新研发的自组装抗氧化剂作为癌症的潜在治疗方法。

Shashni Babita, Nagasaki Yukio

Department of Materials Science, Graduate School of Pure and Applied Sciences, University of Tsukuba, Tennoudai 1-1-1, Tsukuba, Ibaraki 305-8573, Japan.

Master's School of Medical Sciences, Graduate School of Comprehensive Human Sciences, University of Tsukuba, Tennoudai 1-1-1, Tsukuba, Ibaraki 305-8573, Japan.

J Pers Med. 2021 Feb 2;11(2):92. doi: 10.3390/jpm11020092.

Elevated reactive oxygen species (ROS) have been implicated as significant for cancer survival by functioning as oncogene activators and secondary messengers. Hence, the attenuation of ROS-signaling pathways in cancer by antioxidants seems a suitable therapeutic regime for targeting cancers. Low molecular weight (LMW) antioxidants such as 2,2,6,6-tetramethylpyperidine-1-oxyl (TEMPO), although they are catalytically effective in vitro, exerts off-target effects in vivo due to their size, thus, limiting their clinical use. Here, we discuss the superior impacts of our TEMPO radical-conjugated self-assembling antioxidant nanoparticle (RNP) compared to the LMW counterpart in terms of pharmacokinetics, therapeutic effect, and adverse effects in various cancer models.

活性氧（ROS）水平升高已被认为通过作为癌基因激活剂和第二信使对癌症存活具有重要意义。因此，通过抗氧化剂减弱癌症中的ROS信号通路似乎是一种合适的癌症靶向治疗方案。低分子量（LMW）抗氧化剂，如2,2,6,6-四甲基哌啶-1-氧基（TEMPO），尽管它们在体外具有催化活性，但由于其尺寸在体内会产生脱靶效应，因此限制了它们的临床应用。在这里，我们讨论了我们的TEMPO自由基共轭自组装抗氧化纳米颗粒（RNP）与低分子量对应物相比，在各种癌症模型中的药代动力学、治疗效果和不良反应方面的优越影响。