GLOCK Health, Science and Research GmbH, Deutsch-Wagram, Austria.
Maimonides Biomedical Research Institute of Córdoba, Reina Sofía University Hospital, Department of Cell Biology, Physiology and Immunology, University of Córdoba, Córdoba, Spain.
Inflamm Bowel Dis. 2017 Dec 19;24(1):54-66. doi: 10.1093/ibd/izx042.
Clinoptilolite is an aluminium silicate of natural origin; the microporous structure and the net negative charge of its crystal lattice allows for adsorption of ions, toxins, inflammatory mediators, and some microorganisms. We generated 2 preparations of purified clinoptilolite, which differed by about 10-fold in particle size, ie, a standard powder (GHC1) and a microparticulate fraction (GHC2) with a size of 3.6 µm and 0.39 µm (d50) respectively. These were examined for their ability to accelerate the recovery of mice from DSS (dextran sulphate sodium)-induced intestinal inflammation.
Efficacy of clinoptilolite preparations was investigated by administering DSS-treated mice twice daily with 30 mg GHC2 or GHC1 for 5 consecutive days, followed by 5 days of recovery without DSS. To explore the safety of the microparticulate preparation (GHC2), mice were subjected to 4 cycles of DSS-exposure. We specifically verified that clinoptilolite microparticles were not systemically bioavailable by examining the gut tissue and the liver for the accumulation of microparticles by transmission electron microscopy.
Treatment of mice with GHC2 was superior to GHC1 and as effective as the reference compound 5-aminosalicylic acid in ameliorating the damage induced by the exposure to DSS. In addition, no clinoptilolite particle was observed in the intestinal epithelial layer, gut-associated lymph follicles, or in the liver.
Our observations confirm that a microparticulate preparation of clinoptilolite is safe and effective in a murine model of inflammatory bowel disease and supports the hypothesis that the adsorptive capacity of clinoptilolite is of potential therapeutic relevance.
沸石是一种天然来源的硅铝酸盐,其微孔结构和晶格的净负电荷使其能够吸附离子、毒素、炎症介质和一些微生物。我们生成了 2 种不同粒径的纯化沸石制剂,即标准粉末(GHC1)和粒径分别为 3.6 µm 和 0.39 µm(d50)的微颗粒级分(GHC2),相差约 10 倍。我们研究了它们加速小鼠从 DSS(葡聚糖硫酸钠)诱导的肠道炎症中恢复的能力。
通过每天两次给 DSS 处理的小鼠施用 30 mg GHC2 或 GHC1,连续 5 天,然后在没有 DSS 的情况下恢复 5 天,来研究沸石制剂的疗效。为了探索微颗粒制剂(GHC2)的安全性,将小鼠暴露于 4 个周期的 DSS 中。我们通过透射电子显微镜检查肠道组织和肝脏中微颗粒的积累,专门验证了沸石微颗粒不会在体内被系统吸收。
与 GHC1 相比,GHC2 治疗小鼠可改善 DSS 暴露引起的损伤,效果优于参考化合物 5-氨基水杨酸。此外,在肠上皮层、肠道相关淋巴滤泡或肝脏中均未观察到沸石颗粒。
我们的观察结果证实,在炎性肠病的小鼠模型中,微颗粒级分的沸石是安全有效的,并且支持沸石的吸附能力具有潜在治疗相关性的假说。