在蛋白酶可降解的纳米纤维中封装黄金基抗癌剂提高了它们的效力
Yaron Marciano1,2, Virginia Del Solar2, Nazia Nayeem2
1Nanoscience Initiative, Advanced Science Research Center at The Graduate Center of the City University of New York (CUNY), 85 Saint Nicholas Terrace, New York, New York10031, United States.
Journal of the American Chemical Society
|December 21, 2022
概括
两性封装了疏水性黄金抗癌药物,增强了它们的输送和有效性. 这种新的方法通过蛋白酶可切割的结构改善了药物的生物可用性和癌细胞向性.
科学领域:
- 医学化学
- 纳米技术
- 生物结合
背景情况:
- 疏水性金属药物通常具有较低的生物可用性和有限的治疗效果.
- 两性为药物封装和向输送提供了潜在的解决方案.
研究的目的:
- 作为防水金属药物的封装部分,研究两性,蛋白酶可裂的.
- 增强含金剂的生物可用性和抗癌活性.
主要方法:
- 将两种疏水性黄金 ((I) -N-异环碳酸化合物 (1和2) 封装成两性.
- 对序列对超分子包装,药物负载和丝表面负载的影响的研究.
- 对基纳米纤维和含药纳米纤维对癌症和非癌症细胞系的细胞毒性评估.
主要成果:
- 序列决定了超分子包装和药物加载效率,而离子纤维显示了化合物1的有效加载.
- 药物加载效率受到药物和之间的芳香和静电匹配的影响.
- 与免费药物相比,含药纳米纤维对Caki-1和MDA-MB-231癌细胞具有增强的细胞毒性,对非癌细胞没有毒性.
结论:
- 两性,蛋白酶可分离的可以有效地封装疏水性金属药物,改善其抗癌活性.
- 这种增强的"体外活性"归因于在癌细胞附近蛋白酶介导的药物结合片段的释放,从而促进吸收和细胞毒性.
- 这一战略为开发更有效的基于金属药物的癌症疗法提供了有希望的方法.
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