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Ulcerative colitis is a chronic inflammatory condition primarily affecting the colon and rectum. The primary drugs used in the treatment of ulcerative colitis are aminosalicylates. They exhibit anti-inflammatory and immunosuppressive properties. They modulate inflammatory mediators and inhibit the activity of nuclear factor κB (NF-κB). Aminosalicylates also reduce inflammation by inhibiting prostaglandin and leukotriene production and decreasing neutrophil chemotaxis and superoxide generation. 

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含有抗炎药物的纳米囊的合成和表征:

Altevir Rossato Viana1, Luiza Madalozzo Diniz2, Vitoria Hagemann Cauduro1

  • 1Programa de Pós-graduação em Química, Universidade Federal de Santa Maria, Santa Maria, Brazil.

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此摘要是机器生成的。

这项研究探讨了纳米封装的抗炎药物,甲酸 (DA) 和尼米苏利德 (NIME),在维持癌细胞活性的同时,对健康细胞的毒性降低. 这些发现表明针对癌症的治疗方法很有前途.

关键词:
癌症德克萨米松纳米技术尼米苏利德

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科学领域:

  • 纳米技术
  • 药理学
  • 计算化学

背景情况:

  • 癌症是全球主要的死亡原因, 目前的治疗方法往往缺乏选择性,
  • 炎症与瘤进展有关,但抗炎药物很少以向的方式用于癌症治疗.
  • 德克萨米他 (DA) 和尼米苏利德 (NIME) 是常见的抗炎药物,由于副作用,它们的治疗用途可能是有限的.

研究的目的:

  • 研究纳米封装甲酸盐 (DA) 和尼米苏利德 (NIME) 的协同作用,以提高抗癌效果和降低毒性.
  • 描述开发的纳米囊的稳定性和药物释放性.
  • 以计算方式评估DA和NIME与其治疗作用相关的结合亲和性和分子性质.

主要方法:

  • 使用光散射,泽塔电位和电子显微镜进行纳米粒子表征.
  • 使用二极管阵列检测 (HPLC-DAD) 的高性能液体染色学进行稳定性评估.
  • 在健康细胞系 (HaCaT,L929) 和癌细胞系 (HeLa,A375) 上进行了体外细胞毒性测定.
  • 分子对接模拟以预测药物向相互作用 (MMP-13/TIMP-2复合物).
  • 密度功能理论 (DFT) 分析以评估分子反应性和稳定性 (HOMO-LUMO差距).

主要成果:

  • 纳米囊表现出良好的稳定性,多孔性和规律形状,适合持续释放药物.
  • 封装的DA和NIME对健康细胞的毒性降低,同时对癌细胞保持显著的活性.
  • 分子对接显示DA与MMP-13/TIMP-2复合物 (-8.7 kcal/mol) 的结合亲和力比NIME (-6.8 kcal/mol) 的结合亲和力更强.
  • DFT分析表明,NIME具有更高的反应性 (较小的HOMO-LUMO间隙:0.132 eV),DA表现出更大的分子稳定性 (较大的间隙:2.806 eV).

结论:

  • 德克萨米他和尼梅苏利德的纳米封装提供了一种潜在的降低药物毒性的策略,同时保持抗癌效益.
  • 纳米囊的协同作用和有利的物理化学特性需要进一步研究以针对癌症治疗.
  • 计算分析为DA和NIME的不同分子行为提供了洞察力,指导了未来的药物开发工作.