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增强蒂莫金/硫丁乙-β-环德 (SBE-β-CD) 纳入复合物的抗白血病潜力

Eltayeb E M Eid¹, Salah Abdalrazak Alshehade², Amer A Almaiman³

¹Department of Pharmaceutical Chemistry and Pharmacognosy, Unaizah College of Pharmacy, Qassim University, Unaizah 51911, Saudi Arabia.

|July 29, 2023

概括

提摩 (TQ) 复合与硫乙-β-环极 (SBE-β-CD) 显示为白血病治疗的前景. 这种新的配方增强了TQ.

科学领域:

药理学和毒理学药理学和毒理学
生物化学生物化学
癌症研究癌症研究

背景情况:

白血病是一种具有挑战性的癌症,原因是血细胞的异常增殖.
来自黑色种子的thymoquinone (TQ) 具有抗癌作用,但溶解度差限制了使用.
硫乙-β-环氧 (SBE-β-CD) 是一种有前途的药物输送辅助剂.

研究的目的:

为了提高Thymoquinone (TQ) 溶解性和生物可用性,用于使用Sulfobutylether-β-cyclodextrin (SBE-β-CD) 治疗白血病.
评估TQ/SBE-β-CD复合体对K-562细胞的抗白血病作用.
调查该复合物的对端粒酶活性和亡诱导的影响.

主要方法:

提摩 (TQ) 纳入复合物的形成和特征与硫丁乙-β-环极素 (SBE-β-CD).
在K-562白血病细胞中的细胞毒性,亡 (Annexin V-FITC测定) 和端粒酶活性 (qPCR) 的体外评估.
分子对接分析以评估TQ与端粒酶的结合亲和力.

主要成果:

与单独使用TQ相比,TQ/SBE-β-CD复合体显著改善了溶解性和增强了对K-562白血病细胞的细胞毒性作用.
用TQ/SBE-β-CD治疗显著增加了白血病细胞的亡和减少了白血病细胞中的端粒酶活性.
分子对接证实了TQ和端粒酶之间强烈的结合,支持其抑制机制.

结论:

TQ/SBE-β-CD复合体代表了一种可行的策略,以克服Thymoquinone在白血病治疗中的可溶性和生物利用性差.
这种配方通过诱导亡和抑制端粒酶,表现出强烈的抗白血病活性.
进一步的研究是有必要的,以优化治疗结果,并最大限度地减少潜在的副作用,如亡.

关键词:

在 SBE-β-CD 中.灭症 (apoptosis) 是一种死亡的过程.药物输送系统是药物输送系统.这种白血病是白血病.泰罗马酶抑制的抑制作用这种药物是thymoquinone.

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