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草药制剂STW 5-II对肠道促肾上腺皮质激素释放激素信号的调节:肠易激综合征管理的可能机制

Modulation of Intestinal Corticotropin-Releasing Hormone Signaling by the Herbal Preparation STW 5-II: Possible Mechanisms for Irritable Bowel Syndrome Management.

作者信息

Elbadawi Mohamed, Ammar Ramy M, Rabini Sabine, Klauck Sabine M, Efferth Thomas

机构信息

Department of Pharmaceutical Biology, Institute of Pharmaceutical and Biomedical Sciences, Johannes Gutenberg University-Mainz, 55128 Mainz, Germany.

Medical Affairs, Bayer Consumer Health, 64295 Darmstadt, Germany.

出版信息

Pharmaceuticals (Basel). 2022 Sep 8;15(9):1121. doi: 10.3390/ph15091121.

Abstract

Corticotropin-releasing factor (CRF) mediates stress responses and alters the gut-brain axis, contributing to the pathogenesis of irritable bowel syndrome (IBS), which is recognized by abdominal pain accompanied by bowel habit disturbance. STW 5-II, a mixture of six herbal extracts, is clinically effective in functional dyspepsia and IBS. Here we aimed to establish an organoid-based stress-induced IBS-like model to investigate the mechanisms of action of STW 5-II. STW 5-II (10, 20, and 30 g/mL) was applied to intestinal organoids for 24 h before being treated with CRF (100 nM) for 48 h. The effects of STW 5-II on CRF signaling were investigated using several in vitro and in silico approaches. STW 5-II activities were further explored by in silico PyRx screening followed by molecular docking of the main 52 identified compounds in STW 5-II with both CRF receptors CRFR1 and CRFR2. CRF exposure stimulated inflammation and increased proinflammatory mediators, while STW 5-II dose-dependently counteracted these effects. STW 5-II inhibited CRF-induced claudin-2 overexpression and serotonin release. Docking of the STW 5-II constituents oleanolic acid and licorice saponin G2 to CRFR1 and CRFR2, respectively, showed a good affinity. These multi-target activities support and elucidate the clinically proven efficacy of STW 5-II in disorders of gut-brain interaction.

摘要

促肾上腺皮质激素释放因子(CRF)介导应激反应并改变肠-脑轴,促成肠易激综合征(IBS)的发病机制,IBS的特征为腹痛伴排便习惯紊乱。STW 5-II是六种草药提取物的混合物,在功能性消化不良和IBS的治疗中具有临床疗效。在此,我们旨在建立一种基于类器官的应激诱导IBS样模型,以研究STW 5-II的作用机制。在使用CRF(100 nM)处理48小时之前,将STW 5-II(10、20和30 g/mL)应用于肠道类器官24小时。使用多种体外和计算机模拟方法研究STW 5-II对CRF信号传导的影响。通过计算机模拟PyRx筛选,随后将STW 5-II中鉴定出的52种主要化合物与CRF受体CRFR1和CRFR2进行分子对接,进一步探索STW 5-II的活性。CRF暴露会刺激炎症并增加促炎介质,而STW 5-II则呈剂量依赖性地抵消这些影响。STW 5-II抑制CRF诱导的claudin-2过表达和5-羟色胺释放。STW 5-II成分齐墩果酸和甘草皂苷G2分别与CRFR1和CRFR2对接,显示出良好的亲和力。这些多靶点活性支持并阐明了STW 5-II在肠-脑相互作用障碍中的临床验证疗效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b4eb/9504045/0c1bc1189df2/pharmaceuticals-15-01121-g001.jpg

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