• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>RSC Advances >Colon-targeting mutual prodrugs of 5-aminosalicylic acid and butyrate for the treatment of ulcerative colitis
【24h】

Colon-targeting mutual prodrugs of 5-aminosalicylic acid and butyrate for the treatment of ulcerative colitis

机译：结肠靶向5-氨基水杨酸和丁酸盐的相互前水用于治疗溃疡性结肠炎

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

The aim of this study was to design and synthesize four colon-targeting mutual prodrugs of 5-aminosalicylic acid (5-ASA) and butyrate, and evaluate their therapeutic effects on ulcerative colitis. Herein, 5-ASB, 5-ASDB, Ols-DB and Ols-DBP were prepared and characterized, and their lipophilicity, solubility, in vitro and in vivo stability were investigated. Finally, the ameliorative effects of the prodrugs on experimental colitis were evaluated via a series of indicators, including the body weight and survival rates of mice, the colon index and colonic damage score, the disease activity index, the myeloperoxidase activity and levels of superoxide dismutase, malondialdehyde, glutathione and glutathione peroxidase in colonic tissues. As a result, 5-ASB was very stable but Ols-DB showed extreme instability in the environment of the gastrointestinal tract, while 5-ASDB and Ols-DBP showed desirable colon-targeting properties. The four prodrugs all had certain therapeutic effects on the experimental colitis. When orally administered to mice, 5-ASDB and Ols-DBP had significantly greater effects than the mixture of 5-ASA and sodium butyrate. Ols-DB was used as an enema and could be as effective as 5-ASDB and Ols-DBP. In addition, the therapeutic effects of the synthesized prodrugs might be associated with their antioxidative damage ability.
机译：本研究的目的是设计和合成四种靶向5-氨基水杨酸（5-ASA）和丁酸盐的四种靶向相互前药，并评估它们对溃疡性结肠炎的治疗作用。在此制备5-ASB，5-ASDB，OLS-DB和OLS-DBP，并研究了它们的亲脂性，体外，体外稳定性。最后，通过一系列指标评估前药对实验性结肠炎的改进效果，包括小鼠的体重和生存率，结肠指数和结肠伤害评分，疾病活动指数，肌释放酶活性和超氧化物歧化酶的水平结肠组织中丙二醛，谷胱甘肽，谷胱甘肽和谷胱甘肽过氧化物酶。结果，5-ASB非常稳定，但OLS-DB在胃肠道环境中显示出极端的不稳定性，而5- asdb和ols-dbp显示出理想的结肠靶向性质。四个前药都对实验性结肠炎具有一定的治疗效果。当口服给小鼠时，5-ASDB和OLS-DBP的效果明显大于5-ASA和丁酸钠的混合物。 OLS-DB用作灌肠，并且可以与5 - ASDB和OLS-DBP一样有效。此外，合成前药的治疗效果可能与其抗氧化损伤能力有关。

著录项

  • 来源
    《RSC Advances》 |2018年第5期|共14页
  • 作者

    Yan Yan; Sun Jinyao; Xie Xianting; Wang Pengchong; Sun Ying; Dong Yalin; Xing Jianfeng;

  • 作者单位

    Xi An Jiao Tong Univ Sch Pharm 76 Yanta West Rd Xian 710061 Shaanxi Peoples R China;

    Xi An Jiao Tong Univ Affiliated Hosp 1 Dept Pharm Xian Shaanxi Peoples R China;

    Xi An Jiao Tong Univ Affiliated Hosp 1 Dept Pharm Xian Shaanxi Peoples R China;

    Xi An Jiao Tong Univ Sch Pharm 76 Yanta West Rd Xian 710061 Shaanxi Peoples R China;

    Xi An Jiao Tong Univ Sch Pharm 76 Yanta West Rd Xian 710061 Shaanxi Peoples R China;

    Xi An Jiao Tong Univ Affiliated Hosp 1 Dept Pharm Xian Shaanxi Peoples R China;

    Xi An Jiao Tong Univ Sch Pharm 76 Yanta West Rd Xian 710061 Shaanxi Peoples R China;

  • 收录信息
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 化学;
  • 关键词

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号