Elbadawi Mohamed, Ammar Ramy M, Rabini Sabine, Klauck Sabine M, Efferth Thomas
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.
Pharmaceuticals (Basel). 2022 Sep 8;15(9):1121. doi: 10.3390/ph15091121.
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.
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。