Jhundoo Henusha D, Siefen Tobias, Liang Alfred, Schmidt Christoph, Lokhnauth John, Moulari Brice, Béduneau Arnaud, Pellequer Yann, Larsen Crilles Casper, Lamprecht Alf
Department of Pharmaceutics, Institute of Pharmacy, University of Bonn, Bonn 53121, Germany.
Tris Pharma, Monmouth Junction, NJ 08852, USA.
Biomol Ther (Seoul). 2021 Sep 1;29(5):536-544. doi: 10.4062/biomolther.2020.227.
5-amino salicylic acid (5-ASA) is a standard therapy for the treatment of mild to moderate forms of inflammatory bowel diseases (IBD) whereas more severe forms involve the use of steroids and immunosuppressive drugs. Hyaluronic acid (HA) is a naturally occurring non-sulfated glycosaminoglycan that has shown epithelium protective effects in experimental colitis recently. In this study, both 5-ASA (30 mg/kg) and HA (15 mg/kg or 30 mg/kg) were administered rectally and investigated for their potential complementary therapeutic effects in moderate or severe murine colitis models. Intrarectal treatment of moderate and severe colitis with 5-ASA alone or HA alone at a dose of 30 mg/kg led to a significant decrease in clinical activity and histology scores, myeloperoxidase activity (MPO), TNF-α, IL-6 and IL-1β in colitis mice compared to untreated animals. The combination of HA (30 mg/kg) and 5-ASA in severe colitis led to a significant improvement of colitis compared to 5-ASA alone. Combined rectal therapy with HA and 5-ASA could be a treatment alternative for severe cases of IBD as it was the only treatment tested that was not significantly different from the healthy control group. This study further underlines the benefit of searching for yet unexplored drug combinations that show therapeutic potential in IBD without the need of designing completely new drug entities.
5-氨基水杨酸(5-ASA)是治疗轻至中度炎症性肠病(IBD)的标准疗法,而更严重的形式则需要使用类固醇和免疫抑制药物。透明质酸(HA)是一种天然存在的非硫酸化糖胺聚糖,最近在实验性结肠炎中显示出上皮保护作用。在本研究中,5-ASA(30mg/kg)和HA(15mg/kg或30mg/kg)均经直肠给药,并在中度或重度小鼠结肠炎模型中研究它们潜在的互补治疗效果。与未治疗的动物相比,在中度和重度结肠炎小鼠中单独用30mg/kg剂量的5-ASA或HA进行直肠内治疗可导致临床活动度和组织学评分、髓过氧化物酶活性(MPO)、TNF-α、IL-6和IL-1β显著降低。在重度结肠炎中,HA(30mg/kg)和5-ASA联合使用与单独使用5-ASA相比,可显著改善结肠炎。HA和5-ASA联合直肠治疗可能是重度IBD病例的一种治疗选择,因为它是唯一一种与健康对照组无显著差异的测试治疗方法。这项研究进一步强调了寻找尚未探索的药物组合的益处,这些组合在IBD中显示出治疗潜力,而无需设计全新的药物实体。