碳化聚合物点来源于甲胺和L-氨酸,用于瘤细胞膜和线粒体双重向治疗

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Manling Chen¹, Yang Li², Yangcheng Liu³

¹Institute of Clean Energy Chemistry, Key Laboratory for Green Synthesis and Preparative Chemistry of Advanced Materials, College of Chemistry, Liaoning University, Shenyang 110036, Liaoning, P. R. China. liuxue@lnu.edu.cn.

Nanoscale

|October 30, 2023

概括

研究人员使用甲胺开发了新的聚合物点 (MA-dots),以显著增强抗瘤活性. 这些MA点向瘤细胞和线粒体,显示出更高的疗效和减少癌症治疗剂量需求.

科学领域:

纳米技术纳米技术
在瘤学瘤学.
药物运输药物运输药物运输

背景情况:

甲胺显示出抗瘤潜力,但需要高剂量才能有效.
开发更安全,更有效的癌症疗法至关重要.

研究的目的:

通过将甲福胺与L-阿尔金因结合,创建新的聚合物点 (MA-点),以增强抗瘤功效并降低剂量.
研究MA点的向能力和抗瘤机制.

主要方法:

通过微波辅助方法使用甲胺和L-氨酸合成了5纳米的MA点.
评估了MA-dots的抗瘤活性,并将其与甲胺进行了比较.
在A549肺癌模型中评估*in vivo*瘤生长抑制.
研究了MA点的细胞吸收,线粒体积累和分子通路调节 (LAT1,ROS,AMPK/mTOR).

主要成果:

与甲福明相比,MA点的抗瘤活性增加了12倍以上 (IC50: 93.60 μg mL-1 vs 1159.00 μg mL-1).
与大多数甲胺衍生的纳米药物相比,MA-dots显示出更高的抗瘤疗效.
*体内*研究表明,MA点抑制了A549瘤的生长.
MA点通过LAT1准瘤细胞膜,并在线粒体中积累,通过AMPK/mTOR途径调节诱导ROS产生,线粒体损伤和亡.

结论:

这项研究介绍了MA点的快速制造方法,MA点是一种具有双重瘤向和增强瘤抑制作用的新型纳米衍生物.
通过提高疗效和减少所需剂量,MA-dots代表了改善基于甲胺的癌症治疗的有希望的策略.

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