Medical University, 2-1-1-1 Midorigaoka-Higashi, Asahikawa, Hokkaido, 078-8510, Japan.
出版信息
J Pharmacol Sci. 2023 Sep;153(1):26-30. doi: 10.1016/j.jphs.2023.07.002. Epub 2023 Jul 7.
Visceral hypersensitivity and leaky gut, which are mediated via corticotropin-releasing factor (CRF) and Toll-like receptor 4 are key pathophysiology of irritable bowel syndrome (IBS). Metformin was reported to improve these gastrointestinal (GI) changes. In this study, we attempted to determine the effects of imeglimin, which was synthesized from metformin on GI function in IBS rat models. Imeglimin blocked lipopolysaccharide- or CRF-induced visceral hypersensitivity and colonic hyperpermeability. These effects were prevented by compound C or naloxone. These results suggest that imeglimin may be effective for the treatment of IBS by improved visceral sensation and colonic barrier via AMPK and opioid receptor.
通过促肾上腺皮质激素释放因子（CRF）和Toll样受体4介导的内脏高敏感性和肠屏障功能障碍是肠易激综合征（IBS）的关键病理生理学特征。据报道，二甲双胍可改善这些胃肠道变化。在本研究中，我们试图确定由二甲双胍合成的依美格列明对IBS大鼠模型胃肠道功能的影响。依美格列明可阻断脂多糖或CRF诱导的内脏高敏感性和结肠通透性增加。这些作用可被化合物C或纳洛酮阻断。这些结果表明，依美格列明可能通过激活AMPK和作用于阿片受体改善内脏感觉和结肠屏障功能，从而有效治疗IBS。
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